Comparative Pharmacology
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE versus PRINIVIL.
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE versus PRINIVIL.
AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE vs PRINIVIL
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 is an angiotensin-converting enzyme inhibitor that decreases angiotensin II production, reducing vasoconstriction and aldosterone secretion, leading to decreased blood pressure.
Oral, one capsule daily. Initial: 2.5 mg/10 mg for patients not on either drug; up to 10 mg/40 mg daily.
Initial dose 10 mg orally once daily; titrate to target dose of 20-40 mg daily based on blood pressure response.
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 approximately 12 hours, with accumulation noted in renal impairment; effective half-life at steady state extends to 30-50 hours in patients with creatinine clearance <30 mL/min.
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).
Renal excretion accounts for approximately 60% of total clearance, primarily as unchanged lisinopril; fecal excretion accounts for negligible amounts.
Category D/X
Category C
ACE Inhibitor
ACE Inhibitor