Comparative Pharmacology
Head-to-head clinical analysis: EXFORGE HCT versus LONITEN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXFORGE HCT versus LONITEN.
EXFORGE HCT vs LONITEN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
EXFORGE HCT is a combination of amlodipine (a dihydropyridine calcium channel blocker), valsartan (an angiotensin II receptor blocker), and hydrochlorothiazide (a thiazide diuretic). Amlodipine inhibits calcium ion influx across cardiac and vascular smooth muscle cells, leading to vasodilation. Valsartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II. Hydrochlorothiazide increases excretion of sodium and water by inhibiting the Na+/Cl- symporter in the distal convoluted tubule.
Minoxidil is a potassium channel opener that causes direct vasodilation of peripheral arteries. It reduces peripheral vascular resistance and blood pressure by hyperpolarizing vascular smooth muscle cells via activation of ATP-sensitive potassium channels.
One tablet orally once daily. Initial dose based on previous antihypertensive therapy; maximum dose is one tablet of 10 mg amlodipine/320 mg valsartan/25 mg hydrochlorothiazide per day.
10 mg orally twice daily, titrated to 40 mg twice daily for hypertension; for heart failure, start at 2.5-5 mg orally twice daily, max 20 mg twice daily.
None Documented
None Documented
Valsartan: 6 hours (terminal). Amlodipine: 30-50 hours (terminal), permits once-daily dosing. Hydrochlorothiazide: 6-15 hours (terminal).
Terminal elimination half-life: 4.2 hours (range 3.5–5.5); clinically, half-life extends to 14–23 hours after chronic dosing due to drug accumulation.
Valsartan: 13% excreted unchanged in urine, 83% in feces via biliary secretion. Amlodipine: 10% excreted unchanged in urine, 60% as metabolites in urine, 20-25% in feces. Hydrochlorothiazide: ≥95% excreted unchanged in urine.
Renal: 85% (12% unchanged, 73% as glucuronide conjugates); biliary/fecal: 3%
Category C
Category C
Antihypertensive
Antihypertensive