Phase II Flashcards
Antacids
Aluminium & magnesium hydroxide/calcium carbonate
MoA - Gastric acid neutralisation
Indication - Dyspepsia, heartburn
Adverse effects - Nausea
Aluminium & magnesium hydroxide/calcium carbonate
Antacids
MoA - Gastric acid neutralisation
Indication - Dyspepsia, heartburn
Adverse effects - Nausea
What would you prescribe for dyspepsia or heartburn?
Antacids
Aluminium & magnesium hydroxide/calcium carbonate
MoA - Gastric acid neutralisation
Adverse effects - Nausea
Antacids + alginates
Sodium alginate with sodium bicarbonate
MoA - Gastric acid neutralisation
Indication - Gastric reflux
Adverse effects - Abdominal distension
What would you prescribe for gastric reflux?
Antacids + Alginates (sodium alginate with sodium bicarbonate)
or
PPIs (omeprazole, lansoprazole)
H2-receptor antagonists
Ranitidine, Cimetidine
MoA - Blockade of gastric H2 histamine receptors
Indication - Stomach ulcers
Adverse effects - Dizziness
Ranitidine, cimetidine
H2-receptor antagonists
MoA - Blockade of gastric H2 histamine receptors
Indication - Stomach ulcers
Adverse effects - Dizziness
What would you prescribe for stomach ulcers?
H2-receptor antagonists (ranitidine, cimetidine)
or
PPIs (lansoprazole, omeprazole)
PPIs
Omeprazole, Lansoprazole
MoA - Blockade of stomach acid transporters
Indication - Stomach & duodenal ulcers, gastric reflux
Adverse effects - Headache, diarrhoea
Interactions - Warfarin
Pancreatic enzymes
Pancreatin
MoA - Restoration of pancreatic enzymes
Indication - Pancreatic insufficiency - Cystic fibrosis, pancreatitis
What would you prescribe for pancreatic insufficiency (ie. in cystic fibrosis or pancreatitis)?
Pancreatin
Bulk laxatives
Methylcellulose, isphagula husk
MoA - Water absorption in intestinal lumen to bulk stools
Indication - Constipation
Adverse effects/Interactions - Rare
Methylcellulose, isphagula husk
Bulk laxatives
MoA - Water absorption in intestinal lumen to bulk stools
Indication - Constipation
Adverse effects/Interactions - Rare
Faecal softener
Docusate, arachis oil
MoA - Stimulates water and electrolyte secretion into intestinal lumen
Indication - Constipation
Adverse effects/interactions - rare
Docusate, arachis oil
Faecal softener
MoA - Stimulates water and electrolyte secretion into intestinal lumen
Indication - Constipation
Adverse effects/interactions - rare
Osmotic laxatives
Macrogol (PEG), lactulose, magnesium sulphate, magnesium hydroxide
MoA - Water retention in intestinal lumen
Indication - Constipation
Adverse effects - Stomach cramps
Interactions - Antiepileptics
Macrogol (PEG), lactulose, magnesium sulphate, magnesium hydroxide
Osmotic laxatives
MoA - Water retention in intestinal lumen
Indication - Constipation
Adverse effects - Stomach cramps
Interactions - Antiepileptics
Stimulant laxatives
Bisacodyl, Senna
MoA - Increase intestinal motility
Indication - Constipation
Adverse effects - Nausea
Opioid anti-motility agents
Loperamide, codeine
MoA - Agonist for µ-opioid receptors in myenteric plexus. Blocks intestinal muscarinic receptors
Indication - Diarrhoea
Adverse effects/interactions - Rare
Loperamide, codeine
Opioid anti-motility agents
MoA - Agonist for µ-opioid receptors in myenteric plexus. Blocks intestinal muscarinic receptors
Indication - Diarrhoea
Adverse effects/interactions - Rare
Carbonic anhydrase inhibitor
Acetazolamide
MoA - Reduces aqueous humour volume
Indication: Intra-ocular pressure - open & acute closed angle glaucoma
Adverse effects - Paraesthesia
Acetazolamide
Carbonic anhydrase inhibitor
MoA - Reduces aqueous humour volume
Indication: Intra-ocular pressure - open & acute closed angle glaucoma
Adverse effects - Paraesthesia
Osmotic diuretics
Mannitol
MoA - Elevates plasma osmolarity
Indication - Cerebral oedema, intra-ocular pressure
Adverse effects - Hypotension
Mannitol
Osmotic diuretics
MoA - Elevates plasma osmolarity
Indication - Cerebral oedema, intra-ocular pressure
Adverse effects - Hypotension
Loop diuretics
Furosemide
MoA - Inhibits Na+/K+/2Cl- transporter in loop of Henle
Indication - Left ventricular heart failure, oedema
Adverse effects - Nausea, dizziness
