Drug intelligence / Profile preview

extended-release liposomal bupivacaine

Development stage
Unknown
Lead developer
Pacira BioSciences
Modality
Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Local Infiltration, Perineural
01

Overview

Extended-release liposomal bupivacaine is a long-acting local anesthetic formulated as an aqueous suspension of multivesicular liposomes (DepoFoam technology) containing the amide-type anesthetic bupivacaine. This formulation allows for the slow release of bupivacaine over up to 72 hours following a single-dose infiltration or nerve block, providing prolonged postsurgical analgesia and reducing the need for opioid medications. The drug acts by blocking voltage-gated sodium channels in neuronal membranes, thereby inhibiting nerve impulse transmission and preventing pain signal propagation. It is primarily indicated for postsurgical local analgesia via infiltration in adults and children aged 6 years or older, as well as certain peripheral nerve blocks (e.g., brachial plexus block) in adults[1][3][5][8]. Developed using DepoFoam technology to extend duration without altering the active ingredient itself[6], it has been shown to reduce opioid consumption postoperatively.

Brand names
EXPAREL
Other names
bupivacaine liposome injectable suspensionliposomal bupivacaineDepoFoam bupivacaine
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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