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bupivacaine + clonidine + epinephrine + buprenorphine + dexamethasone
- Development stage
- Phase 1
- 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
ADRA1A (α1A)ADRA2A (α2A)GR (Glucocorticoid receptor)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)ADRA1 (Alpha-1 adrenergic receptor family)ADRB1 (β1)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)
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