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Identification
NameOxymorphone
Accession NumberDB01192  (APRD00158)
TypeSmall Molecule
GroupsApproved, Investigational, Vet Approved
Description

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)

Structure
Thumb
Synonyms
14-Hydroxydihydromorphinone
Dihydrohydroxymorphinone
Dihydroxymorphinone
EN3202
Numorphan
Opana
Oximorphonum
Oxymorphine
Oxymorphone
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Numorphan Injection 1.5mg/mlliquid1.5 mgintramuscular; intravenous; subcutaneousBristol Myers Squibb Canada1993-12-312004-08-04Canada
Numorphan Suppository 5mgsuppository5 mgrectalBristol Myers Squibb Canada1993-12-312002-07-04Canada
Opanatablet10 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-09Not applicableUs
Opanatablet5 mg/1oralbryant ranch prepack2006-06-26Not applicableUs
Opanainjection1 mg/mLintramuscular; intravenous; subcutaneousEndo Pharmaceuticals Inc.1959-06-01Not applicableUs
Opanatablet10 mg/1oralEndo Pharmaceuticals2006-06-26Not applicableUs
Opanatablet5 mg/1oralEndo Pharmaceuticals2006-06-26Not applicableUs
Opanatablet5 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-09Not applicableUs
Opanatablet10 mg/1oralSTAT Rx USA LLC2011-12-15Not applicableUs
Opana ERtablet, extended release20 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-10Not applicableUs
Opana ERtablet, film coated, extended release40 mg/1oralSTAT Rx USA LLC2006-06-22Not applicableUs
Opana ERtablet, extended release10 mg/1oralEndo Pharmaceuticals Inc.2012-03-20Not applicableUs
Opana ERtablet20 mg/1oralSt Marys Medical Park Pharmacy2010-12-31Not applicableUs
Opana ERtablet, extended release30 mg/1oralLake Erie Medical DBA Quality Care Products LLC2012-03-20Not applicableUs
Opana ERtablet, extended release10 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-10Not applicableUs
Opana ERtablet, extended release40 mg/1oralbryant ranch prepack2006-06-30Not applicableUs
Opana ERtablet, extended release7.5 mg/1oralEndo Pharmaceuticals Inc.2012-03-20Not applicableUs
Opana ERtablet, extended release40 mg/1oralLake Erie Medical DBA Quality Care Products LLC2012-03-20Not applicableUs
Opana ERtablet20 mg/1oralbryant ranch prepack2010-12-31Not applicableUs
Opana ERtablet, extended release5 mg/1oralEndo Pharmaceuticals Inc.2012-03-20Not applicableUs
Opana ERtablet, extended release20 mg/1oralLake Erie Medical DBA Quality Care Products LLC2012-03-20Not applicableUs
Opana ERtablet, film coated, extended release10 mg/1oralRebel Distributors Corp2006-06-22Not applicableUs
Opana ERtablet (extended-release)40 mgoralValeant Canada Lp Valeant Canada S.E.C.Not applicableNot applicableCanada
Opana ERtablet, extended release40 mg/1oralEndo Pharmaceuticals Inc.2012-03-20Not applicableUs
Opana ERtablet, extended release10 mg/1oralLake Erie Medical DBA Quality Care Products LLC2012-03-20Not applicableUs
Opana ERtablet, film coated, extended release5 mg/1oralRebel Distributors Corp2006-06-22Not applicableUs
Opana ERtablet (extended-release)20 mgoralValeant Canada Lp Valeant Canada S.E.C.Not applicableNot applicableCanada
Opana ERtablet, extended release30 mg/1oralEndo Pharmaceuticals Inc.2012-03-20Not applicableUs
Opana ERtablet, film coated, extended release5 mg/1oralSTAT Rx USA LLC2006-06-22Not applicableUs
Opana ERtablet, extended release20 mg/1oralEndo Pharmaceuticals Inc.2012-03-20Not applicableUs
Opana ERtablet, extended release30 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-14Not applicableUs
Opana ERtablet (extended-release)10 mgoralValeant Canada Lp Valeant Canada S.E.C.Not applicableNot applicableCanada
Opana ERtablet, extended release40 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-14Not applicableUs
Opana ERtablet, film coated, extended release10 mg/1oralSTAT Rx USA LLC2006-06-22Not applicableUs
Opana ERtablet (extended-release)5 mgoralValeant Canada Lp Valeant Canada S.E.C.Not applicableNot applicableCanada
