PHARMA CONTROL 1: CARDIOVASCULAR PHARMACOLOGY

Captopril

Course Section: Hypertension; Heart failure. Classification: ACE inhibitor. Mechanism of Action: Inhibits ACE, decreasing angiotensin II and aldosterone while increasing bradykinin. Therapeutic Use: Hypertension, heart failure, post-MI ventricular dysfunction, diabetic nephropathy. Adverse Effects: Dry cough, hyperkalemia, hypotension, angioedema, renal impairment, rash, taste disturbance. Contraindications: Pregnancy, previous ACE-inhibitor angioedema, bilateral renal artery stenosis, severe hyperkalemia.

Enalapril

Course Section: Hypertension; Heart failure. Classification: ACE inhibitor; prodrug converted to enalaprilat. Mechanism of Action: Inhibits ACE, reducing angiotensin II and aldosterone and increasing bradykinin. Therapeutic Use: Hypertension, heart failure, asymptomatic left-ventricular dysfunction. Adverse Effects: Dry cough, hyperkalemia, hypotension, renal impairment, angioedema. Contraindications: Pregnancy, previous ACE-inhibitor angioedema, bilateral renal artery stenosis, severe hyperkalemia.

Losartan

Course Section: Hypertension; Heart failure. Classification: Angiotensin II receptor blocker; ARB. Mechanism of Action: Blocks AT1 receptors, preventing angiotensin II-mediated vasoconstriction and aldosterone secretion. Therapeutic Use: Hypertension, heart failure, diabetic nephropathy, proteinuric renal disease. Adverse Effects: Hyperkalemia, hypotension, dizziness, renal impairment. Contraindications: Pregnancy, bilateral renal artery stenosis, severe hyperkalemia.

Valsartan

Course Section: Hypertension; Heart failure. Classification: Angiotensin II receptor blocker; ARB. Mechanism of Action: Blocks AT1 receptors, decreasing vasoconstriction and aldosterone effects. Therapeutic Use: Hypertension, heart failure, post-MI ventricular dysfunction. Adverse Effects: Hyperkalemia, hypotension, dizziness, renal impairment. Contraindications: Pregnancy, bilateral renal artery stenosis, severe hyperkalemia.

Verapamil

Course Section: Hypertension; Antianginal drugs. Classification: Non-dihydropyridine calcium-channel blocker. Mechanism of Action: Blocks L-type Ca2+ channels, decreasing AV conduction, heart rate and contractility while causing vasodilation. Therapeutic Use: Hypertension, angina, supraventricular tachyarrhythmias. Adverse Effects: Bradycardia, AV block, hypotension, constipation, worsening heart failure. Contraindications: Severe bradycardia, advanced AV block, systolic heart failure, cardiogenic shock.

Diltiazem

Course Section: Hypertension; Antianginal drugs. Classification: Non-dihydropyridine calcium-channel blocker. Mechanism of Action: Blocks L-type Ca2+ channels in cardiac and vascular smooth muscle. Therapeutic Use: Hypertension, angina, atrial fibrillation/flutter rate control, supraventricular tachycardia. Adverse Effects: Bradycardia, AV block, hypotension, edema, headache, worsening heart failure. Contraindications: Severe bradycardia, advanced AV block, severe hypotension, systolic heart failure.

Nifedipine

Course Section: Hypertension. Classification: Dihydropyridine calcium-channel blocker. Mechanism of Action: Blocks vascular L-type Ca2+ channels, causing arteriolar vasodilation. Therapeutic Use: Hypertension, vasospastic angina, Raynaud phenomenon. Adverse Effects: Peripheral edema, flushing, headache, hypotension, reflex tachycardia, gingival hyperplasia. Contraindications: Severe hypotension and cardiogenic shock.

Amlodipine

Course Section: Hypertension; Antianginal drugs. Classification: Long-acting dihydropyridine calcium-channel blocker. Mechanism of Action: Blocks vascular L-type Ca2+ channels, causing arteriolar vasodilation and reduced afterload. Therapeutic Use: Hypertension, stable angina, vasospastic angina. Adverse Effects: Peripheral edema, flushing, headache, dizziness, palpitations, gingival hyperplasia. Contraindications: Severe hypotension or cardiogenic shock; caution in severe aortic stenosis.

