Peringatan Keamanan

Patients experiencing an overdose of bisacodyl may present with more severe diarrhea and electrolyte imbalance.A7575 Patients should be treated with symptomatic and supportive measures.

The oral LD50 in rats is 4320 mg/kg, and in mice is 17500 mg/kg.L33070

Bisacodyl

DB09020

small molecule approved

Deskripsi

Bisacodyl, a diphenylmethane derivative, is a commonly used over the counter stimulant laxative for occasional constipation.A233300,L13362 Both bisacodyl and picosulfate are metabolized to the same active metabolite bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM).A233290,A233300,A207700

Bisacodyl was patented on 25 September 1956L33045 but has been used as a laxative since 1952.A233300

Struktur Molekul 2D

Berat 361.3906
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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.[A207700]
Volume Distribusi 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.[A207700]
Klirens (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.[A207700]

Absorpsi

Oral formulations of bisacodyl are only 16% bioavailable.A233275,A233280 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.L33070 A 10 mg suppository reaches a Cmax of 0-64 ng/mL.L33070 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.A207700 After multiple doses, the geometric mean AUC decreases to 311 h\*ng/mL.A207700

Metabolisme

Bisacodyl is deacetylated to the active bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM) by an intestinal deacetylase.A233290,A233300,A207700 A small amount of BHPM is absorbed from the gastrointestinal tract, and is glucuronidated before elimination.A207700

Rute Eliminasi

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.A207700

Interaksi Makanan

2 Data
  • 1. Avoid milk and dairy products. Take at least 1 hour before or after antacids and milk.
  • 2. Take separate from antacids. Take at least 1 hour before or after antacids and milk.

Interaksi Obat

429 Data
Cimetidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Cimetidine.
Nizatidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Nizatidine.
Ranitidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Ranitidine.
Famotidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Famotidine.
Methantheline The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Methantheline.
Aluminium The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Aluminium.
Magnesium oxide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Magnesium oxide.
Sodium bicarbonate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Sodium bicarbonate.
Aluminum hydroxide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Aluminum hydroxide.
Calcium carbonate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Calcium carbonate.
Metiamide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Metiamide.
Roxatidine acetate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Roxatidine acetate.
Magaldrate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Magaldrate.
Magnesium hydroxide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Magnesium hydroxide.
Magnesium trisilicate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Magnesium trisilicate.
Magnesium carbonate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Magnesium carbonate.
Lafutidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Lafutidine.
Lavoltidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Lavoltidine.
Bismuth subnitrate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Bismuth subnitrate.
Magnesium silicate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Magnesium silicate.
Aluminium acetoacetate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Aluminium acetoacetate.
Hydrotalcite The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Hydrotalcite.
Magnesium peroxide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Magnesium peroxide.
Almasilate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Almasilate.
Aluminium glycinate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Aluminium glycinate.
Aloglutamol The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Aloglutamol.
Niperotidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Niperotidine.
Calcium silicate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Calcium silicate.
Aluminium phosphate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Aluminium phosphate.
Pantoprazole The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Pantoprazole.
Omeprazole The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Omeprazole.
Lansoprazole The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Lansoprazole.
Esomeprazole The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Esomeprazole.
Rabeprazole The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Rabeprazole.
Dexlansoprazole The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Dexlansoprazole.
Dexrabeprazole The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Dexrabeprazole.
Sodium zirconium cyclosilicate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Sodium zirconium cyclosilicate.
Vonoprazan The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Vonoprazan.
Tramadol The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Tramadol.
Trospium The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Trospium.
Oxyphenonium The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Oxyphenonium.
Benzatropine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Benzatropine.
Ziprasidone The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Ziprasidone.
Disopyramide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Disopyramide.
Amitriptyline The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Amitriptyline.
Ipratropium The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Ipratropium.
Olanzapine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Olanzapine.
Metixene The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Metixene.
Terfenadine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Terfenadine.
Buclizine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Buclizine.
Clozapine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Clozapine.
Doxylamine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Doxylamine.
Trihexyphenidyl The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Trihexyphenidyl.
Oxyphencyclimine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Oxyphencyclimine.
Procyclidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Procyclidine.
Profenamine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Profenamine.
Promazine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Promazine.
Hyoscyamine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Hyoscyamine.
Cyproheptadine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Cyproheptadine.
Imipramine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Imipramine.
Methscopolamine bromide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Methscopolamine bromide.
Chlorpromazine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Chlorpromazine.
Gallamine triethiodide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Gallamine triethiodide.
Darifenacin The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Darifenacin.
Tridihexethyl The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Tridihexethyl.
Triflupromazine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Triflupromazine.
Anisotropine methylbromide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Anisotropine methylbromide.
Nortriptyline The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Nortriptyline.
Amoxapine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Amoxapine.
Atropine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Atropine.
Nicardipine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Nicardipine.
Pirenzepine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Pirenzepine.
Paroxetine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Paroxetine.
Homatropine methylbromide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Homatropine methylbromide.
Rocuronium The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Rocuronium.
Scopolamine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Scopolamine.
Benzquinamide The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Benzquinamide.
Clidinium The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Clidinium.
Propiomazine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Propiomazine.
Propantheline The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Propantheline.
Dicyclomine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Dicyclomine.
Biperiden The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Biperiden.
Brompheniramine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Brompheniramine.
Flupentixol The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Flupentixol.
Cocaine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Cocaine.
Quinidine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Quinidine.
Maprotiline The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Maprotiline.
Cycrimine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Cycrimine.
Glycopyrronium The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Glycopyrronium.
Tolterodine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Tolterodine.
Oxybutynin The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Oxybutynin.
Promethazine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Promethazine.
Diphenhydramine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Diphenhydramine.
Doxacurium The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Doxacurium.
Doxepin The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Doxepin.
Flavoxate The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Flavoxate.
Desipramine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Desipramine.
Orphenadrine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Orphenadrine.
Escitalopram The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Escitalopram.
Quetiapine The therapeutic efficacy of Bisacodyl can be decreased when used in combination with Quetiapine.

