bisacodyl indications/contra

Stem definitionDrug idCAS RN
375 603-50-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bisacodyl
  • brocalax
  • dulcolax
A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871)
  • Molecular weight: 361.40
  • Formula: C22H19NO4
  • CLOGP: 2.85
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 65.49
  • ALOGS: -5.46
  • ROTB: 7

Drug dosage:

DoseUnitRoute
10 mg O
10 mg R

Approvals:

DateAgencyCompanyOrphan
May 10, 2004 FDA BRAINTREE

FDA Adverse Event Reporting System

scroll-->
MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug abuse 148.24 37.65 36 251 18294 3367278
Colitis ischaemic 132.63 37.65 23 264 2165 3383407
Intestinal pseudo-obstruction 130.26 37.65 17 270 223 3385349
Constipation 102.33 37.65 30 257 30782 3354790
Toxicity to various agents 97.94 37.65 32 255 47022 3338550
Hypokalaemia 80.57 37.65 21 266 13784 3371788
Urinary retention 66.46 37.65 16 271 7556 3378016
Abdominal pain 62.98 37.65 23 264 46202 3339370
Diarrhoea 60.18 37.65 28 259 104320 3281252
Delirium 57.74 37.65 15 272 9613 3375959
Mutism 57.54 37.65 9 278 437 3385135
Hyponatraemia 52.42 37.65 16 271 18343 3367229
Vomiting 51.40 37.65 24 263 89507 3296065
Intestinal obstruction 43.36 37.65 11 276 6378 3379194
Asthenia 41.92 37.65 19 268 65646 3319926
Cognitive disorder 41.08 37.65 11 276 7863 3377709
Intentional product misuse 40.19 37.65 12 275 12689 3372883

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC A06AB02 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR CONSTIPATION
DRUGS FOR CONSTIPATION
Contact laxatives
ATC A06AB52 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR CONSTIPATION
DRUGS FOR CONSTIPATION
Contact laxatives
ATC A06AG02 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR CONSTIPATION
DRUGS FOR CONSTIPATION
Enemas
FDA PE N0000009371 Increased Large Intestinal Motility
FDA EPC N0000175812 Stimulant Laxative
FDA PE N0000009871 Stimulation Large Intestine Fluid/Electrolyte Secretion
MeSH PA D002400 Cathartics
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D054368 Laxatives

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Constipation indication 14760008 DOID:2089
Incomplete passage of stool indication 249515001
Anuria contraindication 2472002 DOID:2983
Hypocalcemia contraindication 5291005
Rectal hemorrhage contraindication 12063002
Hyperkalemia contraindication 14140009
Severe chronic ulcerative colitis contraindication 14311001
Acute vomiting contraindication 23971007
Complete atrioventricular block contraindication 27885002
Toxic megacolon contraindication 28536002 DOID:1770
Anal fissure contraindication 30037006
Gastrointestinal ulcer contraindication 40845000
Toxic colitis contraindication 42359007
Hypokalemia contraindication 43339004
Chronic heart failure contraindication 48447003
Gastrointestinal perforation contraindication 51875005
Chronic ulcerative proctitis contraindication 52231000
Congenital myotonia, autosomal dominant form contraindication 57938005
Acute nephropathy contraindication 58574008
Incontinence of feces contraindication 72042002
Appendicitis contraindication 74400008 DOID:8337
Hyperchloremia contraindication 74450001
Third degree burn injury contraindication 80247002
Intestinal obstruction contraindication 81060008 DOID:8437
Oliguria contraindication 83128009
Hyponatremia contraindication 89627008
Kidney disease contraindication 90708001 DOID:2527
Gastrointestinal obstruction contraindication 126765001
Seizure disorder contraindication 128613002 DOID:1826
Hyporeninemic hypoaldosteronism contraindication 236464008
Edema contraindication 267038008
Familial hyperkalemic periodic paralysis contraindication 304737009 DOID:14451
Gastric retention contraindication 307227006
At risk for aspiration contraindication 371736008
Severe dehydration contraindication 450316000

Acid dissociation constants calculated using MoKa v3.0.0

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.39 Basic

Orange Book patent data (new drug applications)

scroll-->
Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
5MG,N/A HALFLYTELY BRAINTREE N021551 July 16, 2010 DISCN FOR SOLUTION, TABLET, DELAYED RELEASE ORAL 7291324 Oct. 22, 2022 GASTROINTESTINAL LAVAGE INDICATED FOR CLEANSING OF THE COLON AS A PREPARATION FOR COLONOSCOPY IN ADULTS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium-dependent dopamine transporter Transporter Ki 5.76 DRUG MATRIX
Kappa-type opioid receptor GPCR Ki 6.01 DRUG MATRIX
Cytochrome P450 2C9 Enzyme IC50 5 DRUG MATRIX

