Oxycodone

oxycodone IR

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Pronunciation: ox-i-KOE-doen

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

Oxycodone ROXICODONE / OXYCONTIN mascot mnemonic cartoon — Visual mnemonic: Oxycodone mascot
**“Perky Ox coding”**

What it isFull mu-opioid receptor agonist; moderate to severe pain.

Why this oneCYP2D6 affects only a minor pathway, so analgesia is less genotype-dependent than with codeine or tramadol.

What limits itRespiratory depression, constipation, tolerance and dependence follow sustained use; benzodiazepines sharply increase overdose risk.

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

FDA-approved for

pain (1950)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion (fatal in children); risks from concomitant benzodiazepines/other CNS depressants; neonatal opioid withdrawal syndrome; Opioid Analgesic REMS; CYP3A4 interaction (inhibitors or inducer discontinuation raise oxycodone levels)

FDA dosing	Population	Start	Target	Max
Pain severe enough to require an opioid analgesic, alternatives inadequate (as first opioid)	Adults (opioid-naïve)	5–15 mg q4–6h PRN	lowest dose providing adequate analgesia	no stated ceiling — titrate balancing analgesia vs adverse reactions

Renal Initiate at lower than usual dosage and titrate carefully (clearance may decrease); monitor for respiratory depression, sedation, hypotension

Hepatic Initiate at lower than usual dosage and titrate carefully (extensively hepatically metabolized); monitor for respiratory depression, sedation, hypotension

Instructions

Use lowest effective dosage for shortest duration; many acute pain conditions need no more than a few days
Converting from other opioids: use conservative estimates — safer to underestimate the 24-h dose
Do not rapidly reduce or abruptly discontinue in physically dependent patients (risk of withdrawal, uncontrolled pain, suicide) — taper gradually
Discuss access to an opioid overdose reversal agent (naloxone/nalmefene) when initiating and renewing
Elderly: start at low end of dosing range (greater sensitivity, decreased organ function)

Available strengths

tab 5, 10, 15, 20, 30 mg

Contraindications

Significant respiratory depression
Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment, or hypercarbia
Known or suspected gastrointestinal obstruction, including paralytic ileus

Cautions

Addiction, abuse, and misuse — can occur at recommended dosages; assess risk before prescribing and reassess regularly
Life-threatening respiratory depression, especially at initiation and after dose increases; heightened risk in chronic pulmonary disease and elderly, cachectic, or debilitated patients
Profound sedation, respiratory depression, coma, death with benzodiazepines or other CNS depressants (incl. alcohol)
Neonatal opioid withdrawal syndrome with extended use in pregnancy
Opioid-induced hyperalgesia and allodynia — consider dose reduction or rotation
Adrenal insufficiency; severe hypotension (avoid in circulatory shock)
Avoid in impaired consciousness/coma; caution with increased ICP, brain tumors, head injury
Seizures — may increase frequency in seizure disorders
Withdrawal on rapid discontinuation in physically dependent patients

Adverse reactions

Nausea
Constipation
Vomiting
Headache
Pruritus
Insomnia
Dizziness
Asthenia
Somnolence

Pregnancy Extended use during pregnancy can cause neonatal opioid withdrawal syndrome (may be life-threatening); insufficient data on birth defects/miscarriage

Lactation Present in breastmilk (milk:plasma ~3.2); IR doses <60 mg/day unlikely to give clinically relevant infant exposure; monitor breastfed infants for excess sedation and respiratory depression

Cost

Oxycodone (OXYCODONE IR)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/unit	CostPlus
5 mg	tab	per unit	$0.09/ea	not offered
10 mg	tab	per unit	$0.16/ea	not offered
15 mg	tab	per unit	$0.20/ea	not offered
20 mg	tab	per unit	$0.25/ea	not offered
30 mg	tab	per unit	$0.36/ea	not offered

Other forms: Oxycodone CR (OXYCONTIN)

Available combined with: oxycodone / acetaminophen

Generic entry2036 est.

⚠ 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 categoryNot assigned — PLLR-era drug

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.