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21 searches — query, source, results, what was kept and why
| # | source | query | seen | kept | rationale |
|---|---|---|---|---|---|
| 1 | PubMed | oxymorphone pharmacology receptor binding pharmacokinetics | 13 | 6 | Selected studies directly addressing oxymorphone receptor pharmacology and binding |
| 2 | PubMed | get_pubmed_article PMIDs 21215785, 25130052, 19567715 | 3 | 3 | Key papers for receptor binding data and pharmacokinetics |
| 3 | PubMed | oxymorphone extended release Opana abuse deterrent reformulation | 4 | 3 | Key studies on oxymorphone ER reformulation and abuse pattern shifts |
| 4 | PubMed | oxymorphone injection HIV hepatitis C epidemiology | 3 | 3 | Landmark public health articles on the Indiana HIV outbreak linked to oxymorphone injection |
| 5 | PubMed | oxymorphone clinical analgesic pain management | 11 | 3 | Clinical efficacy and comparative analgesic data for oxymorphone |
| 6 | PubMed | oxymorphone human pharmacokinetics bioavailability half-life | 3 | 1 | Key study on oxymorphone ER pharmacokinetics and ethanol interaction |
| 7 | ClinicalTrials.gov | oxymorphone / oxymorphone pain treatment clinical trial | 25 | 5 | Directly relevant oxymorphone clinical trials |
| 8 | PubMed | oxymorphone overdose toxicity case report | 2 | 2 | Both are forensic toxicology case reports documenting fatal oxymorphone exposures |
| 9 | OpenAlex | oxymorphone Opana abuse epidemic clinical | 10 | 3 | Highly cited papers on oxymorphone abuse and its public health consequences |
| 10 | PubMed | oxymorphone abuse dependence addiction opioid use disorder | 9 | 3 | Direct studies of oxymorphone abuse liability and opioid dependence mechanisms |
| 11 | PubChem | oxymorphone | 1 | 1 | Primary chemical identity data for oxymorphone |
| 12 | FDA.gov | oxymorphone Opana ER FDA withdrawal 2017 | 1 | 2 | Authoritative regulatory history for oxymorphone |
| 13 | PubMed | oxymorphone drug interaction CYP enzyme | 4 | 3 | Oxymorphone's unique DDI profile (not metabolized via CYP system) |
| 14 | WebSearch | oxymorphone thrombotic microangiopathy TTP injection abuse | 10 | 4 | Critical safety data for oxymorphone IV abuse; unique and severe hematological complication |
| 15 | WebSearch | oxymorphone pharmacokinetics bioavailability half-life | 10 | 3 | Core pharmacokinetic parameters for oxymorphone |
| 16 | PubMed | oxymorphone osteoarthritis chronic pain RCT | 5 | 4 | Key clinical efficacy data for oxymorphone |
| 17 | WebSearch | oxymorphone legal status UK Canada Australia international scheduling | 10 | 2 | International scheduling data |
| 18 | PubMed | oxymorphone N-substituent pharmacological investigation | 1 | 1 | Key structure-activity relationship data for oxymorphone receptor binding |
| 19 | WebSearch | oxymorphone food effect high fat meal bioavailability | 10 | 1 | Important clinical dosing information for oxymorphone |
| 20 | WebSearch | oxymorphone CAS synthesis history 1914 | 10 | 2 | Chemical and historical identity data |
| 21 | Multiple | Volpe 2011 Ki values for oxymorphone at MOR | 3 | 1 | Key binding affinity data |
102 claims by section — every cited sentence, checked against its source
safety37 · 29 ok
No significant SERT activity was detected for oxymorphonesupported
No significant monoamine transporter or sigma-1 receptor binding. journal.pone.0217371
Relative contraindications based on pharmacological mechanism and clinical evidence: Concurrent alcohol use — pharmacokinetic potentiation (Cmax increase 14–80%) and pharmacodynamic synergysupported
ethanol (20-40%) increased oxymorphone ER Cmax by 14-80% j.jpain.2011.10.011
Claim in safety — inconclusiveinconclusiveworking →
Published postmortem data from fatal cases provide reference blood concentrations: Vorce et al. (2010): oxymorphone 0.13 mg/L combined with alprazolam 0.04 mg/L following insufflation of extended-release tabletssupported
One died (blood: oxymorphone 0.13 mg/L, alprazolam 0.04 mg/L). Cause: multiple drug toxicity. pmid:21819798
