racecadotril

Racecadotril is an antidiarrheal medication that acts as a peripheral enkephalinase inhibitor. It is a prodrug that, after oral administration, is rapidly converted to its active metabolite thiorphan. Thiorphan inhibits the enzyme enkephalinase (also known as neutral endopeptidase) in the intestinal epithelium, protecting endogenous enkephalins from degradation. Enkephalins activate δ opioid receptor on enterocytes, leading to reduced cyclic adenosine monophosphate (cAMP) synthesis and decreased secretion of water and electrolytes into the gastrointestinal lumen. This mechanism reduces diarrhea-related hypersecretion without affecting intestinal motility or transit time, distinguishing it from μ-opioid receptor agonists like loperamide. Racecadotril does not cross the blood–brain barrier at therapeutic doses and has no effect on basal secretion or gastrointestinal transit[1][2][3][5][6].

Brand names

HidrasecTiorfanAcetorphan

Other names

acetorphan