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Neurogastroenterology and Motility Oct 2021Bisacodyl 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... (Review)
Review
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.
Topics: Bisacodyl; Constipation; Defecation; Humans; Intestine, Large; Laxatives
PubMed: 33751780
DOI: 10.1111/nmo.14123 -
Biological & Pharmaceutical Bulletin 2021MUC5AC overproduction is commonly observed in chronic inflammatory lung diseases and worsens these conditions. Therefore, drugs that inhibit MUC5AC production are...
MUC5AC overproduction is commonly observed in chronic inflammatory lung diseases and worsens these conditions. Therefore, drugs that inhibit MUC5AC production are urgently needed. To identify novel drugs directly inhibiting MUC5AC production, 640 already approved drugs were screened. We found that the laxative bisacodyl suppressed transforming growth factor (TGF)-α-induced MUC5AC production in a concentration-dependent manner. Additionally, bisacodyl also suppressed TGF-α-induced MUC5AC mRNA expression in the same concentration range. These results suggested that bisacodyl could be a new drug for treating mucin overproduction.
Topics: Antineoplastic Agents; Bisacodyl; Cell Line, Tumor; Humans; L-Lactate Dehydrogenase; Laxatives; Mucin 5AC; Steroids; Transforming Growth Factor alpha
PubMed: 33790109
DOI: 10.1248/bpb.b20-00886 -
Antimicrobial Agents and Chemotherapy Jun 2022Identifying novel antivirals requires significant time and resource investment, and the continuous threat of viruses to human health necessitates commitment to antiviral...
Identifying novel antivirals requires significant time and resource investment, and the continuous threat of viruses to human health necessitates commitment to antiviral identification and development. Developing antivirals requires years of research and validation, and recent outbreaks have highlighted the need for preparedness in counteracting pandemics. One way to facilitate development is to repurpose molecules already used clinically. By screening such compounds, we can accelerate antiviral development. Here, we screened compounds from the National Institutes of Health's Developmental Therapeutic Program for activity against chikungunya virus, an alphavirus that is responsible for a significant outbreak in the Americas in 2013. Using this library, we identified several compounds with known antiviral activity, as well as several novel antivirals. Given its favorable activity and well-described activity, as well as its broad availability, we focused on bisacodyl, a laxative used for the treatment of constipation, for follow-up studies. We find that bisacodyl inhibits chikungunya virus infection in a variety of cell types, over a range of concentrations, and over several rounds of replication. We find that bisacodyl does not disrupt chikungunya virus particles or interfere with their ability to attach to cells, but, instead, bisacodyl inhibits virus replication. Finally, we find that bisacodyl is broadly antiviral against a variety of RNA viruses, including enteroviruses, flaviviruses, bunyaviruses, and alphaviruses; however, it exhibited no activity against the DNA virus vaccinia virus. Together, these data highlight the power of compound screening to identify novel antivirals and suggest that bisacodyl may hold promise as a broad-spectrum antiviral.
Topics: Antiviral Agents; Bisacodyl; Chikungunya Fever; Chikungunya virus; Humans; Virus Replication
PubMed: 35652314
DOI: 10.1128/aac.00292-22 -
The American Journal of Gastroenterology Jun 2021Constipation is commonly treated with over-the-counter (OTC) products whose efficacy and safety remain unclear. We performed a systematic review of OTC therapies for...
INTRODUCTION
Constipation is commonly treated with over-the-counter (OTC) products whose efficacy and safety remain unclear. We performed a systematic review of OTC therapies for chronic constipation and provide evidence-based recommendations.
METHODS
We searched PubMed and Embase for randomized controlled trials of ≥4-week duration that evaluated OTC preparations between 2004 and 2020. Studies were scored using the US Preventive Services Task Force criteria (0-5 scale) including randomization, blinding, and withdrawals. The strengths of evidence were adjudicated within each therapeutic category, and recommendations were graded (A, B, C, D, and I) based on the level of evidence (level I, good; II, fair; or III, poor).
RESULTS
Of 1,297 studies identified, 41 met the inclusion criteria. There was good evidence (grade A recommendation) for the use of the osmotic laxative polyethylene glycol (PEG) and the stimulant senna; moderate evidence (grade B) for psyllium, SupraFiber, magnesium salts, stimulants (bisacodyl and sodium picosulfate), fruit-based laxatives (kiwi, mango, prunes, and ficus), and yogurt with galacto-oligosaccharide/prunes/linseed oil; and insufficient evidence (grade I) for polydextrose, inulin, and fructo-oligosaccharide. Diarrhea, nausea, bloating, and abdominal pain were common adverse events, but no serious adverse events were reported.
DISCUSSION
The spectrum of OTC products has increased and quality of evidence has improved, but methodological issues including variability in study design, primary outcome measures, trial duration, and small sample sizes remain. We found good evidence to recommend polyethylene glycol or senna as first-line laxatives and moderate evidence supporting fiber supplements, fruits, stimulant laxatives, and magnesium-based products. For others, further validation with more rigorously designed studies is warranted.
