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Effects of the prodrug loperamide oxide, loperamide, and placebo on jejunal motor activity

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Abstract

This crossover, double-blind study investigated the effects of single oral doses of the prodrug loperamide oxide, which is reduced gradually to loperamide in the intestine, and loperamide on jejunal motor activity in 12 fasting healthy men. Five minutes after a phase III of the migrating motor complex (MMC), 2 mg loperamide oxide, 4 mg loperamide oxide, 4 mg loperamide, or placebo were administered. Thereafter, motor activity 10–30 cm aborad the ligament of Treitz was recorded with five catheter orifices at 3-cm intervals over 4 hr. Number of contractions and area under curve increased significantly with 4 mg loperamide and 4 mg loperamide oxide, the increases with loperamide oxide occurring more gradually. Placebo and 2 mg loperamide oxide had no discernible effects. With both 4 mg loperamide and 4 mg loperamide oxide, phase I of the MMC was slightly prolonged and phase II and the time from drug administration to the onset of the first phase III slightly shortened. The percentage of aborally propagated contractions in phase II increased with all active treatments, whereas the occurrence of phases III was not altered.

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Authors and Affiliations

  1. Psychophysiology Unit at the Departments of Psychiatry and Surgery I, University of Vienna, Währinger Gürtel 18-20, A-1090, Vienna, Austria

    G. Stacher MD, H. Steinringer PhD, C. Schneider, G. V. Vacariu-Granser MD, F. Castiglione MD, G. Gaupmann, U. Weber & G. Stacher-Janotta

Authors
  1. G. Stacher MD
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  2. H. Steinringer PhD
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  3. C. Schneider
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  4. G. V. Vacariu-Granser MD
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  5. F. Castiglione MD
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  6. G. Gaupmann
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  7. U. Weber
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  8. G. Stacher-Janotta
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Supported by Janssen Pharmaceutica, Beerse, Belgium.

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Stacher, G., Steinringer, H., Schneider, C. et al. Effects of the prodrug loperamide oxide, loperamide, and placebo on jejunal motor activity. Digest Dis Sci 37, 198–204 (1992). https://doi.org/10.1007/BF01308172

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  • DOI: https://doi.org/10.1007/BF01308172

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