Atenolol

Course Section: Hypertension; Antianginal drugs. Classification: Selective β1-adrenoceptor blocker. Mechanism of Action: Blocks cardiac β1 receptors, decreasing heart rate, contractility, cardiac output and renin release. Therapeutic Use: Hypertension, angina, selected tachyarrhythmias, post-MI therapy. Adverse Effects: Bradycardia, hypotension, fatigue, AV block, cold extremities, masking of hypoglycemia. Contraindications: Severe bradycardia, advanced AV block, cardiogenic shock, decompensated heart failure.

Metoprolol

Course Section: Hypertension; Antianginal drugs. Classification: Selective β1-adrenoceptor blocker. Mechanism of Action: Blocks β1 receptors, decreasing heart rate, contractility and renin release. Therapeutic Use: Hypertension, angina, myocardial infarction, tachyarrhythmias, chronic heart failure. Adverse Effects: Bradycardia, AV block, hypotension, fatigue, dizziness, masking of hypoglycemia. Contraindications: Severe bradycardia, advanced AV block, cardiogenic shock, acute decompensated heart failure.

Propranolol

Course Section: Hypertension; Antianginal drugs. Classification: Nonselective β1/β2-adrenoceptor blocker. Mechanism of Action: Blocks β receptors, decreasing heart rate, contractility, cardiac output and renin secretion. Therapeutic Use: Hypertension, angina, arrhythmias, post-MI treatment. Adverse Effects: Bradycardia, AV block, hypotension, fatigue, bronchospasm, masking of hypoglycemia. Contraindications: Asthma, severe bradycardia, advanced AV block, cardiogenic shock, decompensated heart failure.

Clonidine

Course Section: Hypertension. Classification: Centrally acting α2-adrenoceptor agonist. Mechanism of Action: Activates central α2 receptors, decreasing sympathetic outflow. Therapeutic Use: Hypertension. Adverse Effects: Sedation, dry mouth, bradycardia, hypotension, constipation, rebound hypertension. Contraindications: Severe bradycardia or hypotension; avoid abrupt discontinuation.

Methyldopa

Course Section: Hypertension. Classification: Centrally acting sympatholytic; central α2 agonist after metabolism. Mechanism of Action: Converted to α-methylnorepinephrine, reducing sympathetic outflow from the CNS. Therapeutic Use: Hypertension, especially during pregnancy. Adverse Effects: Sedation, dry mouth, orthostatic hypotension, hemolytic anemia, hepatotoxicity, hyperprolactinemia. Contraindications: Active liver disease, previous methyldopa-induced liver injury, MAO inhibitor therapy.

Prazosin

Course Section: Hypertension. Classification: Selective α1-adrenoceptor antagonist. Mechanism of Action: Blocks vascular α1 receptors, causing arterial and venous vasodilation. Therapeutic Use: Hypertension; also benign prostatic hyperplasia. Adverse Effects: First-dose syncope, orthostatic hypotension, dizziness, headache, reflex tachycardia. Contraindications: Significant hypotension; caution with other antihypertensive drugs.

Doxazosin

Course Section: Hypertension. Classification: Selective α1-adrenoceptor antagonist. Mechanism of Action: Blocks α1 receptors in vascular and prostatic smooth muscle. Therapeutic Use: Hypertension and benign prostatic hyperplasia. Adverse Effects: Orthostatic hypotension, first-dose syncope, dizziness, headache, fatigue, edema. Contraindications: Significant hypotension; caution with other vasodilators.

Hydralazine

Course Section: Hypertension; Heart failure. Classification: Direct arteriolar vasodilator. Mechanism of Action: Directly relaxes arteriolar smooth muscle, decreasing systemic vascular resistance and afterload. Therapeutic Use: Severe hypertension, hypertension in pregnancy, heart failure combined with nitrates. Adverse Effects: Reflex tachycardia, headache, flushing, hypotension, fluid retention, lupus-like syndrome. Contraindications: Coronary artery disease and rheumatic mitral-valve disease; caution in tachyarrhythmias.

Minoxidil

Course Section: Hypertension. Classification: Direct arteriolar vasodilator; ATP-sensitive K+ channel opener. Mechanism of Action: Opens KATP channels in vascular smooth muscle, causing hyperpolarization and vasodilation. Therapeutic Use: Severe resistant hypertension; topical form for alopecia. Adverse Effects: Reflex tachycardia, fluid retention, edema, hypertrichosis, pericardial effusion. Contraindications: Pheochromocytoma; caution in severe cardiac disease.

