Strong opioid + peripheral opioid antagonist Pregnancy: Should only be used during pregnancy if the benefit outweighs the possible risks to the unborn child or neonate. Regular use during pregnancy may cause drug dependence in the foetus, leading to withdrawal symptoms in the neonate — advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure appropriate treatment will be available. Administration during labour may depress respiration in the neonate and an antidote for the child should be readily available. Breastfeeding should be discontinued during treatment (oxycodone may be secreted in breast milk and may cause respiratory depression in the infant; milk-plasma ratio 3.4:1).

Oxycodone with naloxone

Brand names: Targinact

Used in: Poisoning & Overdose

A fixed-dose modified-release combination of the strong opioid oxycodone with the opioid antagonist naloxone, used for severe pain where opioid-induced constipation is a concern.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: Adults, opioid-naive: usual starting dose 10 mg/5 mg oxycodone hydrochloride/naloxone hydrochloride at 12-hourly intervals. Patients already receiving opioids may be started on higher doses depending on their previous opioid experience.

Route: Oral — prolonged-release tablets; swallow with sufficient liquid, must not be broken, chewed or crushed (the 10 mg/5 mg tablet can be divided into equal doses)

Frequency: Twice daily (every 12 hours) to a fixed time schedule

Max: 160 mg oxycodone hydrochloride and 80 mg naloxone hydrochloride per day — reserved for patients previously maintained on a stable daily dose who have become in need of an increased dose

The 5 mg/2.5 mg strength is intended for dose titration when initiating opioid therapy and for individual dose adjustment. Titration: adjust every 1-2 days in steps of twice daily 5 mg/2.5 mg, or where necessary <2.5 mg/1.25 mg or >10 mg/5 mg oxycodone hydrochloride/naloxone hydrochloride, until a stable dose is reached. In non-malignant pain therapy, daily doses of up to 40 mg/20 mg oxycodone hydrochloride/naloxone hydrochloride are usually sufficient, but higher doses may be needed. In general the lowest effective analgesic dose should be selected. This is a prolonged-release formulation and is NOT intended for breakthrough pain; a single dose of rescue medication should approximate one sixth of the equivalent daily dose of oxycodone hydrochloride, and the need for more than two rescues per day usually indicates the dose requires upward adjustment. For patients requiring higher doses, supplemental prolonged-release oxycodone hydrochloride at the same time intervals may be considered, taking into account the maximum daily dose of 400 mg prolonged-release oxycodone hydrochloride (in which case naloxone's beneficial effect on bowel function may be impaired). Symmetric 12-hourly dosing suits most patients, but some may benefit from asymmetric dosing tailored to their pain pattern. Should not be administered for longer than absolutely necessary; when opioid treatment is no longer required, withdraw gradually over about a week to reduce the risk of a withdrawal reaction. Before starting, agree a strategy for ending treatment to minimise the risk of addiction and drug withdrawal syndrome. Elderly: as for younger adults, adjust to pain intensity and individual sensitivity. Hepatic impairment: contraindicated in moderate and severe hepatic impairment; caution in mild impairment. Paediatric population: 'The safety and efficacy of Myloxifin in children and adolescents aged below 18 years has not been established. No data are available.' NOTE: SPC section 4.5 (interactions) was NOT retrieved in this fetch and sections 4.4/4.8 were truncated at the source-fetch limit — no interaction list is given below. Source product is Myloxifin 10 mg/5 mg prolonged-release tablets; a US openFDA label for oxycodone hydrochloride alone was also present in the bundle but was NOT used, as it covers only one component of this fixed combination.

Dose adjustments

Renal

Caution should be exercised in patients with renal impairment — plasma concentrations of both oxycodone and naloxone are elevated, with naloxone affected to a higher degree; the clinical relevance is not yet known. Careful medical monitoring is particularly necessary for patients with severe renal impairment, and special attention should be given to patients with compromised renal function if an increased dose is considered.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substances or to any of the excipients
Severe respiratory depression with hypoxia and/or hypercapnia
Severe chronic obstructive pulmonary disease
Cor pulmonale
Severe bronchial asthma
Non-opioid induced paralytic ileus
Moderate to severe hepatic impairment

Side effects

Gastrointestinal (common): constipation, nausea, vomiting, abdominal pain, diarrhoea, dry mouth, dyspepsia, flatulence
Nervous system (common): dizziness, headache, somnolence
Psychiatric (common): insomnia
Skin (common): pruritus, skin reactions, hyperhidrosis
Metabolism (common): decreased appetite up to loss of appetite
General (common): asthenia, fatigue
Respiratory depression (listed in a lower-frequency column of the SPC table; the exact frequency category is not resolvable from the fetched table layout)

Clinical monograph

How it works

Oxycodone provides analgesia through mu opioid receptor agonism, while orally administered naloxone acts locally in the gut to block intestinal opioid receptors yet undergoes extensive first-pass metabolism, so it counteracts opioid-induced constipation without reducing systemic analgesia.

Prescribing in practice

As with all strong opioids, the principal hazard is respiratory depression, with risks of sedation, dependence and overdose, particularly when combined with other CNS depressants.
The naloxone component relies on hepatic first-pass metabolism, so the combination should be avoided in moderate to severe hepatic impairment where naloxone may reach the circulation and reduce analgesia or precipitate withdrawal.
Tablets must be swallowed whole; crushing or chewing the modified-release formulation can lead to rapid opioid release and dangerous overdose.

Monitoring

Monitor pain control, bowel function, sedation and respiratory status, and review regularly for signs of tolerance, dependence or misuse.

Counselling the patient

Swallow the tablets whole—never crush, break or chew them—to avoid a dangerous opioid surge.
Do not drink alcohol; report excessive drowsiness or slow breathing, and do not stop suddenly after regular use.

Evidence & guidelines

The oxycodone–naloxone combination is licensed for severe pain with the aim of reducing opioid-induced constipation, with prescribing guided by the SPC and opioid safety guidance.

Reference: NICE CG140; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways