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Bisacodyl (INN) is an organic compound that is used as a laxative drug. It works directly on the colon to produce a bowel movement. It is typically prescribed for relief of constipation and for the management of neurogenic bowel dysfunction as well as part of bowel preparation before medical examinations, such as for a colonoscopy.^[1]

Bisacodyl is a derivative of triphenylmethane. It was first used as a laxative in 1953 because of its structural similarity to phenolphthalein.^[2]^[3]

Available forms

Bisacodyl is marketed under the trade names Dulcolax/Durolax, Fleet, Nourilax, Alophen, Correctol, and Carter's Little Pills (formerly Carter's Little Liver Pills^[4]) as well as being available generically. It is usually sold as 5 mg tablets, 10 mg suppositories, or 5 mg pediatric suppositories. It is also available as a 1.25 US fluid ounces (37 ml) prepackaged enema containing a 10 mg delivered dose of liquid bisacodyl.^[5]

Administration

When bisacodyl is administered orally, it is usually taken at bedtime. Oral administration is known to produce no action for more than eight hours and then to work suddenly and relatively quickly. This is especially true if more than 10 milligrams is taken at one time. Normally the dosage is 5 or 10 milligrams, but up to 30 milligrams can be taken for complete cleansing of the bowel before a procedure. If taken at the maximum dosage, there will likely be a sudden, extremely powerful, uncontrollable bowel movement and so precautions should be taken. It is not recommended to take bisacodyl within one hour of taking an antacid or milk, as this may destroy the tablet coating and irritate the stomach. If taken too early in the evening, the action of this drug can start during sleep with undesirable results.

When administered rectally in suppository form, it is usually effective in 15 to 60 minutes. Two suppositories can be inserted at once if a very strong, purgative, enema-like result is needed. A few hours after the initial evacuation, there can be a secondary action which will continue as long as there is unexpelled bisacodyl present in the rectum.

As a small commercially prepared enema, it is usually effective in 5 to 20 minutes.^[5]

Mechanism of action

Bisacodyl works by stimulating enteric nerves to cause colonic contractions. It is also a contact laxative; it increases fluid and salt secretion. Action of bisacodyl on small intestine is negligible; stimulant laxatives mainly promote evacuation of the colon.^[5]

References

^ Wexner, S. D.; Beck, D. E.; Baron, T. H.; Fanelli, R. D.; Hyman, N.; Shen, B.; Wasco, K. E.; American Society of Colon and Rectal Surgeons; American Society for Gastrointestinal Endoscopy; Society of American Gastrointestinal and Endoscopic Surgeons (2006). "A consensus document on bowel preparation before colonoscopy: prepared by a task force from the American Society of Colon and Rectal Surgeons (ASCRS), the American Society for Gastrointestinal Endoscopy (ASGE), and the Society of American Gastrointestinal and Endoscopic Surgeons (SAGES)". Gastrointestinal Endoscopy 63 (7): 894–909. doi:10.1016/j.gie.2006.03.918. ISSN 0016-5107. PMID 16733101.
^ Stiens SA; Luttrel W; Binard JE (November 1998). "Polyethylene glycol versus vegetable oil based bisacodyl suppositories to initiate side-lying bowel care: a clinical trial in persons with spinal cord injury" (PDF). Spinal Cord 36 (11): 777–81. doi:10.1038/sj.sc.3100702. PMID 9848486.
^ Evans, I. Lynn, "Methods and techniques: The use of Bisacodyl suppositories in preparation for sigmoidoscopy", Gut, British Medical Journal, 1964, 5, 271
^ "Medicine: Cut Out the Liver". Time. 1951-04-16. Retrieved 2010-04-26.
^ ^a ^b ^c Robert Engelhorn, Ernst Seeger and Jan H. Zwaving "Laxatives" in Ullmann's Encyclopedia of Industrial Chemistry, Wiley-VCH, Weinheim, 2000. doi:10.1002/14356007.a15_183

External links

Bisacodyl at Drugdigest.org
Bisacodyl Consumer Drug Information
Dulcolax Laxative

UpToDate Contents

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1. 成人におけるS状結腸鏡検査および大腸内視鏡検査のための前処置 bowel preparation for colonoscopy and flexible sigmoidoscopy in adults
2. 成人における慢性便秘のマネージメント management of chronic constipation in adults
3. 高齢者における便秘 constipation in the older adult
4. 幼児および小児における慢性機能性便秘および便失禁：治療 chronic functional constipation and fecal incontinence in infants and children treatment
5. 虚偽性下痢症 factitious diarrhea

English Journal

Component analysis of Pu-erh and its anti-constipation effects.

