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Kinetics of oral and intravenous mexiletine: lack of effect of cimetidine and ranitidine

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Summary

The pharmacokinetics of mexiletine, a Class I antiarrhythmic drug, was investigated in 6 healthy volunteers after single oral doses and 15 min intravenous infusions of 3 mg/kg. Cimetidine and ranitidine are commonly used H2-receptor antagonists, which interact adversely with many drugs, e.g. inhibition of the metabolism of Class I antiarrhythmics such as lidocaine and quinidine by cimetidine. To investigate the effects of the two drugs on the kinetics of mexiletine, cimetidine 800 mg·day−1 or ranitidine 600 mg·day−1 were administered orally for one week.

Neither H2-receptor antagonist altered the distribution and elimination of mexiletine, nor did they affect its overall kinetics, or excretion of the metabolites para- and 4-OH-methylmexiletine after oral and intravenous administration of mexiletine.

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Authors and Affiliations

  1. Department of Medicine, Universitätsklinik Essen, Germany

    N. H. Brockmeyer & E. E. Ohnhaus

  2. Universitätsklinik Giessen, Germany

    H. Breithaupt

  3. Department of Pediatrics, Justus Liebig-Universität Gießen, Germany

    W. Ferdinand & M. von Hattingberg

Authors
  1. N. H. Brockmeyer
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  2. H. Breithaupt
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  3. W. Ferdinand
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  4. M. von Hattingberg
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  5. E. E. Ohnhaus
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Brockmeyer, N.H., Breithaupt, H., Ferdinand, W. et al. Kinetics of oral and intravenous mexiletine: lack of effect of cimetidine and ranitidine. Eur J Clin Pharmacol 36, 375–378 (1989). https://doi.org/10.1007/BF00558298

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  • DOI: https://doi.org/10.1007/BF00558298

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