bisacodyl Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
10 mg O
10 mg R

ADMET properties:

PropertyValueReference
BA (Bioavailability) 15 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
May 10, 2004 FDA BRAINTREE

FDA Adverse Event Reporting System (Female)

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
Constipation 186.52 11.73 287 18717 173810 46493248
Hypomania 149.22 11.73 59 18945 4329 46662729
Jaundice cholestatic 144.81 11.73 60 18944 4969 46662089
Schizophrenia 114.28 11.73 60 18944 8508 46658550
Sedation complication 96.60 11.73 41 18963 3604 46663454
Psychotic disorder 91.63 11.73 75 18929 22546 46644512
Cognitive disorder 79.25 11.73 86 18918 36797 46630261
Orthostatic hypotension 72.22 11.73 68 18936 24590 46642468
Drug ineffective 70.25 11.73 105 18899 677733 45989325
Creatinine renal clearance decreased 68.98 11.73 40 18964 6880 46660178
Rheumatoid arthritis 65.18 11.73 10 18994 240205 46426853
Sedation 64.85 11.73 62 18942 22848 46644210
Hepatotoxicity 63.92 11.73 64 18940 24945 46642113
Intestinal pseudo-obstruction 62.00 11.73 19 18985 648 46666410
Blood bilirubin increased 58.71 11.73 71 18933 34113 46632945
Blood calcium decreased 53.28 11.73 47 18957 15626 46651432
Cholelithiasis 48.77 11.73 69 18935 38612 46628446
Mental status changes 38.12 11.73 61 18943 38027 46629031
Balance disorder 35.45 11.73 80 18924 64441 46602617
Hypotension 33.15 11.73 184 18820 232405 46434653
Vomiting 32.31 11.73 303 18701 452491 46214567
Fall 29.08 11.73 231 18773 328866 46338192
Depressed level of consciousness 28.41 11.73 61 18943 47508 46619550
Drug hypersensitivity 27.88 11.73 35 18969 243790 46423268
Mobility decreased 27.74 11.73 70 18934 60524 46606534
Macular degeneration 27.31 11.73 23 18981 7182 46659876
Pneumonia 26.39 11.73 251 18753 376069 46290989
Urinary tract infection 25.45 11.73 165 18839 220101 46446957
Treatment failure 24.93 11.73 4 19000 93083 46573975
Atonic urinary bladder 24.37 11.73 6 18998 88 46666970
Maternal exposure during pregnancy 24.14 11.73 6 18998 102543 46564515
Urinary retention 23.72 11.73 40 18964 26021 46641037
Leukocytosis 22.76 11.73 37 18967 23361 46643697
Loss of bladder sensation 22.44 11.73 5 18999 46 46667012
Alopecia 22.26 11.73 20 18984 162394 46504664
Arthralgia 21.69 11.73 76 18928 364527 46302531
Completed suicide 21.18 11.73 17 18987 145903 46521155
Body dysmorphic disorder 20.88 11.73 6 18998 163 46666895
Mutism 19.92 11.73 10 18994 1290 46665768
Death 19.29 11.73 215 18789 335333 46331725
International normalised ratio increased 19.24 11.73 52 18952 46831 46620227
Small intestinal obstruction 19.13 11.73 28 18976 16144 46650914
Off label use 18.89 11.73 85 18919 379756 46287302
Anal sphincter atony 18.81 11.73 6 18998 234 46666824
Intestinal obstruction 18.60 11.73 36 18968 26039 46641019
Drug intolerance 17.98 11.73 20 18984 147029 46520029
Exposure during pregnancy 17.82 11.73 11 18993 108201 46558857
Headache 17.77 11.73 118 18886 478234 46188824
Colitis ischaemic 17.31 11.73 21 18983 10111 46656947
Neurogenic bladder 16.97 11.73 12 18992 2898 46664160
Failure to thrive 16.92 11.73 17 18987 6647 46660411
Hepatic enzyme increased 16.87 11.73 72 18932 81715 46585343
Heparin-induced thrombocytopenia 16.84 11.73 14 18990 4295 46662763
Contraindicated product administered 16.42 11.73 6 18998 79941 46587117
Hypokalaemia 16.27 11.73 75 18929 87949 46579109
Joint swelling 15.87 11.73 27 18977 166046 46501012
Therapeutic product effect incomplete 15.82 11.73 6 18998 78147 46588911
Drug dose titration not performed 15.82 11.73 6 18998 393 46666665
Hyponatraemia 15.64 11.73 82 18922 101250 46565808
Unresponsive to stimuli 15.59 11.73 38 18966 32136 46634922
Abdominal pain 15.37 11.73 152 18852 229879 46437179
Dehydration 15.15 11.73 114 18890 159426 46507632
Delirium 14.98 11.73 41 18963 37187 46629871
Infusion related reaction 14.42 11.73 12 18992 101196 46565862
Subileus 14.39 11.73 11 18993 2992 46664066
Gastrointestinal motility disorder 14.37 11.73 13 18991 4465 46662593
Therapeutic product effect decreased 14.16 11.73 8 18996 82593 46584465
Anorgasmia 13.47 11.73 6 18998 592 46666466
Pericoronitis 12.98 11.73 3 19001 33 46667025
Decubitus ulcer 12.98 11.73 18 18986 9880 46657178
Nausea 12.83 11.73 368 18636 687086 45979972
Nasopharyngitis 12.15 11.73 28 18976 153970 46513088
Asthenia 11.85 11.73 185 18819 310890 46356168
Anticholinergic syndrome 11.83 11.73 8 18996 1798 46665260