Published postmortem data from fatal cases provide reference blood concentrations: Shimomura et al. (2016): oxymorphone 0.106 mg/dL combined with methylone 0.50 mg/dL and ethanol 130 mg/dLsupported
Fatal case with oxymorphone 0.106 mg/dL, methylone 0.50 mg/dL, ethanol 130 mg/dL in peripheral blood. bkw045
A unique and severe hematological complication — thrombotic microangiopathy (TMA) — was documented beginning in 2012 specifically in patients who injected the reformulated (crush-resistant) Opana ER tablets intravenously.supported
3 cases of hemolytic anemia and acute kidney injury (TMA) from IV Opana ER abuse. j.ajkd.2014.01.015
A unique and severe hematological complication — thrombotic microangiopathy (TMA) — was documented beginning in 2012 specifically in patients who injected the reformulated (crush-resistant) Opana ER tablets intravenously.supported
25-year-old male with IV oxymorphone abuse presenting with hemolytic anemia, thrombocytopenia and AKI. pmid:28718268
A unique and severe hematological complication — thrombotic microangiopathy (TMA) — was documented beginning in 2012 specifically in patients who injected the reformulated (crush-resistant) Opana ER tablets intravenously.supported
37-year-old female with 5-year IV Opana ER abuse presenting with AKI and microscopic TMA on biopsy. 2324709618756423
Claim in safety — inconclusiveinconclusiveworking →
Claim in safety — not_supportednot supportedworking →
Kidney biopsy reveals severe arterial and arteriolar mucoid intimal edema with glomerular and tubular ischemiasupported
Kidney biopsy: severe arterial/arteriolar mucoid intimal edema, glomerular/tubular ischemia. j.ajkd.2014.01.015
Additional complications include bilateral exudative retinal detachments.supported
First reported case of bilateral exudative retinal detachments in context of TMA from IV Opana ER abuse. j.ajoc.2018.06.001
Claim in safety — inconclusiveinconclusiveworking →
Outcomes are poor: in the index case series, 2 of 3 patients required plasma exchange, and renal recovery was incompletepartially supported
All required hemodialysis; poor renal recovery. j.ajkd.2014.01.015
Bonnecaze et al. (2018) confirmed that AKI is common with IV oxymorphone ER abuse and that delayed renal recovery correlates with increased KDIGO staging.supported
Retrospective study on prevalence and outcomes of AKI in IV oxymorphone abusers with TMA. nep.13153
Claim in safety — inconclusiveinconclusiveworking →
Controlled human data from Johnstone et al. (1975) demonstrate that intravenous oxymorphone (1.0 mg/70 kg) reduces minute ventilation from 24.9 ± 11.9 to 14.1 ± 4.9 L/min at constant PETCO₂ of 50 torrsupported
15 healthy volunteers received oxymorphone 1.0 mg/70 kg IV. Caused sedation and ventilatory depression (minute ventilation 24.9 to 14.1 L/min). pmid:48348
THC coadministration additively worsened respiratory depression, reducing the CO₂-ventilation slope from 2.23 to 0.88 L/min/torr.supported
THC further decreased ventilation. CO2-ventilation slope decreased from 2.23 to 0.88 L/min/torr. pmid:48348
Claim in safety — inconclusiveinconclusiveworking →
Claim in safety — inconclusiveinconclusiveworking →
Claim in safety — inconclusiveinconclusiveworking →
Gangahar (2015) documented a case of rhabdomyolysis during severe opioid withdrawal, contradicting the common clinical assertion that opioid withdrawal is never life-threatening.supported
Case report demonstrating that opioid withdrawal can be life-threatening, contrary to common clinical belief. ajad.12255
However, when oxymorphone is generated as a metabolite of oxycodone, CYP3A4 inhibitors increase oxymorphone exposure by redirecting oxycodone metabolism through the CYP2D6 pathway.supported
CYP3A4 inhibitor = up to 3.2x oxymorphone exposure. j.ejps.2023.106689
