Category: Uncategorized
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Warfarin
MECHANISM OF ACTION Coumarin anticoagulant; inhibits hepatic synthesis of vitamin K-dependent clotting factors (II, VII, IX, X) and co-factors (proteins C and S). Thus the predominant action of warfarin is on the extrinsic pathway of the clotting cascade. INDICATIONS DVT. PE. Prophylaxis of VTE in AF, rheumatic heart disease and in patients with prosthetic heart…
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Vasoconstrictor sympathomimetics
EXAMPLES Noradrenaline, ephedrine, phenylephrine MECHANISM OF ACTION Stimulation of peripheral a-adrenoceptors within the vasculature, leading to vasoconstriction and increased systolic and diastolic blood pressure. INDICATIONS Acute hypotension. Cardiac arrest. CAUTIONS AND CONTRA-INDICATIONS Hypertension SIDE-EFFECTS Hypertension. Headache. Arrhythmias. Bradycardia/tachycardia. METABOLISM AND HALF-LIFE Metabolised in the liver and other tissues by MAO and COMT. MONITORING Continuous cardiac…
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Tranexamic acid
MECHANISM OF ACTION Competitively inhibits the activation of plasminogen to plasmin, thereby reducing fibrin clot degradation. At high doses can directly inhibit plasmin activity. INDICATIONS Menorrhagia. Epistaxis. Thrombolytic overdose. Prevent excessive bleeding (dental extraction in haemophilia) CAUTIONS AND CONTRA-INDICATIONS Thromboembolic disease SIDE-EFFECTS GI disturbance. Disturbance in colour vision. METABOLISM AND HALF-LIFE Plasma t½ is between…
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Thiazide diuretics EXAMPLES Bendroflumethiazide
MECHANISM OF ACTION InhibitNa+/Cl symporter in the distal convoluted tubules thereby reducing Na+ reabsorption and reducing water reabsorption. INDICATIONS Hypertension. Oedema in heart failure. CAUTIONS AND CONTRA-INDICATIONS Electrolyte disturbances (including refractory hypokalaemia, hyponatraemia, hypercalcaemia and symptomatic hyperuricaemia). Addison’s disease. Avoid in breastfeeding mothers due to suppression of lactation. SIDE-EFFECTS Postural hypotension. Hyponatraemia. Hypokalaemia. Hyperuricaemia (e.g. gout).…
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Statins EXAMPLES Simvastatin, atorvastatin, pravastatin, rosuvastatin
MECHANISM OF ACTION Inhibition of HMG CoA reductase, preventing the hepatic conversion of mevalonic acid to cholesterol. Reduced cholesterol synthesis in the liver results in decreased plasma LDL. INDICATIONS Prevention of cardiovascular events in patients with atherosclerotic disease or diabetes mellitus. Primary hyperlipidaemia CAUTIONS AND CONTRA-INDICATIONS Active liver disease (caution needed in patients with alcohol…
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Potassium channel activators EXAMPLES
Nicorandil MECHANISM OF ACTION Dual mechanism of action. Opens ATP-sensitive Kþ channels resulting in smooth muscle relaxation, thereby promoting arterial vasodilatation and reducing afterload. Nitric oxide moiety activates guanylyl cyclase to achieve venous relaxation and a reduction in preload. Direct effects on coronary arteries are also seen. INDICATIONS Prophylaxis and treatment of angina CAUTIONS AND…
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Nitrates EXAMPLES Glyceryl trinitrate (GTN), isosorbide mononitrate (ISMN)
MECHANISM OF ACTION Metabolised to nitric oxide that activates guanylyl cyclase, increasing production of cGMP in vascular tissues. This secondary messenger causes smooth muscle relaxation resulting in coronary artery dilatation (increasing oxygen supply to myocardium) and systemic vasodilatation (reducing preload and thereby reducing oxygen demand). INDICATIONS Prophylaxis and treatment of angina LVF CAUTIONS AND CONTRA-INDICATIONS…
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Low molecular weight heparins (LMWH)
EXAMPLES Dalteparin, enoxaparin, tinzaparin MECHANISM OF ACTION Activate antithrombinIII(serine protease inhibitor)thus inhibiting factors IIa (thrombin) and Xa in the common pathway of the clotting cascade. Secondary effects mediated by impairing adhesion and aggregation of platelets. INDICATIONS Prevention of VTE. Treatment of VTE and acute coronary syndrome/MI. Prevention of clotting in extracorporeal circuits CAUTIONS AND CONTRA-INDICATIONS…
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Loop diuretics
EXAMPLES Furosemide, bumetanide MECHANISM OF ACTION Inhibits the reabsorption of Na+ and Cl in the ascending limb of the Loop of Henle by inhibiting the Na+/K+/2Cl co-transporter. This results in increased Naþ excretion and free water clearance, thereby reducing preload. INDICATIONS Pulmonary oedema is secondary to LVF. Chronic heart failure CAUTIONS AND CONTRA-INDICATIONS Severe hypokalaemia/hyponatraemia. Hypovolaemia.…
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Inotropic sympathomimetics
EXAMPLES Adrenaline, dopamine, dobutamine, isoprenaline MECHANISM OF ACTION Actions vary depending on which receptors are stimulated. Adrenalineactsona-(peripheral vasculature)and-adrenoceptors(myocardium), producing positive inotropic and chronotropic effects. Low-dose dopamine and dobutamine stimulate b1-adrenoceptors in the myocardium, predominantly increasing contractility. INDICATIONS Cardiogenic shock. Septic shock. Acute hypotension. Cardiac arrest (adrenaline) CAUTIONS AND CONTRA-INDICATIONS Phaeochromocytoma (dopamine). Atrial and ventricular tachyarrhythmias…