naloxone hydrochloride + oxycodone hydrochloride: clinical use

Prescribing considerations

• Agree treatment goals, review arrangements and an eventual discontinuation plan before initiation.
• Assess respiratory disease, sleep apnoea, frailty, renal or hepatic impairment, substance-use history and concurrent sedating medicines.
• Not intended for breakthrough pain or acute postoperative pain.
• Consider tolerance, opioid-induced hyperalgesia or disease progression if pain control deteriorates.
• Counsel about impairment, safe storage, dependence, overdose and avoiding manipulation of the tablet.

Contraindications and cautions

• Hypersensitivity to an active substance or excipient.
• Severe respiratory depression with hypoxia or hypercapnia.
• Severe chronic obstructive pulmonary disease, cor pulmonale or severe bronchial asthma.
• Paralytic ileus not caused by opioids.
• Moderate or severe hepatic impairment.

Monitoring

• Pain control, function and continued clinical need.
• Sedation, respiratory rate and symptoms of sleep-related breathing disorders.
• Bowel function, including persistent constipation or diarrhoea.
• Tolerance, dependence, withdrawal, early refill requests and other signs of opioid-use disorder.
• Renal and hepatic function where clinically relevant.
• Endocrine symptoms during longer-term exposure and evidence of opioid-induced hyperalgesia.
• Interacting medicines and anticoagulation monitoring where applicable.

Clinical pharmacology

Oxycodone is an opioid-receptor agonist with central analgesic activity. Naloxone is an opioid antagonist with very low oral systemic bioavailability because of first-pass metabolism, allowing predominantly local antagonism in the gut. Oxycodone is metabolised mainly through CYP3A4 and partly through CYP2D6.

Formulation and product differences

• The selected product is an oral prolonged-release, fixed-ratio combination tablet.
• The tablet must remain intact to preserve prolonged release; crushing, chewing or breaking can cause rapid, potentially fatal oxycodone release.
• The selected product contains lactose.
• The empty tablet matrix may occasionally be visible in stools.

Modified-release tablet

Route: Oral

Strengths: 10 mg + 5 mg, 20 mg + 10 mg, 40 mg + 20 mg