Drug intelligence / Profile preview

bupivacaine + epinephrine + dexamethasone + dexmedetomidine

Development stage
Unknown
Lead developer
Montreal Jewish General Hospital
Modality
Small Molecules
Administration
Local Infiltration
01

Overview

This drug combination is a multi-component regional anesthetic solution used for parasternal blocks to manage postoperative pain following cardiac surgery, specifically coronary artery bypass grafting (CABG). It consists of the local anesthetic bupivacaine, the vasoconstrictor epinephrine, and two adjuncts: the corticosteroid dexamethasone and the alpha-2 adrenergic agonist dexmedetomidine. Bupivacaine provides the primary analgesic effect by blocking voltage-gated sodium channels, thereby inhibiting nerve impulse conduction. Epinephrine is included to induce local vasoconstriction, which slows the systemic absorption of the anesthetic and prolongs its duration of action. Dexamethasone and dexmedetomidine serve as perineural adjuncts that have been shown to further extend the duration of sensory blockade and improve the quality of postoperative analgesia. This specific formulation is being evaluated in clinical trials led by the Jewish General Hospital to determine its efficacy in providing long-acting pain relief and reducing opioid consumption after sternotomy.

Other names
Parasternal blocksParasternal block with adjunctsParasternal block with Bupivacaine 0.25% + Epinephrine 1:200,000 + Dexamethasone 5mg and Dexmedetomidine 50mcg
02

Targets

ADRA1A (α1A)NMDAR (Glutamate receptor ionotropic, NMDA)ADRA2A (α2A)NaV (Voltage-gated sodium channels)GR (Glucocorticoid receptor)

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