Comparative Pharmacology
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE versus ZESTRIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE versus ZESTRIL.
AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE vs ZESTRIL
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.
Lisinopril competes with angiotensin I for binding to angiotensin-converting enzyme (ACE), inhibiting its activity, thereby preventing conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. This leads to decreased blood pressure, reduced aldosterone secretion, and decreased sodium and water retention.
Oral, one capsule daily. Initial: 2.5 mg/10 mg for patients not on either drug; up to 10 mg/40 mg daily.
10 mg orally once daily initially; titrate to 20-40 mg orally once daily. Maximum 80 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).
Terminal elimination half-life is about 12 hours for lisinopril; in heart failure, half-life may be prolonged. Steady-state achieved in 2-3 days.
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).
Primarily renal (approximately 70% unchanged), with the remainder excreted as inactive metabolites via feces and urine.
Category D/X
Category C
ACE Inhibitor
ACE Inhibitor