Comparative Pharmacology
Head-to-head clinical analysis: LEXXEL versus QUINAPRIL HYDROCHLORIDE AND HYDROCHLOROTHIAZIDE.
Head-to-head clinical analysis: LEXXEL versus QUINAPRIL HYDROCHLORIDE AND HYDROCHLOROTHIAZIDE.
LEXXEL vs QUINAPRIL HYDROCHLORIDE AND HYDROCHLOROTHIAZIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Quinapril is an ACE inhibitor that inhibits the conversion of angiotensin I to angiotensin II, reducing vasoconstriction and aldosterone secretion; hydrochlorothiazide is a thiazide diuretic that inhibits sodium reabsorption in the distal convoluted tubule, increasing excretion of sodium and water.
1 tablet (felodipine 5 mg / enalapril 5 mg) orally once daily, may increase to 2 tablets once daily after 2-4 weeks if needed.
Initial: 10/12.5 mg (quinapril/hydrochlorothiazide) orally once daily. Titrate based on response to a maximum of 40/25 mg once daily.
None Documented
None Documented
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.
Quinaprilat terminal half-life ~25 hours (effective half-life ~12 hours); hydrochlorothiazide ~6-15 hours (increased in renal impairment).
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.
Renal excretion of quinaprilat (active metabolite) ~50-60% unchanged; hydrochlorothiazide ~70% unchanged. Biliary/fecal elimination accounts for <10% for both components.
Category C
Category D/X
ACE Inhibitor + Calcium Channel Blocker
ACE Inhibitor