OXYMORPHONE HYDRIODIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C17H20NO4.I
Molecular Weight	429.2495
Optical Activity	UNSPECIFIED
Defined Stereocenters	5 / 5
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[I-].C[N@@H+]1CC[C@]23[C@H]4OC5=C(O)C=CC(C[C@@H]1[C@]2(O)CCC4=O)=C35

InChI

InChIKey=QYUPFWJCSOOVKM-KCTCKCTRSA-N

InChI=1S/C17H19NO4.HI/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;1H/t12-,15+,16+,17-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C17H20NO4
Molecular Weight	302.345
Charge	1
Count

Stereochemistry	EPIMERIC
Additional Stereochemistry	No
Defined Stereocenters	5 / 5
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	I
Molecular Weight	126.90447
Charge	-1
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/011707s036lbl.pdf
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.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Mu opioid receptor 231 Target ID: CHEMBL233 Sources: Sinatra R.S., Jahr J.S., Watkins-Pitchford J.M.. (2010) 'The Essence of Analgesia and Analgesics', p.124 Retrieved from \| https://books.google.ru/books?id=ZwPIjKg0XukC	Agonist 2752	0.93 nM [Ki]
Delta opioid receptor 81 Target ID: CHEMBL236 Sources: Sinatra R.S., Jahr J.S., Watkins-Pitchford J.M.. (2010) 'The Essence of Analgesia and Analgesics', p.124 Retrieved from \| https://books.google.ru/books?id=ZwPIjKg0XukC	Agonist 2752	80.5 nM [Ki]
Kappa opioid receptor 115 Target ID: CHEMBL237 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24919067	Agonist 2752	61.6 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pain 619 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/011707s036lbl.pdf	Palliative		Approved 8583	OPANA Approved Use Enter 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 1959
Anxiety 275 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/011707s036lbl.pdf	Palliative		Approved 8583	OPANA Approved Use Enter 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 1959

C_max

Value	Dose	Analyte	Population
0.27 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
1.21 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
2.59 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
0.7 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
2.54 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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

AUC

Value	Dose	Analyte	Population
4.54 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
17.81 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
37.9 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
5.6 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
19.28 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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

T_1/2

Value	Dose	Analyte	Population
11.3 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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
9.89 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/201655s016lbl.pdf	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

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: https://pubmed.ncbi.nlm.nih.gov/15777102	healthy, 27–44 Health Status: healthy Age Group: 27–44 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15777102	Disc. AE: Vomiting, Nausea... AEs leading to discontinuation/dose reduction: Vomiting (mild, 4.3%) Nausea (4.3%) Dizziness (4.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/15777102
79.4 mg 1 times / day multiple, oral Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15629415	unhealthy, 45.5-47.5 Health Status: unhealthy Age Group: 45.5-47.5 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15629415	Disc. AE: Abdominal pain, Chest pain... AEs leading to discontinuation/dose reduction: Abdominal pain (1.4%) Chest pain (1.4%) Serum creatine phosphokinase increased (1.4%) Serum creatine phosphokinase MB increased (1.4%) Back pain (1.4%) Sources: https://pubmed.ncbi.nlm.nih.gov/15629415
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	Disc. AE: Opioid abuse, Respiratory depression... AEs leading to discontinuation/dose reduction: Opioid abuse Respiratory depression Addiction Hypotension (severe) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
1.5 mg 5 times / day multiple, intramuscular\|subcutaneous Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular\|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	Disc. AE: Opioid abuse, Respiratory depression... AEs leading to discontinuation/dose reduction: Opioid abuse Respiratory depression Addiction Hypotension (severe) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	Disc. AE: Opioid abuse, Addiction... AEs leading to discontinuation/dose reduction: Opioid abuse Addiction Respiratory depression (grade 3-5) Withdrawal syndrome neonatal Anaphylaxis Hypotension (severe) Angioedema Hypersensitivity reaction Adrenal insufficiency Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087	inducer 440

