Cardiovascular Agents Flashcards
Norvasc
Generic Name: amlodipine
Class: calcium channel blocker
Uses: hypertension, chronic stable angina, vasospastic angina
MOA: long-acting dihydropyridine calcium-channel-blocking drug with potent arterial and coronary vasodilating properties
Normal Daily Dose: 5-10 mg po daily
Metabolism: hepatic, 90%; major substrate of CYP3A4/5
Tenormin
Generic Name: atenolol
Class: Beta-Adrenergic Blocker, Cardioselective
Uses: angina pectoris; hypertension; acute myocardial infarction
MOA: decreases AV nodal conduction in supraventricular tachycardias and blockade of catecholamine-induced dysrhythmias
Normal Daily Dose: 25-50 mg po daily
Metabolism: limited hepatic
Lipitor
Generic Name: atorvastatin
Class: HMG-CoA Reductase Inhibitor
Uses: primary and secondary prevention of atherosclerotic cardiovascular disease; secondary prevention of cardiovascular events in patients with or at high risk of CAD; familial hypercholesterolemia
MOA: inhibits conversion of HMG-CoA to mevalonate, and early rate-limiting step in cholesterol synthesis
Normal Daily Dose: 1-80 mg po daily
Metabolism: extensive hepatic; major substrate of CYP3A4/5 and P-glycoprotein; inhibits P-glycoprotein
Lotensin
Generic Name: benazepril
Class: ACE-inhibitor; Antihypertensive
Uses: hypertension
MOA: competitive ACE-I: it reduces serum aldosterone, leading to decreased sodium retention, potentiates the vasodilator kallikrein-kinin system, and can alter proteinoid metabolism, inhibits the sympathetic nervous system, and inhibits the tissue renin-angiotensin system
Normal Daily Dose: 10 mg po daily; may titrate to 20-40 mg po daily (max 80mg/d)
Metabolism: extensive hepatic metabolism to 1 active metabolite (benazeprilat)
Zebeta
Generic Name: bisoprolol
Class: Cardio selective Beta-Adrenergic Blocker
Uses: hypertension
MOA: decreases AV nodal conduction in supraventricular tachycardia and blockade of catecholamine-induced dysrhythmias
Normal Daily Dose: 2.5-5 mg po daily, may titrate to max of 20 mg po daily
Metabolism: Extensive hepatic; major substrate of CYP3A4/5
Atacand
Generic Name: candesartan
Class: angiotensin II receptor antagonist
Uses: heart failure; hypertension
MOA: a selective, reversible, competitive antagonist of the angiotensin II receptor type I
Normal Daily Dose:
HTN adults: 16 mg po daily
Heart failure: 4 mg po daily, may titrate to 32 mg po daily
Metabolism: parent compound bioactivated during absorption via ester hydrolysis within intestinal wall to candesartan
Coreg
Generic Name: carvedilol
Class: alpha/beta-adrenergic blocker
Uses: heart failure; hypotension
MOA: a selective alpha1 and nonselective beta-adrenergic blocker that decreases AV nodal conduction in supraventricular tachycardias and blockade of catecholamine-induced dysrhythmia
Normal Daily Dose:
heart failure: 3.125 mg po bid, may titrate to 25 mg po bid for patient weighing <85 kg, 50 mg po bid for patients weighing >85 kg
hypertension: 6.25 mg po bid; max 25 mg po bid
Metabolism: Hepatic 98%; major substrate of CYP2D6, P-glycoprotein
Hygroton, Thalitone
Generic Name: chlorthalidone
Class: thiazide diuretic
Uses: hypertension; edema
MOA: increases sodium and chloride excretion by interfering with their reabsorption in the cortical-diluting segment of the nephron
Normal Daily Dose:
HTN: 25 mg po daily, may titrate to max of 100 mg po daily
Edema: 50 mg po daily, may titrate to max of 200 mg po daily
Metabolism: Hepatic
Catapres, Kapvay
Generic Name: clonidine
Class: alpha2-adrenergic agonist
