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Published in: Drugs 4/2000

01-04-2000 | Adis New Drug Profile

Racecadotril

Authors: Anna J. Matheson, Stuart Noble

Published in: Drugs | Issue 4/2000

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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.
Literature
1.
go back to reference 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): 937–44PubMed 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): 937–44PubMed
2.
go back to reference 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): 653–60PubMed 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): 653–60PubMed
3.
go back to reference Primi MP, Bueno L, Baumer P, et al. Racecadotril demonstrates intestinal antisecretory activity in vivo. Aliment Pharmacol Ther 1999; 13 Suppl. 6: 3–7PubMedCrossRef Primi MP, Bueno L, Baumer P, et al. Racecadotril demonstrates intestinal antisecretory activity in vivo. Aliment Pharmacol Ther 1999; 13 Suppl. 6: 3–7PubMedCrossRef
4.
go back to reference Roques BP, Noble F, Dauge V, et al. Neutral endopeptidase 24.11: structure, inhibition, and experimental and clinical pharmacology. Pharmacol Rev 1993; 45(1): 87–146PubMed Roques BP, Noble F, Dauge V, et al. Neutral endopeptidase 24.11: structure, inhibition, and experimental and clinical pharmacology. Pharmacol Rev 1993; 45(1): 87–146PubMed
5.
go back to reference Baumer P, Danquechin DE, Bertrand J, et al. Effects of acetorphan, an enkephalinase inhibitor, on experimental and acute diarrhoea. Gut 1992 Jun; 33: 753–8PubMedCrossRef Baumer P, Danquechin DE, Bertrand J, et al. Effects of acetorphan, an enkephalinase inhibitor, on experimental and acute diarrhoea. Gut 1992 Jun; 33: 753–8PubMedCrossRef
6.
go back to reference 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: 887–91PubMedCrossRef 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: 887–91PubMedCrossRef
7.
go back to reference Turvill J, Farthing M. Enkephalins and enkephalinase inhibitors in intestinal fluid and electrolyte transport. Eur J Gastroenterol Hepatol 1997 Sep; 9: 877–80PubMedCrossRef Turvill J, Farthing M. Enkephalins and enkephalinase inhibitors in intestinal fluid and electrolyte transport. Eur J Gastroenterol Hepatol 1997 Sep; 9: 877–80PubMedCrossRef
8.
go back to reference Marcais-Collado H, Uchida G, Costentin J, et al. Naloxone-reversible antidiarrheal effects of enkephalinase inhibitors. Eur J Pharmacol 1987 Dec; 144: 125–32PubMedCrossRef Marcais-Collado H, Uchida G, Costentin J, et al. Naloxone-reversible antidiarrheal effects of enkephalinase inhibitors. Eur J Pharmacol 1987 Dec; 144: 125–32PubMedCrossRef
9.
go back to reference Rachmilewitz D, Karmelli F, Chorev M, et al. Effect of opiates on human colonic adenylate cyclase activity. Eur J Pharmacol 1983; 93: 169–73PubMedCrossRef Rachmilewitz D, Karmelli F, Chorev M, et al. Effect of opiates on human colonic adenylate cyclase activity. Eur J Pharmacol 1983; 93: 169–73PubMedCrossRef
10.
go back to reference Bioprojet Pharma. Tiorfan® acétorphan. Product monograph. Bioprojet Pharma. Paris, 1999. (Data on file) Bioprojet Pharma. Tiorfan® acétorphan. Product monograph. Bioprojet Pharma. Paris, 1999. (Data on file)
11.
go back to reference 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 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
12.
go back to reference 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.: A778CrossRef 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.: A778CrossRef
13.
go back to reference Frexinos J, Sallenave J-R. Comparison of loperamide-oxide and acetorphan in acute diarrhoea [abstract no. 981]. Gut 1996; 39 Suppl. 3: A173 Frexinos J, Sallenave J-R. Comparison of loperamide-oxide and acetorphan in acute diarrhoea [abstract no. 981]. Gut 1996; 39 Suppl. 3: A173
14.
go back to reference 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 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
15.
go back to reference 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: 27–32PubMed 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: 27–32PubMed
16.
go back to reference 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: 21–6PubMed 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: 21–6PubMed
17.
go back to reference 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.: A701CrossRef 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.: A701CrossRef
18.
go back to reference 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: 485–9PubMed 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: 485–9PubMed
19.
go back to reference 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 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
20.
go back to reference 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 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
21.
go back to reference 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 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
22.
go back to reference 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 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.
go back to reference 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: 27–30PubMed 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: 27–30PubMed
Metadata
Title
Racecadotril
Authors
Anna J. Matheson
Stuart Noble
Publication date
01-04-2000
Publisher
Springer International Publishing
Published in
Drugs / Issue 4/2000
Print ISSN: 0012-6667
Electronic ISSN: 1179-1950
DOI
https://doi.org/10.2165/00003495-200059040-00010

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