Amlodipine besylate is a long-acting dihydropyridine calcium channel blocker that exerts its effect by blocking the transmembrane influx of calcium ions into cardiac and vascular smooth muscles.
Valsartan is a nonpeptide angiotensin II antagonist that selectively blocks the binding of angiotensin II to the AT 1 receptors in tissues such as vascular smooth muscle and the adrenal gland.
藥動學
Amlodipine:
Bioavailability: (oral), 64% to 90%.
Vd: 21 L, protein binding: 93%.
Metabolism: Liver: about 90%.
Elimination Half Life: about 30 to 50 h.
Valsartan:
Bioavailability: (oral), 10% to 35%.
Vd: 17 L, protein binding: 95%.
Metabolism: Liver: CYP2C9 9%.
Elimination Half Life: about 6h (IV data).
禁忌症
Hypersensitivity to amlodipine, valsartan, or any other component.
Concomitant aliskiren use in patients with diabetes.