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      Lack of Tolerance Development after Long-Term Administration of the Partial Beta-Adrenoceptor Agonist Xamoterol

      , ,

      Cardiology

      S. Karger AG

      Xamoterol, β-Adrenergic receptors, Heart failure

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          Abstract

          Xamoterol is a selective partial β-adrenoceptor agonist. In a double-blind randomized placebo-controlled study, 30 patients (1 female, 29 male) with mild to moderate heart failure were treated with 200 mg of xamoterol twice daily or placebo during 3 months. At baseline and 72 h after the last tablet intake, the hemodynamic and humoral effects of a single intravenous dose of xamoterol (0.2 mg/kg) were assessed by right heart catheterization. At baseline, intravenous xamoterol raised resting heart rate by 3 % (NS) in the placebo and by 6% (NS) in the xamoterol group. On exercise, heart rate was reduced by 10% (p = 0.015) and 7% (p = 0.016), respectively. Pulmonary capillary wedge pressure (PCWP) dropped in both groups: at rest by 4 mm Hg (p = 0.0004) in the placebo group and by 6 mm Hg (p = 0.0002) in the xamoterol group; on exercise by 1 mm Hg (NS) in the placebo and by 6 mm Hg (p = 0.0001) in the xamoterol group. Similar changes of all variables were obtained after long-term therapy in both groups. Mean arterial blood pressure, cardiac index and systemic vascular resistance did not change importantly. Norepinephrine levels did not change, but plasma renin activity decreased at baseline as well as after long-term therapy in both groups by similar amounts. Thus, no signs of tolerance development were observed after an oral treatment with 200 mg of xamoterol twice daily during 3 months. However, xamoterol as a partial agonist exerted only weak changes of cardiac index and PCWP compared to full β-adrenoceptor agonists. The drug was well tolerated, and serious side effects were absent.

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          Author and article information

          Journal
          CRD
          Cardiology
          10.1159/issn.0008-6312
          Cardiology
          S. Karger AG
          0008-6312
          1421-9751
          1990
          1990
          12 November 2008
          : 77
          : 1
          : 30-39
          Affiliations
          Department of Cardiology, University Hospital Eppendorf, Hamburg, FRG
          Article
          174577 Cardiology 1990;77:30–39
          10.1159/000174577
          1972349
          © 1990 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: 10
          Categories
          Original Paper

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