Drug intelligence / Profile preview

paracetamol + nefopam

Development stage
Unknown
Lead developer
Unither Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Paracetamol + nefopam is an investigational fixed-dose or co-administered combination of two non-opioid analgesics being studied by the University Hospital, Clermont-Ferrand for the management of pain. Paracetamol (acetaminophen) is a widely used analgesic and antipyretic that primarily inhibits cyclooxygenase (COX) enzymes in the central nervous system. Nefopam is a centrally-acting analgesic, chemically distinct from opioids and NSAIDs, that functions as a triple monoamine reuptake inhibitor (serotonin, norepinephrine, and dopamine) and modulates voltage-gated sodium and calcium channels. Preclinical evidence indicates that the combination of these two agents produces a synergistic (supra-additive) antinociceptive effect, which may provide superior pain relief or allow for dose reduction of the individual components to minimize side effects such as hepatotoxicity (associated with paracetamol) or tachycardia and sweating (associated with nefopam). A Phase 1 clinical trial was initiated to evaluate the pharmacokinetic interactions and safety profile of this combination in healthy volunteers.

Other names
acetaminophen + nefopamparacetamol and nefopam combination
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)DAT (Dopamine plasma membrane transport protein)CaV (Voltage-gated calcium channel protein complex)PGHS-1 (Prostaglandin G/H Synthase 1)HTR2C (5-hydroxytryptamine 2C receptor)SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)NaV (Voltage-gated sodium channels)

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