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MVST 1B (Fach) / MoDA (Lektion)

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• Caffeine PDE-inhibitor Adenosine receptor antagonist methylxanthine ~ theophylline, IBMX
• Clonidine Use: Hypertension, migraine, Tourette syndrome MoA: Selective α2-adrenoreceptor agonist; centrally acting SE: rebound hypertension if withdrawn suddenly →methyldopa, moxonidine Vet analog: xylazine (sedation), reverse with yohimbine
• D-amphetamine Indirect sympathomimetic Overdose→ diazepam
• Darifenacin Use: urinary frequency, urgency, incontinence MoA: Selective M3-ACh-receptor antagonist SE: antimuscarinic: dry mouth, gastro-intestinal disturbances including constipation, flatulence, taste disturbances, blurred vision, dry eyes, drowsiness, dizziness, fatigue, difficulty in micturition → oxybutynin
• Dipyridamole Use: Not used much anymore MoA: Anti-platelet drug adenosine receptor antagonist, PDE-inhibitor ↑cAMP/cGMP, TXA-synthase inhibitor Coronary steal
• Disulfiram Acetaldehyde dehydrogenase inhibitor Chronic alcoholism
• Dobutamine Use: inotropic support in infarction, cardiac surgery, cardiomyopathies, septic & cardiogenic shock, cardiac stress testing MoA: Selective β1-adrenoreceptor agonist; sStructurally similar to dopamine SE: GI upset, hypertension, rash → ephedrine
• Dyflos Organophosphorous AChE inhibitor --> pralidoxime, atropine, Ca2+ blockers
• Edrophonium Short-acting AChE inhibitor; anionic site; diagonsis of Lambort-Eaton vs Myasthenia Gravis
• Entacapone Peripheral COMT inhibitor; Parkinson's (not first-line)
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• Ergotamine Use: Acute migraine, unresponsive to other treatment MoA: Ergot alkaloid; 5-HT-1A agonist SE: GI upset, dizziness →triptans; paracetamol, NSAIDs; propranolol, sodium valproate
• Imipramine Use: Depression, nocturnal enuresis in children MoA: TCA SE: Antimuscarinic →amitriptyline, nortriptyline, clomipramine, dosulepin
• Malathion Organophosphorous AChE-inhibitor
• Neostigmine Use: glaucoma, myasthenia gravis, reversal of neuromuscular blockade + atropine; Alzheimer's MoA: AChE inhibitor SE: nausea, vomiting, diarrhoea, increased salivation, etc. → pyridostigmine, donepezil
• Pancuronium Use: Long-duration non-depolarising muscle relaxant: surgery, ICU MoA: ACh blocker at NMJ SE: tachycardia, hypertension; no histamine-releasing effect →atracurium, vecuronium; suxamethonium
• Phenoxybenzamine Use: Phaeochromocytoma MoA: Sympatholytic; non-selective irreversible α-adrenoreceptor antagonist →phentolamine  
• Phenylephrine Use: hypotension, priapism MoA: non-selective α-adrenoreceptor agonist, longer-acting than →noradrenaline; vasopressor SE: tachycardia, hypertension, arrythmias → ephedrine, noradrenaline
• Pilocarpine Use: 1ary angle-closure glaucoma MoA: non-selective mACh-receptor agonist SE: headache, blurred vision, mitosis →latanoprost, timolol
• Pirenzepine Selective M1-ACh-receptor antagonist; treats peptic ulcers
• Pralidoxime Use: organophosphorous AChE-inhibitors; in conjunction with →atropine and →diltiazem MoA: Regenerate AChE enzyme by binding to anioning site and releasing poison from esteric site → dyflos
