diphenoxylate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
analgesics, pethidine derivatives	918	915-30-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: diphenoxylate diphenoxylate hydrochloride diphenoxylate HCl	A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. Molecular weight: 452.60 Formula: C30H32N2O2 CLOGP: 5.33 LIPINSKI: 1 HAC: 4 HDO: 0 TPSA: 53.33 ALOGS: -5.49 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

diphenoxylate
diphenoxylate hydrochloride
diphenoxylate HCl

A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.

Molecular weight: 452.60
Formula: C30H32N2O2
CLOGP: 5.33
LIPINSKI: 1
HAC: 4
HDO: 0
TPSA: 53.33
ALOGS: -5.49
ROTB: 9

Status: OFP

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

Drug dosage:

Dose	Unit	Route
15	mg	O

ADMET properties:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.63 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
Sept. 15, 1960	FDA	GD SEARLE LLC

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
Presbyacusis	134.09	16.84	37	6666	2739	50595682
Pleural fibrosis	126.84	16.84	37	6666	3347	50595074
Deafness neurosensory	120.58	16.84	38	6665	4463	50593958
Diarrhoea	114.48	16.84	244	6459	588232	50010189
Pleural thickening	113.45	16.84	32	6671	2567	50595854
Blood magnesium increased	101.39	16.84	30	6673	2850	50595571
Dehydration	97.27	16.84	110	6593	152339	50446082
Epigastric discomfort	91.54	16.84	33	6670	5837	50592584
Osteopenia	80.30	16.84	41	6662	16977	50581444
Cyst	71.31	16.84	34	6669	12153	50586268
Bone cyst	70.88	16.84	21	6682	2003	50596418
Osteosclerosis	67.51	16.84	23	6680	3444	50594977
Skin lesion	63.07	16.84	41	6662	26686	50571735
Blood potassium increased	59.03	16.84	33	6670	16365	50582056
Dry eye	54.01	16.84	40	6663	32055	50566366
Osteoarthritis	49.69	16.84	53	6650	68553	50529868
Exostosis	46.21	16.84	25	6678	11628	50586793
Deformity	42.96	16.84	21	6682	7919	50590502
Off label use	31.17	16.84	12	6691	474414	50124007
Blood creatinine increased	30.98	16.84	44	6659	76116	50522305
Crohn's disease	30.12	16.84	14	6689	4719	50593702
Sleep disorder	26.15	16.84	35	6668	57248	50541173
Abdominal pain	25.63	16.84	79	6624	236149	50362272
Renal impairment	25.45	16.84	40	6663	75621	50522800
Purpura senile	20.77	16.84	6	6697	523	50597898
Myocardial infarction	20.71	16.84	40	6663	88987	50509434
Small intestinal obstruction	20.47	16.84	17	6686	16051	50582370
Gastrointestinal disorder	20.24	16.84	41	6662	94415	50504006
Hypokalaemia	19.82	16.84	39	6664	87953	50510468
Gastroenteritis radiation	17.30	16.84	5	6698	437	50597984
Large intestinal stenosis	17.20	16.84	7	6696	1715	50596706
Clostridial infection	17.05	16.84	9	6694	3981	50594440

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
Dehydration	120.87	19.25	100	3150	114648	29456629
Diarrhoea	96.03	19.25	147	3103	332551	29238726
Small intestinal obstruction	21.66	19.25	15	3235	13046	29558231

FDA Adverse Event Reporting System (Geriatric)

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
Diarrhoea	145.33	17.96	273	6846	722431	63769182
Presbyacusis	143.53	17.96	37	7082	2538	64489075
Pleural fibrosis	135.83	17.96	39	7080	4011	64487602
Dehydration	121.65	17.96	134	6985	216629	64274984
Deafness neurosensory	118.40	17.96	39	7080	6335	64485278
Pleural thickening	117.90	17.96	32	7087	2678	64488935
Blood magnesium increased	103.39	17.96	30	7089	3201	64488412
Epigastric discomfort	92.63	17.96	33	7086	6778	64484835
Osteopenia	84.65	17.96	39	7080	15501	64476112
Cyst	80.93	17.96	35	7084	11992	64479621
Bone cyst	72.96	17.96	21	7098	2176	64489437
Osteosclerosis	67.43	17.96	22	7097	3464	64488149
Osteoarthritis	59.48	17.96	52	7067	63284	64428329
Dry eye	59.28	17.96	38	7081	28981	64462632
Skin lesion	53.67	17.96	39	7080	36443	64455170
Blood potassium increased	53.02	17.96	34	7085	25946	64465667
Deformity	51.30	17.96	21	7098	6276	64485337
Exostosis	42.17	17.96	22	7097	11416	64480197
Sleep disorder	35.24	17.96	38	7081	59671	64431942
Blood creatinine increased	30.31	17.96	54	7065	135728	64355885
Off label use	29.02	17.96	17	7102	632789	63858824
Gastrointestinal disorder	27.23	17.96	41	7078	89668	64401945
Nausea	23.86	17.96	158	6961	785642	63705971
Small intestinal obstruction	21.40	17.96	19	7100	23554	64468059
Drug interaction	19.17	17.96	8	7111	362075	64129538
Abdominal pain	18.67	17.96	76	7043	312299	64179314
Vertigo positional	18.04	17.96	8	7111	2903	64488710

