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Pharmacokinetic approach to equilibrium between ketanserin and ketanserin-ol

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Summary

The metabolic reduction-oxidation equilibrium between ketanserin and ketanserin-ol was studied after oral dosing of both substances to two healthy volunteers. Comparison of plasma Cmax and AUCs indicated that the equilibrium was shifted towards ketanserin-ol. There is evidence that ketanserin-ol elimination is the slowest step dictating the terminal half-life of ketanserin.

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Authors and Affiliations

  1. Department of Drug Metabolism and Pharmacokinetics, Janssen Pharmaceutica, Beerse, Belgium

    A. Van Peer, R. Woestenborghs, L. Embrechts & J. Heykants

Authors
  1. A. Van Peer
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  2. R. Woestenborghs
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  3. L. Embrechts
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  4. J. Heykants
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Van Peer, A., Woestenborghs, R., Embrechts, L. et al. Pharmacokinetic approach to equilibrium between ketanserin and ketanserin-ol. Eur J Clin Pharmacol 31, 339–342 (1986). https://doi.org/10.1007/BF00981134

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  • DOI: https://doi.org/10.1007/BF00981134

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