Comparative Pharmacology
Head-to-head clinical analysis: EXFORGE HCT versus RAPLON.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXFORGE HCT versus RAPLON.
EXFORGE HCT vs RAPLON
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.
RAPLON (levosimendan) is a calcium sensitizer that increases myocardial contractility by sensitizing troponin C to calcium, and it also opens ATP-sensitive potassium channels, causing vasodilation.
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.
0.2 mg/kg IV bolus over 30 seconds; may repeat once if necessary after 15 minutes.
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 approximately 1.5-2.5 hours in patients with normal renal function; prolonged in renal impairment (up to 6-8 hours in end-stage renal disease).
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 excretion of unchanged drug (approximately 80-90% of administered dose within 24 hours); minor biliary/fecal elimination (less than 10%).
Category C
Category C
Antihypertensive
Antihypertensive