OXYCODONE 5/APAP 500
Clinical safety rating: avoid
CNS depressants including alcohol and benzodiazepines increase sedation risk Life-threatening respiratory depression may occur.
Oxycodone: mu-opioid receptor agonist; Acetaminophen: cyclooxygenase (COX) inhibition, analgesic and antipyretic via central action.
| Metabolism | Oxycodone: primarily hepatic via CYP3A4 and to a lesser extent CYP2D6; Acetaminophen: hepatic via glucuronidation, sulfation, and CYP2E1 (minor). |
| Excretion | Renal: Oxycodone ~87% (10% unchanged, 77% as metabolites); Acetaminophen ~85% (2-5% unchanged, rest as glucuronide and sulfate conjugates). Biliary/fecal: Minimal for both. |
| Half-life | Oxycodone: Terminal half-life 3.5-5.6 hours (mean 4.5 h); prolonged in renal/hepatic impairment. Acetaminophen: 2-3 hours. |
| Protein binding | Oxycodone: 38-45% (primarily albumin); Acetaminophen: 10-25% (albumin). |
| Volume of Distribution | Oxycodone: 2.6-3.0 L/kg (reflects moderate tissue distribution); Acetaminophen: 0.9-1.0 L/kg (mainly body water). |
| Bioavailability | Oxycodone oral: 60-87% (first-pass metabolism); Acetaminophen oral: 85-98% (minimal first-pass). |
| Onset of Action | Oral (immediate-release): Oxycodone 15-30 min; Acetaminophen 30-60 min. |
| Duration of Action | Oxycodone: 4-6 hours (analgesia); Acetaminophen: 4-6 hours (antipyretic/analgesic). Note: Combination may have shorter analgesic duration than oxycodone alone at higher doses. |
1-2 tablets (oxycodone 5-10 mg/APAP 500-1000 mg) orally every 4-6 hours as needed for pain; maximum APAP dose 4000 mg/day from all sources.
| Dosage form | TABLET |
| Renal impairment | GFR 10-50 mL/min: extend dosing interval to every 6 hours; GFR <10 mL/min: use with caution, consider reducing dose or extending interval; not recommended in dialysis. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce starting dose by 50% and increase dosing interval; Child-Pugh Class C: avoid use. |
| Pediatric use | Not recommended for children <18 years due to safety concerns with codeine/oxycodone and APAP; for specific use, weight-based dosing of oxycodone 0.05-0.15 mg/kg/dose every 4-6 hours; APAP 10-15 mg/kg/dose every 4-6 hours; max APAP 75 mg/kg/day. |
| Geriatric use | Start at low end of dosing range (e.g., 2.5-5 mg oxycodone) due to increased sensitivity and risk of respiratory depression; monitor renal function; avoid in patients with significant hepatic impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
CNS depressants including alcohol and benzodiazepines increase sedation risk Life-threatening respiratory depression may occur.
| FDA category | Positive |
| Breastfeeding | Oxycodone is excreted into breast milk; M/P ratio is approximately 3.2:1. Relative infant dose is 1.7-6.3% of maternal weight-adjusted dose. Caution is advised; monitor infant for sedation and respiratory depression, especially in CYP2D6 ultra-rapid metabolizers. Acetaminophen is compatible with breastfeeding in usual doses. |
| Teratogenic Risk |
■ FDA Black Box Warning
Addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines or other CNS depressants; hepatotoxicity from acetaminophen overdose.
| Common Effects | Constipation |
| Serious Effects |
Significant respiratory depression; acute or severe bronchial asthma; known or suspected gastrointestinal obstruction; hypersensitivity to oxycodone, acetaminophen, or any component; severe hepatic impairment (acetaminophen-related).
| Precautions | Respiratory depression; drug dependence; abuse potential; hepatotoxicity; hypersensitivity; adrenal insufficiency; hypotension; seizures; severe hypotension; head injury; gastrointestinal obstruction; severe hypertension; severe hepatic or renal impairment; elderly/debilitated patients; pregnancy/breastfeeding. |
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| First trimester: Oxycodone is not associated with a significant increased risk of major congenital malformations in most studies, but data on the combination with acetaminophen are limited. Second and third trimesters: Chronic use or high doses near term may cause neonatal opioid withdrawal syndrome (NOWS). Use during labor may cause respiratory depression in the neonate. Acetaminophen is generally considered low risk, but overdose is hepatotoxic to fetus. |
| Fetal Monitoring | Maternal: Monitor for signs of opioid toxicity (respiratory depression, sedation, constipation), acetaminophen hepatotoxicity (liver enzymes, bilirubin), and development of opioid use disorder. Fetal/Neonatal: Monitor fetal heart rate patterns during labor; assess for NOWS (e.g., feeding difficulties, irritability, tremors) for at least 48-72 hours after delivery if maternal use near term. |
| Fertility Effects | Oxycodone may cause menstrual cycle irregularities (e.g., anovulation) due to opioid-induced hyperprolactinemia and suppression of GnRH, potentially impairing fertility. Acetaminophen at therapeutic doses has no known adverse effect on fertility. |