Drug intelligence / Profile preview

liposome bupivacaine (Pacira BioSciences)

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

Overview

Liposome bupivacaine is an extended-release formulation of the amide-type local anesthetic bupivacaine. It utilizes the DepoFoam multivesicular liposomal drug delivery system, which consists of microscopic, lipid-based particles containing numerous non-concentric internal aqueous chambers that encapsulate the drug. This technology allows for a slow, controlled release of bupivacaine over an extended period (up to 72 hours), providing prolonged postsurgical analgesia and potentially reducing the need for opioids. It works by binding to the intracellular portion of voltage-gated sodium channels, blocking sodium influx into nerve cells, which prevents the generation and conduction of nerve impulses. It is primarily indicated for single-dose infiltration in adults to produce postsurgical local analgesia and as an interscalene brachial plexus nerve block. Clinical trials, such as those conducted by the Anhui Women and Children Medical Center, have explored its efficacy in specific settings like cesarean sections.

Brand names
Exparel
Other names
bupivacaine liposome injectable suspensionliposomal bupivacaine
02

Targets

KATP channel (ATP-sensitive potassium channel)CaV (Voltage-gated calcium channel protein complex)SCN5A (Sodium channel protein type 5 subunit alpha)NaV alpha (Voltage-gated sodium channel alpha subunit family)

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