Oxymorphone has high dependence liability consistent with potent MOR full agonism, supported by converging evidence: At 40 mg oral, oxymorphone produces abuse-related subjective ratings (drug liking, euphoria) equivalent to oxycodone 40 mg; Post-OxyContin reformulation surveillance documented a relative risk of oxymorphone ER abuse increase of 2.91 (95% CI 2.59–3.27) versus the pre-ADF period; The Scott County HIV outbreak demonstrates extreme compulsive injection patterns in a community contextsupported
similar abuse-related subjective ratings at 40mg. adb.12173
Oxymorphone has high dependence liability consistent with potent MOR full agonism, supported by converging evidence: At 40 mg oral, oxymorphone produces abuse-related subjective ratings (drug liking, euphoria) equivalent to oxycodone 40 mg; Post-OxyContin reformulation surveillance documented a relative risk of oxymorphone ER abuse increase of 2.91 (95% CI 2.59–3.27) versus the pre-ADF period; The Scott County HIV outbreak demonstrates extreme compulsive injection patterns in a community contextsupported
Post-ADF OxyContin introduction: significantly greater abuse of ER oxymorphone (RR=2.91) observed. pme.12295
Oxymorphone has high dependence liability consistent with potent MOR full agonism, supported by converging evidence: At 40 mg oral, oxymorphone produces abuse-related subjective ratings (drug liking, euphoria) equivalent to oxycodone 40 mg; Post-OxyContin reformulation surveillance documented a relative risk of oxymorphone ER abuse increase of 2.91 (95% CI 2.59–3.27) versus the pre-ADF period; The Scott County HIV outbreak demonstrates extreme compulsive injection patterns in a community contextsupported
181 HIV cases in Scott County, Indiana. 87.8% reported injecting oxymorphone ER. nejmoa1515195
Pharmacogenomic evidence strengthens the mechanistic link: CYP2D6 poor metabolizers — who cannot convert oxycodone to oxymorphone — are significantly underrepresented among oral opioid-dependent individuals, suggesting that oxymorphone formation contributes to the dependence liability of oxycodone itself.supported
CYP2D6 poor metabolizers underrepresented in oral opiate-dependent subjects. CYP2D6 converts oxycodone to oxymorphone; deficient conversion may reduce dependence risk. pmid:9352573
The ethanol interaction is both pharmacokinetic and pharmacodynamic: 20–40% ethanol co-ingestion increases oxymorphone Cmax by 14–80%, while ethanol independently depresses respiratory drivesupported
ethanol (20-40%) increased oxymorphone ER Cmax by 14-80% j.jpain.2011.10.011
Published fatalities involving oxymorphone have consistently involved co-intoxicants — alprazolam and ethanol with methylone.supported
One died (blood: oxymorphone 0.13 mg/L, alprazolam 0.04 mg/L). Cause: multiple drug toxicity. pmid:21819798
Published fatalities involving oxymorphone have consistently involved co-intoxicants — alprazolam and ethanol with methylone.supported
Fatal case with oxymorphone 0.106 mg/dL, methylone 0.50 mg/dL, ethanol 130 mg/dL. bkw045
Johnstone et al. (1975) measured a reduction in CO₂-ventilation slope from 2.23 to 0.88 L/min/torr when escalating THC doses were combined with IV oxymorphone in 15 healthy volunteerssupported
CO2-ventilation slope decreased from 2.23 to 0.88 L/min/torr. pmid:48348
Oxymorphone does not inhibit or induce CYP2C9 or CYP3A4, and no significant monoamine transporter interactions were detected in comprehensive screeningsupported
Oxymorphone ER (high and low dose) did not significantly affect CYP2C9 (tolbutamide) or CYP3A4 (midazolam, EBT) probe metabolism. pmid:15703368
Oxymorphone does not inhibit or induce CYP2C9 or CYP3A4, and no significant monoamine transporter interactions were detected in comprehensive screeningsupported
Confirms oxymorphone metabolism does not involve hepatic CYP system. jmcp.2020.26.5.668
Oxymorphone does not inhibit or induce CYP2C9 or CYP3A4, and no significant monoamine transporter interactions were detected in comprehensive screeningsupported
No significant monoamine transporter or sigma-1 receptor binding. journal.pone.0217371