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP 450 20	CYP 450 32

Drug as perpetrator

Target	Modality	Activity
CYP 450 22	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/201655lbl.pdf#page=19 Page: 19.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/201655lbl.pdf#page=11 Page: 11.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/201655lbl.pdf#page=11 Page: 11.0	no

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP 450 32	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/201655lbl.pdf#page=19 Page: 19.0	no

Sourcing

Vendor/Aggregator	ID	URL
AHH Chemical co.,ltd	MT-57608	http://www.ahhchemical.com/product/MT-57608.html
Alsachim	4226	http://www.alsachim.com/product-C5544-glo.bal-view.html
Ambinter	Amb22801505	http://www.ambinter.com/reference/22801505
Aurora Fine Chemicals LLC	A17.921.625	http://online.aurorafinechemicals.com/info?ID=A17.921.625
Avantor Inc	75835-940	https://us.vwr.com/store/product/21998648/exempted-drug-of-abuse-reference-standards-restek
BioCrick	BCC5255	http://www.biocrick.com/Oxymorphone-BCC5255.html
Chem Scene	CS-2852	http://www.chemscene.com/Oxymorphone.html
ChemMol	30105081	http://www.chemmol.com/chemmol/30105081.html
LGC Standards	LGCAMP0673.01-01	https://www.lgcstandards.com/US/en/p/LGCAMP0673.01-01
LGC Standards	LGCAMP0673.01-02	https://www.lgcstandards.com/US/en/p/LGCAMP0673.01-02
MedChem Express	HY-B0618	http://www.medchemexpress.com/Oxymorphone.html
Sigma-Aldrich	O-004_CERILLIAN	https://www.sigmaaldrich.com/catalog/product/cerillian/o004?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S619016	https://www.smolecule.com/products/s619016

