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bupivacaine liposomes (Pacira BioSciences)
- Development stage
- Approved
- Lead developer
- Pacira BioSciences
- Modality
- Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Percutaneous
01
Overview
Bupivacaine liposome is an amide-type local anesthetic encapsulated in a multivesicular liposomal delivery system (DepoFoam). This formulation is designed to provide prolonged postsurgical analgesia by slowly releasing bupivacaine over an extended period, typically up to 72 hours. The mechanism of action involves the reversible blockade of voltage-gated sodium channels on the internal surface of nerve cell membranes, which prevents the influx of sodium ions and the subsequent depolarization and conduction of nerve impulses. Developed by Pacira BioSciences (as Exparel) and Luye Pharma (as Luroca), it is indicated for single-dose infiltration in adults to produce postsurgical local analgesia and as an interscalene brachial plexus block to produce postsurgical regional analgesia. The liposomal encapsulation allows for a significantly longer duration of action compared to standard bupivacaine HCl solutions.
- Brand names
- ExparelLurocaNocita
- Other names
- Liposomal bupivacaineBupivacaine liposome injectable suspensionBupivacaine liposomes
02
Targets
SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)SCN5A (Sodium channel protein type 5 subunit alpha)SCN10A (Sodium channel protein type X alpha subunit)SCN9A (Sodium channel protein type 9 subunit alpha)
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