Top 100 Drugs Flashcards
What are the indications of Acetylcysteine (N-acetylcysteine)? (3)
Antidote for paracetamol poisoning
Help prevent renal injury due to radiographic contrast material (contrast nephropathy)
To reduce viscosity of respiratory secretions.
How does Acetylcysteine (N-acetylcysteine) prevent liver damage in paracetamol overdose?
Replenishing the body’s supply of glutathione
What are important adverse effects of Acetylcysteine (N-acetylcysteine)?
Can cause an anaphylactoid reaction (histamine release independent of IgE antibosies).
Can cause bronchospasm.
What should be given with Acetylcysteine (N-acetylcysteine) to lower the risk of bronchospasm?
A bronchodilator e.g. Salbutamol beforehand.
What dose of Acetylcysteine (N-acetylcysteine) is given in paracetamol poisoning?
Weight-adjusted dose, IV infusion over 21 hours (see BNF)
(Follow BNF/local protocols for dosing for each indication)
What information regarding Acetylcysteine (N-acetylcysteine) should you communicate to the patient? (3)
Effective at preventing liver damage if given w/i 8 hours of overdose.
Will take 21 hours to administer
May cause an anaphylactoid reaction.
How should treatment with Acetylcysteine (N-acetylcysteine) be monitored?
For signs of anaphylactoid reaction
INR, ALT (alanine aminotransferase) and creatinine concerntration to assess liver function (INF most sensitive)
What are the indications for activated charcoal? (2)
Reduce absorption of certain poisons (including some drug overdoses)
Increase elimintaion of certain poisons.
What is the mechanism of activated charcoal?
Molecules are adsorbed onto the surface of the charcoal, reducing their absorption into the circulation.
Can increase elimination in multiple doses.
What poisons does Activated Charcoal adsorb effectively and which are not adsorbed effectively?
Effective: Weaky ionic hydrophobic: benzodiazepines, methotrexate.
Ineffective: Alcohols, litium, iron
What are the adverse effects of activated charcoal?
Most common: black stools, vomitting
Serious: pneumonitis, bronchospasm and airway obstruction if aspirated. Can cause intestinal obstruction.
How can the common adverse effects of activated charcoal be managed?
Co-prescribing of a laxative and antiemetic (for vomiting and potential obstruction).
If they have vomited prior to presentation an antiemetic can also help it remain in the gastric tract though it should be avoided if they are actively vomitting.
In what patients in activated charcoal contraindicated?
Warning: Reduced consciousness (increased risk aspiration)
Warning: Presistent vomiting (increased risk aspiration)
Warning: Reduced GI motility, increased risk of obstruction.
What are the important interactions of activated charcoal?
Prevents absorrption of drugs taken theraputically as well as in overdose.
What is the dose of activated charcoal?
Single dose for patients presenting within 1 hours of ingestion of substance absorbed by charcoal or 2 hours with drugs that delay gastric emptying (e.g. aspirin, opioids, tricyclic antidepressants).
Once only prescription of 50g orally
Or 50g 4- hourly for multiple doses.
What are the indications for Adenosine?
First-line diagnostic and theraputic agent in supraventricular tachycardia (SVT)
What is the mechanism of Adenosine?
Agonist of adenosine receptors on cell surfaces, in the heart reduces the frequency of spontaneous depolarisations and increases resistance to depolarisation.
Slows the sinus rate, conduction velocity and increases AV node refractoriness.
This breaks re-entry circuits and allows normal depolarissations from the SA node to resume control of heat rate (cardioversion).
Note: where the circuit does not involve the AV node, e.g. in atrial flutter, adenosine will not induce cardioversion but may assit in diagnosis.
What are the potential adverse effects of adenosine?
Can induce bradycardia and/or asystole
Feels unpleasant for the patient: sinking feeling in the chest, breathlessness and sense of impending doom.
What are the contraindications and warnings of adenosine?
Contraindicated: (In patients who will not tolerate transient bradycardic effects): Hypotension, Coronary ischeamia, Decompensated heart failure.
Contrainidcated: (May cause bronchospasm); Asthma, COPD
Warning: Heart transplant
What are the interactions of adenosine?
Dipyridamole
Theophylline, aminophylline, caffeine
What is the dose and prescription of adenosine?
IV, once-only section
6mg IV (range 3-12mg on circumstances)
Adminstered by senior with resuscitation facilities, proximal large-bore cannula with flush.
What should be communicated to the patient with Adenosine?
‘Reset’ heart to normal rhythm.
Will briefly feel terrible for about 30 seconds.
How is adenosine monitored?
Close monitoring with continuous cardiac rhythm strip.
What are the indications for Adrenaline (epinephrine)? (3)
Cardiac arrest as part of ALS treatment algorithm
Anaphylaxis
(Into tissue to induce local vasoconstriction and reduce bleeding)
(Sometimes mixed with local anaesthetic drugs e.g. lidocaine to prolong local anaesthesia)
What is the mechanism of action of Adrenaline (epinephrine)?
Potent agonist of the a1, a2, b1 and b2 adrenoceptors and has a multitude of sympathetic fight of flight affects.
a1 - vasoconstriction of vessles subblying skin, mucosa and abdominal viscera
b1 - increases heart rate, force of contration and myocardial excitability
b2 - vasodilatation of vessels supplying the heart and muscles
Allows redistribution of blood flow in favour of the heat.
Bronchodilatation and suppressin of inflammatory mediator release from mast cells - b2 for anaphylaxis.
What are the key adverse effects of Adrenaline (epinephrine)?
Adrenaline-induced hypertenson
Anxiety, tremor, headache, palpitations
Angina, myocardial infarction and arrhythmias (esp. with existing heart disease)
What are the contraindications and warning of Adrenaline (epinephrine)?
None in Cardiac arrest and anaphylaxis
Should be used in caution in heart disease
As a combination with local anaesthetic should not be used in areas supplied by an end-artery
What are the important interactions of Adrenaline (epinephrine)?
Beta-blocker, may induce widespread vasoconstriction because a1 mediated vasoconstricting effect is not oppsoed by b2-mediated vasodilatation.
What are the dose and prescription instructions for Adrenaline (epinephrine)?
Shockable rhythm: 1mg IV given after 3rd shock, repeated 3-5 minutes thereafter.
None shockable (asystole or PEA): 1mg IV as soon as access attained, repeated 3-5 minutes thereafter.
Anaphylaxis: 500 micrograms IM, repeated after 5 minutes.
What is the monitoring of Adrenaline (epinephrine)?
Intensive clinical and haemodynamic monitoring
What drugs are in the aldosterone antagonists category?
(One)
Spironolactone
Epleronone
What are the indications for Aldosterone Antagonists? (3)
(Spironolactone, Epleronone)
- Ascites and oedema due to liver cirrhosis: spironolactone
- Chronic heart failure: (with a b-blocker and ace-i/arb)
- Primary hyperaldosteronism, Conn’s syndrome: for patients awaiting surgery or not an option.
What is the mechanism of Aldosterone Antagonists?
(Spironolactone, Epleronone)
Aldosterone is a mineralocorticoid produced in the adrenal cortex, acts on receptors in the distal tubules of the kidney to increase the activity of luminal epithelia sodium channels (ENaC). This increases the reabsorption of sodium and water (which elevates blood pressure) with the by-product of increased potassium excretion.
Aldosterone antagonists inhibit the effect of aldosteone by competitively binding to the aldosterone receptor. This increases sodium and water excretion and potassium retention.
What are the adverse effects of aldosterone antagonists?
Hyperkalemia (increased potassium absorption): Can cause muscle weakness, arrhythmias and cardiac arrest.
Gynaecomastia (impact on adherence)
Liver impairment, jauncide and a cause of Stevens-Johnson syndrome
What are the warning and contraindications of aldosterone antagonists?
Severe renal impairment
Hyperkalaemia
Addison’s disease (who are aldosterone deficient)
Warning: pregnant and lactating women
What are important interactions of aldosterone antagonists?
(Spironolactone, Epleronone)
Can interact with other potassium-elevating drugs, including ACE inhibitors and ARBs, increasing the risk of hyperkalemia.
Should not be combined with potassium supplements.
What is the dose and prescription guidance of aldosterone antagonists?
Spironolactone - all indications
Oral, OD
(25mg (HF) -100mg (Ascites) depending on indication)
What should be communicated to the patient in regards to Aldosterone Antagonists?
Men: gynaecomastia and impotence.
Regular blood tests to check for hyperkalaemia.
How should aldosterone antagonists be monitored?
Monitoring of symptoms and clinical findings: Reduction in ascites, oedema and or blood pressure.
Monitoring of renal function and serum potassium due to risk of renal impairment and hyperkalaemia.
What drugs are aldosterone antagonists typically combined with?
Week diuretic so usually combined with a loop or thiazide diuretic where it counteracts the potassium wasting and potentiates with diuretic effect.
E.g. in ascites, Spironolactone and Furosemide are typically used together.
What drugs are in the Alginates and Antacids class?
Gaviscon and Peptac
What are the indications of Alginates and Antacids?
Gastro-oesophageal reflux disease: for symptomatic relief of heartburn
Dyspepsia: short-term relief of indigestion
What is the mechanism of Alginates and Antacids?
(Gaviscon and Peptac)
Combination of alginate and antacid.
Work by buffering stomach acids and increasing the viscosity of the stomach contents reducing the reflux of stomach acid into the oesophagus.
What are the potential adverse effects of Alginates and Antacids?
Sometimes GI side effects, constipation or diarrhoea.
What are the warnings and contraindications for Alginates and Antacids?
In infants not with thickened milk
Sodium and potassium containing preparations should be used with caution in patients with renal failure.
What are drug interactions with Alginates and Antacids?
Can intefere with several other drugs so should be taken at different times where possible.
What is the dose and prescription advice for Alginates and Antacids?
Instructions on bottle, only proprietary formulas available.
Taken following meals, before bedtime and/or when symptoms occur.
What should be communicated to patients about taking Alginates and Antacids?
Advice that symptomatic relief and only temporary measure.
Discuss lifestyle measures: smaller meals, avoiding trigger food and drink, stop smoking, raise head of bed.
Leave a gap of at least 2 hours between these and other medicines.
Red flags: bleeding, vomiting, dysphagia, weight loss.
What are the indications for Allopurinol? (3)
To prevent acute attacks of gout (not given during attack)
To prevent uric acid and calcium oxylate renal stones
To prevent hyperuricaemia and tumour lysis syndrome associated with chemotherapy
What is the mechanism of Allopurinol?
Xanthine oxidase inhibitor
Lowers plasma uric acid concentration and reduces precipitation of uric acid in the joints or kidneys.
What are the potential adverse effects of allopurinol?
Skin rash - may be milf or sign of SJ syndrome or toxic epidermal necrolysis.
Drug hypersensitivity syndrome
Starting allopurinol can trigger or worsen an acute gout attack.
What are the contraindications and warnings of Allopurinol?
Sould not be started during an acute attack (can be continued if on already)
Recurrent skin rash or severe hyposensitivity
Warnings: severe renal and hepatic impairment.
What are important drug interactions for allopurinol?
Mercaptopurine and Azathioprine (increased risk of toxicity)
Others increase the risk of rash.
What is the dose and prescription advice of allopurinol?
PO, 100-600 mg daily in 1-2 divided doses.
Titrate to serum uric acid concentration.
For gout: co-prescribe with NSAID or colchicine.
Take with meals and good fluid intake.
What should be communicated to the patient in regards to allopurinol?
Purpose is to reduce attacks of gout or formation of kidney stones
Seek medical advice if there is the formation of a rash.
Do not stop if they get an acute attack.
What is the monitoring for Allopurinol treatment?
Serum uric acid concentrations should be checked 4 weeks after starting or after a change in dose, aim to achieve levels of <300 micromol/L.
Stop-and-restart if there is the formation of a mild rash.
What drugs can cause attacks of gout?
Thiazide or loop diuretics
Aspirin
What drugs are in the alpha-blockers class?
(Sin)
Doxazosin
Tamsulosin
Alfuzosin
What are the indications for the use of alpha-blockers? (2)
First-line medical symptomatic improvement in Benign Prostatic Hyperplasia. (After lifestyle changes)
(+ 5a-reductase inhibitors in some cases)
Add on in resistent hypertension
(After CCB, ACE-i/ARB, thiazide diuretics)
What is the mechanism of action of alpha-blockers?
Highly selective for a1-adrenoceptor
Found mainly in smooth muscle, including blood vessels and urinary tract (bladder neck and prostate)
Blockade induced relaxation of this smooth muscle
Cause vasodilatation and reduce resistance to bladder outflow.
What are the potential adverse effects of alpha-blockers?
Postural hypotension
Dizziness
Syncope
What are the warnings and contraindications for Alpha-blockers?
Should not be used in patients with pre-existing postural hypotension.
What are the interactions of alpha blockers?
May combine to cause intense postural hypotension when first started, it may be wise to miss dose of beta-blocker on day of starting.
What is the dose and prescription advice of alpha-blockers?
PO, Doxazosin (both) Tamsulosin (BPH only)
Doxazosin: 1mg daily, increased at 1-2 weeks intervals according to response.
Tamsulosin: 400 micrograms PO, daily.
Take at bedtime to reduce effect of postural hypotension.
What should be communicated to patients regarding Alpha-blockers?
Postural hypotension, take at bedtime
How are alpha-blockers monitored?
Symptom control or blood pressure
Adverse effect of PH can be measured in lying and standing blood pressure
What drugs are in the Aminoglycosides class?
Gentamycin, amikacin.
What type of bacteria are Aminoglycosides effective in treating?
Severe, gram-negative aerobe infections (including pseudomonas aeruginosa)
Not effective against anaerobes.
What are the indications for Aminoglycosides? (4)
(Gentamycin, Amikacin)
Severe infections, caused by gram-negative aerobes:
Severe sepsis (inc. unidentified source)
Pyelonephritis and complicated UTIs
Biliary and intra-abdominal Sepsis
Endocarditis
What should be prescribed with Aminoglycosides in instances where the organism is unknown?
(Gentamycin, amikacin)
Lack activity against streptococci and anaerobes, so should be combined with penecillin and/or metronidazole when the organism is unknown.
What is the mechanism of Aminoglycosides?
Bind irreversibly to bacterial ribosomes and inhibit protein synthesis.
Efffect gram-negative aerobic bacteria, staphylococci and mycobacteria (TB).
Enter cells via oxygen-dependent transport systems so only aerobes.
What are the potential adverse effects of Aminoglycosides?
(Gentamycin, amikacin)
Nephrotoxicity and Ototoxicty
Present as reduced urine output and rising serum creatinine and urea. Or, hearing loss, tinnitus and/or vertigo.
What are the warnings and contraindications of Aminoglycosides?
(Gentamycin, amikacin)
Renally excreted and can cause nephrotixicity
More likely in neonates, the elderly and those with renal impairment.
Avoid in myasthenia gravis.
What are important interactions of Aminoglycosides?
(Gentamycin, Amikacin)
Adverse effects more likely with: loop-diuretics, vancomycin, ciclospirin, cephaosporins.
What is the dose and prescription advice for Aminoglycosides?
No oral form, OD IV infusion.
Calculated on weight (or ideal weight for height if obese) and renal function.
Somewhere between 3-5 mg/kg typically.
Time between doses is determined with drug level monitoring, usually 24hr but may be more with renal impairment.
Usually 7 days or less to reduce risk of toxicity.
Diluted and infused slowly to redue ototoxicity.
What should be communicated to patients with Aminoglycosides?
(Gentamycin, Amikacin)
To treat infection
Report any change in hearing or dizziness.
Blood tests required as dosing depends on plasma concentrations.
IV so requires inpatient stay.
What is the monitoring of Aminoglycosides?
(Gentamycin, Amikacin)
For efficacy - symptoms and signs e.g. pyrexia and blood inflammatory markers e.g. c-reactive protein
Renal function before and during
Plasma drug concentration to assess when next dose is required (<1 mg/mL) if too high withold for longer.
What drugs are in the Aminosalicylates class?
(Salazine)
Mesalazine
Sulfasalazine
What are the indications of Aminosalicylates?
(Mesalazine, Sulfasalazine)
Mesalazine: 1st line in mild-to-moderate Ulcerative Colitis
Sulfasalazine: Rheumatoid arthritis as a DMARD combination therapy.
What is the mechanism of aminosalicylates?
(Mesalazine, Sulfasalazine)
Release 5-aminosalicyclic acid which is thought to have anti-inflammatory and immunosuppresive effects.
What are some of the potential adverse effects of Aminosalicylates?
(Mesalazine, Sulfasalazine)
GI side effects, headache
Rare: Leucopenia, thrombocytopenia
Renal impairment
Oligospermia
Hypersensitivity reaction
What are the warnings and contraindications of aminosalicylates?
(Mesalazine, Sulfasalazine)
Salicylates like aspirin
Should be avoided in aspirin hypersensivity
What are interactions of aminosalicylates?
PPIs and Lactulose
What is the dose and prescription guidance of aminosalicylates?
(Mesalazine, Sulfasalazine)
Mesalasine: Enema. suppository or oral. Taken for 4-6 weeks to induce remission.
Sulfasalazine: Specialist
What should be communicated to patients regarding aminosalicylates?
(Mesalazine, Sulfasalazine)
Make sure understand and happy with rectal administration if this route.
Report any bleeding, bruising of infective symptoms as could be a sign of leucopena or throbocytopenia.
What is the monitoring of aminosalicylates?
Symptoms in UC
RA symptoms plus the c-reactive protein concentraton
Real function should be checked and FBC + liver function tests.
What are the indications for Amiodarone?
Management for a wide range of tachycardias including AF, atrial flutter, SVT, VT and refractory ventricular fibrilation (VF).
Used only when other theraputic options (drugs or electrical cardioversion) are ineffective or inappropriate.
In cardiac arrest after 3rd shock in VF or pulseless VT.
What is the mechanism of Amiodarone?
Myocardial cells: blockade of sodium, calcium and potassium channels, and antagonism of a and b adrenergic receptors.
Reduce spontaneous depolarisation, slow conduction velocity, increase resistance to depolarisation.
Reduced the ventricular rate in AF and atrial flutter.
Increases chance of conversion to sinus rhythm in SVT.
What are the adverse effects of amiodarone?
Hypotension during IV infusion (less than Adenosine)
Chronic use: pneumonitis, bradycardia, AV block, hepatitis, skin photosensitivity and grey discolouration, thyroid abnormalities.
May take months to completely eliminate.
What are the warnings and contraindications to amiodarone?
Avoided in patients with severe hypotension, heart block and active thyroid disease.
(High risk drug)
What are some key interactions of Amiodarone?
Many drugs, very interactive.
Increases plasma concentrations of digoxin, diltiazem and verapamil. May increase the risk of bradycardia, AV block and heart failure.
What is the dose and prescription advice of amiodarone?
Requires senior involvement.
Unless: Cardiac arrest when given for VF or pulseless VT immediately after 3rd shock in ALS algorhythm. 300mg IV with flush, peripheral line.
For repeated or continuous infusion should be given via central line.
What information should be communicated to the patient with the use of Amiodarone?
Treatment to correct their fast or irregular heart rhythm.
Number of important and potentially serious side effects and being used as condition is serious and no other treatments are suitable.
Report signs of breathlessness, cough, jaundice, restlessness, weight loss, tiredness or weight gain.
Don’t drink grapefruit juice and be careful with sun exposure
How is Amiodarone monitored?
Efficacy: Heart rate and rhythm
Safety: IV infusion accompanied by continious cardiac monitoring
Long-term: Renal, liver and thyroid profiles and chest-x ray
Liver and thyroid profiles repeated 6 monthly.
What drugs are in the Angiotensin-converting enzyme (ACE) inhibitors class?
(Pril)
Ramipril
Lisinopril
Perindopril
What are the indications for Angiotensin-converting enzyme (ACE) inhibitors? (4)
- Hypertension - 1st or 2nd line treatment to reduce the risk of stroke, MI and death from CVD
- Chronic heart failure - 1st line treatment of all grades of heart failure
- Ischaemic heart disease - to reduce the risk of subsequent cardiovascular events such as MI and stroke
- Diabetic nephropathy and CKD with proteinuria: to reduce proteinuria and progression of nephropathy.
What is the mechanism of action of Angiotensin-converting enzyme (ACE) inhibitors?
ACE inhibitors block the action of ACE, to prevent the coversion of angiotensin I to angiotensin II.
Aniotensin II is a vasoconstrictor and stimulates aldosterone secretion. Blocking its action preduced peripheral vascular resistance (afterload), which lowers blood pressure.
Also dilates the efferent glomerular arteriole which reduces intraglomerular pressure and slows progression of CKD.
Reducing aldosterone level promotes sodium and water excretion (and causes K+ retention) which can help reduce venous return (preload), having a beneficial affect in heart failure.
What are the reverse effects of Angiotensin-converting enzyme (ACE) inhibitors?
Hypotension (esp. after 1st dose)
Persistent dry cough
Hyperkalaemia (lowered aldosterone)
Can cause or worsen renal failure and CI in renal artery stenosis.
Rare: angioedema and anaphylactoid reactions
What are the warnings and contraindications of Angiotensin-converting enzyme (ACE) inhibitors?
Should be avoided in patients with renal artery stenosis or acute kidney indury (can be used in chronic)
Avoid in pregnancy and breastfeeding
Lower doses in chronic kidney disease
Avoid with potassium elevated drugs and potassium sparing diurets.
What are important drug interactions for Angiotensin-converting enzyme (ACE) inhibitors?
Avoid with potassiuum elevating drugs and potassium-sparing diuretics due to the risk of hyperkalarmia.
Avoid with NSAIDs as increases the risk of renal failure.
What is the dose and prescribing information for Angiotensin-converting enzyme (ACE) inhibitors?
PO
1.25-2.5mg depending on indication
Titrated up to 10mg daily over a period of weeks based on response, side-effects and renal function
Take before bed, PO, OD to reduce symptomatic hypotension.
What should be communicated to patients in the use of Angiotensin-converting enzyme (ACE) inhibitors?
Efficacy: breathlessness, blood pressure
Safety: electrolytes and renal function, repeat 1-2 weeks into treatment and after increasing the dose. (creatine concentration and eGFR).
What can increase the risk of profound hypotension in patients taking Angiotensin-converting enzyme (ACE) inhibitors?
Taking diuretics such as look diuretics and those with limited salt and water intake.
Start at low dose, at bedtime and increase gradually.
What drugs are in the Angiotensin Receptor Blockers (ARBs) class?
(Sartan)
Losartan
Candesartan
Irbesartan
What are the indications for Angiotensin Receptor Blockers (ARBs)? (4)
Used when ACE inhibitors are not tolerated due to cough, the indications are the same.
- Hypertension - 1st or 2nd line treatment to reduce the risk of stroke, MI and death from CVD
- Chronic heart failure - 1st line treatment of all grades of heart failure
- Ischaemic heart disease - to reduce the risk of subsequent cardiovascular events such as MI and stroke
- Diabetic nephropathy and CKD with proteinuria: to reduce proteinuria and progression of nephropathy.
What is the mechanism of Angiotensin Receptor Blockers (ARBs)?
ARBs block the action of angiotensin II on the AT1 receptor.
Aniotensin II is a vasoconstrictor and stimulates aldosterone secretion. Blocking its action preduced peripheral vascular resistance (afterload), which lowers blood pressure.
Also dilates the efferent glomerular arteriole which reduces intraglomerular pressure and slows progression of CKD.
Reducing aldosterone level promotes sodium and water excretion (and causes K+ retention) which can help reduce venous return (preload), having a beneficial affect in heart failure.
What are the potential adverse effects of Angiotensin Receptor Blockers (ARBs)?
Can cause hypotension (esp. 1st dose)
Hyperkalaemia (due to less aldosterone)
Renal failure
(No dry cough or angioedema like ACEi s)
What are the warnings and contraindications of Angiotensin Receptor Blockers (ARBs)?
Avoided in patients with renal artery stenosis and AKI (can cause or make worse)
Unsuitable in pregnancy and breasfeeding
May be used as part of treatment of CKD but in reduced doses with careful monitoring.
What are the important interactions of Angiotensin Receptor Blockers (ARBs)?
Avoid with potassium-elevating drugs, including potassium supplements and potassium sparing diuretics. (Hyperkalaemia)
Avoid with NSAIDs as increases risk of AKI.
What is the dose and precription advice for ARBs?
PO
12.5 - 50 mg depending on indcation Titrated up to the maxiumum dose over a number of weeks accordings to response, side effects and renal function.
Take before bed to help avoid hypotension.
What communication should be given regarding Angiotensin Receptor Blockers (ARBs)?
Improve BP and reduce strain on heart
Risk of dizziness/hypotension - take at night
Need for blood test monitoring as can affect kidneys
Don’t take OTC NSAIDs to reduce the risk of kidney damage
What is the monitoring of Angiotensin Receptor Blockers (ARBs)?