Uses: ADHD; hypertension
MOA: stimulates presynaptic alpha2-adrenergic receptors and blocks postsynaptic alpha2-adrenergic receptors in the CNS by activating inhibitory neurons to decrease sympathetic outflow
Normal Daily Dose:
ADHD children: ?6 y of age, 0,1 mg ER po qhs, may titrate in increments of 0.1mg/d at weekly- max dose of 0.4 mg/d
HTN: 0.1 mg po bid, titrate by 0.1 mg/d at weekly intervals to 0.2-0.6 mg in 2 divided doses, max 2.4mg/d
Metabolism: extensive hepatic metabolism, unknown pathway
Plavix
Generic Name: clopidogrel
Class: platelet aggregation inhibitor
Uses: acute ST segment elevation MI managed/non-managed; Thrombosis prevention in arteriosclerotic vascular disease
MOA: antiplatelet agent that prevents platelet aggregation by direct inhibition of ADP binding to receptor sites, inhibiting subsequent activation of the glycoprotein IIb/IIIa complex
Normal Daily Dose:
acute ST segment elevation MI: 300-600 mg po loading dose, followed by 75 mg po daily
Thrombosis prevention: 75 mg po daily
Metabolism: Prodrug, requires activation by CYP2C19; substrate of CYP2C19, inhibitor of CYP2B6, 2C8
Welchol
Generic Name: colesevelam
Class: hypolipidemic, bile acid sequestrant
Uses: primary and familial hyperlipidemia, diabetes mellitus type 2
MOA: non absorbed, polymeric, lipid-lowering agent that binds intestinal bile acid resulting in the increased clearance of LDL-cholesterol and a reduction in total cholesterol
Normal Daily Dose: 1.875 g po bid or 3.75 g po daily
Metabolism: not absorbed
Pradaxa
Generic Name: dabigatran
Class: direct oral anticoagulant (DOAC)
Uses: treatment and prevention of initial or recurrent DVT and PE; prevention of stroke and systemic embolism in patient with nonvalvular atrial fibrillation; prevention of deep venous thromboembolism and PE after hip/knee replacement
MOA: a competitive, reversible, direct thrombin inhibitor
Normal Daily Dose: 150 mg po bid
Metabolism: extensive hepatic metabolism but not by CYP; substrate of P-glycoprotein
Digitek, Digox, Lanoxin
Generic Name: Digoxin
Class: Digitalis Glycoside
Uses: Atrial fibrillation; heart failure; supraventricular tachyarrhythmia
MOA: exert positive inotropic effects through improved availability of calcium to myocardial contractile elements, thereby increasing cardiac output in heart failure
Normal Daily Dose: loading dose of 0.25 mg po q2h to a total dose of 1.5 mg, then 0.125-0.375 mg po daily
Metabolism: Hepatic; substrate of P-glycoprotein
Cardizem, Cartia XT, Dilacor XR, Dilt-XR, Taztia XT, Tiazac
Generic Name: Diltiazem
Class: calcium channel blocker
Uses: hypertension, stable, chronic angina, atrial arrhythmia and paroxysmal supraventricular tachycardia
MOA: CCB drug that decreases HR, prolongs AV nodal conduction, and decreases arteriolar and coronary vascular tone
Normal Daily Dose: 180-360 mg po daily
Metabolism: extensive hepatic; substrate of CYP3A4/5, P-glycoprotein; moderate inhibitor of CYP3A4/5
Aggrenox, Persantine
Generic Name: Dipyridamole
Class: platelet aggregation inhibitor
Uses: thromboprophylaxis after heart valve replacement
MOA: inhibits the uptake of adenosine into platelets, endothelial cells, and erythrocytes resulting in a increase in local concentrations of adenosine, which is a coronary vasodilator and a platelet aggregation inhibitor
Normal Daily Dose: 75-100 mg po qid as an adjunct to warfarin therapy
Metabolism: extensive metabolized but not by CYP; inhibits P-glycoprotein
Cardura
Generic Name: Doxazosin
Class: alpha 1-adrenergic blocker
