Drug intelligence / Profile preview

Bupivacaine, epinephrine, dexamethasone, and clonidine combination

Development stage
Phase 4
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Perineural
01

Overview

This is a combination of four agents used in peripheral nerve blocks to provide extended analgesia. Bupivacaine is an amide local anesthetic that blocks nerve impulse generation and conduction by inhibiting voltage-gated sodium channels[8]. Epinephrine acts as a vasoconstrictor that prolongs the duration of local anesthetics and serves as a marker for intravascular injections[3]. Dexamethasone is a corticosteroid that significantly extends the duration of sensory and motor blockade when added to local anesthetics[1][4]. Clonidine is an alpha-2 adrenergic agonist that enhances and prolongs the analgesic effects of local anesthetics[3][6]. When combined, these agents work synergistically to provide superior analgesia with prolonged duration. Studies have shown that adding dexamethasone to a bupivacaine-epinephrine-clonidine interscalene block significantly prolongs sensory block (1457 vs. 833 minutes) and motor blockade (1374 vs. 827 minutes) compared to control groups, while also reducing opioid requirements in the first 24 hours post-procedure[1].

Other names
dexamethasone + clonidine + bupivacaine + adrenaline
02

Targets

ADRA1A (α1A)ADRA2A (α2A)GR (Glucocorticoid receptor)KCNQ1 (Potassium voltage-gated channel subfamily KQT member 1)NaV (Voltage-gated sodium channels)

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