Effiicacy: reduction of breathlessness in HF and improved BP in HTN.
Safely: Electrolytes and renal fucntion before starting treatment, check 1-2 weeks into treatment and after increasing the dose. (eGFR and creatinine concetration)
What population are Angiotensin Receptor Blockers (ARBs) sometimes prefered in?
In black people of African or Caribbean origin there is a reduced risk of angioedema as compared to ACEi (though CCB is still 1st line).
What drugs are in the Antidepressants, SSRIs class?
(Pram, Ine)
Citalopram, Fluoxetine, Sertraline, Escitalopram
What are the indications for Antidepressants, SSRIs? (3)
1st line treatment for moderate-to-severe depression, mild if psychological treatment fails
Panic disorder
Obsessive Compulsive Disorder
What is the mechanism of action of Antidepressants, SSRIs?
SSRIs preferentially inhibit neuronal reuptake of serotonin (5-HT) from the synaptic claft, increasing its availability for neurostransmission.
Why might SSRIs be prefered over tricyclic antidepressants?
Fewer adverse effects and less dangerous in overdose
What are the potential adverse effects of Antidepressants, SSRIs?
GI upset
Appetite and weight disturbance (loss or gain)
Hypersensitivity reactions
Hyponatremia (elderly, confusion and reduced consiousness)
Suicidal thoughts/behaviours (particularly young and on starting)
Lowering of seizure threshold
Prolonging of QT interval can cause arrhythmias
Increase risk of bleeding
Serotinin syndrome in high doses or overdose (or combined)
How does serotonin syndrome present?
Autonomic hyperactivity
Altered mental state
Neuromuscular excitation
What can happen in sudden withdrawal of Antidepressants, SSRIs?
GI Upset
Neurological and Influenza-like symptoms
Sleep disturbance
What are the warnings and contraindications to Antidepressants, SSRIs?
Epilepsy (lowers seizure threshold)
Peptic ulcer disease
Young people - suicidal ideation
Hepatic impairment
(All cautions)
What are important interactions of Antidepressants, SSRIs? (4)
Monoamine oxidase inhibitors - increase risk of serotonin syndrome
Gastroprotection when given with aspirin or NSAIDs
Bleeding risk with anticoagulants
Should not be given with other drugs prolonguing the QT interval, such as antipsychotics.
What is the dose and prescription advice for Antidepressants, SSRIs?
PO, OD
Started small dose and increased approx. 20-100 mg.
What information should be communicated to the patient regarding Antidepressants, SSRIs?
Should improve symptoms over a few weeks, particularly sleep and appetite.
Offer psychologicaal therapy in conjunction.
Must take for 6 months after depression is gone, then stopped gradually over 4 weeks.
Side effects may be unpleasant but it is wide to persist with treatment.
How are Antidepressants, SSRIs monitored?
Symptoms should be reviewed 1-2 weeks after starting.
If no effect seen by 4 weeks the drug or dose should be changed, otherwise the dose should not be adjusted till 6-8 weeks of therapy.
What drugs are in the classs Antidepressants, tricyclics and related drugs?
Amitriptyline
Lofepramine
What are the indications for Antidepressants, Tricyclics and related drugs?
(Amitriptyline, Lofepramine)
2nd line treatment for moderate-to-severe depression where 1st line SSRIs are ineffective
Treatment option for neuropathic pain though unlicenced
What is the mechanism of action for Antidepressants, Tricyclics and related drugs?
Inhibit neuronal reuptake of serotonin (5-HT) and noradrenaline from the synaptic cleft, thereby increasing availability for neurotransmission.
Also block other receptors causing extensive adverse effect profile (see adverse effects)
What are the adverse effects of Antidepressants, Tricyclics and related drugs?
Blockade of antimuscarinic receptors: Dry mouth, constipation, urinary retention, blurred vision.
Sedation, hypotensin, arrythmias, ECG changes
Convulsions, hallucinations, mania
Breast changes, sexual dysfunction, extrapyramidal side effects
VERY DANGEROUS IN OVERDOSE: Severe hypotension, arrhythmias, convulsions, coma, respiratory failure.
Sudden withdrawal can cause GI upset, neurological and influeza-like symptoms and sleep disturbance
What are the warnings and contraindications for Antidepressants, Tricyclics and related drugs?
Elderly
Cardiovascular disease
Epilepsy
Constipation
Prostatic hypertrophy
Raised intraocular pressure
What are important interactions for Antidepressants, Tricyclics and related drugs?
Should not be gieevn with Monoamine oxidase inhibitors - hypertension, hyperthermia, serotonin syndrome.
Also interact with more other drugs.
What is the dose and prescription adbie for Antidepressants, Tricyclics and related drugs?
Only when SSRIs are ineffective, more dangerous in overdose.
Loferamine preferred for depression.
Neuropathic pain: Amitriptyline at low dose e.g. 10mg at night instead of around 75 mg for depression.
Prescribe in small quantities to reduce the risk of overdose.
What is the communication advice to the patient for Antidepressants, Tricyclics and related drugs?
Will improve over a few weeks
Also offer psychological therapy
Should carry on for 6 months after they feel better.
Warn them not to stop suddenly as this may cause withdrawal symptoms - reduce slowly over 4 weeks.
Side effects may be unpleasant but should be encouraged to persist.
What is the monitoring of Antidepressants, Tricyclics and related drugs?
Should be reviewed 1-2 weeks after starting treatment, changed if no effect at 4.
What drugs are in the Antidepressants, SNRIs and Atypicals Class
Two main ones
Venlafaxine (SNRIs)
Mirtazapine (Atypical)
What are the indications for the Antidepressants, Venlafaxine and Mirtazapine?
As an option for the treatment of major depression where the 1st line SSRIs are ineffective or not tollerated
Generalised anxiety disorder (Venlafaxine)
What is the mechanism of Antidepressants, Venlafaxine and Mirtazapine?
SNRI and Atypical
Both increase the availability of monoamines for neurotransmission, improving mood and physical symptoms in moderate-to-severe depression.
What are the important adverse effects of Antidepressants, Venlafaxine and Mirtazapine?
GI Upset
Dry mouth, nausea, change in weight, diarrhoae or constipation
CNS effects
Headache, Abnormal dreams, insomnia, confusion and convulsions
Hyponatremia
Serotonin syndrome
Suicidal thoughts and behaviours may increase
Venlafaxine can increase QT interval and cause arrythmias
Sudden withdrawal can cause - GI upset, neurological and infuenza-like symptoms.
What are the warnings and contraindications for Antidepressants, Venlafaxine and Mirtazapine?
Elderly at increased risk of adverse events
Dose reduction in hepatic or renal impairment
Cardiovascular disease, increased risk of arrythmias.
What are the important interactions of Antidepressants, Venlafaxine and Mirtazapine?
With other antidepressants can increase the risk of seratonin syndrome.
What is the dose and prescription advice for Antidepressants, Venlafaxine and Mirtazapine?
PO, Not 1st line.
Started at a low dose
Venlafaxine (37.5 mg PO, BD) increased to up to 375mg daily.
Mirtazapine 15 mg PO up to 45 mg PO OD.
What should be communicated to patients on Antidepressants, Venlafaxine and Mirtazapine?
Improve over few weeks
ALso psychological therapy
Continue after 6 months of feeling better then discontinue over 4 weeks.
May have to persist through unpleasant side effects.
Seditive effect with Mirtazapine.
What drugs are in the class Antiemetics, dopamine D2-receptor antagonists?
Metoclopramide
Domperidone
What are the indications for Antiemetics, dopamine D2-receptor antagonists?
(Metoclopramide, Domperidone)
Prophylaxis and treatment of nausea and vomiting particulrly in the context of reduced gut motility and where this may be caused by dugs (opioids or diabetic gastroparesis)
(Can be used in GORD not responding to conventional treatment)
What is the mechanism of action of Antiemetics, dopamine D2-receptor antagonists?
(Metoclopramide, Domperidone)
Reduced activation of the chemoreceptor trigger zone (CTZ)
Prokinetic effect - promoting gastric emptying
Effective in nausea and vomiting due to CTZ stimulation (e.g. due to drugs) and reduced gut motility (e.g. due to opioids or diabetic gastroparesis)
What are the important adverse effects of Antiemetics, dopamine D2-receptor antagonists?
(Metoclopramide, Domperidone)
Diarrhoea - most common
Metoclopramide - extrapyramidal symtoms through the same mechaism as antipsychotics - acute dystonic reaction such as oculoyric crisis. (Domperidone less likely to cause these effects)
What are some of the warnings and contraindications for Antiemetics, dopamine D2-receptor antagonists?
Extrapyramideal side effects more common in children and young adults (Metoclopramide)
Due to prokinetic effect contraindicated in GI obstruction and perforation.
What are the important interactions for Antiemetics, dopamine D2-receptor antagonists?
(Metoclopramide, Domperidone)
Metoclopramide only:
Antipsychotics - increased risk of extrapyramidal side effects
CI with dopaminergic agents of Parkinson’s disease as will antagonise the effects
What is the dose and prescription advice for Antiemetics, dopamine D2-receptor antagonists?
(Metoclopramide, Domperidone)
Starting dose 10 mg up to TDS
Metoclopramide IM/IV
Domperidone PO or Rectal
(Oral route not suitable if actively vomiting)
Should be given slowly over two minutes IV.
What is the communication advice for Antiemetics, dopamine D2-receptor antagonists?
(Metoclopramide, Domperidone)
Anti-sickness medicine
Watch out for extra-pyramidal side effects with Metoclopramide
What is the monitoring for Antiemetics, dopamine D2-receptor antagonists?
Resolution of symptoms, if prolongued should monitor for extrapyramidal features.
What drugs are in the class Antiemetics, histamine H1-receptor antagonists?
(Zine - think sounds like histamine)
Cyclizine
Cinnarizine
Promethazine
What are the indications for Antiemetics, histamine H1-receptor antagonists?
(Cyclizine, Promethazine)
Prophylaxis and treatment of nausea and vomitting, particulaly in the context of motion sickness and vertigo.
What is the mechanism of action of Antiemetics, histamine H1-receptor antagonists?
(Cyclizine, Promethazine)
Histamine and acetylcholine receptors in the vomiting centre, these are blocked by these drugs reducing the communication with the vestibular centre.
Effective in range of conditions (e.g. drug-induced, post-operative, radiotherapy) but most when associated with motion or vertigo
What are the adverse effects of Antiemetics, histamine H1-receptor antagonists?
(Cyclizine, Promethazine)
Drowsiness
Dry throat and mouth
Transient tachycardia noticed as palpitations
Some excitation or depression
What are the warning and contraindications of Antiemetics, histamine H1-receptor antagonists?
Sedating effect
Avoided in hepatic encephalopathy and prostatic hypertrophy.
What are important interactions of Antiemetics, histamine H1-receptor antagonists?
(Cyclizine, Promethazine)
Sedation may be greated when combined with other sedating drugs e.g. benzodiazepines, opioids
Avoid with ‘tropiums’
What is the prescription and dose guidance for Antiemetics, histamine H1-receptor antagonists?
Cyclizine 50 mg 8 hourly as required - given PO, IV, IM.
PO inappropriate if actively vomitting
IM injections are painful and rapid IV are unpleasant so SLOW IV is okay (2 minutes).
What information should be communicated to the patient with antiemetics, histamine H1-receptor antagonists?
Anti-sickness medicine
May not work for everyone, keep check of symptoms
Advise that they can cause drowsiness and impair the ability to perform tasks such as driving which they should avoid
What over the counter drug can be offered for the treatment of motion sickness?
Hyoscine hydrobromide (an antimuscarinic drug) alternative and effective treatment for motion sickness.
What drugs are in the class Antiemetics, phenothiazines?
Prochlorperazine
Chlorpromazine
What are the indications for Antiemetics, phenothiazine?
(Prochlorperazine, Chlorpromazine)
- Prophylaxis and treatment of nausea and vomiting in a wide range of conditions, particularly due to vertigo. Due to side-effect profile others are usually used first-line.
- Psychotic disorders, such as schizophrenia, where they are used as first-generation (typical) antipsychotics
What is the mechanism of action of Antiemetics, phenothiazine?
Blockade of various receptors in the vomiting and vestibular centre.
Dopamine, Histamine, Acetylcholine
Useful in chemotherapy, radiotherapy and vertigo.
What are the potential adverse effects of Antiemetics, phenothiazine?
Drowsiness, postural hypotension
Extrapyramidal syndromes (Same mechanism as other typical antipsychotics) - acute dystonic reactions such as oculogyric crisis.
Long-term (as antipsychotic) can cause tardive dyskinesia.
QT-interval prolongation (as will all antipsychotics)
What are the warnings and contraindications of Antiemetics, phenothiazine?
Hepatotoxicity - avoid in severe liver disease
Avoin in prostatic hypertrophy
Dose reduction in the elderly
What are important drug interactions of Antiemetics, phenothiazine?
Extensive list of interactions - be wary with other drugs prolonguing the QT interval including - antipsychotics, amiodarone, ciprofloxacin, macrolides, quinine and SSRIs.
What is the dose and prescription advice for Antiemetics, phenothiazine?
Seek senior advice as other drugs can be tried first.
20 mg PO or 12.5 mg IM then further doses
IM injection into large muscle
What information should be communicated to the patient with Antiemetics, phenothiazine?
Anti-sickness medicine
Discuss drowsiness and diziness on standing
Stop taking if any extra pyramidal side effects (muscle spasms or movement abnormalities)
What is the monitoring of Antiemetics, phenothiazine?
Resolution of symptoms
Monitor for extrapyramidal side effects
What drugs are in the class Antiemetics, serotonin 5-HT3-receptor antagonists?
Ondansetron
Granisetron
What are the indications for Antiemetics, serotonin 5-HT3-receptor antagonists?
(Ondansetron, Granisetron)
Prophylaxis and treatment of nausea and vomiting, particularly in the context of general anaesthesia and chemotherapy
What is the mechanism of action of Antiemetics, serotonin 5-HT3-receptor antagonists?
(Ondansetron, Granisetron)
Serotonin receptors in the CTZ, also released in the gut to emetogenic stimuli.
Useful against nausea and vomiting due to CTX stimulation (e.g. drugs) and visceral stimuli (gut infection, radiotherapy) but not in motion sickness.
What are the adverse effects with the use of Antiemetics, serotonin 5-HT3-receptor antagonists?
(Ondansetron, Granisetron)
Constipation, diarrhoea and headaches can occur.
What are the warnings and contraindications for the use of antiemetics, serotonin 5-HT3-receptor antagonists?
(Ondansetron, Granisetron)
Small risk of prolonguing the QT interval, so should be avoided in patients with a long QT-interval.
Also avoid in patients already taking drugs that prolongue the qt interval.
What is the dose and prescription guidance for Antiemetics, serotonin 5-HT3-receptor antagonists?
Ondansetron 4-8 mg, BD, PO or IV
May be higher if chemotherapy induced
IV > IM as less painful - Oral should be given in advance of end of general anaesthesia
What antiemetic may be used in cases of severe morning sickness?
Ondansetron
What drugs are in the class Antifungal Drugs? (3)
Clotrimazole
Fluconazole
Nystatin
What are the indications for Antifungal Drugs? (2)
- Treatment of local fungal infections (e.g. thrush) of the oropharyn, vagina or ski. They may be applied topically (nystatin, clotrimazole) or taken orall (fluconazole)
- Systemic treatment of invasive or disseminated fungal infections - specialist treatment is required.
What is the mechanism of action of Antifungal Drugs?
(Clotrimazole, Fluconazole, Nystatin)
Target ergosterol on fungal cell membranes.
(Resistance to antifungals can happen in long-term treatment in immunosuppressed patients)
What are the adverse effects of antifungal drugs?
(Clotrimazole, Fluconazole, Nystatin)
Topical: local irritation
Oral (Fluconazole): GI upset, headach, hepatitis, hypersensitivity
Rarely: severe hepatic toxicity and prolonged QT interval.
What are the warnings and contraindications of antifungal drugs?
Nystatin and Clotrimazole have no major CIs
Fluconazole caution in liver disease, avoided in pregnancy.
What are the important drug interactions for antifungal drugs?
Fluconazole (Check BNF):
Inhibits cytochrome P450 enzymes - increase in concentration of drugs metabolised by these
Increased risk of arrythmias is prescribed with drugs lengthening QT interval
What is the dose and prescription information for antifungal drugs?
(Clotrimazole, Fluconazole, Nystatin)
Nystatin - Oral or topical thrush - check BNF
Clotrimazole - Oral, topical, pessary - check BNF
Fluconazole - 150mg or 50mg longer course - check BNF
(Reasonably complex and depending on indication so check BNF for these)
How should nystatin in oral suspension be administered?
After food and held in the mouth to allow good contact with lesions, dentures should be removed.
What information should be communicated to patients for antifungal medication?
(Clotrimazole, Fluconazole, Nystatin)
Treatment may take 1-2 weeks for skin infections after symptoms resolve
If prolongued course of Fluconazole look out for signs of liver poisoining inc: nausea, loss of appetitie, lethargy or dark urine.
What is the monitoring for antifungal medication?
Efficacy: clinical symptoms
Fluconazole: liver enzymes before and during prolongued courses of treatment to assess for hepatic toxicity
What drugs make people more suceptible to oral thrush in hospital and how should this initially be treated?
Elderly in hospital
Antibiotics and systemic or inhaled corticosteroids
Antimuscarinics reduce saliva
Encourage mouth care and prescribe nystatin to promote recovery
What drugs are in the Antihistamines (H1-receptor antagonists) Class?
Cetirizine
Loratadine
Fexofenadine
Chlorphenamine
What are the indications for Antihistamines (H1-receptor antagonists)? (4)
(Certirizine, Loratadine, Fexofenadine, Chlorphenamine)
- First-line treatment for allergies inc. hayfever (seasonal allergic rhinitis)
- To relieve itchiness (pruritis) and hives (urticaria) due to insect bites, infections (e.g. chicken pox) and drug allergies
- Adjunct treatment in anaphylaxis with adrenaline
- Other drugs in class may be used for nausea and vomitting (Antiemetics, histamine H1-receptor antagonisits) - Cyclizine, cinnarizine, promthazine.
What is the mechanism of action of antihistamines (H1-receptor antagnosists)?
(Certirizine, Loratadine, Fexofenadine, Chlorphenamine)
Antagonist of the H1-receptor
Histamine induces the features of immediate-type (type 1) hypersensitivity, they block these effects.
What are the adverse effects of Antihistamines (H1-receptor antagonits)?
(Certirizine, Loratadine, Fexofenadine, Chlorphenamine)
1st generation (e.g. chlorphenamine) causes sedation.
Newer ones (Loratadine, Fexofenadine, Certirizine) do not have such a sedetive effect.
What are the warnings and contraindications of antihistamines (H1-receptor antagonists)?
Safe in most patients
1st generation - Chlorphenamine
Avoid in severe liver disease (as can cause hepatic encephalopathy) and in people operating heavy machinery.
What is the dose and prescription advice of antihistamines (H1-receptor antagonists)?
(Cetirizine, Loratadine, Fexofenadine, Chlorphenamine)
Cetirizine 10 mg, Loratidine 10 mg, Chlorphenamine 4 mg tablets and 2mg/5ml solution - can be purchased OTC without prescription.
PO, OD (Chlorphenamine 4-6 hourly)
Chlorphenamine 10 mg IV or IM in anaphylaxis (with adrenaline)
What communication should be given to patients regarding antihistamines (H1-receptor antagonists)?
(Cetirizine, Loratadine, Fexofenadine, Chlorphenamine)
Treatment to relive allergic symptoms
Chlorphenamine - may become tired and lost concentration - avoid if driving or other tasts, avoid combining with alcohol
Cheaper to buy from a pharmacist over prescriptions.
What drugs are in the class Antimotility Drugs?
Loperamide, Codeine Phosphate
What are the indications for the Antimotility Drugs?
(Loperamide, Codeine Phosphate)
Symptomatic treatment for diarrhoea, in the context of IBS or viral gastroenteritis.
What is the mechanism of Antimotility Drugs?
(Loperamide, Codeine Phosphate)
Both opioids.
Loperamide doesn’t cross CNS so no analgesic effects, agonist of the opioid u-receptors in the GI tract.
Transit of bowel contents is slowed and anal sphicter tone is increased
Slower bowel transit allows more time for water absorption.
(Codeine phosphate not preferable unless analgesic effect also required)
What are the adverse effects of antimotility drugs?
(Loperamide, Codeine Phosphate)
GI effects - Constipation (mechnism), abdominal cramping, flatulence.
If codeine phosphate is used - risk of opioid toxicity and dependence.
What are the warnings and contraindications of Antimotility Drugs?
Avoid in acute unlerative colitis where inhibition of peristalsis may increase the risk of megacolon and perforation.
Avoided in C.diff (diarhoea following BS antibiotic use)
Avoid in acute bloody diarrhoea (dysentery) - likely bacterial infection.
What is the dose and prescription advice for Antimotility Drugs?
(Loperamide, Codeine Phosphate)
Loperamide may be purchased over the counter without prescription - 4 mg followed by 2 mg with each loose stool, maximum 8 mg per day.
PO
What should be communicated with patients in the use of Antimotility Drugs?
(Loperamide, Codeine Phosphate)
Will help settle diarrhoea, will not treat the underlying cause.
Stop taking if they develop consipation, abdominal pain, or if taken for >5 days.
Cheaper to buy OTC.
What are the rules regarding prescribing Antimotility Drugs for bacterial infection?
High risk to inhibit peristalsis in context of C.diff colitis.
Should not prescribe if devleoped in hospital or on antibiotics - unless positive viral PCR and/or negative C.difficile toxin test.
Explain this is why you cannot prescribe in this context even if they would usually buy OTC.
What drugs are in the class Antimuscarinics, bronchodilators?
Ipratropium, Tiotropium, Glycopyrronium
What are the indications for the use of antimuscarinics, bronchodilators (4)?
(Ipratropium, Tiotropium, Glycopyrronium)
- In COPD,
Short-acting antimuscarinics (Ipratropium) are used to relieve breathlessness e.g. brought on by exercise or during exacerbations.
Long-acting antimuscarinics (Tiotropium, Glycopyrronium) are used to prevent breathlessness and exacerbations
- In asthma
SAMAs used as an adjuvant treatment for relief of breathlessness during acute exacerbations (added to a short-acting B2-agonist e.g. Salbutamol).
LAMA are added to high-dose inhaled corticosteroids and long-acting B2-agnosits at step 4 in the treatment of chronic asthma.
What is the mechanism of action of antimuscarinics, bronchodilators?
(Ipratropium, Tiotropium, Glycopyrronium)
Antimuscarinic drugs bind to the muscarinic receptors, where they act as a competitive inhibitor of acetylcholine.
Antimuscarinics increase heart rate and conduction, reduce smooth muscle tone (in respiratory tract) and reduce secretions from glands (resp and GI tract).
(In the eye they cause relaxation of the pupillary constrictor and ciliary muscles, causing pupillary dilatation and preventing accomodation respectively)
What are the adverse effects of antimuscarinics, bronchodilators?
(Ipratropium, Tiotropium, Glycopyrronium)
Little systemic absorption when inhaled, dry mouth may occur
What are the warnings and contraindications for antimuscarinics, bronchodilators?
Used in caution in patients susceptible to angle-closure glaucome, in whom can presipitate a dangerous rise in intraocular pressure.
Mild risk in arrythmias.
What is the dose and prescription advice for antimuscarinics, bronchodilators?
Short-acting antimuscarinics - Ipratropium - QDS or as needed when feeling breathless. - 40 micrograms by inhalation for stable patients - 250-500 mcrorams 6hrly by nebulisation during acute attacks.
(Inhaler or nebulised)
Long-acting antimuscarinics - Tiotropium, Glycopyrronium are prescribed for regular administrations - OD.
What information should be communciated to patients with the use of antimuscarinics, bronchodilators?
(Ipratropium, Tiotropium, Glycopyrronium)
Offering a treatment to make airways relax, should improve breathing.
Treatment of symptoms, not the disease.
Use of inhalers and nebulisers, may cause dry mouth.
How is treatment with antimuscarinics, bronchodilators monitored?
(Ipratropium, Tiotropium, Glycopyrronium)
Check symptoms and peak flow measurements (asthma)
Check inhaler technique
What is the maximum dose of short-acting muscarinics?
40 micrograms (standard dose) QDS
(B2-agonists, salbutamol) - can be administered more frequently (e.g 2-hourly as needed)
What Drugs are in the Class Antimuscarinics, Cardiovascular and Gastrointestinal Uses?
Atropine
Hyoscine Butylbromide
Glycopyrronium
What are the indications for the drugs Antimuscarinics, Cardiovascular and Gastrointestinal Uses (3)?