PubMed

Title	Date	PubMed
Sex differences in the pharmacokinetics, oxidative metabolism and oral bioavailability of oxycodone in the Sprague-Dawley rat.	2008-03	17973932
Comment: Oral oxymorphone for pain management.	2007-12	17971405
Determination of opioid analgesics in hair samples using liquid chromatography/tandem mass spectrometry and application to patients under palliative care.	2007-10	17898660
Method for quantification of opioids and their metabolites in autopsy blood by liquid chromatography-tandem mass spectrometry.	2007-09	17725888
Rapid analysis of metabolites and drugs of abuse from urine samples by desorption electrospray ionization-mass spectrometry.	2007-09	17710261
GC-MS analysis of multiply derivatized opioids in urine.	2007-08	17567826
Absence of conditioned place preference or reinstatement with bivalent ligands containing mu-opioid receptor agonist and delta-opioid receptor antagonist pharmacophores.	2007-07-02	17383633
Oral extended-release oxymorphone: a new choice for chronic pain relief.	2007-07	17661733
Oral oxymorphone for pain management.	2007-07	17595308
Nociception increases during opioid infusion in opioid receptor triple knock-out mice.	2007-06-29	17544222
Efficacy and tolerability of oxymorphone immediate release for acute postoperative pain after abdominal surgery: a randomized, double-blind, active- and placebo-controlled, parallel-group trial.	2007-06	17692717
Requirements and ontology for a G protein-coupled receptor oligomerization knowledge base.	2007-05-30	17537266
Use of oral oxymorphone in the elderly.	2007-05	17658959
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.	2007-04-01	17098487
Two years follow-up study of the pain-relieving effect of gold bead implantation in dogs with hip-joint arthritis.	2007-03-23	17381835
Local peripheral antinociceptive effects of 14-O-methyloxymorphone derivatives in inflammatory and neuropathic pain in the rat.	2007-03-08	17204264
Oxymorphone hydrochloride, a potent opioid analgesic, is not carcinogenic in rats or mice.	2007-03	17138599
Activation of kappa-opioid receptor as a method for prevention of ischemic and reperfusion arrhythmias: role of protein kinase C and K(ATP) channels.	2007-02	17970197
Extended-duration agents for perioperative pain management.	2007-02	17214919
Effect of naloxone-3-glucuronide and N-methylnaloxone on the motility of the isolated rat colon after morphine.	2007-02	17211696
Efficacy and safety of OPANA ER (oxymorphone extended release) for relief of moderate to severe chronic low back pain in opioid-experienced patients: a 12-week, randomized, double-blind, placebo-controlled study.	2007-02	17145204
Evidence that oxymorphone-induced increases in micronuclei occur secondary to hyperthermia.	2007-02	17077185
The effect of opiates on the activity of human placental aromatase/CYP19.	2007-01-15	17118343
Oral oxymorphone (Opana).	2007-01-01	17179898
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.	2007-01	17257473
New pain management options: drugs.	2007-01	17198138
Incomplete recovery of prescription opioids in urine using enzymatic hydrolysis of glucuronide metabolites.	2006-10	17132254
Antinociception by spinal and systemic oxycodone: why does the route make a difference? In vitro and in vivo studies in rats.	2006-10	17006080
A synthetic fraction of feline facial pheromones calms but does not reduce struggling in cats before venous catheterization.	2006-07	16764591
Controlled clinical trials in cancer pain. How controlled should they be? A qualitative systematic review.	2006-06-05	16705312
Pharmacokinetics and pharmacodynamics of oral oxycodone in healthy human subjects: role of circulating active metabolites.	2006-05	16678548
An automated and fully validated LC-MS/MS procedure for the simultaneous determination of 11 opioids used in palliative care, with 5 of their metabolites.	2006-05	16541404
Predictors of opioid misuse in patients with chronic pain: a prospective cohort study.	2006-04-04	16595013
Opioid receptor-mediated hyperalgesia and antinociceptive tolerance induced by sustained opiate delivery.	2006-03-20	16343768
Opioid analgesics in primary care: challenges and new advances in the management of noncancer pain.	2006-03-04	16513905
A 2-week, multicenter, randomized, double-blind, placebo-controlled, dose-ranging, phase III trial comparing the efficacy of oxymorphone extended release and placebo in adults with pain associated with osteoarthritis of the hip or knee.	2006-03	16750450
Comparison of an automated and point-of-care immunoassay to GC-MS for urine oxycodone testing in the clinical laboratory.	2006-03	16620541
Comparison of the antinociceptive response to morphine and morphine-like compounds in male and female Sprague-Dawley rats.	2006-03	16291875
Comparison of the in vitro efficacy of mu, delta, kappa and ORL1 receptor agonists and non-selective opioid agonists in dog brain membranes.	2006-02-16	16443205
Oxymorphone: a review.	2006-02	16317569
Effects of oxymorphone and hydromorphone on the minimum alveolar concentration of isoflurane in dogs.	2006-01	16412134
Comparison of oxycodone pharmacokinetics after buccal and sublingual administration in children.	2006	16802855
Dissociative anaesthesia during field and hospital conditions for castration of colts.	2006	16722301
Efficacy and safety of oxymorphone immediate release for the treatment of mild to moderate pain after ambulatory orthopedic surgery: results of a randomized, double-blind, placebo-controlled trial.	2005-12	16344024
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.	2005-11-04	16266356
Direct analysis of opiates in urine by liquid chromatography-tandem mass spectrometry.	2005-10	16419404
Evaluation of the DRI oxycodone immunoassay for the detection of oxycodone in urine.	2005-10	16419399
Comparison of the pharmacokinetics of oxycodone and noroxycodone in male dark agouti and Sprague--Dawley rats: influence of streptozotocin-induced diabetes.	2005-09	16132361
Evaluation of induction by use of a combination of oxymorphone and diazepam or hydromorphone and diazepam and maintenance of anesthesia by use of isoflurane in dogs with experimentally induced hypovolemia.	2005-07	16111163
Prevalence of opioid adverse events in chronic non-malignant pain: systematic review of randomised trials of oral opioids.	2005	16207320

Patents

Sample Use Guides

In Vivo Use Guide

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

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 `Wed Apr 02 12:06:48 GMT 2025` Edited by `admin` on `Wed Apr 02 12:06:48 GMT 2025`
Record UNII	SYR9B86WW7
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