FDA Adverse Event Reporting System (Male)

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
Constipation 108.58 12.34 186 13124 112720 29826448
Urinary tract infection 56.29 12.34 110 13200 73549 29865619
Sepsis 34.92 12.34 143 13167 146252 29792916
Urosepsis 29.97 12.34 30 13280 10702 29928466
Completed suicide 26.28 12.34 6 13304 99486 29839682
Victim of child abuse 25.16 12.34 8 13302 282 29938886
Drug ineffective 24.58 12.34 74 13236 340313 29598855
Hyponatraemia 24.01 12.34 75 13235 67127 29872041
Vomiting 23.21 12.34 172 13138 219646 29719522
Appendicolith 22.39 12.34 10 13300 909 29938259
Decubitus ulcer 20.34 12.34 21 13289 7767 29931401
Child abuse 18.77 12.34 6 13304 215 29938953
Dehydration 18.08 12.34 105 13205 123434 29815734
Transcription medication error 17.25 12.34 5 13305 128 29939040
Alveolar proteinosis 17.00 12.34 6 13304 293 29938875
Pneumonia 16.77 12.34 224 13086 334082 29605086
Urinary retention 15.91 12.34 41 13269 32876 29906292
Respiratory failure 15.68 12.34 87 13223 100555 29838613
Stevens-Johnson syndrome 15.60 12.34 28 13282 17528 29921640
Sitting disability 15.40 12.34 4 13306 67 29939101
Deep vein thrombosis 15.09 12.34 60 13250 60441 29878727
Unresponsive to stimuli 14.99 12.34 35 13275 26384 29912784
Quality of life decreased 14.96 12.34 12 13298 3205 29935963
Heparin-induced thrombocytopenia 14.94 12.34 15 13295 5368 29933800
Failure to thrive 14.66 12.34 18 13292 8036 29931132
Mental status changes 13.80 12.34 42 13268 37037 29902131
Respiratory depression 13.79 12.34 21 13289 11482 29927686
Convulsive threshold lowered 13.67 12.34 6 13304 523 29938645
Abdominal pain 13.63 12.34 105 13205 135549 29803619
Cerebellar infarction 13.37 12.34 9 13301 1840 29937328
Sputum culture positive 13.03 12.34 9 13301 1918 29937250
Haematocrit decreased 12.59 12.34 36 13274 30663 29908505
Pneumonia aspiration 12.42 12.34 41 13269 37739 29901429
Small intestinal obstruction 12.41 12.34 22 13288 13637 29925531

