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Peripheral μ-opioid receptor antagonist

Naldemedine

Brand names: Rizmoic

Naldemedine is a peripherally acting mu-opioid receptor antagonist taken orally to treat opioid-induced constipation in adults who have had an inadequate response to laxatives.

Dosing — being independently re-sourced

ClinCalc Pro is rebuilding its dose data from primary open sources — the manufacturer SmPC (eMC), the WHO Model Formulary and other official references — under clinician review. This drug's structured dose is not yet published here. Confirm all doses against the product SmPC and your local formulary before prescribing.

Clinical monograph

How it works

It antagonises mu-opioid receptors in the gastrointestinal tract; its limited penetration of the central nervous system means it relieves opioid-induced constipation without reversing central analgesia.

Prescribing in practice

  • Contraindicated in known or suspected gastrointestinal obstruction because of the risk of perforation.
  • It is taken orally once daily and may be given with or without food.
  • Discontinue if opioid treatment is stopped, and consider stopping if severe diarrhoea develops.

Monitoring

Monitor for severe abdominal pain or diarrhoea and for symptoms suggesting opioid withdrawal, particularly in patients with disrupted blood-brain barrier integrity.

Counselling the patient

  • Advise patients to report severe, persistent or worsening abdominal pain or diarrhoea promptly.
  • Explain that the medicine targets constipation in the gut and should not reduce pain control from their opioid.

Evidence & guidelines

Naldemedine is recommended by NICE as an option for treating opioid-induced constipation in adults who have had an inadequate response to laxatives.

Reference: NICE TA651; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.