MORPHINAN-6-ONE, 4,5-EPOXY-3,14-DIHYDROXY-17-METHYL-, HYDRIODIDE (1:1), (5.ALPHA.)-

Preferred Name

English

OXYMORPHONE HYDRIODIDE

Common Name

English

Code System Code Type Description

FDA UNII

SYR9B86WW7

Created by admin on Wed Apr 02 12:06:48 GMT 2025 , Edited by admin on Wed Apr 02 12:06:48 GMT 2025

PRIMARY

CAS

1188266-21-8

Created by admin on Wed Apr 02 12:06:48 GMT 2025 , Edited by admin on Wed Apr 02 12:06:48 GMT 2025

PRIMARY

PUBCHEM

69271637

Created by admin on Wed Apr 02 12:06:48 GMT 2025 , Edited by admin on Wed Apr 02 12:06:48 GMT 2025

PRIMARY

Related Record Type Details


					9VXA968E0C

OXYMORPHONE

PARENT -> SALT/SOLVATE

Amount:

Related Record Type Details


					9VXA968E0C

OXYMORPHONE

ACTIVE MOIETY

Amount:

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: https://pubmed.ncbi.nlm.nih.gov/15777102	healthy, 27–44 Health Status: healthy Age Group: 27–44 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15777102
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: https://pubmed.ncbi.nlm.nih.gov/15777102	healthy, 27–44 Health Status: healthy Age Group: 27–44 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15777102
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: https://pubmed.ncbi.nlm.nih.gov/15777102	healthy, 27–44 Health Status: healthy Age Group: 27–44 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15777102
Abdominal pain	1.4% Disc. AE	79.4 mg 1 times / day multiple, oral Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15629415	unhealthy, 45.5-47.5 Health Status: unhealthy Age Group: 45.5-47.5 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15629415
Back pain	1.4% Disc. AE	79.4 mg 1 times / day multiple, oral Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15629415	unhealthy, 45.5-47.5 Health Status: unhealthy Age Group: 45.5-47.5 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15629415
Chest pain	1.4% Disc. AE	79.4 mg 1 times / day multiple, oral Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15629415	unhealthy, 45.5-47.5 Health Status: unhealthy Age Group: 45.5-47.5 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15629415
Serum creatine phosphokinase MB increased	1.4% Disc. AE	79.4 mg 1 times / day multiple, oral Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15629415	unhealthy, 45.5-47.5 Health Status: unhealthy Age Group: 45.5-47.5 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15629415
Serum creatine phosphokinase increased	1.4% Disc. AE	79.4 mg 1 times / day multiple, oral Highest studied dose Dose: 79.4 mg, 1 times / day Route: oral Route: multiple Dose: 79.4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15629415	unhealthy, 45.5-47.5 Health Status: unhealthy Age Group: 45.5-47.5 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/15629415
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
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: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
Addiction	Disc. AE	1.5 mg 5 times / day multiple, intramuscular\|subcutaneous Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular\|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
Opioid abuse	Disc. AE	1.5 mg 5 times / day multiple, intramuscular\|subcutaneous Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular\|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
Respiratory depression	Disc. AE	1.5 mg 5 times / day multiple, intramuscular\|subcutaneous Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular\|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
Hypotension	severe Disc. AE	1.5 mg 5 times / day multiple, intramuscular\|subcutaneous Recommended Dose: 1.5 mg, 5 times / day Route: intramuscular\|subcutaneous Route: multiple Dose: 1.5 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011707s031lbl.pdf
Addiction	Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
Adrenal insufficiency	Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
Anaphylaxis	Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
Angioedema	Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
Hypersensitivity reaction	Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
Opioid abuse	Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
Withdrawal syndrome neonatal	Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
Respiratory depression	grade 3-5 Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf
Hypotension	severe Disc. AE	20 mg 5 times / day multiple, oral Recommended Dose: 20 mg, 5 times / day Route: oral Route: multiple Dose: 20 mg, 5 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021611s010lbl.pdf

Details

SMILES

InChI

DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/011707s036lbl.pdfCurator'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

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Approved Use

Launch Date

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/011707s036lbl.pdf
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

C_max

T_1/2

Drug as perpetrator