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Pharmacokinetic and Antihypertensive Profile of Amlodipine and Felodipine-ER in Young Versus Older Hypertensives.

Author(s): Leenen FH, Coletta E

Affiliation(s): Hypertension Unit, University of Ottawa Heart Institute, Ottawa, ON Canada.

Publication date & source: 2010-09-25, J Cardiovasc Pharmacol., [Epub ahead of print]

To evaluate the impact of age on the pharmacokinetics and blood pressure (BP) responses of a dihydropyridine (DHP) with large versus small first-pass metabolism in hypertensive subjects, young (n=28) and older (n=35) hypertensives were randomized to placebo, felodipine-ER 5mg/day or amlodipine 5mg/day. In the young subjects, the first dose of either DHP did not decrease BP, and chronic dosing by approximately 10 mmHg, which had disappeared by 24 hrs. In the older group felodipine-ER decreased systolic BP by approximately 10 mmHg after the first dose and by approximately 20 mmHg after chronic dosing which had disappeared after 24 hrs. The first dose of amlodipine caused a gradual fall in BP, and chronic dosing by approximately 20 mmHg, and still by approximately 10 mmHg at 120 hrs. Older subjects showed approximately 30% higher AUC and plasma concentrations of felodipine and amlodipine, but (apparent) elimination half lives did not differ between younger and older subjects. The chronic antihypertensive responses correlated well with both plasma levels and pre-treatment BP. Age has only a modest impact on the pharmacokinetics of amlodipine and felodipine-ER, but markedly affects the BP response to the first dose of either DHP and the duration of action after chronic dosing of amlodipine.

Page last updated: 2010-10-05

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