(Atropine, hyoscine butylbromide, glycopyrronium)
- Atropine - used in the 1st line management of severe or symptomatic bradycardia to increase heart rate
- Hyoscine butylbromide - 1st line pharmacological treatment option for IBS where used for antispasmodic effect.
- Hyoscine butylbromide - palliative care, role in reducing copious respiratory secretions.
What is the mechanism of action of Antimuscarinics, Cardiovascular and Gastrointestinal Uses?
(Atropine, Hyoscine butylbromide, Glycopyrronium)
Antimuscarinic drugs bind to the muscarine receptor where they act as a competitive inhibitor of acetylcholine.
Increases heart rate and conduction, reduce smooth muscle tone and peristaltic contractions including the gut and urinary tract
Reduce secretions from glands in the respiratory and gut.
What are the adverse effects of Antimuscarinics, Cardiovascular and Gastrointestinal Uses?
(Atropine, Hyoscine Butylbromide, Glycopyrronium)
Tachycardia, dry mouth, constipation.
Can cause urinary retention in patients with benign prostatic hypertrophy
Can case blurred vision
Can cause drowsiness and confusion
What are the warnings and contraindications for the drugs Antimuscarinics, Cardiovascular and Gastrointestinal Uses?
(Atropine, hyoscine butylbromide, glycopyrronium)
Caution: acute-closure glaucoma
Caution: Arrythmias and significant cardiovascular disease.
What are the interactions for Antimuscarinics, Cardiovascular and Gastrointestinal Uses?
(More than for respiratory/inhaled as systemic absorption)
Adverse effects more pronounced when combined with other drugs with antimuscarinic effects, such as tricyclic antidepressants
What is the dose and prescription advice fro Antimuscarinics, Cardiovascular and Gastrointestinal Uses? (3)
Atropine - Bradycardia - IV in incremental doses - 300-600 micrograms every 1-2 minutes, until acceptable HR restored
(Atropine for IV administration in pre-filled syringes, check concentration)
(Glycopyrronium is an alternative)
Hyoscine butylbromide (Buscopan) - PO - 10 mg - 8 hourly - available without prescription
Hyoscine butylbromide - Respiratory secretions - SC
(Beware sounds similar to hyoscine hydrobromide - be careful)
What is the monitoring for Antimuscarinics, Cardiovascular and Gastrointestinal Uses?
(Atropine, Hyoscine Butylbromide (Buscopan), Glycopyrronium)
Atropine for bradycardia - administed by specialist with high-intensity monitoring - continuous cardiac rhythm monitoring
Or symptomatic for other uses
What are the drugs in the class Antimuscarinics, genitourinary uses?
Oxybutynin
Tolterodine
Solifenacine
What are the indications for Antimuscarinics, genitourinary uses?
(Oxybutynin, Tolterodine, Solifenacin)
To reduce urinary frequency, urgency and urge incontinence in overactive bladder, as a first-line pharmacological treatment if bladder training is ineffective.
What is the mechanism of action of Antimuscarinics, genitourinary uses?
(Oxybutynin, Tolterodine, Solifenacin)
Bind to antimuscarinic drugs where they are a competitive inhibitor of acetylcholine.
Contraction of the smooth muscle of the bladder is under parasympathetic control.
Blocking muscarinic receptors promotes bladder relaxation
What are the adverse effects of Antimuscarinics, genitourinary uses?
(Oxybutynin, Tolterodine, Solifenacin)
Dry mouth
Tachycardia
Constipation
Blurred Vision
What are the warnings and contraindications for the drugs Antimuscarinics, genitourinary uses?
Antimuscarinics are contraindicated in urinary tract infections (urinalysis before treatment)
CNS side effects difficult in elderly and those with dementia
Caution in angle-closure glaucoma
Caution in arrythmias or at risk of urinary retention
What drugs interact with Antimuscarinics, genitourinary uses?
Other drugs with antimuscarinic effects, such as tricyclic antidepressants
What is the dose and prescription advice for Antimuscarinics, genitourinary uses?
(Oxybutynin, Tolterodine, Solifenacin)
Prescribe antimuscarinics for urge incontinence only after adequate trial of bladder retraining
5 mg - PO. 8-13 hrly
Immediate release tried first, modified release only when not tolerated
What should be communicated to patients with the use of Antimuscarinics, genitourinary uses?
(Oxybutynin, Tolterodine, Solifenacin)
Relax the bladder, reducing the frequency and urgency with which they need to urinate
Explain that dry mouth is a common side effect
Elderly - may cause drowsiness and confusion
What can be used to combat the dry mouth caused by Antimuscarinics, genitourinary uses?
Chewing gum or sucking sweets (sugar-free)
Increased risk of dental decay due to dry mouth.
What are the names of the drug in the class Antipsychotics, first-generation (typical)?
Haloperidol
Chlorpromazine (also antiemetic - phenothiazine)
Prochlorperazine (also antiemetic - phenothiazine)
What are the indications for Antipsychotics, first-generation (typical)? (4)
(Haloperidol, Chlorpromazine, Prochlorperazine)
- Urgent treatment of severe psychomotor agitation that is causing dangerous or violent behavior, or to calm patients to permit assessment.
- Schizophrenia, particularly when the metabolic side effects of second-generation (atypical) antipsychotics are likely to be problematic.
- Bipolar disorder, particularly in acute episodes of mania or hypomania
- Nausea and vomiting, particulalry in the palliative care setting (Antiemetic - Chlorpromazine, Prochlorperazine)
What is the mechanism of action of Antipsychotics, first-generation (typical)?
(Haloperidol, Chlorpromazine, Prochlorperazine)
Antipsychotic drugs block post-synaptic dopamine D2 receptors.
All have some seditive effect.
What are the adverse effects of Antipsychotics, first-generation (typical)?
(Haloperidol, Chlorpromazine, Prochlorperazine)
Extrapyramidal effects - movement abnormalities - main drawback of 1st generation antipsychotics - oculogyric crisis
Acute dystonic reactions - involuntary parkinsonian movements or muscle spasms
Akathisia
Neuroleptic malignant syndrome - rare but life-threatening - rigidity, confusion, autonomic dysregulation and pyrexia.
Tardive dyskinesia - late effect (months - years) - movements that are pointless, involuntary and repetitive (i.e. lip smacking) - may not resolve with stopping treatment
Drowsiness, hypotension, QT-interval prolongation (arrhythmias), erectile dysfunction, hyperprolactinaemia (menstrual disturbance, galactorrhoea, breast pain)
What are the warnings and contraindications for Antipsychotics, first-generation (typical)?
(Haloperidol, Chlorpromazine, Prochorperazine)
Elderly - sensitive
Avoided in demetia
Avoid in Parkinson’s disease - due to extrapyramidal side effects
What are the interactions with Antipsychotics, first-generation (typical)?
Drugs also prolonguing the QT-interval (e.g. Amiodarone, Macrolides)
What is the dose and prescription advice for Antipsychotics, first-generation (typical)?
(Haloperidol, Chlorpromazine, Prochloreperazine)
For schizophrenia - under guidance of Psychiatrist
Single dose for acute or violent behaviour - Haloperidol - 0.5-3.0 mg IM)
Nausea - Haloperidol - Regular PO or SC doses - e.g. 1.5mg at night or continuous SC infusion
How can Antipsychotics, first-generation (typical) be taken for regular administration?
(Haloperidol, Prochlorperazine, Chorpromazine)
Regular administration - typical antipsychoics - taken orally or given by slow release IM ‘depot’ injections.
In emergencies given by rapid acting IM injection and occasionally IV for rapid control of symptoms (very rare/specialist/intense side effects)
What should be communicated to patients in regards to Antipsychotics, first-generation (typical)?
(Haloperidol, Chlorpromazine, Prochlorperazine)
Adherence is a significant issue due to underlying psychosis and side effects (multiple)
Good communication necessary
Patients should report that they are taking to other healthcare professionals due to interactions.
How are Antipsychotics, first-generation (typical) monitored?
(Haloperidol, Prochlorperazine, Chlorpromazine)
Control of antipsychotic symptoms
Antipsychotic effects may take time to be established
Montoring for neurological, respiratory and cardiovascular depression.
Dose-response relationshop is unpredictable
What drugs are in the class Antipsychotic, second-generation (atypical)?
(Pine + Risperidone)
Quetiapine
Olanzapine
Risperidone
Clozapine
What are the indications for Antipsychotic, second-generation (atypical) (3)?
(Quetiapine, Olanzapine, Risperidone, Clozapine)
- Urgent treatment of severe psychomotor agitation leading to dangerous or violent behaviour, or to calm such patients to permit assessment
- Schizophrenia, when extrapyramidal side effects have complicated the use of first-generation (typical) antipsychotics, or when negative symptoms are prominent.
- Bipolar disoder, particularly in acute episodes of mania or hypomania
What is the mechanism of Antipsychotic, second-generation (atypical)?
(Quetiapine, Olanzapine, Risperidone, Clozapine)
Antipsychotic drugs block post-synaptic dopamine D2 receptors.
Clozapine particulalrly useful in ‘treatment-resistant’ schozophrenia, against negative symptoms, and have lower risk of extrapyramidal side effects.
Higher affinity for other receptors and characteristic of looser binding to D2 receptors.
What are the adverse effects of Antipsychotic, second-generation (atypical)?
(Quetiapine, Olanzapine, Risperidone, Clozapine)
Sedation
Extrapyramidal effects - more common with 1st generation
Metabolic distrubance - weight gain, diabetes melltus, lipid changes (more common with 2nd generation)
Antipsychotics can prolongue the QT interval and cause arrythmias
Risperidone - hyperprolactineamia, breast symptoms and sexual dysfunction.
Clozapine - agranulocytosis and myocarditis (rare but dangerous)
What are the warnings and contraindications for Antipsychotic, second-generation (atypical)?
(Quetiapine, Olanzapine, Risperidone, Clozapine)
Cardiovascular disease
Clozapine (not in severe heart disease or history of neutropenia - agranulocytosis)
What are the interactions with Antipsychotic, second-generation (atypical)?
Sedation may be more pronounced when used with other sedating drugs
Not comined with dopamine-blocking antiemetics
Drugs that prolong the QT interval - amiodarone, quinine, macrolides, SSRIs
What is the dose and prescription advice for Antipsychotic, second-generation (atypical)?
(Quetiapine, Olanzapine, Risperidone, Clozapine)
Decisions should be taken by psychiatrist
Used for treatment of acute symptoms and prevention of subsequent attacks
Daily PO or depot IM injections
Clozapine when other agents ineffective or intollerable - poor side effect profile.
Best taken at bedtime
What is the communication for Antipsychotic, second-generation (atypical)?
(Quetiapine, Olanzapine, Risperidone, Clozapine)
You will only deal with patients already on, a psychiatrist will establish treatment.
Clozapine - regular blood test monitoring is required for agranulocytosis.
Know what side-effects to look out for.
What is the monitoring of Antipsychotic, second-generation (atypical)?
(Quetiapine, Olanzapine, Risperidone, Clozapine)
Signs and symptoms
For most - blood tests FBC, liver and renal at start and periodically
For clozapine - intensive monitoring due to the risk of agranulocytosis
Monitoring of metabolic and cardiovascular side efects important for second-generation ASPs - includes weight, lipid profile, fasting blood glucose (weight gain, diabetes mellitus - metabolic effects)
For 1st generation the extrapyramidal side effects more likely.
What should you always check for a patient presenting to a hosptial on antipsychotic medication?
The QT-interval on the ECG
May be lengthened and may be exacerbated into arrythmias by other drugs e.g. Amiodarone, Macrolides, SSRIs
What are the indications for treatment with Aspirin? (4)
- Acute coronary syndrome and acute ischaemic stroke, where rapid inhibition of platelet aggregation can prevent or limit arterial thrombosis and reduce mortality.
- For long-term secondary prevention of thrombotic arterial events in patients with cardiovascular, cerebrovascular and peripheral arterial disease.
- To reduce the risk of intracardiac thrombus and embolic stroke in atrial fibrilation where warfarin and NOACs are contraindicated
- To control mild-to-moderate pain and fever (NSAIDs) although other drugs usually preferable
What is the mechanism of action of Aspirin?
Aspirin irreversibly inhibits cyclooxygenase (COX) to reduce the production of the pro-aggregatory factor thromboxane, reducing platelet aggregation and the risk of arterial occluision.
The antiplatelet effect of aspirin occurs at low doses and lasts for the lifetime of the platelet - it wears off as new platelets are made.
What are the adverse effects of aspirin?
GI irritation - Aspirin is an NSAID
Can cause gastrointestinal ulceration and haemorrhage.
Hypersensitivity reactions - bronchospasm
Regular high dose can cause tinnitus
Aspirin is life-threatening in overdose - features include hyperventilation, earing changes, metabolic acidosis and confusion, followed by convulsions, cardiovascular collapse and respiratory arrest
What are the warnings and contraindications for Aspirin?
Not given to children due to the risk of Reye’s syndrome
Aspirin hypersensitivity (who have had bronchospasm or other allergic symptoms triggered by exposure to aspirin or another NSAID)
Avoided in third trimester of pregnancy
Peptic ulceration - with gastroprotection
Gout - can presipitiate an acute attack
What are the important interactions for Aspirin?
Acts synergistically with other antiplatelet agents, which although therapeutically beneficial can lead to increased risk of bleeding.
Caution when given with other antiplatelet drugs (clopidogrel, dipyridamole) and anticoagulants (hepain, warfarin) in some situations e.g. ACS.
What is the dose and prescription advice for Aspirin?
Acute coronary syndrome - initially once-only loading dose (300mg - PO or rectal) followed by regular dose of 75 mg daily.
Acute ischaemic stroke - 300 mg daily for 2 weeks, then 75 mg daily.
Long-term prevention of thrombosis after acute event or in atriial fibrilation - low dose aspirin 75 mg daily.
(Much higher dose in pain maximum 4 g daily)
Gastroprotection e.g. Omeprazole 20 mg daily may be co-prescribed
In which patients taking Aspirin should Gastroprotection be considered?
Gastroprotection e.g. Omeprazole 20 mg daily should be considered for patients taking low-dose aspirin who are at increased risk of gastric complications inc: age >65 years, previous peptic ulcer disease, comorbidities such as cardiovascular disease, diabetes and cocurrent therapy with NSAIDs or prednisilone.
What are the administration instructions for Aspirin?
To minimise gastric irritaton should be taken after food.
What should be communicated to patients with the use of NSAIDs?
Warn to watch out for indigestion or bleeding symptoms.
Why is Aspirin only used for primary prevention not secondary prevention?
Absolute risk of serious vascular events in this group is low and any potential benefits of low-dose aspirin are offset by the increased risk of serious bleeding
What drugs are in the class Benzodiazepines?
Diazepam
Temazepam
Lorazepam
Chlordiazepoxide
Midazolam
What are the indications for Benzodiazepines (5)?
(Diazepam, Temazepam, Lorazepam, Chlordiazepoxide, Midazolam)
- First line management of seizures and status epilepticus
- First line management of alcohol withdrawal reactions
- Common choice for sedation for interventional procedures, if general anaesthesia isn’t used.
- Short-term management of severe, disabling or distressing anxiety
- For short-term treatment of severe, disabling or distressing insomnia.
What is the mechanism of action of Benzodiazepines?
(Diazepam, Temazepam, Lorazepam, Chlordiazepoxide, Midazolam)
Target GABA receptors.
GABA is the main inhibitory neurotransmitter in the brain.
Benzodiazepines facilitate and enhance banding of GABA to the GABA receptors. Having a widespread depressant effect on synaptic transmission.
Reduces anxiety, causes sleepiness, sedation and anticonvulsive effects.
Why are Benzodizepines used in the treatment of alcohol withdrawal?
Alcohol also acts on the GABA receptors and in chronic excess the patient becomes tolerant to its presence. Abrupt cessation then provokes the excitatory state of alcohol withdrawal. This can be treated by introducing a Benzodiazepine
What are the adverse effects of Benzodiazepines?
(Diazepam, Temazepam, Lorazepam, Chlordiazepoxide, Midazolam)
Dose-dependent drowsiness, sedation and coma.
Little cardiorespiratory depression in overdose but loss of airway reflexes can lead to airway obstruction and death.
Dependence can develop if taken for more than a few weeks
Abrupt cessation can produce a withdrawal reaction similar to that seen with alcohol
What are the warnings and contraindications for Benzodiazepines?
(Diazepam, Temazepam, Lorazepam, Chlordiazepoxide, Midazolam)
Elderly more susceptible to effects
Best avoided in patients with signficant respiratory impairment or neuromuscular disease (e.g. myasthenia gravis).
Should also be avoided in liver failure but if use is essential e.g. alcohol withdrawal - Lorazepam may be best choice.
What are the interactions of Benzodiazepines?
Additive to other sedating drugs including alcohol and opioids
Most depend on cytochrome P450 enzymes for elimination so concurrent use with cytochrome P450 inhibitors may increase effects
What is the dose and prescription advice for Benzodiazepines?
(Diazepam, Temazepam, Lorazepam, Chlordiazepoxide, Midazolam)
(Duration of action varies)
Seizures - long-acting - Lorazepam - 4mg IV or Diazepam 10mg or Diazepam - rectal solution
Alcohol withdrawal - Oral chlordiazepoxide
Sedation - Midazolam
Insomniaa and Anxiety - Temazepam
What is the administration advice for Benzodiazepines?
Senior supervision
Injected slowly
What should be communicated to patients with the use of Benzodiazepines?
Only a short term measure for depression and anxiety
Discuss the risk of dependence, don’t take for >4 weeks
Don’t drive or operate heavy machinery
What is the monitoring advice for Benzodiazepines?
(Diazepam, Temazepam, Lorazepam, Chlordiazepoxide, Midazolam)
Close monitoring of the patient’s clinical status and vtal signs are essential following IV or high dose Benzos.
What drug is an antagonist of Benzodiazepines?
Flumazenil
(Rarely indicated - not when mixed or uncertain overdose)
What drugs are in the class Beta2-agonists?
Salbutamol
Salmeterol
Formoterol
Terbutaline
What are the indications for Beta2-agonists?
(Salbutamol, Salmeterol, Formoterol, Terbutaline)
- Asthma: short acting B2-agonists are used to relieve breathlessness. Long-acting B2-agonists are used in step 3 treatment for chronic asthma, but must always be given in combination with inhaled corticosteroids.
- COPD: short acting B2-agonists are used to relive breathlessness. Long-acting B2-agonists are an option for second-line therapy of COPD.
- Hyperkalaemia: nebulised salbutamol may be used as an additional treatment (alongside insulin, glucose and calcium gluconate) for the urgent treatment of high serum potassium concentration.
What is the mechanism of action of Beta2-agonists?
(Salbutamol, Salmeterol, Formoterol, Terbutaline)
Beta2-receptors are found in smooth muscle of the bronchi.
(also GI tract, uterus and blood vessels)
Stimulation leads to smooth muscle relaxation
This improves airflow in consricted airways.
Like insulin also stimulates Na+/K+-ATPase pumps on cell serface membranes, causing a shift of K+ from the extracellular to intracellular compartment.
What are the short and long-acting Beta2-agonists?
(Salbutamol, Salmeterol, Formoterol, Terbutaline)
Short-acting: Salbutamol, Terbutaline
Long-acting: Salmeterol, Formoterol
What are the adverse effects of Beta2-agonists?
‘Fight or flight’ adverse effects
Tachycardia, palpitations, anxiety and tremor
Promote glucogenolysis so may increase serum glucose concentration
Long-acting B2-agonists can cause muscle cramps
What are the warnings and contraindications for Beta2-agonists?
Long-acting B2-agonists useding in asthma only if an inhaled corticosteroid is also used.
This is because without there is an increased riskof asthma deaths
Caution in cardiovascular disease as the tachycardia can provoke angina and arrhythmias
What are the important interactions for Beta-2 agonists?
(Salbutamol, Salmeterol, Formoterol, Terbutaline)
Beta-blockers ma reduce the effectiveness of B2-agonists.
Concomitant use of B2-agonists with theophylline and corticosteroids can lead to hypokalaemia so serum potassium should be monitored.
What is the dose and prescription advice for Beta2-agonists?
(Salbutamol, Salmeterol, Formoterol, Terbutaline)
Short-acting - Salbutamol, Terbultaline - As required - 100-200 micrograms inhaled as required
In asthma and COPD requiring hospital treatment, nebulised - salbutamol 2.5 mg nebulised 4-hourly (spacer possible)
Long-actng - maintenance therapy - BD - must be with steroid in asthma so can be combined inhaler e.g. Seretide or Symbicort - improves convenience also.
What is the administration advice for Beta2-agonists?
Aerosol - Metered dose inhaler
Dry powder
Spacer with metered dose inhalers
Inhaler technique should be checked and corrected at every consultation
What should be communicated to patients with the use of Beta2-agonists?
Medicine to relax airways and improve breathing
Treats symptoms not disease
If they need to use freqently seek medical advice
Make sure know inhaler technique
What is the monitoring for Beta2-agonists?
Symptoms and serial measurements of peak expiratory flow rate
Adjust reatment with guidance from action plan
COPD: severity and exacerbation rates
What drugs are in the class Beta-blockers?
Bisoprolol
Atenolol
Propranolol
Metoprolol
What are the indications for Beta-blockers (5)?
(Bisoprolol, Atenolol, Propranolol, Metoprolol)
- Ischaemic heart disease: 1st line option to improve symptoms and prognosis associated with angina and acute coronary syndrome
- Chronic heart failure: 1st line option to improve prognosis
- Atrial fibrillation: 1st line option to reduce the ventricular rate and, in paroxysmal atrial fibrillaiton, to maintain sinus rhythm.
- Supraventricular tachycardia (SVT): as a 1st line option in patients without circulatory compromise to restore sinus rhythm
- Hypertension: may be used when other treatments: CCB, ACEi and theiazide diuretics are insufficient or inappropriate.
What is the mechanism of action of beta-blockers?
(Bisoprolol, Atenolol, Propranolol, Metoprolol)
Beta1-adrenoreceptors are located mainty in the heart, Beta2-adrenoreceptors are found mostly in smooth muscle of blood vessels and airways.
Via the B1-receptor, Beta-blockers reduce force of contration and speed of conduction in the heart.
This relives myocaridal ischamia by reducing cardiac work and oxygen demand, and increasing myocaridal perfusion. They improve prognosis in heart failure by ‘protecting’ the heart from the effects of chronic sympathetic stimulation.
They slow the ventricular rate in atrial fibrilation mainly by prolonguing the refractory period of the atrioventricular (AV) node.
Reduce renin secretion from the kidneys to lower high blood pressure.
What are the adverse effects of beta-blockers?
(Bisoprolol, Atenolol, Propranolol, Metoprolol)
Fatigue
Cold extremities
Headache
Nausea
Sleep disturbance and nightmares
Impotence in men
What are the warnings and contraindicaitons for beta-blockers?
(Bisoprolol, Atenolol, Propranolol, Metoprolol)
Asthma - can cause life-threatening bronchospasm - contraindicated.
Caution in COPD - but use B1-selective
Heart failure: gradual increase
Contraindicated in heart block
Reduced dose in hepatic failure
What are the important interactions for beta-blockers?
Not used with non-dihydropyridine calcium channel blockers (e.g. verapamil, diltiazem) as can cause heart failure, bradycardia and asystole.
What is the dose and prescription advice for beta-blockers?
(Bisoprolol, Atenolol, Propranolol, Metoprolol)
PO - dose varies according to drug and indication.
Start at lowest dose and increase
IV is possible where rapid effect is required.
Taken at regular intervals
What is the communication advice for beta-blockers?
Discuss Sfx
With Heart Failure about risk of initial deterioration in symptoms
COPD: stop and seek help if difficulty breathing develops
What is the monitoring advice for beta-blockers?
(Bisoprolol, Atenolol, Propranolol, Metoprolol)
Dose adjust to patient’s symptoms and hr in ischarmic heart disease.
What beta-blocker is most suitable for treatment of acute coronary syndrome?
Metoprolol
(Short half-life so better to start with this at first then convert to once daily at later point)
What drugs are in the class Bisphosphonates?
Alendronic Acid
Disodium Pamidronate
Zoledronic Acid
What are the indications for Bisphosphonates (4)?
(Alendronic Acid, Disodium Pamidronate, Zoledronic Acid)
- Risk of osteoporotic fragility fractures - Alendronic acid
- Severe hypercalcaemia of malignancy - Pamidronate and Zoledronic acid after IV rehydration
- Myeloma and breast cancer with bone mets - Pamidronate and Zoledronic acid - reduces risk of pathological fractures, cord compression and need for radiotherapy and surgery
- Paget’s disease - 1st line treatment when metabolically active, aim of reducing bone turnover and pain.
What is the mechanism of action of Bisphosphonates?
Reduce bone turnover by inhibiting the action of osteoclasts, the cells responsible for bone resorption.
Net effect is reduction in bone loss and improvement in bone mass.
What are the potential adverse effects of Bisphosphonates?
