Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C17H19NO4 |
Molecular Weight | 301.3377 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CC[C@@]23c4c5ccc(c4O[C@@]3([H])C(=O)CC[C@]2([C@@]1([H])C5)O)O
InChI
InChIKey=UQCNKQCJZOAFTQ-ISWURRPUSA-N
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
Molecular Formula | C17H19NO4 |
Molecular Weight | 301.3377 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment:: description was created based on several sources, including:
http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021611lbl.pdf | https://www.drugs.com/pro/oxymorphone.html
Curator's Comment:: description was created based on several sources, including:
http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021611lbl.pdf | https://www.drugs.com/pro/oxymorphone.html
Oxymorphone is an analgesic that is FDA approved for the treatment of moderate to severe pain. It is also indicated for relief of anxiety in patients with dyspnea associated with pulmonary edema secondary to acute left ventricular dysfunction. Oxymorphone (brand names Opana, Numorphan, Numorphone) is a full opioid agonist and is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. Adverse reactions (≥ 2% of patients): seen with the immediate release tablet formulation Nausea, pyrexia, somnolence, vomiting, pruritus, headache, dizziness, constipation, and confusion. Concomitant use with serotonergic drugs may result in serotonin syndrome. Avoid use of mixed agonist/antagonist and partial agonist opioid analgesics with Opana because they may reduce analgesic effect of Opana or precipitate withdrawal symptoms.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
0.93 nM [Ki] | |||
80.5 nM [Ki] | |||
Target ID: CHEMBL237 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24919067 |
61.6 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | OPANA Approved UseEnter section text here - OPANA ER is an opioid agonist indicated for the relief of moderate to severe pain in patients requiring continuous around-the-clock opioid treatment for an extended period of time. (1) - Not intended for use as an as needed analgesic. Not indicated in the immediate post-operative period or if the pain is mild or not expected to persist for an extended period of time. (1), 1 INDICATIONS AND USAGE 1 INDICATIONS AND USAGE OPANA ER is indicated for the relief of moderate to severe pain in patients requiring continuous, around-the-clock opioid treatment for an extended period of time. Limitations of Usage OPANA ER is not intended for use as an as needed analgesic. OPANA ER is not indicated for pain in the immediate post-operative period if the pain is mild, or not expected to persist for an extended period of time. OPANA ER is only indicated for post-operative use if the patient is already receiving the drug prior to surgery or if the post-operative pain is expected to be moderate or severe and persist for an extended period of time. Physicians should individualize treatment, moving from parenteral to oral analgesics as appropriate. (See American Pain Society guidelines). Launch Date-3.39292815E11 |
|||
Palliative | OPANA Approved UseEnter section text here - OPANA ER is an opioid agonist indicated for the relief of moderate to severe pain in patients requiring continuous around-the-clock opioid treatment for an extended period of time. (1) - Not intended for use as an as needed analgesic. Not indicated in the immediate post-operative period or if the pain is mild or not expected to persist for an extended period of time. (1), 1 INDICATIONS AND USAGE 1 INDICATIONS AND USAGE OPANA ER is indicated for the relief of moderate to severe pain in patients requiring continuous, around-the-clock opioid treatment for an extended period of time. Limitations of Usage OPANA ER is not intended for use as an as needed analgesic. OPANA ER is not indicated for pain in the immediate post-operative period if the pain is mild, or not expected to persist for an extended period of time. OPANA ER is only indicated for post-operative use if the patient is already receiving the drug prior to surgery or if the post-operative pain is expected to be moderate or severe and persist for an extended period of time. Physicians should individualize treatment, moving from parenteral to oral analgesics as appropriate. (See American Pain Society guidelines). Launch Date-3.39292815E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.21 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.54 ng/mL |
20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4.47 ng/mL |
40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2.59 ng/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
