Drug intelligence / Profile preview

bupivacaine + ketofol

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous, Spinal, Intraarticular, Epidural, Perineural
01

Overview

Bupivacaine + ketofol is a combination of the local anesthetic bupivacaine and the sedative-analgesic mixture known as "ketofol" (a blend of ketamine and propofol). Bupivacaine acts primarily by blocking voltage-gated sodium channels in neuronal membranes, thereby inhibiting nerve impulse conduction and providing local or regional anesthesia[3][6][8]. Ketamine is an NMDA receptor antagonist that provides analgesia, sedation, and amnesia; it also has some activity at monoaminergic receptors and voltage-sensitive calcium channels[5]. Propofol is a short-acting intravenous anesthetic agent that potentiates GABA-A receptor activity. The combination "ketofol" (ketamine plus propofol) is used for procedural sedation due to its synergistic effects—propofol provides rapid onset sedation while ketamine offers analgesia with minimal respiratory depression. When combined with bupivacaine for regional or local anesthesia/analgesia protocols (such as spinal or intra-articular administration), this regimen aims to provide enhanced pain control during and after surgical procedures by leveraging both peripheral nerve blockade (bupivacaine) and central analgesic/sedative effects (ketamine-propofol)[1][2].

Other names
bupivacaine + ketofolbupivacaine + ketamine-propofolbupivacaine plus ketofol
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)GABRR (GABA-A receptor subunit rho)NaV (Voltage-gated sodium channels)

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