Bisacodyl: A review of pharmacology and clinical evidence to guide use in clinical practice in patients with constipation

Abstract

Background: Bisacodyl is a member of the diphenylmethane family and is considered to be a stimulant laxative. It has a dual prokinetic and secretory action and needs to be converted into the active metabolite bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM) in the gut to achieve the desired laxative effect. Bisacodyl acts locally in the large bowel by directly enhancing the motility, reducing transit time, and increasing the water content of the stool. A recent network meta-analysis concluded that bisacodyl showed similar efficacy to prucalopride, lubiprostone, linaclotide, tegaserod, velusetrag, elobixibat, and sodium picosulfate for the primary endpoint of ≥3 complete spontaneous bowel movements (CSBM)/week and an increase of ≥1 CSBM/week over baseline. The meta-analysis also found that bisacodyl may be superior to the other laxatives for the secondary endpoint of change from baseline in the number of spontaneous bowel movements per week in patients with chronic constipation. This observation stimulated the authors to review the available literature on bisacodyl, which has been available on the market since the 1950 s.

Purpose: The aim of the current review was to provide an overview of the historic background, structure, function, and mechanism of action of bisacodyl. Additionally, we discuss the important features and studies for bisacodyl to understand its peculiar characteristics and guide its use in clinical practice, but also stimulate research on open questions.

Keywords: Bisacodyl; constipation; laxative; mode of action; secretagogue; sodium picosulfate.

FIGURE 1

Metabolism of bisacodyl and sodium picosulfate into BHPM. BHPM, bis‐(p‐hydroxyphenyl)‐pyridyl‐2‐methane.

FIGURE 2

Structure of the bisacodyl dragee.

FIGURE 3

Efficacy and safety data per week over the 4 week treatment period. (A) Change in bowel movement frequency, (B) Percentage of patients experiencing AEs, (C) Percentage of patients taking 1 or 2 tablets bisacodyl or placebo. Patients can self‐manage their stimulant laxative dose to achieve effective relief of chronic constipation, as demonstrated in two randomized trials. Poster number S1328 presented at Digestive Disease Week 2010, republished with permission from Clinical Gastroenterology and Hepatology and the authors, respectively. AE, adverse event; CSBM, complete spontaneous bowel movement; SBM, spontaneous bowel movement. Data from Kamm et al.,2011 and Mueller‐Lissner et al., 2018

FIGURE 4

Serum levels of sodium and potassium at the beginning and end of treatment with bisacodyl, sodium picosulfate, and placebo, respectively, for 4 weeks (mean ±SD). SPS, sodium picosulfate; Republished with permission, from Mueller‐Lissner, Open J Gastroenterology, 2013.

FIGURE 5

Overview of mechanism of laxative action of bisacodyl and sodium picosulfate.