0.27 ng/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
0.7 ng/mL |
5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
17.81 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
19.28 ng × h/mL |
20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
36.98 ng × h/mL |
40 mg 2 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
37.9 ng × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
4.54 ng × h/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
5.6 ng × h/mL |
5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9.89 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
9.35 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
11.3 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYMORPHONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
20 mg 4 times / day multiple, oral Recommended Dose: 20 mg, 4 times / day Route: oral Route: multiple Dose: 20 mg, 4 times / day Sources: Page: p.97 |
healthy, 27–44 n = 23 Health Status: healthy Age Group: 27–44 Sex: M+F Population Size: 23 Sources: Page: p.97 |
Disc. AE: Vomiting, Nausea... AEs leading to discontinuation/dose reduction: Vomiting (mild, 4.3%) Sources: Page: p.97Nausea (4.3%) Dizziness (4.3%) |
79.4 mg 1 times / day multiple, oral (mean) Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: Page: p.26 |
unhealthy, 45.5-47.5 n = 71 Health Status: unhealthy Condition: Back pain Age Group: 45.5-47.5 Sex: M+F Population Size: 71 Sources: Page: p.26 |
Disc. AE: Abdominal pain, Chest pain... AEs leading to discontinuation/dose reduction: Abdominal pain (1.4%) Sources: Page: p.26Chest pain (1.4%) Serum creatine phosphokinase increased (1.4%) Serum creatine phosphokinase MB increased (1.4%) Back pain (1.4%) |
0.5 mg 5 times / day multiple, intravenous Recommended Dose: 0.5 mg, 5 times / day Route: intravenous Route: multiple Dose: 0.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Disc. AE: Opioid abuse, Respiratory depression... AEs leading to discontinuation/dose reduction: Opioid abuse Sources: Page: p.6Respiratory depression Addiction Hypotension (severe) |
1.5 mg 5 times / day multiple, intramuscular|subcutaneous (max) Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Disc. AE: Opioid abuse, Respiratory depression... AEs leading to discontinuation/dose reduction: Opioid abuse Sources: Page: p.6Respiratory depression Addiction Hypotension (severe) |
20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Disc. AE: Opioid abuse, Addiction... AEs leading to discontinuation/dose reduction: Opioid abuse Sources: Page: p.1Addiction Respiratory depression (grade 3-5) Withdrawal syndrome neonatal Anaphylaxis Hypotension (severe) Angioedema Hypersensitivity reaction Adrenal insufficiency |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dizziness | 4.3% Disc. AE |
20 mg 4 times / day multiple, oral Recommended Dose: 20 mg, 4 times / day Route: oral Route: multiple Dose: 20 mg, 4 times / day Sources: Page: p.97 |
healthy, 27–44 n = 23 Health Status: healthy Age Group: 27–44 Sex: M+F Population Size: 23 Sources: Page: p.97 |
Nausea | 4.3% Disc. AE |
20 mg 4 times / day multiple, oral Recommended Dose: 20 mg, 4 times / day Route: oral Route: multiple Dose: 20 mg, 4 times / day Sources: Page: p.97 |
healthy, 27–44 n = 23 Health Status: healthy Age Group: 27–44 Sex: M+F Population Size: 23 Sources: Page: p.97 |
Vomiting | mild, 4.3% Disc. AE |
20 mg 4 times / day multiple, oral Recommended Dose: 20 mg, 4 times / day Route: oral Route: multiple Dose: 20 mg, 4 times / day Sources: Page: p.97 |
healthy, 27–44 n = 23 Health Status: healthy Age Group: 27–44 Sex: M+F Population Size: 23 Sources: Page: p.97 |
Abdominal pain | 1.4% Disc. AE |
79.4 mg 1 times / day multiple, oral (mean) Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: Page: p.26 |
unhealthy, 45.5-47.5 n = 71 Health Status: unhealthy Condition: Back pain Age Group: 45.5-47.5 Sex: M+F Population Size: 71 Sources: Page: p.26 |
Back pain | 1.4% Disc. AE |
79.4 mg 1 times / day multiple, oral (mean) Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: Page: p.26 |
unhealthy, 45.5-47.5 n = 71 Health Status: unhealthy Condition: Back pain Age Group: 45.5-47.5 Sex: M+F Population Size: 71 Sources: Page: p.26 |
Chest pain | 1.4% Disc. AE |
79.4 mg 1 times / day multiple, oral (mean) Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: Page: p.26 |
unhealthy, 45.5-47.5 n = 71 Health Status: unhealthy Condition: Back pain Age Group: 45.5-47.5 Sex: M+F Population Size: 71 Sources: Page: p.26 |
Serum creatine phosphokinase MB increased | 1.4% Disc. AE |
79.4 mg 1 times / day multiple, oral (mean) Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: Page: p.26 |