(Alendronic Acid, Disodium Pamidronate, Zoledronic Acid)
Common: Oesophagitis and hypophosphataemia
Rare but serious: Osteonecrosis of the jaw, more likely in high dose IV therapy
Good dental care is important
Rare but serious: Atypical femoral fracture, long-term use.
What are the warnings and contraindications for Bisphosphonates?
Avoid in severe renal impairment
CI in hypocalcaemia (will increase)
Oral CI in upper Gi disorders
Caution in smokers and dental disease: (osteonecrosis of the jaw)
What are the important interactions of Bisphosphonates?
(Alendronic Acid, Disodium Pamidronate, Zoledronic Acid)
Bind calcium
Absorption is thefere reduced if taken with calcium salts (including milk) as well as antacids and iron salts.
What is the dose and prescription advice for Bisphosphonates?
(Alendronic Acid, Disodium Pamidronate, Zoledronic Acid)
Osteoporosis: PO, 70mg once Weekly
Severe hypercalcaemia and bone metastases: Pamidronate or Zolendronic acid: Slow IV infusions.
Paget’s disease: Risedronate PO or Pamidronate IV.
What is the administration advice for Bisphosphonates?
(Alendronic Acid, Disodium Pamidronate, Zoledronic Acid)
30 minutes before food or other medications
Sitting upright for 30 minutes
Take with plenty of water
Ensure good dental health and see dentist
Report any symptoms of oesophangel irritation
What is the monitoring of Bisphosphonates?
(Alendronic Acid, Disodium Pamidronate, Zoledronic Acid)
In osteoporosis: check and replace calcium and vitamin D before treatment. Monitor efficacy using dual-energy X-ray absorptiometry (DEXA) scans every 1-2 years to check bone density is stable or increasing.
Hypercalcaemia - calcium levels
Myeloma, bone mets, Paget’s disease - Bone pain, fractures
Symptoms of oesophagitis, osteonecrosis of the jaw - monitor calcium and phosphate levels.
What drugs are in the class Calcium and Vitamin D?
Calcium Carbonate
Calcium Gluconate
Colecalciferol
Alfacalcidol
What are the Indications for Calcium and Vitamin D (5)?
(Calcium Carbonate, Calcium Gluconate, Colecalciferol, Alfacalcidol)
- Osteoporosis: Calcium and vitamin D supplements used to ensure positive calcium balance when dietary intake and/or sunlight exposure are insufficient. (+ Bisphosphonates)
- Chronic Kidney Disease: to treat and prevent secondary hyperparathyroisism and renal osteodystrophy.
- Severe hyperkalaemia: Calcium gluconate to prevent life-threatening arrythmias (+ insulin and glucose)
- Severe or symptomatic hypocalcaemia
- Vitamin D deficiency: Rickets in children and Osteomalacia in adults.
What is the mechanism of action of Calcium and vitamim D?
(Calcium Carbonate, Calcium Gluconate, Colecalciferol, Alfacalcidol)
Calcium homeostasis is controlled by parathyroid hormone and vitamin D, which increase serum calcium levels and bone mineralisation, and calcitonin which reduces serum calcium levels.
In severe CKD, impaired phosphate excretion and reduced activation of vitamin D cause hyperphosphataemia and hypocalcaemia. This stimulates secondary hyperparathyroisism, which leads to a range of bone changes called renal osteodystrophy.
In hyperkalaemia, calcium raises the myocaridal thresshold potential, reducing excitability and the risk of arrhythmias, it does not alter the serum potassium levels.
What are the adverse effects of Calcium and Vitamin D?
Oral calcium can cause dyspepsia and constipaiton.
When IV for the treatment of hyperkalaemia, calcium gluconate can cause cardiovascular collapse if administered too fast and local tissue damage if accidentally given into subcutaneous tissue.
What are the warnings and contraindications for Calcium and Vitamin D?
(Calcium Carbonate, Calcium Gluconate, Colecalciferol, Alfacalcidol)
Hypercalcaemia
What are the important interactions for Calcium and Vitamin D?
Oral calcium reduces the absorption of many drugs including iron, bisphosphonates, tethracyclines and levothyroxine.
IV calcium carbinate cannot be given with sodium bicarbonate as risk of precipitation.
What is the dose and prescription advice for Calcium and Vitamin D?
(Calcium Carbonate, Calcium Gluconate, Colecalciferol, Alfacalcidol)
Osteoporosis: 1-1.2 g of Calcium and 800 units of vitamin D per day.
Adcal D2: TD (Combined prescription)
Severe hyperkalaemia: 10 ml calcium gluconate 10% for administration by slow IV injection (repeat doses if ECG cahnges persist)
Senior advice: Hypocalcaemia, Vit D deficiency and Severe CKD.
What is the administration advice for Calcium and Vitamin D?
(Calcium Carbonate, Calcium Gluconate, Colecalciferol, Alfacalcidol)
Oral calcium should be chewed and swallowed.
Separate from interacting medicines
Calcium glucontae: Slow IV injection in large vein over 5-10 minutes
What is the monitoring of Calcium and Vitamin D?
Calcium gluconate: Severe hyperkalaemia, continuous cardiac monitoring. Repeat 12 leas EVG to confirm resolution of abnromalities.
For calcium and vitamin D supplements, check serum calcium levels at regular intervals or if they develop symtoms or hypercalcaemia.
Calcium Gluconate if the 1st line treatment for Hyperkalaemia in emergencies, what is the dose?
10 ml of calcium gluconate 10% IV over 5-10 minutes
What drugs are in the class Calcium Channel Blockers?
Amlodipine
Nifedipine
Diltiazem
Verapamil
What are the indications for Calcium Channel Blockers (3)?
(Amlodipine, Nifedipine, Diltiazem, Verapamil)
- Hypertension - Amlodipine/Nifedipine are used for 1st or 2nd line treatment of hypertension to reduce risk of stroke, MI and death from CVD.
- Stable angina: B-blockers 1st line but CCB can also be used for symptom control
- Supraventricular arrhythmias: Diltiazem and verapamil are used to control cardiac rate in SVT, Atrial flutter and AF
What is the mechanism of action of Calcium Channel Blockers?
(Amlodipine, Nifedipine, Diltiazem, Verapamil)
CCBs decrease calcium entry into vascular and caridac cells.
This causes relaxation and vasodilation in arterial smooth muscle, lowering arterial pressure.
In the heart, CCBs reduce myocarial contractility and suppress cardiac conduction.
All reduce oxygen demand, preventing angina.
What are the two groups of calcium channel blockers?
(Amlodipine, Nifedipine, Diltiazem, Verapamil)
Dihydropyridines: amodipine and nifedipine - selective for vasculature
Non-dihydropyridines: verapamol, diltiazem - selective for the heart.
What are the potential adverse effects of Calcium Channel Blockers?
(Amlodipine, Nifedipine, Diltiazem, Verapamil)
Dihydropyridines (Vascular selective): Amlodipine, Nifedipine: Ankle swelling, flushing, headache and palpitations - caused by vasodilatation and compensatory tachycardia.
Verapamil - constipation, bradycardia, heart block rarely - cardiac failure.
What are the warnings and contraindications for Calcium Channel Blockers?
Verapamil and Diltiazem: caution in poor left ventricular function - can precipitate or worsen heart failure.
Avoided in AV nodal condiction delay - can precipitate heart block
Amlodipine and Nifedipine - useful for stable angina but CI in unstable angina .
Avoided in severe aortic stenosis.
What are the important interactions for Calcium Channel Blockers?
(Amlodipine, Nifedipine, Diltiazem, Verapamil)
Non-dihydropyridine (Verapamil and Diltiazem) should not be prescribed with B-blockers - can cause heart failure.
What is the dose and prescription advice for Calcium Channel Blockers?
(Amlodipine, Nifedipine, Diltiazem, Verapamil)
PO - Amlodipine - OD
Ohters more frequently - 8hr or 12 hr
Hypertension: Amlodipine: 5-10 mg PO, OD
Angina: Diltiazem MR 90mg PO, TD
Supreventricular arrythmias: Verapamil 40-120 mg PO, TDS
What should be communicated to patients in regards to Calcium Channel Blockers?
(Amlodipine, Nifedipine, Diltiazem, Verapamil)
Other factors to reduce CVS risk
Common side effects: Ankle oedema
What is the monitoring of Calcium Channel Blockers?
(Amlodipine, Nifedipine, Diltiazem, Verapamil)
Regular blood pressure monitoring for HTN
Angina: chest pain
Pulse rate, ECG
24- hour tape ECG for arrythmias
What are the indications for treatment with Carbamazepine (3)?
- Epilepsy - 1st choice for focal seizures with and without secondary generalisation and for primary generalised seizures
- Trigeminal Neuralgia - 1st choice to control pain and reduce frequency and severity of attacks
- Bipolar disordeir - Option for prohylaxis in patients resistant or intolerant to other medications.
What is the mechanism of action of Carbamazepine?
Appears to inhibit neuronal sodium channels, reducing neuronal excitability.
What are the adverse effects of Carbamazepine?
GI Upset (nausea and vomiting)
Neurological effects (dizziness and ataxia)
Hypersensitivity (10%)
Antiepileptic hypersensitivity syndrome - skin reactions, ever and lymphadenopathy with systemic involvement, mortality 10%
Oedema and hyponatraemia
What are the warnings and contraindications for Carbamazepine?
Caution in pregancy - may cause defects, should have high-dose folic acid supplements before conception
Prior antiepileptic hypersensitivity syndrome is a CI to carbamazepine and phenytoin
Caustion with hepatic, renal or caridac disease
What are the important interactions of Carbamazepine?
Induces P450 enzymes, reducing plasma concentration and efficacy of drugs that are metabolised by P4450 enzymes.
Effects increased by cytochrome P450 inhibitors
Complex interactions with other antiepeleptic durgs and drugs loweing seizure threshold (tricyclic antidepressants, antipsychotic, tramadol)
What is the dose and prescription advice for Carbamazepine?
PO or PR
Started low dose 100-200 mg OD or BD
Tradually increased to up to 1.6 g/day in divided doses
Treatment should be stopped slowly under medical supervision
What should be communicated with the use of Carbamazepine?
Signs of severe hypersensitivity: Skin rashes, bruising , bleeding, high temp, mouth ulcers.
Discuss contraception and pregnancy
Must not drive unless seizure free for 12 months, shoud not drive for 6 months after changing or stopping seizures.
What is the monitoring of Carbamazepine?
Monitored by comparing seizure frequency before and after starting treatment or dose adjustment.
For safety: report symptoms hypersensitivity
Plasma carbamazepine (selvct cases)
What drugs, newer than Carbamazepine may also be used for seizure prevention?
Lamotrigine
Levetiracetam (Keppra)
Choice depending on seizure type, epilepsy syndrome, co-medication, comorbidities and patient choice.
Carbamazepine first choice for focal seizures and sometimes for primary focal seizures
What drugs are in the class Cephalosporins and Carbapenems?
Cefalexin
Cefotaxime
Meropenem
Ertapenem
What are the indications for Cephalosporins and Carbapenems?
(Cefalexin, Cefotaxime, Meropenem, Ertapenem)
- Oral cephalosporins are 2nd and 3rd line treatment options for UTIs and RTIs
- IV cephalosporins and carbapenems are for the treatment of infections that are very severe or complicated, or caused by antibiotic-resistant organisms. Due to their broad antimicrobial spectrum they can be used for most indications.
What is the mechanism of Cephalosporins or Carbapenems?
(Cefalexin, Cefotaxime, Meropenem, Ertapenem)
Antimicrobial effect due to ß-lactam ring.
Weakens bacterial cell wall leading to swelling, lysis and death.
More resistant to beta-lactamases than penecillins
What are the potential adverse effects of Cephalosporins and Carbapenems?
(Cefalexin, Cefotaxime, Meropenem, Ertapenem)
GI upset - nausea and diarrhoea
Antibiotic-associated colitis - when broad spectrum antibiotics kill normal gut flora, allowing overgrowth of toxin producing c.diff.
Hypersensitivity and cross-reactivity in penecillin-alergic patients
CNS toxicity is possible
What are the warnings and contraindications for Cephalosporins and Carbapenems?
(Cefalexin, Cefotaxime, Meropenem, Ertapenem)
In caution in ptts at risk of C.diff infection
Allergy to penecillins, cephalosporins or carbapenems (CI if anaphylactic)
Caution in epilepsy and renal impairment
What are the important interactions for Cephalosporins and Carbapenems?
(Cefalexin, Cefotaxime, Meropenem, Ertapenem)
Can enhance the anticoagulant effect of Warfarin by killing normal gut flora that synthesise vitamin K
Increase nephrotoxicity of animoglycosides
Reduce plasma concentration and efficacy of valporate.
What is the dose and prescription advice for Cephalosporins and Carbapenems?
(Cefalexin, Cefotaxime, Meropenem, Ertapenem)
Check BNF
Orally or oral suspension by injection.
(Ertapenem best for outpatient therapy as OD)
In many hospitals cannot be prescribed without the approval of a microbiologist
What is the communication advice for Cephalosporins and Carbapenems?
(Cefalexin, Cefotaxime, Meropenem, Ertapenem)
Check for allergy to penecillins or B-lactam antibiotics.
What is the monitoring for Cephalosporins and Carbapenems?
(Cefalexin, Cefotaxime, Meropenem, Ertapenem)
Clinical signs of infection resolving e.g. resolution of pyrexia
Blood tests: falling of C-reactive protein and WCC.
What are the indications for Clopidogrel?
(Generally prescribed with aspirin, though may be used alone where aspirin is contraindicated or not tolerated)
- For treatment of acute coronary syndrome (ACS), prevent or limit arterial thrombosis.
- To prevent occlusion of coronary artery stents
- For long-term 2nd prevention of thrombotic arterial events in patients with cardiobascular, cerebrovascular and peripheral arterial disease
- To reduce the risk of intracardiac thrombus and embolic stroke in atrial fibrillation where warfarin and NOACs are contraindicated.
What is the mechanism of action of Clopidogrel?
Thrombotic events occur when a platelet-rich thrombus forms in atheromatous arteries and occludes the circulation.
Clopidogrel prevents platelet aggregation and reduces the risk of arterial occlusion by bindin to ADP receptors.
Actions are syndergistic with aspirin.
What are the potential adverse effects of Clopidogrel?
Bleeding - esp if GI, Neuro or Surgical
GI Upset
Rare: Thrombocytopenia
What are the warnings and contraindications of clopidogrel?
Not with active bleeding
Stopped 7 days before elective surgery
Used with caution in renal and hepatic impairment
What are the important interactions of Clopidogrel?
Pro-drug requiring metabolism by hepatic cytochrome P450 enzymes to active form
Efficacy may be reduced by cytochrome P450 inhibitors
Co-prescription with other antiplatet drugs (e.g. aspirin) or anticoagulants (e.g. heparin) or NSAIDs increases the risk of bleeding.
What is the dose and prescription advice for Clopidogrel?
PO
May require loading dose
300mg for ACS in once only before maintenance dose
Maintenance dose of 75mg PO OD
(For drug-eluting coronary stent dual antiplatelet therapy should be continued for 12 months)
What is the communication advice for Clopidogrel?
Redudes risk of heat attacks and strokes and prolongs life.
Ask about active bleeding
Explain if bleeding occurs may take longer to stop.
Why is clopidogrel stopped 7 days before elective surgery?
Acts irreversibly for the lifespan of the platelet 7-10 days.
In emergency cases, patients taking clopidogrel may require platelet transfusions to help stop bleeding.
What drugs are in the class Compound (ß2-agonist-corticosteroid) inhalers?
Seretide
Symbicort
What are the indications for Compound (ß2-agonist-corticosteroid) inhalers?
(Seretide, Symbicort)
- Asthma: control of symptoms and prevention of exacerbations, used at ‘steps 3-4’ in the management of chronic asthama.
- COPD: to control symtpoms and prevent exacerbations in patients who have severe airflow obstruction on spirometry and/or recurrent exacerbations
What is the mechanism of action of Compound (ß2-agonist-corticosteroid) inhalers?
(Seretide, Symbicort)
Inhaled corticosteroid to suppress airway inflammation
Long-acting B2-agonist (LABA) to stimulate bronchodilation
Combined prescription reduces number of inhalerss and increases adherence.
LABA must be taken with a corticosteroid as otherwise associated with more deaths.
(Seretide - fluticasone and salmeterol)
(Symbicort - budesonide and formoterol)
What are the important adverse effects of Compound (ß2-agonist-corticosteroid) inhalers?
Inhaled corticosteroids - oral thrush, hoaese voice
High-dose, long-time - Systemic effects - Adrenal suppression, growth retardation, osteoporosis
LABAs - Tremor, tachycardia, arrythmias, muscle cramps
What are the warnings and contraindications for Compound (ß2-agonist-corticosteroid) inhalers?
Caution in:
COPD patients with Hx of pneumonia
Children
Cardiovascular disease - tachycardia may provoke angina or arrhythmias.
What are the important interactions for Compound (ß2-agonist-corticosteroid) inhalers?
(Seretide, Symbicort)
Beta-blockers (CI asthma) may reduce the efficaacy of B2-agonists.
What is the dose and prescription advice for Compound (ß2-agonist-corticosteroid) inhalers?
(Seretide, Symbicort)
By brand name, inhaler type and strength: no.x / no.x (in micrograms) + number of ‘puffs’ and frequency
What should be communicated to patients with Compound (ß2-agonist-corticosteroid) inhalers?
New inhaler will prevent attacks and improve breathlessness, but must be taken without fail every morning and evening to have benefit.
Rinse mouth and gargle after taking the inhaler.
What is the monitoring advice for Compound (ß2-agonist-corticosteroid) inhalers?
(Seretide, Symbicort)
Ask about symptoms, check worked by reviewing peak flow measurements (asthma) or exacerbation frequency (CODP and asthma)
What drugs are in the class Corticosteroids (glucocorticoids), systemic?
Prednisolone
Hydrocortisone
Dexamethasone
What are the indications for Corticosteroids (glucocorticoids), systemic (4)?
(Prednisolone, Hydrocortisone, Dexamethasone)
- Treating allergic and inflammatory disorders: e.g. anaphylacis, asthma.
- To suppress autoimmune disease e.g. IBD, inflammatory arthritis
- Treatment of cancers (part of chemo or reduce swelling)
- Hormone replacment in adrenal insufficiency or hypopituitarism.
What is the mechanism of action of Corticosteroids (glucocorticoids), systemic?
(Prednisolone, Hydrocortisone, Dexamethasone)
Exert glucocorticoid effects
Modify the immune response to reduce inflammation.
Metabolic effects - increased gluconeogenesis from increased circulating amino and fatty acids, released by catabolism (breakdown) of muscle and fat.
Mineralocorticoid effects - Stimulates Na+ and water retention and K+ excretion in the renal tubule.
What are the adverse effects of Corticosteroids (glucocorticoids), systemic?
(Prednisolone, Hydrocordisone, Dexamethasone)
Immunosuppression - increases risk and severity of infection
Metabolic effects - diabetes melitus and osteoporosis. Proximal muscle weakness, skin thinning, easy brusing and gastritis (increased catabolism)
Mood and behavioral changes: Insomnia, confusion, psychosis and suicidal ideas.
Mineralocordicoid actions: hypokalaemia and oedema.
Adrenal atrophy and Addisonian Crisis (Long-term/withdrawal)
When in the use of Corticosteroids (glucocorticoids), systemic does an Addisonian crisis occur and why?
(Prednisolone, Hydrocortisone, Dexamethasone)
If there is sudden withdrawal following prolongued use.
Corticosteroids suppress pituitary ACTH secretion, switching off the stimulus for normal adrenal cortisone production. In prolongued treatment this causes adrenal atrophy, preventing endogenous cortisol secretion. If they are withdrawn suddely and acute Addisonian crisis with cardiovascular collapse.
Slow withdrawal is necessary to allow recovery of adrenal fucntion. Symptoms of chronic glucocorticoid deficiency that occur during treatment withdrawal include fatigue, weight loss and arthralgia.
What are the warnings and contraindications for the use of Corticosteroids (glucocorticoids), systemic?
(Prednisolone, Hydrocortisone, Dexamethasone)
In caution in people with:
Infection (Immunosuppresion)
Children (Growth-suppression)
What are the important interactions for Corticosteroids (glucocorticoids), systemic?
(Dexamethasone, Hydrocortisone, Prednisolone)
NSAIDS: increase the risk of peptic ulceration and GI bleeding
Hypokalaema: with B2 agonists, theophylline, loop and thiazide diuretics.
Efficacy can be reduced by cytochrome 450 inducers
Reduce immune response to vaccines.
What is the dose and prescription advice for Corticosteroids (glucocorticoids), systemic?
Dexamethasone - most potent - 750 micrograms
Prednisolone - moderate - 5 mg
Hydrocortisone - 20 mg
PO, IV or IM
Emergencies - cerebral oedema (cancer) - Dexamethasone
Acute asthma - Prednisolone - 40 mg PO OD.
Long term e.g. arthritis - Lowest dose of oral prednisolone (May require co-prescription of steroid-sparing agents e.g. azithioprine/methotrexate)
Also consider the use of bisphosphonates and PPIs to reduce some of the steroid side effects.
What is the administration advice for Corticosteroids (glucocorticoids), systemic?
(Prednisolone, Hydrocortisone, Dexamethasone)
OD taken in the morning, to mimic natural circadian rhythm and reduce insomnia.
Do not stop treatment suddently as could make them very unwell - carry a steroid card.
Discuss the long term benefits and risks.
What is the monitoring for Corticosteroids (glucocorticoids), systemic?
(Prednisolone, Hydrocortisone, Dexamethasone)
Monitoring of efficacy on conditon treated
Asthma - peak flow recordings
Inflammatory arthritis - blood inflammatory markers
Adverse effects - HbA1c (DM) DEXA scan (Osteoporosis)
When might an increased dose of Corticosteroids (glucocorticoids), systemic be required?
If on long-term corticosteroid treatment, may have atrophic adrenal galnds and be unable to increase cortisol treatment in response to stress.
May need to provide artificially when there is illness (potentially double dose)
What drugs are in the class Corticosteroids (glucocorticoids), inhaled (3)?
Beclometasone
Budesonide
Fluticasone
What is the indication for Corticosteroids (glucocorticoids), inhaled (2)?
(Beclometasone, Budesonide, Fluticasone)
- Asthma: to treat airway inflammation and control symptoms at ‘step 2’ of therapy when not controlled by a short-acting Beta2-agonist (e.g. Salbutamol) alone.
- COPD: severe or frequent exacerbations. Usually with LABA, or LAMA. Can be combined as Seratide or Symbicort.
What is the mechanism of action for Corticosteroids (glucocorticoids), inhaled?
(Beclometasone, Budesonide, Fluticasone)
Down regulates pro-inflammatory and uprates anti-inflammatory proteins.
Reduces mucosal inflammation, widens the airways and reduces mucus secretion.
Improves symptoms and reduces exacerbations in asthma and COPD.
What are the adverse effects of Corticosteroids (glucocorticoids), inhaled?
(Beclometasone, Budesonide, Fluticasone)
Oral thrus, hoarse voice
COPD - may increase risk of pneumonia
(Little systemic effect unless high doses for very long time - adrenal suppression, growth retardation and osteoporosis)
What are the warnings and contraindications for Corticosteroids (glucocorticoids), inhaled?
High dose in caustion:
COPD with history of pneumonia
Children
What is the dose and prescription advice for Corticosteroids (glucocorticoids), inhaled?
(Beclometasone, Budesonide, Fluticasone)
Twice daily - dose dependent on drug and severity.
Brand name prescribing may be required.
(Aerosol or dry powder form) - Spacers can help - inahler technique should be checked at every consultation
What should be communicated to patients regarding the use of Corticosteroids (glucocorticoids), inhaled?
(Beclometasone, Budesonide, Fluticasone)
Steroid inhaler to dampen down the inflammation in the lung
Rinse mouth and gargle to prevent oral thrush
Show correct inhaler technique and must be reviewed at each appointment
What is the monitoring advice for Corticosteroids (glucocorticoids), inhaled?
(Beclometasone, Budesonide, Fluticasone)
Asthma: severity and serial peak flow measurements
COPD: symptom severity and exacerbation rates (review 3-6 months)
(Have the potential to prevent disease progression in asthma)
What drugs are in the class Corticosteroids (glucocorticoids), topical?
Hydrocortisone (also oral)
Betamethasone (note. not Beclometasone)
What are the indications for Corticosteroids (glucocorticoids), topical (1)?
(Hydrocortisone, Betamethasone)
- Used in inflammatory skin conditions e.g. eczema to treat disease flares or to control chronic disease where emollients alone are ineffective.
What are the three brances of effects of Corticosteroids?
Immunosuppressive
Metabolic
Mineralocorticoid
What is the mechanism of action of Corticosteroids (glucocorticoids), topical?
Where applied topically, mostly limited to site of application.
