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Pharmacokinetic and pharmacodynamic studies following the intravenous and oral administration of the antiparkinsonian drug biperiden to normal subjects

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Summary

The pharmacokinetics and pharmacodynamics (changes in pupil size and salivary flow) of biperiden following a single oral and intravenous dose were investigated in six normal subjects.

After the injection plasma concentrations declined biphasically, with half-times of 1.5 h for the rapid phase and 24 h for the terminal phase. Clearance and apparent volume of distribution were high (12 ml·min−1·kg−1 and 24 l·kg−1 respectively). Absorption was rapid but the systemic availability was incomplete (33%), probably due to first-pass metabolism.

Central nervous system (CNS) adverse effects and changes in pupil size were observed after both routes of administration while salivary flow was affected only by the injection.

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Authors and Affiliations

  1. Institute of Medical Pharmacology, University of Pavia, Pavia, Italy

    R. Grimaldi, E. Perucca & A. Crema

  2. Institute of Ophthalmology, University of Pavia, Pavia, Italy

    G. Ruberto, C. Gelmi & F. Trimarchi

  3. Experimental Medical Research and Development, Knoll AG, Ludwigshafen, Federal Republic of Germany

    M. Hollmann

Authors
  1. R. Grimaldi
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  2. E. Perucca
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  3. G. Ruberto
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  4. C. Gelmi
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  5. F. Trimarchi
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  6. M. Hollmann
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  7. A. Crema
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Grimaldi, R., Perucca, E., Ruberto, G. et al. Pharmacokinetic and pharmacodynamic studies following the intravenous and oral administration of the antiparkinsonian drug biperiden to normal subjects. Eur J Clin Pharmacol 29, 735–737 (1986). https://doi.org/10.1007/BF00615970

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  • DOI: https://doi.org/10.1007/BF00615970

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