Opana ERtablet, extended release15 mg/1oralEndo Pharmaceuticals Inc.2012-03-20Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralAmerican Health Packaging2015-12-21Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralQualitest Pharmaceuticals2010-09-29Not applicableUs
Oxymorphone Hydrochloridetablet5 mg/1oralQualitest Pharmaceuticals2010-09-29Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Oxymorphone Hydrochloridetablet, extended release7.5 mg/1oralActavis Elizabeth LLC2010-12-31Not applicableUs
Oxymorphone Hydrochloridetablet5 mg/1oralRoxane Laboratories, Inc2010-09-27Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release30 mg/1oralImpax Generics2013-01-02Not applicableUs
Oxymorphone Hydrochloridetablet5 mg/1oralCore Pharma, Llc2015-01-17Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release40 mg/1oralRanbaxy Pharmaceuticals Inc.2015-04-13Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralLake Erie Medical DBA Quality Care Products LLC2013-02-11Not applicableUs
Oxymorphone Hydrochloridetablet, extended release40 mg/1oralActavis Elizabeth LLC2010-12-31Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release15 mg/1oralImpax Generics2013-01-02Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release30 mg/1oralRanbaxy Pharmaceuticals Inc.2015-04-13Not applicableUs
Oxymorphone Hydrochloridetablet5 mg/1oralLake Erie Medical DBA Quality Care Products LLC2013-02-11Not applicableUs
Oxymorphone Hydrochloridetablet, extended release20 mg/1oralActavis Elizabeth LLC2010-12-31Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release7.5 mg/1oralImpax Generics2013-01-02Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release20 mg/1oralRanbaxy Pharmaceuticals Inc.2015-04-13Not applicableUs
Oxymorphone Hydrochloridetablet, extended release15 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-12-31Not applicableUs
Oxymorphone Hydrochloridetablet, extended release10 mg/1oralActavis Elizabeth LLC2010-12-31Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release40 mg/1oralImpax Generics2013-01-02Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release15 mg/1oralRanbaxy Pharmaceuticals Inc.2015-04-13Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-11-29Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release20 mg/1oralImpax Generics2013-01-02Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release10 mg/1oralRanbaxy Pharmaceuticals Inc.2015-04-13Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralKvk Tech, Inc.2013-02-11Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralMallinckrodt, Inc.2012-04-12Not applicableUs
Oxymorphone Hydrochloridetablet, extended release5 mg/1oralActavis Elizabeth LLC2010-12-31Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release10 mg/1oralImpax Generics2013-01-02Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release7.5 mg/1oralRanbaxy Pharmaceuticals Inc.2015-04-13Not applicableUs
Oxymorphone Hydrochloridetablet5 mg/1oralKvk Tech, Inc.2013-02-11Not applicableUs
Oxymorphone Hydrochloridetablet5 mg/1oralMallinckrodt, Inc.2012-04-12Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralTeva Pharmaceuticals USA Inc2013-04-11Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release5 mg/1oralRanbaxy Pharmaceuticals Inc.2015-04-13Not applicableUs
Oxymorphone Hydrochloridetablet, extended release30 mg/1oralActavis Elizabeth LLC2010-12-31Not applicableUs
Oxymorphone Hydrochloridetablet5 mg/1oralTeva Pharmaceuticals USA Inc2013-04-11Not applicableUs
Oxymorphone Hydrochloridetablet, film coated, extended release5 mg/1oralImpax Generics2013-01-02Not applicableUs
Oxymorphone Hydrochloridetablet, extended release15 mg/1oralActavis Elizabeth LLC2010-12-31Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralRoxane Laboratories, Inc2010-09-27Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralCore Pharma, Llc2015-01-17Not applicableUs
Oxymorphone Hydrochloridetablet10 mg/1oralPhysicians Total Care, Inc.2012-12-10Not applicableUs
Oxymorphone Hydrochloride Extended-releasetablet, extended release40 mg/1oralMallinckrodt, Inc.2014-06-27Not applicableUs
