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Oxymorphone

Oxymorphone molecule structureOxymorphone molecule structure
(4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one
Opana, Numorphan, Stop Signs
Psychoactive Class
Chemical Class
Morphinan

Oxymorphone is a semi-synthetic opioid analgesic of the morphinan class, structurally related to morphine and heroin.citation needed First developed in Germany in 1914 and introduced to the American market in 1959, it was designed to produce fewer side effects than its predecessors. Oxymorphone is approximately seven times more potent than morphine and is used in the management of moderate to severe pain. Notably, it is almost entirely devoid of antitussive properties.

Dosage & Duration

Dosage

Doses are population estimates that vary widely between individuals.

Threshold~2.5 mg
Light2.5-10 mg
Moderate10-20 mg
Strong20-30 mg
Heavy30+ mg
Bioavailability
10%

Duration

Onset20-45 minutes
After Effects1-12 hours
Total4-6 hours
Half-life
1.3 hours (±0.7)

Subjective Effects

Legacy content. A statistically backed ontology from Mindstate Design Labs is coming soon.

The experience is dominated by classic opioid effects: potent pain relief, sedation, and a warm sense of physical and emotional well-being. As a full mu-opioid agonist considerably more potent than morphine, oxymorphone produces a heavy, relaxed state with pronounced euphoria and mood lift, accompanied by little in the way of sensory alteration. Central nervous system depression scales with dose, progressing from drowsiness toward stupor, with respiratory depression as the principal danger at high doses.

Physical

The body feels heavy, relaxed, and free of pain. Side effects typical of opioids are common, including itchiness, constipation, dry mouth, nausea, dizziness, sweating, and constricted pupils; respiratory depression becomes dangerous at higher doses.

Comfortable

Sedation

Uncomfortable

DizzinessConstipationDry mouthIncreased perspiration

Cognitive

The headspace is characterized by euphoria, an elevated mood, and a pervasive sense of well-being and contentment, set against a background of increasing sedation and drowsiness.

Emotional

Reagent Testing

Expected colorimetric results for common reagent tests. Colors show reaction change over 1–2 minutes.

Marquis(MQ)
white → purple2 → purple2
Mecke(ME)
white → yellow2 → brown2
Mandelin(MD)
yellow2 → black3
Froe(FR)
white → blue2 → purple2
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Pharmacology

Pharmacodynamics

Oxymorphone exerts its primary effects through agonism of the μ-opioid receptor.1 It also interacts with the δ-opioid receptor and, to a much lesser extent, the κ-opioid receptor. The nature of its δ-opioid interaction is not fully agreed upon: it has been characterized as antagonism, but has also been described as an activating interaction that may augment its μ-opioid effects. Through μ-opioid receptors on GABAergic interneurons, oxymorphone disinhibits descending pain modulation pathways. It is approximately 10 times more potent than morphine, with 1 mg of oxymorphone hydrochloride considered equivalent to approximately 9.85 mg of morphine sulfate.citation needed

Pharmacokinetics

Oxymorphone undergoes extensive hepatic metabolism.1 Oral bioavailability is notably low at approximately 10%, attributable to substantial first-pass metabolism,citation needed though co-administration with a large fatty meal can increase it to approximately 40%. The primary metabolic pathway involves conjugation, with the oxymorphone conjugate accounting for the majority of urinary metabolites.2 Additional metabolism occurs via 6-keto reduction, yielding 6β-carbinol and 6α-carbinol derivatives that are subsequently conjugated.citation needed The elimination half-life is approximately 1.3 hours.2

Interactions

Dangerous

Highest risk

These combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.

AlcoholBenzodiazepinesCocaineDXMGHB/GBLKetamineMXEPregabalinTramadol

Unsafe

Avoid

There is considerable risk of physical harm when taking these combinations, they should be avoided where possible.

Caution

Use caution

These combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.

AmphetaminesMAOIsMephedroneNitrous oxidePCP
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Tolerance

Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.

Full Tolerance
Sustained repeated oxymorphone use can produce tolerance to many effects, including therapeutic effects. Tolerance develops at different rates across effects, with constipation-related tolerance emerging especially slowly compared with other opioid effects.
Cross Tolerance

All other opioids

Harm Potential

Addiction & Dependence

Psychological

Extremely High

Oxymorphone is considered extremely addictive with high abuse potential.citation needed Compulsive redosing is commonly reported, and the drug has been classified as a high-risk opioid due to misuse and abuse concerns.

Physical

High

Chronic use reliably produces physical dependence with withdrawal symptoms occurring upon cessation.citation needed Neonatal withdrawal syndrome can occur in infants born to mothers who used oxymorphone during pregnancy.