Li G, Wang Q, Qian Y, Zhou Y, Wang R, Zhao X.Author information Department of Biological and Chemical Engineering, Chongqing University of Education, Chongqing 400067, P.R. China.AbstractThe aim of this study was to investigate the effects of Pu-erh tea on activated carbon-induced constipation in ICR mice. The changes in body weight, dietary intake, gastrointestinal transit, first black stool defecation time, number and weight of feces, water content of feces and various levels of substances in serum were used to evaluate the anti-constipation effects of Pu-erh tea. Body weight, dietary intake and the amount of water consumed by mice decreased with activated carbon-induced constipation and those of the sample treated group mice were higher than the control group mice. The first black stool time of normal, control, bisacodyl (100 mg/kg) and 200, 400 and 800 mg/kg Pu-erh tea treated mice were 90, 221, 118, 178, 155 and 139 min, respectively. Following oral administration of 200, 400 and 800 mg/kg of Pu-erh tea and 100 mg/kg of bisacodyl, the gastrointestinal transit rates were shortened by 48.6, 59.6, 78.0 and 91.9%, respectively. Serum levels of motilin (MTL), gastrin (Gas), endothelin (ET), acetylcholine enzyme (AchE), substance P (SP) and vasoactive intestinal peptide (VIP) were significantly increased and somatostatin (SS) was decreased when the mice were treated with different concentrations of Pu-erh tea compared with the untreated control mice. These results demonstrate that Pu-erh tea has a similar preventive effect to bisacodyl and it may be used as a functional food to prevent constipation.
Molecular medicine reports.Mol Med Rep.2014 May;9(5):2003-9. doi: 10.3892/mmr.2014.2009. Epub 2014 Mar 5.
The aim of this study was to investigate the effects of Pu-erh tea on activated carbon-induced constipation in ICR mice. The changes in body weight, dietary intake, gastrointestinal transit, first black stool defecation time, number and weight of feces, water content of feces and various levels of s
PMID 24604453

Monitoring of 29 weight loss compounds in foods and dietary supplements by LC-MS/MS.

Kim HJ1, Lee JH, Park HJ, Cho SH, Cho S, Kim WS.Author information 1a Advanced Analysis Team, Toxicological Evaluation and Research Department, National Institute of Food and Drug Safety Evaluation , Ministry of Food and Drug Safety , Cheongwon-gun , Chungcheongbuk-do , Korea.AbstractBecause of the rapid growth in dietary supplement availability and public concern for weight control, the investigation of foods and various dietary supplements illegally adulterated with weight loss compounds has become increasingly important. A total of 29 weight loss compounds, including sennoside, sibutramine, ephedrine and their analogues, found to be adulterated in foods and dietary supplements were simultaneously examined by LC-MS/MS. The 188 samples were collected between 2009 and 2012 in South Korea, and method validation was performed to determine the adulterants to the weight loss compounds. LODs, LOQs and linearity ranged from 0.03 to 7.5 ng ml-1, from 0.08 to 30.00 ng ml-1, and from 0.990 to 0.999, respectively. The results showed that nine weight loss compounds, namely bisacodyl, desmethylsibutramine, didesmethylsibutramine, ephedrine, fluoxetine, pseudoephedrine, sennoside A, sennoside B and sibutramine, were detected in 62 of all collected samples and were found in order of frequency as follows: sibutramine, 25.7%; sennoside A, 22.9%; sennoside B, 20.0%; fluoxetine, 8.6%; desmethylsibutramine, 7.1%; bisacodyl, ephedrine, and pseudoephedrine, 4.3%; and didesmethylsibutramine, 2.9%. Sibutramine, which was the most frequently found adulterant, ranged in levels from 0.03 to 132.40 mg g-1 (2010), from 0.88 to 76.2 mg g-1 (2011), and from 0.07 to 0.24 mg g-1 (2012). Although the concentrations of most compounds ranged widely, some compounds such as bisacodyl and fluoxetine were found at high concentrations in several samples.
Food additives & contaminants. Part A, Chemistry, analysis, control, exposure & risk assessment.Food Addit Contam Part A Chem Anal Control Expo Risk Assess.2014 Mar 26. [Epub ahead of print]
Because of the rapid growth in dietary supplement availability and public concern for weight control, the investigation of foods and various dietary supplements illegally adulterated with weight loss compounds has become increasingly important. A total of 29 weight loss compounds, including sennosid
PMID 24499058

Adjuncts to colonic cleansing before colonoscopy.

