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      Pharmacokinetics and Pharmacodynamics of Amlodipine

      Cardiology

      S. Karger AG

      Pharmacokinetics, Pharmacodynamics, Amlodipine

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          Abstract

          Amlodipine is a low-clearance, dihydropyridine calcium antagonist. The slow rate of elimination (elimination half-life of 40-60 h) confers several pharmacokinetic characteristics that are not seen with other calcium-antagonist drugs. It has high oral bioavailability (60-80%) and accumulates to a steady-state with once-daily administration over a period of 1-1 ½ weeks. Fluctuation of plasma drug concentration between doses is between 20 and 25% when once-daily dosing is used. Onset of effect is gradual after oral administration which is due, in part, to an intermediate rate of drug absorption (peak plasma drug concentration occurs 6-8 h after dosing) and perhaps also to the physicochemical characteristics of the drug-cell membrane-receptor interaction. The pharmacodynamic profile of the drug in hypertensive patients is consistent with the disposition of the drug. After single doses, blood pressure decreases gradually over 4-8 h and may slowly return to baseline over 24-72 h. No change in heart rate is noted after the dose as the onset is gradual and physiological reflexes are not activated. During chronic, oral, once-daily dosing blood pressure is decreased from pretreatment baseline with little fluctuation over the 24-hour dose interval. Discontinuation of amlodipine treatment results in a slow return of blood pressure to baseline over 7-10 days, with no evidence of a ‘rebound’ effect. Amlodipine is a low-clearance, dihydropyridine calcium antagonist which is effective for the treatment of hypertension and angina pectoris with once-daily dosing.

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          Author and article information

          Journal
          CRD
          Cardiology
          10.1159/issn.0008-6312
          Cardiology
          S. Karger AG
          978-3-8055-5613-2
          978-3-318-01670-3
          0008-6312
          1421-9751
          1992
          1992
          12 November 2008
          : 80
          : Suppl 1
          : 31-36
          Affiliations
          Division of Clinical Pharmacology, Brown University, Department of Medicine, Roger Williams General Hospital, Providence, R.I., USA
          Article
          175050 Cardiology 1992;80:31–36
          10.1159/000175050
          1534713
          © 1992 S. Karger AG, Basel

          Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher. Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug. Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements.

          Page count
          Pages: 6
          Categories
          Session II

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