Drug intelligence / Profile preview

lidocaine + bupivacaine + hyaluronidase

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Therapeutic Enzymes → Recombinant Proteins and Enzymes, Small Molecules
Administration
Peribulbar, Sub-tenon's, Perineural, Infiltration
01

Overview

This is a combination of two amide-type local anesthetics, lidocaine and bupivacaine, with the enzyme hyaluronidase. Lidocaine provides rapid onset of anesthesia, while bupivacaine offers prolonged duration. Hyaluronidase acts as an adjuvant by breaking down hyaluronic acid in connective tissue, increasing tissue permeability and facilitating the spread of local anesthetics. This combination is commonly used for regional anesthesia techniques such as peribulbar or sub-Tenon's blocks in ophthalmic surgery and for peripheral nerve blocks (e.g., brachial plexus block). The addition of hyaluronidase has been shown to hasten the onset and improve the quality of anesthesia by enhancing diffusion through tissues[1][2][3][4]. The mechanism involves sodium channel blockade (lidocaine/bupivacaine) and enzymatic degradation of extracellular matrix components (hyaluronidase).

02

Targets

SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)SCN3A (Sodium channel protein type 3 subunit alpha)

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