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

Stem definition	Drug id	CAS RN
	375	603-50-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
10	mg	O
10	mg	R

ADMET properties:

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

Approvals:

Date	Agency	Company	Orphan
May 10, 2004	FDA	BRAINTREE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	4.39	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN	Ki	5.76	DRUG MATRIX
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN	Ki	6.01	DRUG MATRIX
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN	IC50	5	DRUG MATRIX

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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