Ide Yasuo
Department of Anesthesia, Toho University Sakura Medical Center, Sakura 285-8741.
Masui. 2013 Jul;62(7):808-13.
Pregabalin has been available in Japan since June 2010 for neuropathic pain. The adverse effects of pregabalin might be serious, and one must start at minimal doses and increase gradually to effective doses with enough explanation to patients. Pregabalin is a derivative of y-aminobutyric acid (GABA), but it has no effects on GABA receptors. Pregabalin reduces allodynia and hyperalgesia that are main symptoms of neuropathic pain. There are reports about the supportive effects of pregabalin for perioperative analgesic action of opioids. In the spinal nerve ligation (SNL) model, mRNA of alpha2delta-1 subunit of voltage gated calcium channels (VGCCs) is increased in the dorsal root ganglion (DRG) and alpha2delta-1 subunit of the spinal dorsal horn is increased. The effects of pregabalin is to bind alpha2delta-1 subunit and normalize the numbers of VGCCs at neuron surface and decreases neurotransmission, especially by excitatory amino acid. The descending facilitating serotonergic system from rostral ventromedial medulla may have effects on the occurrence and maintenance for the chronic pain. New drugs with less adverse effects may be developed.
普瑞巴林自2010年6月起在日本被用于治疗神经性疼痛。普瑞巴林的不良反应可能很严重，必须从最小剂量开始，并在向患者充分解释的情况下逐渐增加至有效剂量。普瑞巴林是γ-氨基丁酸（GABA）的衍生物，但它对GABA受体没有作用。普瑞巴林可减轻作为神经性疼痛主要症状的异常性疼痛和痛觉过敏。有报道称普瑞巴林对阿片类药物的围手术期镇痛作用有辅助效果。在脊神经结扎（SNL）模型中，背根神经节（DRG）中电压门控钙通道（VGCCs）的α2δ-1亚基的信使核糖核酸（mRNA）增加，脊髓背角的α2δ-1亚基也增加。普瑞巴林的作用是结合α2δ-1亚基，使神经元表面的VGCCs数量正常化，并减少神经传递，尤其是通过兴奋性氨基酸的传递。来自延髓头端腹内侧的下行易化5-羟色胺能系统可能对慢性疼痛的发生和维持有影响。可能会研发出不良反应较少的新药。
