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Oral naloxone antagonizes loperamide-induced delay of orocecal transit

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Abstract

Orocecal transit time was determined by the lactulose hydrogen breath test in nine healthy volunteers after administration of placebo, loperamide (16 mgper os), and loperamide (16 mgper os) followed by oral naloxone at doses of 16 and 32 mg. The four tests were performed in double-blind conditions and in random sequences. Transit time (mean,sd) after loperamide (128.8 min, 32.9) was significantly increased (P<0.05) compared with placebo (85.5 min, 35.7), loperamide followed by naloxone 16 mg (88.8 min, 46.2), and loperamide followed by naloxone 32 mg (84.4 min, 40.6). These results show that the peripheral opioid agonist loperamide delays orocecal transit in healthy subjects and that naloxoneper os at adequate doses antagonizes this effect.

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References

  1. Jaffe JH, Martin WR: Opioid analgesics and antagonists.In The Pharmacological Basis of Therapeutics. Goodman Gilman A, Goodman LS, Gilman A (eds). New York, Macmillan, 1980, pp 494–534

    Google Scholar 

  2. Basilisco G, Bozzani A, Camboni G, Recchia M, Quatrini M, Conte D, Penagini R, Bianchi PA: Effect of loperamide and naloxone on mouth-to-caecum transit time evaluated by lactulose hydrogen breath test. Gut 26:700–703, 1985

    Google Scholar 

  3. Fishman J, Roffwarg H, Hellman H: Disposition of naloxone-7,8-3H in normal and narcotic-dependent men. J. Pharmacol Exp Ther 187:575–580, 1973

    Google Scholar 

  4. Nutt JG, Jasinski DR: Methadone-naloxone mixtures for use in methadone maintenance programs. I. An evaluation in man of their pharmacological feasibility. II. Demonstration of acute physical dependence. Clin Pharmacol Ther 15:156–166, 1974

    Google Scholar 

  5. Zaks A, Jones T, Fink M, Freedman AM: Naloxone treatment of opiate dependence. JAMA 215:2108–2110, 1971

    Google Scholar 

  6. Bromm B, Meier W, Scharein E: Antagonism between tilidine and naloxone on cerebral potentials and pain ratings in man. Eur J Pharmacol 87:431–439, 1983

    Google Scholar 

  7. Metz G, Gassul MA, Leeds AR, Blendis LM, Jenkis DJA: A simple method of measuring breath hydrogen in carbohydrate malbsorption by end-expiratory sampling. Clin Sci Mol Med 50:237–240, 1976

    Google Scholar 

  8. Zuccato E, Andreoletti M, Bozzani A, Marcucci F, Velio P, Bianchi P, Mussini E: Respiratory excretion of hydrogen and methane in Italian subjects after ingestion of lactose and milk. Eur J Clin Invest 13:261–266, 1983

    Google Scholar 

  9. Bond JH, Levitt MD: Investigation of small bowel transit time in man utilizing pulmonary hydrogen (H2) measurements. J Lab Clin Med 85:546–555, 1975

    Google Scholar 

  10. Shafer RB, Prentiss RA, Bond JH: Gastrointestinal transit in thyroid disease. Gastroenterology 86:852–855, 1984

    Google Scholar 

  11. Read NW, Al-Janabi MN, Bates TE, Holgate AM, Cann PA, Kinsman RI, McFarlane A, Brown C: Interpretation of the breath hydrogen profile obtained after ingesting a solid meal containing unabsorbable carbohydrate. Gut 26:834–842, 1985

    Google Scholar 

  12. Ooms LAA, Degryse AD, Janssen PAJ: Mechanism of action of loperamide. Scand J Gastroenterol 19:145–158, 1984

    Google Scholar 

  13. Wald A, Van Thiel DH, Hoechstetter L, Gavaler JS, Egler KM, Verma R, Scott L, Lester R: Gastrointestinal transit: The effect of the menstrual cycle. Gastroenterology 80:1497–1500, 1981

    Google Scholar 

  14. Kirk RE: Experimental Design: Procedures for the Behavioral Sciences. Belmont, California, Brooks/Cole Publishing, 1968, pp 245–318

    Google Scholar 

  15. LaBrooy SJ, Male PJ, Beavis AK, Misiewicz JJ: Assessment of the reproducibility of the lactulose H2 breath test as a measure of mouth-to-caecum transit time. Gut 24:893–896, 1983

    Google Scholar 

  16. Corbett CL, Thomas S, Read NW, Hobson N, Bergman I, Holdsworth CD: Electrochemical detector for breath hydrogen determination: Measurement of small-bowel transit time in normal subjects and patients with the irritable bowel syndrome. Gut 22:836–840, 1981

    Google Scholar 

  17. Van Wyk N, Sommers K, Steyn AGW: Evaluation of gastrointestinal motility using the hydrogen breath test. Br J Clin Pharmacol 20:479–481, 1985

    Google Scholar 

  18. Cann PA, Read NW, Holdsworth CD, Barends D: Role of loperamide and placebo in management of irritable bowel syndrome (IBS). Dig Dis Sci 29:239–247, 1984

    Google Scholar 

  19. Morley JE, Levine AS, Yamada T, Gebhard RL, Prigge WF, Shafer RB, Goetz FC, Silvis FE: Effect of exorphins on gastroentestinal function, hormonal release and appetite. Gastroenterology 84:1517–1523, 1983

    Google Scholar 

  20. Kreek MJ, Hahn EP, Schaefer RA, Fishman J: Naloxone, a specific opioid antagonist, reverses chronic idiopathic constipation. Lancet 1:261–262, 1983

    Google Scholar 

  21. Kreek MJ, Paris P, Bartol MA, Mueller D: Effects of short-term oral administration of the specific opioid antagonist naloxone on fecal evacuation in geriatric patients. Gastroenterology 86:1144, 1984

    Google Scholar 

  22. Schang IC, Devroede G, Perreault R: Naloxone therapy in small intestinal pseudoobstruction. Preliminary results about two cases. Am J Gastroenterol 79:828, 1984

    Google Scholar 

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Basilisco, G., Camboni, G., Bozzani, A. et al. Oral naloxone antagonizes loperamide-induced delay of orocecal transit. Digest Dis Sci 32, 829–832 (1987). https://doi.org/10.1007/BF01296704

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  • DOI: https://doi.org/10.1007/BF01296704

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