Skip to main content
SpringerLink
Log in

Racecadotril

  • Adis New Drug Profile
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

  • ▴ 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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3

Similar content being viewed by others

References

  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): 937–44

    PubMed  CAS  Google Scholar 

  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): 653–60

    PubMed  CAS  Google Scholar 

  3. Primi MP, Bueno L, Baumer P, et al. Racecadotril demonstrates intestinal antisecretory activity in vivo. Aliment Pharmacol Ther 1999; 13 Suppl. 6: 3–7

    Article  PubMed  CAS  Google Scholar 

  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): 87–146

    PubMed  CAS  Google Scholar 

  5. Baumer P, Danquechin DE, Bertrand J, et al. Effects of acetorphan, an enkephalinase inhibitor, on experimental and acute diarrhoea. Gut 1992 Jun; 33: 753–8

    Article  PubMed  CAS  Google Scholar 

  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: 887–91

    Article  PubMed  CAS  Google Scholar 

  7. Turvill J, Farthing M. Enkephalins and enkephalinase inhibitors in intestinal fluid and electrolyte transport. Eur J Gastroenterol Hepatol 1997 Sep; 9: 877–80

    Article  PubMed  CAS  Google Scholar 

  8. Marcais-Collado H, Uchida G, Costentin J, et al. Naloxone-reversible antidiarrheal effects of enkephalinase inhibitors. Eur J Pharmacol 1987 Dec; 144: 125–32

    Article  PubMed  CAS  Google Scholar 

  9. Rachmilewitz D, Karmelli F, Chorev M, et al. Effect of opiates on human colonic adenylate cyclase activity. Eur J Pharmacol 1983; 93: 169–73

    Article  PubMed  CAS  Google Scholar 

  10. Bioprojet Pharma. Tiorfan® acétorphan. Product monograph. Bioprojet Pharma. Paris, 1999. (Data on file)

  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.: A795

    Google Scholar 

  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.: A778

    Article  Google Scholar 

  13. Frexinos J, Sallenave J-R. Comparison of loperamide-oxide and acetorphan in acute diarrhoea [abstract no. 981]. Gut 1996; 39 Suppl. 3: A173

    Google Scholar 

  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: 352–4

    CAS  Google Scholar 

  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: 27–32

    PubMed  CAS  Google Scholar 

  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: 21–6

    PubMed  CAS  Google Scholar 

  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.: A701

    Article  Google Scholar 

  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: 485–9

    PubMed  CAS  Google Scholar 

  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: 128

    Google Scholar 

  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: 128

    Google Scholar 

  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: 211

    Google Scholar 

  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, 239

  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: 27–30

    PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland, 10, New Zealand

    Anna J. Matheson & Stuart Noble

Authors
  1. Anna J. Matheson
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Stuart Noble
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Anna J. Matheson.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Matheson, A.J., Noble, S. Racecadotril. Drugs 59, 829–835 (2000). https://doi.org/10.2165/00003495-200059040-00010

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-200059040-00010

Keywords

Search

Navigation