unhealthy, 45.5-47.5 n = 71 Health Status: unhealthy Condition: Back pain Age Group: 45.5-47.5 Sex: M+F Population Size: 71 Sources: Page: p.26 |
Serum creatine phosphokinase increased | 1.4% Disc. AE |
79.4 mg 1 times / day multiple, oral (mean) Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: Page: p.26 |
unhealthy, 45.5-47.5 n = 71 Health Status: unhealthy Condition: Back pain Age Group: 45.5-47.5 Sex: M+F Population Size: 71 Sources: Page: p.26 |
Addiction | Disc. AE | 0.5 mg 5 times / day multiple, intravenous Recommended Dose: 0.5 mg, 5 times / day Route: intravenous Route: multiple Dose: 0.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Opioid abuse | Disc. AE | 0.5 mg 5 times / day multiple, intravenous Recommended Dose: 0.5 mg, 5 times / day Route: intravenous Route: multiple Dose: 0.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Respiratory depression | Disc. AE | 0.5 mg 5 times / day multiple, intravenous Recommended Dose: 0.5 mg, 5 times / day Route: intravenous Route: multiple Dose: 0.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Hypotension | severe Disc. AE |
0.5 mg 5 times / day multiple, intravenous Recommended Dose: 0.5 mg, 5 times / day Route: intravenous Route: multiple Dose: 0.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Addiction | Disc. AE | 1.5 mg 5 times / day multiple, intramuscular|subcutaneous (max) Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Opioid abuse | Disc. AE | 1.5 mg 5 times / day multiple, intramuscular|subcutaneous (max) Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Respiratory depression | Disc. AE | 1.5 mg 5 times / day multiple, intramuscular|subcutaneous (max) Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Hypotension | severe Disc. AE |
1.5 mg 5 times / day multiple, intramuscular|subcutaneous (max) Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: Page: p.6 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.6 |
Addiction | Disc. AE | 20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Adrenal insufficiency | Disc. AE | 20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Anaphylaxis | Disc. AE | 20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Angioedema | Disc. AE | 20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Hypersensitivity reaction | Disc. AE | 20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Opioid abuse | Disc. AE | 20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Withdrawal syndrome neonatal | Disc. AE | 20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Respiratory depression | grade 3-5 Disc. AE |
20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
Hypotension | severe Disc. AE |
20 mg 5 times / day multiple, oral (max) Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain Sources: Page: p.1 |
PubMed
Title | Date | PubMed |
---|---|---|
Double-blind, randomized comparison of the analgesic and pharmacokinetic profiles of controlled- and immediate-release oral oxycodone in cancer pain patients. | 2001 May |
|
Capillary electrophoresis and capillary electrophoresis-ion trap multiple-stage mass spectrometry for the differentiation and identification of oxycodone and its major metabolites in human urine. | 2002 Apr 25 |
|
Investigation of 4,5-epoxymorphinan degradation during analysis by HPLC. | 2002 Aug 22 |
|
Clinical pharmacology of opioids for pain. | 2002 Jul-Aug |
|
Synergy between mu opioid ligands: evidence for functional interactions among mu opioid receptor subtypes. | 2002 Nov |
|
Comparison of the effects of buprenorphine, oxymorphone hydrochloride, and ketoprofen for postoperative analgesia after onychectomy or onychectomy and sterilization in cats. | 2002 Nov-Dec |
|
Simultaneous quantitation of opioids in blood by GC-EI-MS analysis following deproteination, detautomerization of keto analytes, solid-phase extraction, and trimethylsilyl derivatization. | 2002 Oct |
|
Oxymorphone--Endo/Penwest: EN 3202, EN 3203. | 2003 |
|
Supraspinal antinociceptive effects of mu and delta agonists involve modulation of adenosine uptake. | 2003 Feb |
|
Quantification of the O- and N-demethylated metabolites of hydrocodone and oxycodone in human liver microsomes using liquid chromatography with ultraviolet absorbance detection. | 2003 Feb 25 |
|
The use of liquid chromatography/mass spectrometry for quantitative analysis of oxycodone, oxymorphone and noroxycodone in Ringer solution, rat plasma and rat brain tissue. | 2004 |
|
Antagonism in opioid peptides: the role of conformation. | 2004 |
|
Cardiopulmonary effects of medetomidine, oxymorphone, or butorphanol in selegiline-treated dogs. | 2004 Apr |
|
