oxymorphone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists, morphinan derivates 2034 76-41-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • oxymorphone
  • 14-Hydroxydihydromorphinone
  • (-)-Oxymorphone
  • oxymorphone hydrochloride
  • oxymorphone HCl
An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)
  • Molecular weight: 301.34
  • Formula: C17H19NO4
  • CLOGP: -0.48
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 70
  • ALOGS: -1.07
  • ROTB: 0

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 24 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1.90 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.43 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 10 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
April 2, 1959 FDA ENDO PHARMS

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
Drug abuse 324.59 28.11 127 2685 63281 46619969
Toxicity to various agents 292.84 28.11 172 2640 211594 46471656
Completed suicide 194.16 28.11 116 2696 145804 46537446
Drug use disorder 121.26 28.11 29 2783 2706 46680544
Intentional product misuse 96.67 28.11 50 2762 47078 46636172
Respiratory arrest 93.56 28.11 44 2768 33772 46649478
Intentional product use issue 67.27 28.11 41 2771 52739 46630511
Cardiac arrest 64.44 28.11 49 2763 90350 46592900
Accidental poisoning 63.47 28.11 13 2799 592 46682658
Injection site abscess 62.39 28.11 14 2798 985 46682265
Death 58.07 28.11 85 2727 335463 46347787
Cardio-respiratory arrest 55.31 28.11 38 2774 59831 46623419
Accidental death 53.93 28.11 14 2798 1821 46681429
Staphylococcal bacteraemia 52.24 28.11 17 2795 4887 46678363
Injection site cellulitis 44.69 28.11 11 2801 1154 46682096
Endocarditis 43.93 28.11 15 2797 4997 46678253
Poisoning 34.96 28.11 17 2795 13977 46669273
Unresponsive to stimuli 31.04 28.11 21 2791 32153 46651097

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
Drug abuse 621.83 39.58 236 2215 81836 29868191
Toxicity to various agents 265.54 39.58 169 2282 177014 29773013
Respiratory arrest 215.04 39.58 83 2368 29175 29920852
Completed suicide 145.62 39.58 94 2357 99398 29850629
Intentional product misuse 142.19 39.58 65 2386 34602 29915425
Cardiac arrest 138.98 39.58 89 2362 92761 29857266
Poisoning 100.43 39.58 37 2414 11345 29938682
Drug use disorder 93.56 39.58 26 2425 3222 29946805
Accidental overdose 93.26 39.58 40 2411 18235 29931792
Cardio-respiratory arrest 88.12 39.58 56 2395 57250 29892777
Drug dependence 87.38 39.58 40 2411 21255 29928772
Intentional product use issue 72.39 39.58 42 2409 36398 29913629
Injection site abscess 68.45 39.58 15 2436 693 29949334
Accidental death 56.92 39.58 16 2435 2063 29947964
Injection site cellulitis 56.24 39.58 12 2439 488 29949539
Endocarditis 47.26 39.58 18 2433 6025 29944002
Drug withdrawal syndrome 45.13 39.58 25 2426 19784 29930243
Substance abuse 44.59 39.58 18 2433 7022 29943005
Death 41.20 39.58 90 2361 357193 29592834

Pharmacologic Action:

SourceCodeDescription
ATC N02AA11 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Natural opium alkaloids
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009294 Narcotics
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
FDA MoA N0000175684 Full Opioid Agonists
FDA EPC N0000175690 Opioid Agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Pain indication 22253000
General anesthesia indication 50697003
Severe pain indication 76948002
Chronic pain indication 82423001
Labor pain indication 247412007
Local anesthesia indication 386761002
Severe Pain with Opioid Tolerance indication
Chronic Pain with Opioid Tolerance indication
Anxiety due to Cardiac Asthma indication
Suicidal thoughts contraindication 6471006
Dependent drug abuse contraindication 6525002
Alcohol withdrawal delirium contraindication 8635005
Asthenia contraindication 13791008
Constipation contraindication 14760008 DOID:2089
Mood swings contraindication 18963009
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Hypercapnia contraindication 29596007
Dehydration contraindication 34095006
Disorder of gallbladder contraindication 39621005 DOID:0060262
Hypothyroidism contraindication 40930008 DOID:1459
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Ulcerative colitis contraindication 64766004 DOID:8577
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Urethral stricture contraindication 76618002
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Cor pulmonale contraindication 83291003 DOID:8515
Pulmonary emphysema contraindication 87433001
Kidney disease contraindication 90708001 DOID:557
Acute abdominal pain contraindication 116290004
Neoplasm of brain contraindication 126952004 DOID:1319
Seizure disorder contraindication 128613002
Drug-induced psychosis contraindication 191483003 DOID:1742
Disease of liver contraindication 235856003 DOID:409
Morbid obesity contraindication 238136002 DOID:11981
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Exacerbation of asthma contraindication 281239006
Lesion of brain contraindication 301766008
Coma contraindication 371632003
Primary adrenocortical insufficiency contraindication 373662000
Operation on gastrointestinal tract contraindication 386621005
Hypoxia contraindication 389086002
Central nervous system depression contraindication 418072004
Dysfunction of sphincter of Oddi contraindication 430887001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.31 acidic
pKa2 7.97 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG OPANULL ENDO PHARMS N021611 June 22, 2006 DISCN TABLET ORAL Oct. 25, 2022 ADDITIONULLL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
5MG OPANULL ENDO PHARMS N021611 June 22, 2006 DISCN TABLET ORAL Oct. 25, 2022 ADDITIONULLL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Kappa-type opioid receptor GPCR AGONIST Ki 6.83 WOMBAT-PK CHEMBL
Delta-type opioid receptor GPCR AGONIST Ki 7.30 CHEMBL CHEMBL
Mu-type opioid receptor GPCR AGONIST Ki 9.44 WOMBAT-PK CHEMBL
Kappa-type opioid receptor GPCR Ki 7.24 CHEMBL
Delta-type opioid receptor GPCR Ki 6.21 CHEMBL
Mu-type opioid receptor GPCR Ki 8.30 CHEMBL
Kappa-type opioid receptor GPCR Ki 7.02 CHEMBL
Delta-type opioid receptor GPCR Ki 7.09 CHEMBL
Mu-type opioid receptor GPCR Ki 9.01 CHEMBL
Mu-type opioid receptor GPCR Ki 9.27 CHEMBL
Opioid receptor GPCR IC50 10.89 CHEMBL
Opioid receptors; mu and delta GPCR Ki 8.33 CHEMBL

