Identification

Name
Oxymorphone
Accession Number
DB01192  (APRD00158)
Type
Small Molecule
Groups
Approved, 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). 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.

Structure
Thumb
Synonyms
  • (14S)-14-Hydroxydihydromorphinone
  • 14-Hydroxydihydromorphinone
  • Dihydrohydroxymorphinone
  • Dihydroxymorphinone
  • Oximorfona
  • Oximorphonum
  • Oxymorphonum
External IDs
IDS-NO-003 / NIH 10323 / NSC-19045
Product Ingredients
IngredientUNIICASInChI Key
Oxymorphone hydrochloride5Y2EI94NBC357-07-3BCGJBQBWUGVESK-KCTCKCTRSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NumorphanInjection1 mg/1mLParenteralEndo Pharmaceuticals1959-05-142009-07-31Us
NumorphanSuppository5 mg/1RectalEndo Pharmaceuticals1959-05-142009-08-31Us
NumorphanInjection1.5 mg/1mLParenteralEndo Pharmaceuticals1959-05-142009-07-31Us
Numorphan Injection 1.5mg/mlLiquid1.5 mgIntramuscular; Intravenous; SubcutaneousBristol Myers Squibb1993-12-312004-08-04Canada
Numorphan Suppository 5mgSuppository5 mgRectalBristol Myers Squibb1993-12-312002-07-04Canada
OpanaTablet5 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-02-092013-12-31Us
OpanaTablet5 mg/1Oralbryant ranch prepack2006-06-262018-05-29Us
OpanaTablet10 mg/1OralEndo Pharmaceuticals, Inc.2006-06-26Not applicableUs
OpanaTablet10 mg/1OralStat Rx USA2011-12-15Not applicableUs
OpanaInjection1 mg/1mLIntramuscular; Intravenous; SubcutaneousEndo Pharmaceuticals1959-06-012017-08-01Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Oxymorphone hydrochlorideTablet, film coated, extended release15 mg/1OralRanbaxy Inc.2015-04-13Not applicableUs
Oxymorphone hydrochlorideTablet, film coated, extended release20 mg/1OralImpax Generics2013-01-02Not applicableUs
Oxymorphone hydrochlorideTablet, film coated, extended release15 mg/1OralLake Erie Medical DBA Quality Care Products LLC2013-01-02Not applicableUs
Oxymorphone HydrochlorideTablet10 mg/1OralPhysicians Total Care, Inc.2012-12-10Not applicableUs
Oxymorphone HydrochlorideTablet5 mg/1OralCamber Pharmaceuticals Inc2018-03-01Not applicableUs
Oxymorphone hydrochlorideTablet, extended release10 mg/1OralActavis Pharma Company2013-09-132017-12-31Us
Oxymorphone HydrochlorideTablet10 mg/1OralKvk Tech,Inc2013-02-11Not applicableUs
Oxymorphone HydrochlorideTablet5 mg/1OralSpecGx LLC2013-07-23Not applicableUs
Oxymorphone HydrochlorideTablet5 mg/1OralCore Pharma, Llc2015-01-172017-09-30Us
Oxymorphone hydrochlorideTablet, extended release20 mg/1OralActavis Pharma Company2013-09-132017-12-31Us
International/Other Brands
Numorphan / Opana
Categories
UNII
9VXA968E0C
CAS number
76-41-5
Weight
Average: 301.3371
Monoisotopic: 301.131408101
Chemical Formula
C17H19NO4
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

Pharmacology

Indication

For the treatment of moderate-to-severe pain.

Associated Conditions
Associated Therapies
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.

TargetActionsOrganism
AMu-type opioid receptor
agonist
Human
UDelta-type opioid receptor
antagonist
Human
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%).

