Bisacodyl

Mechanism of action:
Bisacodyl is a diphenylmethane derivative. In the intestine, bisacodyl is converted by intestinal bacteria into the active metabolite bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM), which stimulates the myenteric plexus through mechanisms that remain incompletely defined, thereby promoting intestinal smooth muscle contraction and increasing peristalsis. It may also promote activation of adenylate cyclase in intestinal epithelial cells, increasing cAMP, which leads to enhanced mucus secretion and chloride ion (Cl⁻) release, while inhibiting sodium (Na⁺) and water absorption. As a result, stool water content rises, stool volume increases, and the likelihood of triggering defecation-related reflexes is enhanced.
Reference(s):
1. Kudo K et al. (1998). Laxative poisoning: toxicological analysis of bisacodyl and its metabolite in urine, serum, and stool. J Anal Toxicol.
2. Roth W et al. (1988). Pharmacokinetics and laxative effect of bisacodyl following administration of various dosage forms. Arzneimittelforschung.
3. Manabe N et al. (2009). Effects of bisacodyl on ascending colon emptying and overall colonic transit in healthy volunteers. Aliment Pharmacol Ther.
