Drug intelligence / Profile preview

levobupivacaine + nalbuphine

Development stage
Unknown
Lead developer
Trevi Therapeutics
Modality
Small Molecules
Administration
Perineural, Epidural, Intrathecal, Infiltration
01

Overview

Levobupivacaine + nalbuphine is a combination of two pharmaceutical agents used primarily as an adjuvant regimen for regional anesthesia and postoperative analgesia. Levobupivacaine is a long-acting amide-type local anesthetic that works by blocking voltage-gated sodium channels on neuronal membranes, thereby inhibiting nerve impulse conduction and producing loss of sensation in the targeted area. Nalbuphine is an opioid analgesic with mixed agonist-antagonist activity; it acts as an agonist at kappa opioid receptors and as a partial antagonist or weak agonist at mu opioid receptors, providing effective pain relief with reduced risk of typical opioid side effects such as respiratory depression. The combination has been shown to prolong the duration of sensory and motor block, extend postoperative analgesia, reduce total rescue analgesic requirements, and maintain a favorable safety profile in both adult and pediatric populations undergoing various surgical procedures[1][2][3][4][5][7].

02

Targets

KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)NaV (Voltage-gated sodium channels)

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