Quantitative contribution of CYP2D6 and CYP3A to oxycodone metabolism in human liver and intestinal microsomes. | 2004 Apr |
|
Effects of acepromazine on the incidence of vomiting associated with opioid administration in dogs. | 2004 Jan |
|
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. | 2004 Mar 11 |
|
The efficacy and safety of oral immediate-release oxymorphone for postsurgical pain. | 2004 Nov |
|
Pain management in cats--past, present and future. Part 2. Treatment of pain--clinical pharmacology. | 2004 Oct |
|
Efficacy and safety of oxymorphone extended release in chronic low back pain: results of a randomized, double-blind, placebo- and active-controlled phase III study. | 2005 Jan |
|
Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities. | 2005 May 5 |
|
Oxymorphone extended-release tablets relieve moderate to severe pain and improve physical function in osteoarthritis: results of a randomized, double-blind, placebo- and active-controlled phase III trial. | 2005 Sep-Oct |
|
Comparison of oxycodone pharmacokinetics after buccal and sublingual administration in children. | 2006 |
|
Oxymorphone: a review. | 2006 Feb |
|
Comparison of the in vitro efficacy of mu, delta, kappa and ORL1 receptor agonists and non-selective opioid agonists in dog brain membranes. | 2006 Feb 16 |
|
A synthetic fraction of feline facial pheromones calms but does not reduce struggling in cats before venous catheterization. | 2006 Jul |
|
Opioid analgesics in primary care: challenges and new advances in the management of noncancer pain. | 2006 Mar-Apr |
|
Incomplete recovery of prescription opioids in urine using enzymatic hydrolysis of glucuronide metabolites. | 2006 Oct |
|
Antinociception by spinal and systemic oxycodone: why does the route make a difference? In vitro and in vivo studies in rats. | 2006 Oct |
|
Low-level quantitation of oxycodone and its oxidative metabolites, noroxycodone, and oxymorphone, in rat plasma by high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry. | 2007 Apr 1 |
|
Comment: Oral oxymorphone for pain management. | 2007 Dec |
|
Activation of kappa-opioid receptor as a method for prevention of ischemic and reperfusion arrhythmias: role of protein kinase C and K(ATP) channels. | 2007 Feb |
|
Extended-duration agents for perioperative pain management. | 2007 Feb |
|
A 12-week, randomized, placebo-controlled trial assessing the safety and efficacy of oxymorphone extended release for opioid-naive patients with chronic low back pain. | 2007 Jan |
|
The effect of opiates on the activity of human placental aromatase/CYP19. | 2007 Jan 15 |
|
Absence of conditioned place preference or reinstatement with bivalent ligands containing mu-opioid receptor agonist and delta-opioid receptor antagonist pharmacophores. | 2007 Jul 2 |
|
Oxymorphone hydrochloride, a potent opioid analgesic, is not carcinogenic in rats or mice. | 2007 Mar |
|
Two years follow-up study of the pain-relieving effect of gold bead implantation in dogs with hip-joint arthritis. | 2007 Mar 23 |
|
Use of oral oxymorphone in the elderly. | 2007 May |
|
Requirements and ontology for a G protein-coupled receptor oligomerization knowledge base. | 2007 May 30 |
|
Determination of opioid analgesics in hair samples using liquid chromatography/tandem mass spectrometry and application to patients under palliative care. | 2007 Oct |
|
Method for quantification of opioids and their metabolites in autopsy blood by liquid chromatography-tandem mass spectrometry. | 2007 Sep |
|
Rapid analysis of metabolites and drugs of abuse from urine samples by desorption electrospray ionization-mass spectrometry. | 2007 Sep |
|
Sex differences in the pharmacokinetics, oxidative metabolism and oral bioavailability of oxycodone in the Sprague-Dawley rat. | 2008 Mar |
Sample Use Guides
In Vivo Use Guide
Curator's Comment:: http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021611lbl.pdf
Subcutaneous or Intramuscular administration: Initiate treatment with 1mg to 1.5 mg, every 4 to 6 hours.
Intravenous Administration: 0.5 mg initially
Oral: 10 to 20 mg every four to six hours.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.drugs.com/pro/oxymorphone.html
Oxymorphone hydrochloride was not mutagenic when tested in the in vitro bacterial reverse mutation assay (Ames test) at concentrations of ≤5270 ug/plate, or in an in vitro mammalian cell chromosome aberration assay performed with human peripheral blood lymphocytes at concentrations ≤5000 ug/mL with or without metabolic activation.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Jun 26 02:14:48 UTC 2021
by
admin
on
Sat Jun 26 02:14:48 UTC 2021
|
Record UNII |
9VXA968E0C
