Comparative Pharmacology
Head-to-head clinical analysis: DILACOR XR versus LEXXEL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DILACOR XR versus LEXXEL.
DILACOR XR vs LEXXEL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Diltiazem inhibits calcium ion influx across cardiac and vascular smooth muscle cells, resulting in dilation of coronary and systemic arteries, decreased myocardial contractility, and reduced sinoatrial and atrioventricular conduction velocity.
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.
180 to 240 mg orally once daily, administered on an empty stomach; maximum dose 480 mg once 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
Terminal half-life: 6-12 hours (prolonged in elderly, hepatic impairment, or with CYP3A4 inhibitors)
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.
Renal (70% as metabolites, 3-4% as unchanged drug); biliary/fecal (25-30%)
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 C
Category C
Calcium Channel Blocker
ACE Inhibitor + Calcium Channel Blocker