oxymorphone ๐Ÿถ Veterinary Use | 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 ยตM/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
Toxicity to various agents 227.62 27.65 137 2576 247113 63239196
Drug abuse 224.52 27.65 92 2621 72426 63413883
Completed suicide 188.35 27.65 101 2612 145572 63340737
Drug use disorder 113.87 27.65 29 2684 4955 63481354
Intentional product misuse 94.88 27.65 48 2665 60869 63425440
Respiratory arrest 69.82 27.65 32 2681 32613 63453696
Injection site abscess 64.64 27.65 14 2699 1184 63485125
Cardio-respiratory arrest 61.91 27.65 36 2677 59923 63426386
Staphylococcal bacteraemia 55.98 27.65 17 2696 5513 63480796
Accidental poisoning 55.22 27.65 11 2702 617 63485692
Death 52.89 27.65 72 2641 374309 63112000
Cardiac arrest 47.66 27.65 36 2677 92509 63393800
Injection site cellulitis 47.64 27.65 11 2702 1243 63485066
Intentional product use issue 47.32 27.65 41 2672 127851 63358458
Endocarditis 46.96 27.65 15 2698 5735 63480574
Fanconi syndrome 41.32 27.65 10 2703 1382 63484927
Accidental death 37.85 27.65 10 2703 1966 63484343
Overdose 34.89 27.65 33 2680 115045 63371264
Drug dependence 31.49 27.65 17 2696 24466 63461843
Drug screen positive 27.72 27.65 9 2704 3620 63482689

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 285.18 37.27 130 1896 98966 34855939
Toxicity to various agents 209.14 37.27 134 1892 200228 34754677
Drug use disorder 124.68 37.27 32 1994 4159 34950746
Drug dependence 102.56 37.27 42 1984 24175 34930730
Completed suicide 97.44 37.27 64 1962 98104 34856801
Intentional product misuse 94.31 37.27 48 1978 45563 34909342
Accidental overdose 75.36 37.27 32 1994 20108 34934797
Drug withdrawal syndrome 72.51 37.27 31 1995 19803 34935102
Injection site abscess 70.90 37.27 15 2011 834 34954071
Intentional product use issue 66.60 37.27 42 1984 59774 34895131
Injection site cellulitis 58.58 37.27 12 2014 569 34954336
Endocarditis 48.18 37.27 17 2009 6494 34948411
Overdose 40.58 37.27 37 1989 91022 34863883
Therapeutic product effect decreased 37.61 37.27 24 2002 34719 34920186
Pneumomediastinum 37.39 37.27 11 2015 2356 34952549

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
Drug abuse 471.87 27.33 204 3675 162487 79578022
Toxicity to various agents 433.72 27.33 262 3617 421278 79319231
Completed suicide 280.46 27.33 164 3715 245603 79494906
Drug use disorder 238.48 27.33 60 3819 8591 79731918
Intentional product misuse 185.64 27.33 91 3788 95074 79645435
Injection site abscess 142.17 27.33 29 3850 1611 79738898
Intentional product use issue 113.76 27.33 78 3801 152034 79588475
Injection site cellulitis 106.90 27.33 23 3856 1655 79738854
Endocarditis 100.75 27.33 32 3847 10565 79729944
Respiratory arrest 100.12 27.33 51 3828 57499 79683010
Staphylococcal bacteraemia 96.28 27.33 32 3847 12186 79728323
Cardio-respiratory arrest 91.51 27.33 60 3819 108450 79632059
Accidental overdose 89.60 27.33 42 3837 39539 79700970
Death 86.72 27.33 121 3758 566393 79174116
Drug dependence 76.36 27.33 38 3841 40731 79699778
Cardiac arrest 62.96 27.33 58 3821 172038 79568471
Accidental death 62.48 27.33 18 3861 4273 79736236
Staphylococcal infection 53.42 27.33 34 3845 58261 79682248
Drug withdrawal syndrome 52.41 27.33 28 3851 34690 79705819
Overdose 48.64 27.33 52 3827 184154 79556355
Accidental poisoning 43.17 27.33 11 3868 1646 79738863
Acute kidney injury 41.42 27.33 83 3796 519321 79221188
Drug screen positive 40.36 27.33 14 3865 6049 79734460
Thrombotic microangiopathy 38.33 27.33 19 3860 20150 79720359
Pneumomediastinum 34.53 27.33 11 3868 3656 79736853
Substance abuse 29.58 27.33 13 3866 10513 79729996
Oesophageal rupture 28.28 27.33 7 3872 932 79739577

FDA Adverse Event Reporting System (Pediatric)

None

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 | Suggest Off label Use Form| |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