Oxymorphone Hydrochloride Extended-releasetablet, extended release7.5 mg/1oralMallinckrodt, Inc.2014-06-27Not applicableUs
Oxymorphone Hydrochloride Extended-releasetablet, extended release20 mg/1oralMallinckrodt, Inc.2014-06-27Not applicableUs
Oxymorphone Hydrochloride Extended-releasetablet, extended release10 mg/1oralMallinckrodt, Inc.2014-06-27Not applicableUs
Oxymorphone Hydrochloride Extended-releasetablet, extended release5 mg/1oralMallinckrodt, Inc.2014-06-27Not applicableUs
Oxymorphone Hydrochloride Extended-releasetablet, extended release30 mg/1oralMallinckrodt, Inc.2014-06-27Not applicableUs
Oxymorphone Hydrochloride Extended-releasetablet, extended release15 mg/1oralMallinckrodt, Inc.2014-06-27Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
NumorphanNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Oxymorphone hydrochloride
ThumbNot applicableDBSALT001249
Categories
UNII9VXA968E0C
CAS number76-41-5
WeightAverage: 301.3371
Monoisotopic: 301.131408101
Chemical FormulaC17H19NO4
InChI KeyInChIKey=UQCNKQCJZOAFTQ-ISWURRPUSA-N
InChI
InChI=1S/C17H19NO4/c1-18-7-6-16-13-9-2-3-10(19)14(13)22-15(16)11(20)4-5-17(16,21)12(18)8-9/h2-3,12,15,19,21H,4-8H2,1H3/t12-,15+,16+,17-/m1/s1
IUPAC Name
(1S,5R,13R,17S)-10,17-dihydroxy-4-methyl-12-oxa-4-azapentacyclo[9.6.1.0¹,¹³.0⁵,¹⁷.0⁷,¹⁸]octadeca-7(18),8,10-trien-14-one
SMILES
[H][C@@]12OC3=C(O)C=CC4=C3[C@@]11CCN(C)[C@]([H])(C4)[C@]1(O)CCC2=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as morphinans. These are polycyclic compounds with a four-ring skeleton with three condensed six-member rings forming a partially hydrogenated phenanthrene moiety, one of which is aromatic while the two others are alicyclic.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassMorphinans
Sub ClassNot Available
Direct ParentMorphinans
Alternative Parents
Substituents
  • Morphinan
  • Benzylisoquinoline
  • Phenanthrene
  • Isoquinolone
  • Tetralin
  • Benzofuran
  • Aralkylamine
  • Cyclohexanone
  • Alkyl aryl ether
  • Benzenoid
  • Piperidine
  • Tertiary alcohol
  • Cyclic alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketone
  • 1,2-aminoalcohol
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of moderate-to-severe pain.
PharmacodynamicsOxymorphone is a semi-synthetic opioid substitute for morphine. It is a potent analgesic. Opioid analgesics exert their principal pharmacologic effects on the CNS and the gastrointestinal tract. The principal actions of therapeutic value are analgesia and sedation. Opioids produce respiratory depression by direct action on brain stem respiratory centers. The mechanism of respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation.
Mechanism of actionOxymorphone interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. Also, it has been shown that oxymorphone binds to and inhibits GABA inhibitory interneurons via mu-receptors. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Oxymorphone undergoes extensive hepatic metabolism in humans. After a 10 mg oral dose, 49% was excreted over a five-day period in the urine. Of this, 82% was excreted in the first 24 hours after administration. The recovered drug-related products contained the oxymorphone (1.9%), the conjugate of oxymorphone (44.1%), the 6(beta)-carbinol produced by 6-keto reduction of oxymorphone (0.3%), and the conjugates of 6(beta)-carbinol (2.6%) and 6(alpha)-carbinol (0.1%).

SubstrateEnzymesProduct
Oxymorphone
noroxycodoneDetails
Oxymorphone
noroxymorphoneDetails
Oxymorphone
alpha-noroxycodolDetails
Oxymorphone
beta-noroxycodolDetails
Oxymorphone
oxymorphoneDetails
Oxymorphone
beta-oxymorpholDetails
Oxymorphone
alpha-oxycodolDetails
Oxymorphone
beta-oxycodolDetails
Route of eliminationOxymorphone is highly metabolized, principally in the liver, and undergoes reduction or conjugation with glucuronic acid to form both active and inactive products. Because oxymorphone is extensively metabolized, <1% of the administered dose is excreted unchanged in the urine.
