diphenoxylate ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

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 142.32 16.89 38 7365 2827 63478792
Pleural fibrosis 135.09 16.89 38 7365 3434 63478185
Deafness neurosensory 126.74 16.89 39 7364 4816 63476803
Pleural thickening 118.77 16.89 33 7370 2850 63478769
Diarrhoea 109.74 16.89 250 7153 715116 62766503
Blood magnesium increased 108.04 16.89 31 7372 3007 63478612
Dehydration 104.01 16.89 114 7289 173240 63308379
Epigastric discomfort 94.75 16.89 34 7369 6746 63474873
Osteopenia 85.21 16.89 43 7360 19742 63461877
Macular degeneration 85.03 16.89 46 7357 24330 63457289
Osteosclerosis 75.74 16.89 25 7378 3863 63477756
Bone cyst 75.70 16.89 22 7381 2232 63479387
Cyst 73.76 16.89 35 7368 14064 63467555
Skin lesion 65.07 16.89 42 7361 30679 63450940
Blood potassium increased 62.31 16.89 34 7369 18275 63463344
Dry eye 52.19 16.89 41 7362 40720 63440899
Exostosis 44.30 16.89 27 7376 17835 63463784
Osteoarthritis 44.18 16.89 55 7348 95288 63386331
Deformity 40.59 16.89 22 7381 11662 63469957
Blood creatinine increased 33.42 16.89 46 7357 87798 63393821
Chronic sinusitis 33.36 16.89 20 7383 12823 63468796
Crohn's disease 31.33 16.89 14 7389 4899 63476720
Paraesthesia oral 28.22 16.89 21 7382 19235 63462384
Renal impairment 27.39 16.89 42 7361 88313 63393306
Abdominal pain 25.82 16.89 84 7319 293372 63188247
Procedural pain 24.01 16.89 20 7383 21549 63460070
Nausea 23.60 16.89 175 7228 854296 62627323
Myocardial infarction 23.58 16.89 42 7361 99851 63381768
Sleep disorder 22.83 16.89 37 7366 81529 63400090
Small intestinal obstruction 22.50 16.89 18 7385 18319 63463300
Hypokalaemia 21.18 16.89 41 7362 103763 63377856
Purpura senile 21.16 16.89 6 7397 557 63481062
Bone hypertrophy 18.13 16.89 5 7398 419 63481200
Gastroenteritis radiation 17.60 16.89 5 7398 467 63481152
Clostridial infection 17.32 16.89 9 7394 4383 63477236
Large intestinal stenosis 17.18 16.89 7 7396 1956 63479663

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 123.77 18.81 100 3181 129869 34823781
Diarrhoea 100.20 18.81 150 3131 389762 34563888
Small intestinal obstruction 24.46 18.81 16 3265 14850 34938800
Off label use 22.26 18.81 6 3275 419518 34534132

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 152.63 17.97 38 7582 2622 79734146
Pleural fibrosis 144.89 17.97 40 7580 4127 79732641
Diarrhoea 140.92 17.97 278 7342 880211 78856557
Dehydration 126.08 17.97 136 7484 248051 79488717
Deafness neurosensory 124.99 17.97 40 7580 6858 79729910
Pleural thickening 124.17 17.97 33 7587 2949 79733819
Blood magnesium increased 109.75 17.97 31 7589 3475 79733293
Epigastric discomfort 96.30 17.97 34 7586 7862 79728906
Osteopenia 90.06 17.97 41 7579 18323 79718445
Cyst 84.35 17.97 36 7584 13804 79722964
Osteosclerosis 71.82 17.97 23 7597 3948 79732820
Bone cyst 70.88 17.97 22 7598 3411 79733357
Dry eye 58.31 17.97 39 7581 36892 79699876
Blood potassium increased 56.30 17.97 35 7585 29240 79707528
Skin lesion 56.20 17.97 40 7580 41804 79694964
Osteoarthritis 53.47 17.97 53 7567 87256 79649512
Deformity 48.84 17.97 22 7598 9583 79727185
Exostosis 39.79 17.97 23 7597 16835 79719933
Chronic sinusitis 34.05 17.97 19 7601 13007 79723761
Macular degeneration 33.75 17.97 18 7602 11278 79725490
Blood creatinine increased 33.39 17.97 56 7564 155001 79581767
Nausea 32.48 17.97 178 7442 957018 78779750
Sleep disorder 30.13 17.97 39 7581 85638 79651130
Paraesthesia oral 28.47 17.97 20 7600 20451 79716317
Gastrointestinal disorder 24.80 17.97 43 7577 122162 79614606
Procedural pain 24.14 17.97 19 7601 23065 79713703
Small intestinal obstruction 23.38 17.97 20 7600 27252 79709516
Myocardial infarction 18.85 17.97 49 7571 184080 79552688
Crohn's disease 18.20 17.97 7 7613 2053 79734715
Vertigo positional 18.12 17.97 8 7612 3322 79733446
Purpura senile 18.01 17.97 5 7615 525 79736243

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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
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 21 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 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 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 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 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 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