Diseases of the Colon & Rectum

, Volume 35, Issue 9, pp 857–861 | Cite as

Influence of loperamide and loperamide oxide on the anal sphincter

A manometric study
  • M. Göke
  • K. Ewe
  • K. Donner
  • K. -H. Meyer zum Büschenfelde
Original Contributions


The objective of this study was to investigate the effects of the opioid loperamide and its recently synthesized pharmacologically inactive prodrug loperamide oxide on the anal sphincter. In a double-blind, placebo-controlled crossover study, anorectal manometry was performed in 12 healthy volunteers five hours after oral bolus application of 10 mg of loperamide, loperamide oxide, or placebo. Loperamide significantly increased the threshold volumes for minimal perception and urgency to defecate (P <0.05) and raised the volume required to abolish recovery of the rectoanal inhibitory reflex (P < 0.05). These findings suggest that loperamide has a specific continence-improving action on the anal sphincter. However, anal resting pressure and maximal squeeze pressure were unaffected in our study and do not seem to be responsible for this effect. The effects under loperamide oxide showed a similar tendency but were without statistical significance.

Key words

Anal sphincter Anorectal manometry Loperamide Loperamide oxide 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Shee CD, Pounder RE. Loperamide, diphenoxylate and codeine phosphate in chronic diarrhoea. BMJ 1980;280:524.CrossRefPubMedGoogle Scholar
  2. 2.
    Galambos JT, Hersh T, Schroder S, Wenger J. A new antidiarrheal agent in the treatment of chronic diarrhea. Gastroenterology 1976;70:1026–9.PubMedGoogle Scholar
  3. 3.
    Palmer KR, Corbett CL, Holdsworth CD. Doubleblind cross-over study comparing loperamide, codeine and diphenoxylate in the treatment of chronic diarrhea. Gastroenterology 1980;79:1272–5.PubMedGoogle Scholar
  4. 4.
    Hughes S, Higgs NB, Turnberg LA. Loperamide has antisecretory activity in the human jejunum in vivo. Gut 1984;25:931–5.PubMedGoogle Scholar
  5. 5.
    Schiller LR, Santa Ana CA, Morawski SG, Fordtran JS. Mechanism of the antidiarrheal effect of loperamide. Gastroenterology 1984;86:1475–80.PubMedGoogle Scholar
  6. 6.
    Kachel G, Ruppin H, Hagel J, Barina W, Meinhardt M, Domschke W. Human intestinal motor activity and transport: effects of a synthetic opiate. Gastroenterology 1986;90:85–93.PubMedGoogle Scholar
  7. 7.
    Press AG, Ewe K, Schmidt J, Junge H. Effect of loperamide on jejunal electrolyte and water transport, prostaglandin E2-induced secretion and intestinal transit time in man. Eur J Clin Pharmacol 1991;41:239–43.CrossRefPubMedGoogle Scholar
  8. 8.
    Kachur JF, Miller RJ, Field M. Control of guinea pig intestinal electrolyte secretion by aδ-opiate receptor. Proc Natl Acad Sci U S A 1980;77:2753–6.PubMedGoogle Scholar
  9. 9.
    Read M, Read NW, Barber DC, Duthie HL. Effects of loperamide on anal sphincter function in patients complaining of chronic diarrhea with fecal incontinence and urgency. Dig Dis Sci 1982;27:807–14.CrossRefPubMedGoogle Scholar
  10. 10.
    Emblem R, Stien R, Morkrid L. The effect of loperamide on bowel habits and anal sphincter function in patients with ileoanal anastomosis. Scand J Gastroenterol 1989;24:1019–24.PubMedGoogle Scholar
  11. 11.
    Loperamide oxide (R 58425)—antidiarrhoeal. Investigational new drug brochure (agency publication). 2nd ed. Beerse, Belgium: Janssen Research Foundation, 1989.Google Scholar
  12. 12.
    Arndorfer RC, Steff JJ, Dodds WJ, Linehan JH, Hogan WJ. Improved infusion system for intraluminal oesophageal manometry. Gastroenterology 1977;73:23–7.PubMedGoogle Scholar
  13. 13.
    Kestenberg A, Becker JM, Sharp W. Effect of loperamide on the anal sphincter of the cat. Gastroenterology 1986;90:1492.Google Scholar
  14. 14.
    Rattan S, Culver PJ. Influence of loperamide on the internal anal sphincter in the opossum. Gastroenterology 1987;93:121–8.PubMedGoogle Scholar
  15. 15.
    McKirdy HC. Effect of loperamide on human isolated internal anal sphincter (Abstr). J Physiol (Lond) 1981;316:18P.Google Scholar
  16. 16.
    Read NW. A randomized, double-blind, placebo controlled, crossover study to determine the effects of loperamide oxide on bowel transit and anorectal function in normal volunteers. Clinical research report. Beerse, Belgium: Janssen Research Foundation, 1989.Google Scholar

Copyright information

© American Society of Colon and Rectal Surgeons 1992

Authors and Affiliations

  • M. Göke
    • 1
  • K. Ewe
    • 1
  • K. Donner
    • 1
  • K. -H. Meyer zum Büschenfelde
    • 1
  1. 1.I. Department of MedicineUniversity of MainzMainzGermany

Personalised recommendations