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Chemistry

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Also known as: 603-50-9, Dulcolax, Brocalax, Bicol, Durolax, Fenilaxan
Molecular Formula
C22H19NO4
Molecular Weight
361.4  g/mol
InChI Key
KHOITXIGCFIULA-UHFFFAOYSA-N
FDA UNII
10X0709Y6I

Bisacodyl
A diphenylmethane stimulant laxative used for the treatment of constipation and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871)
Bisacodyl is a Stimulant Laxative. The physiologic effect of bisacodyl is by means of Increased Large Intestinal Motility, and Stimulation Large Intestine Fluid/Electrolyte Secretion.
1 2D Structure

Bisacodyl

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
[4-[(4-acetyloxyphenyl)-pyridin-2-ylmethyl]phenyl] acetate
2.1.2 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
2.1.3 InChI Key
KHOITXIGCFIULA-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC(=O)OC1=CC=C(C=C1)C(C2=CC=C(C=C2)OC(=O)C)C3=CC=CC=N3
2.2 Other Identifiers
2.2.1 UNII
10X0709Y6I
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Agaroletten

2. Apo Bisacodyl

3. Apo-bisacodyl

4. Bekunis Bisacodyl

5. Bicol

6. Bisac Evac

7. Bisac-evac

8. Bisacodyl Tannex

9. Bisacodyl Uniserts

10. Bisacodyl, Bekunis

11. Bisacodyl, Fleet

12. Bisalax

13. Bisco Lax

14. Bisco Zitron

15. Bisco-lax

16. Bisco-zitron

17. Dulco Lax

18. Dulco Lax Perles

19. Dulco-lax

20. Dulco-lax Perles

21. Dulcolax

22. Dulcolax Perles

23. Durolax

24. Fleet Bisacodyl

25. Florisan N

26. Lnolax

27. Laxagetten

28. Laxanin

29. Laxans Ratiopharm

30. Laxans-ratiopharm

31. Laxbene

32. Laxysat Brger

33. Ratio Bisacodyl

34. Ratio-bisacodyl

35. Rytmil

36. Tannex, Bisacodyl

37. Ulcolax

38. Uniserts, Bisacodyl

2.3.2 Depositor-Supplied Synonyms

1. 603-50-9

2. Dulcolax

3. Brocalax

4. Bicol

5. Durolax

6. Fenilaxan

7. Sanvacual

8. Theralax

9. Sk-bisacodyl

10. Dulcolan

11. Endokolat

12. Hillcolax

13. Stadalax

14. Eulaxan

15. Godalax

16. Ivilax

17. Laxadin

18. Laxans

19. Laxine

20. Laxorex

21. Neolax

22. Nigalax

23. Pyrilax

24. Telemin

25. Zetrax

26. Laxanin N

27. Laco

28. Modane

29. Phenol, 4,4'-(2-pyridinylmethylene)bis-, Diacetate (ester)

30. Evac-q-tabs

31. La96a

32. (pyridin-2-ylmethylene)bis(4,1-phenylene) Diacetate

33. Bis(p-acetoxyphenyl)-2-pyridylmethane

34. Di-(p-acetoxyphenyl)-2-pyridylmethane

35. Di-(4-acetoxyphenyl)-2-pyridylmethane

36. Feen-a-mint Tablets

37. Mls000069729

38. 2-(4,4'-diacetoxydiphenylmethyl)pyridine

39. 4,4'-(2-pyridylmethylene)diphenol Diacetate (ester)

