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Active Pharma Ingredients / 21 Sep 2026

CEBRANOPADOL

Generic Name: CEBRANOPADOL

ABSTRACT -

Cebranopadol is a first-in-class analgesic that simultaneously activates the nociceptin/orphanin FQ peptide (NOP/ORL1) receptor and the classical mu, delta, and kappa opioid receptors. The dual mechanism is hypothesised to provide superior analgesia in nociceptive, neuropathic, and cancer pain while potentially offering a more favourable respiratory safety and abuse liability profile than pure mu-opioid agonists. Phase II/III trials evaluated it in chronic pain and cancer pain.

DOSAGE -

Oral tablet; 200–1000 µg once daily studied in Phase II/III trials for chronic pain; dose titrated based on analgesic response and tolerability.

SIDE EEFECTS -

  • Nausea
  • Dizziness
  • Somnolence
  • Constipation
  • Vomiting

ALLERGIC REACTIONS -

These symptoms may indicate an allergic reaction and require immediate medical attention.

  • Skin rash
  • Urticaria
  • Drug hypersensitivity
  • Anaphylaxis (rare)

DRUG INTERACTIONS-

  • CNS depressants (benzodiazepines, alcohol, sedatives) — additive respiratory depression and sedation
  • Strong CYP3A4 inhibitors increase cebranopadol exposure
  • MAO inhibitors — potential serotonin syndrome risk

PREAUTONS–

  • Assess abuse potential — schedule designation pending regulatory review
  • Respiratory function monitoring especially in COPD or sleep apnoea
  • Do not abruptly discontinue — taper to avoid withdrawal
  • Pregnancy: neonatal opioid withdrawal syndrome risk

WARNINGS –

  • Respiratory depression risk — titrate carefully, avoid in severe respiratory impairment
  • Abuse and dependence potential — controlled substance status likely in most markets
  • Neonatal opioid withdrawal syndrome if used during pregnancy

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