Drug intelligence / Profile preview

bupivacaine + dexmedetomidine + fentanyl

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intrathecal, Epidural
01

Overview

This is a combination of three drugs—bupivacaine, dexmedetomidine, and fentanyl—used primarily as an intrathecal or epidural anesthetic mixture for surgical anesthesia and postoperative analgesia. - **Bupivacaine** is a long-acting amide-type local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, inhibiting nerve impulse transmission and providing regional anesthesia. - **Dexmedetomidine** is a highly selective alpha-2 adrenergic receptor agonist that acts centrally to produce sedation, anxiolysis, and analgesia by inhibiting norepinephrine release in the spinal cord. It also enhances the quality and duration of sensory/motor block when used as an adjuvant to local anesthetics[1][2][3][5][8]. - **Fentanyl** is a potent synthetic opioid agonist at the mu-opioid receptor, providing rapid-onset analgesia with minimal hemodynamic effects when administered neuraxially[1][3][4]. The combination aims to maximize intraoperative anesthesia quality and prolong postoperative pain relief while minimizing opioid consumption. Studies show that adding dexmedetomidine or fentanyl to bupivacaine improves block characteristics; using all three may further enhance duration of sensory/motor blockade and reduce rescue analgesic requirements after surgery[1][8].

02

Targets

MOR (Mu opioid receptor)ADRA2A (α2A)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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