Comparative Pharmacology
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE versus LEXXEL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE versus LEXXEL.
AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE vs LEXXEL
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.
LEXXEL is a combination of felodipine, a dihydropyridine calcium channel blocker that inhibits calcium influx into vascular smooth muscle and cardiac muscle, causing vasodilation and reduced myocardial contractility, and enalapril, an angiotensin-converting enzyme (ACE) inhibitor that prevents conversion of angiotensin I to angiotensin II, reducing vasoconstriction, aldosterone secretion, and sodium reabsorption.
Oral, one capsule daily. Initial: 2.5 mg/10 mg for patients not on either drug; up to 10 mg/40 mg daily.
1 tablet (felodipine 5 mg / enalapril 5 mg) orally once daily, may increase to 2 tablets once daily after 2-4 weeks if needed.
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).
Enalapril: ~1.3 hours; Enalaprilat: terminal half-life ~35-38 hours, with multiple-dose accumulation half-life ~11 hours; effective half-life for ACE inhibition ~24 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).
Renal: ~35-50% as unchanged drug (enalaprilat), biliary/fecal: ~15-30% as metabolites and unchanged drug; total renal elimination of enalaprilat accounts for ~60-80% of dose.
Category D/X
Category C
ACE Inhibitor
ACE Inhibitor + Calcium Channel Blocker