Drug intelligence / Profile preview

nalbuphine

Development stage
Approved
Lead developer
Endo Laboratories
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular, Subcutaneous
01

Overview

Nalbuphine is a semi-synthetic opioid analgesic classified as a mixed agonist-antagonist. It primarily acts as an agonist at kappa opioid receptors and as an antagonist at mu opioid receptors. This dual mechanism provides effective analgesia comparable to morphine but with a lower risk of respiratory depression and dependence. Nalbuphine is used for the management of moderate to severe pain, including postoperative pain, cancer pain, and pain associated with various medical conditions. Its onset of action is rapid (5–10 minutes), with effects lasting 3–6 hours. Compared to traditional opioids like morphine or fentanyl, nalbuphine has fewer side effects such as pruritus (itching), nausea, vomiting, and less potential for abuse or addiction[1][4][5][6]. It can be used alone or in combination with other analgesics in multimodal pain management strategies.

Brand names
Nubain
Other names
纳布啡nalbuphine hydrochloride盐酸纳布啡
02

Targets

DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)KOR (Kappa opioid receptor)

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