The Enkephalinase Inhibitor, Acetorphan, in Acute Diarrhoea: A Double-Blind, Controlled Clinical Trial versus Loperamide

Abstract

The antidiarrhoeal properties of acetorphan, an inhibitor of enkephalinase (EC 3.4.24.11) that prevents endogenous enkephalin degradation, and loperamide, a mu opiate receptor agonist, were compared. The double-blind study included 69 patients with acute diarrhoea of presumed infectious origin, allocated at random to two parallel groups. Acetorphan and loperamide were both rapidly and similarly effective, diarrhoea resolving in both cases in nearly 2 days. With acetorphan, however, abdominal distension vanished significantly more rapidly, and reactive constipation was less frequent (8% versus 31% with loperamide). These differences can be accounted for by the distinct mechanisms of antidiarrhoeal activity of the two drugs--that is, primary antitransit effect for loperamide and antisecretory activity for acetorphan.

Prospective randomized double-blind trial of racecadotril compared with loperamide in elderly people with gastroenteritis living in nursing homes

“…In agreement with another study [34], we found that in racecadotril treatment, abdominal distension vanished rapidly, and reactive constipation was less frequent with respect to the loperamide group. These differences can be accounted for by the distinct mechanisms of antidiarrheal activity of the two drugs as above described.…”

“…Hamza et al [32] and Vetel et al [33] reported that racecadotril produced a significant (P=0.025) decrease in stool weight during the first day of treatment compared with placebo and was also associated with significantly fewer diarrheic stools than placebo after 1 day of treatment. Other studies in adult patients reported that racecadotril was able to reduce diarrhea in about 19 h [27,34]. In agreement with these studies, we documented that racecadotril reduced diarrhea in all patients in about 1 day in all episodes of gastroenteritis.…”

Tolerability of Racecadotril in Acute Watery Diarrhoea in Children

“…It was concluded that racecadotril is more safe and tolerable than loperamide and is effective in resolving the symptoms associated with diarrhoea. Similar results were reported in other studies by Roge et al, 29 Prado et al 30 and Wang et al 25 …”

Antidiarrhoeal effect of the crude methanol extract of the dried fruit of Adansonia digitata L. (Malvaceae)

“…Most modern antidiarrhoeal agents are beyond the reach of the common man in developing countries. In addition, they have some levels of toxic effect [4,5]. To overcome the menace of diarrhoeal disease in developing countries, the World Health Organization (WHO) has included a programme for the control of diarrhoea, which involves the use of traditional herbal medicine [6].…”