Drug intelligence / Profile preview

liposomal bupivicaine (bupivacaine) (Pacira BioSciences, 045423)

Development stage
Approved
Lead developer
Pacira BioSciences
Modality
Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Percutaneous, Parenteral
01

Overview

Liposomal bupivacaine (EXPAREL) is an extended-release formulation of the amide-type local anesthetic bupivacaine. It utilizes the DepoFoam® multivesicular liposomal drug delivery system to encapsulate bupivacaine, allowing for a prolonged duration of action (up to 72 hours) compared to standard bupivacaine. The drug works by binding to and blocking voltage-gated sodium channels on the internal surface of nerve cell membranes, which prevents the influx of sodium ions and inhibits the initiation and conduction of nerve impulses, thereby producing local anesthesia and analgesia. Developed by Pacira BioSciences, it is FDA-approved for single-dose infiltration in adults to produce postsurgical local analgesia and as an interscalene brachial plexus nerve block for regional analgesia.

Brand names
EXPAREL
Other names
liposomal bupivacainebupivacaine liposome injectable suspension
02

Targets

CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)Kir (Inward-rectifier potassium channels)NaV (Voltage-gated sodium channels)

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