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	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 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	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:

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
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)

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)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

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
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:

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 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