Therapeutics Flashcards
What are the 3 features of opiate overdose?
Miosis
Respiratory depression
Coma
Nausea and vomitting,Tinnitus, Deafness, Sweating and
Hyperventilation are the 5 features of __________ overdose?
Salicylate (aspirin)
Mydriasis, Hyperthermia, Tachycardia, Arrhythmia
and Agiation are the 5 features of ___________ overdose?
Ecstacy/ cocaine
What is the drink driving limit for alcohol content (blood and breath tests)?
Blood- 80mg/ 100ml
Breath- 35mg/100ml
What is the recommended paracetamol doseage?
2 x 500mg tablet, every 4-6 hours.
1 tablet if <50kg
What is the recommended Ibuprofen doseage?
1 x 400mg tablet, 4 times per day
What is the recommended Diclofenac doseage?
1 x 50mg tablet, 3 times per day
What is “neuropathic” pain?
Pain generated ectopically, often in the absence of noxious events, by pathological processes in the nervous system
What is “psychogenic” pain?
Pain with no apparent organic basis
What is the recommended tramadol doseage?
50-100mg every 4 hours
Which drugs should be avoided in renal impairment? (MANPLN)
Metformin, Aminoglycosides (Gentamicin-nephrotoxic), Nitrofurantoin, Potassium sparing diuretics, Lithium, NSAIDs (exacerbate oedema)
Which drugs should be avoided in hepatic impairment? (NWSSD)
NSAIDS and steroids -> fluid overload
Sedatives and diuretics -> hepatic encepalopathy
Warfarin -> Reduced clotting
Which AEDs cause weight gain as a side effect?
Sodium valproate, Gabapentin
Which AEDs cause weight loss as a side effect?
Topiramate
Which AED causes behavioural changes as a side effect?
Leveteracitam
What drug is the antedote to paracetamol overdose?
N-acetylcysteine (NAC) which detoxifies NAPQUI
What is used for stimulant overdose?
Diazepam 10mg IV
What is used for sedative overdose?
Naloxone IV/IM (opiate receptor antagonist)
What drugs are examples of dopamine agonists?
Bromocryptine/ Cabergoline- used in prolactinoma
Pramipexole/ Rapinirole- used in Parkinsons
Which drugs should be avoided in children?
Chloramphenicol
Aspirin
Tetracyclines
Why should tetracyclines e g. Doxycyline be avoided in children?
Leads to discoloured teeth and bone issues
Which drugs should be avoided in the 1st Trimester of pregnancy? (ACLQRSTW)
A- Androgens C- Cytotoxics L- Lithium Q- Quinolones eg. Ciprofloxacin, Levofloxacin R- Retinoids eg Vitamin A S- Sodium valproate T- Thalidomide W- Warfarin
Which drugs should be avoided in the 2nd Trimester of pregnancy? (AABSTON)
A- ACEIs/ ARBS A- Aminoglycosides eg Gentamicin B- Benzodiazepines S- Sulfonamides T- Tetracyclines eg. Doxycycline O- Opiates N- NSAIDs
Which drugs should be avoided in breastfeeding? (AABSRRL)
A- Antithyroid drugs A- Amiodarone B- Benzodiazepines S- Sulfonamides S- Statins R- Radioactive iodine L- Lithium
How are pharmacokinetics affected in pregnancy?
Increased IM and Inhaled absorption
Increased fat, increased plasma volume, increased volume of distribution = Maternal drug concentrations are often lower; doses may need to be increased
How should NAC be given for paracetamol overdose?
Use 3 bags IV over 21 hours
Which drugs are examples of stimulants?
Cocaine, MDMA, Amphetamines, Mephedrone
Which drugs are examples of hallucinogens?
LSD, Magic mushrooms, synthetic tryptamines
Which drugs are examples of sedatives?
Alcohol, opiates
What are the 4 main classes of drugs for depression? Give examples of drugs in each class.
- Tricyclic antidepressants- Amitryptaline, Imipramine
- Selective Serotonin Reuptake Inhibitors- Fluoxetine, Sertraline, Citalopram
- Serotonin and Norepinephrine Reuptake Inhibitors- Duloxetine, Venlaflaxine
- Monoamine Oxidase Inhibitors- Phenelzine
Give 4 examples of opiod drugs.
Morphine Codeine Oxycodone Fentanyl Tramodol
What are the main classes of non-opiod analgesics?