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A07DA01	ALIMENTARY TRACT AND METABOLISM ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS ANTIPROPULSIVES Antipropulsives
CHEBI has role	CHEBI:55323	antidiarrheal drug
MeSH PA	D000700	Analgesics
MeSH PA	D000701	Analgesics, Opioid
MeSH PA	D000930	Antidiarrheals
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D009294	Narcotics
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
FDA EPC	N0000178374	Antidiarrheal

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Diarrhea	indication	62315008
Chemotherapy-Induced Diarrhea	off-label use
Alcoholism	contraindication	7200002
Severe chronic ulcerative colitis	contraindication	14311001
Infectious diarrheal disease	contraindication	19213003	DOID:13250
Dehydration	contraindication	34095006
Shigellosis	contraindication	36188001
Hepatorenal syndrome	contraindication	51292008	DOID:11823
Obstructive hyperbilirubinemia	contraindication	59848001
Drug AND/OR toxin-induced diarrhea	contraindication	65979008
Kidney disease	contraindication	90708001	DOID:557
Disease of liver	contraindication	235856003	DOID:409
Angle-closure glaucoma	contraindication	392291006	DOID:13550
Pseudomembranous enterocolitis	contraindication	397683000
Gastroenteritis due to Salmonella	contraindication
Diarrhea due to E. Coli	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.82	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	IC50	7.17		WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily A member 3	Ion channel	P22001	KCNA3_HUMAN		IC50	5.30		CHEMBL

External reference:

ID	Source
4019726	VUID
N0000147818	NUI
D03860	KEGG_DRUG
3810-80-8	SECONDARY_CAS_RN
3500	RXNORM
4017877	VANDF
4019726	VANDF
C0012525	UMLSCUI
CHEBI:4639	CHEBI
CHEMBL1201294	ChEMBL_ID
CHEMBL1200665	ChEMBL_ID
D004157	MESH_DESCRIPTOR_UI
DB01081	DRUGBANK_ID
7164	IUPHAR_LIGAND_ID
850	INN_ID
73312P173G	UNII
13505	PUBCHEM_CID
4613	MMSL
d03071	MMSL
001153	NDDF
004544	NDDF
15052009	SNOMEDCT_US
440585000	SNOMEDCT_US
71563009	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Lomotil	HUMAN PRESCRIPTION DRUG LABEL	2	0025-0061	TABLET	2.50 mg	ORAL	NDA	23 sections
Lomotil	HUMAN PRESCRIPTION DRUG LABEL	2	0025-0061	TABLET	2.50 mg	ORAL	NDA	23 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	0054-3194	SOLUTION	2.50 mg	ORAL	ANDA	20 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	0378-0415	TABLET	2.50 mg	ORAL	ANDA	20 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	0406-1236	TABLET	2.50 mg	ORAL	ANDA	23 sections
DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE	HUMAN PRESCRIPTION DRUG LABEL	2	0527-1170	TABLET	2.50 mg	ORAL	ANDA	12 sections
Diphenoxylate hydrochloride and atropine sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	0832-0590	TABLET	2.50 mg	ORAL	ANDA	21 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	12634-531	TABLET	2.50 mg	ORAL	ANDA	21 sections
Diphenoxylate Hcl and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	16590-080	TABLET	2.50 mg	ORAL	ANDA	13 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	17856-1061	TABLET	2.50 mg	ORAL	NDA AUTHORIZED GENERIC	23 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	17856-3194	SOLUTION	2.50 mg	ORAL	ANDA	20 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	21695-688	TABLET	2.50 mg	ORAL	ANDA	21 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	33261-685	TABLET	2.50 mg	ORAL	ANDA	21 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	43063-089	TABLET	2.50 mg	ORAL	ANDA	20 sections
Diphenoxylate hydrochloride and atropine sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	43063-957	TABLET	2.50 mg	ORAL	ANDA	21 sections
Diphenoxylate hydrochloride and atropine sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	43063-957	TABLET	2.50 mg	ORAL	ANDA	21 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	43353-083	TABLET	2.50 mg	ORAL	NDA AUTHORIZED GENERIC	23 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	43353-594	TABLET	2.50 mg	ORAL	ANDA	21 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	49884-771	TABLET	2.50 mg	ORAL	ANDA	20 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	50090-0039	TABLET	2.50 mg	ORAL	ANDA	20 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	50090-0040	TABLET	2.50 mg	ORAL	ANDA	20 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	50090-2641	TABLET	2.50 mg	ORAL	NDA AUTHORIZED GENERIC	23 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	50090-2872	TABLET	2.50 mg	ORAL	NDA AUTHORIZED GENERIC	23 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	50090-3452	TABLET	2.50 mg	ORAL	ANDA	19 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	50090-3456	TABLET	2.50 mg	ORAL	ANDA	19 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	50090-5589	TABLET	2.50 mg	ORAL	ANDA	18 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	50090-5592	TABLET	2.50 mg	ORAL	ANDA	18 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	51293-618	TABLET	2.50 mg	ORAL	ANDA	23 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	51293-618	TABLET	2.50 mg	ORAL	ANDA	23 sections
Diphenoxylate Hydrochloride and Atropine Sulfate	HUMAN PRESCRIPTION DRUG LABEL	2	53002-3400	TABLET	2.50 mg	ORAL	ANDA	19 sections