Drug intelligence / Profile preview

bupivacaine + clonidine + epinephrine + buprenorphine + dexamethasone

Development stage
Unknown
Lead developer
Wake Forest University Health Sciences
Modality
Small Molecules
Administration
Perineural
01

Overview

This drug is a multimodal analgesic combination consisting of the local anesthetic bupivacaine and four adjuvants: clonidine, epinephrine, buprenorphine, and dexamethasone. Developed by Wake Forest University Health Sciences, it is specifically designed for perineural administration (e.g., adductor canal and iPACK blocks) to provide prolonged postoperative pain relief following major orthopedic surgeries such as total knee arthroplasty. Each component serves a specific role: bupivacaine provides the primary nerve block by inhibiting sodium channels; clonidine (an alpha-2 agonist) and dexamethasone (a corticosteroid) extend the duration of sensory blockade; epinephrine acts as a vasoconstrictor to limit systemic absorption; and buprenorphine (a partial opioid agonist) further enhances the analgesic effect. This "cocktail" approach aims to provide superior or non-inferior analgesia compared to liposomal bupivacaine formulations.

Other names
Bupivacaine, Clonidine, Epinephrine, Buprenorphine and Dexamethasone Combination
02

Targets

KOR (Kappa opioid receptor)MOR (Mu opioid receptor)ADRA1A (α1A)NaV (Voltage-gated sodium channels)GR (Glucocorticoid receptor)ADRA2A (α2A)

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