Uses: benign prostatic hyperplasia, hypertension
MOA: selectively blocks postsynaptic alpha 1-adrenergic receptors, reducing peripheral resistance through arterial and venous dilations
Normal Daily Dose: 1 mg po daily, may titrate to 1-8 mg po daily
Metabolism: extensive hepatic; substrate of CYP3A4/5
Vasotec
Generic Name: enalapril
Class: ACE inhibitor, antihypertensive
Uses: heart failure; hypertension; kidney disease, nondiabetic
MOA: a prodrug that is rapidly converted to its active metabolite, enalaprilat, a competitive ACE inhibitor. It reduces serum aldosterone, leading to decreased sodium retention, potentiates the vasodilator kallikrein
Normal Daily Dose: 2.5-5 mg po daily
Metabolism: extensive hepatic to 1 active metabolite
Lovenox
Generic Name: enoxaparin
Class: anticoagulant, low-molecular-weight heparin
Uses: DVT prophylaxis, acute ST-segment elevation AMI, unstable angina
MOA: a low-molecular-weight heparin which has anti-factor Xa and IIa properties
Normal Daily Dose: 40 mg SUBQ
Metabolism: Hepatic
Zetia
Generic Name: ezetimibe
Class: antihyperlipidemic, cholesterol absorption inhibitor
Uses: familial, mixed, primary hypercholesterolemia
MOA: localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver
Normal Daily Dose: 10 mg po daily
Metabolism: In intestine and liver, not via CYP450
Plendil
Generic Name: Felodipine
Class: calcium channel blocker, dihydropyridine
Uses: hypertension
MOA: CCB drug with potent arterial and coronary vasodilating properties
Normal Daily Dose: 2.5-5 mg po once daily
Metabolism: extensive hepatic metabolism, CYP3A4/5 substrate; moderate CYP2C8 inhibitor
Antara, Fenoglide, Lipofen, Lofibra, Trillpix
Generic Name: Fenofibrate
Class: antihyperlipidemic
Uses: hypertriglyceridemia
MOA: fibric acid derivatives activate peroxisome proliferator-activated receptor a (PPARa), which increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-11
Normal Daily Dose: 54-160mg po daily
Metabolism: prodrug that undergoes rapid hydrolysis at the ester bond to Feno fibric acid; fenofibric acid is glucuronidated in the liver
Monopril
Generic Name: fosinopril
Class: ACE inhibitor, Antihypertensive
Uses: Heart failure, hypertension
MOA: competitive ACE Inhibitor, it reduces serum aldosterone, leading to decreased sodium retention, potentiates the vasodilator kallikrein-kinin system
Normal Daily Dose:
heart failure: 5-10 mg po daily, may titrate to 40 mg po daily
HTN: 10 mg po daily, may titrate to 80 mg po daily
Metabolism: metabolized in liver to active metabolite (fosinoprilat) not via CYP450
Lasix
Generic Name: furosemide
Class: loop diuretic
Uses: edema of volume overload related to heart failure, renal failure
MOA: a loop diuretic that is actively secreted via the nonspecific organic acid transport system into the lumen of the thick ascending limb of Henle’s loop, where it decreases sodium reabsorption by competing for the chloride site on the NA+ -K -2Cl- cotransporter
Normal Daily Dose: initial 20-80 mg po daily, may titrate to maintenance dose (max 600 mg/d)
Metabolism:
Lopid
Generic Name: gemfibrozil
Class: antihyperlipidemic, fibric acid
Uses: coronary arteriosclerosis; prophylaxis-familial combined hyperlipidemia; familial type V hyperlipoproteinemia
MOA: fibric acid derivatives activate PPAR-alpha, which increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III
Normal Daily Dose: 600 mg po bid
Metabolism: <20% hepatic, CYP3A4/5 substrate. Inhibitor of CYP1A2 (moderate), CYP2C19 (strong), CYP2C8 (strong), CYP2C9 (strong)