40. (4,4'-diacetoxydiphenyl)(2-pyridyl)methane

41. 4,4'-(2-pyridylmethylene)diphenol Diacetate

42. [4-[(4-acetyloxyphenyl)-pyridin-2-ylmethyl]phenyl] Acetate

43. Correctol Tablets, Caplets

44. Nsc-755914

45. 4,4'-diacetoxydiphenylpyridyl-2-methane

46. Smr000058226

47. Mls002701749

48. Phenol, 4,4'-(2-pyridylmethylene)di-, Diacetate (ester)

49. Ulcolax

50. Nsc614826

51. 10x0709y6i

52. Ncgc00016522-05

53. Ncgc00016522-10

54. 4-{[4-(acetyloxy)phenyl](pyridin-2-yl)methyl}phenyl Acetate

55. Bisacodyl 100 Microg/ml In Acetonitrile

56. Cas-603-50-9

57. Deficol

58. Phenol, 4,4'-(2-pyridinylmethylene)bis-, 1,1'-diacetate

59. Dsstox_cid_2681

60. Dsstox_rid_76689

61. Dsstox_gsid_22681

62. 4,4'-(pyridin-2-ylmethylene)bis(4,1-phenylene) Diacetate

63. Bisacodilo

64. Bisacodylum

65. Halflytely

66. Bisacodylum [inn-latin]

67. Bisacodilo [inn-spanish]

68. Hsdb 3016

69. (pyridin-2-ylmethylene)di-4,1-phenylene Diacetate

70. Sr-01000000233

71. Einecs 210-044-4

72. Brn 0323727

73. Horton

74. Ccris 8864

75. Unii-10x0709y6i

76. Bisacodyl [usp:inn:ban:jan]

77. Bisacodyl,(s)

78. Dulcolax (tn)

79. Prestwick_780

80. Mfcd00038039

81. Spectrum_000086

82. Halflytely (salt/mix)

83. Bisacodyl [inn]

84. Bisacodyl [jan]

85. Opera_id_884

86. Bisacodyl [mi]

87. Bisacodyl [hsdb]

88. Prestwick0_000419

89. Prestwick1_000419

90. Prestwick2_000419

91. Prestwick3_000419

92. Spectrum2_000149

93. Spectrum3_000318

94. Spectrum4_000256

95. Spectrum5_000898

96. Bisacodyl [vandf]

97. 4,4'-(2-pyridylmethylene)bisphenol Diacetate

98. Bisacodyl [mart.]

99. Chembl942

100. Ncichal_000004

101. Ncimech_000456

102. Bisacodyl [usp-rs]

103. Bisacodyl [who-dd]

104. Cid_2391

105. Regid_for_cid_2391

106. Schembl21044

107. Bspbio_000378

108. Bspbio_001916

109. Kbiogr_000692

110. Kbioss_000506

111. Divk1c_000347

112. Spectrum1500147

113. Spbio_000258

114. Spbio_002317

115. Bisacodyl (jp17/usp/inn)

116. Bpbio1_000416

117. Chebi:3125

118. Bisacodyl [orange Book]

119. Bisacodyl For System Suitability

120. Bisacodyl [ep Monograph]

121. Dtxsid1022681

122. Bdbm61400

123. Bisacodyl For Peak Identification

124. Hms501b09

125. Kbio1_000347

126. Kbio2_000506

127. Kbio2_003074

128. Kbio2_005642

129. Kbio3_001416

130. Bisacodyl [usp Monograph]

131. Ninds_000347

132. Hms1569c20

133. Hms1920g21

134. Hms2090k15

135. Hms2091o03

136. Hms2096c20

137. Hms2235i11

138. Hms3373l17

139. Hms3652e04

140. Hms3713c20

141. Pharmakon1600-01500147

142. Bcp18567

143. Hy-b0557

144. Zinc3830321

145. Tox21_110472

146. Tox21_200338

147. Ccg-35661

148. Ccg-36442

149. Halflytely Component Bisacodyl

150. Nsc755914

151. S4047

152. Stk293202

153. Akos001599884

154. Tox21_110472_1

155. Db09020

156. Nsc 755914

157. Nsc-614826

158. Bisacodyl Component Of Halflytely

159. Idi1_000347

160. 4,4'-diacetoxydiphenylpyrid-2-ylmethane

161. Bisacodyl, Active Ingredient Of Viraplex

162. Ncgc00016522-01

163. Ncgc00016522-02

164. Ncgc00016522-03

165. Ncgc00016522-04

166. Ncgc00016522-06

167. Ncgc00016522-07

168. Ncgc00016522-08

169. Ncgc00016522-09

170. Ncgc00016522-11

171. Ncgc00016522-12

172. Ncgc00023260-03

173. Ncgc00023260-04

174. Ncgc00023260-05

175. Ncgc00023260-06

176. Ncgc00257892-01

177. Ac-24284

178. As-15820

179. Nci60_004954

180. Sbi-0051297.p003

181. 4,4-(2-pyridylmethylene)diphenol Diacetate

182. Ab00051928

183. B1898

184. B5066

185. Ft-0603486

186. Sw196918-3

187. A14914

188. D00245

189. D81813

190. Ab00051928-17

191. Ab00051928_18

192. Ab00051928_19

193. Bisacodyl, Analytical Standard, For Drug Analysis

194. A832704

195. Phenol, 4,4'-(2-pyridylmethylene)di-, Diacetate

196. Q417874

197. Q-200726

198. Q-200727

199. Sr-01000000233-2

200. Sr-01000000233-3

201. (pyridin-2-ylmethanediyl)dibenzene-4,1-diyl Diacetate

202. Brd-k39987650-001-05-0

203. Brd-k39987650-001-15-9

204. Phenol, 4,4'-(2-pyridinylmethylene)bis-, Diacetate

205. Phenol,4'-(2-pyridinylmethylene)bis-, Diacetate (ester)

206. Phenol,4,4'-(2-pyridinylmethylene)bis-,1,1'-diacetate

207. 4-[[4-(acetyloxy)phenyl](2-pyridyl)methyl]phenyl Acetate

208. Bisacodyl, European Pharmacopoeia (ep) Reference Standard

209. 4-[[4-(acetyloxy)phenyl](2-pyridinyl)methyl]phenyl Acetate #

210. Bisacodyl, United States Pharmacopeia (usp) Reference Standard

211. [4-[(4-acetoxyphenyl)-(2-pyridyl)methyl]phenyl] Acetate;bisacodyl

212. Bisacodyl For Peak Identification, European Pharmacopoeia (ep) Reference Standard

213. Bisacodyl For System Suitability, European Pharmacopoeia (ep) Reference Standard

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 361.4 g/mol
Molecular Formula C22H19NO4
XLogP33.8
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count5
Rotatable Bond Count7
Exact Mass361.13140809 g/mol
Monoisotopic Mass361.13140809 g/mol
Topological Polar Surface Area65.5 Ų
Heavy Atom Count27
Formal Charge0
Complexity457
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 2  
Drug NameHalflytely
Active Ingredientsodium chloride; sodium bicarbonate; Bisacodyl; potassium chloride; polyethylene glycol 3350
Dosage FormFor solution, tablet, delayed release
RouteOral
Strength5mg,n/a; n/a,5.6gm; n/a,210gm; n/a,0.74gm; n/a,2.86gm
Market StatusPrescription
CompanyBraintree

2 of 2  
Drug NameHalflytely
Active Ingredientsodium chloride; sodium bicarbonate; Bisacodyl; potassium chloride; polyethylene glycol 3350
Dosage FormFor solution, tablet, delayed release
RouteOral
Strength5mg,n/a; n/a,5.6gm; n/a,210gm; n/a,0.74gm; n/a,2.86gm
Market StatusPrescription
CompanyBraintree

4.2 Therapeutic Uses

Cathartics

National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)


Oral bulk-forming, lubricant, and stool softener laxatives are indicated prophylactically in patients who should not strain during defecation, such as those with an episiotomy wound, painful thrombosed hemorrhoids, fissures or perianal abscesses, body wall and diaphragmatic hernias , anorectal stenosis, or postmyocardial infarction. /Laxatives; Included in US product labeling/

Thomson.Micromedex. Drug Information for the Health Care Professional. 24th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2004., p. 1731


Oral laxatives are indicated for the short-term relief of constipation. Oral bulk-forming laxatives, stimulant laxatives, and carbon dioxide-releasing suppositories are indicated to facilitate defecation in geriatric patients with diminished colonic motor response... /Laxatives; Included in US product labeling/

Thomson.Micromedex. Drug Information for the Health Care Professional. 24th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2004., p. 1731


Bisacodyl is useful as a laxative for the occasional relief of constipation and in bowel cleansing preparation for x-ray or endoscopic examination. Bisacodyl may be used as a laxative in postoperative, antepartum, or postpartum care or in preparation for delivery

Physicians Desk Reference. 58th ed. Thomson PDR. Montvale, NJ 2004., p. 1285


In severe cases of constipation, such as with fecal impaction, mineral oil and stool softener laxatives administered orally or rectally are indicated to soften the impacted feces. To help complete the evacuation of the impacted colon, a rectal stimulant or saline laxative may follow. /Laxatives; Included in US product labeling/

Thomson.Micromedex. Drug Information for the Health Care Professional. 24th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2004., p. 1731


4.3 Drug Warning

In therapeutic oral doses, all stimulant laxatives may produce some degree of abdominal discomfort, nausea, mild cramps, griping, and/or faintness. Rectal administration of bisacodyl suspensions ... may cause irritation and a sensation of burning of the rectal mucosa and mild proctitis. /Stimulant laxatives/

McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 2784


Weakness, incoordination, and orthostatic hypotension may be exacerbated in elderly patients as a result of significant electrolyte loss when stimulant laxatives are used repeatedly to evacuate the colon. /Stimulant laxatives/

Thomson.Micromedex. Drug Information for the Health Care Professional. 24th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2004., p. 1732


Bisacodyl enteric-coated tablets are not recommenced for children up to 6 years of age since patients in this age group may have difficulty swallowing the tablet without chewing it. Gastric irritation may develop if the enteric coating is destroyed by chewing.

Thomson.Micromedex. Drug Information for the Health Care Professional. 24th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2004., p. 1732


Laxatives should not be given to young children unless prescribed by a physician. Since children are not usually able to describe their symptoms precisely, proper diagnosis should precede the use of laxatives. This will avoid the complication of an existing condition (eg appendicitis) or the appearance of more severe side effects. /Laxatives/

Thomson.Micromedex. Drug Information for the Health Care Professional. 24th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2004., p. 1732


For more Drug Warnings (Complete) data for BISACODYL (12 total), please visit the HSDB record page.


4.4 Drug Indication

Bisacodyl is indicated to relieve occasional constipation and irregularity.


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Patients should be counselled regarding abdominal pain, nausea, vomiting, or a change in bowel function that lasts longer than 2 weeks. It has a wide therapeutic index, as patients can take 5-15 mg orally. Patients taking bisacodyl should be counselled before taking the medication if they are already experiencing abdominal pain, nausea, vomiting, or a change in bowel function lasting longer than 2 weeks. Patients should also be counselled to stop taking the medication if they experience rectal bleeding or no bowel movement in 12 hours.


5.2 MeSH Pharmacological Classification

Cathartics

Agents that are used to stimulate evacuation of the bowels. (See all compounds classified as Cathartics.)


Laxatives

Agents that produce a soft formed stool, and relax and loosen the bowels, typically used over a protracted period, to relieve CONSTIPATION. (See all compounds classified as Laxatives.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
BISACODYL
5.3.2 FDA UNII
10X0709Y6I
5.3.3 Pharmacological Classes
Stimulant Laxative [EPC]; Stimulation Large Intestine Fluid/Electrolyte Secretion [PE]; Increased Large Intestinal Motility [PE]
5.4 ATC Code

A06AB02

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355


A - Alimentary tract and metabolism

A06 - Drugs for constipation

A06A - Drugs for constipation

A06AB - Contact laxatives

A06AB02 - Bisacodyl


A - Alimentary tract and metabolism

A06 - Drugs for constipation

A06A - Drugs for constipation

A06AG - Enemas

A06AG02 - Bisacodyl


5.5 Absorption, Distribution and Excretion

Absorption

Oral formulations of bisacodyl are only 16% bioavailable. A 10 mg enteric coated oral tablet reaches a Cmax of 26 ng/mL with a Tmax of 8 hours, while a 10 mg oral solution reaches a Cmax of 237 ng/mL with a Tmax of 1.7 hours. A 10 mg suppository reaches a Cmax of 0-64 ng/mL. In lactating women, 10mg of oral bisacodyl reaches a Cmax of 20.5-195 ng/mL, with a Tmax of 3-4 hours, and a geometric mean AUC after a single dose of 471 h\*ng/mL. After multiple doses, the geometric mean AUC decreases to 311 h\*ng/mL.


Route of Elimination

The majority of bisacodyl is eliminated in the feces. 13.8-17.0% of a bisacodyl dose is eliminated in the urine as the active metabolite BHPM.


Volume of Distribution

Data regarding the volume of distribution of bisacodyl is not readily available. However, the volume of distribution of the active metabolite, BHPM, in lactating women is 181 L after a single dose and 289 L at steady state.


Clearance

Data regarding the clearance of bisacodyl is not readily available. The apparent plasma clearance of the active metabolite, BHPM, in lactating women after a single 10 mg oral dose is 272 mL/min and after multiple doses is 412 mL/min.


Absorption of bisacodyl ... is minimal following oral or rectal administration. Any bisacodyl that is absorbed is metabolized in the liver and excreted in the urine and/or distributed in milk.

McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 2787


Following oral administration of therapeutic dosages of diphenylmethane derivatives, /bowel/ evacuation is produced in 6 to 8 hours. Rectally administered bisacodyl ... produces evacuation of the colon in within 15 minutes to 1 hour.

McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 2787


As much as 5% of orally administered dose is absorbed & excreted in urine as glucuronide.

Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 1046


Excreted primarily in the feces ...

Cowl, C.T. Physician's Handbook 10th edition. Lippincott Williams & Wilkins, Philadelphia, PA. 2003, p. 209


The absorption and plasma level profile and laxative effects of 10 mg bisacodyl as an experimental solution ... in 12 healthy volunteers are described. Results indicate only small amounts of drug were systemically available after administration of /solution/, dragee /(sugar coated capsule)/ and suppository. Urinary excretion was 43.4% for solution, 9.2% for dragee and 3.1% for suppository.

Roth W; Arzneim Forsch 39 (4): 570-74 (1988)


5.6 Metabolism/Metabolites

Bisacodyl is deacetylated to the active bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM) by an intestinal deacetylase. A small amount of BHPM is absorbed from the gastrointestinal tract, and is glucuronidated before elimination.


Following oral or rectal administration bisacodyl is converted to the active desacetyl metabolite bis(p-hydroxyphenyl)pyridyl-2-methane by intestinal and bacterial enzymes.

Reynolds, J.E.F., Prasad, A.B. (eds.) Martindale-The Extra Pharmacopoeia. 28th ed. London: The Pharmaceutical Press, 1982., p. 1363


HPLC method which permits simultaneous detection of bisacodyl (BIS) & its monodesacetylated (mono) as well as totally desacetylated (DES) form, was used to study the intestinal handling of BIS (20 nmol/mL), when incubated for 60 min at the mucosal side of the preparations specified. In jejunal mucosa fluid, BIS disappeared completely in short time, & there was nearly equivalent rise in DES; mono was transitorily present. Hydrolysis was also rapid in mucosal fluid which had been in contact with jejunal sacs for 30 sec, but BIS was stable in blank incubations. Hydrolysis of BIS was slower by colonic than by jejunal sacs, & all 3 forms were present during incubation. It seemed still lower in mucosal fluid which had been in contact with colonic sac for 5 min. BIS & DES accumulate in jejunal & colonic serosal fluid mainly as conjugates (above 95%), & DES was in all cases the only conjugated metabolite present. Accumulation in jejunal serosal fluid was same whether BIS or DES was added.