Pharmacologic Action:

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 PE N0000009871 Stimulation Large Intestine Fluid/Electrolyte Secretion
FDA EPC N0000175812 Stimulant Laxative
MeSH PA D002400 Cathartics
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D054368 Laxatives

Drug Use (View source of the data)

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:557
Gastrointestinal obstruction contraindication 126765001
Seizure disorder contraindication 128613002
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

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.39 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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:

IDSource
10X0709Y6I UNII
4018526 VUID
N0000146848 NUI
D00245 KEGG_DRUG
4018526 VANDF
C0005632 UMLSCUI
CHEBI:3125 CHEBI
CHEMBL942 ChEMBL_ID
DB09020 DRUGBANK_ID
D001726 MESH_DESCRIPTOR_UI
824 INN_ID
2391 PUBCHEM_CID
151672 RXNORM
4286 MMSL
4855 MMSL
d01015 MMSL
001172 NDDF
13565005 SNOMEDCT_US
387075009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fleet HUMAN OTC DRUG LABEL 1 0132-0703 ENEMA 10 mg RECTAL OTC monograph not final 11 sections
Gentle Laxative HUMAN OTC DRUG LABEL 1 0363-0327 TABLET 5 mg ORAL OTC MONOGRAPH NOT FINULLL 15 sections
Walgreens Gentle Laxative HUMAN OTC DRUG LABEL 1 0363-0466 SUPPOSITORY 10 mg RECTAL OTC monograph not final 14 sections
Walgreens Gentle Laxative HUMAN OTC DRUG LABEL 1 0363-0466 SUPPOSITORY 10 mg RECTAL OTC monograph not final 14 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 FINULLL 15 sections
WOMENS GENTLE LAXATIVE HUMAN OTC DRUG LABEL 1 0363-3011 CAPSULE, GELATIN COATED 5 mg ORAL OTC monograph not final 16 sections
Laxative HUMAN OTC DRUG LABEL 1 0363-6760 TABLET, COATED 5 mg ORAL OTC monograph not final 15 sections
Rugby Gentle Laxative HUMAN OTC DRUG LABEL 1 0536-1238 SUPPOSITORY 10 mg RECTAL OTC monograph not final 15 sections
ENTERIC COATED STIMULANT LAXATIVE HUMAN OTC DRUG LABEL 1 0536-3381 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 6 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 0574-7050 SUPPOSITORY 10 mg RECTAL OTC monograph not final 15 sections
Dulcolax HUMAN OTC DRUG LABEL 1 0597-0012 TABLET, COATED 5 mg ORAL OTC monograph not final 15 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 12 sections
Dulcolax HUMAN OTC DRUG LABEL 1 0597-0162 SUPPOSITORY 10 mg RECTAL OTC monograph not final 14 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 15 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 0615-0598 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINULLL 14 sections
BISAC-EVAC HUMAN OTC DRUG LABEL 1 0713-0109 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 FINULLL 15 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 0904-6748 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINULLL 15 sections
Leader Gentle Laxative HUMAN OTC DRUG LABEL 1 0904-6981 SUPPOSITORY 10 mg RECTAL OTC monograph not final 15 sections
Leader Gentle Laxative HUMAN OTC DRUG LABEL 1 0904-6981 SUPPOSITORY 10 mg RECTAL OTC monograph not final 15 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 0904-7142 SUPPOSITORY 10 mg RECTAL OTC monograph not final 14 sections
Carters Little PillsSodium-Free 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
LaxativeEnteric Coated HUMAN OTC DRUG LABEL 1 11673-053 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINULLL 15 sections
up and up gentle laxative HUMAN OTC DRUG LABEL 1 11673-116 TABLET, COATED 5 mg ORAL OTC monograph not final 15 sections