Nalbuphine is an opioid agonist-antagonist used to treat pain, for pre and postoperative analgesia, and for analgesia in labor and delivery. It appears to be an agonist at kappa opioid receptors and an antagonist or partial agonist at mu opioid receptors.
- Mechanism
- Curator reviewed
The exact mechanism of action is unknown, but is believed to interact with an opiate receptor site in the CNS (probably in or associated with the limbic system). The opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but may also be a result of other mechanisms. Nalbuphine is thought primarily to be a kappa agonist. It is also a partial mu antagonist analgesic, with some binding to the delta receptor and minimal agonist activity at the sigma receptor.
- Primary indication
- For the relief of moderate to severe pain.Curator reviewed · 4 structured indications
- Formula / weight
- C21H27NO4 · 357.4434 g/mol (avg)
- First approval
- Canada, 2006 · United States, 1979
- Code names
- EN-2234 A
- Brand names
Resolves to
NETZHAKZCGBWSS-CEDHKZHLSA-NSMILESO[C@H]1CC[C@@]2(O)[C@H]3CC4=CC=C(O)C5=C4[C@@]2(CCN3CC2CCC2)[C@H]1O5What you can answer from here — as of September 23, 2026
Which drugs share a target with Nalbuphine, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account