Hillestad B et al; Intestinal Handling of Bisacodyl and Picosulphate by Everted Sacs of the Rat Jejunum and Stripped Colon; Acta Pharmacol Toxicol 51(4) 388 (1982)


5.7 Biological Half-Life

Data regarding the half life of bisacodyl is not readily available. The half life of the active metabolite, BHPM, in lactating women was 7.3 h after a single 10 mg oral dose and 10.0 h after multiple doses.


5.8 Mechanism of Action

Bisacodyl is deacetylated to the active bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM) by an intestinal deacetylase. BHPM can stimulate parasympathetic nerves in the colon directly to increase motility and secretions. Bisacodyl stimulates adenylate cyclase, increasing cyclic AMP, leading to active transport of chloride and bicarbonate out of cells. Sodium ions, potassium ions, and water passively leave the cell; while sodium and chloride ions are unable to be reabsorbed. Water is also be transported from the luminal side of cells into the vasculature by aquaporin 3. Bisacodyl decreases expression of aquaporin 3, preventing water from moving into the vasculature, which may contribute to increased water in the colon. Bisacodyl directly stimulates parasympathetic nerves in the colon, stimulating contraction of longitudinal smooth muscle but not circular smooth muscle.


Bisacodyl is a stimulant laxative, ... acting directly on the colonic mucosa-where it stimulates sensory nerve endings to produce parasympathetic reflexes resulting in increased peristaltic contractions of the colon. The contact action of the drug is restricted to the colon, and motility of the small intestine is not appreciably influenced.

Physicians Desk Reference. 58th ed. Thomson PDR. Montvale, NJ 2004., p. 1285


/Bisacodyl/ increases water retention in the stool by coating surfaces of stool and intestines with a water-immisicible film. Lubricant effect eases passage of contents through intestines. Emulsification of lubricant tends to enhance its ability to soften stool mass. /Laxatives/

Thomson.Micromedex. Drug Information for the Health Care Professional. 24th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2004., p. 1731


Recent studies show that these drugs alter fluid and electrolyte absorption producing net intestinal fluid accumulation and laxation. Some of these drugs may directly stimulate active intestinal ion secretion. Increased concentrations of cyclic 3',5'-adenosine monophosphate (cAMP), occurring in colonic mucosa cells following administration of stimulant laxatives, may alter the permeability of these cells and mediate active ion secretion thereby producing net fluid accumulation and laxative action. /Stimulant Laxatives/

McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 2782


Bisacodyl caused dose-dependent contractions in isolated guinea pig ileum & taenia coli which was not prevented by atropine or pheniramine. It prevented acetylcholine- & histamine-induced contractions. Bisacodyl-induced contractions were not caused by a decrease in endogenous cyclic amp level. However, both endogenous cyclic amp & verapamil (a calcium transport inhibitor) inhibited bisacodyl-induced contractions, suggesting site of action on calcium-dependent contractile system of smooth muscle cells.

Schubert et al; Mode of Action of Bisacodyl on the Smooth Muscle of the Small and Large Intestine of the Guinea Pig; Arzneim-Forsch 25(7) 1053 (1975)


Intestinal secretagogues as well as the laxative, bisacodyl, raise the K+ efflux rate across the mucosal border by 200-300%. Results suggest that laxatives may increase rate of K+ secretion into the colonic lumen by raising the K+ permeability of the mucosal border.

Moreto M et al; Effects of Secretagogues on the Potassium Ion Permeability of Mucosal and Serosal Borders of Rabbit Colonic Mucosa; Biochim Biophys Acta 648(29) 215 (1981)


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07-Jan-2021
22-Aug-2024
KGS
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