Nefopam: A Comprehensive Pharmacological and Clinical Review

I. Introduction and Overview

A. Drug Identification

Nefopam is a centrally acting analgesic agent that is structurally and pharmacologically distinct from opioid analgesics and non-steroidal anti-inflammatory drugs (NSAIDs).[1] It is classified as a small molecule drug [2] and is marketed under various brand names, including Acupan.[1] For precise identification in scientific literature and databases, Nefopam is assigned the DrugBank ID DB12293 [1] and the Chemical Abstracts Service (CAS) Number 13669-70-0 for the base compound.[2] The hydrochloride salt, a common pharmaceutical form, is identified by CAS Number 23327-57-3.[2] These identifiers are crucial for unambiguous referencing in research and clinical practice.

B. Brief Summary of Therapeutic Use

Nefopam is primarily indicated for the relief of moderate to severe pain.[1] Its application is particularly prominent in acute pain settings, such as post-operative pain, dental pain, musculoskeletal pain, and certain types of cancer-related pain.[7] While its role in chronic pain management is less well-established, it is sometimes utilized when other analgesics are contraindicated or have proven ineffective.[1]

C. Historical Background and Development

Nefopam, a benzoxazocine derivative, was developed in the 1960s and initially introduced under the name Fenazoxine.[1] Its early therapeutic exploration was quite broad, with initial applications including the management of shivering, use as a muscle relaxant, and even as an antidepressant.[1] Over time, its utility as an analgesic agent became more distinctly recognized, leading to its current primary indication for pain relief.