New Release: Alpha testing version has been released.

Bisacodyl

A06A - Drugs for constipation ATC A06AB02 Small molecule approved 2004 Oral Prodrug Natural product

Active form: Dihydroxydiphenyl-Pyridyl Methane.

JFDA label: Laxadyl Adult Supp

Mechanism of Action

— Unknown

Indications

Approved

  • Bowel cleansing (enema only)
  • Constipation

Dosing

Source: Lexicomp

Bowel cleansing (enema only): Rectal: 10 mg (1 enema) as single dose Constipation: Oral: 5 to 15 mg once daily Rectal: Enema, suppository: 10 mg (1 enema or suppository) once daily
(For additional information see "Bisacodyl: Pediatric drug information") Constipation: Bowel cleansing (enema only): Children ≥12 years and Adolescents: Rectal: Refer to adult dosing. Constipation: Oral: Manufacturer's labeling: Children 6 to Children ≥12 years and Adolescents: Refer to adult dosing. Alternate dosing: Limited data available (Tabbers [NASPGHAN/ESPGHAN], 2014): Children 3 to 10 years: 5 mg once daily Children >10 years and Adolescents: 5 to 10 mg once daily Rectal: Manufacturer's labeling: Suppository: Children 6 to 1/2 suppository) once daily Children ≥12 years and Adolescents: Refer to adult dosing. Enema: Children ≥12 years and Adolescents: Refer to adult dosing. Alternate dosing: Limited data available (Tabbers [NASPGHAN/ESPGHAN] 2014): Enema, suppository: Children 2 to 10 years: 5 mg (1/2 suppository) once daily Children >10 years and Adolescents: 5 to 10 mg (1/2 to 1 enema or suppository) once daily
Refer to adult dosing.
There are no dosage adjustments provided in the manufacturer’s labeling.
There are no dosage adjustments provided in the manufacturer’s labeling.

Warnings & Precautions

Source: Lexicomp

Benzyl alcohol and derivatives

Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer’s labeling. Other warnings/precautions:

Appropriate use

Tablets: Do not chew or crush; do not use if you cannot swallow without chewing. Do not administer within 1 hour after taking an antacid, milk, or any dairy products.

Appropriate use

Enema/Suppositories: For rectal use only, discontinue use and consult a health care provider if rectal bleeding occurs or if no bowel movement is produced after use.

Self-medication (OTC use)

Consult a health care provider prior to use if stomach pain, nausea, vomiting, or a sudden change in bowel movements lasting >2 weeks occurs, or if you have already used a laxative, including bisacodyl, for >1 week. Use may cause stomach discomfort, faintness, rectal burning, and mild cramps. Discontinue use and consult a health care provider if use >1 week is needed.

Pregnancy & Lactation

Pregnancy

Systemic exposure following maternal use of bisacodyl is limited. Plasma concentrations of BHPM (the active metabolite of bisacodyl) are low (median: 61 ng/mL; range: 20 to 118 ng/mL) and the pharmacokinetics are highly variable following oral doses of 10 mg/day for 7 days to women immediately postpartum (Friedrich 2011). Treatment of constipation in pregnant women is similar to that of nonpregnant patients and medications may be used when diet and lifestyle modifications are not effective. Agents other than bisacodyl are preferred as initial treatment. Stimulant laxatives, including bisacodyl, are not recommended for chronic use, but may be used intermittently when needed (ACG [Christie 2007]).

Lactation

It is not known if bisacodyl is present in breast milk. Systemic exposure following maternal use is limited. Neither bisacodyl nor its active metabolite (BHPM) were detectable in breast milk following administration of bisacodyl 10 mg once daily for 7 days to eight breastfeeding women (lower limit of detection: 1 ng/mL) (Friedrich 2011).

Chemistry & Properties

2D structure
FormulaC22H19NO4
Molecular weight361.4 g/mol
IUPAC name[4-[(4-acetyloxyphenyl)-pyridin-2-ylmethyl]phenyl] acetate
CAS603-50-9
PubChem CID2391
InChIKeyKHOITXIGCFIULA-UHFFFAOYSA-N
logP4.11 (XLogP 3.8)
Polar surface area65.49 Ų
H-bond acceptors / donors5 / 0
Drug-likeness (QED)0.51
Lipinski violations0
SMILESCC(=O)Oc1ccc(C(c2ccc(OC(C)=O)cc2)c2ccccn2)cc1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrantNo

Enzyme interactions

EnzymeRoleDetail
CYP1A2Substrate
CYP2C9Inhibitor IC₅₀ 10.0 µM
CYP3A4Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drugSeverityManagement
Abarelix moderate
Abiraterone moderate
Acetazolamide moderate
Alfuzosin moderate
Alimemazine moderate
Aluminum hydroxide moderate
Amiloride moderate
Amiodarone moderate
Amisulpride moderate
Anagrelide moderate
Apalutamide moderate
Apomorphine moderate
Arsenic trioxide moderate
Asenapine moderate
Astemizole moderate
Atomoxetine moderate
Azithromycin moderate
Bedaquiline moderate
Bendroflumethiazide moderate
Benzthiazide moderate
Bepridil moderate
Betamethasone moderate
Bicalutamide moderate
Bosutinib moderate
Bumetanide moderate
Buprenorphine moderate
Cabozantinib moderate
Calcium carbonate moderate
Ceritinib moderate
Chlorothiazide moderate
Chlorpromazine moderate
Chlorthalidone moderate
Cilostazol moderate
Ciprofloxacin moderate
Cisapride moderate
Citalopram moderate
Clarithromycin moderate
Clofazimine moderate
Clozapine moderate
Corticotropin moderate

Showing 40 of 100+.

Registered Products (6)

BrandForm / strengthPackAgentCitizen (JOD)
Laxadyl Pediatric Suppositories Suppository 5 mg 5 pack varies The Arab Pharmaceutical Manufacturing PSC/Salt 0.820
Laxadyl Adult Supp Suppository 10 mg 5 pack varies The Arab Pharmaceutical Manufacturing PSC/Salt 0.900
Dulcolax Tab Tablet 5 mg 40 tab THE ARAB DRUG STORE P.S.C 2.010
DULCOLAX Tab. Tablet 5 mg 100 tab THE ARAB DRUG STORE P.S.C 4.770
Laxadyl Pediatric Suppositories Suppository 5 mg 100 pack varies The Arab Pharmaceutical Manufacturing PSC/Salt 13.940
Laxadyl Adult Supp Suppository 10 mg 100 pack varies The Arab Pharmaceutical Manufacturing PSC/Salt 15.300