Drug intelligence / Profile preview

nefopam + propacetamol

Development stage
Unknown
Lead developer
Unither Pharmaceuticals
Modality
Small Molecules, Implantable Devices → Device-based Delivery → Drug Delivery Systems, Transdermal Patches → Device-based Delivery → Drug Delivery Systems, Inhalation Devices → Device-based Delivery → Drug Delivery Systems
Administration
Oral, Intravenous, Intramuscular
01

Overview

Nefopam + propacetamol is a combination analgesic therapy consisting of nefopam, a centrally acting non-opioid analgesic, and propacetamol, an injectable prodrug of paracetamol (acetaminophen). Nefopam inhibits the reuptake of serotonin, norepinephrine, and dopamine in the central nervous system and modulates pain through both central and peripheral mechanisms. Propacetamol is rapidly hydrolyzed to paracetamol after administration; paracetamol acts primarily by inhibiting prostaglandin synthesis in the CNS. The combination aims to provide synergistic or additive analgesic effects for acute postoperative pain management while reducing opioid requirements. Clinical studies have shown that combining nefopam with acetaminophen or its prodrug (propacetamol) enhances analgesia compared to either agent alone[5][6]. This approach may allow dose reduction of each drug while maintaining effective pain control.

02

Targets

HTR2C (5-hydroxytryptamine 2C receptor)DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)SERT (Sodium-dependent serotonin transporter)

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