Kim Kyung Hoon, Abdi Salahadin
Department of Anesthesia and Pain Medicine, School of Medicine, Pusan National University, Yangsan, Korea.
Department of Pain Medicine, Division of Anesthesiology and Critical Care, The University of Texas MD Anderson Cancer Center, Houston, TX, USA.
Korean J Pain. 2014 Apr;27(2):103-11. doi: 10.3344/kjp.2014.27.2.103. Epub 2014 Mar 28.
Nefopam (NFP) is a non-opioid, non-steroidal, centrally acting analgesic drug that is derivative of the non-sedative benzoxazocine, developed and known in 1960s as fenazocine. Although the mechanisms of analgesic action of NFP are not well understood, they are similar to those of triple neurotransmitter (serotonin, norepinephrine, and dopamine) reuptake inhibitors and anticonvulsants. It has been used mainly as an analgesic drug for nociceptive pain, as well as a treatment for the prevention of postoperative shivering and hiccups. Based on NFP's mechanisms of analgesic action, it is more suitable for the treatment of neuropathic pain. Intravenous administration of NFP should be given in single doses of 20 mg slowly over 15-20 min or with continuous infusion of 60-120 mg/d to minimize adverse effects, such as nausea, cold sweating, dizziness, tachycardia, or drowsiness. The usual dose of oral administration is three to six times per day totaling 90-180 mg. The ceiling effect of its analgesia is uncertain depending on the mechanism of pain relief. In conclusion, the recently discovered dual analgesic mechanisms of action, namely, a) descending pain modulation by triple neurotransmitter reuptake inhibition similar to antidepressants, and b) inhibition of long-term potentiation mediated by NMDA from the inhibition of calcium influx like gabapentinoid anticonvulsants or blockade of voltage-sensitive sodium channels like carbamazepine, enable NFP to be used as a therapeutic agent to treat neuropathic pain.
奈福泮（NFP）是一种非阿片类、非甾体类、中枢性镇痛药，它是无镇静作用的苯并恶唑嗪的衍生物，于20世纪60年代作为非那佐辛研发并为人所知。尽管奈福泮的镇痛作用机制尚未完全明确，但与三重神经递质（血清素、去甲肾上腺素和多巴胺）再摄取抑制剂及抗惊厥药的作用机制相似。它主要用作伤害性疼痛的镇痛药，也用于预防术后寒战和呃逆。基于奈福泮的镇痛作用机制，它更适合用于治疗神经性疼痛。静脉注射奈福泮时，应单次缓慢注射20mg，持续15 - 20分钟，或每日持续输注60 - 120mg，以尽量减少不良反应，如恶心、冷汗、头晕、心动过速或嗜睡。口服的常用剂量是每天三到六次，总计90 - 180mg。其镇痛的封顶效应取决于疼痛缓解机制，尚不确定。总之，最近发现的双重镇痛作用机制，即：a）通过类似于抗抑郁药的三重神经递质再摄取抑制实现下行性疼痛调制，以及b）像加巴喷丁类抗惊厥药那样通过抑制钙内流或像卡马西平那样阻断电压敏感性钠通道来抑制NMDA介导的长时程增强，使得奈福泮能够用作治疗神经性疼痛的治疗药物。