External reference:

scroll-->
IDSource
4018526 VUID
N0000146848 NUI
C0005632 UMLSCUI
D00245 KEGG_DRUG
10X0709Y6I UNII
824 INN_ID
CHEMBL942 ChEMBL_ID
4018526 VANDF
N0000146848 NDFRT
N0000005898 NDFRT
001172 NDDF
4855 MMSL
1596 RXNORM
13565005 SNOMEDCT_US
387075009 SNOMEDCT_US
4286 MMSL
d01015 MMSL
2391 PUBCHEM_CID
D001726 MESH_DESCRIPTOR_UI
DB09020 DRUGBANK_ID
CHEBI:3125 CHEBI

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Fleet HUMAN OTC DRUG LABEL 1 0132-0703 ENEMA 10 mg RECTAL OTC monograph not final 10 sections
Womens Laxative HUMAN OTC DRUG LABEL 1 0363-0326 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
Gentle Laxative HUMAN OTC DRUG LABEL 1 0363-0327 TABLET 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
Walgreens Gentle Laxative HUMAN OTC DRUG LABEL 1 0363-0466 SUPPOSITORY 10 mg RECTAL OTC monograph not final 14 sections
Womens laxative HUMAN OTC DRUG LABEL 1 0363-0676 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
WOMENS GENTLE LAXATIVE HUMAN OTC DRUG LABEL 1 0363-3011 CAPSULE, GELATIN COATED 5 mg ORAL OTC monograph not final 10 sections
Biscolax HUMAN OTC DRUG LABEL 1 0536-1355 SUPPOSITORY 10 mg RECTAL OTC MONOGRAPH NOT FINAL 10 sections
Enteric Coated Stimulant Laxative HUMAN OTC DRUG LABEL 1 0536-3381 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 15 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 0574-7050 SUPPOSITORY 10 mg RECTAL OTC monograph not final 11 sections
Dulcolax HUMAN OTC DRUG LABEL 1 0597-0012 TABLET, COATED 5 mg ORAL OTC monograph not final 8 sections
Dulcolax Pink HUMAN OTC DRUG LABEL 1 0597-0051 TABLET, COATED 5 mg ORAL OTC monograph not final 13 sections
Dulcolax HUMAN OTC DRUG LABEL 1 0597-0052 SUPPOSITORY 10 mg RECTAL OTC monograph not final 7 sections
Dulcolax HUMAN OTC DRUG LABEL 1 0597-0162 SUPPOSITORY 10 mg RECTAL OTC monograph not final 2 sections
Dulcolax Pink HUMAN OTC DRUG LABEL 1 0597-0169 TABLET, COATED 5 mg ORAL OTC monograph not final 13 sections
Dulcolax Pink HUMAN OTC DRUG LABEL 1 0597-0335 TABLET, COATED 5 mg ORAL OTC monograph not final 13 sections
Dulcolax HUMAN OTC DRUG LABEL 1 0597-0340 TABLET, COATED 5 mg ORAL OTC monograph not final 8 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 0615-0598 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
BISAC-EVAC HUMAN OTC DRUG LABEL 1 0713-0109 SUPPOSITORY 10 mg RECTAL OTC monograph not final 10 sections
Biscolax Laxative HUMAN OTC DRUG LABEL 1 0904-5058 SUPPOSITORY 10 mg RECTAL OTC monograph not final 10 sections
Unit Dose Bisacodyl HUMAN OTC DRUG LABEL 1 0904-6407 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 0904-7927 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 10 sections
Carters Little Pills HUMAN OTC DRUG LABEL 1 10237-906 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 11 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 11534-013 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 13 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 11534-156 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 12 sections
Laxative HUMAN OTC DRUG LABEL 1 11673-053 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
up and up gentle laxative HUMAN OTC DRUG LABEL 1 11673-116 TABLET, COATED 5 mg ORAL OTC monograph not final 8 sections
WOMENS LAXATIVE HUMAN OTC DRUG LABEL 1 11673-120 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
Laxative for Women HUMAN OTC DRUG LABEL 1 11822-0326 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
Laxative HUMAN OTC DRUG LABEL 1 11822-0327 TABLET, SUGAR COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections
laxative for women HUMAN OTC DRUG LABEL 1 11822-0676 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 9 sections