- Paracetamol
- Non steroidal anti-inflammatory drugs- Aspirin, Ibuprofen, Naproxen
- Antidepressants: Amtryptaline (TCA) or Duloxetine (SNRI)
- Anticonvulsants- Gabapentin or pregabalin
How does the drug morphine work?
Binds to opiod receptor (Mu) which is a G protein coupled receptor:
- inhibits calcium entry
-inhibits release of neurotransmitters
-enhances outward potassium movement
-inhibits adenylate cyclase from converting ATP-> cAMP
THIS RESULTS IN HYPERPOLARISATION, so that downwards signalling of pain doesn’t happen.
Name some common side effects of morphine.
Respiratory depression Euphoria Low blood pressure Constipation Hypogonadism
How does paracetamol work?
Inhibits production of prostaglandin by inhibiting the COX1-3 enzymes.
What are some of the common side effects of paracetamol?
Allergy
Overdose can lead to hepatotoxicity
Name some NSAIDs and give their mechanism of action.
Ibuprofen, Naproxen and Aspirin.
Inhibit production of prostaglandin by inhibiting the COX 1 and 2 enzymes. They also have anti-inflammatory and anti-platelet effects.
What are some common TCAs and their side effects?
Amitryptaline, Imipramine.
Side effects: Dry mouth, constipation, reduction in urine output, and cardiotoxicity.
What are some common SSRIs and their side effects?
Fluoxetine
Citalopram
Sertraline
Side effects: Dry mouth, bleeding risk
What are the main classes of drugs used in Parkinson’s?
- Levo-dopa
- Dopamine agonists: Pramipexole, Rapinirole
- Monoamine Oxidase B inhibitors: Selegiline, Rasagiline
- Catechol-o-methyl transferase inhibitors: Entacapone, Tolcapone
Name some side effects of Levo-dopa?
Hypotension
Dyskinesia
Nausea/ vomitting
Effectiveness decreases over time
Name some side effects of dopamine agonists?
Hypotension
Hallucinations
Addictive traits
Give examples of the two classes of anti-psychotic drugs.
Typical/ 1st generation: Chlorpromazine, Haloperidol
Atypical/ 2nd generation: Clozapine, Rispirodone
How do the first generation anti-psychotics work?
D2 receptor antagonists, so decrease the positive symptoms of schizophrenia. Side effects are related to reduction of dopamine in the nigro-striatal pathway= extra-pyramidal side effects
How do the second generation anti-psychotics work?
Act on serotonin, norepinephrine and dopamine. Avoids Parkinson’s like effects of typical anti-psychotics.
These have fewer neuromuscular and sexual side effects, but side effects do include weight gain, hyperprolactinaemia and blurred vision.
What is the mechanism of action of sodium valproate?
Blocks sodium channels. It also increase levels of the inhibitory neurotransmitter GABA in the brain.
__________ is the ability of a drug receptor complex to produce a maximal functional response
Efficacy
What are the 2 types of adverse drug reactions?
Type A reactions: dose dependent, predictable based on the pharmacology of the drug
Type B reactions: idiosyncratic and not preditcable based on the pharmacology
How is drug metabolism and distribution different in elderly patients?
Decreased 1st pass metabolism = Increased bioavailability
Increased fat so lipid soluble drugs accumulate
Decreased total body water
Decreased plasma protein conc
What are the 3 steps of the WHO pain ladder?
Step 1: Non opiod eg Paracetamol
Step 2: Weak opiod eg. Codeine and non opiod
Step 3: Strong opiod eg. Morphine and non opiod
Which are the older generation of AEDS?
Sodium valproate
Carbamazepine
Phenytoin
Phenobarbital
Which are the newer generation of AEDs?
Topiramate
Levetiracetam
Lamotrigine
Gabapentin and pregabalin
Which AEDs work by inhibiting Na channels?
Sodium valproate Carbamazepine Phenytoin Topiramate Lamotrigine
If a patient has a paracetamol concentration of __________mg/kg they are at risk of possible liver damage.
150 mg/kg
Which drug is given in Thiamine (Vitamin B1) deficiency?
Pabrinex
What are the effects of alcohol on GABA amd NMDA?
Increases GABA (inhibitory NT) Antagonises NMDA (excitatory NT)
What is used for Benzodiazepine overdoses?
Flumazenil
Which drugs are 1st line for Hypertension in patients aged <55years?
ACEIs/ ARBS
Which drugs are 1st line for Hypertension in patients aged >55years/ black afro Carribean?
CCBs
What are the main side effects of CCBs (dihydropyridines)?
