Drug intelligence / Profile preview

ketorolac + nefopam

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Oral
01

Overview

Ketorolac + nefopam is a combination of two analgesic drugs used for the management of moderate to severe pain, particularly in postoperative settings. Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID) that exerts its effect primarily by inhibiting cyclooxygenase (COX) enzymes, thereby reducing prostaglandin synthesis and providing peripheral analgesia and anti-inflammatory effects. Nefopam is a centrally acting, non-opioid analgesic whose mechanism involves inhibition of monoamine reuptake (serotonin, norepinephrine, dopamine) and modulation of central pain pathways; it does not possess anti-inflammatory properties. The combination leverages the distinct mechanisms—peripheral action from ketorolac and central action from nefopam—to provide synergistic or additive analgesic effects while potentially reducing opioid requirements when used as part of multimodal pain management[1][4][5]. Studies suggest that this combination can offer effective postoperative pain control with an opioid-sparing effect[1][4].

Other names
ketorolac + nefopam
02

Targets

HTR2A (5-hydroxytryptamine receptor 2A)HTR2B (5-Hydroxytryptamine Receptor 2B)SERT (Sodium-dependent serotonin transporter)HTR2C (5-hydroxytryptamine 2C receptor)PGHS-1 (Prostaglandin G/H Synthase 1)DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)

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