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 272.14 11.95 365 21055 198047 53129599
Macular degeneration 196.51 11.95 97 21323 12264 53315382
Sedation complication 179.10 11.95 77 21343 7089 53320557
Hypomania 175.22 11.95 68 21352 4814 53322832
Jaundice cholestatic 173.84 11.95 70 21350 5464 53322182
Orthostatic hypotension 162.17 11.95 117 21303 29636 53298010
Cognitive disorder 161.57 11.95 138 21282 44640 53283006
Creatinine renal clearance decreased 152.88 11.95 78 21342 10573 53317073
Sedation 148.87 11.95 111 21309 29564 53298082
Schizophrenia 129.57 11.95 69 21351 10210 53317436
Blood calcium decreased 122.15 11.95 84 21336 19710 53307936
Psychotic disorder 115.17 11.95 88 21332 24297 53303349
Balance disorder 92.91 11.95 130 21290 73077 53254569
Rheumatoid arthritis 91.24 11.95 10 21410 314521 53013125
Hepatotoxicity 75.16 11.95 73 21347 27807 53299839
Blood bilirubin increased 73.66 11.95 81 21339 35649 53291997
Intestinal pseudo-obstruction 72.12 11.95 22 21398 749 53326897
Depressed level of consciousness 71.05 11.95 98 21322 54330 53273316
Hypotension 63.53 11.95 235 21185 253841 53073805
Cholelithiasis 61.51 11.95 79 21341 40885 53286761
Mobility decreased 61.43 11.95 110 21310 76161 53251485
Fall 60.47 11.95 294 21126 358146 52969500
Alopecia 40.32 11.95 22 21398 234561 53093085
Maternal exposure during pregnancy 40.24 11.95 7 21413 155632 53172014
Mental status changes 39.73 11.95 63 21357 39508 53288138
Systemic lupus erythematosus 38.95 11.95 3 21417 125411 53202235
Treatment failure 37.38 11.95 4 21416 128399 53199247
Vomiting 36.94 11.95 332 21088 496807 52830839
Drug ineffective 36.45 11.95 187 21233 817058 52510588
Contraindicated product administered 35.28 11.95 6 21414 135623 53192023
Arthralgia 33.46 11.95 80 21340 439703 52887943
Joint swelling 32.34 11.95 28 21392 234610 53093036
Drug hypersensitivity 31.57 11.95 36 21384 265206 53062440
Drug intolerance 31.51 11.95 22 21398 205471 53122175
Urinary retention 30.92 11.95 47 21373 28419 53299227
Pneumonia 28.21 11.95 268 21152 406901 52920745
Glossodynia 27.06 11.95 4 21416 100287 53227359
Hypokalaemia 26.36 11.95 92 21328 96425 53231221
Delirium 25.08 11.95 53 21367 41376 53286270
Urinary tract infection 24.77 11.95 173 21247 239730 53087916
Hypersensitivity 24.61 11.95 29 21391 210636 53117010
Atonic urinary bladder 24.45 11.95 6 21414 88 53327558
Abdominal pain 24.38 11.95 181 21239 255722 53071924
Therapeutic product effect decreased 24.31 11.95 10 21410 125645 53202001
Intestinal obstruction 22.54 11.95 41 21379 28700 53298946
Loss of bladder sensation 22.51 11.95 5 21415 46 53327600
Flatulence 22.27 11.95 43 21377 31474 53296172
Infusion related reaction 22.22 11.95 18 21402 155939 53171707
Death 22.22 11.95 230 21190 357002 52970644
Mutism 22.18 11.95 11 21409 1402 53326244
Arthropathy 21.86 11.95 15 21405 141438 53186208
Wound 21.81 11.95 5 21415 91552 53236094
International normalised ratio increased 21.11 11.95 54 21366 47707 53279939
Headache 21.02 11.95 128 21292 536693 52790953
Rash 20.41 11.95 101 21319 446090 52881556
Hyponatraemia 20.35 11.95 92 21328 108515 53219131
Leukocytosis 20.31 11.95 36 21384 24698 53302948
Failure to thrive 20.15 11.95 19 21401 6973 53320673
Prescription drug used without a prescription 19.71 11.95 11 21409 1783 53325863
Exposure during pregnancy 19.62 11.95 13 21407 124847 53202799
Small intestinal obstruction 19.60 11.95 29 21391 17118 53310528
Nausea 19.58 11.95 418 21002 755673 52571973
Toxicity to various agents 19.05 11.95 152 21268 219446 53108200
Body dysmorphic disorder 18.96 11.95 6 21414 231 53327415
Dehydration 18.89 11.95 124 21296 168286 53159360
Sinusitis 18.84 11.95 24 21396 168540 53159106
Anal sphincter atony 18.72 11.95 6 21414 241 53327405
Completed suicide 18.41 11.95 17 21403 138184 53189462
Off label use 18.26 11.95 113 21307 472099 52855547
Nasopharyngitis 17.97 11.95 31 21389 192264 53135382
Colitis ischaemic 17.95 11.95 22 21398 10852 53316794
Foreign body 17.95 11.95 11 21409 2120 53325526
Therapeutic product effect incomplete 16.65 11.95 8 21412 91776 53235870
Neurogenic bladder 16.59 11.95 12 21408 3044 53324602
Product use issue 16.52 11.95 19 21401 139565 53188081
Heparin-induced thrombocytopenia 16.34 11.95 14 21406 4535 53323111
Subileus 16.05 11.95 12 21408 3204 53324442
Unresponsive to stimuli 16.04 11.95 39 21381 33387 53294259
Musculoskeletal stiffness 15.48 11.95 16 21404 123352 53204294
Drug dose titration not performed 14.68 11.95 6 21414 486 53327160
Decubitus ulcer 13.84 11.95 19 21401 10474 53317172
Listless 13.73 11.95 10 21410 2566 53325080
Ascites 13.67 11.95 41 21379 39694 53287952
Lower respiratory tract infection 13.59 11.95 10 21410 90971 53236675
Neurogenic bowel 13.56 11.95 4 21416 121 53327525
Gastrointestinal motility disorder 13.53 11.95 13 21407 4883 53322763
Anorgasmia 13.45 11.95 6 21414 603 53327043
Urticaria 12.60 11.95 22 21398 135863 53191783
Arthritis 12.52 11.95 10 21410 87288 53240358
Pericoronitis 12.49 11.95 3 21417 40 53327606
Reduced facial expression 12.15 11.95 8 21412 1746 53325900

