Drug intelligence / Profile preview

bupivacaine + epinephrine + fentanyl

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Epidural, Intrathecal
01

Overview

This is a combination of three drugs—bupivacaine, epinephrine (adrenaline), and fentanyl—commonly used in regional anesthesia, particularly for epidural or spinal analgesia during labor, cesarean section, and postoperative pain management. - **Bupivacaine** is an amide-type local anesthetic that blocks voltage-gated sodium channels on neuronal membranes, inhibiting nerve impulse conduction and providing local or regional anesthesia[6][10]. - **Epinephrine** acts as a vasoconstrictor by stimulating alpha-adrenergic receptors. When added to local anesthetics like bupivacaine (and opioids like fentanyl), it reduces systemic absorption of the drugs at the injection site by constricting blood vessels. This prolongs the duration of action and enhances analgesic effects[4][5][7]. - **Fentanyl** is a potent synthetic opioid agonist at the mu-opioid receptor. It provides additional analgesia through central nervous system action[9]. The combination leverages synergistic effects between these agents to improve pain relief quality and duration while potentially reducing required doses of each component[1][4][5].

Other names
bupivacaine-fentanyl-epinephrineBFE mixture
02

Targets

MOR (Mu opioid receptor)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)ADRA1 (Alpha-1 adrenergic receptor family)

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