Systemic absorption can occur with potent or prolonged use.
Topical: mild, moderately potent, potent and very potent.
Immunosuppresive effects in topical use.
What are the potential adverse effects of Corticosteroids (glucocorticoids), topical?
(Hydrocortisone, Betamethasone)
Uncommon with mild or moderately potent.
Potent and above: Local adverse effects: skin thinning, striae, telangiectasia, contact dermatitis.
Face: perioral dermatitis, acne.
Withdrawal: Rebound worseing of the underlying skin condition.
Rare: systemic effects e.g. adrenal suppression.
What are the warnings and contraindications for Corticosteroids (glucocorticoids), topical?
(Hydrocortisone, Betamethasone)
Where there is infection or facial lesions (unless very mild steroid used)
What is the dose and prescription advice for Corticosteroids (glucocorticoids), topical?
(Hydrocortisone, Betamethasone)
Use as mild as possible for as little time as possible (max 2 weeks)
Potency and name in prescription. + whether lotion, cream or ointment + amount supplied.
e.g Hydrocortisone 1% (mild), cream, supply 30g
(Also where and OD or BD, spaced equally)
What is the administration advice for Corticosteroids (glucocorticoids), topical?
(Hydrocortisone, Betamethasone)
Very thinly, only where disease is active.
Wash hands after use.
Space applications equally.
What is the communication advice for Corticosteroids (glucocorticoids), topical?
(Betamethasone, Hydrocortisone)
Topical therapy to improve skin problem
May take 1-2 weeks
Emollients should be applied 5 minutes after this
Warn risk of skin damage if applied to the wrong areas of for too long.
Fingertip - 1st crease should be enough for 2x palms.
What are the indications for Digoxin (2)?
- AF and atrial flutter, to reduce ventricular rate.
(B-blocker or non-dihydropyridine CCB (verapamil or diltiazem) usually 1st line)
- Severe heart failure: 3rd line when already taking an ACE-inhibitor, B-blocker and either an aldosterone antagonist (spironolactone) or ARB (losartan)). At an earlier stage if have AF.
(Not used particularly often anymore)
What is the mechanism of action of digoxin?
Effects on the heart:
Reduces heart rate
Increases force of contraction
What are the potential adverse effects of Digoxin?
Bradycardia, GI disturbance, Rash, Dizziness, Visual disturbance.
Low theraputic index - safety margin between the theraputic and toxic doses is narrow
Ride range of arrhythmias can occur in digoxin toxicity
What are the warnings and contraindications for Digoxin?
May worsen conduction abnromalities - CI in heart block.
Not used in ventricular arrythmias
Reduced in renal failure
Electrolyte abnormalities increase the risk of toxicity particularly hypokalaemia.
What are the important interactions for Digoxin?
Loop and thiazide diuretics - can cause hypokalaemia increasing the risk of toxicity
Some others as well can increase the risk of toxicity
What is the dose and prescription advice for Digoxin?
PO ir IV
Loading dose is required if a rapid effect is needed
500 micrograms followed by 250-500 micrograms 6 hours later depending on response
Maintenance dose 125-250 micrograms daily
IV must be given slowly
What is the communication advice for Digoxin?
Treatment should slow down abnormally fast heart rate and make heart beat more strongly
Common side effects: sickness, diarrhoea, headache
If side effects get very bad dose may be too high
What is the monitoring advice for Digoxin?
Efficacy: Symptoms and heart rate.
Check ECG, electrolytes and renal fucntion periodically.
Theraputic doses of digoxin cause ST-segment depresson - ‘reverse tick’ sign
In acute therapy: continuous cardiac monitoring is advisable.
Digoxin levels do not need to be monitored routinely - only if toxicity is suspected.
What are the indications for Dipyridamole?
- Cerebrovascular disease:
Secondary prevention of stroke:
1st line following a TIA (alone or with aspirin)
2nd line follwing ischaemic stroke where clopidogrel is contraindicated or not tolerated.
(Usually given with aspirin)
- To induce tachycardia during a myocardial perfusion scan in the diagnosis of ischaemic heart disease.
What is the mechanism of Dipyridamole?
Antiplatelet and vasodilatory effects
Increase in intra-platelet cAMP that inhibits platelet aggregation, reducing the risk of arterial occlusions.
Blocks cellular uptake of adenosine, prolonging it’s effect on blood vessels to produce vasodilation.
What are the potential adverse effects of Dipyridamole?
Vasodilatory effects: Headache, flushing, dizziness, GI symptoms
Increased risk of bleeding
Rarely: Thrombocytopenia
What are the warnings and contraindications for Dipyridamole?
In caution with:
Ischaemic heart disease
Aortic stenosis
Heart failure
What are the important interactions of Dipyridamole?
Inhibits cellular uptake of adenosine. Prolonguing effect on the heart and increasing the risk of cardiac arrest.
Incrreased risk of bleeding with other antiplatelet agents (aspirin, clopidogrel) and anticoagulants (heparin, warfarin)
What is the dose and prescription advice for Dipyridamole?
PO, Modified release in secondary prevention of stroke (Only if clopidogrel + aspirin is not tolerated)
Dipyridamole MR - 200 mg - BD
Long-term treatment
Taken with food
What communication is given to patients with Dipyridamole?
Purpose is to reduce the risk of further strokes, should keep taking indefinitely.
Increased risk of bleeding
Side effects: headache, flushing, dizziness and GI distrubance should improve with time.
What drugs are in the class Diuretics, loop?
Furosemide
Bumetanide
What are the indications for Diuretics, loop (3)?
(Furosemide, Bumetanide)
- Acute Pulmonary Oedema: For relief of breathlessness in conjunction with oxygen and nitrates
- Chronic heart failure: Symptomatic relief of fluid overload
- Other oedematous states: Symptomatic relief of fluid overload e.g. due to liver disease or renal failure (may be given with other diuretics)
What is the mechanism of action of loop diuretics?
(Furosemide, Bumetanide)
Act on the ascending limb of the loop of Henle. where they inhibit the Na+/K+/2Cl- co-transporter.
This proten transports Na+ K+ and Cl- uins from the tubular lumen into the epithelial cells and water follows by osmosis.
Inhibiting this process has a potent diuretic effect.
They also effect blood vessels, dilating capacitance veins, in heart failure this reduces preload and improves contractile function of the heart muscle.
What are the adverse effects of loop diuretics?
(Furosemide, Bumetanide)
Dehydration, Hypotension
Inhibiting Na+/K+/Cl- increases urinary loss of sodium, potassium and chloride. This also increases the excretion of magnesium, calcium and hydrogen. They are also associated with almost any low electrolyte state e.g. hyponatraema, hypokalaemia, hypochloraemia, hypocalcaemia, mypomagnesaemia and metabolic alkalosis.
Can cause hearing loss and tinnitus
What are the warnings and contraindications for loop diuretics?
(Furosemide, Bumetanide)
CI in severe hypovolaemia and dehydration
Caution if risk of hepatic encephalopathy
Caution if hypokalaemia or hyponatraemia
Can worsen gout
What are important interactions for loop diuretics?
(Furosemide, Bumetanide)
Can affect drugs excreted by the kidneys: e.g. lithium levels are increased, digoxin toxicity may be increased (diuretic associated hypokalaemia), aminoglycosides.
What is the dose and prescription advice for loop diuretics?
(Furosemide, Bumetanide)
PO or IV
In acute pulmonary oedema IV (once-only) then either more or regular oral maintenance doses.
IV slow administration
PO in the morning to avoid nocturia
What is the communication advice for loop diuretics?
Body is overloaded with water so medication to increase urine output.
Will need to urinate more, take in the morning.
What is the monitoring advice for loop diuretics?
Efficacy in pulmonary oedema: Symptoms, tachycardia, hypertension, oxygen requirements
Urine output increases more slowly than resolution of symptoms
Long-term measure symptoms, signs and body weight (slow reduction)
Safety: periodic moitoring of serum sodium, potassium and renal function is advisable.
What drugs are in the class Diuretics, potassium-sparing?
Amiloride (as co-amilofruse, co-amilozide)
What are the indications for Diuretics, potassium-sparing?
(Amiloride)
- As part of combination therapy, for the treatment of hypokalaemia arising from loop or thiazide-diuretic therapy. Aldosterone antagonists (spironolactone) also have a potassium-sparing effect and may be used as an alternative.
What is the mechanism of action of Diuretics, potassium-sparing?
(Amiloride)
PSDs are relatively weak diuretics alone. However, in combination with other diuretics they can counteract potassium loss and enhance diuresis.
Amiloride acts on the distal convoluted tubules in the kidney.
It inhibbits the reabsorption of sodium (and therefore water) by ENaC channels, leading to sodium and eater excretion and retention of potassium.
This counteracts the K+ losses of loop and thiazide diuretic therapy.
What are the combination formulations of Diuretics, potassium-sparing?
Amiloride alone or used as part of combination tablet with furosemide (a loop diuretic) as co-amilofruse, or with hydrochlorothiazide (a thiazide diuretic) as co-amilozide.
Ratio is designed to have a neutral effect on potassium balance.
What are the potential adverse effects of potassium-sparing diuretics?
(Amiloride)
GI Upset
With other diuretics: hypotension, sizziness and urinary symptoms
Electrolyte disturbances: should cancel out but still possible.
What are the warnings and contraindications for Diuretics, potassium-sparing?
Severe renal impairment
Hyperkalaemia
(Combination therapy e.g. co-amilofruse, co-amilozide, not started in hypokalaemia, only amiloride alone)
Volume depletion
What are important interactions for Diuretics, potassium-sparing?
(Amiloride)
Do not use in combination with other potassium-elevating drugs including potassium supplements and aldosterone antagonists due to the risk of hyperkalaemia
Renal clearance of other drugs may be affected.
What is the dose and prescription advice for Diuretics, potassium-sparing?
(Amiloride, co-amilofuse, co-amilozide)
Co-amilofruse most common.
State the strength of the tablet/ratio if combined.
Dose should match the dose of existing loop or thiazide diuretic if combination therapy
What is the communication for Diuretics, potassium-sparing?
(Amiloride)
Explain their potassium level is low due to the water tablet they are taking so you are changing water tablet to reduce this
Take in the morning to minimise nocturia
Sfx: Gi upset, urinary frequency
Blood test monitoring to check K+ in normal range
What is the monitoring for Diuretics, potassium-sparing?
(Amiloride)
Efficacy: reduction in symptoms for fluid overload (co-amilofruse) or blood pressure (co-amilozide)
Monitor serum potassium concentration to ensure this returns to normal (intensity of monitoring dependent on severity of imbalance)
When might a potassium-sparing diuretic be preferable to an aldosterone antagonist?
Amiloride vs. Spironolactone
Both inhibit sodium absorption through ENaC, and retain potassium.
Amiloride may be a useful alternative to spironolactone, for examble in the treatment of hypertension due to hyperaldosteronism (Conn’s syndrome) or added to loop or thiazide diuretics, particularly when the adverse effects of spironolatone (such as gynaecomastic) are unacceptable.
What are the drugs in the class Diuretics, thiazide and thiazide-like?
Bendroflumethiazide
Indapamide
Chlortalidone
What are the indications for the drugs Diuretics, thiazide and thiazide-like?
(Bendroflumethiazine, Indapamide, Chlortalidone)
- Hypertension: Alternative 1st line treatment for hypetension where a calcium channel blocker would otherwise be used but is either unsuitable (due to odema) or there are features of heart failure.
- Hypertension add-on: Add on treatment for hypertension in patients whose blood pressure is not adequately controlled by a calcium channel blocker + ACE inhibitor or ARB.
What is the mechanism of action of Diuretics, thiazide and thiazide-like?
(Bendroflumethiazide, Indapamide, Chlortalidone)
Thiazides (thiazide and thiazide-like diuretics) inhibit the Na+/Cl- co-transporter in the distal convoluted tubule of the nephron.
This prevents reabsorption of sodium and its osmotically associaed water. The resulting diuresis causes an inital fall in exracellular fluid volume. Long-term this is compensated so not useful for fluid overload but also have vasodilatory effect which means they are suitable and long-term antihypertensives.
What are the adverse effects of Diuretics, thiazide and thiazide-like?
(Bendroflumethiazide, Indapamide, Chlortalidone)
Hyponatraemia: Preventing sodium ion reabsorption from the nephron.
Hypokalaemia –> Cardiac arrhythmias: Increased delivery of sodium to the distal tubule, where it can be exchanged for potassium, increasing urinary potassium losses.
Impotence in men
What are the warnings and contraindications for Diuretics, thiazide and thiazide-like?
(Bendroflumethiazide, Indapamide, Chlortalidone)
Avoided in hypokalaemia, hyponatraemia
May precipitate gout
What are important interactions for Diuretics, thiazide and thiazide-like?
(Bendroflumethiazide, Indapamide, Chlortalidone)
Effectiveness reduced by NSAIDs
Combination with other potassium lowering drugs e.g. Loop diuretics is best avodied.
What is the dose and prescription advice for Diuretics, thiazide and thiazide-like?
What is the communication advice for Diuretics, thiazide and thiazide-like?
(Bendroflumethiazide, Indapamide, Chlortalidone)
Take in the morning to prevent nocturia
Water-tablet to treat high blood pressure. May also help with leg oedema.
Likely to need to wee more.
Ibruprofen may effect the way it works
Warn men about the risk of impotence.
What is the monitoring for Diuretics, thiazide and thiazide-like?
(Bendroflumethiazide, Indapamide, Chlortalidone)
Blood pressure and leg oedema
Measure serum electrolyte before starting and 2-4 weeks into therapy
What is a benefit of the combination of ACEi/ARB with thiazide-like diuretics?
Thiazides can cause hypokalaemia, ACEi/ARB can cause hyperkalaemia.
They have syndergistic blood pressure lowering effects
Together can improve blood pressure control and maintain a neutral potassium balance.
What drugs are in the class dopaminergic drugs?
Levodopa (as co-careldopa, co-beneldopa)
Ropinirole
Pramipexol
What are the indications for Dopaminergic Drugs?
(Levodopa (co-careldopa, co-deneldopa), Ropinirole, Pramipexol)
- Early Parkinson’s Disease: Dopamine agonists (ropinirole, pramipexol) may be preferred over levodopa.
- Later Parkinson’s Disease: Levodopa (main) others may be add ons.
- Secondary Parkinsonism: Parkinsonism symptoms due to a cause other than idiopathic Parkinson’s disease (addressing the underlying cause is better)
What is the mechanism of action of dopaminergic drugs?
(Levodopa (co-careldopa, co-deneldopa), Ropinirole, Pramipexol)
In Parkinson’s disease there is a deficiency of dopamine in the nigrostriatal pathway (substrantia nigra).
Levodopa is a precursor of dopamine that can increase dopaminergic stimulation to the striatum.
Ropinirole and pramipexol are agonists of the D2 receptor which predominates in the striatum.
What are the potential adverse effects of dopaminergic drugs?
(Levodopa (co-careldopa, co-deneldopa), Ropinirole, Pramipexol)
Nausea
Drowsiness
Confusion
Hallucinations
Hypotension
Levodopa: Wearing-off effect: Patient’s symptoms worsen towards the end of the dosage interval, this gets worse as the duration of therapy increases.
Increasing the dose can generate the opposide effect (dyskinesias)
Together called the: on-off effect. Symptoms at start and end of treatment interval.
What are the warnings and contraindications for dopaminergic drugs?
Cautiously in the elderly and those with existing cognitive or psychiatric disease as increase confusion and hallucinations
Caution in cardiovascular disease as risk of hypotension
What are the important interactions for dopaminergic drugs?
(Levodopa (co-careldopa, co-deneldopa), Ropinirole, Pramipexol)
Levodopa is always given with a peripheral dopa-decarboxylas inhibitor e.g. carbidopa to reduce conversion to dopamine outside the brain..
This desirable interaction reduces nausea and lowers sthe dose needed for theraputic effect.
Should not be combined with antipsychotics or metoclopramide (dopamine antagonist antiemetic) because effects on dopamine receptors are contradictory (which is why these can cause parkinsonism).
What is the dose and prescrption advice for Dopaminergic drugs?
(Levodopa (co-careldopa, co-deneldopa), Ropinirole, Pramipexol)
Starting or altering done by specialists.
Tend to reserve Levodopa for later in treatment to defer the development of on-off effects.
Levodopa is ONLY AVAILABLE combined with peripheral dopa-decarboxylast inhibitors: with benserazide (co-beneldopa) or carbidopa (co-careldopa).
What is the communication advice for dopaminergic drugs?
(Levodopa (co-careldopa, co-deneldopa), Ropinirole, Pramipexol)
Taken at times to achieve best symptom control for the patient.
Parkinson’s nurses and specialist teams.
What is the monitoring advice for dopaminergic drugs?
(Levodopa (co-careldopa, co-deneldopa), Ropinirole, Pramipexol)
Clinical efficacy and side effects
Blood pressure monitoring for hypotension
As a junior doctor, what role are you most likely to play in the administration of dopaminergic drugs?
Ensuring that a patient’s therapy is maintained (dose and timing) if they are admitted to hospital.
Immediate stopping can presipitate neuroleptic malignant syndrome.
What drugs are in the class Emollients?
Aqueous cream
Liquid paraffin
What are the indications for treatment with Emollients?
(Aqueous cream, liquid paraffin)
- Topical treatment for all dry or scaling skin disorders:
Alone of with topical corticosteroids in the treatment of eczema. Can reduce cracking and dryness in psoriasis (alone or in combination)
What is the mechanism of action of Emolllients?
(Aqueous cream, liquid paraffin)
Help replace water content in dry skin.
Contain oils or paraffin-based products that can help soften the skin and can reduce water loss by protecting against evaporation.
Can be used as a soap substitute as soap is drying.
What are the important adverse effects of emollients?
(Aqueous cream, liquid paraffin)
Main tolerability issue is that they cause greasiness of the skin.
Can exacerbate acne vulgaris and folliculitis by blocking pores.
What are the warnings and contraindications for emollients?
Safe but fire hazard, highly flammable.
What are the important interactions of Emollients?
(Aqueous cream, liquid paraffin)
Spaced out when using corticosteroids, applied after or may prevent them working.
What is the dose and prescription advice for emollients?
(Aqueous cream, liquid paraffin)
Lotions: Thin, Creams: Thicker, Ointments: Thickest
More useful but harder to apply
Apply at least two or three times a day
Prescribe in large volumes e.g. 500g to ensure sufficient supply
Continue treatment after improvement of symptoms to prevent recurrence
What should be communicated to patients with the use of Emollients?
(Aqueous cream, liquid paraffin)
Improve skin dryness, may taje a whikke
Apply as often as possible
Use insead of soap
Flammable and can make surfaces slippery
Apply all over and keep using when the disease is controlled
Apply corticosteroids or other treatments first
What is the monitoring advice for emollients?
See if effective by symptoms and if not add another topical treatment.
What drugs are in the class Fibrinolytic drugs?
Alteplase
Streptokinase
What are the indications for Fibrinolytic drugs (3)?
(Alteplase, Streptokinase)
- Acute ischaemic stroke (given w/i 4.5 hours of onset) - MAIN USE must exclude haemorrhagic stroke first
2. Acute ST elevation myocardial infarction (given w/i 12 hours with antiplatelet agents and anticoagulants) however PCI is usually used instead
3. Massive pulmonary embolism with haemodynamic instability
What is the mechanism of action of Fibrinolytic drugs?
(Alteplase, Streptokinase)
Catalyse the conversion of plasminogen to plasmin, dissolving fibrinous clots and re-canalising occluded vessels.
This allows reperfusion of affected tissue, preventing or limiting tissue infarction and cell death.
What are the adverse effects of Fibrinolytic drugs?
(Alteplase, Streptokinase)
Nausea, vomitting, bruising, hypotension
Stop treatment if: serious bleeding, allergic reaction, cardiogenic shock, cardiac arrest.
Reperfusion of infarcted brain or heart tissue can lead to cerebral oedema and arrythmias, respectively.
What are the warnings and contraindications for fibrinolytic drugs?
Bleeding:
Recent haemorrhage, trauma or surgery, bleeding disorders, severe hypertension, peptic ulcers.
Intercranial haemorrhage/haemorrhagic stroke must be excluded with CT scan
Previous streptokinase treatment - antibodies can block effect.
What are the important interactions for fibrinolytic drugs?
(Alteplase, Streptokinase)
Risk of haemorrgae increased if taking anticoagulants and antiplatelets.
What is the dose and prescription advice for Fibrinolytic drugs?
(Alteplase, Streptokinase)
IV, under specialist supervision, in high dependency area.
Check BNF
What should be communicated to patients with the use of fibrinolytic drugs?
(Alteplase, Streptokinase)
Risks and benefits, senior discussion with next of kin.
Only works if given within 4.5 hours.
Symptoms can get wose and 1/3 strokes are fatal.
Chance of death initially increased but chance of independenced may be increased.
What is the monitoring advice for fibrinolytic drugs?
(Alteplase, Streptokinase)
Should be monitored in high dependence area, with vital signs checked every 15 minutes for the first 2 hours + bleeding, anyphylaxis and neurological deterioration.
What are the indications for Gabapentin and Pregabalin (4)?
- Focal epilepsies: with or without secondary generalisation, usually when other anti-epileptic drugs e.g. carbamazepine provides inadequate control
- Neuropathic pain: pregabalin 2nd line after duloxetine (SNRI) for painful diabetic neuropathy and first-line in other painful neuropathies.
3. Generalised Anxiety Disorder: Pregabalin
What is the mechanism of action of Gabapentin and Pregabalin?
Structurally related to GABA but unsure of effect.
Binds to voltage sensitive Ca2+ calcium channels, where prevents the inflow of Ca2+ and inhibits neurotransmitter release. Reduces neurotransmission and excitability.
What are the potential adverse effects of Gabapentin and Pregabalin?
Generally better tolerated than other antiepileptics
Drowsiness, dizziness and ataxia, which usually improve over time.
What are the warnings and contraindications for Gabapentin and Pregabalin?
Dependent on kidneys for elimination so reduced in renal impairment
What are important interactions for Gabapentin and Pregabalin?
Seditive effect may be combined with other seditive drugs e.g. benzodiazepines
Otherwise few interactions so useful in combination regimes
What is the dose and prescription advice for Gabapentin and Pregabalin?
PO, started at low doses
Check BNF
What should be communicated to patients with the use of Gabapentin and Pregabalin?
Reduce fits, neuropathic pain or anxiety.
May cause some drowsiness or diziness, should improve
Don’t operate machinery until symptoms have settled.
What is the appropriate monitoring advice for Gabapentin and Pregabalin?
Symptom management
How can gabapentin show up on urine testing?
A false-positive result for the detection of protein. Can be sent for quantitative analysis.
What drugs are in the class H2-receptor antagonists?
Ranitidine
What are the indications for H2-receptor antagonists?
(Ranitidine)
- Peptic ulcer disease: 2nd line for treatment and prevention of gastric and duodenal ulcers and NSAID-associated ulcers. though PPIs are more effective and 1st line.
- GORD and dyspepsia: 2nd line for relief of symptoms. PPIs may be used instead.
What is the mechanism of action of H2-receptor antagonists?
(Ranitidine)
Histamine H2-receptor antagonists reduce gastric acid secretion.
The proton pumps in the stomach are related in part by histamine. Blocking the H2-receptors reduces acid secretion.
(PPIs have a more complete suppresive effect)
What are the important adverse effects of H2-receptor antagonists?
Few side effects
Bowel disturbance, headache and dizziness
What are the warnings and contraindications for H2-receptor antagonists?
(Ranitidine)
Reduced in severe renal impairment
Can disguise the symptoms of gastric cancer
What is the dose and prescription advice for H2-receptor antagonists?
(Ranitidine)
Can be purchased OTC
Prescribied if > 2 weeks
150 mg BD is standard
What is the communication for H2-receptor antagonists?
(Ranitidine)
Treatment to reduce stomach acid and relieve symptoms.
Report alarm symptoms: weight loss, swallowing difficulty
What is the monitoring for H2-receptor antagonists?
(Ranitidine)
For peptic ulcer disease, repeat endoscopy may be necessary in some cases to confirm healing
For dyspepsia and gord, the reporting of reduced symptoms is best guide.
PPIs have largely superceded H2-receptor antagonists, but what benefit do H2-receptor antagonists have?
Rapid onset of effect
In patients with GORD due to undergo GA, can help prevent reflux, can be prescribed to help prevent.
What drugs are in the class Heparins and fondaparinux?
Enoxaparin
Dalteparin
Fondaparinux
Unfractionated heparin
What are the indications for Heparins and fondaparinux?
(Enoxaparin, Dalteparin, Fondaparinux, Unfractioned Heparin)
- Venous throboembolism (VTE): LMWH is the 1st choice phramacological VTE prophylaxis in hospital inpatients, and for the initial treatment of DVT and PE.