Relative contraindications based on pharmacological mechanism and clinical evidence: Concurrent benzodiazepine or CNS depressant use — additive respiratory depression; documented in fatal casessupported
Two juvenile females snorted crushed Opana ER plus alprazolam. One died. Cause: multiple drug toxicity. pmid:21819798
No specific PK studies identified; History of substance use disorder — high abuse liability confirmed in human laboratory and surveillance datasupported
similar abuse-related subjective ratings at 40mg. adb.12173
No specific PK studies identified; History of substance use disorder — high abuse liability confirmed in human laboratory and surveillance datasupported
Post-ADF OxyContin introduction: significantly greater abuse of ER oxymorphone (RR=2.91) observed. pme.12295
comparative-pharmacology11 · 9 ok
The most rigorous direct comparison is the within-subject, double-blind, placebo-controlled study by Babalonis et al. (2016), which tested oral oxymorphone (10, 20, 40 mg) against oxycodone (10, 20, 40 mg) in 9 non-dependent opioid-experienced volunteers.supported
Double-blind, placebo-controlled crossover study (n=9 opioid abusers). Compared oral oxymorphone (10, 20, 40mg) vs oxycodone. adb.12173
Key findings: Oxymorphone produced approximately twofold less potent miosis (pupil constriction) than oxycodone at identical doses — an unexpected result given published equianalgesic ratios; Oxymorphone produced lesser magnitude respiratory depression than oxycodone at identical mg-for-mg doses; At 40 mg, oxymorphone was similar to oxycodone 40 mg on abuse-related subjective ratings (drug liking, euphoria); Formal relative potency analyses were largely invalid because oxycodone produced substantially greater effects at the lower doses tested; The investigators concluded that 'oxymorphone is less potent on most pharmacodynamic measures, although at higher doses, its abuse liability is similar to oxycodone'supported
Oxymorphone produced ~twofold less potent miosis and lesser respiratory depression, but similar abuse-related subjective ratings at 40mg. adb.12173
Key findings: Oxymorphone produced approximately twofold less potent miosis (pupil constriction) than oxycodone at identical doses — an unexpected result given published equianalgesic ratios; Oxymorphone produced lesser magnitude respiratory depression than oxycodone at identical mg-for-mg doses; At 40 mg, oxymorphone was similar to oxycodone 40 mg on abuse-related subjective ratings (drug liking, euphoria); Formal relative potency analyses were largely invalid because oxycodone produced substantially greater effects at the lower doses tested; The investigators concluded that 'oxymorphone is less potent on most pharmacodynamic measures, although at higher doses, its abuse liability is similar to oxycodone'supported
Oxymorphone produced ~twofold less potent miosis and lesser respiratory depression, but similar abuse-related subjective ratings at 40mg. adb.12173
Key findings: Oxymorphone produced approximately twofold less potent miosis (pupil constriction) than oxycodone at identical doses — an unexpected result given published equianalgesic ratios; Oxymorphone produced lesser magnitude respiratory depression than oxycodone at identical mg-for-mg doses; At 40 mg, oxymorphone was similar to oxycodone 40 mg on abuse-related subjective ratings (drug liking, euphoria); Formal relative potency analyses were largely invalid because oxycodone produced substantially greater effects at the lower doses tested; The investigators concluded that 'oxymorphone is less potent on most pharmacodynamic measures, although at higher doses, its abuse liability is similar to oxycodone'supported
Oxymorphone produced ~twofold less potent miosis and lesser respiratory depression, but similar abuse-related subjective ratings at 40mg. adb.12173
