Comparative Pharmacology
Head-to-head clinical analysis: EXFORGE HCT versus SERPALAN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXFORGE HCT versus SERPALAN.
EXFORGE HCT vs SERPALAN
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.
Selective serotonin reuptake inhibitor (SSRI) that potentiates serotonergic activity in the CNS by blocking the reuptake of serotonin at the presynaptic terminal.
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.
100 mg orally 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 is 12-14 hours in adults with normal renal function; prolonged to 24-36 hours in moderate renal impairment (CrCl 30-50 mL/min) and up to 60 hours in severe renal impairment (CrCl <30 mL/min).
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.
Primarily renal elimination (60-70% unchanged drug), with 20-30% biliary/fecal excretion as metabolites; less than 10% excreted unchanged in feces.
Category C
Category C
Antihypertensive
Antihypertensive