Fixed-dose combination: long-acting opioid analgesic plus peripheral opioid receptor antagonist
ATC code: N02AA55 (Oxycodone and naloxone)
Oxycodone provides analgesia through μ-opioid receptors. Oral naloxone has very low systemic bioavailability (<3% due to first-pass metabolism) but blocks intestinal μ-receptors, reducing opioid-induced constipation. No systemic naloxone effect; opioid analgesia is preserved. RCTs show 40-50% reduction in constipation vs oxycodone monotherapy.
Third line
Severe chronic pain requiring long-term opioid analgesia with established or anticipated opioid-induced constipation. Per EAU 2024 and SED 2024, used mainly for cancer pain and severe neuropathic pain refractory to standard therapy. Dose: 10/5, 20/10, 40/20 mg every 12 hours. Not first-line for chronic non-cancer pain – see CDC 2022 opioid limits. Before starting, exclude severe hepatic impairment (raised naloxone bioavailability).
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Acute postoperative and post-traumatic pain. A strong opioid with fixed 12-hour dosing is not suited for variable acute pain – flexible titration with immediate-release agents is needed. Per SED 2024, acute pain is managed with short-course immediate-release oxycodone or morphine. If Targin was prescribed for 1-2 weeks of postoperative pain, consider getting a second opinion.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Boxed warning
FDA Black Box: risk of addiction and fatal respiratory depression; neonatal opioid withdrawal syndrome; fatal interactions with benzodiazepines and alcohol.
Not recommended in pregnancy. Long-term use causes neonatal opioid withdrawal. Taper 1-2 months before planned conception.
Long-term use not recommended – infant sedation risk. Hale L3. Short course under supervision if acutely necessary.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Oxycodone + Naloxone is evaluated for the following indications with varying evidence strength: Chronic pain (evidence tier B), Acute pain (evidence tier D). See the full indication matrix with dosing and citations above on this page.
Common side effects of Oxycodone + Naloxone (≥ 1 in 100): Constipation (still occurs but less than with monotherapy), Nausea, vomiting, Drowsiness, Dry mouth, Dizziness, Pruritus. See the Safety section for uncommon and serious reactions.
FDA category C. Not recommended in pregnancy. Long-term use causes neonatal opioid withdrawal. Taper 1-2 months before planned conception.
Long-term use not recommended – infant sedation risk. Hale L3. Short course under supervision if acutely necessary.
Oxycodone + Naloxone is contraindicated in: Hypersensitivity to oxycodone or naloxone; Respiratory depression, severe COPD, asthma exacerbation; Paralytic ileus; Severe hepatic impairment (Child-Pugh B-C); Acute alcohol or psychotropic intoxication. Full list in the Safety section.
FDA Black Box: risk of addiction and fatal respiratory depression; neonatal opioid withdrawal syndrome; fatal interactions with benzodiazepines and alcohol.