Drug intelligence / Profile preview

nalbuphine + sufentanil

Development stage
Phase 3
Lead developer
Endo International
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Epidural
01

Overview

Nalbuphine + sufentanil is a combination of two opioid analgesics used primarily for the management of moderate to severe pain, especially in perioperative and obstetric settings such as post-cesarean section and labor analgesia. Nalbuphine is a synthetic opioid that acts as an agonist at kappa-opioid receptors and an antagonist at mu-opioid receptors, providing potent analgesia with a ceiling effect on respiratory depression. Sufentanil is a highly potent mu-opioid receptor agonist known for its strong analgesic effects and relatively favorable side effect profile compared to other opioids. When combined, these drugs provide superior pain relief compared to sufentanil alone, with reduced rates of certain opioid-related side effects such as respiratory depression. This combination has been shown to be effective in patient-controlled intravenous or epidural analgesia regimens after cesarean section and during labor[1][2][5]. The mechanism involves both central kappa-agonism (nalbuphine) and mu-agonism (sufentanil), resulting in synergistic or additive analgesic effects.

Other names
nalbuphine and sufentanil combinationnalbuphine/sufentanil
02

Targets

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

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