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bupivacaine + morphine + ketamine

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intrathecal, Epidural, Intravenous, Intraarticular, Regional/Local Infiltration
01

Overview

This is a combination of three drugs—bupivacaine, morphine, and ketamine—used primarily for enhanced postoperative or chronic pain management. Bupivacaine is an amide-type local anesthetic that blocks voltage-gated sodium channels to inhibit nerve impulse transmission, providing regional anesthesia and analgesia. Morphine is a classic opioid agonist at the mu-opioid receptor, producing potent analgesia by inhibiting nociceptive neurotransmission in the central nervous system. Ketamine acts as a non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, reducing central sensitization and opioid tolerance while also providing additional analgesic effects. The combination aims to achieve superior pain control with reduced opioid consumption and side effects compared to monotherapy. This regimen has been studied in various settings including intrathecal (spinal), epidural, intravenous, and intraarticular administration for perioperative pain control or refractory chronic pain[1][2][10].

02

Targets

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

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