ROXYBOND
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ROXYBOND (ROXYBOND).
ROXYBOND is an immediate-release formulation of oxycodone, a full mu-opioid receptor agonist. It binds to mu-opioid receptors in the central nervous system (CNS), inhibiting ascending pain pathways and altering pain perception and emotional response to pain.
| Metabolism | Primarily hepatic via CYP3A4 and to a lesser extent CYP2D6. Oxycodone is metabolized to noroxycodone (via CYP3A4), oxymorphone (via CYP2D6), and other minor metabolites. |
| Excretion | Primarily renal (90% as free drug and glucuronide conjugates). Fecal elimination accounts for <10%. |
| Half-life | 3.5–6 hours; prolonged in renal impairment, hepatic impairment, or elderly patients, requiring dose adjustment. |
| Protein binding | Approximately 20–30%, primarily to albumin. |
| Volume of Distribution | 2.6–4.0 L/kg, indicating extensive tissue distribution (e.g., brain, lungs, liver). |
| Bioavailability | Oral: 10–20% (extensive first-pass metabolism); intranasal: 30–50%; intravenous: 100%. |
| Onset of Action | Oral immediate-release: 30 minutes; intranasal: 10–15 minutes; intravenous: 2–5 minutes. |
| Duration of Action | Immediate-release oral: 4–6 hours; intranasal: 3–5 hours; intravenous: 3–4 hours. Extended-release formulations provide up to 12-hour duration. |
| Molecular Weight | 351.82 |
Immediate-release oral tablets: 5-15 mg every 4-6 hours as needed for pain. Maximum 60 mg/day. For extended-release: 10-20 mg every 12 hours, adjusted based on prior opioid use.
| Dosage form | TABLET |
| Renal impairment | For GFR 30-59 mL/min: reduce dose by 25% and increase dosing interval. For GFR <30 mL/min: reduce dose by 50% and administer every 12 hours. Avoid in ESRD. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50% and increase interval. Child-Pugh Class C: avoid use. |
| Pediatric use | Weight-based dosing: 0.1-0.2 mg/kg/dose every 4-6 hours as needed. Maximum single dose: 5 mg for <50 kg, 10 mg for ≥50 kg. |
| Geriatric use | Start at lowest effective dose (2.5-5 mg every 4-6 hours). Titrate slowly due to increased sensitivity and risk of respiratory depression. Monitor renal function. |
| 1st trimester | Contraindicated due to potential for neural tube defects and other congenital anomalies reported with opioid use in first trimester. |
| 2nd trimester | Exposure associated with risk of miscarriage, preterm birth, and low birth weight; use only if clearly needed and no alternative. |
| 3rd trimester | Chronic use may cause neonatal opioid withdrawal syndrome (NOWS); avoid prolonged use near term. |
Clinical note
Comprehensive clinical and safety monograph for ROXYBOND (ROXYBOND).
| Placental transfer | Oxycodone readily crosses the placenta with fetal concentrations approximately equal to maternal plasma levels. |
| Breastfeeding | ROXYBOND (oxycodone) is excreted into breast milk in low concentrations; however, the risk of infant sedation and respiratory depression warrants caution. The American Academy of Pediatrics considers oxycodone use compatible with breastfeeding, but monitoring of the infant for signs of opioid effects is recommended. Consider using the lowest effective dose and shortest duration. |
■ 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; and Risk of Medication Errors (due to immediate-release formulation, which requires careful dose conversion from other oxycodone products).
| Serious Effects |
Significant respiratory depressionAcute or severe bronchial asthmaKnown or suspected gastrointestinal obstructionParalytic ileusHypersensitivity to oxycodone
| Precautions | Life-threatening respiratory depression, especially in elderly, cachectic, or debilitated patients and those with pre-existing respiratory conditions., Risk of opioid-induced hyperalgesia., Adrenal insufficiency with prolonged use., Severe hypotension, including orthostatic hypotension, in patients with compromised ability to maintain blood pressure., Risk of serotonin syndrome with concomitant serotonergic drugs., Seizures in patients with seizure disorders or taking other seizure threshold-lowering drugs., Avoid abrupt discontinuation; taper dose to prevent withdrawal syndrome. |
| Food/Dietary |
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| Lactation Rating | L3 (Moderately Safe) – limited data suggest potential for adverse effects; benefit should outweigh risk. |
| Teratogenic Risk | ROXYBOND (oxycodone) is an opioid agonist. First trimester: Limited human data; animal studies show no teratogenicity at clinically relevant doses. Second and third trimesters: Chronic use may lead to fetal dependence and neonatal opioid withdrawal syndrome (NOWS) after delivery. Avoid during labor due to respiratory depression in the newborn. |
| Fetal Monitoring | Monitor maternal respiratory status, sedation level, and bowel function. Fetal monitoring: assess for heart rate variability and signs of opioid withdrawal. Neonatal: observe for NOWS (irritability, hypertonia, tremors, poor feeding) for 48-72 hours after birth. |
| Fertility Effects | Oxycodone may suppress gonadotropin release via opioid receptor activation, leading to decreased libido, anovulation, and menstrual irregularities in females; in males, reduced testosterone and sperm motility. Effects are reversible upon discontinuation. |
| Avoid alcohol and any alcohol-containing foods or beverages. Grapefruit and grapefruit juice may increase oxycodone levels; avoid concurrent use. |
| Clinical Pearls | ROXYBOND (oxycodone hydrochloride) is an immediate-release opioid agonist indicated for acute pain severe enough to require an opioid. Its unique formulation resists crushing and dissolution, but it can still be abused intravenously. Be aware of the risk of respiratory depression, particularly in opioid-naive patients. Use with caution in patients with respiratory disease, or in elderly or debilitated patients. Tolerance and dependence can develop; monitor for signs of misuse. Naloxone is the reversal agent. Not indicated for as-needed use; prescribe the lowest effective dose for the shortest possible duration. |
| Patient Advice | Take exactly as prescribed; do not break, crush, chew, or dissolve the tablet as it can cause rapid release and fatal overdose. · Do not consume alcohol or any alcohol-containing products while taking ROXYBOND. · Store securely out of sight and reach of children and pets; properly dispose of unused tablets via a drug take-back program. · Side effects include constipation, nausea, dizziness, and drowsiness; contact your healthcare provider if you experience difficulty breathing or extreme sleepiness. · Avoid driving or operating heavy machinery until you know how ROXYBOND affects you. · Do not share this medication with others; it can cause addiction and death. · Inform your doctor about all other medications, especially sedatives, tranquilizers, or antidepressants. |