Key findings: Oxymorphone produced approximately twofold less potent miosis (pupil constriction) than oxycodone at identical doses — an unexpected result given published equianalgesic ratios; Oxymorphone produced lesser magnitude respiratory depression than oxycodone at identical mg-for-mg doses; At 40 mg, oxymorphone was similar to oxycodone 40 mg on abuse-related subjective ratings (drug liking, euphoria); Formal relative potency analyses were largely invalid because oxycodone produced substantially greater effects at the lower doses tested; The investigators concluded that 'oxymorphone is less potent on most pharmacodynamic measures, although at higher doses, its abuse liability is similar to oxycodone'supported
Oxymorphone produced ~twofold less potent miosis and lesser respiratory depression, but similar abuse-related subjective ratings at 40mg. adb.12173
Key findings: Oxymorphone produced approximately twofold less potent miosis (pupil constriction) than oxycodone at identical doses — an unexpected result given published equianalgesic ratios; Oxymorphone produced lesser magnitude respiratory depression than oxycodone at identical mg-for-mg doses; At 40 mg, oxymorphone was similar to oxycodone 40 mg on abuse-related subjective ratings (drug liking, euphoria); Formal relative potency analyses were largely invalid because oxycodone produced substantially greater effects at the lower doses tested; The investigators concluded that 'oxymorphone is less potent on most pharmacodynamic measures, although at higher doses, its abuse liability is similar to oxycodone'supported
Oxymorphone produced ~twofold less potent miosis and lesser respiratory depression, but similar abuse-related subjective ratings at 40mg. adb.12173
Schoedel et al. (2011) compared oxymorphone ER vs. oxycodone CR in recreational opioid users, providing additional subjective effects data consistent with the Babalonis findings.supported
Compared subjective effects of oxymorphone ER vs oxycodone CR in recreational opioid users. pmid:21823549
Claim in comparative-pharmacology — inconclusiveinconclusiveworking →
Claim in comparative-pharmacology — inconclusiveinconclusiveworking →
Oxymorphone differs from oxycodone and most other clinical opioids in three pharmacokinetically significant ways: oral bioavailability ~10% (vs. ~60–87% for oxycodone, ~30% for morphine); CYP independence: metabolism via UGT2B7 glucuronidation rather than CYP enzymes; protein binding: 10–12% (vs. ~45% for oxycodone, ~35% for morphine)supported
Confirms oxymorphone metabolism does not involve hepatic CYP system. jmcp.2020.26.5.668
These pharmacokinetic distinctions carry clinical implications: the CYP independence reduces drug-drug interaction risk in polypharmacy populations, while the low oral bioavailability and low protein binding produce a pharmacokinetic profile that is unusually sensitive to food and ethanol co-ingestion.supported
ethanol (20-40%) increased oxymorphone ER Cmax by 14-80% j.jpain.2011.10.011
pharmacology11 · 4 ok
Critically, oxymorphone does not undergo hepatic CYP450 metabolism, distinguishing it from nearly all other clinical opioids and conferring minimal CYP-mediated drug-drug interaction risk.supported
Confirms oxymorphone metabolism does not involve hepatic CYP system. jmcp.2020.26.5.668
Claim in pharmacology — inconclusiveinconclusiveworking →
PBPK modeling confirms oxymorphone has 40–60-fold higher MOR affinity than its parent compound oxycodone.supported
Oxymorphone has 40-60x higher mu-opioid receptor affinity than parent oxycodone. j.ejps.2023.106689
Claim in pharmacology — inconclusiveinconclusiveworking →
Comprehensive multi-target pharmacological screening across 9 pain-relevant receptor systems identifies oxymorphone as the most MOR-selective clinical opioid tested, with no significant activity at delta (DOR), kappa (KOR), or nociceptin (NOP) opioid receptors, sigma-1 receptors, cannabinoid CB1 receptors, or monoamine transporters (NET, SERT, DAT).supported
Screened 9 clinically relevant opioids against 9 pain-related receptor targets. Found oxymorphone to be most MOR-selective drug tested. No significant monoamine transporter or sigma-1 receptor binding. journal.pone.0217371
