Drug intelligence / Profile preview

bupivacaine + dexamethasone + epinephrine

Development stage
Phase 4
Lead developer
Leiters Health
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Local Infiltration, Perineural, Epidural, Intraarticular
01

Overview

This is a compounded, sterile, preservative-free combination of three non-opioid drugs—bupivacaine hydrochloride (a long-acting amide local anesthetic), dexamethasone sodium phosphate (a synthetic glucocorticoid corticosteroid), and epinephrine (adrenaline, a vasoconstrictor)—formulated for use in regional anesthesia and analgesia. The combination is designed to provide prolonged pain relief while reducing opioid requirements. Bupivacaine blocks voltage-gated sodium channels in neuronal membranes to inhibit nerve impulse transmission and produce local anesthesia. Dexamethasone acts as an anti-inflammatory agent by binding to the glucocorticoid receptor and modulating gene expression, thereby reducing inflammation and prolonging the duration of nerve block analgesia. Epinephrine acts on adrenergic receptors causing vasoconstriction at the injection site, which decreases systemic absorption of bupivacaine, prolongs its effect, and reduces bleeding risk[1][4][5][10]. This preparation is used primarily for surgical anesthesia or postoperative pain management.

Other names
bupivacaine/dexamethasone/epinephrinebupivacaine dexamethasone plus epinephrine
02

Targets

ADRA1A (α1A)ADRB2 (β2)GR (Glucocorticoid receptor)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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