Comparative Pharmacology
Head-to-head clinical analysis: AMLODIPINE BESYLATE VALSARTAN AND HYDROCHLOROTHIAZIDE versus AVALIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMLODIPINE BESYLATE VALSARTAN AND HYDROCHLOROTHIAZIDE versus AVALIDE.
AMLODIPINE BESYLATE, VALSARTAN AND HYDROCHLOROTHIAZIDE vs AVALIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Amlodipine is a dihydropyridine calcium channel blocker that inhibits calcium ion influx across cardiac and vascular smooth muscle cells, causing vasodilation and reduced peripheral resistance. Valsartan is an angiotensin II receptor blocker (ARB) that selectively blocks AT1 receptors, inhibiting vasoconstriction and aldosterone release. Hydrochlorothiazide is a thiazide diuretic that inhibits the Na+/Cl- symporter in the distal convoluted tubule, increasing sodium and water excretion.
Avalide is a combination of an angiotensin II receptor blocker (irbesartan) and a thiazide diuretic (hydrochlorothiazide). Irbesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively antagonizing the AT1 receptor. Hydrochlorothiazide increases sodium and water excretion by inhibiting the Na+/Cl- symporter in the distal convoluted tubule.
One tablet orally once daily. Available strengths: amlodipine 5 mg/valsartan 160 mg/HCTZ 12.5 mg, amlodipine 5 mg/valsartan 160 mg/HCTZ 25 mg, amlodipine 10 mg/valsartan 160 mg/HCTZ 12.5 mg, amlodipine 10 mg/valsartan 160 mg/HCTZ 25 mg, amlodipine 10 mg/valsartan 320 mg/HCTZ 25 mg. Titrate based on response, max dose: amlodipine 10 mg/valsartan 320 mg/HCTZ 25 mg daily.
AVALIDE (irbesartan/hydrochlorothiazide) is available as tablets containing 150/12.5 mg, 300/12.5 mg, or 300/25 mg. The typical starting dose is 150/12.5 mg once daily, titrated to 300/12.5 mg once daily as needed. Maximum dose is 300/25 mg once daily.
None Documented
None Documented
Amlodipine: 30-50 hours (terminal, allows once-daily dosing); Valsartan: 6 hours; Hydrochlorothiazide: 6-15 hours (prolonged in renal impairment).
Irbesartan: 11-15 h (terminal), HCTZ: 6-15 h (terminal). Clinical context: Steady state reached in 3-5 days; allows once-daily dosing.
Amlodipine: 60% renal, 20-25% biliary/fecal; Valsartan: 83% fecal via bile, 13% renal; Hydrochlorothiazide: ≥95% renal as unchanged drug.
Renal: HCTZ ~70% unchanged; Irbesartan ~20% unchanged, remainder as metabolites via biliary (60%) and renal (20%). Combined: Renal ~50%, biliary/fecal ~50%.
Category D/X
Category C
ARB
ARB and Thiazide Diuretic Combination