• Propranolol Use: Somatic anxiety, panic attacks, essential tremor migraine prophylaxis, oesophageal varices phaeochromocytoma, hyperthyroidism hypertension, arrhythmias, angina MoA: non-selective β-adrenoreceptor antagonist; Inhibits insulin release! SE: typical + hyperglycaemia, sexual dysfunction, cold hands
• Salbutamol* Use: Asthma (acute + maintenance); acute COPD; premature labour; hyperkalaemia MoA: Selective β2-adrenoreceptor agonist → bronchodilatation Dose: PO: 4mg 3-4x/d Aerosol inhalation: 100-200mcg (1-2 puffs) up to 4x/d Powder inhalation: 2-5 - 5mg up to 4x/d IV injection: 250mcg; infusion 3-20 mcg/min SE: fine tremor, nervous tension, headache, muscle cramps, palpitation; lactic acidosis if IV ~ terbutaline; → salmeterol
• Selegiline Use: Symptomatic Parkinson's disease MoA: Selective MAO-B inhibitor SE: GI upset, depression, psychosis, confusion → rasigiline; Co-carel/benel-dopa; ropinirole, pramipexol, apomorphine; entacapone; procyclidine, benzatropine
• Sildenafil Use: erectile dysfunction, pulmonary arterial hypertension MoA: PDE-V inhibitor SE: GI upset, headache (including migraine), flushing, dizziness, myalgia, back pain, visual disturbances (non-arteritic anterior ischaemic optic neuropathy → stop drug), nasal congestion → bosentan
• Suxamethonium Use: Short-acting paralysis during anaesthesia MoA: Depolarizing muscle relaxant; nACh-receptor agonist at NMJ, prolonged by AChE-I's (→neostigmine), irreversible SE: post-OP apnoea (→non-specific plasma choline esterases), hypersensitvity, hyperkalaemia, muscle pain
• Tetanus toxin Cleaves synaptobrevin in inhibitory interneurons (Renshaw cells) → spastic paralysis
• Tyramine Cheese effect w/ MAO-I's; converted into false transmitter octopamine
• Abciximab Antiplatelet drug; GPIIa/IIIb antibody
• Acetazolamide Use: pevention of mountain sickness, adjunct in glaucoma MoA: Carbonic anhydrase inhibitor; mild diuretic SE: Sulfa drug → blood disorders, skin rash → timolol, lanasoprost, pilocarpine
• Alteplase Use: Acute MI (<12h after), PE, ischaemic stroke (<4.5h after); line thrombosis MoA: Fibrinolytic; recombinant tissue Plasminogen Activator (r-tPA) SE: nausea, vomiting; bleeding →streptokinase, desmoteplase
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• Amiloride Use: Oedema, congestive heart failurel adjunct to K+-losing diuretics; hepatic cirrhosis w/ ascites MoA: K+ sparing diuretic, ENaC inhibitor → triamterene; spironolactone, epleronone
• Aminocaproic acid Use: Anti-fibrinolytic "amicar" MoA: Lysine analogue → plasmin inhibitor
• Amiodarone Clinical use: Chemical cardioversion AF → sinus rhythm AF with accessory pathway (WPW syndrome); → flecainide w/ structural abnormalities ALS shockable rhythms (VF, puseless VT): 300mg MoA: K+ channel blocker; Vaughan-Williams class III anti-dyshythmic prolongs refractory period of cardiac action potential SE: Nausea, vomiting Fibrosis: lower lung, liver Thyroid: hyper- and hypo- corneal deposits, slate-grey appearance, phototoxicity Arrythmias, e.g. torsades de point  → sotalol, adenosine
• (In)Amrinone Use: Heart failure MoA: PDE-III inhibitor → Milrinone, enoximone
