PMID: 7515992Mar 1, 1994Paper

Pharmacokinetics of amlodipine and its occupancy of calcium antagonist receptors

Journal of Cardiovascular Pharmacology
S YamadaR Kimura

Abstract

We characterized the occupancy of dihydropyridine (DHP) calcium antagonist receptors by amlodipine in spontaneously hypertensive rats (SHR) in relation to its pharmacokinetics. Oral administration of amlodipine (10 mg/kg) in SHR produced a significant (20-70%) decrease in the number of specific (+)[3H]PN 200-110 binding sites in cardiac tissues 0.5-18 h later, and the effect was greatest 3 h later. In these rats, there was little change in cerebral cortical (+)[3H]PN 200-110 binding. Occupancy of cardiac calcium antagonist receptors after oral administration of amlodipine correlated well with its plasma concentration. In vitro blockade of cardiac (+)[3H]PN 200-110 binding sites induced by amlodipine also persisted after the tissues were washed by centrifugation and suspension, whereas that induced by nifedipine was reversible under these conditions. Thus, our results suggest that the gradual onset and long-lasting pharmacologic effect of amlodipine are due to its slow binding kinetics (association and dissociation) of cardiovascular receptor sites in addition to its slow pharmacokinetics.

Citations

Aug 31, 2001·Pharmacology, Biochemistry, and Behavior·R M KamińskiS J Czuczwar
Dec 7, 2013·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Gianfranco Parati, Helmut Schumacher
May 22, 1998·Journal of Veterinary Internal Medicine·K L Cooke, P S Snyder
Mar 28, 2012·Annals of Neurology·Connie MarrasPeter C Austin
Dec 22, 2000·Neurobiology of Learning and Memory·D QuartermainA Kwan

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