Sodium nitroprusside

Course Section: Hypertension; Heart failure. Classification: Direct arterial and venous vasodilator; nitric-oxide donor. Mechanism of Action: Releases NO, increasing cGMP and causing rapid arterial and venous dilation. Therapeutic Use: Hypertensive emergencies and acute severe heart failure. Adverse Effects: Severe hypotension, reflex tachycardia, cyanide toxicity, thiocyanate toxicity, metabolic acidosis. Contraindications: Severe compensatory hypertension; caution in renal or hepatic failure and prolonged therapy.

Nitroglycerine (Glyceryl trinitrate)

Course Section: Antianginal drugs. Classification: Organic nitrate; nitric-oxide donor. Mechanism of Action: Generates NO, increasing cGMP; predominantly causes venodilation and decreases preload. Therapeutic Use: Acute angina, acute coronary syndromes, acute pulmonary edema. Adverse Effects: Headache, flushing, dizziness, hypotension, reflex tachycardia, tolerance. Contraindications: PDE5 inhibitor use, severe hypotension, right-ventricular infarction, markedly increased intracranial pressure.

Isosorbide mononitrate

Course Section: Antianginal drugs; Heart failure. Classification: Long-acting organic nitrate. Mechanism of Action: Generates NO and increases cGMP, producing mainly venodilation and reduced preload. Therapeutic Use: Prevention of chronic angina and vasodilator therapy in selected heart-failure patients. Adverse Effects: Headache, flushing, dizziness, hypotension, reflex tachycardia, tolerance. Contraindications: PDE5 inhibitor use, severe hypotension, shock.

Isosorbide dinitrate

Course Section: Antianginal drugs; Heart failure. Classification: Organic nitrate; nitric-oxide donor. Mechanism of Action: Increases NO and cGMP, producing predominantly venous dilation. Therapeutic Use: Angina and heart failure in combination with hydralazine. Adverse Effects: Headache, flushing, hypotension, dizziness, reflex tachycardia, tolerance. Contraindications: PDE5 inhibitor use, severe hypotension, circulatory shock.

Digoxin

Course Section: Heart failure. Classification: Cardiac glycoside. Mechanism of Action: Inhibits Na+/K+-ATPase, indirectly increasing intracellular Ca2+; also increases vagal tone. Therapeutic Use: Selected symptomatic heart failure and ventricular-rate control in atrial fibrillation. Adverse Effects: Nausea, vomiting, anorexia, confusion, visual disturbances, bradycardia, dangerous arrhythmias. Contraindications: Ventricular fibrillation; caution in AV block, renal impairment, hypokalemia, WPW with atrial fibrillation.

Dopamine

Course Section: Heart failure. Classification: Dose-dependent dopaminergic and adrenergic agonist. Mechanism of Action: Stimulates D1 at low doses, β1 at moderate doses, and α1 at high doses. Therapeutic Use: Selected shock states with low cardiac output and symptomatic bradycardia. Adverse Effects: Tachycardia, arrhythmias, hypertension, myocardial ischemia, peripheral ischemia. Contraindications: Pheochromocytoma and uncorrected tachyarrhythmias.

Dobutamine

Course Section: Heart failure. Classification: Predominantly β1-adrenoceptor agonist. Mechanism of Action: Stimulates β1 receptors and increases myocardial contractility and cardiac output. Therapeutic Use: Acute decompensated heart failure and cardiogenic shock. Adverse Effects: Tachycardia, arrhythmias, angina, hypertension or hypotension. Contraindications: Hypertrophic obstructive cardiomyopathy and uncontrolled tachyarrhythmias.

Acetazolamide

Course Section: Diuretics. Classification: Carbonic-anhydrase inhibitor. Mechanism of Action: Inhibits carbonic anhydrase in the proximal tubule, reducing NaHCO3 reabsorption. Therapeutic Use: Glaucoma, altitude sickness, metabolic alkalosis, idiopathic intracranial hypertension. Adverse Effects: Metabolic acidosis, hypokalemia, paresthesia, kidney stones, polyuria. Contraindications: Severe renal or hepatic disease, hyponatremia, hypokalemia, hyperchloremic acidosis.

Furosemide

Course Section: Diuretics. Classification: Loop diuretic. Mechanism of Action: Inhibits the Na+/K+/2Cl− cotransporter in the thick ascending limb. Therapeutic Use: Pulmonary edema, heart-failure edema, hypertension, hypercalcemia. Adverse Effects: Hypokalemia, dehydration, hypotension, metabolic alkalosis, hypomagnesemia, ototoxicity, hyperuricemia. Contraindications: Anuria and severe volume or electrolyte depletion.

