diphenoxylate ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
analgesics, pethidine derivatives 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

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 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 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 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 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
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:

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
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