(Usually given with warfarin)
2. Acute Coronary Syndrome (ACS): LMWH or fondaparinux are part of 1st line therapy to improve revascularisation and prevent intracoronary thrombus progression (ROMANCE)
What is the mechanism of action of Heparins and fondaparinux?
(Enoxaparin, Dalteparin, Fondaparinux, Unfractioned Heparin)
Throbin and factor Ca are key components of the coagulation pathway.
Heparins and fondaparinux inhibit their function, preventing the formation and propagation of blood clots.
(LMWH preferred over UFH in most cases)
What are the common adverse effects of Heparins and fondaparinux?
(Enoxaparin, Dalteparin, Fondaparinux, Unfractioned Heparin)
Bleeding (Reduced with fondaparinux)
Injection site reactions
Rare: heparin-induced thrombocytopenia
What are the warnings and contraindications for Heparins and fondaparinux?
(Enoxaparin, Dalteparin, Fondaparinux, Unfractioned Heparin)
Caution: Increased risk of bleeding: Clotting disorders, severe uncontrolled hypertension, recent surgery or trauma.
Avoided around the time of invasive procedures (esp. lumbar puncture and spinal anaesthetia.
Lower dose in renal impairment
What are the important interactions for Heparins and fondaparinux?
Combining antithrombotic drugs increases the risk of bleeding.
Should be avoided unless part of specific treatment plan.
What can be given in the instance of major bleeding associated with heparin therapy?
(Enoxaparin, Dalteparin, Fondaparinux, Unfractioned Heparin)
Protamine
What is the dose and prescription advice for Heparins and fondaparinux?
(Enoxaparin, Dalteparin, Fondaparinux, Unfractioned Heparin)
(Some have dedicated anticoagulation chart)
SC Injection
Prophylaxis of VTE in inpatients: enoxaparin 40mg SC or dalteparin 5000 units SC daily.
VTE and ACS: Higher doses
What is the administration advice for Heparins and fondaparinux?
SC into the subcutaneous tissue of the abdominal wall.
What should be communicated to patients with the use of Heparins and fondaparinux?
(Enoxaparin, Dalteparin, Fondaparinux, Unfractioned Heparin)
VTE prophylaxis: daily injection to reduce the risk of blood clots
Discuss risks and benifits, avoid activities increasing the risk of bleeding e.g. contact sports
If appropriate train how to administer SC injections
What is the monitoring for Heparins and fondaparinux?
(Enoxaparin, Dalteparin, Fondaparinux, Unfractioned Heparin)
Activated partial thromboplastin ratio (APTR) for UFH - 6 hourly
Anticoagulant effects of LMWH and fondaparinux rarely require monitoring. If required e.g. in prgnancy can be monitored by anti-Xa activity
FBC and renal profile should be checked in all cases
If >4 days platelet count should be monitored for heparin-induced thrombocytopenia
What drugs are in the class Iron supplements?
Ferrous fumarate
Ferrous sulfate
What are the indications for iron supplements?
(Ferrous fumarate, ferrous sulfate)
1. Treatment of iron-deficiency anaemia
2. Prophylaxis of iron-deficiency anaemia in patients at risk due to poor diet, malabsorption, menorrhagia, gastrectomy, haemodialysis and infants with low birth weight
What is the mechanism of action of Iron supplements?
(Ferrous fumarate, ferrous sulfate)
Replenish iron stores, whcih are essential for erythropoiesis (the formation of new red blood cells). Required for the synthesis of haem.
(Absorbed in the duodenum and jejunum)
What are the adverse effects of Iron supplements?
(Ferrous fumarate, ferrous sulfate)
GI upset, nausea, epigastric pain, constipation and diarrhoea.
Black stools
Injection site irrritation and hypersensitivity reactions.
What are the warnings and contraindications for Iron supplements?
(Ferrous fumarate, ferrous sulfate)
Oral therapy may exacerbate bowel symptoms in patients with intestinal disease.
What are the important interactions for Iron supplements?
(Ferrous fumarate, ferrous sulfate)
Can reduce the absorption of some drugs including levothyroxine and bisphosphonates.
What is the dose and prescription advice for Iron supplements?
(Ferrous fumarate, ferrous sulfate)
PO or IV
Iron-deficiency anaemia: 100-200 mg or elemental iron, differents anoungs for two formulations, check BNF.
(Once normal continue for 3 months)
Prophylaxis of iron-deficiency anemia: Ferrous sulfare 1-2 tablets daily.
What should be communicated to patients with iron supplements?
(Ferrous fumarate, ferrous sulfate)
Improve or prevent symptoms of anaemia. May be some GI upset and stools may turn black
Different salt may be useful with GI upset.
What is the monitoring for Iron Supplements?
(Ferrous fumarate, ferrous sulfate)
FBC until haemoglobin returns to normal
What procedure may someone have to investigate anaemia?
Colonoscopy
Iron should be stopped 7-days before procedure
What drugs are in the class Laxitives, bulk-forming?
Ispaghula husk
Methylcellulose
Sterculia
What are the indications for Laxitives, bulk-forming?
(Ispaghula husk, Methylcellulose, Sterculia)
- Constibation and faecal impaction, in patients who cannot increase diatary fibre intake
- Mild chronic diarrhoea associated with diverticular disease or IBS
What is the mechanism of action of bulk-forming laxitives?
(Ispaghula husk, Methylcellulose, Sterculia)
Bulk-forming laxatives contain a hydrophilic substance which is not broken down in the gut. Like dietary fibre, this attracts water into the stool and increases its mass.
Adequate fluid intake is important in the mechanism.
Increased stool bullk stimulates peristalsis and helps relieve constipaton. It can also help in chronic diarrhoea (IBS, DD)
What are the potential adverse effects of bulk-forming laxitives?
(Ispaghula husk, Methylcellulose, Sterculia)
Mild abdominat distension and flatulence
Can cause fecal impaction and GI obstruction (even though used to treat this)
What are the warnings and contraindications for bulk-forming laxitives?
(Ispaghula husk, Methylcellulose, Sterculia)
Not used with sub-acute or esteplished intestinal obstruction or faecal impaction, (only constipation) and in general should not be used in ileus.
Do not prescribe for patients with new-onset constipation in patients who have just had abdominal surgery as they are at risk of surgical (paralytic) ileus and increased risk of obstruction.
What is the dose and prescription advice for bulk-forming laxitives?
(Ispaghula husk, Methylcellulose, Sterculia)
Administration around meal times, common choice is ispaghula husk 1 sachet BD.
Granules or powder to be disolved in water or tablets, should be taken with plenty of water as this is essential for effect.
What should be communicated to patients with the use of bulk-forming laxitives?
(Ispaghula husk, Methylcellulose, Sterculia)
Using a laxitive that works as a fibre supplement
Take with a meal and plenty of fluid
How is the effect of laxitives monitored?
For inpatients, stool charts can be useful.
What drugs are in the class Laxitives, osmotic?
Lactulose
Macrogol
Phosphate enema
What are the indications for the use of osmotic laxitives?
(Lactulose, Macrogol, Phosphate Enema)
- Constipation and faecal impaction
- Bowel preparation prior to surgery or endoscopy
- Hepatic encephalopathy
What is the mechanism of action of osmotic laxitives?
(Lactulose, Macrogol, Phosphate Enema)
Based on osmotically active substances (sugars or alcohol) that are not digested or absorbed and remain in the gut lumen.
They hold water in the stool maintaining the colme and stimulating peristalsis.
(Also helpful in liver failure/hepatic encephalopathy as inhibit thr proliferation of ammonia-producing bacteria)
What are the potential adverse effects of osmotic laxitives?
(Lactulose, Macrogol, Phosphate Enema)
Flatulence, abdominal cramps, nausea
Diarrhoea
Phosphate enemas can cause local irritation and electrolyte distrubances.
What are the warnings and contraindications for osmotic laxitives?
(Lactulose, Macrogol, Phosphate Enema)
CI: Intestinal obstruction: risk of perforation
Can cause fluid shits so with caution in: heart failure, ascites and electrolyte distrubances.
What is the dose and prescription advice for osmotic laxitives?
(Lactulose, Macrogol, Phosphate Enema)
Example: Lactulose 15 ml PO, BD
(Titrate to reponse, may take a few days to see effect)
Phosphate enema for faecal impaction, once only or as required.
Hepatic encephalopathy: Lactulose 30-50 mL TDS.
What is the communication advice of osmotic laxitives?
(Lactulose, Macrogol, Phosphate Enema)
Laxitive to make stool softer and easier to pass. Must drink plenty of water.
Cramps and flatulence may occur.
What are the treatment options for faecal impaction?
Can try a rectally administered glycerol suppository (stimulant laxitive) then if this doesn’t work a phosphate enema (osmotic laxitive - may case electrolyte disturbance and more uncomfortable)
What drugs are in the class stimulant laxitives?
Senna
Docusate Sodium
Bisacodyl
Glycerol Suppositories
What are the indications for stimulant laxatives?
(Senna, docusate sodium, bisacodyl, glycerol suppositories)
- Constipation - (particularly useful in the elderly in opioid use where consiptation can cause confusion)
- As glycerol suppositories for faecal impaction
What is the mechanism of action for stimulant laxatives?
(Senna, docusate sodium, bisacodyl, glycerol suppositories)
Stimulant laxatives increase water and electrolyte secretion from the colonic mucose, thereby increasing the volume of colonic content and stimulating peristalsis.
Direct pro-peristaltic action.
Docusate sodium has stimulant and faecal softening actions
What are the adverse effects of stimulant laxatives?
Abdominal pain and cramping
Diarrhoea
Melanosis coli (reversible pigmentation of the intestinal wall)
What are the warnings and contraindications for stimulant laxatives?
(Senna, docusate sodium, bisacodyl, glycerol suppositories)
Intestinal onstruction: risk of perforation
Rectal preparations: avoided in haemorrhoids or anal fissure
What is the dose and prescription advice for stimulant laxitives?
(Senna, docusate sodium, bisacodyl, glycerol suppositories)
DB, e.g. 1-2 tablets of senna
Titrate to effect
For faecal impaction, rectal stimulant lacatives should be prescribed once only in a 24 hour period
What should be communicated to patients with the use of stimulant laxtives?
(Senna, docusate sodium, bisacodyl, glycerol suppositories)
Help stool pass
Glood fluid intake necessary
May take a few doses before effect seen
Adjust dose or comfort
Abdominal pain and flatulence may occur
What are the indications for Lidocaine?
- 1st choice local anaesthetic in urinary catheterisation and minor producedures (e.g. suturing)
(Can be used as an antiarrhythmmic drug for VT and VF: Refractory to electrical cardioverstion (amiodarone) preferred)
What is the mechanism of action of Lidocaine?
Inside cells blocks voltage-gated sodium channels on surface membranes. Prevents initiation and propagation of action potentials in nerves and muscles, inducing local anaestesia in the area supplied by blocked nerve fibres.
(Role in heart in slowing conduction and increasing refractory period, terminating VT and improving chances treating VF)
What are the adverse effects of Lidocaine?
Initial stinging locally
Systemic (intentiaonal or accidental intravascular administration): Drowsiness, restless, tremor, fits.
Overdose: hypotension, arrhythmias.
What are the warnings and contraindications for Lidocaine?
Dose reduced in states of reduced cardiac output.
What drug may Lidocaine interact with?
When used with locally administered adrenaline/epinephrine can prolongue action of anaesthetic effect.
What is the dose and prescription advice for Lidocaine?
Urinary catheterisation: Instillagel
Minor procedures: 1% (10mg/ml) solution of lidocaine hydrochloride. Maximum dose 200 mg or 3mg/kg whatever is lower (more if combined with adrenaline). On deal body weight.
Use enough to produce adequate anaesthesia.
(Not systemic administration at Foundation level)
How long does Lidocaine typically take to produce local anaesthesia?
Around 5 minutes, do not test before this.
What drugs are in the class Macrolides?
Clarithromycin
Erythromycin
Azithromycin
What are the indications for treatment with Macrolides?
(Clarithromycin, Erythromycin, Azithromycin)
- Treatment of respiratory and skin and soft tissue infections as an alternative to a penicillin.
- In severe pneumonia added to a penicillin to cover atypical organisms including Legionella pneumophilia and Mycoplasma pneumonia. (evidence of consolidation on chest x-ray)
- Eradication of Helicobacter pylori (for example causing peptic ulcer disease) in combination with a PPO and either amoxicillin or metronidazole.
What is the mechanism of action of Macrolides?
(Clarithromycin, Erythromycin, Azithromycin)
Inhibit bacterial protein synthesis‘bacteriostatic’ which assists in the immune system killing and removing the bacteria from the body.
What are the potential adverse effects of Macrolides?
(Clarithromycin, Erythromycin, Azithromycin)
Irritant: can cause nausea, vomiting, GI upset, diarrhoea
IV: throbophlebitis
Allergy and antibiotic-associated colitis
Liver abnormalities: cholestatic jaundice
Prolongation of the QT interval –> arrhythmias
Ototoxicity at high doses
What are the warnings and contraindications for Macrolides?
(Clarithromycin, Erythromycin, Azithromycin)
Macrolide hypersensitivity (but useful in Penecillin allergy)
CI in severe renal and hepatic impairment
What are the important interactions with Macrolides?
(Clarithromycin, Erythromycin, Azithromycin)
Inhibit cytochrome P450 enzymes increasing plasma conc of drugs metabolised by P450 enzymes.
Warfarin and statins
Caution in drugs increasing QT interval: amiodarone, antipsychotics, quinine, quinolone antibiotics, SSRIs
What is the dose and prescription advice for Macrolides?
(Clarithromycin, Erythromycin, Azithromycin)
Clarithromycin most common
PO or IV if CI to PO (e.g. vomiting)
Usual dose Clarithromycin 250-500 mg BD 7-14 days
Include indication and duration in prescription: antibiotic stewardship.
IV Clarithromycin must be given as an infusion over at least 60 minutes not IV or IM bolus to reduce the risk of arrythmias.
PO much cheaper than IV so do this as soon as possible
What is the communication advice for Macrolides?
(Clarithromycin, Erythromycin, Azithromycin)
Getting rid of infection and improving symptoms.
Encourage to complete prescribed course
Check for no allergy to Macrolides
Seek medical adice if signs of allergy: e.g. rash ect and don’t take in future.
What is the monitoring advice for Macrolides?
Check resolution of infection by:
Resolution of symptoms
Examination: resolution of pyrexia, lung crackles
Blood tests: falling C-reactive protein and WCC
What are the indications for treatment with Methotrexate?
- Disease-modifying treatment for rheumatoid arthritis
2. Chemotherapy: as part of regimens for cancers, leukaemia, lymphoma and some solid tumours.
- Severe Psoriasis (and psoriatic arthritis) that is resistant to other therapies
What is the mechanism of action of Methotrexate?
Inhibits dihydrogolate reductase, preventing formation of FH4 and so preventing cellular replication.
Actively dividing cells are particularly sensitive to the effects of methotrexate accounting for it’s efficacy in cancer.
(Also highly teratogenic)
It also has anti-inflammatory and immunosuppresive effects - inhibiting IL-6, IL-8 and TNF-a.
What are the important adverse effects of Methotrexate?
Mucosal damage (sore mouth, GI upset)
Bone marrow suppression (neutropenia and increased risk infection)
Hypersensitivity reactions: cutaneous, hepatitis, pneumoniitis
Hepatic cirrhosis and pulmonary fibrosis - long-term
Once weeky: risk of overdose if OD accidentally: Severe renal and hepatotoxicity. Headaches, seizures and coma.
What are the warnings and contraindications for treatment with Methotrexate?
Teratogenic - pregnancy
Men and women must use effective contraception during and 3 months after stopping treatment
CI in severe renal impairment
Avoid in abnormal liver function
What are the important interactions of Methotrexate?
Toxicity more likely with drugs that inhibit renal excretion e.g. NSAIDs penecillins.
With other folate antagonists e.g. Trimethoprim and phenytoin increases the risk of haematological abnormalities.
What is the dose and prescription advice for Methotrexate?
Autoimmune disease: PO 7.5-20 mg Once WEEKLY
Adjust according to response and adverse effects
(Folic acid 5mg can be prescribed to days Methotrexate isn’t to reduce adverse effects)
For cancer, methotrexate can be given IV, IM or intrathecal routes to induce remission, then orally: specialist only.
(FY1 Doctors should not start a Methotrexate prescription)
What advice should be communicated to the patient with the use of Methotrexate?
Improve swollen painful joints or psoriasis, may take some time
To be taken ONCE A WEEK
Urgent medical advice if develops sore throad, fever, brusing or bleeding (neutropenia - bone marrow suppression), nausea, abdominal pain, or dark urine (liver poisoning) or breathlessness (pulmonary fibrosis).
Give advice regarding contraception (at time and 3 months after).
What is the monitoring advice for Methotrexate?
Symptoms and clincal examination
Blood tests (inflammatory markers)
Safety monitoring: symptoms. FBC, liver and renal function - before starting and 1-2 weeks in on establishing then every 2-3 months thereafter.
Stop immediately if any side-effects.
What are the indications for treatment with Metronidazole?
Anaerobic bacterial infections in:
- Antibiotic-associated colitis caused by Clostridium difficile, a gram-positive anaerobe.
- Oral infections (e.g. abscess) or aspiration pneumonia caused by gram-negtive anaerobe from the mouth
- Surgical and gynaecological infections caused by gram-negative anaerobes from the colon, for example Bacteroides fragilis.
- Protozoal infections: trichomonal vaginal infection, amoebic dysentery, giardiasis
What is the mechanism of action of Metronidazole?
In anaerobic bacteria, reduces DNA synthesis causing widespread damage, DNA degradation and cell death.
(Doesn’t work in aerobes)
What are the adverse effects of Metronidazole?
GI Upset: nausea and vomitting (most abx.)
Immediate and delayed hypersensitivity reactions
Long-use: Peripheral and optic neuropathy, seizures, encephalopathy
What are the warnings and contraindications for the use of Metronidazole?
Metabolised by P450 so reduced in severe liver disease.
Alcohol should not be drunk as can cause ‘disulfiram-like’ reactiion including, headache, flushing, nausea and vomiting.
What are the important interactions for Metronidazole?
Inhibitory effect on cytochrme P450 enzymes, increasing wardarin and phenytoin levels.
Reverse interaction can heppen with inducer.
Increased risk of toxicity with Lithium.
What is the dose and prescription guidance for Metronidazole?
PO for GI infection (C.diff) - 400 mg PO, 8 hourly
IV 500 mg IV, 8 hourly systemic/ PO not available/ severe
Metronidazone gel or topical for bacterial vaginosis
What should be communicated to patients with the use of Metronidazole?
Complete course
Check no allergy
DON’T DRINK ALCOHOL
Look out for signs of allegy
What is the monitoring advice for metronidazole?
Resolution of infection (same all abx.)
Treatment >10 days FBC and LFTs for adverse effects
What are the indications for Naloxone?
- Treatment of opioid toxicity associated with respiratory and/or neurological depression
What is the mechanism of action of Naloxone?
Binds to opioid receptors inc. opioid u-receptors, acts as a competitive antagonist
Has little/no effect in the absence of an exogenous opioid (e.g. morphine, heroin). If one is present it displaces it’s receptors and reverses effects. Will restore consciousness and respiratory state.
What are the adverse effects of Naloxone?
When given to opioid-dependent individual, an opioid withdrawal reaction may occur. This presents with pain (if underlying), restlessess, nausea and vomiting, dilated pupils and cold dry skin with piloerection (cold-turkey).
No other adverse effects
What are the warnings and contraindications for Naloxone?
In caution in opioid dependence: may trigger withdrawal
Lower doses in the palliative care setting to reduce the risk of complete reversal of analgesia
What is the dose and prescription advice for Naloxone?
Usually effective: 400-1200 micrograms IV, titrated (small incremental doses) to effect, smaller increments in palliative care
Can be given IM, C or intranasally.
(Can be written immediately after in emegency)
What is the communication advice for Naloxone?
Explain given antidote to counteract the effect of too much opioid.
May need to discuss how it happened to try to prevent future occurances.
What is the monitoring advice for Naloxone?
Closely monitored as the dose is titrated to effect.
Once adequate reversal is achieved keep monitoring for an hour.
The duration of action (about 20-60 min) is shorter than most opioids - so toxicity can recur when the effect has dissipated.
What are the indications for Nicorandil?
- Prevention and treatment of chest pain in people with stable angina.
1st choice is B-blockers (or CCBs), individually or in combination. (Not the Non-Dyhydropyridine Ones - Verapamil, Diltiazem)
Nicorandil (or a long acting Nitrate) can be used if these drugs are insufficient or not tolerated.
(Actual treatment and management, not just symptomatic relief of GTN spray)
What is the mechanism of action of Nicorandil?
Causes arterial and venous vasodiatation through the action as a nitrate and by activating K+-ATP channels (causing relaxation and vasodilatation)
This reduces cardiac preload and systemic and coronary vascular resistance.
This improves myocardial perfusion and decrreases myocardial work and oxygen demand. This reduces the frequency and severity of angina attacks.
What are the adverse effects of Nicorandil?
Unwanted effects of vasodilatation: flushing, dizziness and headache.
Nausea, vomiting and hypotension.
Rarely: GI, skin or mucosal ulceration
What are the warnings and contraindications for Nicorandil?
Caution: Poor left ventricular function, hypotension, pulmonary oedema
What are the important interactions for Nicorandil?
Hypotensive effects enhanced with phosphodiesterase inhibitors e.g. sildenafil (Not prescribed together)
What is the dose and prescription advice for Nicorandil?
PO, 5-10 mg BD, increased up to 20-30 mg BD
(Develops tolerance to vasodilatory adverse effects)
What is the communication advice for Nicorandil?
Reduce attacks of chest pain
Discuss other measures to reduce cardiovascular risk
Do not drive or use heavy machinery until angina and hypotension adverse effects have settled
What is the monitoring advice for Nicorandil?
Symptoms
Blood pressure: For the adverse effect of hypotension
Why would the prescription of Nicorandil also lead to referral to a cardiologist?
Patients whose symptoms are not controlled on 2 anti-anginal drugs (e.g. Beta-blocker and CCB) need referral to consider angiographhy and revascularisation.
What are the drugs in class Nicotine replacement and related drugs?
Nicotine
Varenicline
Bupropion
What are the indications for Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Smoking cessation to control physical replacement of nicotine withdrawal.
What is the mechanism of action of Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
In CNS nicotine activates nicotinic acetylcholine receptors, increasing neurotransmitter levels and causing euphoria and relaxation.
Nicotine replacement therapy prevents withdrawal symptoms by maintaining receptor activation.
Varenicline: partial agonist, reduces withdrawal and reduces rewarding effects of smoking.
Bupropion: increases noradrenaline and dopamine in synaptic cleft.
What are the potential adverse effects of Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Better than continuing smoking
Local irritation, GI upset (oral)
Palpitations and abnormal dreams
Varenicline: Same + nausea, headache, insomnia. Rare: suicidal ideation.
Bupropion: Dry mouth, GI upset, neurological and psychiatric adverse effects. Hypersensitivity.
What are the warnings and contraindications for Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Caution if haemodynamically unstable
Bupropion, Varenicline: risk of seizures, psychiatric disease
Hepatic and renal impairment
What are the important interactions of Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Only Bupropion - metabolised by cytochrome P450, so plasma levels increased by P450 inhibitors
What is the dose and prescription advice for Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Nicotine replacment therapy - continous-release patch to reduce or prevent cravings and/or an immediate-release preparation to control the acute urge to smoke.
Treatment starts either before attempt or when stopiing.
Varencline or Bupropion should start 1-2 weeks BEFORE the target quit date. Continued for 9-12 weeks.
What is the administration advice for Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Applied in the morning to an area of dry, airless skin and taken off at night to prevent insomnia
Different site each day to reduce skin irritation
Immediate-release: as and when the urge to smoke strikes
What is the communication advice for Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Medicine to help reduce the cravingfor a cigarette and irritability.
Need a plan + offer support and counselling, such as smoking cessation clinic.
What is the monitoring advice for Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Monitoring of success of quit attempt and side effects of treatment by patient report, reviewed monthly.
What is the cost/NHS prescription guidance for Nicotine replacement and related drugs?
(Nicotine, Varenicline, Bupropion)
Prescribed on NHS with clear plan
Stop if attempt fails and don’t repeat within 6 months unless exceptional circumstances.
What drugs are in the class Nitrates
Isosorbide Mononitrate
Glyceryl Trinitrate
What are the indications for treatment with Nitrates (3)?
(Isosorbide mononitrate, Glyceryl trinitrate)
- Short-acting nitrates (GTN) are used in the treatment of acute angina and chest pain associated with acute coronary syndrome.
- Long-acting nitrates (e.g. isosorbide mononitrate) are used in the prophylaxis of angina where B-blocker and/or a calciu channel blocker are insufficient or not toleated.
