Identification
- Summary
Oxymorphone is an opioid analgesic used in the management of moderate-to-severe pain and for analgesic therapies.
- Brand Names
- Opana
- Generic Name
- Oxymorphone
- DrugBank Accession Number
- DB01192
- Background
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). On June 8, 2017, FDA requested Endo Pharmaceuticals to remove the medication from the market due to opioid misuse and abuse risks associated with the product's injectable reformulation.
- Type
- Small Molecule
- Groups
- Approved, Investigational, Vet approved
- Structure
Structure for Oxymorphone (DB01192)
- Weight
- Average: 301.3371
Monoisotopic: 301.131408101 - Chemical Formula
- C17H19NO4
- Synonyms
- (14S)-14-Hydroxydihydromorphinone
- 14-Hydroxydihydromorphinone
- Dihydrohydroxymorphinone
- Dihydroxymorphinone
- Oximorfona
- Oximorphonum
- Oxymorphone
- Oxymorphonum
- External IDs
- IDS-NO-003
- NIH 10323
- NSC-19045
Pharmacology
- Indication
For the treatment of moderate-to-severe pain.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Anxiety •••••••••••• ••••••••• Management of Severe pain •••••••••••• •••••••••• ••••••• •••••••• ••••••• Management of Moderate pain •••••••••••• ••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Oxymorphone 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 action
Oxymorphone 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.
Target Actions Organism AMu-type opioid receptor agonistHumans UDelta-type opioid receptor antagonistHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not 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%).
Hover over products below to view reaction partners
- Route of elimination
Oxymorphone 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-life
1.3 (+/-0.7) hours
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Oxymorphone 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. Patients experiencing an overdose may develop apnea, circulatory collapse, and cardiac arrest. Intravenous mouse LD50 is 172 mg/kg.
- Pathways
Pathway Category Oxymorphone Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of adverse effects can be increased when Oxymorphone is combined with 1,2-Benzodiazepine. Abametapir The serum concentration of Oxymorphone can be increased when it is combined with Abametapir. Abatacept The metabolism of Oxymorphone can be increased when combined with Abatacept. Abiraterone The metabolism of Oxymorphone can be decreased when combined with Abiraterone. Acebutolol The metabolism of Oxymorphone can be decreased when combined with Acebutolol. - Food Interactions
- Avoid alcohol. Ingesting alcohol has unpredictable effects on the pharmacokinetics of oxymorphone. Alcohol may also potentiate the CNS depressant effects of oxymorphone.
- Take on an empty stomach. Take oxymorphone at least one hour before or two hours after eating as food may increase the absorption of oxymorphone.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Oxymorphone hydrochloride 5Y2EI94NBC 357-07-3 BCGJBQBWUGVESK-KCTCKCTRSA-N - Product Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Numorphan Injection 1 mg/1mL Parenteral Endo Pharmaceuticals 1959-05-14 2009-07-31 US 
Numorphan Suppository 5 mg/1 Rectal Endo Pharmaceuticals 1959-05-14 2009-08-31 US Numorphan Injection 1.5 mg/1mL Parenteral Endo Pharmaceuticals 1959-05-14 2009-07-31 US Numorphan Injection 1.5mg/ml Liquid 1.5 mg / mL Intramuscular; Intravenous; Subcutaneous Bristol Myers Squibb 1993-12-31 2004-08-04 Canada 
Numorphan Suppository 5mg Suppository 5 mg Rectal Bristol Myers Squibb 1993-12-31 2002-07-04 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Oxymorphone Hydrochloride Tablet 10 mg/1 Oral XLCare Pharmaceuticals, Inc. 2020-05-06 Not applicable US Oxymorphone hydrochloride Tablet, film coated, extended release 5 mg/1 Oral Lake Erie Medical DBA Quality Care Products LLC 2013-01-02 2018-11-02 US Oxymorphone hydrochloride Tablet, film coated, extended release 15 mg/1 Oral Ranbaxy Inc. 2015-04-13 Not applicable US Oxymorphone Hydrochloride Tablet 5 mg/1 Oral Aurolife Pharma, LLC 2016-04-26 Not applicable US Oxymorphone hydrochloride Tablet, film coated, extended release 20 mg/1 Oral Amneal Pharmaceuticals of New York Llc 2013-01-02 Not applicable US