Interactions - NSAIDs, ACE inhibitors
Furosemide
Loop diuretic
MoA - Inhibits Na+/K+/2Cl- transporter in loop of Henle
Indication - Left ventricular heart failure, oedema
Adverse effects - Nausea, dizziness
Interactions - NSAIDs, ACE inhibitors
Thiazides
Indapamide, Bendroflumethiazide,
Chlorthalidone
Hydrochlorothiazide
MoA - Decreases sodium and chloride reabsorption
Indication - Hypertension
Adverse effects - Electrolyte imbalance, exacerbation or precipitation of gout
Interactions - NSAIDs, digoxin
Indapamide, Bendroflumethiazide,
Chlorthalidone
Hydrochlorothiazide
Thiazides
MoA - Decreases sodium and chloride reabsorption
Indication - Hypertension
Adverse effects - Electrolyte imbalance, exacerbation or precipitation of gout
Interactions - NSAIDs, digoxin
Potassium sparing diuretics
Spironolactone, eplerenone (mineralocorticoid receptor blockade)
Amiloride (Blockade of sodium reabsorption via ENaC channel)
Indication - Oedema, congestive heart failure
Adverse effects - GI
Interactions - NSAIDs, ACEi
Spironolactone, eplerenone
Potassium sparing diuretics (mineralocorticoid receptor blockade)
Indication - Oedema, congestive heart failure
Adverse effects - GI
Interactions - NSAIDs, ACEi
Amiloride
Potassium sparing diuretics (Blockade of sodium reabsorption via ENaC channel)
Indication - Oedema, congestive heart failure
Adverse effects - GI
Interactions - NSAIDs, ACEi
Mannitol
Osmotic diuretic
MoA - Elevates plasma osmolarity
Indication - Cerebral oedema, intra-ocular pressure
Adverse effects - Hypotension
Acetazolamide
Carbonic anhydrase inhibitor
MoA - Reduces aqueous humour volume
Indication - Intra-ocular pressure - open & acute closed angle glaucoma
Adverse effects - Paraesthesia
Ramipril, captopril, lisinopril
ACE inhibitors
MoA - Inhibits conversion of angiotensin I to angiotensin II. Blocks vasoconstriction.
Indication - hypertension, diabetic nephropathy, heart failure
Adverse effects - cough, hyperkalaemia
Interactions - Lithium, NSAIDs
Losartan, valsartan
ARBs
MoA - Blocks angiotensin-renin system
Indication - hypertension, diabetic nephropathy, heart failure
Adverse effects - hypotension, fatigue
Interactions - Diuretics
Sacubitril (in combination with the ARB valsartan)
Neprilysin inhibitors (used in combination with an ARB)
MoA - Inhibition of natriuretic peptide breakdown
Indication - Heart failure (with reduced ejection fraction)
Adverse effects - hypokalaemia, hypoglycaemia (from BNF)
Bisoprolol, atenolol
Beta-blockers (Beta-1 selective)
MoA - Negative inotropic/chronotropic agent
Indication - Hypertension, stable angina
Adverse effects - Bradycardia, bronchospasm
Interactions - NSAIDs, digoxin
Propranolol
Beta-blockers (Beta-1 and beta-2 selective)
MoA - Negative inotropic/chronotropic agent
Indication - Hypertension, stable angina
Adverse effects - Bradycardia, bronchospasm
Interactions - NSAIDs, digoxin
Doxazosin
Alpha adrenergic blockers
MoA - vasodilator, decreases total peripheral resistance
Indication - Hypertension
Adverse effects - dizziness, headache
Interactions - hypotensive drugs
Amlodipine, nifedipine, diltiazem
Calcium channel blockers
MoA - Blockade of vascular smooth muscle contraction
Indication - Hypertension, stable angina
Adverse effects - ankle swelling, oedema
Interactions - beta blockers, digoxin
Glyceryl trinitrate (GTN), Isosorbide Mononitrate (ISMN)
Nitrates
MoA - Nitric oxide release, leading to smooth muscle relaxation and vasodilation
Indication - Acute angina pectoris (GTN), heart failure
Adverse effects - Hypotension, headache
Interactions - Antihypertensives
Adrenaline, dobutamine, noradrenaline
Sympathomimetics
MoA - Adrenergic stimulation, increased inotropy
Indication - Cardiac arrest, cariogenic shock
Adverse effects - Arrhythmia
Aspirin, clopidogrel
Antiplatelet drugs
MoA:
Aspirin - Inhibition of thromboxane synthesis
Clopidogrel - Inhibition of platelet activation by ADP
Indication - Primary and secondary relief for CVD, anticoagulant prophylaxis
Adverse effects - GI irritation and bleeding
Interactions - Anticoagulants
Warfarin
Anticoagulants - coumarin
MoA - Inhibition of vitamin K epoxide reductase complex 1 (VKORC1) enzyme.
