Curran Monique P, Wagstaff Antona J
Adis International Limited, Auckland, New Zealand.
CNS Drugs. 2003;17(13):975-82. doi: 10.2165/00023210-200317130-00004.
Gabapentin is a structural analogue of the neurotransmitter gamma-aminobutyric acid (GABA) approved for use in adults with postherpetic neuralgia. Gabapentin does not bind to GABA(A) or GABA(B) receptors. Its mechanism of action in humans is unclear, but may involve binding to alpha2delta calcium channel subunits in animal models. Reductions in the mean daily pain score from baseline to week 7 or 8 of treatment (primary endpoint) were significantly greater with gabapentin 1800-3600 mg/day than placebo therapy in two well designed trials in patients with postherpetic neuralgia. The proportion of responders (patients showing a > or =50% reduction in mean daily pain score at endpoint versus baseline) was significantly greater with gabapentin than placebo. Daily sleep rating scores, the Short Form McGill Pain Questionnaire (total pain scores), Patient and Clinician Global Impression of Change and measures on the Short Form-36 Health Survey (including physical functioning, role-physical, bodily pain, vitality or mental health) improved to a significantly greater extent with gabapentin than placebo. Adverse events associated with gabapentin in patients with postherpetic neuralgia were usually mild to moderate in intensity, with dizziness, somnolence and peripheral oedema being commonly reported.
加巴喷丁是神经递质γ-氨基丁酸（GABA）的结构类似物，已被批准用于治疗成人带状疱疹后神经痛。加巴喷丁不与GABA（A）或GABA（B）受体结合。其在人体内的作用机制尚不清楚，但在动物模型中可能涉及与α2δ钙通道亚基结合。在两项针对带状疱疹后神经痛患者的精心设计试验中，与安慰剂治疗相比，加巴喷丁1800 - 3600毫克/天在治疗第7周或第8周时（主要终点）使平均每日疼痛评分较基线水平降低的幅度显著更大。加巴喷丁治疗组的应答者比例（与基线相比，终点时平均每日疼痛评分降低≥50%的患者）显著高于安慰剂组。与安慰剂相比，加巴喷丁在每日睡眠评分、简短麦吉尔疼痛问卷（总疼痛评分）、患者和临床医生总体改善印象以及简短健康调查问卷36项（包括身体功能、身体角色、身体疼痛、活力或心理健康）方面的改善程度显著更大。带状疱疹后神经痛患者中与加巴喷丁相关的不良事件通常强度为轻至中度，常见的有头晕、嗜睡和外周水肿。
