Is bisacodyl absorbed at all from suppositories in man?

Flig, E.; Hermann, T; Zabel, Maciej

doi:10.1016/s0378-5173(99)00385-3

Cited by 33 publications

(18 citation statements)

References 3 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Bisacodyl [bis(p-acetoxyphenyl)-2-pyridylmethane] (BIS) is a stimulant laxative. After oral administration it is rapidly converted to the active metabolite bis(p-hydroxyphenyl)-2-pyridylmethane (BHPM) and its laxative action is initiated through a direct interaction of the drug in the intestine by activating protein kinase C, releasing prostaglandin E2 and, thereby, inducing net fluid secretion (13,14). About 50% of the dose is eliminated in the faeces as BHPM (14).…”

Section: Pilot Studymentioning

confidence: 99%

“…After oral administration it is rapidly converted to the active metabolite bis(p-hydroxyphenyl)-2-pyridylmethane (BHPM) and its laxative action is initiated through a direct interaction of the drug in the intestine by activating protein kinase C, releasing prostaglandin E2 and, thereby, inducing net fluid secretion (13,14). About 50% of the dose is eliminated in the faeces as BHPM (14). Bisacodyl has been used in the past for similar sampling procedures (15), and its effects on the intralumenal physiology have been shown to be reversible (16,17).…”

Section: Pilot Studymentioning

confidence: 99%

See 1 more Smart Citation

Characterization of the Contents of Ascending Colon to Which Drugs are Exposed After Oral Administration to Healthy Adults

et al. 2009

View full text Add to dashboard Cite

show abstract

Section: Pilot Studymentioning

confidence: 99%

Section: Pilot Studymentioning

confidence: 99%

Characterization of the Contents of Ascending Colon to Which Drugs are Exposed After Oral Administration to Healthy Adults

et al. 2009

View full text Add to dashboard Cite

show abstract

“…The laxative effect of DAB is believed to be due to a direct interaction with the lower intestine because the effect did not correlate with plasma DAB concentrations after oral or rectal bisacodyl administration (7,20). Our results support the previous findings because the mucosal application of DAB induced increases in I sc and G t in the rat distal colon, but serosal applications did not (Fig.…”

Section: Dab-induced Electrolyte Transport Is Mucosal Sidespecific Inmentioning

confidence: 99%

“…In addition, DAB induces a more potent mucus secretory response than bisacodyl (9); this secretory response probably contributes to its laxative action. DAB may also directly interact with the mucosal side of the colon because no correlation was noted between plasma concentrations of DAB and its laxative response (7). According to previous reports, oral or rectal administration of bisacodyl induces laxative effects in rats (16).…”

mentioning

confidence: 99%

Desacetyl bisacodyl-induced epithelial Cl− secretion in rat colon and rectum

Fujita

Karaki

Tateoka³

et al. 2016

Biomed. Res.

View full text Add to dashboard Cite

The purpose of this study was to clarify the mode of desacetyl bisacodyl (DAB)-induced secretory action in intestinal tissues using an Ussing chamber assay. DAB is the active metabolite of the laxative bisacodyl. In mucosal-submucosal preparations, mucosal application of DAB induced a transient decrease followed by subsequent increases in short-circuit current and tissue conductance in a concentration-dependent manner. DAB-induced responses occurred from the middle colon to the rectal segment but not in the proximal colon. Moreover, these responses were not observed under chloride (Cl − )-free conditions or in the presence of DAB on the serosal side of the mucosalsubmucosal specimens. Treatment with tetrodotoxin had no effect on the DAB-induced responses; however, mucosal treatment with a COX inhibitor piroxicam resulted in the elimination of responses. These results suggest that DAB may contribute to the laxative action by inducing Cl − secretion which is associated with the COX signaling pathway. This study also demonstrated that the DAB target molecule is present on the mucosal side from the middle colon to the rectal segment.Bisacodyl, a diphenylmethane derivative, is a stimulant laxative used for treating constipation or for pretreatment prior to a bowel operation. Desacetyl bisacodyl [DAB; IUPAC name: bis-(p-hydroxypheny)-pyridyl-2-methane] is the active form of bisacodyl, which is rapidly converted to DAB by intestinal brush border enzymes and bacterial enzymes after oral administration (17, 21). In addition, DAB induces a more potent mucus secretory response than bisacodyl (9); this secretory response probably contributes to its laxative action. DAB may also directly interact with the mucosal side of the colon because no correlation was noted between plasma concentrations of DAB and its laxative response (7). According to previous reports, oral or rectal administration of bisacodyl induces laxative effects in rats (16). Bisacodyl also induces fluid accumulation, which was demonstrated by the colonic loop method or the measurement of water content in feces (9,11,22). Oral administration of bisacodyl induced Na/KATPase inhibition and an increase in PGE 2 and adenyl cyclase activity in rat colonic mucosa (19). Na/ K ATPase-inhibition may contribute to the inhibition of water absorption, and the increases in PGE 2 and adenyl cyclase activity could lead to the secretion of fluid into the lumen. These results indicated that bisacodyl may influence water transport in the colon. However, at present, it is still not clear whether bisacodyl induces water and electrolyte secretion. Because bisacodyl-induced laxative effects did not correlate with plasma and/or urine levels of the laxative (7), the pharmacologic responses of bisacodyl may have occurred on the mucosal side of the colon. It suggested the possibility that DAB directly interacted with the mucosal side of the colon. Re-

show abstract

“…Contraction of the colonic smooth muscle is caused by increasing the myoelectrical activity through direct irritation of the bowel wall [ 206,207 ] . Systemic absorption is <5% with onset of action between 4 and 6 h for oral administration and 0.25-1 h for rectal administration [ 207,208 ] . The small fraction that is absorbed is conjugated by the liver and excreted in urine.…”

Section: Stimulant Laxatives Bisacodylmentioning

confidence: 99%