External reference:

IDSource
4019871 VUID
N0000147956 NUI
D00844 KEGG_DRUG
357-07-3 SECONDARY_CAS_RN
4019062 VANDF
4019871 VANDF
C0030073 UMLSCUI
CHEBI:7865 CHEBI
5284604 PUBCHEM_CID
DB01192 DRUGBANK_ID
CHEMBL963 ChEMBL_ID
CHEMBL1200794 ChEMBL_ID
D010111 MESH_DESCRIPTOR_UI
7094 IUPHAR_LIGAND_ID
937 INN_ID
9VXA968E0C UNII
7814 RXNORM
177273 MMSL
5220 MMSL
d00833 MMSL
001548 NDDF
004623 NDDF
24751001 SNOMEDCT_US
370266008 SNOMEDCT_US
69899006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0283 TABLET 5 mg ORAL ANDA 33 sections
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0284 TABLET 10 mg ORAL ANDA 33 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1231 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 32 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1232 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 32 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1233 TABLET, FILM COATED, EXTENDED RELEASE 20 mg ORAL ANDA 32 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1234 TABLET, FILM COATED, EXTENDED RELEASE 40 mg ORAL ANDA 32 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1315 TABLET, FILM COATED, EXTENDED RELEASE 7.50 mg ORAL ANDA 32 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1316 TABLET, FILM COATED, EXTENDED RELEASE 15 mg ORAL ANDA 32 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1317 TABLET, FILM COATED, EXTENDED RELEASE 30 mg ORAL ANDA 32 sections
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10702-070 TABLET 5 mg ORAL ANDA 35 sections
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10702-071 TABLET 10 mg ORAL ANDA 35 sections
Oxymorphone Hydrochloride Human Prescription Drug Label 1 13107-103 TABLET 5 mg ORAL ANDA 33 sections
Oxymorphone Hydrochloride Human Prescription Drug Label 1 13107-104 TABLET 10 mg ORAL ANDA 33 sections
OPANULLER HUMAN PRESCRIPTION DRUG LABEL 1 16590-609 TABLET, FILM COATED, EXTENDED RELEASE 40 mg ORAL NDA 18 sections
OPANULLER HUMAN PRESCRIPTION DRUG LABEL 1 16590-747 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 18 sections
OPANULL HUMAN PRESCRIPTION DRUG LABEL 1 16590-765 TABLET 10 mg ORAL NDA 30 sections
OPANULLER HUMAN PRESCRIPTION DRUG LABEL 1 16590-767 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 18 sections
OPANULL ER HUMAN PRESCRIPTION DRUG LABEL 1 21695-948 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 27 sections
OPANULL ER HUMAN PRESCRIPTION DRUG LABEL 1 21695-949 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 27 sections
OXYMORPHONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 31722-929 TABLET 5 mg ORAL ANDA 21 sections
OXYMORPHONE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 31722-930 TABLET 10 mg ORAL ANDA 21 sections
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 35356-967 TABLET 5 mg ORAL ANDA 30 sections
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 35356-968 TABLET 10 mg ORAL ANDA 30 sections
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-330 TABLET 5 mg ORAL ANDA 31 sections
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-331 TABLET 10 mg ORAL ANDA 31 sections
Oxymorphone Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54868-6379 TABLET 10 mg ORAL ANDA 32 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 55700-788 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 33 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63304-218 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 33 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63304-219 TABLET, FILM COATED, EXTENDED RELEASE 7.50 mg ORAL ANDA 33 sections
Oxymorphone hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 63304-220 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 33 sections