Drug intelligence / Profile preview

bupivacaine + meloxicam + ketorolac

Development stage
Preclinical
Lead developer
Heron Therapeutics
Modality
Small Molecules
Administration
Local (injection Into Surgical Site Or Tissue Block), Intravenous (ketorolac May Be Administered Iv In Some Protocols)
01

Overview

A combination of **bupivacaine**, **meloxicam**, and **ketorolac** consists of three agents with complementary mechanisms for multimodal pain management following surgery. - **Bupivacaine** is a local anesthetic that blocks sodium channels, preventing nerve impulse transmission and leading to localized numbness and loss of pain sensation. - **Meloxicam** is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) enzymes, decreasing prostaglandin synthesis and thereby mitigating inflammation and pain. - **Ketorolac** is another NSAID with strong analgesic properties, also acting through COX inhibition to reduce prostaglandin production. Used together (typically as a perioperative or postoperative formulation), this combination is intended to provide enhanced, sustained analgesia and reduce opioid requirements. The synergy arises from targeting both peripheral (inflammatory) and central (nervous) components of pain. While combinations of bupivacaine and meloxicam (e.g., Zynrelef) are marketed and studied for postsurgical pain[2][3][4][5][6], clinical trials have investigated bupivacaine combined with ketorolac for extended postoperative pain control[1]. However, a fixed product or standardized formulation combining all three ingredients has not appeared in regulatory databases or commercial offerings and may represent an investigational or off-label practice rather than a commercial product.

02

Targets

NaV alpha (Voltage-gated sodium channel alpha subunit family)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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