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FABAD  J. Pharm. Sci.
ISSN 1300-4182
Copyright Ó 2011 FABAD. All rights reserved 

FABAD J. Pharm. Sci., 36(4), 207-222, 2011. PDF (615 KB)

Scientific Review

ABSTRACT

Bioavailability File: Amlodipine
 Mustafa Sinan KAYNAK*
,°, Agata BOGACZ*,***, Michał STELMASIN´ SKI*,***, Selma ŞAHİN**
 * İnönü University, Faculty of Pharmacy, Department of Pharmaceutical Technology, 44280 MALATYA, TURKEY
 ** Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Technology, 06100 Ankara, TURKEY
 *** İnönü University, Faculty of Pharmacy, Undergraduate ERASMUS Exchange Student, 44280, MALATYA, TURKEY.
 ° Corresponding Author E-mail: mustafa.kaynak@inonu.edu.tr


Summary


Bioavailability File: Amlodipine
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.

Key Words :
Amlodipine, Bioavailability, Pharmacokinetics, Biopharmaceutics Classification System (BCS).