Indication - DVT, prophylaxis of stroke from AF
Adverse effects - Abnormal bleeding
Interactions - multiple drug interactions, notably NSAIDs, diuretics
Dabigatran
Anticoagulants - direct thrombin inhibitor
MoA - Inhibition of thrombin (also called Factor IIa)
Indication - Prophylaxis of venous thromboembolism post-surgery
Adverse effects - Abnormal bleeding
Apixaban, Edoxaban, Rivaroxaban
Anticoagulants - direct Factor Xa inhibitor
MoA - Inhibition of Factor Xa in coagulation cascade
Indication - Prophylaxis of stroke from atrial fibrillation; DVT
Adverse effects - Abnormal bleeding
Dalteparin, tinzaparin, enoxaparin (low molecular weight); unfractionated heparins
Anticoagulants - Heparins
MoA - Inactivation of thrombin and Factor Xa via complexing antithrombin III
Indication - Prophylaxis of venous thrombosis and pulmonary embolism
Adverse effects - abnormal bleeding
Alteplase, streptokinase, urokinase
Thrombolytics/fibrinolytics
MoA - Activation of plasminogen for proteolytic breakdown of thrombus fibrin
Indication - Myocardial infarction, ischaemic stroke
Simvastatin, atorvastatin (statins)
HMG-CoA Reductase inhibitors
MoA - Inhibition of mavelonate pathway required for cholesterol synthesis
Indication - Hypercholesterolaemia, risk of CVD and stroke
Adverse effects - Myalgia
Interactions - Verpamil, macrolides
Disopyramide, Quinidine
Class Ia anti-arrhythmic drugs,
Sodium channel blockers
MoA - Voltage-sensitive sodium channel blockade
Prolong QT interval, increase QRS duration.
Indications - Ventricular and supra ventricular arrhythmias
Adverse effects - oedema
Lidocaine
Class Ib anti-arrhythmic drug,
Sodium channel blocker
MoA - Voltage-sensitive sodium channel blockade
Prolong QT interval, increase QRS duration
Indication - CPR (used IV)
Adverse effects - oedema
Flecainide, Propafenone
Class Ic anti-arrhythmic drug,
Sodium channel blocker
MoA - Voltage-sensitive sodium channel blockade
Prolong QT interval, increase QRS duration
Indication - Paroxysmal atrial fibrillation and ventricular ectopic beats “pill in pocket”
Adverse effects - oedema
Class II anti-arrhythmic drugs
Beta-blockers:
Atenolol, bisoprolol, metoprolol
MoA - Beta-adrenergic receptor blockade – reduction in adrenergic effects on rate and inotropy
Indication - Prophylaxis of paroxysmal atrial tachycardia or fibrillation
Adverse effects - Hypotension
Amiodarone, dronedarone, sotalol
Class III Anti-Arrhythmic drugs – potassium channel blockers
(Sotalol also has some beta blocker activity)
MoA - Potassium channel blockade, also evidence of beta blocker and calcium channel blocker properties – prolong QT interval
Indication - Supraventricular, nodal and ventricular tachyarrhythmias, atrial fibrillation, (CPR - used IV)
Adverse effects - Nausea, vomiting
Verapamil, diltiazem
Class IV anti-arrhythmics – calcium channel blockers (phenylalkylamine & benzothiazepine subclasses)
MoA - Cardiac calcium channel blockade – reduction of action potential & cardiac output
Indication - Supraventricular tachycardia (especially paroxysmal SVT)
Adverse effects - Hypotension (verapamil), Constipation (diltiazem)
Digoxin
Cardiac glycosides
MoA - reduces conductivity of AV node