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Record Status |
Validated (UNII)
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Record Version |
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-
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NDF-RT |
N0000175690
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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NCI_THESAURUS |
C67413
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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LIVERTOX |
728
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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NDF-RT |
N0000175684
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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NCI_THESAURUS |
C1506
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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FDA ORPHAN DRUG |
6185
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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DEA NO. |
9652
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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Code System | Code | Type | Description | ||
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8060
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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7814
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | RxNorm | ||
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C29314
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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5284604
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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SUB09569MIG
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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1488000
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | USP-RS | ||
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M8338
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | Merck Index | ||
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OXYMORPHONE
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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DB01192
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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200-959-7
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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CHEMBL963
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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76-41-5
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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9VXA968E0C
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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2034
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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Oxymorphone
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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937
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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D010111
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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7094
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY | |||
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76-41-5
Created by
admin on Sat Jun 26 02:14:49 UTC 2021 , Edited by admin on Sat Jun 26 02:14:49 UTC 2021
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PRIMARY |
Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
APPROXIMATE PURE ANHYDROUS DRUG CONTENT (IN PERCENT)
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BINDER->LIGAND |
BINDING
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SALT/SOLVATE -> PARENT |
APPROXIMATE PURE ANHYDROUS DRUG CONTENT (IN PERCENT)
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
6-OH-oxymorphone has been shown in animal studies to have analgesic bioactivity
MAJOR
PLASMA; URINE
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PARENT -> METABOLITE ACTIVE |
Highly variable 40 fold higher potency than Oxycodone
MINOR
PLASMA; URINE
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METABOLITE -> PARENT |
MAJOR
PLASMA
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METABOLITE -> PARENT |
6-OH-oxymorphone has been shown in animal studies to have analgesic bioactivity.
MAJOR
URINE
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Related Record | Type | Details | ||
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Elimination PHARMACOKINETIC PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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