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bupivacaine + morphine + ketorolac

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intraarticular, Infiltration, Epidural, Perineural
01

Overview

This is a combination of three drugs—bupivacaine, morphine, and ketorolac—used primarily for multimodal analgesia in perioperative and postoperative settings. - **Bupivacaine** is an amide-type local anesthetic that blocks voltage-gated sodium channels on neuronal membranes, inhibiting nerve impulse transmission and providing local or regional anesthesia[7][8]. - **Morphine** is an opioid analgesic that acts as an agonist at the mu-opioid receptor, modulating pain perception in the central nervous system. - **Ketorolac** is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis to provide analgesic and anti-inflammatory effects. The combination leverages synergistic mechanisms to enhance pain relief while potentially reducing the required doses of each component and minimizing side effects associated with higher single-agent dosing. This regimen has been studied for intra-articular injection after orthopedic procedures (such as knee arthroscopy), transversus abdominis plane block after gynecological surgery, and other surgical contexts[1][2][3][4]. The addition of morphine and ketorolac to bupivacaine has been shown to improve postoperative pain control, reduce opioid consumption post-surgery, prolong duration of analgesia, improve patient satisfaction with pain management, and facilitate earlier mobilization without significantly increasing adverse events[1][2][3][4].

02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)MOR (Mu opioid receptor)

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