Half life1.3 (+/-0.7) hours
ClearanceNot Available
ToxicityOxymorphone overdosage is characterized by respiratory depression, extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. In a severe case of overdose, apnea, circulatory collapse, cardiac arrest, and death may occur. Intravenous mouse LD50 is 172 mg/kg.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Oxymorphone Action PathwayDrug actionSMP00412
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9934
Blood Brain Barrier+0.9382
Caco-2 permeable+0.7798
P-glycoprotein substrateSubstrate0.9112
P-glycoprotein inhibitor INon-inhibitor0.8887
P-glycoprotein inhibitor IINon-inhibitor0.9734
Renal organic cation transporterNon-inhibitor0.5585
CYP450 2C9 substrateNon-substrate0.8014
CYP450 2D6 substrateSubstrate0.8105
CYP450 3A4 substrateSubstrate0.7439
CYP450 1A2 substrateNon-inhibitor0.8796
CYP450 2C9 inhibitorNon-inhibitor0.9459
CYP450 2D6 inhibitorNon-inhibitor0.7168
CYP450 2C19 inhibitorNon-inhibitor0.8455
CYP450 3A4 inhibitorNon-inhibitor0.9219
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9812
Ames testNon AMES toxic0.6663
CarcinogenicityNon-carcinogens0.9635
BiodegradationNot ready biodegradable0.9758
Rat acute toxicity2.9920 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9345
hERG inhibition (predictor II)Non-inhibitor0.9374
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Liquidintramuscular; intravenous; subcutaneous1.5 mg
Suppositoryrectal5 mg
Injectionintramuscular; intravenous; subcutaneous1 mg/mL
Tabletoral20 mg/1
Tablet (extended-release)oral10 mg
Tablet (extended-release)oral20 mg
Tablet (extended-release)oral40 mg
Tablet (extended-release)oral5 mg
Tablet, film coated, extended releaseoral10 mg/1
Tablet, film coated, extended releaseoral40 mg/1
Tablet, film coated, extended releaseoral5 mg/1
Tabletoral10 mg/1
Tabletoral5 mg/1
Tablet, extended releaseoral10 mg/1
Tablet, extended releaseoral15 mg/1
Tablet, extended releaseoral20 mg/1
Tablet, extended releaseoral30 mg/1
Tablet, extended releaseoral40 mg/1
Tablet, extended releaseoral5 mg/1
Tablet, extended releaseoral7.5 mg/1
Tablet, film coated, extended releaseoral15 mg/1
Tablet, film coated, extended releaseoral20 mg/1
Tablet, film coated, extended releaseoral30 mg/1
Tablet, film coated, extended releaseoral7.5 mg/1
Prices
Unit descriptionCostUnit
Opana er 40 mg tablet21.82USD tablet
Opana er 30 mg tablet17.39USD tablet
Opana ER 40 mg 12 Hour tablet12.42USD tablet
Opana er 20 mg tablet12.12USD tablet
Opana ER 30 mg 12 Hour tablet9.76USD tablet
Opana er 15 mg tablet9.26USD tablet
Opana ER 20 mg 12 Hour tablet7.17USD tablet
Opana ER 15 mg 12 Hour tablet5.82USD tablet
Opana er 5 mg tablet5.53USD tablet
Opana ER 10 mg 12 Hour tablet4.4USD tablet
Opana er 10 mg tablet3.95USD tablet
Opana ER 7.5 mg 12 Hour tablet3.3USD tablet
Numorphan 1 mg/ml ampul3.13USD ml
Opana er 7.5 mg tablet3.0USD tablet
Opana ER 5 mg 12 Hour tablet2.3USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5662933 No1993-09-092013-09-09Us
US7276250 No2003-02-042023-02-04Us
US7851482 No2009-07-102029-07-10Us
US8075872 No2003-11-202023-11-20Us
US8114383 No2004-08-082024-08-08Us
US8192722 No2005-09-152025-09-15Us
US8309060 No2003-11-202023-11-20Us
US8309122 No2003-02-042023-02-04Us
US8329216 No2003-02-042023-02-04Us
US8808737 No2007-06-212027-06-21Us
US8871779 No2009-11-222029-11-22Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point248-249 °CPhysProp
water solubility2.4E+004 mg/LNot Available
logP0.83HANSCH,C ET AL. (1995)
pKa8.17SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility25.6 mg/mLALOGPS
logP1.26ALOGPS
logP0.78ChemAxon
logS-1.1ALOGPS
pKa (Strongest Acidic)7.34ChemAxon
pKa (Strongest Basic)10.93ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area70 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity79.56 m3·mol-1ChemAxon
Polarizability30.77 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-0udl-7932000000-89141254d526ca629dacView in MoNA
References
Synthesis Reference

Bao-Shan Huang, Yansong Lu, Ben-Yi Ji, Aris P Christodoulou, “Preparation of oxymorphone from morphine.” U.S. Patent US5922876, issued May, 1992.