Torasemide (Torsemide)

Course Section: Diuretics. Classification: Loop diuretic. Mechanism of Action: Inhibits the Na+/K+/2Cl− cotransporter in the thick ascending limb. Therapeutic Use: Edema from heart failure, renal or hepatic disease, and hypertension. Adverse Effects: Hypokalemia, hyponatremia, dehydration, hypotension, metabolic alkalosis, hyperuricemia. Contraindications: Anuria and severe electrolyte or volume depletion.

Hydrochlorothiazide

Course Section: Diuretics. Classification: Thiazide diuretic. Mechanism of Action: Inhibits the Na+/Cl− cotransporter in the distal convoluted tubule. Therapeutic Use: Hypertension, mild edema, nephrogenic diabetes insipidus, prevention of calcium stones. Adverse Effects: Hypokalemia, hyponatremia, hyperuricemia, hyperglycemia, hypercalcemia, metabolic alkalosis. Contraindications: Anuria; caution in severe renal dysfunction and significant electrolyte depletion.

Spironolactone

Course Section: Diuretics. Classification: Potassium-sparing diuretic; mineralocorticoid-receptor antagonist. Mechanism of Action: Blocks aldosterone receptors in the collecting duct, reducing Na+ reabsorption and K+ excretion. Therapeutic Use: Heart failure, resistant hypertension, hyperaldosteronism, ascites. Adverse Effects: Hyperkalemia, metabolic acidosis, gynecomastia, impotence, menstrual irregularities. Contraindications: Hyperkalemia, Addison disease, severe renal impairment, anuria.

Heparin

Course Section: Blood coagulation. Classification: Unfractionated heparin anticoagulant. Mechanism of Action: Activates antithrombin, increasing inhibition of thrombin and factor Xa. Therapeutic Use: Prevention and treatment of venous thromboembolism and acute coronary syndromes. Adverse Effects: Bleeding, heparin-induced thrombocytopenia, osteoporosis, hyperkalemia. Contraindications: Active major bleeding, history of HIT, severe thrombocytopenia.

Dalteparin

Course Section: Blood coagulation. Classification: Low-molecular-weight heparin. Mechanism of Action: Activates antithrombin and preferentially inhibits factor Xa. Therapeutic Use: Prevention and treatment of venous thromboembolism and selected acute coronary syndromes. Adverse Effects: Bleeding, thrombocytopenia, injection-site hematoma. Contraindications: Active major bleeding and history of immune-mediated HIT.

Enoxaparin

Course Section: Blood coagulation. Classification: Low-molecular-weight heparin. Mechanism of Action: Enhances antithrombin-mediated inhibition of factor Xa more than thrombin. Therapeutic Use: Prevention and treatment of DVT/PE and acute coronary syndromes. Adverse Effects: Bleeding, thrombocytopenia, injection-site hematoma, hyperkalemia. Contraindications: Active major bleeding and recent immune-mediated HIT.

Warfarin

Course Section: Blood coagulation. Classification: Vitamin K antagonist anticoagulant. Mechanism of Action: Inhibits vitamin K epoxide reductase, reducing functional factors II, VII, IX and X. Therapeutic Use: Prevention and treatment of thromboembolism, atrial fibrillation, mechanical heart valves. Adverse Effects: Bleeding, skin necrosis, purple-toe syndrome, drug/food interactions, teratogenicity. Contraindications: Pregnancy, active major bleeding, severe uncontrolled hypertension.

Argatroban

Course Section: Blood coagulation. Classification: Direct thrombin inhibitor. Mechanism of Action: Directly and reversibly inhibits free and clot-bound thrombin. Therapeutic Use: Anticoagulation in patients with heparin-induced thrombocytopenia. Adverse Effects: Bleeding, hypotension, anemia, elevated liver enzymes. Contraindications: Active major bleeding; caution and dose reduction in hepatic impairment.

Acetylsalicylic acid (Aspirin)

Course Section: Blood coagulation. Classification: Antiplatelet drug; irreversible COX inhibitor. Mechanism of Action: Irreversibly inhibits platelet COX-1 and decreases thromboxane A2 synthesis. Therapeutic Use: Acute coronary syndromes and secondary prevention of myocardial infarction and ischemic stroke. Adverse Effects: GI bleeding, peptic ulceration, hypersensitivity, bronchospasm, renal impairment, tinnitus. Contraindications: Active bleeding, peptic ulcer, aspirin hypersensitivity, aspirin-sensitive asthma, viral illness in children.

