diphenoxylate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
analgesics, pethidine derivatives and other synthetic small molecule miu-opioid receptor agonists 918 915-30-0

Description:

MoleculeDescription

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:

DoseUnitRoute
15 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.63 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK 49
kinase-selectivity-class AXL,EIF2AK3,EPHB4,ERBB2,GRK2,PDK4,SIK2 7
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Sept. 15, 1960 FDA GD SEARLE LLC

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
Presbyacusis 155.37 17.96 39 7992 3003 90617413
Pleural fibrosis 148.89 17.96 39 7992 3557 90616859
Pleural thickening 128.60 17.96 34 7997 3214 90617202
Deafness neurosensory 128.28 17.96 40 7991 6801 90613615
Dehydration 123.04 17.96 116 7915 194331 90426085
Diarrhoea 122.54 17.96 261 7770 938929 89681487
Macular degeneration 119.32 17.96 61 7970 37909 90582507
Blood magnesium increased 117.58 17.96 32 7999 3376 90617040
Epigastric discomfort 104.17 17.96 35 7996 7533 90612883
Osteopenia 93.32 17.96 44 7987 22958 90597458
Cyst 80.74 17.96 36 7995 16525 90603891
Bone cyst 80.50 17.96 22 8009 2356 90618060
Osteosclerosis 79.90 17.96 25 8006 4295 90616121
Chronic sinusitis 74.06 17.96 38 7993 23764 90596652
Skin lesion 70.66 17.96 43 7988 37322 90583094
Blood potassium increased 70.03 17.96 35 7996 20714 90599702
Paraesthesia oral 66.54 17.96 39 7992 31620 90588796
Procedural pain 59.53 17.96 37 7994 33323 90587093
Dry eye 53.62 17.96 43 7988 57888 90562528
Deformity 45.45 17.96 22 8009 12148 90608268
Abdominal pain 43.34 17.96 103 7928 395618 90224798
Female genital tract fistula 42.86 17.96 24 8007 17844 90602572
Colitis 42.74 17.96 41 7990 69901 90550515
Vaginal flatulence 41.70 17.96 21 8010 12617 90607799
Proctitis 40.74 17.96 22 8009 15237 90605179
Blood creatinine increased 39.84 17.96 47 7984 101339 90519077
Rectal haemorrhage 38.71 17.96 42 7989 82702 90537714
Nausea 37.37 17.96 195 7836 1110121 89510295
Radiculopathy 36.79 17.96 22 8009 18483 90601933
Vaginal discharge 35.76 17.96 22 8009 19442 90600974
Crohn's disease 35.21 17.96 14 8017 4837 90615579
Renal impairment 32.06 17.96 43 7988 105378 90515038
Weight decreased 29.44 17.96 87 7944 379823 90240593
Myocardial infarction 28.88 17.96 41 7990 105931 90514485
Oral candidiasis 27.97 17.96 24 8007 35431 90584985
Osteoarthritis 27.07 17.96 56 7975 195674 90424742
Colitis ulcerative 25.44 17.96 29 8002 60237 90560179
Exostosis 24.89 17.96 27 8004 53107 90567309
Small intestinal obstruction 24.55 17.96 18 8013 21216 90599200
Purpura senile 22.27 17.96 6 8025 609 90619807
Haematochezia 21.67 17.96 29 8002 70884 90549532
Hypokalaemia 21.12 17.96 40 7991 131076 90489340
Anaemia 20.28 17.96 73 7958 352729 90267687
Peripheral swelling 19.82 17.96 6 8025 413100 90207316
Systemic lupus erythematosus 19.79 17.96 4 8027 361892 90258524
Product use issue 19.45 17.96 3 8028 329916 90290500
Clostridial infection 19.20 17.96 9 8022 4627 90615789
Bone hypertrophy 18.91 17.96 5 8026 472 90619944
Frequent bowel movements 18.50 17.96 24 8007 56911 90563505
Tarsal tunnel syndrome 17.97 17.96 5 8026 572 90619844
Gastroenteritis radiation 17.97 17.96 5 8026 572 90619844

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
Dehydration 130.89 19.94 100 3283 141667 42476285
Diarrhoea 103.10 19.94 152 3231 460697 42157255
Off label use 34.40 19.94 5 3378 638330 41979622
Small intestinal obstruction 27.40 19.94 17 3366 17044 42600908

FDA Adverse Event Reporting System (Geriatric)

