Bennett Michael I, Simpson Karen H
St Gemma's Hospice, Leeds, UK.
Palliat Med. 2004 Jan;18(1):5-11. doi: 10.1191/0269216304pm845ra.
This paper reviews the pharmacology and clinical effectiveness of gabapentin in the treatment of neuropathic pain. Gabapentin has antihyperalgesic and antiallodynic properties but does not have significant actions as an anti-nociceptive agent. Its mechanisms of action appear to be a complex synergy between increased GABA synthesis, non-NMDA receptor antagonism and binding to the alpha2delta subunit of voltage dependent calcium channels. The latter action inhibits the release of excitatory neurotransmitters. Clinically, several large randomized controlled trials have demonstrated its effectiveness in the treatment of a variety of neuropathic pain syndromes. Patients with neuropathic pain can expect a mean reduction in pain score of 2.05 points on an 11 point numerical rating scale compared with a reduction of 0.94 points if they had taken the placebo. Around 30% of patients can expect to achieve more than 50% pain relief and a similar number will also experience minor adverse events; the most common of which are somnolence and dizziness. In patients with neuropathic pain due to cancer, higher response rates might be observed with gabapentin when administered with opioids because of a synergistic interaction.
本文综述了加巴喷丁治疗神经性疼痛的药理学及临床疗效。加巴喷丁具有抗痛觉过敏和抗异常性疼痛的特性，但作为一种抗伤害感受剂，其作用并不显著。其作用机制似乎是增加γ-氨基丁酸（GABA）合成、非N-甲基-D-天冬氨酸（NMDA）受体拮抗以及与电压依赖性钙通道的α2δ亚基结合之间的复杂协同作用。后一种作用抑制兴奋性神经递质的释放。临床上，多项大型随机对照试验已证明其在治疗多种神经性疼痛综合征方面的有效性。与服用安慰剂相比，神经性疼痛患者在11分数字评分量表上的疼痛评分平均降低2.05分，而服用安慰剂的患者疼痛评分平均降低0.94分。约30%的患者有望实现超过50%的疼痛缓解，且有相似比例的患者会经历轻微不良事件；其中最常见的是嗜睡和头晕。在因癌症导致神经性疼痛的患者中，加巴喷丁与阿片类药物联合使用时，由于协同相互作用，可能会观察到更高的缓解率。
