ROXYBOND

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ROXYBOND (ROXYBOND).

How it works

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.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ROXYBOND (ROXYBOND).

Breastfeeding	Small amounts of oxycodone are excreted into breast milk. The milk-to-plasma (M/P) ratio is approximately 3:1. Use with caution, especially in mothers who are ultrarapid metabolizers of CYP2D6, as this increases risk of toxicity in the infant. Monitor infant for drowsiness, poor feeding, and respiratory depression.
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.

Warnings & precautions

■ 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).

Side Effect Profile

Serious Effects

Absolute Contraindications

["Significant respiratory depression","Acute or severe bronchial asthma in an unmonitored setting or without resuscitative equipment","Known or suspected gastrointestinal obstruction, including paralytic ileus","Hypersensitivity to oxycodone or any component of the formulation"]

Clinical Precautions

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."]

Clinical Tips & Counseling

Drug interactions

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ROXYBOND

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ROXYBOND (ROXYBOND).

How it works

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ROXYBOND (ROXYBOND).

Breastfeeding	Small amounts of oxycodone are excreted into breast milk. The milk-to-plasma (M/P) ratio is approximately 3:1. Use with caution, especially in mothers who are ultrarapid metabolizers of CYP2D6, as this increases risk of toxicity in the infant. Monitor infant for drowsiness, poor feeding, and respiratory depression.
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.