Ankle swelling
Acid reflux
What are the 2 main types of CCB?
Dihydropyridines eg. Amlodipine (cause vasodilation)
Non-dihydropyridines eg. Diltiazem (act on heart and blood vessles)
Give an example of a Thiazide diuretic and its MOA.
Bendroflumethiazide
Acts in the DCT to block Na/Cl cotransport
What are the main side effects of Bendroflumethiazide (thiazide diuretic)?
Gout
Erectile dysfunction
Electrolyte disturbance
Hyperglycaemia
Give examples of a thiazide like diuretic.
Indipamide
How do loop diuretics work? When are they used?
Inhibit the NKCC2 cotransporter in the Loop of Henle.
Not in hypertension, more for heart failure, renal failure, ascites and pulmonary oedema.
What are common side effects of loop diuretics?
Hypokalaemia
Polyuria
Hypovolaemia
Give an example of a potassium sparing (aldosterone antagonist) diuretic and its MOA?
Spironalactone
Antatonises aldosterone, so blocks sodium reabsorption and potassium excretion.
What are common side effects of potassium sparing (aldosterone antagonist) diuretics?
Hyperkalaemia
Gynaecomastia
What is the starting dose of Ramipril?
2.5mg
Give an example of an alpha blocker used in 4th line hypertension treatment? What is a common side effect?
Doxazosin
Postural hypotension
What is the effect of B1 receptor binding?
Increased cardiac rate and force
cardioselective
What is the effect of B2 receptor binding?
Vasodilation, bronchodilation, muscle tremor
non-cardioselective
Give examples of cardioselective Beta blockers?
Bisoprolol
Atenolol
Give an example of a non-cardioselective Beta blocker?
Propanolol
What are the side effects of Beta blockers?
Cold extremities
Bradycardia
Erectile dysfunction
Hypoglycaemia
Which drug is used for orthostatic hypotension?
Fludrocortisone
Which drugs can be used for heart failure with reduced ejection fraction (systolic)?
- Diuretics eg. Potassium sparing- Spironalactone
- ACEI/ ARB
- B blockers eg. Bisoprolol, Carvedilol (but can worsen heart failure initially)
- Other diuretics…. loop, thiazide. Digoxin- increases force of contraction. Hydralyzine and nitrates.
What are the 4 classes of anti-arrhythmic drugs?
Class 1- Block Na channels- eg. Flecainide, Phenytoin
Class 2- Beta blockers
Class 3-Prolong the action potential eg. Amiodarone
Class 4- CCBs
Which drug is used in SVT?
Adenosine IV via a large bore cannula if vagal manouevres are unsuccessful
Briefly blocks transmission through the AV node, resulting in restoration of normal sinus rhythm
How is AF normally treated (which drug classes)?
Anticoagulants
AND
Rate control (B blockers, CCBs, Digoxin) OR Rhythm control (Amiodarone, Flecainide)
What is CHADS VASc?
Used in patients with AF to consider their risk of stroke: C- CCF H- Hypertension A- Age > 75 D- Diabetes S- Previous stroke/ TIA
V-Vascular disease
A- Age >65
Sc- Female
What is the HAS BLED score?
Used to estimate the risk of a major bleed for patients on anticoagulation:
H- Hypertension
A- Abnormal liver or renal function
S- Stroke
B- Bleeding
L- Labile (changing) INRs
E- Elderly >65 years
D- Drugs/ alcohol
What is Flecainide used for?
AF
WPW
Which drugs INHIBIT warfarin breakdown (so Increase INR)?
Cranberry Juice
Clarithromyin
Ciprofloxacin
Metronidazole
Which drugs INCREASE warfarin breakdown (so DECREASE INR)?
Vitamin K
St Johns Wort
Rifampicin
Carbamazepine
How do Apixaban and Rivoroxaban work?
Direct inhibition of Factor Xa
How does Dabigatran work?
Direct inhibition of thrombin
__________ can NOT be given for anticoagulating patients with metalic heart valves.
DOACs
Which drugs can be used for smoking cessation?
Buproprion- licenced for depression and anxiety. Contraindicated in seizures.
Varenicline- nicotine receptor partial agonist
What is the role of Orlistat?
Reduces fat absorption from diet, used in Obesity.
Side effects are steathorrhoea and faecal urgency
How do statins work?
They are HMG CoA Reductase inhibitors- reduce LDL cholesterol
What is a key side effect of statins?
Increased risk of developing diabetes
Ezetimibe is an alternative to ___________ and blocks NPC1L1 transport in the duodenum.
