Comparative Pharmacology
Head-to-head clinical analysis: EXFORGE HCT versus FENOLDOPAM MESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXFORGE HCT versus FENOLDOPAM MESYLATE.
EXFORGE HCT vs FENOLDOPAM MESYLATE
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.
Dopamine D1-like receptor agonist (D1 and D5) causing vasodilation in renal, mesenteric, coronary, and cerebral arteries; increases renal blood flow and natriuresis.
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.
0.1 to 0.3 mcg/kg/min IV continuous infusion, titrated every 15-20 minutes by 0.05-0.1 mcg/kg/min; max dose 1.6 mcg/kg/min.
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 approximately 10 minutes (range 5–20 min) in healthy adults; clinically, continuous infusion is required to maintain therapeutic effect due to rapid clearance.
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 (80% as metabolites, 10% as unchanged drug); fecal/biliary minor (10%)
Category C
Category C
Antihypertensive
Antihypertensive