Drug intelligence / Profile preview

nefopam

Development stage
Phase 4
Lead developer
Rivopharm
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Nefopam is a centrally acting, non-opioid analgesic used for the relief of moderate to severe pain, including acute and chronic pain such as post-operative pain, dental pain, musculoskeletal pain, acute traumatic pain, and cancer-related pain. It is structurally related to orphenadrine and diphenhydramine. Nefopam's mechanism of action is not fully understood but involves inhibition of the reuptake of serotonin, noradrenaline (norepinephrine), and dopamine in the central nervous system. It also blocks sodium and calcium channels in the CNS. Unlike opioids, it does not cause respiratory depression or significant abuse potential but can cause side effects such as nausea, dizziness, sweating, tachycardia, anticholinergic effects (e.g., dry mouth), confusion (especially in elderly), hallucinations at higher doses or overdose. Nefopam may be used when other analgesics are ineffective or contraindicated[2][3][4][5][6].

Brand names
Acupan
Other names
nefopam hydrochloride
02

Targets

SERT (Sodium-dependent serotonin transporter)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)ADRA1A (α1A)NaV (Voltage-gated sodium channels)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)DRD1 (Dopamine D1 Receptor)DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)HTR2B (5-Hydroxytryptamine Receptor 2B)

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