US5922876
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (9.95 MB)
MSDSDownload (133 KB)
Interactions
Drug Interactions
Drug
AcepromazineAcepromazine may increase the hypotensive activities of Oxymorphone.
AcetazolamideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Acetazolamide.
AlvimopanThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Alvimopan.
AmilorideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Amiloride.
Ammonium chlorideAmmonium chloride may increase the excretion rate of Oxymorphone which could result in a higher serum level.
AmphetamineAmphetamine may increase the analgesic activities of Oxymorphone.
AzelastineOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Oxymorphone.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Bendroflumethiazide.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
BumetanideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Bumetanide.
ButorphanolButorphanol may decrease the analgesic activities of Oxymorphone.
CathinoneCathinone may increase the analgesic activities of Oxymorphone.
ChlorothiazideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Chlorothiazide.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Chlorthalidone.
CyclothiazideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Cyclothiazide.
DesmopressinThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Desmopressin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
EluxadolineOxymorphone may increase the activities of Eluxadoline.
Etacrynic acidThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Ethacrynic acid.
EthanolOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthoxzolamideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Ethoxzolamide.
FurosemideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Furosemide.
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Hydrochlorothiazide.
HydrocodoneOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroflumethiazideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Hydroflumethiazide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
IndapamideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Indapamide.
IsocarboxazidThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Isocarboxazid.
LinezolidThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Linezolid.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Oxymorphone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
MethotrimeprazineOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetolazoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Metolazone.
MetyrosineOxymorphone may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
MirtazapineOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoclobemideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Moclobemide.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
NaltrexoneThe therapeutic efficacy of Oxymorphone can be decreased when used in combination with Naltrexone.
OrphenadrineOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineOxymorphone may increase the serotonergic activities of Paroxetine.
PegvisomantThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Oxymorphone.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
PhenelzineThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Phenelzine.
PramipexoleOxymorphone may increase the sedative activities of Pramipexole.
ProcarbazineThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Procarbazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Oxymorphone.
RamosetronOxymorphone may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Rasagiline.
RopiniroleOxymorphone may increase the sedative activities of Ropinirole.
RotigotineOxymorphone may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Oxymorphone.
SelegilineThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Selegiline.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
SpironolactoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Spironolactone.
SuccinylcholineSuccinylcholine may increase the bradycardic activities of Oxymorphone.
SuvorexantOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Tedizolid Phosphate.
ThalidomideOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TicrynafenThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Ticrynafen.
TorasemideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Torasemide.
TranylcypromineThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Tranylcypromine.
TriamtereneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Triamterene.
TrichlormethiazideThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Trichlormethiazide.
ZolpidemOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Voltage-gated calcium channel activity
Specific Function:
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 Da
References
  1. Spetea M, Nevin ST, Hosztafi S, Ronai AZ, Toth G, Borsodi A: Affinity profiles of novel delta-receptor selective benzofuran derivatives of non-peptide opioids. Neurochem Res. 1998 Sep;23(9):1211-6. [PubMed:9712193 ]
  2. Lemberg KK, Kontinen VK, Siiskonen AO, Viljakka KM, Yli-Kauhaluoma JT, Korpi ER, Kalso EA: Antinociception by spinal and systemic oxycodone: why does the route make a difference? In vitro and in vivo studies in rats. Anesthesiology. 2006 Oct;105(4):801-12. [PubMed:17006080 ]
  3. Chamberlin KW, Cottle M, Neville R, Tan J: Oral oxymorphone for pain management. Ann Pharmacother. 2007 Jul;41(7):1144-52. Epub 2007 Jun 26. [PubMed:17595308 ]
  4. Halimi G, Devaux C, Clot-Faybesse O, Sampol J, Legof L, Rochat H, Guieu R: Modulation of adenosine concentration by opioid receptor agonists in rat striatum. Eur J Pharmacol. 2000 Jun 16;398(2):217-24. [PubMed:10854833 ]
  5. Gardell LR, King T, Ossipov MH, Rice KC, Lai J, Vanderah TW, Porreca F: Opioid receptor-mediated hyperalgesia and antinociceptive tolerance induced by sustained opiate delivery. Neurosci Lett. 2006 Mar 20;396(1):44-9. Epub 2005 Dec 15. [PubMed:16343768 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurot...
