Drug intelligence / Profile preview

bupivacaine

Development stage
Approved
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Epidural, Intrathecal, Perineural, Infiltration, Dental, Surgical Implant
01

Overview

Bupivacaine is a potent amide-type local anesthetic widely used to induce local or regional anesthesia for surgical procedures, labor and delivery, dental work, and other medical interventions. It works primarily by blocking voltage-gated sodium channels on neuronal membranes from the intracellular side. This blockade prevents sodium influx during depolarization and inhibits the generation and conduction of nerve impulses (action potentials), resulting in loss of sensation in the targeted area[1][5][8]. The order of sensory loss typically progresses from pain to temperature to touch to proprioception and finally skeletal muscle tone[1][8]. Bupivacaine may also exert additional analgesic effects through inhibition of prostaglandin E2 receptor EP1 subtype activity[1] and has been shown experimentally to inhibit NMDA receptor-mediated synaptic transmission in the spinal cord[6]. First discovered in 1957 as part of the amide group of local anesthetics[4], bupivacaine is characterized by its long duration of action compared with other agents in its class.

Brand names
MarcaineMarcaine HClMarcaine SpinalSensorcaineSensorcaine-MPFSensorcaine-MPF SpinalXaracoll
Other names
bupivacaine liposomal injectionbupivacaine liposome injectable suspension
02

Targets

NaV (Voltage-gated sodium channels)NMDAR (Glutamate receptor ionotropic, NMDA)

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