• Aspirin* Uses: Pain/inflammation, stroke/ACS, CVS prevention MoA: NSAID; (ir)reversible COX inhibitor; anti-platelet via →PGI2 / ↓TXA2 Dose: Analgesic: 300-900mg up to 6x daily, max 4g/d antiplatelet: 300mg acutely, 75mg maintenance Side effects: Gastric bleeding, ulceration, Reye's synrome, Samter's triade (aspirin-induced asthma) Prevention:  PPI's (→omeprazole, →lansoprazole), PGE analogs (→misoprostol)   →Clopidogrel
• Bosentan Use: pulmonary hypertension, systemic sclerosis wih ongoing digital ulcer disease MoA: Non-selective endothelin receptor antagonist (on SMC's) → sildenafil, iloprost
• Captopril Use: Hypertension (=A), heart failure, post-MI, diabetic nephropathy (type I); not used anymore MoA: ACE-Inhibitor, ↓circulating angiotensin II SE: Hypotension; hyperkalaemia, dry cough, angiooedema, alopecia, sleep disorder → lisinopril, enalapril, ramipril
• Carvedilol Use: Stable heart failure MoA: selective α1-, non-selective β-adrenoreceptor blocker SE: typical → propranolol → bisoprolol, metoprolol, atenolol
• Clopidogrel* Use: ACS/stroke, CVS prevention MoA: Antiplatelet drug; P2Y12-ADP-receptor antagonist Dose: Acutely 300mg, maintenance 75mg SE: Bleeding, GI upset   → aspirin
• Digoxin* Use: Angina, heart failure; SVT, esp. AF MoA: Cardiac glycoside; Na+/K+-ATPase-inhibitor; stimulates n. vagus → classical ECG feature: oddly-shaped ST depression SE: Digoxin toxicity (esp. with ↓K+; → digifab): blurred green-yellow vision, GI-upset, confusion Arrythmias, AV block
• Enalapril Use: HTN, Heart failure, post-MI MoA: ACE-Inhibitor (pro-drug for enalaprilat), ↓circulating angiotensin II SE: hypotension, hyperkalaemia, dry cough, angiooedema   → lisinopril, ramipril, captopril
• Eptifibatide GP IIb/IIIa-receptor antagonist; cyclic heptapeptide; anti-platelet agent → aspirin, clopidogrel, dipyridamole, abciximab, tirofiban
• Furosemide* Use: Heart failure, oedema, resistant hypertension MoA: Loop diuretic:Na+/K+/2Cl- transport inhibitor SE: Hypokalaemia, hyponatraemia, ototoxicity, gout Dose: 40mg PO OM   → bumetanide
• Heparin Use: VTE, incl PE, DVT; thromboprophylaxis MoA: Antithrombin activator; intravenous administration; low molecular weight (Factors Xa, longer half-life) vs unfractionated (Xa + others) SE: bleeding, thrombocytopaenia (=HIT); overdose → protamine sulphate Dose: 5000 units LMWH for VTE prophylaxis →warfarin, dabigatran, bivalirudin
• Hydrochlorothiazide Use: HTN ('D'), heart failure, oedema MoA: Inhibits Na+ reabsorption in distal convoluted tubule SE: Electrolytes: ↓K+, ↓Na+, ↑Ca2+, ↑uric acid, ↓Mg2+ Oligospermia, impaired glycaemic control → bendroflumethiazide, chlortalidone, indapamide, metolazone    
• Levosimendan Inodilator → Ca2+ sensitizer, heart failure
• Losartan HTN, Heart failure, diabetic nephropathy, ? beneficial in gout ? MoA: Angiotensin-II-receptor (AT-1) antagonist SE:Hyperkalaemia   → candesartan, irbesartan
• Mannitol Use: maintain urinary flow in kidney failure; cerebral oedema, increased intraoccular pressure MoA: Osmotic diuretic SE: hypotension → loop diuretics; thiazide diuretics, K+ sparing diuretics
• Pimobendan Inodilator → Ca2+ sensitizer; heart failure
• Streptokinase Use: Myocardial infacrction, DVT, PE, central retinal vein / artery occlusion MoA: Bacterial plasminogen activator; immunogenic SE: Nausea, vomiting; bleeding →alteplase, desmoteplase

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