OXYCONTIN
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 351.82 |
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 | Limited human data; animal studies show increased risk of neural tube defects with high doses. Use only if potential benefit justifies risk. |
| 2nd trimester | Chronic use may lead to fetal opioid dependence and neonatal withdrawal syndrome. Use only if clearly needed. |
| 3rd trimester | Prolonged use may cause neonatal opioid withdrawal syndrome (NOWS) and respiratory depression. Avoid during labor due to risk of respiratory depression in neonate. |
Clinical note
Comprehensive clinical and safety monograph for OXYCONTIN (OXYCONTIN).
| Placental transfer | Oxycodone readily crosses the placenta; serum levels in fetus may approach maternal levels. |
| Breastfeeding | Present in breast milk; possible infant sedation, respiratory depression, and withdrawal if chronic maternal use. The American Academy of Pediatrics considers use compatible with breastfeeding if maternal dose is low and infant monitored for adverse effects. |
| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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. |
■ 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 depressionAcute or severe bronchial asthma in an unmonitored setting or without resuscitative equipmentKnown or suspected gastrointestinal obstruction including paralytic ileusHypersensitivity to oxycodone or any components of OxyContin
| 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. |
| Food/Dietary | Avoid alcohol, which can increase oxycodone absorption and central nervous system depression. Grapefruit juice may alter oxycodone metabolism; limit or avoid consumption. No specific food restrictions, but high-fat meals may slow absorption slightly; take with or without food consistently. |
| Clinical Pearls | OxyContin is an extended-release formulation of oxycodone, indicated for around-the-clock pain management. Do not crush, chew, or break tablets, as this can lead to rapid release and fatal overdose. Use with caution in patients with respiratory compromise, head injury, or increased intracranial pressure. Monitor for signs of misuse, abuse, or addiction. Abrupt discontinuation may precipitate withdrawal; taper dose gradually. Constipation is common; consider prophylactic laxatives. Contraindicated in severe asthma, paralytic ileus, or hypersensitivity. |
| Patient Advice | Take OxyContin exactly as prescribed, usually every 12 hours. Do not take more or less than directed. · Swallow the tablet whole with water. Do not crush, chew, or break the tablet, as this can cause a dangerous overdose. · Avoid alcohol and other central nervous system depressants (e.g., benzodiazepines, sedatives) as they increase the risk of severe sedation, respiratory depression, and death. · Do not stop taking OxyContin suddenly; ask your doctor how to safely discontinue the medication to avoid withdrawal symptoms. · Common side effects include constipation, nausea, drowsiness, and dizziness. Contact your doctor if you experience severe constipation, difficulty breathing, or signs of allergic reaction. · Store OxyContin in a secure place out of sight and reach of children and pets. Dispose of unused medication via a drug take-back program. · Do not drive or operate heavy machinery until you know how OxyContin affects you. · Inform all healthcare providers that you are taking OxyContin, especially before surgery or emergency treatment. |
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