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Öğe Bioavailability file: Amlodipine(Ankara University, 2011) Kaynak M.S.; Bogacz A.; Stelmasi?ski M.; Şahin S.Amlodipine (AML), a third-generation dihydropiridin, is a long-acting L-calcium channel blocker used in the treatment of hypertension and angina pectoris. It exerts its effects by blocking the voltage-dependent L-calcium channels and binding to both dihydropiridin and nondihydropiridin binding sites. AML is well absorbed (96%) after oral administration and its bioavailability is between 64-90%. Its volume of distribution is about 16 to 21 L/kg and protein binding is 98% after oral administration. AML is extensively metabolized in the liver and its elimination from the plasma is biphasic with a terminal half-life of 30 to 50 h. It is excreted by renal route about 60%. According to Biopharmaceutics Classification System, AML is classified as class I drug by WHO. In this review physicochemical properties, pharmacology, analytical methods, pharmacokinetics and bioavailability of amlodipine are discussed.