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
Presbyacusis 164.50 19.15 39 8316 2780 110578164
Pleural fibrosis 157.70 19.15 41 8314 4267 110576677
Diarrhoea 147.13 19.15 287 8068 1139218 109441726
Dehydration 142.99 19.15 138 8217 279373 110301571
Pleural thickening 132.44 19.15 34 8321 3365 110577579
Deafness neurosensory 125.17 19.15 41 8314 9578 110571366
Blood magnesium increased 118.99 19.15 32 8323 3791 110577153
Epigastric discomfort 103.63 19.15 35 8320 8980 110571964
Osteopenia 95.02 19.15 42 8313 22167 110558777
Cyst 89.78 19.15 37 8318 16459 110564485
Macular degeneration 76.99 19.15 36 8319 21623 110559321
Bone cyst 74.93 19.15 22 8333 3581 110577363
Chronic sinusitis 74.92 19.15 37 8318 25047 110555897
Osteosclerosis 74.23 19.15 23 8332 4492 110576452
Paraesthesia oral 67.37 19.15 38 8317 33633 110547311
Blood potassium increased 65.11 19.15 37 8318 33212 110547732
Procedural pain 62.79 19.15 37 8318 35528 110545416
Skin lesion 59.43 19.15 41 8314 51590 110529354
Dry eye 56.57 19.15 41 8314 55752 110525192
Deformity 52.62 19.15 22 8333 10138 110570806
Vaginal flatulence 45.69 19.15 21 8334 12123 110568821
Nausea 44.89 19.15 198 8157 1235492 109345452
Female genital tract fistula 42.40 19.15 22 8333 16497 110564447
Proctitis 41.90 19.15 22 8333 16905 110564039
Vaginal discharge 40.73 19.15 22 8333 17886 110563058
Colitis 40.33 19.15 44 8311 102279 110478665
Blood creatinine increased 37.71 19.15 57 8298 182832 110398112
Radiculopathy 36.46 19.15 21 8334 19315 110561629
Osteoarthritis 33.58 19.15 54 8301 182569 110398375
Abdominal pain 32.82 19.15 99 8256 512890 110068054
Rectal haemorrhage 31.57 19.15 42 8313 119791 110461153
Weight decreased 29.62 19.15 90 8265 467967 110112977
Oral candidiasis 28.42 19.15 25 8330 44735 110536209
Colitis ulcerative 28.29 19.15 32 8323 77331 110503613
Dyspepsia 27.91 19.15 51 8304 190914 110390030
Small intestinal obstruction 26.71 19.15 21 8334 32192 110548752
Myocardial infarction 24.00 19.15 48 8307 192035 110388909
Exostosis 23.98 19.15 23 8332 45933 110535011
Crohn's disease 19.88 19.15 7 8348 2031 110578913

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Related Drugs by ATC class:

A07DA Antipropulsives 5 drugs
difenoxineluxadolineloperamideloperamide oxidemorphine

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 6.82 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
Mu-type opioid receptor GPCR AGONIST IC50 7.17 WOMBAT-PK CHEMBL
Potassium voltage-gated channel subfamily A member 3 Ion channel IC50 5.30 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 21 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 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 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 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 50090-5589 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 53002-3400 TABLET 2.50 mg ORAL ANDA 19 sections
Diphenoxylate Hydrochloride and Atropine Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 53002-3401 TABLET 2.50 mg ORAL ANDA 18 sections
Diphenoxylate Hydrochloride and Atropine Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 54868-0032 TABLET 2.50 mg ORAL ANDA 12 sections
Lomotil HUMAN PRESCRIPTION DRUG LABEL 2 54868-0427 TABLET 2.50 mg ORAL NDA 12 sections
LOMOTIL HUMAN PRESCRIPTION DRUG LABEL 2 55466-783 TABLET 2.50 mg ORAL Export only 1 sections
Diphenoxylate Hydrochloride and Atropine Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 59762-1061 TABLET 2.50 mg ORAL NDA authorized generic 23 sections
Diphenoxylate Hydrochloride and Atropine Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 60687-890 TABLET 2.50 mg ORAL ANDA 20 sections
DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE HUMAN PRESCRIPTION DRUG LABEL 2 61919-080 TABLET 2.50 mg ORAL NDA authorized generic 13 sections
Diphenoxylate hydrochloride and atropine sulfate HUMAN PRESCRIPTION DRUG LABEL 2 62135-618 TABLET 2.50 mg ORAL ANDA 19 sections
Diphenoxylate Hydrochloride and Atropine Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 62559-490 TABLET 2.50 mg ORAL ANDA 19 sections
Diphenoxylate Hydrochloride and Atropine Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 63187-939 TABLET 2.50 mg ORAL ANDA 19 sections
Diphenoxylate Hydrochloride and Atropine Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 63629-1933 TABLET 2.50 mg ORAL ANDA 19 sections
Diphenoxylate Hydrochloride and Atropine Sulfate HUMAN PRESCRIPTION DRUG LABEL 2 66336-437 TABLET 2.50 mg ORAL ANDA 11 sections