Oxymorphone has an oral bioavailability of approximately 10% due to extensive first-pass hepatic metabolism — substantially lower than most other clinical opioidssupported
oral bioavailability ~10% pmid:19209260
Claim in pharmacology — inconclusiveinconclusiveworking →
Claim in pharmacology — inconclusiveinconclusiveworking →
Claim in pharmacology — inconclusiveinconclusiveworking →
Claim in pharmacology — inconclusiveinconclusiveworking →
Claim in pharmacology — inconclusiveinconclusiveworking →
summary11 · 8 ok
Claim in summary — inconclusiveinconclusiveworking →
Oral immediate-release formulations produce analgesia lasting 4–6 hours with onset at 20–45 minutes; extended-release formulations extend duration to approximately 12 hours.supported
oral bioavailability ~10%; duration 4-6h (IR), 12h (ER). pmid:19209260
The 2012 reformulation of Opana ER with a crush-resistant matrix precipitated a public health crisis: the 2014–2015 Scott County, Indiana HIV outbreak — 181 confirmed cases in a population of 4,200, the largest rural HIV outbreak in US history — was directly attributable to injection abuse of the reformulated tabletssupported
181 HIV cases in Scott County, Indiana. 87.8% reported injecting oxymorphone ER. nejmoa1515195
Comprehensive multi-target screening identifies oxymorphone as the most MOR-selective clinical opioid tested to date, with no significant activity at delta, kappa, or nociceptin opioid receptors, sigma-1 receptors, or monoamine transporterssupported
Found oxymorphone to be most MOR-selective drug tested. No significant monoamine transporter or sigma-1 receptor binding. journal.pone.0217371
Claim in summary — inconclusiveinconclusiveworking →
The C-6 carbonyl group distinguishing oxymorphone from morphine enhances both MOR affinity and agonist potency in vitro and in vivo.supported
Carbonyl at C-6 (oxymorphone vs morphine) enhances MOP affinity and agonist potency. journal.pone.0099231
Claim in summary — inconclusiveinconclusiveworking →
Oxymorphone carries high acute toxicity with a narrow therapeutic index; fatal respiratory depression has occurred at blood concentrations as low as 0.13 mg/L in polydrug contextssupported
One died (blood: oxymorphone 0.13 mg/L, alprazolam 0.04 mg/L). Cause: multiple drug toxicity. pmid:21819798
Intravenous abuse of the reformulated extended-release tablets produces thrombotic microangiopathy — a unique complication attributable to the polyethylene oxide excipient rather than oxymorphone itselfpartially supported
3 cases of hemolytic anemia and acute kidney injury (TMA) from IV Opana ER abuse. j.ajkd.2014.01.015
Oral bioavailability is approximately 10%, but food and ethanol co-ingestion increase peak plasma concentrations by approximately 38% and 14–80% respectively — a pharmacokinetic vulnerability with direct harm reduction implicationspartially supported
oral bioavailability ~10% pmid:19209260
Oral bioavailability is approximately 10%, but food and ethanol co-ingestion increase peak plasma concentrations by approximately 38% and 14–80% respectively — a pharmacokinetic vulnerability with direct harm reduction implicationspartially supported
ethanol (20-40%) increased oxymorphone ER Cmax by 14-80% j.jpain.2011.10.011
history9 · 8 ok
Phase III trials demonstrated efficacy in postsurgical pain and osteoarthritis, with a systematic review of six controlled studies (n = 1,489) confirming superiority over placebo at daily doses of 40–100 mg.supported
Phase III RCT of oxymorphone ER for osteoarthritis pain. 12h dosing with low peak-to-trough fluctuation. pmid:16750450
Phase III trials demonstrated efficacy in postsurgical pain and osteoarthritis, with a systematic review of six controlled studies (n = 1,489) confirming superiority over placebo at daily doses of 40–100 mg.supported
Oxymorphone IR 10, 20, 30 mg superior to placebo for 8h pain relief (p<0.05). 01.ane.0000132548.91622.b3