Target Protein

Aquaporin-3 AQP3
Sodium/Potassium Transporting ATPase ATP1A1

Referensi & Sumber

Synthesis reference: U.S. Patent 2,764,590.
Artikel (PubMed)
  • PMID: 9681329
    Kudo K, Miyazaki C, Kadoya R, Imamura T, Jitsufuchi N, Ikeda N: Laxative poisoning: toxicological analysis of bisacodyl and its metabolite in urine, serum, and stool. J Anal Toxicol. 1998 Jul-Aug;22(4):274-8.
  • PMID: 3401271
    Roth W, Beschke K: Pharmacokinetics and laxative effect of bisacodyl following administration of various dosage forms. Arzneimittelforschung. 1988 Apr;38(4):570-4.
  • PMID: 19678812
    Manabe N, Cremonini F, Camilleri M, Sandborn WJ, Burton DD: Effects of bisacodyl on ascending colon emptying and overall colonic transit in healthy volunteers. Aliment Pharmacol Ther. 2009 Nov 1;30(9):930-6. doi: 10.1111/j.1365-2036.2009.04118.x. Epub 2009 Aug 12.
  • PMID: 29441646
    Krueger D, Demir IE, Ceyhan GO, Zeller F, Schemann M: bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM)-the active metabolite of the laxatives bisacodyl and sodium picosulfate-enhances contractility and secretion in human intestine in vitro. Neurogastroenterol Motil. 2018 Jul;30(7):e13311. doi: 10.1111/nmo.13311. Epub 2018 Feb 14.
  • PMID: 31613513
    Lawrensia S, Raja A: Bisacodyl .
  • PMID: 21697613
    Friedrich C, Richter E, Trommeshauser D, de Kruif S, van Iersel T, Mandel K, Gessner U: Absence of excretion of the active moiety of bisacodyl and sodium picosulfate into human breast milk: an open-label, parallel-group, multiple-dose study in healthy lactating women. Drug Metab Pharmacokinet. 2011;26(5):458-64. doi: 10.2133/dmpk.dmpk-11-rg-007. Epub 2011 Jun 21.
  • PMID: 21868635
    Ikarashi N, Baba K, Ushiki T, Kon R, Mimura A, Toda T, Ishii M, Ochiai W, Sugiyama K: The laxative effect of bisacodyl is attributable to decreased aquaporin-3 expression in the colon induced by increased PGE2 secretion from macrophages. Am J Physiol Gastrointest Liver Physiol. 2011 Nov;301(5):G887-95. doi: 10.1152/ajpgi.00286.2011. Epub 2011 Aug 25.

Contoh Produk & Brand

Produk: 387 • International brands: 12
Produk
  • Ag-bisacodyl EC
    Tablet • 5 mg • Oral • Canada • Generic • OTC • Approved
  • Alophen
    Tablet, coated • 5 mg/1 • Oral • US • OTC
  • Alophen Tablets
    Tablet, delayed release • 5 mg / tab • Oral • Canada • OTC • Approved
  • Amb-bisacodyl
    Suppository • 10 mg • Rectal • Canada • OTC • Approved
  • Apo-bisacodyl
    Tablet, delayed release • 5 mg • Oral • Canada • Generic • OTC • Approved
  • Apo-bisacodyl Sup 10mg
    Suppository • 10 mg / sup • Rectal • Canada • Generic • OTC • Approved
  • Avedana Gentle Laxative
    Suppository • 10 mg/1 • Rectal • US • OTC
  • Becolax Tablets
    Tablet, delayed release • 5 mg • Oral • Canada • OTC • Approved
Menampilkan 8 dari 387 produk.
International Brands
  • Bisalax — Actavis
  • Bolax — Unifarma
  • Boots Constipation Relief — Boots
  • Derderance — Nisshin Seiyaku
  • Dulco-Lax — Boehringer Ingelheim
  • Dulcolaxo — Boehringer Ingelheim
  • Fleet Laxative — Baxter
  • Florisan — Boehringer Ingelheim
  • Laxitab — Ranbaxy
  • Reliable Gentle Laxative Tablets — Teva

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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