Racecadotril

Racecadotril is a prodrug, which means the body has to hydrolyse it to its active metabolite, thiorphan. Thiorphan blocks enkephalinase. This enzyme is a peptidase found on cell membranes in several tissues, especially in the epithelium of the small intestine, and it breaks down both exogenous peptides and endogenous peptides (the enkephalins).

By protecting the enkephalins from this enzymatic breakdown, racecadotril prolongs their action at the enkephalinergic synapses in the small intestine. The result is less hypersecretion of water and electrolytes. Racecadotril works as an antidiarrhoeal quickly, and it does this without changing the duration of intestinal transit. It does not cause abdominal distension.