Drug intelligence / Profile preview

lidocaine + bupivacaine + epinephrine + dexamethasone

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Local Infiltration, Peripheral Nerve Block, Epidural, Intrathecal, Intraarticular, Perineural
01

Overview

This is a compounded combination of four agents commonly used in local and regional anesthesia for surgical, dental, or pain management procedures. Lidocaine and bupivacaine are both amide-type local anesthetics; lidocaine provides rapid onset of anesthesia while bupivacaine offers prolonged duration. Epinephrine (adrenaline) is added as a vasoconstrictor to reduce systemic absorption of the anesthetics, prolong their effect, and decrease bleeding at the injection site. Dexamethasone is a synthetic glucocorticoid corticosteroid included to further prolong analgesia by reducing inflammation and possibly modulating nociceptive pathways. This combination aims to provide fast onset, long-lasting anesthesia/analgesia with reduced postoperative pain and inflammation[2][3][5].

02

Targets

ADRA1A (α1A)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)GR (Glucocorticoid receptor)SCN1B (Sodium channel regulatory subunit beta-1)

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