普瑞巴林治疗神经病理性疼痛的研究进展_谢菡

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783.(收稿日期:2011 02 2

8) 作者单位:

210008 南京市,中国药科大学临床药学专业(谢菡);南京大学医学院附属鼓楼医院镇痛科(陆丽娟)

通信作者:陆丽娟,Email:932200932@qq

.com普瑞巴林治疗神经病理性疼痛的研究进展

谢菡 陆丽娟

神经病理性疼痛是临床疼痛治疗的难点之一,新型抗癫痫药物加巴喷丁、

普瑞巴林等的出现为神经病理性疼痛的治疗提供了新的选择。普瑞巴林是继加巴喷丁之后的又一治疗神经病理性疼痛的抗癫痫药,可与中枢神经系统电压依赖性钙通道的I型α2-δ亚基相结合,减少钙离子内流,从而减少兴奋性神经递质的释放,进而控制疼痛

[1]

。该药于2004

年在美国上市,在我国尚处于神经病理性疼痛的临床研究阶段,本文对其治疗神经病理性疼痛的基础研究和临床应用进行综述。

普瑞巴林的药理作用

普瑞巴林化学名为:(3S)-3-氨甲基-5-甲基己酸,分子式为:C8H17NO2,相对分子质量159.2道尔顿,结构与加巴喷丁类似。与加巴喷丁相比,普瑞巴林具有服药剂量低、服药

次数少和不良反应小等优点[

2]

。普瑞巴林为外消旋化合物,脂溶性高,不与血浆蛋白结合,容易通过血脑屏障。口服普瑞巴林后吸收迅速,其吸收部位主要在结肠近端,给药后约1h达峰浓度(Cmax),不同剂量普瑞巴林的口服生物利用度均为90%以上,口服后的表观分布容积为0.5L/kg,血药浓度与药物剂量为线性关系,消除半衰期为4.6~6.8h,不受剂量影响。口服后24~48h达到稳态,

无蓄积现象。普瑞巴林在体内几乎不代谢,约98%的药物以原型(代谢产物<2%)经肾脏排泄,模型拟合结果显示,单次给药剂

·

39·临床麻醉学杂志2012年1月第28卷第1期 J Clin Anesthesiol,January 

2012,Vol.28,No.1

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