Categories
- ATC Codes
- N02AA11 — Oxymorphone
- Drug Categories
- Adjuvants
- Adjuvants, Anesthesia
- Alkaloids
- Analgesics
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Heterocyclic Compounds, Fused-Ring
- High-risk opioids
- Morphinans
- Morphine Derivatives
- Narcotics
- Natural Opium Alkaloids
- Nervous System
- Opiate Agonists
- Opiate Alkaloids
- Opioid Agonist
- Opioids
- Peripheral Nervous System Agents
- Phenanthrenes
- Sensory System Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenanthrenes and derivatives
- Sub Class
- Not Available
- Direct Parent
- Phenanthrenes and derivatives
- Alternative Parents
- Isoquinolones and derivatives / Tetralins / Coumarans / 1-hydroxy-2-unsubstituted benzenoids / Alkyl aryl ethers / Aralkylamines / Piperidines / Tertiary alcohols / Trialkylamines / 1,2-aminoalcohols show 7 more
- Substituents
- 1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / Alcohol / Alkyl aryl ether / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Carbonyl group / Coumaran show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- morphinane alkaloid (CHEBI:7865)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 9VXA968E0C
- CAS number
- 76-41-5
- InChI Key
- 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[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]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
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 References
- FDA Approved Drug Products: OPANA® ER (oxymorphone hydrochloride) extended-release tablets, for oral use, CII [Link]
- External Links
- Human Metabolome Database
- HMDB0015323
- KEGG Drug
- D08323
- KEGG Compound
- C08019
- PubChem Compound
- 5284604
- PubChem Substance
- 46505296
- ChemSpider
- 4447650
- BindingDB
- 50001707
- 7814
- ChEBI
- 7865
- ChEMBL
- CHEMBL963
- ZINC
- ZINC000003875483
- Therapeutic Targets Database
- DAP001138
- PharmGKB
- PA450748
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Oxymorphone
- FDA label
- Download (9.95 MB)
- MSDS
- Download (133 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Basic Science Healthy Subjects (HS) 1 4 Completed Treatment Chronic Pain 1 4 Terminated Treatment Narcotic Abuse / Opiate Addiction / Opioid Related Disorders / Substance Abuse 1 4 Terminated Treatment Spinal Stenosis of Lumbar Region 1 3 Completed Treatment Acute Pain 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Bristol-Myers Squibb Co.
- DSM Corp.
- Endo Pharmaceuticals Inc.
- Lake Erie Medical and Surgical Supply
- Novartis AG
- Nucare Pharmaceuticals Inc.
- Quality Care
- Stat Rx Usa
- Dosage Forms
Form Route Strength Injection Parenteral 1 mg/1mL Injection Parenteral 1.5 mg/1mL Suppository Rectal 5 mg/1 Liquid Intramuscular; Intravenous; Subcutaneous 1.5 mg / mL Suppository Rectal 5 mg Injection Intramuscular; Intravenous; Subcutaneous 1 mg/1mL Tablet Oral 10 mg/1 Tablet Oral 20 mg/1 Tablet, extended release Oral 10 mg/1 Tablet, extended release Oral 10 mg Tablet, extended release Oral 15 mg/1 Tablet, extended release Oral 20 mg/1 Tablet, extended release Oral 20 mg Tablet, extended release Oral 30 mg/1 Tablet, extended release Oral 40 mg/1 Tablet, extended release Oral 40 mg Tablet, extended release Oral 5 mg Tablet, extended release Oral 5 mg/1 Tablet, extended release Oral 7.5 mg/1 Tablet, film coated, extended release Oral 10 mg/1 Tablet, film coated, extended release Oral 40 mg/1 Tablet, film coated, extended release Oral 5 mg/1 Tablet Oral 5 mg/1 Tablet, film coated, extended release Oral 15 mg/1 Tablet, film coated, extended release Oral 20 mg/1 Tablet, film coated, extended release Oral 30 mg/1 Tablet, film coated, extended release Oral 7.5 mg/1 - Prices