Indication - arrhythmias, AF, congestive heart failure
Adverse effects - fatigue, nausea
Adenosine
MoA - Activates adenosine receptors – causes hyperpolarization,
Slows conduction through AV Node
Indication - supraventricular tachycardia
Adverse effects - Nausea; contraindicated in obstructive airway disease
Atropine
Antimuscarinic
MoA - Blockade of vagal muscarinic acetylcholine receptors
Indication - Emergency bradycardia
Adverse effects - Urinary retention
Magnesium sulphate (IV)
MoA - Unclear – possible alteration of Na+, K+ and Ca2+ ion balance via ion channels and transporters
Indication - Emergency arrhythmia
(Also used IV for emergency asthma)
Adverse effects - Electrolyte irregularities
Salbutamol, terbutaline
Short-acting Beta-2 adrenergic agonists
MoA - Dilates bronchial smooth muscle
Indications - Asthma, reversible airways obstruction
Adverse effects - Tachycardia, tremor
Interactions - Diuretics
Ipratropium
Short-acting anti-muscarinic
MoA - Blocks muscarinic receptors to promote bronchial dilation
Indication - Acute asthma, bronchiospasm in COPD
Adverse effects - Dry mouth, constipation
Tiotropium
Long-acting anti-muscarinic
MoA - Blocks muscarinic receptors to promote bronchial dilation
Indication - Acute asthma, bronchiospasm in COPD
Adverse effects - Dry mouth, constipation
Theophylline, aminophylline
Methylxanthines
MoA - Bronchodilator, increases cAMP in smooth muscle
Indications - Acute asthma, reversible airways obstruction
Adverse effects - Headache, nausea
Interactions - Antidepressants, salbutamol
Beclomethasone, Prednisolone, Hydrocortisone, Fluticasone
Glucocorticoids
MoA - Reduction of inflammation and mucus production
Indications - Asthma, allergic rhinitis
Adverse effects - Cough
Interactions - Aspirin
Montelukast, zafirlukast
Leukotriene antagonists
MoA - Blockade of leukotriene receptors
Indications - Asthma, allergic rhinitis
Adverse effects - Abdominal pain
Interactions - Phenobarbital
Dornase alfa
Mucolytic
MoA - Synthetic DNAse 1 – breakdown of extracellular DNA to reduce sputum viscosity
Indication - Cystic fibrosis
Dopaminergics
Levodopa (precursor); Pramipexole, Ropinirole, Rotigotine (synthetic agonists)
MoA - Increased dopamine synthesis and dopaminergic function
Indication - Parkinson’s Disease
Adverse effects - Confusion, agitation
Interactions - MAOI
Dopa-decarboxylase inhibitor
Carbidopa, Benserazide
MoA - Stops breakdown of Levadopa in the periphery by inhibiting dopa-decarboxylase
Indication - Parkinson’s Disease
Adverse effects - Confusion, agitation
Inhibitors of Monoamine Oxidase B (MAOI)
Selegiline, Rasagiline
MoA - Inhibition of dopamine breakdown
Indication - Parkinson’s Disease
COMT (catechol-O-methyl transferase) Inhibitors
Entacapone, Tolcapone
MoA - Blockade of dopamine precursor breakdown by inhibition of COMT
Indication - Parkinson’s Disease
Adverse effects - N+V
Anticholinergics
Orphenadrine, Procyclidine, Trihexphenidyl
MoA - Muscarinic cholinergic receptor antagonist
Adverse effects - Dry mouth, constipation
Dopamine-depleting drugs
Tetrabenazine
MoA - Blocks VMAT, preventing uptake of DA into vesicles
Indications - Huntingdon’s chorea