Phase III trials demonstrated efficacy in postsurgical pain and osteoarthritis, with a systematic review of six controlled studies (n = 1,489) confirming superiority over placebo at daily doses of 40–100 mg.supported
Phase III RCT of oxymorphone ER vs placebo and active control for chronic osteoarthritis pain. Significant pain relief and functional improvement. pmid:16266356
Phase III trials demonstrated efficacy in postsurgical pain and osteoarthritis, with a systematic review of six controlled studies (n = 1,489) confirming superiority over placebo at daily doses of 40–100 mg.supported
6 controlled studies (n=1489). Oxymorphone 40-100 mg/day superior to placebo. j.jpainsymman.2009.07.010
After OxyContin (oxycodone ER) was reformulated with abuse-deterrent properties in 2010, surveillance data documented a relative risk of abuse increase of 2.91 (95% CI 2.59–3.27) for oxymorphone ER compared with the pre-ADF period, as users migrated from the newly tamper-resistant oxycodone formulation.supported
Post-ADF OxyContin introduction: significantly greater abuse of ER oxymorphone (RR=2.91) observed. Injection, snorting, and oral oxymorphone abuse all increased. pme.12295
Claim in history — not_supportednot supportedworking →
Between late 2014 and 2015, Scott County, Indiana (population approximately 4,200) experienced 181 confirmed HIV cases linked to injection of dissolved Opana ER tablets — the largest rural HIV outbreak in US historypartially supported
135 HIV cases in small Indiana community of 4,200 linked to oxymorphone injection by April 2015. pmid:25928470
A public health emergency was declared in March 2015, and Indiana established its first statewide syringe service program in responsesupported
Public health emergency declared March 2015. First statewide syringe service program established. nejmoa1515195
Separately, clinicians documented a previously unrecognized syndrome — thrombotic microangiopathy (TMA) with acute kidney injury — in patients who injected the reformulated tablets, attributable to the PEO excipient rather than oxymorphone itself.partially supported
3 cases of hemolytic anemia and acute kidney injury (TMA) from IV Opana ER abuse. j.ajkd.2014.01.015
pharmacokinetic-detail9 · 7 ok
Single- and multiple-dose pharmacokinetic studies demonstrate dose proportionality for immediate-release oxymorphone across the 5–20 mg range, with linear increases in Cmax and AUC.supported
Studied pharmacokinetics of new oxymorphone IR tablet formulation and metabolites in healthy volunteers. Documents dose-proportional PK. pmid:15777102
Tyndale et al. (1997) demonstrated that CYP2D6 poor metabolizers are underrepresented in oral opioid-dependent populations, suggesting that oxymorphone formation contributes to the dependence liability of oxycodone.supported
CYP2D6 poor metabolizers underrepresented in oral opiate-dependent subjects. CYP2D6 converts oxycodone to oxymorphone; deficient conversion may reduce dependence risk. pmid:9352573
Values from published clinical pharmacokinetic reviews.supported
Review of oxymorphone pharmacology, clinical trials. pmid:19209260
Values from published clinical pharmacokinetic reviews.supported
Studied pharmacokinetics of new oxymorphone IR tablet formulation and metabolites in healthy volunteers. pmid:15777102
Oxymorphone's metabolic pathway is atypical among clinical opioids in that it does not involve the hepatic cytochrome P450 (CYP) enzyme system.supported
Confirms oxymorphone metabolism does not involve hepatic CYP system. jmcp.2020.26.5.668
Claim in pharmacokinetic-detail — inconclusiveinconclusiveworking →
Claim in pharmacokinetic-detail — inconclusiveinconclusiveworking →
A 14-day randomized study confirmed that oxymorphone ER does not significantly affect CYP2C9 or CYP3A4 metabolic activities, in contrast to the strong CYP inducer rifampin used as a positive controlsupported
Two 14-day RCTs in healthy subjects. Oxymorphone ER did not significantly affect CYP2C9 or CYP3A4 probe metabolism. Rifampin did. pmid:15703368