Statins
What drug classes can be used as alternatives to statins?
Ezetimibe
PCSK9 Inhibitors
Fibrates
Which drugs can be used in STABLE angina?
- Rate limiting drugs: Beta blockers, CCBs, Ivabradine
- Nitrates eg. Isosorbide mononitrate
- Nicorandil
Which drugs are used for ACS?
(MONA)
1. Morphine IV 5-10mg and Anti-emetic IV Metoclopramide 10mg IV
- Oxygen to maintain sats
- GTN sublingual spray
- Aspirin 300mg loading. Clopidogrel loading dose. LMWH eg. Enoxaparin 2mg/kg BD
Which drugs are used for thrombolysis?
Alteplase (a tissue plasminogen activator)
Clopidogrel is a prodrug, and requires conversion by which enzymes?
Cytochrome p450
How is asthma treated?
(Use SABA eg. Salbutamol, Terbutaline as required)
Step 1: Low dose ICS eg. Beclometasone, Fluticasone
Step 2: Add LABA eg. Salmeterol
Step 3: Increase the ICS dose and add SR theophyline, or Leukotriene receptor antagonist eg. Monteleukast
Step 4: Oral steroids
Give examples of SABAs and their MOA and side effects.
SABA- Salbutamol. Terbutaline
Treat bronchospasms, to be used as necessary
Side effects: Tremor, tachycardia, HYPOkalaemia
Give examples of ICS and their MOA and side effects.
ICS: Beclometasone, Fluticasone, Budesonide
Preventatory; anti inflammatory, decrease oedema and inhibit leukocyte infiltration, used 2x daily (eg. 800mg beclometasone, 2 puffs twice per day)
Side effects: Oral thrush, oesteoporosis, growth suppression in children
Give examples of LABAs
Salmeterol, Formoterol
Should always be used with ICS
Give an example of a Leukotriene Receptor Antagonist and its side effects.
Monteleukast (oral)
Antiinflammatory and bronchodilation
Side effects: GI upset, hypersensitivity
Give an example of a Xanthene Derivative and reasons why its use is limited.
Slow Release oral theophylline
HAS A NARROW THERAPEUTIC INDEX SO USE IS LIMITED, stopping smoking alters drug levels, used by specialists only.
What are the differential diagnoses for asthma?
COPD
GORD
Bronchiectasis
What is acute severe asthma?
- Unable to complete sentence in one breath
- Hr >110bpm
- RR > 25
- PEFR <50% predicted
How is acute severe asthma treated?
- Oxygen
- Salbutamol Nebuliser driven via oxygen
- Prednisolone PO or Hydrocortisone IV
- Ipratropium bromide (SAMA) neb if poor response
How is COPD managed?
Initially SABA/SAMA (ipatropium)
If no improvement:
If FEV1 >50% predicted: Add on LABA or LAMA
If FEV1 <50% predicted: Add on LABA and ICS or LAMA
What size should inhaler particles be?
2-5um
What are the side effects of alpha blockers used for BPH?
Drowsiness Depression Hypotension Dry mouth Extra pyramidal signs Ejaculatory failure
Which drugs can be used in BPH?
- Alpha blockers eg. Doxazosin, Tamsulosin- decrease smooth muscle tone
- 5aplha reductase inhibitors eg. Finasteride- decrease conversion of testosterone to Dihydrotestosterone
Which diuretics work on the DCT?
Thiazide diuretics eg. Bendroflumethiazide
Thiazide like diuretics eg. Indapamide
Which diuretics work on the collecting duct?
Potassium sparing eg. Spironalactone
Which diuretics work on the PCT?
Osmotic diuretics eg. Mannitol
Carbonic anhydrase inhibitors eg. Acetazolamide
Which class of Parkinso’s medications interact with sinus medications?
MAOB inhibitors (Rasagiline, Selegiline)
Which antibiotics are used for bacterial pneumonia?
- Coamoxiclav/ Amoxicyclin
- Macrolides (Clarithromycin/ Erythromycin)
- Tetracyclines (Doxycycline)
Which antibiotics are used for Strep pharyngitis?
Phenoxymethylpenicillin
If allergic to penicillin:
Clarithromycin/ Erythromycin
Which antibiotics are used for pyelonephritis?
Cephalosporins (Cefalexin)
Amoxicillin/ Coamoxiclav
Trimethoprim
Which antibiotics are used for gonorrhoea?
Ceftriaxone