Drug intelligence / Profile preview

bupivacaine + ketamine

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

Overview

Bupivacaine + ketamine is a non-branded combination of two pharmaceutical agents used primarily for enhanced local or regional anesthesia and postoperative analgesia. Bupivacaine is an amide-type local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, inhibiting nerve impulse conduction and providing anesthesia. Ketamine is a dissociative anesthetic that acts as an N-methyl-D-aspartate (NMDA) receptor antagonist, providing analgesic effects at subanesthetic doses. When combined, ketamine enhances the duration and efficacy of bupivacaine’s local anesthetic effect through both peripheral mechanisms (by prolonging nerve block) and central mechanisms (by reducing central sensitization to pain). This combination has been studied in various settings including wound infiltration, caudal epidural block, topical application for postoperative pain management, neuropathic pain syndromes, fibromyalgia, complex regional pain syndrome, osteoarthritis, herniorrhaphy surgery in adults and children[2][4][6][7][9]. The addition of ketamine to bupivacaine can significantly prolong the duration of analgesia without increasing adverse effects at optimal dosing.

Other names
bupivacaine and ketamineketamine and bupivacaine
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)NaV (Voltage-gated sodium channels)

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