Unit description Cost Unit Opana er 40 mg tablet 21.82USD tablet Opana er 30 mg tablet 17.39USD tablet Opana ER 40 mg 12 Hour tablet 12.42USD tablet Opana er 20 mg tablet 12.12USD tablet Opana ER 30 mg 12 Hour tablet 9.76USD tablet Opana er 15 mg tablet 9.26USD tablet Opana ER 20 mg 12 Hour tablet 7.17USD tablet Opana ER 15 mg 12 Hour tablet 5.82USD tablet Opana er 5 mg tablet 5.53USD tablet Opana ER 10 mg 12 Hour tablet 4.4USD tablet Opana er 10 mg tablet 3.95USD tablet Opana ER 7.5 mg 12 Hour tablet 3.3USD tablet Numorphan 1 mg/ml ampul 3.13USD ml Opana er 7.5 mg tablet 3.0USD tablet Opana ER 5 mg 12 Hour tablet 2.3USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5662933 No 1997-09-02 2013-09-09 US US7276250 No 2007-10-02 2023-02-04 US US8309060 No 2012-11-13 2023-11-20 US US8114383 No 2012-02-14 2024-10-10 US US8808737 No 2014-08-19 2027-06-21 US US8871779 No 2014-10-28 2029-11-22 US US8192722 No 2012-06-05 2025-09-15 US US8075872 No 2011-12-13 2023-11-20 US US7851482 No 2010-12-14 2029-07-10 US US8329216 No 2012-12-11 2023-02-04 US US8309122 No 2012-11-13 2023-02-04 US US8309112 No 2012-11-13 2023-02-04 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 248-249 °C PhysProp water solubility 2.4E+004 mg/L Not Available logP 0.83 HANSCH,C ET AL. (1995) pKa 8.17 SANGSTER (1994) - Predicted Properties
Property Value Source Water Solubility 25.6 mg/mL ALOGPS logP 1.26 ALOGPS logP 0.78 Chemaxon logS -1.1 ALOGPS pKa (Strongest Acidic) 10.07 Chemaxon pKa (Strongest Basic) 8.21 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 70 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 79.56 m3·mol-1 Chemaxon Polarizability 30.77 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9934 Blood Brain Barrier + 0.9382 Caco-2 permeable + 0.7798 P-glycoprotein substrate Substrate 0.9112 P-glycoprotein inhibitor I Non-inhibitor 0.8887 P-glycoprotein inhibitor II Non-inhibitor 0.9734 Renal organic cation transporter Non-inhibitor 0.5585 CYP450 2C9 substrate Non-substrate 0.8014 CYP450 2D6 substrate Substrate 0.8105 CYP450 3A4 substrate Substrate 0.7439 CYP450 1A2 substrate Non-inhibitor 0.8796 CYP450 2C9 inhibitor Non-inhibitor 0.9459 CYP450 2D6 inhibitor Non-inhibitor 0.7168 CYP450 2C19 inhibitor Non-inhibitor 0.8455 CYP450 3A4 inhibitor Non-inhibitor 0.9219 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9812 Ames test Non AMES toxic 0.6663 Carcinogenicity Non-carcinogens 0.9635 Biodegradation Not ready biodegradable 0.9758 Rat acute toxicity 2.9920 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9345 hERG inhibition (predictor II) Non-inhibitor 0.9374
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 171.7636379 predictedDarkChem Lite v0.1.0 [M-H]- 170.2621379 predictedDarkChem Lite v0.1.0 [M-H]- 176.03879 predictedDeepCCS 1.0 (2019) [M-H]- 171.7636379 predictedDarkChem Lite v0.1.0 [M-H]- 170.2621379 predictedDarkChem Lite v0.1.0 [M-H]- 176.03879 predictedDeepCCS 1.0 (2019) [M+H]+ 171.8439379 predictedDarkChem Lite v0.1.0 [M+H]+ 170.8877379 predictedDarkChem Lite v0.1.0 [M+H]+ 178.3968 predictedDeepCCS 1.0 (2019) [M+H]+ 171.8439379 predictedDarkChem Lite v0.1.0 [M+H]+ 170.8877379 predictedDarkChem Lite v0.1.0 [M+H]+ 178.3968 predictedDeepCCS 1.0 (2019) [M+Na]+ 171.7116379 predictedDarkChem Lite v0.1.0 [M+Na]+ 170.3857379 predictedDarkChem Lite v0.1.0 [M+Na]+ 186.22691 predictedDeepCCS 1.0 (2019) [M+Na]+ 171.7116379 predictedDarkChem Lite v0.1.0 [M+Na]+ 170.3857379 predictedDarkChem Lite v0.1.0 [M+Na]+ 186.22691 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- 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...
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- 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 n...
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
References
- 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. [Article]
- 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. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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 react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55