PBPK modeling demonstrates that oxymorphone exposure from oxycodone administration varies up to 55-fold depending on CYP2D6 and UGT2B7 phenotype and concurrent CYP3A4 inhibitor usesupported
55-fold range in exposure. CYP2D6 UM + UGT2B7 mutation = 2.3x oxymorphone exposure. CYP3A4 inhibitor = up to 3.2x oxymorphone exposure. j.ejps.2023.106689
clinical-evidence4 · 4 ok
All three doses were superior to placebo over 8 hours, with significant analgesic onset by 45 minutes at the 20 and 30 mg doses.supported
Oxymorphone IR 10, 20, 30 mg superior to placebo for 8h pain relief (p<0.05). Significant pain reduction by 45 min (20-30 mg). 01.ane.0000132548.91622.b3
Aqua et al. (2007) evaluated oxymorphone IR in a randomized, double-blind, active- and placebo-controlled trial for acute pain following abdominal surgery, confirming both efficacy and tolerability.supported
RCT of oxymorphone IR for postoperative pain after abdominal surgery. pmid:17692717
Two Phase III trials demonstrated efficacy of oxymorphone ER in osteoarthritis of the hip or knee: Kivitz et al. (2006): a 2-week, multicenter, dose-ranging trial confirming superiority over placebo; Matsumoto et al. (2005): a randomized, double-blind trial demonstrating significant improvement in pain and physical function compared with placebo, with efficacy comparable to the active control oxycodone CRsupported
Phase III RCT of oxymorphone ER vs placebo and active control for chronic osteoarthritis pain. Significant pain relief and functional improvement. pmid:16266356
Migliorini et al. (2021) included oxymorphone in a Bayesian network meta-analysis of opioids for chronic low back pain, providing comparative effectiveness data within the broader opioid landscape.supported
NMA of RCTs: oxymorphone, tapentadol, and fentanyl showed highest efficacy in chronic low back pain. Data from 2933 patients. 17512433.2021.1903316
chemistry3 · 1 ok
The C-6 carbonyl enhances mu opioid receptor affinity and agonist potency relative to morphine.supported
Carbonyl at C-6 (oxymorphone vs morphine) enhances MOP affinity and agonist potency. journal.pone.0099231
Claim in chemistry — inconclusiveinconclusiveworking →
Claim in chemistry — inconclusiveinconclusiveworking →
neuroscience3 · 1 ok
Claim in neuroscience — inconclusiveinconclusiveworking →
The high MOR selectivity of oxymorphone suggests that its reward signal is mediated almost exclusively through this MOR-dependent dopaminergic mechanism, without the kappa-mediated dysphoric modulation seen in mixed agonist-antagonists or the monoamine transporter effects of drugs such as tramadol.supported
Found oxymorphone to be most MOR-selective drug tested. No significant monoamine transporter or sigma-1 receptor binding. journal.pone.0217371
Claim in neuroscience — inconclusiveinconclusiveworking →
receptor-pharmacology3 · 2 ok
Claim in receptor-pharmacology — inconclusiveinconclusiveworking →
Olson et al. (2019) performed the most comprehensive multi-target screening of clinical opioids to date, testing oxymorphone against 9 pain-relevant molecular targets: MOR, DOR, KOR, NOP receptor, CB1 receptor, sigma-1 receptor, NET, SERT, and DATsupported
Screened 9 clinically relevant opioids against 9 pain-related receptor targets. journal.pone.0217371
PBPK modeling by Klose et al. (2024) quantifies oxymorphone's MOR affinity at 40–60-fold higher than the parent compound oxycodone, establishing that even low plasma concentrations of oxymorphone (produced as a metabolite of oxycodone via CYP2D6) are pharmacologically significant.supported
Oxymorphone has 40-60x higher mu-opioid receptor affinity than parent oxycodone. j.ejps.2023.106689
effects-overview1 · 1 ok
Relative to oxycodone, oxymorphone produces less potent miosis and respiratory depression at identical milligram doses but comparable drug liking and euphoria at higher dosessupported
Oxymorphone produced ~twofold less potent miosis and lesser respiratory depression, but similar abuse-related subjective ratings at 40mg. adb.12173