PERCODAN
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 351.82 |
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 | Avoid due to risk of neural tube defects and other malformations associated with opioid exposure in first trimester. |
| 2nd trimester | Avoid; chronic use may lead to fetal dependence and withdrawal; use only if clearly needed. |
| 3rd trimester | Avoid; risk of neonatal opioid withdrawal syndrome (NOWS) and respiratory depression at birth; use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for PERCODAN (PERCODAN).
| Placental transfer | Oxycodone (active component) crosses the placenta freely; detected in fetal tissues and amniotic fluid. |
| Breastfeeding | Oxycodone passes into breast milk; the relative infant dose is estimated at 1.7-8.6% of maternal weight-adjusted dose. Monitor infant for respiratory depression and sedation. Consider benefits vs risks. |
| Lactation Rating | L3 (Moderately Safe) – limited data suggest potential adverse effects. |
| 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. |
| 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). |
■ 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 or aspirinAsthmaBleeding disordersSevere hepatic impairmentSignificant respiratory depressionConcurrent MAO inhibitors
| 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) |
| Food/Dietary | Avoid alcohol. Grapefruit and grapefruit juice may increase oxycodone levels, enhancing side effects; avoid concurrent consumption. Aspirin component may cause gastrointestinal irritation; take with food or milk to reduce upset. Do not consume high-dose vitamin C or other acidifying agents as they may increase aspirin absorption and risk of salicylate toxicity. |
| Clinical Pearls | PERCODAN contains oxycodone and aspirin. Use with caution in patients with bleeding disorders or those on anticoagulants due to aspirin's antiplatelet effect. Monitor for respiratory depression, especially in elderly or opioid-naive patients. Avoid in children and adolescents with viral infections due to Reye's syndrome risk from aspirin. The oxycodone component may cause histamine release leading to pruritus; consider antihistamine co-prescription. Taper dose to avoid withdrawal symptoms upon discontinuation. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Avoid alcohol and other central nervous system depressants (sedatives, tranquilizers) as they may cause dangerous drowsiness or slowed breathing. · Do not drive or operate heavy machinery until you know how this medication affects you. · Aspirin in this medication increases bleeding risk; avoid other NSAIDs or anticoagulants unless approved by your doctor. · Seek emergency care if you experience signs of allergic reaction (rash, swelling, difficulty breathing) or signs of bleeding (unusual bruising, black/tarry stools). · Do not crush or chew tablets; swallow whole to avoid rapid release of oxycodone. · Store securely away from children and pets; dispose of unused medication properly via drug take-back programs. · Do not stop suddenly without medical guidance to avoid withdrawal symptoms (anxiety, sweating, nausea, muscle aches). |
Loading safety data…