- Intravenous nitrates are used in the treatment of pulmonary oedema, usually combination with furosemide and oxygen
What is the mechanism of action of Nitrates?
(Isosorbide mononitrate, Glyceryl trinitrate)
Converted to nitric oxide (NO). NO increases cGMP synthesis, which reduces intracellular Ca2+, relaxing vascular smooth muscle tone.
Caues venous and some arterial vasodilatation.
Relaxation of venous capacitance vessels reduces cardiac preload and left ventricular filling. These effects reduce cardiac work and myocardial oxygen demand, relieving angina and cardiac failure.
What are the adverse effects of Nitrates?
(Isosorbide mononitrate, Glyceryl trinitrate)
Flushing,headaches, light-headedness and hypotension. Sustained use can lead to tolerance, with reduced symptom relief dispite continued use.
What are the warnings and contraindications for the use of Nitrates?
(Isosorbide mononitrate, Glyceryl trinitrate)
CI: Severe aortic stenosis; cadiovascular collapse.
Avoided in haemodynamic instability and hypotension.
What are the important interactions of nitrates?
Phosphodiesterase inhibitors (e.g. sildenafil) because prolongue hypotensive effects.
Caution with other hypotensive medications
What is the dose and prescription advice for Nitrates?
(Isosorbide mononitrate, Glyceryl trinitrate)
Stable angina, GTN sublingually as tablets or spray for immediate relief of chest pain.
In ACS or heart failure, GTN as continuous IV infusion.
Recurrrent angina, (not treated w/ BB or CCB) isosorbide mononitrate (ISMN) is prescripted 2-3 times daily as immediate release tablets (also available as MR tablets or transdermal patches)
What is the communication advice for the use of Nitrates?
(Isosorbide mononitrate, Glyceryl trinitrate)
Nitrate to relieve chest pain and/or breathlessness
May develop short headache
Should use sublingual GTN BEFORE tasks that usually bring on their angina
May be good to sit and rest for 5 minutes to counteract hypotension.
Remove patch/dont take at nighttime to prevent tolerance (tachyphylaxis)/ in periods of inactivity.
What is the monitoring advice for the use of Nitrates?
Symptoms (e.g. chest pain, breathlessness)
When administering by IV infusion, blood pressure shoudl be monitored frequently.
What are the indications for Nitrofurantoin?
- Uncomplicated lower urinary tract infection (UTI), as a 1st line. Alternatives are trimethoprim or amoxicillin.
What is the mechanism of action of Nitrofurantoin?
Metabolised in bacterial cells to active metabolites which damage bacterial DNA and cause cell death.
Active against the gram -ve and +ve bacteria commonly causing UTIs.
What are the adverse effects of Nitrofurantoin?
GI Upset (nausea and diarrhoea)
Immediate and delayed hypersensitivity
Can turn urine dark yellow or brown
Rarely: pneumonitis and fibrosis, hepatiits and peripheral neuropathy, haemolytic anaemia of the newborn.
What are the warnings and contraindications for Nitrofurantoin?
Not in pregnant women 3rd trimester/towards term or for babies in 1st 3 months of life
Renal impariment
Not for long-term prevention of UTIs as increased risk of chronic adverse effects.
What is the dose and prescription advice for Nitrofurantoin?
PO - maximum urinary concentrations 2-4 hours after dosing
Treatment of acute UTI: 50-100 mg 6-hrly. Treatment duration depends on severity, usually 3 days in women and 7 days in men.
Prevention of recurrent UTIs, nightly dose 50-100 mg up to 6 months (requires monitoring)
Take with food to minimise GI side effects
What is the communication advice for Nitrofurantoin?
Complete course
Check for allergy
Urine may become dark
Watch out for pins and needs (neuropathy) or breathlessness (pneumonitis and fibrosis) for harmful side effects
What is the monitoring for Nitrofurantoin?
Efficacy: Treatment of UTI, resolution of symptoms or sterility of urine.
Report any symptoms of neuropathy or respiratory side effects
For what infections is Nitrofurantoin not suitable for and what are alternatives?
Not suitable for pyelonephritis or complicated UTIs, suitable is co-amoxiclav or gentamicin
What drugs are in the class NSAIDS?
Naproxen
Ibuprofen
Etoricoxib
What are the indications for treatment with NSAIDs?
(Naproxen, Ibuprofen, Etoricoxib)
- PNR for mild-to-moderate pain and/or paracetamol. Paracetamol preferred in those at risk of adverse effects.
- Regular treatment for pain related to inflammation particularly of the MSK system e.g. MSK injury, RA, osteoarthritis or gout
What is the mechanism of action of NSAIDS?
Inhibit sythesis of prostaglandins from arachidonic acid by inhibiting cyclooxygenase (COX).
(The theraputic effects are principally medicated by COX-2 inhibition and adverse effects by COX-1 inhibition. Selective COX-2 inhibitors e.g. etoricoxib are developed to try to reduce adverse effects)
What are the potential adverse effects of NSAIDs?
(Naproxen, Ibuprofen, Etoricoxib)
GI toxicity: Peptic ulcers
Renal impairment
Increased risk CV events: MI and stroke
(Different onces have different AE profiles)
Hypersensitivity reactions: bronchospasm, angioedema
Fluid retention: Can worsen hypertension and heart failure
What are the warnings and contraindications of NSAIDs?
CI: Severe renal impairment, heart failure, liver failure, known NSAID hypersneitivity
In peptic ulcer disease, GI bleeding, CVD, renal impariment - if unavoidable use the lowet effective dose for the shortest possible time.
What are the important interactions of NSAIDs?
(Naproxen, Ibuprofen, Etoricoxib)
Drugs inc risk GI ulceration: Aspirin, Corticosteroids
GI Bleeding: Anticoagulants, SSRIs, Venlafaxine, Warfarin
Renal impariment: ACE inhibitors, diuretics,
Reduce theraputic effects of antihypertensives and diuretics
What is the dose and prescription advice for NSAIDS?
(Naproxen, Ibuprofen, Etoricoxib)
PO, topical, suppositories, injectable
e.g. RA, naproxen 500 mg PO, 12 hrly
Regular treatment for at least 3 weeks is necessary before full anti-inflammatory effect is seen.
Acute pain: naproxen 250 mg PO, 6-8 hrly as needed
(Different tollerance and AE profile with different drugs)
Take with food to minimise GI upset
What is the communication advice for NSAIDS?
(Naproxen, Ibuprofen, Etoricoxib)
Anti-inflammatory drug to help pain, swelling and/or fever
Most common SFx is indigestion - stop and seek medical advice if this occurs
For acute pain, do not use > 10 days
Chronic use/renal impairment: Stop if become acutely unwell or dehydrated to reduce the risk of damage to the kidneys.
What is the monitoring advice for NSAIDs?
(Naproxen, Ibuprofen, Etoricoxib)
Efficacy: control of symptoms
Renal function monitored in those with existing renal impairment
What gastroprotection is required for use with NSAIDs?
(Naproxen, Ibuprofen, Etoricoxib)
Should be considered for all patients prescribed NSAIDS who are at increased risk of GI complications: Age > 65 years, previous peptic ulcer disease, comorbidities (e.g. diabetes), concurrent therapy with other drugs with GI sfx (esp, aspirin and prednisolone)
Use with PPI (Lansoprazole 15 mg OD)
What drugs are in the class Ocular lubricants?
Hypromellose
Carbomers
Liquid and white soft paraffin
What are the indications for Ocular lubricants?
(Hypromellose, Carbomers, Liquid and white soft paraffin)
1st line symptomatic treatment of dry eye conditions (including keratoconjunctivitis sicca and Sjogren’s syndrome, alongside environmental coping strategies and avoiding precipitants)
What is the mechanism of action of ocular lubricants?
(Hypromellose, Carbomers, Liquid and white soft paraffin)
Soothing effect and help protect the eye surfaces from abrasive damage.
Increasing thickness and duration but may cause blurred vision.
What are the potential adverse effects of ocular lubricants?
(Hypromellose, Carbomers, Liquid and white soft paraffin)
Mild stinging and temporary blurring of vision (increased with ointments)
May cause mild allergic reaction in some patients
(No warnings and ICs and no interactions)
What is the dose and prescription advice for Ocular lubricants?
(Hypromellose, Carbomers, Liquid and white soft paraffin)
Most can be purchased OTC (Sjoren’s needs supervision/medical intervention)
Liquid > Gel > Paraffin
Paraffin usually only at night due to blurring effect
What is the communication advice for ocular lubricants?
(Hypromellose, Carbomers, Liquid and white soft paraffin)
Artificial tears in the hope of improving dry eyes.
Can sting when applied, advice on how to apply
With continued use the previous abrasive damage may be repaired, they will probably need to take treatment indefinitely to reduce new damage.
What drugs are in the class Opioids, compound preparations?
Co-codamol
Co-dydramol
What are the indications for Opioids, compound preparations?
(Co-codamol, Co-dydramol)
1. Mild-to-moderate pain: as second-line agents when simple analgesics, such as paracetamol, are insufficent.
Second ‘rung’ if the WHO pain ladder.
What is the mechanism of action of Opioids, compound preparations?
(Co-codamol, co-dydramol)
Paracetamol: Weak inhibitor of cyclooxygenase (COX)
Opiods metabolised to morphine/morphine related metabolites - agonists of opioid u-receptors.
What are the adverse effects of Opioids, compound preparations?
(Co-codamol, co-dydramol)
Opioids: Nausea, consitpaiton and drowsiness
Paracetamol OD: hepatotoxicity
Opioid OD: Neurological and respiratory depression
What are the warnings and contraindications of Opioids, compound preparations?
(Co-codamol, Co-dydramol)
Significant respiratory depression
Reduced doses in real and hepatic impairment (opioid excretion)
Caution in the elderly
What are the interactions of Opioids, compound preparations?
(Co-codamol, Co-dydramol)
Not used with other sedating drugs: antipsychotics, benzodiazepines, tricyclic antidepressants.
(Close monitoring if combination required)
What is the dose and prescription advice for Opioids, compound preparations?
(Co-codamol, Co-dydramol)
PO
All tablets contain 500 mg of paracetamol and dose of opioid varies.
Opioid x mg/ Paracatamol x mg (Go for one with 1g paracetamol 6 hrly)
What should you also prescribe with the regular administration of an opioid?
A stimulant laxative, for example senna.
What should be communicated with the use of Opioids, compound preparations?
Painkiller which is a weaker version of morphine
To be taken at regular intervals
Side effects and laxitive if required
Avoid driving or operating heavy machinery if they become drowsy or confused whilst taking medication
What is the monitoring advice for Opioids, compound preparations?
(Co-codamol, Co-dydramol)
Efficacy: Pain relief
No special monitoring
What drus are in the class Opioids, strong?
Morpine
Oxycodone
What are the indications for Opioids, strong (4)?
(Morphine, Oxycodone)
- Rapid relief of acute severe pain (inc. post-operative and acute MI)
- Chronic pain: 3rd rung - when paracetamol, NSAIDs and weak opioids are insufficient
- Breathlessness in end-of-life care
- To relieve breathlessness and anxiety in acutre pulmonary odema with oxygen, furosemide and nitrates
What is the mechanism of action of strong opioids?
(Morphine, Oxycodone)
Activation of opioid u (mu) receptors in the CNS, reducing neuronal excitability and pain transmission.
By relieving pain, breathlessness and anxiety, opioids reduce sympathetic nervous system activity. Thus in MI and acute pulmonary oedema they reduce cardiac work and oxygen demand as well as symptoms.
What are the important adverse effects of Opioids, strong?
(Morphine, Oxycodone)
Respiratory depression by reducing respiratory drive
Euphoria and detachment and neurological depression
Nausea and vomitting (usually settles)
Pupillary constriction
Constipation
Itching, urticaria, vasodilation and sweating
Continued use: tolerance and dependence
If dependent: withdrawal reaction
What are the warnings and contraindications for Opioids, strong?
(Morphine, Oxycodone)
Liver and kidney elimination: reduced in hepatic failure and renal impairment
Elderly
Respiratory failure
Not in biliary colic
What are the important interactions of Opioids, strong?
(Morphine, Oxycodone)
Close monitoring if used with other sedating drugs: Antipsychotics, Benzodiazepines, Tricyclic antidepressants
What is the dose and prescription advice for Opioids, strong?
(Morphine, Oxycodone)
Acute severe pain (high-dependency): Morphine IV for rapid onset (2-10 mg)
(If general ward: IM and SC is prefered)
Chronic pain: PO e.g. Oramorph 5 mg PO 4 hourly
(When optimum dose found, converted to a modified release form e.g. MST Continus 15 mg 12 hrly - make sure equivalent)
Breakthrough analgesia: Prescribe immediate-release morphin at a dose of 1/6th total daily dose e.g. Oramorph 5 mg 2 hourly in as required section
What should be communicated to patients with the use of Opioids, strong?
(Morphine, Oxycodone)
Addiction not usually issue when used for pain relief
Dose may need to be increased due to tolerance
Take slow release tablets for ‘background pain’ then fast acting for ‘background pain’.
Nausea settles over a few days but can offer antiemetic Metoclopramide
For consitpation senna and hydration
Do not drive or operate heavy machinery if drowsy or confused
What is the monitoring advice for Opioids, strong?
(Morphine, Oxycodone)
Pain relief, respiratory and neurological depression.
What are the symptoms of strong opioid withdrawal?
Anxiety
Pain and breathlessness
Dilated pupils
Dry and cool skin with piloerection (Cold-turkey)
What drugs are in the weak opioids class?
Tramadol
Codeine
Dihydrocodeine
What are the indications for treatment with weak opioids?
(Tramadol, Codeine, Dihydrocodeine)
Mild-to-moderate pain, incuding post-operative pain, as 2nd line agents when simple analgesics such as paracetamol are inappropriate (2nd rung)
What is the mechanism of action of weak opioids?
(Tramadol, Codeine, Dihydrocodeine)
Metabolised in liver to morphine and related metabolites
Agonists of the u (mu) opioid receptors
(10% of caucasians may find less effective)
Tramadol is more moderate in strength
What are the potential adverse effects of weak opioids?
(Tramadol, Codeine, Dihydrocodeine)
Nausea
Constipation
Dizziness
Drowsiness
Neurological and Respiratory Depression
Codeine and Dihydrocodien MUST NOT be given IV as can have severe reaction similar to anapylaxis.
What are the warnings and contraindications for the use of weak opioids?
(Tramadol, Codeine, Dihydrocodeine)
Caution in: significant respiratory disease.
Reduced doses in renal and hepatic impairment and elderly
Tramadol - caution in epilepsy
What are the interactions for weak opioids?
(Tramadol, Codeine, Dihydrocodeine)
Ideally not used or strict monitoring with other sedating drugs:
Antipsychotics, Benzodiazepines, Tricyclic antidepressants
Tramadol not with drugs lowering the seizure threshold: SSRIs and tricyclic antidepressants
What is the dose and prescription advice for weak opioids?
(Tramadol, Codeine, Dihydrocodeine)
PO where possible
IM in operating theatre - DO NOT GIVE IV
Regular preferable to as-redquired
e.g. Codeine or dihydrocodeine 30 mg PO 4-ourly
Co-prescribe a stimulant laxitive such as Senna
What is the communication advice for Opioids, weak?
(Tramadol, Codeine, Dihydrocodeine)
Painkiller weaker mophine
Take at regular intervals
Laxitives for constipation
Avoid driving or operating heavy machinery if drowsy or confused.
How are weak opioids sometimes given post-operatively?
Anaesthetists sometimes give IM towards end
NOT IV CAUSES REACTION
May leave rede mark on lateral aspect of leg due to local reaction
What are the indications for treatment with Paracetamol?
- 1st line analegis for acute and chronic pain - 1st rung of pain ladder
- Antipyretic anc can reduce fever and shivering
What is the mechanism of action of Paracetamol?
Weak inhibitor of cyclooxygenase (COX) the enzyme involved in prostaglandin metabolism.
Increases pain threshold and reduces prostaglanding concentration.
(Weak anti-inflammatory)
What are the adverse effects of paracetamol?
Treatment doses: Safe
(Lack of COX-1 inhibition means doesn’t cause NSAID Sfx)
In overdose, causes hepatotoxicity (NAPQI accumulation cauing hepatocellular necrosis - can be treated with acetylcysteine)
What are the warnings and contraindications for Paracetamol?
Reduced in those at increased risk of liver toxicity
Chronic excessive alcohol use, malnutrition, blow body weight and severe hepatic impariment
What are the important interactions for Paracetamol?
Cytochrome P450 incudes increase rate of NAPQI producion and increase risk of liver toxicity in overdose
What is the dose and prescription advice for paracetamol?
PO, IV or rectal
0.5-1 g every 4-6 hours, maximum 4 g daily
Can be regular or as required (must state daily maximum dose)
What is the communication advice for paracetamol?
Aim of reducing or relieving pain, effects in 30 mins
Take 6 hourly if regular of 4-6 hourly if PRN
At review check if step-up is required
Overdose: blood tests INR, ALT to see if acetylcystine treatment is required.
What drugs should you look out for when prescribing paracetamol?
Co-codamol or Co-dydramol as this would mean they are already having paracetamol
What drugs are in the class Penicillins?
Benzylpenicillin
Phenoxymethylpenicillin
What are the indications for treatment with penicillins (3)?
(Benzylpenicillin, Phenoxymethylpenicillin)
- Strep infections including tonsillitis, pneumonia (with macrolide if severe), endocarditis and skin and soft tissue infections (added to flucloxaxillin if severe)
- Clostridal infection, e.g. tetanus
- Meningococcal infection, e.g. meningitis, septicaemia
What is the mechanism of action of Penicillins?
(Benzylpenicillin, Phenoxymethylpenicillin)
Weaken cell walls, causing cell swelling, lysis and death
Penicillins contain a B-lactam ring, which is responsible for antimucrobal activity. Bacteria producing B-lactamases are resistant to treatment with Penicillins.
What are the adverse effects of Penicillins?
(Benzylpenicillin, Phenoxymethylpenicillin)
Penicillin allergy: 1-10% people
Skin rash 7-10 days after exposure or 1-2 days after repeat exposure (dubacute IgG-mediated reaction) less commonly a life threatening (minutes to house) IgE anaphylactic reaction may occur: Hypotension, bronchial and laryngeal spasm/oedema and angioedema.
CNS toxicity can occurr where there are high doses or severe impairment.
What are the warnings and contraindications for Penicillins?
(Benzylpenicillin, Phenoxymethylpenicillin)
Reduced dose in renal impariment
CI: History of penicillin allergy
Penicillins Interactions
Increase methotrexate toxicity
What is the dose and prescription advice for penicillins?
(Benzylpenicillin, Phenoxymethylpenicillin)
Benzylpenicillin IM or IV only (severe infections)
Phenoxymethylpenicillin PO (less severe infections)
4-6 hourly
Include indication and duration of treatment in prescription
What is the communication advice for Penicillins?
Complete course
Check for allergy
What is the monitoring advice for penicillins?
(Benzylpenicillin, Phenoxymethylpenicillin)
Symptom reduction: Pyrexia, lung crackles
Blood markers: Falling C-reactive protein and WCC
What antibiotic should be used to treat a young person with a sore throat of unknown cause?
Phenoxymethylpenicillin
Amoxicillin when due to EBV can cause a rash which may lead to a lifetime of avoidance of penicillin.
What drugs are in the class Penicillins, antipseudomonal?
Piperacillin with Tazobactam e.g. Tazocin
What are the indications for treatment with Penicillins, antipseudomonal (4)?
(Piperacillin with Tazobactam e.g. Tazocin)
For severe infection, where there is a broad spectrum of potential causative pathogens inc: Pseudomonas aeruginosa, where antibiotic resistance is likely (hospital-aquired infection) or patients are immunocompromised.
- LRTI
- UTI
- Intra-abdominal sepsis
- Skin and soft tissue infection
What is the mechanism of action of Penicillins, antipseudomonal?
(Piperacillin with Tazobactam e.g. Tazocin)
Weaken cell walls, leading to cell swelling, lysis and death
Penicillins contain a B-lactam ring.
Addition of tazobactam (a B-lactamase inhibitor, canfers antimicrobilal activity against B-lactamase-producing bacteria e.g. Staph aureus, Gram-neg anaerobes, Pseudomonas aeruginosa
What are the adverse effects of penicillins, antipseudomonal?
(Piperacillin with Tazobactam e.g. Tazocin)
GI upset: nausea and diarrhoea
Antibiotic-resistant colitis (due to broad spectrim - overgrowth of C.diff)
Delayed or immediate hypersensitivity reactions
What are the warnings and contraindicaitons for the use of penicillins, antipseudomonal?
(Piperacillin with Tazobactam e.g. Tazocin)
Caution in at risk of C.diff
CI: History of penicillin allergy
Reduced in moderate-severe renal impariement
What are the important interactions for Penicillins, antipseudomonal?
(Piperacillin with Tazobactam e.g. Tazocin)
Reduce excretion of methotrexate increasing toxicity
Antipsuedomonal penicillins can enhance the anticoagulation effect of warfarin
What is the dose and prescription advice for penicillins, antipseudomonal?
(Piperacillin with Tazobactam e.g. Tazocin)
IV. 5-14 days. 4.5g containing 4 g piperacillin and 500 mg tazobactam 6-8 hourly .
(Include indication and duration in prescription)
Pweder diluted in water and sodium chloride + glucose
What is the communication advice for penicillins, antipseudomonal?
(Piperacillin with Tazobactam e.g. Tazocin)
Check for allergy and warning signs.
Advice will be in hosptial for a while (5-14 days) IV treatment
What drugs are in the class Penicillins, broad-spectrum?
Amoxicillin
Co-amoxiclav
What are the indications for threatment with Penicillins, broad-spectrum (4)?
(Amoxicillin, Co-amoxiclav)
- Empirical treatment of pneumonia, which may be cause by gram-positive (strep pneumonia) or gram-negative pathogens (haemophilus influenzae)
- Empirical treatment of UTI most likely caused by e.coli, can use Nitrofurantoin
- Combination treatment (co-amoxiclav) for hospital-aquired infection or intra-abdominal sepsis.
- As part of combination treatment for H/pylori-assocaited peptic ulcers
What is the mechanism of action of Penicillins, broad-spectrum?
(Amoxicillin, co-amoxiclav)
Weaken cell walls leading to cell, swelling lysis and death.
Penicillins contain a B-lactam ring, which is responsible for their antimicrobial activity.
(Co-amoxiclav contains clavulanic acid, which increases the spectrum of antimicrobial activity to include B-lacamase-producing bacteria such as Staph aureaus and gram-negativ anaerobes)
What are the adverse effects of Penicillins, broad-spectrum?
(Amoxicillin, co-amoxiclav)
GI Upset: Nausea and diarrhoea
Antibiotic-associated colitis: C.diff overgrowth (can lead to colonic perforation and/or death)
Penicillin allergy: Rash or anaphylaxis
Anaphylactic reaction: Hypotension, bronchospasm and angioedema
Cholestatic jaundice: co-amoxiclav
What are the warnings and contraindications for the use of Penicillins, broad-spectrum?
(Amoxicillin, Co-amoxiclav)
Caution in those at risk of C.diff infection
CI: Penicillin allergy
Reduced dose in severe renal impairment
What are the important interactions with Penicillins, broad-spectrum?
(Amoxicillin, Co-amoxiclav)
Increasee plasma concentration of Methotrexate
Enhance anti-coagulant effect of warfarin.
What is the dose and prescription advice for Penicillins, broad-spectrum?
(Amoxicillin, Co-amoxiclav)
Severe infection: Amoxicillin (high-dose 1g 8-hrly) IV should be switched to oral after 48hrs if clinically indicated and patient is improving.
Mild-to-moderate infection: PO lower dose amoxicillin (250-500 mg 8hrly) co-amoxiclav (co-amoxiclav 500/125 indicated amoxicillin/clavuanic acid)
(Include indication and dose of treatment)
What should be communicated to patients with the use of broad-spectrum antibiotics?
(Amoxicillin, Co-amoxiclav)
Oral: Complete prescribedcourse
Ceck for allergy
Warnings if allergy develops
What drugs are in the class Penicillins, penicillinase-resistant?
Flucloxacillin
What are the indications for treatment with Penicillins, penicillinase-resistant (3)?
(Flucloxacillin)
Staphylococcal infection:
- Skin and soft tissue infections such as cellulitis (in combination with benzylpenicillin for more severe infections)
- Osteomyelitis and septic arthritis
- Other infections, including endocarditis
What is the mechanism of action of Penicillins, penicillinase-resistant?
(Flucloxacillin)
Weaken cell walls, causing cell swelling, lysis and death.
Penicillins contain a B-lactam ring, which is responsible for antimicrobial activity.
Flucloxacillin has side chain which makes effective against B-lactamase producing staphylococci. (MRSA is resistant)
What are the adverse effects of Penicillins, penicillinase-resistant?
