ROXICODONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ROXICODONE (ROXICODONE).
Oxycodone is a full opioid agonist with high affinity for mu-opioid receptors, also binding to kappa and delta receptors. It acts primarily on the central nervous system and gastrointestinal tract.
| Metabolism | Hepatic, primarily via CYP3A4 and CYP2D6; major metabolites include noroxycodone and oxymorphone. |
| Excretion | Renal excretion: 70-80% as unchanged drug and metabolites (oxymorphone, noroxycodone); fecal: 10-20%. |
| Half-life | 3.5-5 hours for immediate-release; 4.5-5.5 hours for extended-release. Accumulation may occur with repeated dosing, especially in elderly or hepatic impairment. |
| Protein binding | 45% bound to albumin. |
| Volume of Distribution | 2.0-2.5 L/kg. Large Vd indicates extensive tissue distribution, including to brain and adipose tissue. |
| Bioavailability | Oral immediate-release: 60-87%; oral extended-release: 40-60% (first-pass metabolism); intravenous: 100%; intramuscular: ~80%. |
| Onset of Action | Oral immediate-release: 10-15 min; oral extended-release: 60-120 min; intravenous: 2-3 min; intramuscular: 10-15 min. |
| Duration of Action | Immediate-release: 4-6 hours; extended-release: 8-12 hours. Duration may be shorter with acute pain or longer with chronic use. |
| Molecular Weight | 315.36 |
5-15 mg orally every 4-6 hours as needed for pain; immediate-release formulation. Maximum 60 mg total daily dose for opioid-naive patients.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | For eGFR 30-59 mL/min: administer at 50-75% of usual dose; for eGFR 10-29 mL/min: 50% of usual dose; for eGFR <10 mL/min: avoid use or use 25% of usual dose with extended intervals. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use or reduce dose by 75% with extended dosing intervals. |
| Pediatric use | Children aged 11 years and older: 0.1-0.2 mg/kg per dose orally every 4-6 hours as needed; maximum 10 mg per dose. Not recommended for children under 11 years due to limited data. |
| Geriatric use | Initiate at 3-5 mg orally every 4-6 hours; titrate cautiously. Avoid in patients with severe renal or hepatic impairment. Monitor for respiratory depression, constipation, and falls. |
| 1st trimester | Limited human data; animal studies show increased risk of neural tube defects and other malformations. Use only if benefit outweighs risk. |
| 2nd trimester | Use with caution; may cause fetal opioid dependence and withdrawal. Monitor for growth abnormalities. |
| 3rd trimester | Avoid prolonged use; risk of neonatal opioid withdrawal syndrome (NOWS). Use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for ROXICODONE (ROXICODONE).
| Placental transfer | Roxicodone crosses the placenta; evidence of transfer in humans and animals. |
| Breastfeeding | Roxicodone is excreted into breast milk in low concentrations. Monitor infant for drowsiness, respiratory depression, and constipation. The American Academy of Pediatrics considers it compatible with breastfeeding, but caution is advised. |
■ FDA Black Box Warning
Risk of addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines or other CNS depressants; interaction with alcohol.
| Serious Effects |
Hypersensitivity to oxycodone or any componentSignificant respiratory depressionAcute or severe bronchial asthmaParalytic ileusConcurrent use of MAOIs or within 14 daysKnown or suspected gastrointestinal obstruction
| Precautions | Addiction, abuse, and misuse; life-threatening respiratory depression; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines; severe hypotension; adrenal insufficiency; seizures; risks in patients with head injuries, increased intracranial pressure; severe hypertension; gastrointestinal obstruction; impaired renal or hepatic function; elderly and debilitated patients; pregnancy; lactation. |
| Food/Dietary | Avoid alcohol. No significant food interactions; take with or without food. Grapefruit/grapefruit juice may increase oxycodone levels; limit or avoid. |
Loading safety data…
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | First trimester: Increased risk of neural tube defects and congenital heart defects (odds ratio 2.0-3.0 for any opioid). Second and third trimesters: Risk of fetal growth restriction, preterm birth, and neonatal opioid withdrawal syndrome (NOWS). Considered low to moderate teratogenic risk; no specific malformation pattern identified. |
| Fetal Monitoring | Maternal: Respiratory rate, sedation level, bowel function. Fetal: Ultrasound for growth (every 4-6 weeks) and nonstress test (NST) or biophysical profile (BPP) weekly from 32 weeks if prolonged use. Neonatal: Observe for NOWS (e.g., irritability, feeding difficulties) for 72 hours postpartum. |
| Fertility Effects | May reduce fertility in both sexes due to hormonal alterations (e.g., hypogonadotropic hypogonadism, hyperprolactinemia). In women, may disrupt ovulatory cycles. Effects are reversible upon discontinuation. |
| Clinical Pearls | Roxicodone is a high-potency immediate-release oxycodone formulation. Avoid crushing or chewing tablets. Use with caution in patients with renal impairment (CrCl < 60 mL/min) as active metabolite oxymorphone accumulates. Consider naltrexone or naloxone for opioid-induced constipation. Monitor for respiratory depression, especially with concomitant CNS depressants. Do not use in patients with acute or severe bronchial asthma. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency. · Swallow tablets whole; do not crush, chew, or dissolve. · Avoid alcohol and other sedatives (e.g., benzodiazepines, muscle relaxants). · May cause drowsiness; do not drive or operate machinery until you know how you react. · Store securely out of sight and reach of children and pets. · Do not stop suddenly; taper under medical supervision to avoid withdrawal. · Report signs of serotonin syndrome (agitation, hallucinations, rapid heart rate) or adrenal insufficiency (nausea, vomiting, loss of appetite, fatigue). |