Drug intelligence / Profile preview

liposomal bupivicaine (bupivacaine) (Pacira BioSciences)

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

Overview

Liposomal bupivacaine (marketed as Exparel) is an amide-type local anesthetic consisting of bupivacaine encapsulated within multivesicular liposomes using DepoFoam technology. This formulation is designed for single-dose administration to provide prolonged postsurgical analgesia by slowly releasing bupivacaine over an extended period, typically lasting up to 72 hours. It works by binding to voltage-gated sodium channels on the internal surface of nerve cell membranes, which inhibits the ionic fluxes required for the initiation and conduction of nerve impulses, thereby providing local anesthesia. Developed by Pacira BioSciences and FDA-approved since 2011, it is indicated for local infiltration and various peripheral nerve blocks (such as interscalene brachial plexus, sciatic, and adductor canal blocks) in both adults and pediatric patients aged 6 years and older to manage post-operative pain.

Brand names
Exparel
Other names
liposomal bupivacainebupivacaine liposomebupivacaine liposome injectable suspension
02

Targets

SCN4A (Voltage-gated sodium channel protein type 4 subunit alpha)SCN5A (Sodium channel protein type 5 subunit alpha)NaV (Voltage-gated sodium channels)

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