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).