Oxymorphone

OPANA

Open Oxymorphone in the interactive console ↗

Pronunciation: OX-i-mor-foen

Oxymorphone ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Oxymorphone ballicule

Oxymorphone OPANA mascot mnemonic cartoon — Visual mnemonic: Oxymorphone mascot
**“Ox sees more phones”**
pinpoint pupils → opioid

What it isPotent full mu-opioid agonist; severe pain.

Why this oneMinimal CYP metabolism avoids CYP2D6 phenotype variability seen with several other opioids.

What limits itRespiratory depression, dependence, and benzodiazepine co-use drive overdose risk; alcohol can disrupt some extended-release formulations.

Oxymorphone molecular structure (skeletal formula) — Molecular structure: Oxymorphone

FDA-approved for

pain (2006)

FDA label

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BOXED WARNING Addiction, abuse, misuse; life-threatening respiratory depression; neonatal opioid withdrawal syndrome; risks with benzodiazepines/other CNS depressants; interaction with ethanol

FDA dosing	Population	Start	Target	Max
Acute pain (opioid-naive)	Adults	10-20 mg q4-6h PRN	lowest dose for adequate analgesia

Renal Moderate-severe renal impairment: start at lowest dose (increased bioavailability)

Hepatic Contraindicated in moderate-severe hepatic impairment; mild: start at lowest dose

Instructions

Take on empty stomach, at least 1 h before or 2 h after eating
Taper gradually to discontinue in physically dependent patients

Available strengths

tab 5, 10 mg
ER tab 5, 7.5, 10, 15, 20, 30, 40 mg

Contraindications

Significant respiratory depression
Acute or severe bronchial asthma in unmonitored setting or absence of resuscitative equipment
Known or suspected GI obstruction, including paralytic ileus
Moderate or severe hepatic impairment

Cautions

Addiction, abuse, and misuse
Life-threatening respiratory depression
Neonatal opioid withdrawal syndrome
Additive effects with benzodiazepines/CNS depressants
Adrenal insufficiency
Severe hypotension

Adverse reactions

Nausea
Pyrexia
Somnolence
Vomiting
Pruritus
Headache
Dizziness
Constipation
Confusion

Pregnancy Prolonged use during pregnancy may cause neonatal opioid withdrawal syndrome

Lactation Undefined

Cost

Oxymorphone (OPANA)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/unit	CostPlus
5 mg	tab	per unit		not offered
10 mg	tab	per unit	$1.22/ea	not offered

Generic entry2010

⚠ BOXED WARNINGS

Addiction, abuse and misuse
Life-threatening respiratory depression
Risk from concomitant use with benzodiazepines

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger4 / 4

Weight-gain liability0 / 4

Sedation liability2 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityRespiratory depression, dependence and overdose; risk rises sharply with sedatives or impaired clearance.

Serotonicity

This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.

Opioid effects and respiratory/CNS-depressant interactions remain important, but this drug is not a clinically significant SRI by the Gillman framework.

Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.