Comparative Pharmacology
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE versus ZESTORETIC.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE versus ZESTORETIC.
AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE vs ZESTORETIC
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Amlodipine is a dihydropyridine calcium channel blocker that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle, causing peripheral vasodilation and reduction of peripheral vascular resistance. Benazepril is a prodrug that is hydrolyzed to benazeprilat, a competitive inhibitor of angiotensin-converting enzyme (ACE), preventing conversion of angiotensin I to angiotensin II, thereby reducing vasoconstriction, aldosterone secretion, and sodium and water retention.
Combination of lisinopril (ACE inhibitor) and hydrochlorothiazide (thiazide diuretic). Lisinopril inhibits angiotensin-converting enzyme, reducing angiotensin II formation, decreasing vasoconstriction and aldosterone secretion. Hydrochlorothiazide inhibits sodium reabsorption in distal convoluted tubule, increasing diuresis and reducing plasma volume.
Oral, one capsule daily. Initial: 2.5 mg/10 mg for patients not on either drug; up to 10 mg/40 mg daily.
Zestoretic (lisinopril/hydrochlorothiazide) is available in fixed-dose combinations. Typical adult dose: 10 mg/12.5 mg, 20 mg/12.5 mg, or 20 mg/25 mg orally once daily. Maximum dose: lisinopril 80 mg/day, hydrochlorothiazide 50 mg/day.
None Documented
None Documented
Amlodipine terminal half-life 30-50 hours (allows once-daily dosing; steady state reached after 7-10 days). Benazeprilat effective half-life 10-11 hours (accumulation minimal).
Lisinopril: terminal half-life approximately 12 hours (accumulation half-life 13.8 hours in patients with normal renal function). Hydrochlorothiazide: terminal half-life 5.6–14.8 hours (mean 9.6 hours).
Amlodipine: 60% renal (10% unchanged, rest as metabolites), 20-25% biliary/feces. Benazepril: 11-12% renal (as unchanged benazepril and benazeprilat), 85-90% biliary (as benazeprilat conjugates).
Lisinopril is excreted unchanged in urine; 100% renal elimination. Hydrochlorothiazide is excreted primarily by the kidney (≥95% as unchanged drug) via tubular secretion.
Category D/X
Category C
ACE Inhibitor
ACE Inhibitor + Diuretic