Amlodipine:Absorption Tmax is 6 to 12 h.
Distribution Bioavailability is 64% to 90%. About 93% is protein bound.
Metabolism About 90% is converted to inactive metabolites in the liver.
Elimination 10% of the parent compound and 60% of the metabolites are excreted in the urine. Elimination is biphasic. T½ is about 30 to 50 h.
Duration 24 h.
Special Populations Hepatic Function Impairment Clearance is decreased and AUC may increase about 40% to 60%. May require lower initial dose.
Elderly Clearance is decreased and AUC may increase about 40% to 60%. May require lower initial dose.
Moderate to severe heart failure Clearance is decreased and AUC may increase about 40% to 60%. May require lower initial dose.
Valsartan:Absorption T max is 2 to 4 h after dosing. Bioavailability is about 10% to 35%. Food decreases AUC about 40% and decreases C max about 50%.
Distribution Vd is about 17 L. Highly bound to albumin (about 95%).
Metabolism The major metabolite, valeryl 4-hydroxy valsartan, accounts for about 9% of the dose.
Elimination Half-life is about 6 h. Valsartan is primarily recovered in the feces (about 83%) and urine (about 13%). Recovery is mainly unchanged drug, with only about 20% of the dose recovered as metabolite. The plasma Cl is about 2 L/h.
Special Populations Renal Function Impairment No correlation between renal function and exposure to the drug.
Hepatic Function Impairment Patients with mild to moderate chronic liver disease have about twice the AUC value.
Elderly AUC is about 70% higher and t ½ is about 35% longer in elderly patients.
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