Drug intelligence / Profile preview

bupivacaine + epinephrine + dexamethasone + clonidine

Development stage
Phase 4
Lead developer
Tufts Medical Center
Modality
Small Molecules
Administration
Infiltration
01

Overview

This drug is a multi-component analgesic solution used for regional anesthesia and postoperative pain management, specifically in the context of Erector Spinae Plane (ESP) blocks. It consists of the local anesthetic bupivacaine combined with three adjuvants: epinephrine, dexamethasone, and clonidine. Bupivacaine provides the primary anesthetic effect by blocking voltage-gated sodium channels, thereby inhibiting nerve impulse conduction. Epinephrine acts as a vasoconstrictor to reduce systemic absorption and prolong the local effect. Dexamethasone, a synthetic glucocorticoid, and clonidine, an alpha-2 adrenergic agonist, are included as adjuvants to further extend the duration of the nerve block and enhance analgesic efficacy. This specific combination is utilized by Tufts Medical Center as a standard-of-care comparator in clinical trials evaluating the efficacy of liposomal bupivacaine for patients undergoing oncoplastic breast surgery.

Other names
standard bupivacaine cocktailbupivacaine mixed with epinephrine, dexamethasone, and clonidine
02

Targets

ADRA1A (α1A)ADRA2A (α2A)ADRB1 (β1)GR (Glucocorticoid receptor)NaV (Voltage-gated sodium channels)

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