Park S, Lim YJ.Author information Sanghoon Park, Department of Internal Medicine, KEPCO Medical Center, KEPCO Medical Foundation, Seoul 132-703, South Korea.AbstractPre-procedural cleansing of the bowel can maximize the effectiveness and efficiency of colonoscopy. Yet, efficacy of the current gold standard colonic preparation method - high-volume oral administration of purgative agents 12-24 h prior to the procedure - is limited by several factors, such as patient compliance (due to poor palatability and inconvenience of the dosing regimen) and risks of complications (due to drug interactions or intolerance). Attempts to resolve these limitations have included providing adjunctive agents and methods to promote the colonic cleansing ability of the principal purgative agent, with the aim of lessening unpleasant side effects (such as bloating) and reducing the large ingested volume requirement. Several promising adjunctive agents are bisacodyl, magnesium citrate, senna, simethicone, metoclopramide, and prokinetics, and each are being investigated for their potential. This review provides an up to date summary of the reported investigations into the potencies and weaknesses of the key adjuncts currently being applied in clinic as supplements to the traditional bowel preparation agents. While the comparative analysis of these adjuncts showed that no single agent or method has yet achieved the goal of completely overcoming the limitations of the current gold standard preparation method, they at least provide endoscopists with an array of alternatives to help improve the suboptimal efficacy of the main cleansing solutions when used alone. To aid in this clinical endeavor, a subjective grade was assigned to each adjunct to indicate its practical value. In addition, the systematic review of the currently available agents and methods provides insight into the features of each that may be overcome or exploited to create novel drugs and strategies that may become adopted as effective bowel cleansing adjuncts or alternatives.
World journal of gastroenterology : WJG.World J Gastroenterol.2014 Mar 21;20(11):2735-2740.
Pre-procedural cleansing of the bowel can maximize the effectiveness and efficiency of colonoscopy. Yet, efficacy of the current gold standard colonic preparation method - high-volume oral administration of purgative agents 12-24 h prior to the procedure - is limited by several factors, such as pati
PMID 24659864

Japanese Journal

An assessment of bisacodyl-based bowel preparation for colonoscopy in children

SHAOUL RON,HALOON LINA
Journal of gastroenterology 42(1), 26-28, 2007-01-01
NAID 10018540784

臨床の実際緩下剤bisacodyl大量服用中止後に高度の浮腫をきたした慢性便秘症の1例

野村昌哉,井上善文,桂浩 [他]
外科治療 93(1), 117-120, 2005-07
NAID 40006821669

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リンク元	「大腸刺激性下剤」「ビサコジル」

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Bisacodyl
Systematic (IUPAC) name
	(pyridin-2-ylmethanediyl)dibenzene-4,1-diyl diacetate; OR; 4,4'-(pyridin-2-ylmethylene)bis(4,1-phenylene) diacetate
Clinical data
AHFS/Drugs.com	monograph
MedlinePlus	a601027
Pregnancy; category	C;
Legal status	OTC;
Routes of; administration	Oral, rectal
Pharmacokinetic data
Bioavailability	15%
Metabolism	Hepatic (CYP450-mediated)
Biological half-life	16 Hours
Excretion	primarily in the feces, systemically absorbed drug is excreted in the urine
Identifiers
CAS Registry Number	603-50-9
ATC code	A06AB02 A06AG02
PubChem	CID: 2391
DrugBank	DB09020
ChemSpider	2299
UNII	10X0709Y6I
KEGG	D00245
ChEMBL	CHEMBL942
Chemical data
Formula	C22H19NO4
Molecular mass	361.391 g/mol
	SMILES O=C(Oc1ccc(cc1)C(c2ccc(OC(=O)C)cc2)c3ncccc3)C ;
	InChI InChI=1S/C22H19NO4/c1-15(24)26-19-10-6-17(7-11-19)22(21-5-3-4-14-23-21)18-8-12-20(13-9-18)27-16(2)25/h3-14,22H,1-2H3 ; Key:KHOITXIGCFIULA-UHFFFAOYSA-N ;
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