Clopidogrel

Course Section: Blood coagulation. Classification: Antiplatelet drug; irreversible P2Y12 receptor antagonist. Mechanism of Action: Blocks ADP-mediated platelet activation and GP IIb/IIIa activation. Therapeutic Use: Acute coronary syndromes, coronary stenting, secondary prevention of MI and ischemic stroke. Adverse Effects: Bleeding, bruising, diarrhea, rash, rare thrombotic thrombocytopenic purpura. Contraindications: Active pathological bleeding and severe hypersensitivity.

Dipyridamole

Course Section: Blood coagulation. Classification: Antiplatelet drug and vasodilator. Mechanism of Action: Inhibits phosphodiesterase and adenosine uptake, increasing platelet cAMP. Therapeutic Use: Secondary stroke prevention with aspirin and selected cardiac indications. Adverse Effects: Headache, flushing, dizziness, hypotension, GI upset, possible coronary steal. Contraindications: Severe hypotension; caution in unstable angina or severe coronary disease.

Abciximab

Course Section: Blood coagulation. Classification: GP IIb/IIIa receptor antagonist; monoclonal-antibody fragment. Mechanism of Action: Blocks GP IIb/IIIa receptors and prevents fibrinogen-mediated platelet aggregation. Therapeutic Use: High-risk PCI and selected acute coronary syndromes. Adverse Effects: Major bleeding, thrombocytopenia, hypotension, hypersensitivity. Contraindications: Active bleeding, severe thrombocytopenia, recent major surgery or stroke, uncontrolled severe hypertension.

Tirofiban

Course Section: Blood coagulation. Classification: GP IIb/IIIa receptor antagonist. Mechanism of Action: Reversibly blocks GP IIb/IIIa receptors and prevents fibrinogen binding. Therapeutic Use: Selected acute coronary syndromes and PCI. Adverse Effects: Bleeding and thrombocytopenia. Contraindications: Active bleeding, severe thrombocytopenia, recent intracranial hemorrhage or major surgery.

Epoprostenol

Course Section: Blood coagulation. Classification: Prostacyclin PGI2 analogue; antiplatelet and vasodilator. Mechanism of Action: Activates prostacyclin receptors, increasing cAMP and inhibiting platelet aggregation. Therapeutic Use: Primarily pulmonary arterial hypertension; inhibition of platelet aggregation in extracorporeal circulation. Adverse Effects: Flushing, headache, hypotension, jaw pain, nausea, bleeding. Contraindications: Severe left-ventricular dysfunction with pulmonary edema; caution with active bleeding.

Streptokinase

Course Section: Blood coagulation. Classification: Thrombolytic; fibrinolytic drug. Mechanism of Action: Forms a complex with plasminogen that promotes formation of plasmin and fibrin degradation. Therapeutic Use: Thrombolysis in selected myocardial infarction, pulmonary embolism and severe thrombosis. Adverse Effects: Major bleeding, intracranial hemorrhage, hypotension, allergic reactions, fever. Contraindications: Active internal bleeding, previous hemorrhagic stroke, recent major surgery or trauma, intracranial tumor, severe uncontrolled hypertension.

Alteplase

Course Section: Blood coagulation. Classification: Recombinant tissue plasminogen activator; tPA thrombolytic. Mechanism of Action: Converts fibrin-bound plasminogen to plasmin, causing fibrin-clot degradation. Therapeutic Use: Selected acute ischemic stroke, STEMI, massive pulmonary embolism, catheter thrombosis. Adverse Effects: Major bleeding, intracranial hemorrhage, angioedema. Contraindications: Active internal bleeding, previous intracranial hemorrhage, recent major intracranial surgery or head trauma, suspected aortic dissection.

Tranexamic acid

Course Section: Blood coagulation. Classification: Antifibrinolytic drug; synthetic lysine analogue. Mechanism of Action: Blocks lysine-binding sites on plasminogen and plasmin, preventing fibrin degradation. Therapeutic Use: Excessive bleeding in trauma, surgery, heavy menstrual bleeding and hyperfibrinolytic states. Adverse Effects: Nausea, vomiting, diarrhea, dizziness, visual disturbance, seizures at high doses, possible thrombosis. Contraindications: Active intravascular thrombosis and acquired defective color vision; caution in renal impairme