Toxicity

Respiratory

Heavy doses can cause respiratory depression leading to dangerous or fatal levels of oxygen deprivation; this is the primary mechanism of opioid overdose death and risk increases substantially when combined with other depressants.citation needed

Gastrointestinal

Constipation occurs commonly with use and tolerance to this effect develops particularly slowly compared to other opioid effects.citation needed

Cardiovascular

Severe overdose may cause bradycardia, hypotension, circulatory collapse, and cardiac arrest.3

Hematological

Intravenous injection of the reformulated oral tablet has been associated with a rare TTP-like syndrome (thrombotic microangiopathy); this appears specific to abuse of the crush-resistant formulation and does not occur with intended routes of administration.citation needed

History & Culture

Discovery and Development

Oxymorphone was first developed in Germany in 1914citation needed as part of efforts to create opioid analgesics with improved side effect profiles compared to morphine and heroin. The compound exhibits actions and uses similar to morphine, though notably lacks cough suppressant activity.

Legality

International

Oxymorphone is internationally scheduled in Schedule I of the 1961 Single Convention on Narcotic Drugs. It is not listed in the schedules to the 1971 Convention on Psychotropic Substances or in the tables to the 1988 Convention against Illicit Traffic.

By Country

Illegal1
Russia flagRussiaIllegal
Controlled / restricted1
Germany flagGermanyRestricted
Prescription17
United States flagUnited StatesPrescription only
Argentina flagArgentinaPrescription only
Brazil flagBrazilPrescription only
Canada flagCanadaPrescription only
Indonesia flagIndonesiaPrescription only
Ireland flagIrelandPrescription only
Italy flagItalyPrescription only
Japan flagJapanPrescription only
New Zealand flagNew ZealandPrescription only
Philippines flagPhilippinesPrescription only
Singapore flagSingaporePrescription only
South Africa flagSouth AfricaPrescription only
Sweden flagSwedenPrescription only
Switzerland flagSwitzerlandPrescription only
Turkey flagTurkeyPrescription only
United Arab Emirates flagUnited Arab EmiratesPrescription only
United Kingdom flagUnited KingdomPrescription only

References

Source Pages

  1. DrugBank
  2. Erowid
  3. Erowid: Oxymorphone Vault
  4. Isomer Design (TiHKAL/PiHKAL)
  5. PsychonautWiki
  6. TripSit Factsheet: Oxymorphone
  7. TripSit Factsheets
  8. TripSit Wiki
  9. Wikipedia

Citations

  1. OPANA (oxymorphone hydrochloride) tablets prescribing information. Endo Pharmaceuticals / DailyMed (n.d.). https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=285e60f8-2404-47d0-a171-a4f075d6f41812
  2. Numorphan (oxymorphone) prescribing information. Endo Pharmaceuticals / RxList (n.d.). https://www.rxlist.com/numorphan-drug.htm12345
  3. Oxymorphone Hydrochloride Tablets — Full Prescribing Information. DailyMed / U.S. National Library of Medicine (n.d.). https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=560e9425-dfcb-4fb4-a759-b1e3f8f40fdb12
  4. Thrombotic Thrombocytopenic Purpura (TTP)–Like Illness Associated with Intravenous Opana ER Abuse — Tennessee, 2012. Morbidity and Mortality Weekly Report, 62(1), 1–4 (January 11, 2013). https://www.cdc.gov/mmwr/preview/mmwrhtml/mm6201a1.htm1
  5. U.S. Food and Drug Administration. (8 June 2017). FDA Requests Removal of Opana ER for Risks Related to Abuse. https://www.hiv.gov/blog/fda-requests-removal-opana-er-risks-related-abuse123
  6. CDC. (11 January 2013). Thrombotic Thrombocytopenic Purpura (TTP)–Like Illness Associated with Intravenous Opana ER Abuse — Tennessee, 2012. MMWR Morbidity and Mortality Weekly Report, 62(1), 1–4. https://pmc.ncbi.nlm.nih.gov/articles/PMC4604918/1
  7. Ley N.º 17.818 (Estupefacientes). servicios.infoleg.gob.ar (n.d.). https://servicios.infoleg.gob.ar/infolegInternet/anexos/20000-24999/20883/texact.htm1
  8. Ley N.º 17.818 (Estupefacientes). servicios.infoleg.gob.ar (n.d.). https://servicios.infoleg.gob.ar/infolegInternet/anexos/305000-309999/306114/norma.htm1
  9. Portaria SVS/MS nº 344/1998, Lista A1. bvsms.saude.gov.br (n.d.). https://bvsms.saude.gov.br/bvs/saudelegis/svs/1998/prt0344_12_05_1998_rep.html1
  10. Controlled Drugs and Substances Act, Schedule I. laws-lois.justice.gc.ca (n.d.). https://laws-lois.justice.gc.ca/eng/acts/C-38.8/FullText.html1

Further Reading

  1. NIST Chemistry WebBook: Oxymorphone
  2. Olson et al. 2019 - Comprehensive molecular pharmacology screening reveals potential new receptor interactions for clinically relevant opioids

Article Status

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Recent changes8 human edits · latest

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16 August 2026

  1. Lyrea · Changed a word in Dosage & DurationRoutes 1 › Dose ranges › Light

24 January 2026

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