OXYCONTIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OXYCONTIN (OXYCONTIN).
Oxycodone is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of oxycodone is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with oxycodone. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression.
| Metabolism | Oxycodone is metabolized primarily via CYP3A4 to noroxycodone (major metabolite) and via CYP2D6 to oxymorphone (minor metabolite). Both metabolites are active, with oxymorphone having higher potency. Oxycodone and its metabolites are conjugated and excreted in urine. |
| Excretion | Primarily renal (90% as metabolites, 10% unchanged). Also biliary/fecal (10%). |
| Half-life | 4.5-5.0 hours (immediate-release); controlled-release OXYCONTIN has an apparent half-life of 4.5-8.7 hours. Terminal half-life is ~3.5-4 hours for immediate-release, reflecting context-sensitive elimination. |
| Protein binding | 38-45%, primarily bound to albumin. |
| Volume of Distribution | 2.6-3.0 L/kg. Extensive tissue distribution, high Vd indicates penetration into peripheral tissues. |
| Bioavailability | Oral immediate-release: 60-87% (first-pass metabolism). Oral extended-release (OxyContin): 60-87% (similar). Intravenous: 100%. |
| Onset of Action | Oral immediate-release: 15-30 minutes. Oral extended-release (OxyContin): 30-60 minutes. Intravenous: 5-10 minutes. |
| Duration of Action | Immediate-release: 3-4 hours (analgesic). Extended-release: 8-12 hours (analgesic). Note: Duration depends on dose and pain severity. |
10 mg orally every 12 hours; titrate based on pain severity and prior opioid exposure.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | CrCl 30-60 mL/min: reduce dose by 25%; CrCl <30 mL/min: reduce dose by 50% and administer every 12 hours; hemodialysis: avoid use. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use. |
| Pediatric use | Not approved for pediatric patients <18 years; for children ≥11 years (opioid-tolerant): 0.2 mg/kg orally every 12 hours, titrate; maximum single dose 10 mg. |
| Geriatric use | Initiate at 5 mg orally every 12 hours; titrate cautiously; monitor for respiratory depression and constipation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OXYCONTIN (OXYCONTIN).
| Breastfeeding | Oxycodone is excreted into breast milk; relative infant dose is approximately 2.7–8.8% of maternal weight-adjusted dose. M/P ratio unknown. Monitor infant for sedation, respiratory depression, and poor feeding. American Academy of Pediatrics considers oxycodone compatible with breastfeeding with caution; avoid rapid accumulation in mothers with impaired metabolism (CYP2D6 poor metabolizers). |
| Teratogenic Risk | FDA Pregnancy Category C prior to 2020; no adequate studies in pregnant women. First trimester: Limited data suggest possible increased risk of neural tube defects (1.8-fold) and oral clefts (1.5-fold) with opioid use, but confounded by underlying conditions. Second and third trimesters: Chronic use may cause fetal opioid dependence and neonatal abstinence syndrome (NAS); maternal withdrawal may precipitate preterm labor. Avoid prolonged use near term due to risk of neonatal respiratory depression. |
■ FDA Black Box Warning
WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME; and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS
| Serious Effects |
["Significant respiratory depression","Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment","Known or suspected gastrointestinal obstruction, including paralytic ileus","Hypersensitivity (e.g., anaphylaxis) to oxycodone or any other components of the product"]
| Precautions | ["Addiction, abuse, and misuse: OxyContin exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death. Assess each patient's risk prior to prescribing, and monitor all patients regularly for the development of these behaviors or conditions.","Life-threatening respiratory depression: Serious, life-threatening, or fatal respiratory depression may occur. Monitor for respiratory depression, especially during initiation of therapy or following a dose increase. Instruct patients to swallow tablets whole; crushing, chewing, or dissolving can cause rapid release and absorption of a potentially fatal dose.","Accidental ingestion: Accidental ingestion of even one dose of OxyContin, especially by children, can result in a fatal overdose of oxycodone.","Neonatal opioid withdrawal syndrome: Prolonged use of OxyContin during pregnancy can result in withdrawal in the neonate. Neonatal opioid withdrawal syndrome, unlike opioid withdrawal in adults, may be life-threatening if not recognized and treated.","Risks from concomitant use with benzodiazepines or other CNS depressants: Concomitant use of opioids with benzodiazepines or other CNS depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing for use in patients for whom alternative treatment options are inadequate."] |
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| Fetal Monitoring | Monitor maternal vital signs (respiratory rate, sedation level) and bowel function. Serial fetal ultrasound for growth and anatomy if prolonged use. Near term: fetal nonstress test and biophysical profile if concern for fetal growth restriction or placental insufficiency. Postnatal: observe neonate for signs of NAS (e.g., tremors, irritability, poor feeding) for at least 48 hours after delivery. |
| Fertility Effects | Opioid use may impair fertility in both sexes. In females: disruption of hypothalamic-pituitary-ovarian axis leading to anovulation, amenorrhea, and decreased libido. In males: reduced sperm motility and morphology, erectile dysfunction. Effects are generally reversible upon discontinuation. |