PERCODAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PERCODAN (PERCODAN).
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. Oxycodone acts on the central nervous system (CNS) to produce analgesia. Aspirin inhibits cyclooxygenase, leading to decreased prostaglandin synthesis, which reduces pain and inflammation.
| Metabolism | Oxycodone is metabolized primarily via CYP3A4 to noroxycodone and via CYP2D6 to oxymorphone, a more potent analgesic. Aspirin is hydrolyzed to salicylate, which is further conjugated with glycine (forming salicyluric acid) and glucuronic acid. |
| Excretion | Oxycodone: primarily renal (65-87% as parent and metabolites, mostly noroxycodone and oxymorphone conjugates); ~10% fecal. Aspirin: renal (75-90% as salicylates and metabolites, dose-dependent). |
| Half-life | Oxycodone: 3-5 hours, prolonged in elderly, hepatic/renal impairment. Aspirin: 2-3 hours at low doses; 15-30 hours at anti-inflammatory doses due to saturable metabolism. |
| Protein binding | Oxycodone: 38-45% bound to albumin. Aspirin: 80-90% bound to albumin (saturable). |
| Volume of Distribution | Oxycodone: 2.0-3.5 L/kg, extensive tissue distribution. Aspirin: 0.15-0.2 L/kg (low Vd). |
| Bioavailability | Oxycodone: oral 60-87% (first-pass metabolism). Aspirin: oral 50-75% (dose-dependent; hydrolyzed to salicylate). |
| Onset of Action | Oral: oxycodone 10-15 minutes; aspirin 15-30 minutes. |
| Duration of Action | Immediate-release: 4-6 hours for oxycodone; 4-6 hours for aspirin's analgesic effect. |
1-2 tablets orally every 4-6 hours as needed for pain. Each tablet contains oxycodone 4.5 mg and aspirin 325 mg.
| Dosage form | TABLET |
| Renal impairment | Avoid use if GFR < 30 mL/min. For GFR 30-60 mL/min: reduce dose or extend interval; consider alternative therapy due to aspirin component. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh C). In moderate impairment (Child-Pugh B): reduce dose by 50% and monitor. In mild impairment (Child-Pugh A): use with caution. |
| Pediatric use | Not recommended for children < 12 years. For children ≥ 12 years: 1 tablet orally every 4-6 hours as needed; maximum 4 tablets/day. |
| Geriatric use | Start with 1 tablet orally every 6 hours; titrate cautiously due to increased sensitivity to oxycodone and risk of aspirin-induced GI bleeding. Monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PERCODAN (PERCODAN).
| Breastfeeding | Breastfeeding safety: oxycodone is excreted into breast milk (M/P ratio approximately 3.4:1). Aspirin is also excreted. Potential for infant opioid toxicity and Reye's syndrome. Use is not recommended; if essential, monitor infant for sedation, respiratory depression, and poor feeding. |
| Teratogenic Risk | Percodan (oxycodone/aspirin) is contraindicated in pregnancy. Aspirin is associated with premature ductus arteriosus closure and oligohydramnios in third trimester; risk of premature closure increases with gestational age. Oxycodone use in first trimester may increase risk of congenital malformations (neural tube defects, cardiac defects). Chronic use in third trimester may cause neonatal opioid withdrawal syndrome. Avoid in all trimesters unless clear benefit outweighs risks. |
■ FDA Black Box Warning
WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; ULTRA-RAPID METABOLISM IN CYP2D6 POOR METABOLIZERS; NEONATAL OPIOID WITHDRAWAL SYNDROME; RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS; and INTERACTION WITH ALCOHOL.
| Serious Effects |
["Hypersensitivity to oxycodone, aspirin, or any component","Significant respiratory depression","Acute or severe bronchial asthma","Paralytic ileus","Suspected surgical abdomen","Severe bleeding disorders","Children with viral illness (aspirin risk of Reye syndrome)","Concomitant use with MAO inhibitors or within 14 days of discontinuation"]
| Precautions | ["Risk of respiratory depression, especially in elderly or debilitated patients","Risk of opioid-induced hyperalgesia","Adrenal insufficiency with prolonged use","Severe hypotension","Gastrointestinal obstruction or severe constipation","Seizures in patients with seizure disorders","Serotonin syndrome with serotonergic drugs","Reye syndrome in children with viral illnesses (due to aspirin)"] |
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| Fetal Monitoring | If used despite risks: monitor fetal growth and amniotic fluid volume (ultrasound) due to aspirin effect; fetal echocardiography for ductus arteriosus patency after 20 weeks; neonatal monitoring for withdrawal symptoms (Finnegan score) after delivery. Maternal monitoring: signs of bleeding (aspirin), opioid-related adverse effects. |
| Fertility Effects | Oxycodone may impair fertility in females by disrupting menstrual cycle and in males by decreasing libido and causing erectile dysfunction. Aspirin may inhibit prostaglandin synthesis required for ovulation; reversible upon discontinuation. Chronic use may affect sperm parameters (motility, count). |