| Description | Racecadotril, also known as acetorphan, is a kind of antidiarrheal drug acting as a peripherally acting enkephalinase inhibitor. It has an antisecretory effect, reducing the secretion of water and electrolytes into the intestine. Racecadotril is a pro-drug that is metabolized in vivo into the active compound, thiorphan. Thiorphan exerts its inhibitory effect on enkephalinase, reducing the amount of secreted water produced by the intestines. In this case, the body loses less fluid, and the symptoms of diarrhea can be alleviated. |
| Chemical Properties | White Solid |
| Originator | Bioprojet (France) |
| Uses | Racecadotril is an enkephalinase inhibitor that prevents the degradation of endogenous opioids. It demonstrates antidiarrheal activity by reducing hypersecretion of water and electrolytes into the intestinal lumen. It is an effective and safe treatment for acute diarrhea in adults and children. |
| Definition | ChEBI: Racecadotril is a N-acyl-amino acid. It is a pro-drug that is metabolized in vivo into the active compound, thiorphan. It has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis. |
| Brand name | Tiorfan |
| Clinical Use | Acetorphan is an orally-active enkephalinase inhibitor introduced in 1993 for the treatment of acute diarrhea in adults.It displays antidiarrheal activity via a purely antisecretory mechanism without inhibiting intestinal transit. |
| Metabolism | Quickly metabolised by hydrolysis to active metabolite,
thiorphan. Racecadotril is eliminated as active and
inactive metabolites. Elimination is mainly via the renal
route, and to a much lesser extent via the faecal route
(around 8%). The pulmonary route is not significant (less
than 1% of the dose). |
| Mode of action | Acetorphan acts as rapidly as loperamide, a classical muopiate receptor agonist that exhibits its antidiarrheal effect via an antitransit mechanism, without producing constipation or other side effects. The novel mechanism of action may render acetorphan potentially useful in the management of infectious diarrhea. |
| References | https://en.wikipedia.org/wiki/Racecadotril
https://patient.info/medicine/racecadotril-for-acute-diarrhoea-hidrasec |