Gene Name:
OPRD1
Uniprot ID:
P41143
Molecular Weight:
40368.235 Da
References
  1. Chamberlin KW, Cottle M, Neville R, Tan J: Oral oxymorphone for pain management. Ann Pharmacother. 2007 Jul;41(7):1144-52. Epub 2007 Jun 26. [PubMed:17595308 ]
  2. Ananthan S, Khare NK, Saini SK, Seitz LE, Bartlett JL, Davis P, Dersch CM, Porreca F, Rothman RB, Bilsky EJ: Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. J Med Chem. 2004 Mar 11;47(6):1400-12. [PubMed:14998329 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Gronlund J, Saari TI, Hagelberg NM, Neuvonen PJ, Olkkola KT, Laine K: Exposure to oral oxycodone is increased by concomitant inhibition of CYP2D6 and 3A4 pathways, but not by inhibition of CYP2D6 alone. Br J Clin Pharmacol. 2010 Jul;70(1):78-87. doi: 10.1111/j.1365-2125.2010.03653.x. [PubMed:20642550 ]
  2. Samer CF, Daali Y, Wagner M, Hopfgartner G, Eap CB, Rebsamen MC, Rossier MF, Hochstrasser D, Dayer P, Desmeules JA: The effects of CYP2D6 and CYP3A activities on the pharmacokinetics of immediate release oxycodone. Br J Pharmacol. 2010 Jun;160(4):907-18. doi: 10.1111/j.1476-5381.2010.00673.x. [PubMed:20590587 ]
  3. Lalovic B, Kharasch E, Hoffer C, Risler L, Liu-Chen LY, Shen DD: Pharmacokinetics and pharmacodynamics of oral oxycodone in healthy human subjects: role of circulating active metabolites. Clin Pharmacol Ther. 2006 May;79(5):461-79. [PubMed:16678548 ]
  4. Adams M, Pieniaszek HJ Jr, Gammaitoni AR, Ahdieh H: Oxymorphone extended release does not affect CYP2C9 or CYP3A4 metabolic pathways. J Clin Pharmacol. 2005 Mar;45(3):337-45. [PubMed:15703368 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Gronlund J, Saari TI, Hagelberg NM, Neuvonen PJ, Olkkola KT, Laine K: Exposure to oral oxycodone is increased by concomitant inhibition of CYP2D6 and 3A4 pathways, but not by inhibition of CYP2D6 alone. Br J Clin Pharmacol. 2010 Jul;70(1):78-87. doi: 10.1111/j.1365-2125.2010.03653.x. [PubMed:20642550 ]
  2. Samer CF, Daali Y, Wagner M, Hopfgartner G, Eap CB, Rebsamen MC, Rossier MF, Hochstrasser D, Dayer P, Desmeules JA: The effects of CYP2D6 and CYP3A activities on the pharmacokinetics of immediate release oxycodone. Br J Pharmacol. 2010 Jun;160(4):907-18. doi: 10.1111/j.1476-5381.2010.00673.x. [PubMed:20590587 ]
  3. Lalovic B, Kharasch E, Hoffer C, Risler L, Liu-Chen LY, Shen DD: Pharmacokinetics and pharmacodynamics of oral oxycodone in healthy human subjects: role of circulating active metabolites. Clin Pharmacol Ther. 2006 May;79(5):461-79. [PubMed:16678548 ]
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Drug created on June 13, 2005 07:24 / Updated on May 25, 2016 02:17