Comparative Pharmacology
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND VALSARTAN versus BENICAR HCT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMLODIPINE BESYLATE AND VALSARTAN versus BENICAR HCT.
AMLODIPINE BESYLATE AND VALSARTAN vs BENICAR HCT
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Amlodipine is a dihydropyridine calcium channel blocker that inhibits the influx of calcium ions into vascular smooth muscle and cardiac muscle, causing vasodilation and reduced peripheral vascular resistance. Valsartan is an angiotensin II receptor blocker that selectively blocks the binding of angiotensin II to AT1 receptors, resulting in vasodilation and reduced aldosterone secretion.
Combination of an angiotensin II receptor blocker (ARB) and a thiazide diuretic. Olmesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively antagonizing the AT1 receptor. Hydrochlorothiazide inhibits the sodium-chloride symporter in the distal convoluted tubule, increasing excretion of sodium, chloride, and water, thereby reducing plasma volume.
Adults: initial combination therapy 5/160 mg (amlodipine/valsartan) orally once daily; titrate based on response, maximum 10/320 mg once daily.
One tablet orally once daily. Available strengths: 40 mg olmesartan / 12.5 mg hydrochlorothiazide, 40 mg olmesartan / 25 mg hydrochlorothiazide. Dose may be titrated after 2-4 weeks based on response.
None Documented
None Documented
Amlodipine: 30-50 hours (terminal); Valsartan: 6-9 hours. Amlodipine's long half-life allows once-daily dosing; steady state achieved after 7-10 days.
Olmesartan: Terminal elimination half-life is 10-15 hours, supporting once-daily dosing. Hydrochlorothiazide: Terminal half-life is 5.6-14.8 hours (mean ~10 hours), prolonged in renal impairment.
Amlodipine: ~60% renal (10% as unchanged drug), ~20-25% biliary/fecal. Valsartan: ~83% fecal via biliary, ~13% renal (mainly unchanged).
Olmesartan: Approximately 50-65% of absorbed dose excreted in urine (10-20% as unchanged drug, remainder as metabolites), 35-50% in feces via biliary excretion. Hydrochlorothiazide: ≥95% excreted renally as unchanged drug.
Category D/X
Category C
ARB
ARB + Thiazide Diuretic