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
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. 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
PathwayCategory
Oxymorphone Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Oxymorphone.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Oxymorphone.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Oxymorphone is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Oxymorphone is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when Oxymorphone is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Oxymorphone.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when Oxymorphone is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Oxymorphone.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Oxymorphone is combined with 4-Methoxyamphetamine.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Oxymorphone.
Food Interactions
Not Available

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
Not Available
External Links
Human Metabolome Database
HMDB0015323
KEGG Drug
D08323
KEGG Compound
C08019
PubChem Compound
5284604
PubChem Substance
46505296
ChemSpider
4447650
BindingDB
50001707
ChEBI
7865
ChEMBL
CHEMBL963
Therapeutic Targets Database
DAP001138
PharmGKB
PA450748
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Oxymorphone
AHFS Codes
  • 28:08.08 — Opiate Agonists
FDA label
Download (9.95 MB)
MSDS
Download (133 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingSupportive CareMetastatic Malignant Neoplasm / Neoplasms, Malignant / Pain NOS1
1CompletedTreatmentPain NOS3
2RecruitingBasic ScienceOpioid Abuse / Opioid-use Disorder1
3CompletedTreatmentBack Pain Lower Back / Cancers, Pain1
3CompletedTreatmentDisease, Chronic / Pain NOS1
3CompletedTreatmentMalignancies / Pain, Chronic / Pain, Neuropathic1
3CompletedTreatmentPain NOS1
3CompletedTreatmentPain, Acute1
3CompletedTreatmentPain, Chronic2
3CompletedTreatmentPost Operative Pain1
3CompletedTreatmentPost-Operative Pain1
3CompletedTreatmentPostoperative pain1
3RecruitingTreatmentPain, Acute / Post-Operative Pain1
3TerminatedTreatmentPain, Chronic1
3WithdrawnTreatmentPain, Chronic1
4Active Not RecruitingTreatmentNarcotic Abuse / Opiate Addiction / Opioid-Related Disorders / Substance Abuse1
4CompletedBasic ScienceHealthy Volunteers1
4CompletedTreatmentPain, Chronic1
Not AvailableCompletedPreventionPost-Operative Nausea and Vomiting (PONV)1
Not AvailableCompletedTreatmentPain NOS1
Not AvailableUnknown StatusSupportive CareChronic Nociceptive Pain / Non-cancer Pain / Pain, Neuropathic1

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
FormRouteStrength
InjectionParenteral1 mg/1mL
InjectionParenteral1.5 mg/1mL
SuppositoryRectal5 mg/1
LiquidIntramuscular; Intravenous; Subcutaneous1.5 mg
SuppositoryRectal5 mg
InjectionIntramuscular; Intravenous; Subcutaneous1 mg/1mL
TabletOral10 mg/1
TabletOral20 mg/1
Tablet, extended releaseOral10 mg/1
Tablet, extended releaseOral10 mg
Tablet, extended releaseOral15 mg/1
Tablet, extended releaseOral20 mg
Tablet, extended releaseOral20 mg/1
Tablet, extended releaseOral30 mg/1
Tablet, extended releaseOral40 mg/1
Tablet, extended releaseOral40 mg
Tablet, extended releaseOral5 mg/1
Tablet, extended releaseOral5 mg
Tablet, extended releaseOral7.5 mg/1
Tablet, film coated, extended releaseOral10 mg/1
Tablet, film coated, extended releaseOral40 mg/1
Tablet, film coated, extended releaseOral5 mg/1
TabletOral5 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)
US5662933No1997-09-022013-09-09Us
US7276250No2007-10-022023-02-04Us
US8309060No2012-11-132023-11-20Us
US8114383No2012-02-142024-10-10Us
US8808737No2014-08-192027-06-21Us
US8871779No2014-10-282029-11-22Us
US8192722No2012-06-052025-09-15Us
US8075872No2011-12-132023-11-20Us
US7851482No2010-12-142029-07-10Us
US8329216No2012-12-112023-02-04Us
US8309122No2012-11-132023-02-04Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)248-249 °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)10.07ChemAxon
pKa (Strongest Basic)8.21ChemAxon
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0udl-7932000000-89141254d526ca629dac
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

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
Phenanthrene / Isoquinolone / Tetralin / Coumaran / 1-hydroxy-2-unsubstituted benzenoid / Alkyl aryl ether / Aralkylamine / Piperidine / Cyclic alcohol / Tertiary alcohol
show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
morphinane alkaloid (CHEBI:7865)

Targets

Details
1. Mu-type opioid receptor
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...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
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 n...
Gene Name
OPRD1
Uniprot ID
P41143
Uniprot Name
Delta-type opioid receptor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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]

Drug created on June 13, 2005 07:24 / Updated on December 10, 2018 13:39