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DMAT PA-1 PHARMACY CACHE CARDIOVASCULAR AGENTS Saundra Martino, RpH ANGIOTENSIN CONVERTING ENZYME INHIBITORS • • • LISINOPRIL 20MG TABS ENALAPRIL 1.25 MG/ ML INJ 2ML Inhibit conversion of Angiotensin I ---------------> Angiotensin II (weak vasoconstrictor) (potent vasoconstrictor) reduces aldosterone output (na reabsorption in kidney) USES: Congestive heart failure Hypertension …..peripheral vasodilation/dec in total peripheral vascular resistance dec blood pressure dec workload on heart inc renal blood flow ……dec fluid volume/dec water retention inc in potassium levels reflex inc in renin secretion • KEY FACTS: chronic cough in up to 39% of patients first dose may cause profound dec in blood pressure angioedema—can occur at anytime during treatment esp. with blacks hyperkalemia>4% Never use in pregnancy dec. dose if CrCl<30ml/min CASCADE: renin--angiotensinogen----angiotensin I---angiotensin II----aldosterone BETA-BLOCKERS • • • • • ATENOLOL 50MG TABS METOPROLOL TARTRATE 50MG TABS METOPROLOL INJ 1MG/ML 5ML PROPRANOLOL HCL 20MG TABS PROPRANOLOL INJ 1MG/ML MULTIPLE MECHANISMS: dec release of renin from kidneys dec stimulation of sympathetic NS in heart & vascular smooth muscle negative chronotropic effect negative inotropic effect some posess antiarrhythmic properties / class II antiarrhythmic B1 receptors : heart, vascular smooth muscle B2 receptors: lungs (bronchioles), uterus dec peripheral vasoconstriction .. Dec bp systolic & diast olic dec fluid retention dec HR both resting & exercise dec cardiac output dec in myocardial oxygen demand inhibit reflex response to orthostatic hypotension USES: Angina Hypertension Migraine prophylaxis Tremors Arrhythmias Pheochromocytoma KEY FACTS; *B1 selective can lose their selectivity at high doses –then block b2 receptors—causes problems in asthmatics *Caution use with asthma, COPD, lung disease---may cause bronchospasms *Caution with diabetics—may cause hypoglycemia *Slowly wean off over 1-2 weeks abrupt d/c can cause exacerbation of angina, MI, ventricular arrhythmias CALCIUM CHANNEL BLOCKERS • • • • NIFEDIPINE 10MG CAPS VERAPAMIL 80MG TABS VERAPAMIL SR 240MG TABS DILTIAZEM HCL INJ. 5MG/ML 5ML USES: Angina Hypertension Supraventricular arrhythmias Inhibit influx of extracellular calcium across the myocardial & peripheral vascular smooth muscle membranes---this inhibits contactile process of myocardial smooth muscle cells --causes relaxation dilation of coronary & systemic arteries inc coronary blood flow Verapamil & Diltiazem depress impulse formation at SA & AV nodes antiarrhythmics /class IV antiarrhythmics slows conduction velocity dec automaticity depresses SA nodal firing KEY FACTS: inc oxygen to myocardial tissue dec in total peripheral resistance dec blood pressure dec afterload dec heart rate DIURETICS • • • HYDROCHLOROTHIAZIDE 25MG TABS FUROSEMIDE 40MG TABS FUROSEMIDE INJ 10MG/ML 10ML USES: Edema Hypertension affect electrolyte transport in kidneys Thiazide Diuretics inhibit Na reabsorption at a point distal to Loop Of Henle get inc excretion of Na & water dec in total fluid volume alter carbohydrate metabolism therefore inc in glucose can inc effectiveness of other antihypertensive agents by preventing reexpansion of extracellular & plasma volumes ineffective iif CrCl<,30ml/min caution with diabetics can exacerbate hyponatremia & hyperg;lycemia sulfonamide derivatives-- pho tosensitivity potassium loss Loop Diuretics inhibit Na reabsorption at Loop of Henle get inc excretion of Na & water interferes with Mg reabsorption at Loop of Henle hypomagnesemia very potent can exacerbate SLE ototoxicity with injectable can cause overdiuresis orthostatic hypotension, electrolyte imbalances & volume depletion can cause hyperglycemia sulfonamide derivatives…photosensitivity potassium loss CARDIAC GLYCOSIDES • • DIGOXIN 0.125MG TABS DIGOXIN INJ 0.25MG/ML 2ML Increase myocardial contractility & efficiency produce positive inotropic effect produce negative chronotropic effect inc cardiac output improve systemic circulation Improve renal perfusion reduce edema effects on electrical activity of heart dec/slows ventricuar rate Digoxin ,makes the heart beat stronger with more regular rhythms !!!!! USES: Congestive heart failure Atrial fibrillation KEY FACTS: narrow therapeutic index NITRATES • • • • NITROGLYCERIN SL 0.4MG TABS NITROGLYCERIN TRANSDERM 0.2MG/HR NITROGLYCERIN INJ. 5MG/ML 10M ISOSORBIDE 10MG TABS vasodilation peripheral veins, peripheral arteries, & coronary arteries dec blood flow to heart dec ventricular filling pressures dec myocardial work—dec oxygen demand dec in anginal pain By dec pressure in cardiac tissue facilitate collateral circulation inc blood distribution to ischemic areas Tolerance…develops within 24-48 hours prevent with a nitrate-free period of 8-12 hours interaction with PDE5 inhibitors—additive vasodilation—potentially fatal hypotension USES: relief of anginal pain dec preload dec afterload Decrease workload of heart—dec oxygen demand !!!!!! CENTRALLY ACTING ALPHA2 AGONIST • CLONIDINE 0.1MG TABS stimulation of alpha2 receptors inhibitory effect on sympathetic nervous system dec in heart rate dec in peripheral resistance dec in blood pressure dec cardiac output dec in stroke volume USES: Hypertension ADHD (attention-deficit hyperac tivity disorder) abrupt withdrawl after prolonged treatment can lead to hypertensive crisis Tricyclic antidepressants & beta-blockers enhance potential for hypertensive crisis upon withdrawl Can cause drowsiness Can exacerbate depression DIRECT VASODILATORS • HYDRALAZINE 20MG/ML 1ML USES: Hypertensive crisis peripheral vasodil;ator relaxes arterial smooth muscle dec peripheral vascular resistance dec blood pressure (diastolic more than systolic) reflex autonomic response inc hr, stroke volume, cardiac output, left ventricular ejection fraction inc plasma renin activity • • • • • Dosage adjustments needed in renal impairment Risk of drug-induced SLE Never a single agent ---used with diuretic or beta-blocker in hypertensive emergencies produces reflex tachycardia Affected by genetic variation