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 9.31 acidic
pKa2 7.97 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 June 22, 2006 DISCN TABLET, EXTENDED RELEASE ORAL 7276250 Feb. 4, 2023 RELIEF OF MODERATE TO SEVERE PAIN
15MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 Feb. 29, 2008 DISCN TABLET, EXTENDED RELEASE ORAL 7276250 Feb. 4, 2023 RELIEF OF MODERATE TO SEVERE PAIN
20MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 June 22, 2006 DISCN TABLET, EXTENDED RELEASE ORAL 7276250 Feb. 4, 2023 RELIEF OF MODERATE TO SEVERE PAIN
30MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 Feb. 29, 2008 DISCN TABLET, EXTENDED RELEASE ORAL 7276250 Feb. 4, 2023 RELIEF OF MODERATE TO SEVERE PAIN
40MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 June 22, 2006 DISCN TABLET, EXTENDED RELEASE ORAL 7276250 Feb. 4, 2023 RELIEF OF MODERATE TO SEVERE PAIN
5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 June 22, 2006 DISCN TABLET, EXTENDED RELEASE ORAL 7276250 Feb. 4, 2023 RELIEF OF MODERATE TO SEVERE PAIN
7.5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 Feb. 29, 2008 DISCN TABLET, EXTENDED RELEASE ORAL 7276250 Feb. 4, 2023 RELIEF OF MODERATE TO SEVERE PAIN
10MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 June 22, 2006 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 DOSE MODIFICATION FOR RENAL IMPAIRMENT
15MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 Feb. 29, 2008 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 DOSE MODIFICATION FOR RENAL IMPAIRMENT
20MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 June 22, 2006 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 DOSE MODIFICATION FOR RENAL IMPAIRMENT
30MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 Feb. 29, 2008 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 DOSE MODIFICATION FOR RENAL IMPAIRMENT
40MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 June 22, 2006 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 DOSE MODIFICATION FOR RENAL IMPAIRMENT
5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 June 22, 2006 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 DOSE MODIFICATION FOR RENAL IMPAIRMENT
7.5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** OPANA ER ENDO PHARMS N021610 Feb. 29, 2008 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 DOSE MODIFICATION FOR RENAL IMPAIRMENT
10MG OPANA ER ENDO PHARMS N201655 Dec. 9, 2011 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 METHOD OF ADMINISTRATION OF CONTROLLED RELEASE OXYMORPHONE
15MG OPANA ER ENDO PHARMS N201655 Dec. 9, 2011 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 METHOD OF ADMINISTRATION OF CONTROLLED RELEASE OXYMORPHONE
20MG OPANA ER ENDO PHARMS N201655 Dec. 9, 2011 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 METHOD OF ADMINISTRATION OF CONTROLLED RELEASE OXYMORPHONE
30MG OPANA ER ENDO PHARMS N201655 Dec. 9, 2011 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 METHOD OF ADMINISTRATION OF CONTROLLED RELEASE OXYMORPHONE
40MG OPANA ER ENDO PHARMS N201655 Dec. 9, 2011 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 METHOD OF ADMINISTRATION OF CONTROLLED RELEASE OXYMORPHONE
5MG OPANA ER ENDO PHARMS N201655 Dec. 9, 2011 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 METHOD OF ADMINISTRATION OF CONTROLLED RELEASE OXYMORPHONE
7.5MG OPANA ER ENDO PHARMS N201655 Dec. 9, 2011 DISCN TABLET, EXTENDED RELEASE ORAL 8808737 June 21, 2027 METHOD OF ADMINISTRATION OF CONTROLLED RELEASE OXYMORPHONE

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 Ki 9.44 WOMBAT-PK CHEMBL
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 Ki 9.01 CHEMBL
Mu-type opioid receptor GPCR Ki 8.30 CHEMBL
Mu-type opioid receptor GPCR Ki 9.27 CHEMBL
Delta-type opioid receptor GPCR Ki 6.21 CHEMBL
Delta-type opioid receptor GPCR Ki 7.09 CHEMBL
Kappa-type opioid receptor GPCR Ki 7.24 CHEMBL
Kappa-type opioid receptor GPCR Ki 7.02 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
CHEMBL963 ChEMBL_ID
DB01192 DRUGBANK_ID
CHEMBL1200794 ChEMBL_ID
D010111 MESH_DESCRIPTOR_UI
5284604 PUBCHEM_CID
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 0054-0283 TABLET 5 mg ORAL ANDA 33 sections
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 0054-0284 TABLET 10 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 0115-1231 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 0115-1232 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 0115-1233 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 0115-1234 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 0115-1315 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 0115-1316 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 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 10702-070 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 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
OPANAER HUMAN PRESCRIPTION DRUG LABEL 1 16590-609 TABLET, FILM COATED, EXTENDED RELEASE 40 mg ORAL NDA 18 sections
OPANAER HUMAN PRESCRIPTION DRUG LABEL 1 16590-747 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 18 sections
OPANA HUMAN PRESCRIPTION DRUG LABEL 1 16590-765 TABLET 10 mg ORAL NDA 30 sections
OPANAER HUMAN PRESCRIPTION DRUG LABEL 1 16590-767 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 18 sections