Drug intelligence / Profile preview

bupivacaine + dextrose + fentanyl + morphine

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

Overview

This is a combination drug formulation containing bupivacaine, dextrose, fentanyl, and morphine. It is used primarily for intrathecal (spinal) or epidural administration to provide regional anesthesia and analgesia, especially in obstetric (labor), perioperative, and postoperative pain management settings. Bupivacaine is an amide-type local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, inhibiting nerve impulse transmission and producing sensory and motor block. Dextrose serves as a baricity modifier to create hyperbaric or hypobaric solutions for targeted spinal anesthesia distribution. Fentanyl is a potent lipophilic opioid agonist at the mu-opioid receptor providing rapid-onset analgesia; morphine is a hydrophilic opioid agonist at the mu-opioid receptor with slower onset but longer duration of action. The combination leverages synergistic effects between local anesthetics and opioids to enhance analgesic efficacy while potentially reducing individual drug doses and side effects[1][2][4][5][6][7].

02

Targets

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

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