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