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 162.11 12.83 243 14854 126130 32372299
Appendicolith 113.94 12.83 46 15051 3119 32495310
Victim of child abuse 76.94 12.83 24 15073 759 32497670
Appendicitis 73.73 12.83 48 15049 8889 32489540
Sepsis 63.05 12.83 189 14908 158645 32339784
Hyponatraemia 56.74 12.83 114 14983 74399 32424030
Urinary tract infection 53.38 12.83 116 14981 79955 32418474
Cardiogenic shock 50.70 12.83 55 15042 20607 32477822
Respiratory depression 48.88 12.83 44 15053 13167 32485262
Abdominal distension 40.85 12.83 80 15017 51215 32447214
Vomiting 36.70 12.83 210 14887 235347 32263082
Stress 35.10 12.83 49 15048 23733 32474696
Ascites 32.38 12.83 63 15034 40128 32458301
Urosepsis 31.55 12.83 33 15064 11857 32486572
Abdominal pain 29.93 12.83 143 14954 149386 32349043
Epidural lipomatosis 28.75 12.83 11 15086 646 32497783
Drug dependence 26.94 12.83 43 15054 23441 32474988
Multiple organ dysfunction syndrome 24.73 12.83 80 15017 69774 32428655
Mixed dementia 23.92 12.83 8 15089 317 32498112
Completed suicide 23.30 12.83 7 15090 92510 32405919
Sitting disability 22.18 12.83 6 15091 113 32498316
General physical health deterioration 21.45 12.83 108 14989 115151 32383278
Drug ineffective 19.99 12.83 101 14996 383376 32115053
Juvenile idiopathic arthritis 19.93 12.83 11 15086 1507 32496922
Decubitus ulcer 19.80 12.83 22 15075 8459 32489970
Product prescribing error 19.79 12.83 34 15063 19683 32478746
Child abuse 19.33 12.83 7 15090 352 32498077
Urinary retention 17.56 12.83 46 15051 35651 32462778
Nausea 16.52 12.83 224 14873 320625 32177804
Alveolar proteinosis 15.83 12.83 6 15091 343 32498086
Dehydration 15.07 12.83 107 14990 128851 32369578
Transcription medication error 15.05 12.83 5 15092 194 32498235
Ventricular fibrillation 15.00 12.83 28 15069 17282 32481147
Stevens-Johnson syndrome 14.66 12.83 29 15068 18680 32479749
Fall 14.54 12.83 147 14950 196054 32302375
Quality of life decreased 13.79 12.83 12 15085 3430 32494999
Heparin-induced thrombocytopenia 13.64 12.83 15 15082 5699 32492730
Mental status changes 13.64 12.83 44 15053 38293 32460136
Pneumonia aspiration 13.54 12.83 46 15051 41110 32457319
Failure to thrive 13.38 12.83 18 15079 8417 32490012
Convulsive threshold lowered 13.30 12.83 6 15091 534 32497895
Unresponsive to stimuli 12.99 12.83 35 15062 27574 32470855

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
MeSH PA D002400 Cathartics
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D054368 Laxatives
FDA EPC N0000175812 Stimulant Laxative

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
5MG,N/A;N/A,210GM;N/A,0.74GM;N/A,2.86GM;N/A,5.6GM 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:

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

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 FINAL 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 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
Bisacodyl HUMAN OTC DRUG LABEL 1 0615-0598 TABLET, COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 14 sections
Unit Dose Bisacodyl HUMAN OTC DRUG LABEL 1 0904-6407 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 15 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 0904-6748 TABLET, COATED 5 mg ORAL 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
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 FINAL 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
WOMENS GENTLE LAXATIVE HUMAN OTC DRUG LABEL 1 11673-151 TABLET 5 mg ORAL OTC monograph not final 8 sections
BISACODYL HUMAN OTC DRUG LABEL 1 11673-182 TABLET, COATED 5 mg ORAL OTC monograph not final 7 sections
Laxative HUMAN OTC DRUG LABEL 1 11822-0327 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 15 sections
laxative for women HUMAN OTC DRUG LABEL 1 11822-0676 TABLET, COATED 5 mg ORAL OTC monograph not final 15 sections
Rite Aid fast relief laxative HUMAN OTC DRUG LABEL 1 11822-4600 SUPPOSITORY 10 mg RECTAL OTC monograph not final 13 sections
Rite Aid fast relief laxative HUMAN OTC DRUG LABEL 1 11822-4601 SUPPOSITORY 10 mg RECTAL OTC monograph not final 12 sections
DELAYED RELEASE LAXATIVE BISACODYL HUMAN OTC DRUG LABEL 1 11822-7850 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 15 sections
Bisacodyl HUMAN OTC DRUG LABEL 1 16103-367 TABLET, DELAYED RELEASE 5 mg ORAL OTC monograph not final 15 sections
Laxative HUMAN OTC DRUG LABEL 1 21130-327 TABLET, SUGAR COATED 5 mg ORAL OTC MONOGRAPH NOT FINAL 15 sections