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Chlormezanone plasma and blood levels in patients after single and repeated oral doses and after suicidal drug overdose

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Summary

Chlormezanone plasma concentrations were determined in 5 volunteers (group 1) after a single oral dose of 200 mg of chlormezanone with high performance liquid chromatography. A plasma elimination half-life of 23 ± 2.3 h was calculated. The mean peak chlormezanone plasma level was 1.86 ± 0.2 ug/ml, 1 h after ingestion. Additionally, chlormezanone plasma levels were determined after repeated oral doses of chlormezanone recommended for treatment of muscular spasms due to degenerative skeletal disease. After 5 days of repeated daily doses of 3 × 200 mg (group 2; 12 patients) or 3 × 400 mg (group 3; 10 patients) of chlormezanone, mean predose chlormezanone plasma levels were 12.0 ± 2.0 ug/ml (group 2) and 22.7 ± 4.0 ug/ml (group 3), respectively. Comparable plasma concentrations were determined after 10 days of repeated doses of 3 × 200 mg or 3 × 400 mg of chlormezanone in 3 patients from each of these 2 groups. In 7 patients of group 3, chlormezanone had to be discontinued on the 5th day due to increasing muscular weakness, ataxia and exercise-inducible tachycardia. After a loading dose of 800 mg and repeated doses of 3 × 200 mg chlormezanone to 5 patients (group 4), plasma levels of 6.5 ±2.1 Ug/ml, 8.9 ± 2.2 ug/ml, 12.7 ± 2.0 ug/ml, and 10.4 ± 2.4 ug/ml were determined after 2, 8, 16, and 36 h, respectively. Trace amounts of a degradation product of the acid-labile chlormezanone could be detected in plasma besides the unchanged drug after administration of repeated oral doses. Chlormezanone is equally distributed between plasma and erythrocytes. In 3 cases of fatal drug overdose involving chlormezanone/diazepam (case 1), chlormezanone/acetaminophen/diazepam (case 2), and chlormezanone/acetaminophen (case 3), chlormezanone blood levels amounted to 53,13 and 9 ug/ml, respectively. Tissue levels were determined in addition.

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Authors and Affiliations

  1. Reanimationszentrum, Klinikum Rudolf Virchow, Standort Charlottenburg, Freie Universität Berlin, Spandauer Damm 130, D-1000, Berlin 19, FRG

    C. Köppel & F. Martens

  2. Department of Pharmacology, University of Iceland, Reykjavik, Iceland

    J. Kristinsson

  3. Department of Toxicology, Landesuntersuchungsinstitut für Lebensmittel, Arzneimittel und Tierseuchen Berlin, Berlin, Germany

    A. Wagemann & J. Tenczer

Authors
  1. C. Köppel
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  2. J. Kristinsson
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  3. A. Wagemann
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  4. J. Tenczer
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  5. F. Martens
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Köppel, C., Kristinsson, J., Wagemann, A. et al. Chlormezanone plasma and blood levels in patients after single and repeated oral doses and after suicidal drug overdose. European Journal of Drug Metabolism and Pharmacokinetics 16, 43–47 (1991). https://doi.org/10.1007/BF03189873

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  • DOI: https://doi.org/10.1007/BF03189873

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