Topics: Bisacodyl; Cathartics; Chronic Disease; Citrates; Constipation; Defecation; Fruit; Gastrointestinal Agents; Glucans; Humans; Inulin; Laxatives; Magnesium; Nonprescription Drugs; Oligosaccharides; Organometallic Compounds; Picolines; Polyethylene Glycols; Psyllium; Senna Extract; Yogurt
PubMed: 33767108
DOI: 10.14309/ajg.0000000000001222 -
Journal de Pharmacie de Belgique Jun 2016Obstipation is a common complaint in pharmacies and one of the treatment strategies is the delivery of enteric coated bisacodyL tablets. This article reviews the... (Review)
Review
Obstipation is a common complaint in pharmacies and one of the treatment strategies is the delivery of enteric coated bisacodyL tablets. This article reviews the different aspects that are important for pharmacists to guarantee patient safety: whether medical treatment is required or not, which advice should be given on how to use the drug, and to conclude what is the analytical quality of the commercial products on the Belgian market.
Topics: Belgium; Bisacodyl; Constipation; Humans; Laxatives; Pharmaceutical Services; Pharmacy
PubMed: 30281225
DOI: No ID Found -
Annals of Gastroenterology 2013Quality of bowel preparation prior to colonoscopy is essential. Studies have shown a reduced volume of polyethylene glycol (PEG) with bisacodyl may improve visualization... (Review)
Review
BACKGROUND
Quality of bowel preparation prior to colonoscopy is essential. Studies have shown a reduced volume of polyethylene glycol (PEG) with bisacodyl may improve visualization and tolerability, but results have varied. Therefore, a meta-analysis was performed to analyze the efficacy of a low-volume PEG bowel preparation with bisacodyl for bowel preparation prior to colonoscopy.
METHODS
Multiple databases were searched (June 2012). Only randomized controlled trials in peer-reviewed journals on adult subjects comparing low-volume PEG (2 L) with bisacodyl versus 4 L PEG were included. Meta-analysis for the efficacy of low-volume PEG with bisacodyl and 4 L PEG were analyzed by calculating pooled estimates of number of satisfactory, excellent, and poor bowel preparations as well as adverse patient events (abdominal pain, nausea, vomiting, bloating).
RESULTS
Six studies (N=1,540) met the inclusion criteria. No statistically significant differences were noted between low-volume PEG (2 L) with bisacodyl and 4 liters PEG for number of satisfactory (OR 0.86; 95% CI: 0.45-1.63, P=0.64), excellent (OR 1.08; 95% CI: 0.78-1.50, P=0.63), or poor bowel preparations (OR 0.68; 95% CI: 0.35-1.34, P=0.27). A statistically significant decrease in nausea (OR 0.57; 95% CI: 0.36-0.89, P=0.01), vomiting (OR 0.57; 95% CI: 0.40-0.81, P<0.01), and bloating (OR 0.65; 95% CI: 0.49-0.87, P<0.01) was noted for the low-volume PEG with bisacodyl as compared to 4 L PEG. No statistically significant differences were noted between the two groups for abdominal pain (P=0.62).
CONCLUSION
Low-volume PEG (2 L) with bisacodyl demonstrates less nausea, vomiting, and bloating without adversely affecting the bowel preparation.
PubMed: 24714413
DOI: No ID Found -
Gut Sep 2017To compare efficacy of pharmacotherapies for chronic idiopathic constipation (CIC) based on comparisons to placebo using Bayesian network meta-analysis. (Meta-Analysis)
Meta-Analysis Review
OBJECTIVE
To compare efficacy of pharmacotherapies for chronic idiopathic constipation (CIC) based on comparisons to placebo using Bayesian network meta-analysis.
DATA SOURCES
We conducted searches (inception to May 2015) of MEDLINE, EMBASE, Scopus and Cochrane Central, as well as original data from authors or drug companies for the medications used for CIC.
STUDY SELECTION
Phase IIB and phase III randomised, placebo-controlled trials (RCT) of ≥4 weeks' treatment for CIC in adults with Rome II or III criteria for functional constipation; trials included at least one of four end points.
DATA EXTRACTION AND SYNTHESIS
Two investigators independently evaluated all full-text articles that met inclusion criteria and extracted data for primary and secondary end points, risk of bias and quality of evidence.
OUTCOMES
Primary end points were ≥3 complete spontaneous bowel movements (CSBM)/week and increase over baseline by ≥1 CSBM/week. Secondary end points were change from baseline (Δ) in the number of SBM/week and Δ CSBM/week.
RESULTS
Twenty-one RCTs (9189 patients) met inclusion and end point criteria: 9 prucalopride, 3 lubiprostone, 3 linaclotide, 2 tegaserod, 1 each velusetrag, elobixibat, bisacodyl and sodium picosulphate (NaP). All prespecified end points were unavailable in four polyethylene glycol studies. Bisacodyl, NaP, prucalopride and velusetrag were superior to placebo for the ≥3 CSBM/week end point. No drug was superior at improving the primary end points on network meta-analysis. Bisacodyl appeared superior to the other drugs for the secondary end point, Δ in number of SBM/week.