(Flucloxacillin)
GI upset: Nausea and vomitting
Allergy: Rash (delayed IgG) anaphylaxis (IgE)
Liver toxicity
CNS toxicity - high dose or severe renal impairment
What are the warnings and contraindications for Penicillins, penicillinase-resistant?
(Flucloxacillin)
Renal failure: reduced dose
CI: History of penicillin allergy
CI: Previous flucloxacillin realted hepatotoxicity
What is the dose and prescription advice for Penicillins, penicillinase-resistant?
(Flucloxacillin)
Flucloxacillin: High-dose IV for severe infection, where systemically unwell (up to 6 weeks may be required for osteomyelitis or endocarditis)
Less severe: PO 250-500 mg 6 hrly
(Include duration and indication in prescription)
What us the communication advice for Penicillins, penicillinase-resistant?
(Flucloxacillin)
Complete course
Check for allergy (note nausea may not be a reaction but instead a dose related adverse effect)
What are the indications for treatment with Phenytoin (2)?
- To control seizures in status epilepticus where benzodiazepines are ineffective
- Reduce frequency of generalised or focal seizures in epilepsy, though drugs with fewer adverse effects and interactions eg. Valproate, lamotrigine, levetriacetam are usually preferred.
What is the mechanism of action of Phenytoin?
Reduces neuronal excitability and electrical conductance among brain cells. Seems to bind to Na+ neuronal channels.
(Similar effect in cardiac Purkinje fibres may account for antiarrythmic and cardiotoxic effects)
What are the adverse effects of Phenytoin?
Long term: Change in appearance - skin coarsening, acne, hirsuitism and gum hypertrophy.
Neurological effects: Cerebellar toxicity (e.g. nystagmus, ataxia and discoordination) and impaired cognition or consciousness
Haematological disorders and osteomalacia by incuding folic acid and vitamin D metabolism
Hypersensitivity
Phenytoin toxicity: cardiovascular collapse and respiratory depression (can be fatal)
What are the warnings and contraindications for treatment with Phenytoin?
Hepatic impairment: Metabolised in liver with zero-order kinetics and with low theraputic index - dose reduced in hepatic impairment.
Teratogenic: Craniofacial deformity and reduced IQ, women with epilepsy planning pregnancy should take HIGH DOSE folic acid before conception
What are the important interactions for phenytoin?
Enzyme inducer so reduces plasma concentrations of drugs metabolised by P450 enzymes.
Concentration increased by cytochrome P450 inhibitors
Complex interactions with other antiepileptic drugs
Efficacy reduced by drugs lowering the seizure thereshold
What is the dose and prescription advice for Phenytoin?
Status epilepticus: IV phenytoin loading dose of 20mg/kg (max 2g) followed by maintenance dose of 100 mg 6-8 hourly.
Long term Oral phenytoin for chronic epilepsy is commenced at 150-300 mg daily, in 1-2 divided doses.
Phenytoin dosage is adjusted according to plasma concentations.
Treatment should not be stopped suddenly but should be withdrawn gradually to reduce risk of recurrence.
(Slow IV, flushed and need resus facilities)
What is the communication advice for Phenytoin?
To reduce frequency of seizures
Advice to take regularly with food and don’t miss doses
Seek medical advice for rashes, bruising or signs of infection
For women: discuss contraception and preganncy
DVLA - Don’t drive uness seizure free for 12 months and for 6 months after changing or stopping treatment
What is the monitoring advice for Phenytoin?
Plasma phenytoin concentrations are measure immediately before the next dose and should be 10-20 mg/L.
Make small changes in dose due to zero-order kinetics.
Efficacy: Compare seizure frequency before and after starting or changing treatment.
IV treatment: BP, ECG, Respiratory rate, oxygen saturations
What drugs are in the class Phosphodiesterase (type 5) inhibitors?
Sildenafil
What are the indications for Phosphodiesterase (type 5) inhibitors (2)?
(Sildenafil)
- Erectile dysfunction
- Primary pulmonary hypertension
What is the mechanism of action of Phosphodiesterase (type 5) inhibitors?
(Sildenafil)
Selective for PDE type 5 which is found predominantly in the smooth muscle of the corpus cavernosum of the penis and arteries of the lung.
For an erection to occur, sexual simulation is required. As PDE5 is responsible for the breakdown of cGMP, inhibition of this enzyme by sildenafil increases cGMP concentrations, improving penile blood flow and erection quality.
In primary pulmonary vasculature, sildenafil causes arterial vasodilatation by similar mechanisms so is used to treat primary pulmonary hypertension.
What are the potential adverse effects of Phosphodiesterase (type 5) inhibitors?
(Sildenafil)
Flushing, headache, dizziness, nasal congestion
Hypoension, tachycardia and palpitations
Small risk of vascular events: MI, stroke
Priapism (Urgent medical review)
Visual disorders (Urgent medical review)
What are the warnings and contraindications for Phosphodiesterase (type 5) inhibitors?
(Sildenafil)
Recent stroke or ACS
Significant CVD
Severe renal or hepatic impairment
What are the important interactions for Phosphodiesterase (type 5) inhibitors?
(Sildenafil)
Not with nitrates: can cause cardiovascular collapse: Nitrates or Nicorandil
Caution with a-blockers and CCBs - increased risk hypotension
Concentrations increased by cytochrome P450 inhibitors.
Do not take with amyl nitrate (poppers) as may cause collapse
What is the dose and prescription advice for Phosphodiesterase (type 5) inhibitors?
(Sildenafil)
Viagra: erectile dysfunction 50 mg PO, 1 day maximum
Revatio: primary pulmonary hypertension.
What should be communicated to patients with the use of Phosphodiesterase (type 5) inhibitors?
(Sildenafil)
Will help have and maintain an erection but will not work without sexual stimulation
Should be taken an hour befre sex to allow sufficient time for absorption
Seek medical advice if the erection does not subside within two hours after sexual activity has finished
Be aware of any eyesight changes
For who can Phosphodiesterase (type 5) inhibitors be prescribed on the NHS?
Only where erectile dysfunction is secondary to chronic disease or trauma or if causing significant psychological or social distress.
Now available without prescription.
What drugs are in the class Potassium?
Potassium Chloride
Potassium Bicarbonate
What are the indications for treatment with potassium?
(Potassium Chloride, Potassium Bicarbonate)
- Treatment and prevention of potassim depletion/hypokalaemia.
(Where this is caused by a loop or thiazide diuretic, addition of a potassium sparing diuretic is preferable.
IV potassium chloride is preferreed in the initial treatment of hypokalaemia that is severe (<2.5 mmol/L), symptomatic or causing arrythmias.
What is the mechanism of action of potassium?
(Potassium Chloride, Potassium Bicarbonate)
Causes of hypokalaemia: diarrhoea, vomiting, secondary hyperaldosteronism. - Supplement is treatment
Where caused by loop or thiazide diuretic, requires potassium-sparing diuretic or aldosterone antagonist.
Redistribtive hypokalaemia: total body potassium is normal but serum concentration is low because of distribution into cells (insulin or salbutamol)
MANAGEMENT ADDRESS UNDERLYING CAUSE
What are the adverse effects of treatment with potassium?
(Potassium Chloride, Potassium Bicarbonate)
Oral: Unpalatable and cause GI disturbance: nausea, vomiting, pain, diarrhoea, flatulence.
Modified release: GI obstruction, ulceration and bleeding
Overtreatment: Hyperkalaemia and resultant risk of arrhytmias.
What are the warnings and contraindications for treatment with potassium?
(Potassium Chloride, Potassium Bicarbonate)
Caution in renal impairment and avoided in severe renal impairment
What are the important interactions of potassium?
(Potassium Chloride, Potassium Bicarbonate)
Additive effect with IV potassium, aldosterone antagonists, potassium-sparing diuretics, ACE inhibitors and ARBs.
What is the dose and prescription advice for potassium?
(Potassium Chloride, Potassium Bicarbonate)
Treat if <2.5-3.5 depending on risk of arrythmias (inc. in digoxin)
Sando-K or Kay-Cee-L syrup
Dose adjusted to response
Dissolved in water, may be more palpable with food.
What is communicated to patients for treatment with Potassium?
(Potassium Chloride, Potassium Bicarbonate)
Low level of potassium blood could upset heart rhythm. Blood test monitoring will be required
SFx may be reduced if combined with meal or snack
Do not consume salt substitutes as these have high potassium concent and count interact with treatment.
What is the monitoring advice for treatment with potassium?
(Potassium Chloride, Potassium Bicarbonate)
Baseline: ECG to confirm the absence of hypokalaemia changes: IV over oral treatment.
Potassium concentration should be monitored during therapy.
What drugs are in the class Prostaglandin analogue eye drops?
Latanprost
Bimatoprost
What are the indications for treatment with Prostaglandin analogue eye drops?
(Latanoprost, Bimatoprost)
- 1st line agent to lower intraocular pressure in open-angle glaucoma and ocular hypertension. Usually prefered over topical B-blocker (the main alternative class) as they cause fewer systemic side effects.
What is the mechanism of action of Prostaglandin analogue eye drops?
(Latanoprost, Bimatoprost)
Ocular hypertension is a risk factor for open-angle glaucoma
Prostaglandin analogue eye drops reduce intraocular pressure by increasing outflow of aqueous humour via the uveoscleral pathway.
(Glaucoma is characterised by progressive optic nerve damage associated with visual field loss and eventually blindness, it is usually though not always associated with elevated intraocular pressure)
What are the potential adverse effects of Prostaglandin analogue eye drops?
(Latanoprost, Bimatoprost)
Blurred vision, conjunctival redening and ocular irritation and pain
May cause permanent ch.ange in eye colour
What are the warnings and contraindications for treatment with Prostaglandin analogue eye drops?
(Latanoprost, Bimatoprost)
Eyes in which the lens is absent or artificial
In patients with or at risk of iritis, uveitis or macular oedema
(Topical beta-blockers risk of bronchoconstrction)
What is the dose and prescription advice for Prostaglandin analogue eye drops?
(Latanoprost, Bimatoprost)
Specialist decision with ocular hypertension
Open-angle glaucoma all offered treatment with specialist involvement - usually Latanoprost 1 drop daily, in the evening.
What is communicated to patients with the use of Prostaglandin analogue eye drops?
(Latanoprost, Bimatoprost)
Aim of treatment is to reduce the risk of sight loss.
Advice how to administed
Explain the risk of eye colour change
Gently compress the medial canthus (nasal corner) of the eye for a minute after adminstration to reduce systemic absorption of the drug.
What drugs are in the class PPIs?
Lansoprozole
Omeprazole
Prantoprazole
What are the indications for treatment with PPIs?
(Lansoprazole, Omeprazole, Pantoprazole)
1st line for:
- Prevention and treatment of peptic ulcer disease, including NSAID-associated ulcers
- Symptomatic relief of dyspepsia and GORD
- Eradication of Helicobacter pylori infection, where they are used with antibiotics
What is the mechanism of action of PPIs?
(Lansoprazole, Omeprazole, Pantoprazole)
Reduce gastric acid secretion by irreversibly inhibiting H+/K+-ATPase in gastric parietal cells.
This is the proton pump responsible for secreting H+ and generating gastric acid.
(More complete action than H2-receptor antagonists)
What are the adverse effects of PPIs?
(Lansoprazole, Omeprazole, Pantoprazole)
GI disturbance and headache
May increase risk of C.diff in some people
Prolongued treatment: hypomagnesaemia (tetany and ventricular arrhythmia)
What are the warnings and contraindications for treatment with PPIs?
(Lansoprazole, Omeprazole, Pantoprazole)
PPIs may disguise symptoms of gastric cancer, so check red flags before and after treatment.
May increase risk of fracture, so caution in Osteoporosis
What are the important interactions for PPIs?
(Lansoprazole, Omeprazole, Pantoprazole)
May reduce antiplatelet effect of clopidogrel.
What is the dose and prescription advice for PPIs?
(Lansoprazole, Omeprazole, Pantoprazole)
PO or IV, dose on drug and indication.
Lowest possible for shortest period of time, take in morning.
What is the communication advice for PPIs?
(Lansoprazole, Omeprazole, Pantoprazole)
Hopefully reduce discomfort and help ulcers to heal.
Ensure clear on duration on therapy and how success will be judged.
Red flags: Weight loss, swallowing difficulty
What is the monitoring for PPIs?
(Lansoprazole, Omeprazole, Pantoprazole)
Symptomatic response
Healing of peptic ulcers judged by endoscopic examination/appearance.
If >1 year, check serum magnesium levels due to risk of hypomagnesaemia.
When investigating for H.pylori what should be done with PPI treatment?
Witheld for 2 weeks as increases the risk of a false negative result
What are the indications for treatment with Quinine Sulfate (2)?
- Nightime leg cramps (when disturb sleep and non-pharmacological methods have failed)
- Plasmodium falciparum malaria
What is the mechanism of action of Quinine Sulfate?
Reduces excitability of motor end plates, reducing frequency of muscle contraction - Leg cramps
Kills P.falciparum parasites in the blood - Malaria
What are the adverse effects of Quinine Sulfate?
Safe at recommended doses
Overdose: Tinitus, deafness, blindness, GI upset and hypersensitivity reactions.
Prolongued QT interval - arrythmias
Hypoglycaemia
What are the warnings and contraindications for treatment with Quinine Sulfate?
Caution: existing hearning or visual loss
Teratogenic: not in 1st trimester of pregnancy
Avoid in G6PD deficiency
What are the important interactions of Quinine Sulfate?
Other drugs prolonging the QT interval: amiodarone, antipsychotics, quinolones, macrolides and SSRIs.
What is the dose and prescription advice for Quinine Sulfate?
Leg cramps: 200-300 mg PO, at night.
Malaria: Higher doses, PO or IV (with doxycycline)
What is the communication advice for Quinine Sulfate?
Leg cramps: trial for 4 weeks.
Report: Hearning loss, visual disturbance and palpiations immediately (ears, eyes and heart)
What is the monitoring advice for Quinine Sulfate?
Review at 4-weeks and stop if no improvement.
Try to stop at 3-months due to risk of serious side effects.
What drugs are in the class Quinolones?
Ciprofloxacin
Moxifloxacin
Levofloxacin
What are the indications for treatment with Quinolones (4)?
(Ciprofloxacin, Moxifloxacin, Levofloxacin)
2nd and 3rd line for:
- UTIs
- Severe GI Infection
- LRTI infection
- Pseudomonas aeruginosa
What is the mechanism of action of Quinolones?
(Ciprofloxacin, Moxifloxacin, Levofloxacin)
Kill bacteria by inhibiting DNA synthesis.
Bacteria rapidly develop resistance to quinolones.
What are the adverse effects of Quinolones?
(Ciprofloxacin, Moxifloxacin, Levofloxacin)
GI Upset: nausea and diarrhoea (all Abx)
Immediate and delayed hypersensitivity reactions
Neurological effects: Lowering seizure threshold and hallucinations
Inflammation and rupture of muscle tendons
Quinolones: Prolong the QT interval - increase risk arrythmias
Promote C.diff infection
What are the warnings and contraindications for Quinolones?
(Ciprofloxacin, Moxifloxacin, Levofloxacin)
Caution in those at risk of seizures, children, QT prolongation.
What are the interactions of Quinolones?
(Ciprofloxacin, Moxifloxacin, Levofloxacin)
Multiple, check BNF.
What is the dose and prescription advice for Quinolones?
(Ciprofloxacin, Moxifloxacin, Levofloxacin)
PO if possible but IV is possible
12-24 hours
What is the communication advice for Quinolones?
(Ciprofloxacin, Moxifloxacin, Levofloxacin)
Complete course, check for allergy.
What conditions are Quinolones particularly effective against?
(Ciprofloxacin, Moxifloxacin, Levofloxacin)
Severe traveller’s diarrhoea: shigella, salmonella, campylobacter.
(Reserved for systemic involvement)
What drugs are in the class Statins?
Simvastatin
Atorvastatin
Pravastatin
Rosuvastatin
What are the indications of treatment with statins (3)?
(Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin)
- Primary prevention of cardiovascular disease: to prevent cardiovascular events in people over 40 years of age with a 10-year cardiovascular risk >20%
- Secondary prevention of cardiovascular disease: first line alongside lifestyle changes, to prevent further cardiovascular events in those who have evidence of cardiovascular disease
- Primary hyperlipidemia: 1st line in primary hypercholesterolemia, mixed dyslipedaemia and familial hypercholesterolemia.
What is the mechanism of action of statins?
(Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin)
Reduce serum cholesterol levels by inhibiting HMG CoA reductase. An enzyme involved in making cholesterol.
Slow the alterosclerotic proccess.
What are the adverse effects of Statins?
(Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin)
Headache and GI disturbances
Muscle: can cause aches, myopathy or (rare) rhabdomyolysis.
Liver: rise in liver enzymes (ALT), (rare) drug induced hepatitis.
What are the warnings and contraindications for the use of Statins?
(Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin)
Caution: Hepatic impariment
Dose reducedd in renal impairment
Avoided in pregnancy and breastfeeding
What are the important interactions for Statins?
(Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin)
Accumulation with cytochrome P450 inhibitors.
Amlodipine
What is the dose and prescription advice for statins?
(Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin)
PO, OD, e.g. 40 mg daily Simvastatin or 10 mg daily Atorvastatin
Taken in the evening
What is the communication advice for statins?
(Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin)
Medicine to lower cholesterol and reduce the risk of heart attack or stroke in the future.
Seek help if experience muscle symptoms
Blood tests in 3 and 12 months
Teep alcohol intake to a minimum and avoid grapefruit juice.
What is the monitoring advice for statins?
(Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin)
Primary prevention: lipid profilebefore treatment.
Secondary prevention: efficacy by serial lipid profiles to meet targets. Safety: liver enzymes ALT at 3 and 12 months. Creatinine kinase if muscle symptoms are reported.
What should be checked prior to starting treatment with statins?
Thyroid function as hypothyroidism is a reversible cause of hyperlipidaemia and should be corrected instead of statin treatment.
What drugs are in the class tetracyclines?
Doxycycline
Lymecycline
What are the indications for treatment with tetracyclines (4)?
(Doxycycline, Lymecycline)
- Acne vulgaris
2. LRTIs including: Infective COPD, Pneumonia and atypical pneumonia.
- Chlamydial infection including pelvic inflammatory disease (PID)
4. Typhoid, anthrax, malaria, Lyme disease
What is the mechanism of tetracyclines?
(Doxycycline, Lymecycline)
Inhibit bacterial protein synthesis - bacteriostatic and kills bacteria.
What are the adverse effects of tetracyclines?
(Doxycycline, Lymecycline)
GI upset: Nausea, vomtting and diarrhoea
Hypersensitivity reactions Immediate and delayed
Specific to tetracyclines: Oesophageal irritation, ulceration and dysphagia, photosensitivity, discolouration or hypoplasia of tooth enamel. Intracranial hypertension.
What are the warnings and contraindications for treatment with tetracyclines?
(Doxycycline, Lymecycline)
Bind to teeth and bones during foetal development and childhood: Pregnancy, breastfeeding, Children <12
Renal impairment
What are the interactions with tetracyclines?
(Doxycycline, Lymecycline)
Enhance anticoagulant effect of warfarin (many Abx can)
What is the dose and prescription advice for tetracyclines?
(Doxycycline, Lymecycline)
PO Only
Vaires between drugs
Duration depending on indication
Include indication and duration on prescription
(With water whilst upright as can otherwise cause ulceration of the oesophagus)
Take with food as can cause nausea and vomitting if not but not with dairy products as can interact with them
What is the communication advice for tetracyclines?
(Doxycycline, Lymecycline)
Complete course
Check for allergy
What is the monitoring advice for Tetracyclines?
(Doxycycline, Lymecycline)
Resoution of infection and blood marers (reduced inflammatory markers)
What drugs are in the class Thyroid hormones?
(Levothyroxine, Liothyronine)
What are the indications for treatment with Thyroid hormones?
(Levothyroxine, Liothyronine)
- Primary hypothyroidism
- Hypothyroidism secondary to hypopituitarism
What is the mechanism of action of Thyroid hormones?
(Levothyroxine, Liothyronine)
The thyroid gland produces thyroxine (T4) which is converted to the active triiodothyronine (T3) in target tissues.
Thyroid hormones regulate metabolism and growth.
Hypothyroidism is treated by long-term replacement of thyroid hormones, most usually as levothyroxine (synthertic T4) or liothyronin (synthetic T3).
Liothyronine is used for emergency treatment of severe or acute hypothyroidism.
What are the adverse effects of thyroid hormones?
(Levothyroxine, Liothyronine)
Excessive doses: hyperthyroidism - GI (diarrhoea, vomiting, weight loss), cardiac (palpitations, arrhythmias, angina) and neurological (e.g. tremor, restlessness, insomnia), manifestations.
What are the warnings and contraindications of treatment with thyroid hormones?
(Levothyroxine, Liothyronine)
Increase heart rate and metabolism: can prescipitate cardiac ischaemia in people with coronary artery disease.
In hypopituitarism - corticosteroid therapy must be initiated before thyroid hormone replacement to avoid precipitating an addisonian crisis.
What are the important interactions of thyroid hormones?
(Levothyroxine, Liothyronine)
Multiple
Cytochrome P450 inducers can decrease dose
Can alter insulin and glycaemic requirements in diabetes
What is the dose and prescription advice for Thyroid Hormones?
(Levothyroxine, Liothyronine)
Levothyroxine PO only (25-100 micrograms)
Write MICROGRAMS
Liothyronine IV: for emergencies only
What is the communication advice for Thyroid hormones?
(Levothyroxine, Liothyronine)
Replacing a natural hormone that their body has stopped making - may take months to feel back to normal
Lifelong treatment
Look out for signs of too much: hyperthyroidism
Don’t take with calcium and iron supplements
What is the monitoring advice for thyroid hormones?
(Levothyroxine, Liothyronine)
Return patients to euthoroid state
Thyroid function tests measured at 3 months after starting treatment or change in dose
In primary hypothyroidism, thyroid stimulating hormone (TSH) is the main guide to dosing. It is elevated due to loss of negative feedback of T4 on the pituitary. With adequate levothyroxine replacement, TSH should return to normal or low-normal concentratons. Stable patients should have annual clinical review and thyroid function tests.
What drugs are in the class Trimethoprim?
(Trimethoprim, Co-trimoxazole)
What are the indications for treatment with Trimethoprim (2)?
(Trimethoprim, Co-trimoxazole)
- Trimethoprim 1st choice for uncomplicated UTIs (or nitrofurantoin and amoxicillin)
- Co-trimoxazole is used for the treatment of prevention of pneumocystis pneumonia in people with immunosuppression e.g. due to HIV infection
What is the mechansim of action of trimethoprim?
(Trimethoprim, Co-trimoxazole)
Inhibits bacterial folate synthesis
(There is widespread bacterial resistance limiting clinical utility)
What are the potential adverse effects of Trimethoprim?
(Trimethoprim, Co-trimoxazole)
GI Upset (Nausea, vomiting, sore mouth)
Skin rash
Hypersensitivity
A folate antagonist so can impair haematopoiesis, causing haematoloical disorders - megaloblastic anaemia, lecopenia, throbocytopenia.
Can cause hyperkalaemia and elevation of plasma creatinine concentrations.
What are the warnings and contraindications for the use of Trimethoprim?
(Trimethoprim, Co-trimoxazole)
CI 1st trimester of pregnancy as folate antagonist
Caution: folate deficiency
Renal impairment
Reduced: Neonates, elderly and HIV infection
What are the important interactions of Trimethoprim?
(Trimethoprim, Co-trimoxazole)
Can cause hyperkalaemia and more likely when used with potassium elevating drugs (aldosterone antagonists, ACE inhibitors, ARBs)
Folate antagonists: Methotrezatte and increase risk of adverse haematological effects.
Can enhance anticoagulation effect of arfrin by killing normal gut flora synthesising vitamin K
What is the dose and prescription advice for Trimethoprim?
(Trimethoprim, Co-trimoxazole)
PO Only 200 mg 12 hourly
Otherwise variable by indication: check BNF.
Co-trimoxazole is suitable for IV and PO administration
What monitoring is there for Trimethoprim?
(Trimethoprim, Co-trimoxazole)
Acute infection: resolution of symptoms, signs and investigations (urine culture in some cases)
Long-term treatment: FBC monitoring may aid early detection and treatment of haematological disodders.
What can Trimethoprim do to serum creatinin?
Can lead to a small, reversible risk in serum creatinine concentraton. eGFR remains the same. Less effective for treatment of UTI in renal impairment though.
What drugs are in the class Valproate?
(Sodium Valproate, Valproic Acid)
What are the indications for treatment with Valproate?
(Sodium Valproate, Valproic Acid)
- Epilepsy 1st choice for control of generalised or abscence seizures and option for focal seizures
- Bipolar disorder acute treatment of manic episodes and prophylaxis against recurrence.
What is the mechanism of action of Valproate?
