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Strong opioid + peripheral opioid antagonist

Oxycodone with naloxone

Brand names: Targinact

Adult dose

Dose: 5/2.5mg or 10/5mg PO BD initially, titrate; max 80/40mg BD
Route: PO
Frequency: BD

Clinical pearls

  • Severe pain where opioid-induced constipation refractory to laxatives
  • Naloxone has very low oral bioavailability — selectively antagonises gut μ-receptors

Contraindications

  • Moderate-severe hepatic impairment
  • Acute respiratory depression
  • Paralytic ileus
  • Concurrent MAOI

Side effects

  • Constipation (less than oxycodone alone)
  • As oxycodone
  • Naloxone-mediated opioid withdrawal at higher doses

Interactions

  • CNS depressants
  • MAOIs
  • Strong CYP3A4 modulators

Monitoring

  • Pain
  • Bowel function
  • Sedation

Reference: BNF; NICE CG140; SmPC; https://bnf.nice.org.uk/drugs/oxycodone-with-naloxone/. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.