, Volume 59, Issue 4, pp 829–835 | Cite as


  • Anna J. Matheson
  • Stuart Noble
Adis New Drug Profile


  • ▴ Racecadotril is an oral enkephalinase inhibitor used in the treatment of acute diarrhoea. It prevents the degradation of endogenous opioids (enkephalins), thereby reducing hypersecretion of water and electrolytes into the intestinal lumen.

  • ▴ In a randomised double-blind study in 6 adult volunteers with castor oil-induced diarrhoea, racecadotril significantly reduced stool weight and stool number in comparison with placebo. Similar results have been obtained in treating castor oil-induced diarrhoea in rats.

  • ▴ Racecadotril was significantly more effective than placebo in randomised double-blind studies in adults or children with diarrhoea (of infectious origin or in adults with HIV infection).

  • ▴ In well controlled trials, racecadotril had efficacy similar to that of loperamide and was generally as effective as loperamide-oxide.

  • ▴ Racecadotril had a similar tolerability profile to placebo, and was better tolerated than loperamide, in adults and children with diarrhoea. It caused significantly less constipation after resolution of diarrhoea than loperamide.


Loperamide Acute Diarrhoea Infectious Origin Stool Weight Racecadotril 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


  1. 1.
    Lecomte JM, Costentin J, Vlaiculescu A, et al. Pharmacological properties of acetorphan, a parenterally active “enkephalinase” inhibitor. J Pharmacol Exp Ther 1986 Jun; 237(3): 937–44PubMedGoogle Scholar
  2. 2.
    De-la-Baume S, Brion F, Dam-Trung-Tuong M, et al. Evaluation of enkephalinase inhibition in the living mouse, using [3H]acetorphan as a probe. J Pharmacol Exp Ther 1988 Nov; 247(2): 653–60PubMedGoogle Scholar
  3. 3.
    Primi MP, Bueno L, Baumer P, et al. Racecadotril demonstrates intestinal antisecretory activity in vivo. Aliment Pharmacol Ther 1999; 13 Suppl. 6: 3–7PubMedCrossRefGoogle Scholar
  4. 4.
    Roques BP, Noble F, Dauge V, et al. Neutral endopeptidase 24.11: structure, inhibition, and experimental and clinical pharmacology. Pharmacol Rev 1993; 45(1): 87–146PubMedGoogle Scholar
  5. 5.
    Baumer P, Danquechin DE, Bertrand J, et al. Effects of acetorphan, an enkephalinase inhibitor, on experimental and acute diarrhoea. Gut 1992 Jun; 33: 753–8PubMedCrossRefGoogle Scholar
  6. 6.
    Hinterleitner TA, Petritsch W, Dimsity G, et al. Acetorphan prevents cholera-toxin-induced water and electrolyte secretion in the human jejunum. Eur J Gastroenterol Hepatol 1997 Sep; 9: 887–91PubMedCrossRefGoogle Scholar
  7. 7.
    Turvill J, Farthing M. Enkephalins and enkephalinase inhibitors in intestinal fluid and electrolyte transport. Eur J Gastroenterol Hepatol 1997 Sep; 9: 877–80PubMedCrossRefGoogle Scholar
  8. 8.
    Marcais-Collado H, Uchida G, Costentin J, et al. Naloxone-reversible antidiarrheal effects of enkephalinase inhibitors. Eur J Pharmacol 1987 Dec; 144: 125–32PubMedCrossRefGoogle Scholar
  9. 9.
    Rachmilewitz D, Karmelli F, Chorev M, et al. Effect of opiates on human colonic adenylate cyclase activity. Eur J Pharmacol 1983; 93: 169–73PubMedCrossRefGoogle Scholar
  10. 10.
    Bioprojet Pharma. Tiorfan® acétorphan. Product monograph. Bioprojet Pharma. Paris, 1999. (Data on file)Google Scholar
  11. 11.
    Cézard JP, Duhamel JF, Meyer M, et al. Efficacy and tolerance of acetorphan in infant acute diarrhea. A multicentric double blind study [abstract]. Gastroenterology 1996 Apr; 110(4) Suppl.: A795Google Scholar
  12. 12.
    Baumer P, Duvivier C, Bérard H, et al. HIV-related diarrhea: efficacy of acetorphan in a randomized controlled trial [abstract]. Gastroenterology 1995 Apr; 108(4) Suppl.: A778CrossRefGoogle Scholar
  13. 13.
    Frexinos J, Sallenave J-R. Comparison of loperamide-oxide and acetorphan in acute diarrhoea [abstract no. 981]. Gut 1996; 39 Suppl. 3: A173Google Scholar
  14. 14.
    Roge J, Baumer P, Berard H, et al. The enkephalinase inhibitor, acetorphan, in acute diarrhoea. A double-blind, controlled clinical trial versus loperamide. Scand J Gastroenterol 1993 Apr; 28: 352–4Google Scholar
  15. 15.
    Turck D, Bérard H, Frétault N, et al. Comparison of racecadotril and loperamide in children with acute diarrhoea. Aliment Pharmacol Ther 1999; 13 Suppl. 6: 27–32PubMedGoogle Scholar
  16. 16.
    Vetel JM, Berard H, Fretault N, et al. Comparison of racecadotril and loperamide in adults with acute diarrhoea. Aliment Pharmacol Ther 1999; 13 Suppl. 6: 21–6PubMedGoogle Scholar
  17. 17.
    Turck D, Bérard H, Frétault N, et al. Treatment of acute diarrhea in children. Comparison of the safety and the efficacy of acetorphan and loperamide in a double-blind versus placebo randomized study [abstract]. Gastroenterology 1995 Apr; 108(4) Suppl.: A701CrossRefGoogle Scholar
  18. 18.
    Beaugerie L, Baumer P, Chaussade S, et al. Treatment of refractory diarrhoea in AIDS with acetorphan and octreotide: a randomized crossover study. Eur J Gastroenterol Hepatol 1996 May; 8: 485–9PubMedGoogle Scholar
  19. 19.
    Ychou M, Rougier P, Douillard JY, et al. A phase II study of CPT-11 (irinotecan) in colorectal cancer (CRC) refractory to 5-FU, with preventive treatment of delayed diarrhea using acetorphan [abstract no. 454]. Ann Oncol 1996; 7 Suppl. 1: 128Google Scholar
  20. 20.
    Misset JL, Saliba F, Giachetti S, et al. Pathophysiology and therapy of irinotecan (CPT-11)-induced delayed diarrhea: a prospective assessment [abstract no. 455]. Ann Oncol 1996; 7 Suppl. 1: 128Google Scholar
  21. 21.
    Merrouche Y, Bugat R, Brunet R, et al. High dose acetorphan (HDA) versus acetorphan + loperamide (A+L) in the treatment of CPT-11 induced (DD) diarrhea: preliminary report of a randomized phase II study in patients (Pts) with advanced colorectal cancer (CRC) [abstract no. 487]. Proc Am Soc Clin Oncol 1996 Mar; 15: 211Google Scholar
  22. 22.
    Hagipantelli R, Misset JL, Saliba F, et al. Pathophysiology and therapy of CPT-11 induced diarrhea. Preliminary data of an ongoing phase I-II study [abstract no. 1425]. 86th Annual Meeting of the American Association for Cancer Research; 1995 Mar 18–22; Toronto, 239Google Scholar
  23. 23.
    Dorval ED, Regimbeau C, Gamelin E, et al. Effect of enkephalinase inhibition on acute chemotherapy-induced diarrhoea in man: results of a pilot study [in French]. Gastroenterol Clin Biol 1995 Jan; 19: 27–30PubMedGoogle Scholar

Copyright information

© Adis International Limited 2000

Authors and Affiliations

  1. 1.Adis International LimitedMairangi Bay, AucklandNew Zealand

Personalised recommendations