CONCLUSIONS
Current drugs for CIC show similar efficacy. Bisacodyl may be superior to prescription medications for Δ in the number of SBM/week in CIC.
Topics: Azabicyclo Compounds; Benzofurans; Bisacodyl; Chronic Disease; Citrates; Constipation; Defecation; Drug Monitoring; Gastrointestinal Agents; Humans; Organometallic Compounds; Picolines; Randomized Controlled Trials as Topic; Treatment Outcome
PubMed: 27287486
DOI: 10.1136/gutjnl-2016-311835 -
Neurogastroenterology and Motility Aug 2020Colonic manometry with intraluminal bisacodyl infusion can be used to assess colonic neuromuscular function in children with treatment-refractory constipation. If...
BACKGROUND
Colonic manometry with intraluminal bisacodyl infusion can be used to assess colonic neuromuscular function in children with treatment-refractory constipation. If bisacodyl does not induce high-amplitude propagating contractions (HAPCs), this can be an indication for surgical intervention. A detailed characterization of the colonic response to intraluminal bisacodyl in children with constipation may help to inform clinical interpretation of colonic manometry studies.
METHODS
Studies were performed in five pediatric hospitals. Analysis included identification of HAPCs, reporting HAPCs characteristics, and an area under the curve (AUC) analysis. Comparisons were performed between hospitals, catheter type, placement techniques, and site of bisacodyl infusion.
RESULTS
One hundred and sixty-five children were included (median age 10, range 1-17 years; n = 96 girls). One thousand eight hundred and ninety-three HAPCs were identified in 154 children (12.3 ± 8.8 HAPCs per child, 0.32 ± 0.21 HAPCs per min; amplitude 113.6 ± 31.5 mm Hg; velocity 8.6 ± 3.8 mm/s, propagation length 368 ± 175 mm). The mean time to first HAPC following bisacodyl was 553 ± 669 s. Prior to the first HAPC, there was no change in AUC when comparing pre- vs post-bisacodyl (Z = -0.53, P = .60). The majority of HAPCs terminated in a synchronous pressurization in the rectosigmoid. Defecation was associated with HAPCs (χ (1)=7.04, P < .01). Site of bisacodyl administration, catheter type, and hospital location did not alter the response.
CONCLUSIONS AND INFERENCES
Intraluminal bisacodyl induced HAPCs in 93% of children with treatment-refractory constipation. The bisacodyl response is characterized by ≥1 HAPC within 12 minutes of infusion. The majority of HAPCs terminate in a synchronous pressurization in the rectosigmoid. Optimal clinical management based upon colonic manometry findings is yet to be determined.
Topics: Adolescent; Bisacodyl; Child; Child, Preschool; Colon; Constipation; Female; Gastrointestinal Motility; Humans; Infant; Laxatives; Male; Manometry; Retrospective Studies; Treatment Outcome
PubMed: 32281199
DOI: 10.1111/nmo.13851 -
Journal of Pediatric Gastroenterology... Sep 2020Standard therapy for pediatric constipation includes osmotic laxatives with stimulant laxatives use only as rescue therapy. Limited information is available on regular...
OBJECTIVES
Standard therapy for pediatric constipation includes osmotic laxatives with stimulant laxatives use only as rescue therapy. Limited information is available on regular and long-term use of bisacodyl in pediatric population despite its common use in adult and pediatric constipation.
METHODS
Retrospective review of patients with functional constipation refractory to conventional therapy (regular use of osmotic laxatives and intermittent use of stimulant laxatives only as a rescue therapy) referred to tertiary care children's hospital (January 2007-December 2014). Patients had a bowel movement (BM) frequency of ≤2 per week and were treated with bisacodyl regularly for longer than 4 weeks. Demographic variables, bisacodyl dose and treatment duration, number of BM/week before and after treatment, side effects, and length of follow-up were recorded. Response to therapy was successful when frequency of BM increased from baseline to ≥3 BM/wk.
RESULTS
A total of 164 patients were included, 52% girls, median age 9.45 years (0.9-21 years). Bisacodyl median dose was 5 mg/day, median duration of treatment was 14 months (1-77 months) with 90% of patients taking the medication for <36 months. Median number of BM/wk doubled after initiation of bisacodyl from 2 to 4 bm/w (P < 0.001). Approximately 57% of patients had successful response. At long-term follow-up 55% of patients were successfully weaned off bisacodyl (median time of 18 months). Side effects reported in 9% of patients.
CONCLUSIONS
Bisacodyl is effective and well tolerated in the long-term treatment of pediatric functional constipation refractory to conventional therapy. Most of patients with a favorable response were successfully weaned off the medication.
Topics: Adult; Bisacodyl; Child; Constipation; Female; Gastrointestinal Agents; Humans; Laxatives; Male; Retrospective Studies
PubMed: 32459741
DOI: 10.1097/MPG.0000000000002795