GYLAXA

Bisacodyl, a diphenylmethane derivative, is a commonly used over the counter stimulant laxative for occasional constipation. 5, 9 Both bisacodyl and picosulfate are metabolized to the same active metabolite bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM). 4, 5, 6 Bisacodyl was patented on 25 September 1956 8 but has been used as a laxative since 1952.

Bisacodyl is indicated to relieve occasional constipation and irregularity.

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 Oral.

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.

Oral formulations of bisacodyl are only 16% bioavailable. 2, 3 A 10 mg enteric coated oral tablet reaches a C max of 26 ng/mL with a T max of 8 hours, while a 10 mg oral solution reaches a C max of 237 ng/mL with a T max of 1.7 hours.

A 10 mg suppository reaches a C max of 0-64 ng/mL.

In lactating women, 10 mg of oral bisacodyl reaches a C max of 20.5-195 ng/mL, with a T max 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.

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.

Bisacodyl is deacetylated to the active bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM) by an intestinal deacetylase. 4, 5, 6 A small amount of BHPM is absorbed from the gastrointestinal tract, and is glucuronidated before elimination.

Hover over products below to view reaction partners Bisacodyl Bis-(p-hydroxyphenyl)-pyridyl-2-methane.

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.

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.

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.

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Patients experiencing an overdose of bisacodyl may present with more severe diarrhea and electrolyte imbalance.

Patients should be treated with symptomatic and supportive measures.

The oral

LD in rats is 4320 mg/kg, and in mice is 17500 mg/kg.

For rectal use only.

Directions -detach one suppository from the strip -remove wrapper before inserting into the rectum adults and children 12 years of age and older 1 suppository once daily children to under 12 years 1/2 suppository once daily children under 6 years do not use.

Other information

Other information -Store at room temperature.

Do not exceed 30 o C (86 o F) -Lot No. & Exp.

Date: see wrapper or box.