Burgess J, Javed S, Frank B, Malik R A, Alam U
Diabetes and Endocrinology Research, Department of Eye and Vision Sciences, Institute of Ageing and Chronic Disease and the Pain Research Institute, University of Liverpool and Liverpool University Hospital NHS Foundation Trust, Liverpool, UK.
Institute of Cardiovascular Sciences, University of Manchester, Manchester, UK.
Drugs Today (Barc). 2020 Feb;56(2):135-149. doi: 10.1358/dot.2020.56.2.3100504.
Neuropathic pain (NeP) is a global cause of suffering and debilitation leading to significant morbidity and reduced quality of life. New treatments are needed to address the growing prevalence of NeP and its impact on sleep, mood and functionality. Mirogabalin besylate (mirogabalin, Tarlige) is a gabapentinoid therapy developed by Daiichi Sankyo which is approved in Japan for the treatment of postherpetic neuralgia and painful diabetic peripheral neuropathy. Mirogabalin has a potent pain-modulating effect with a unique high affinity and prolonged dissociation rate for the a2delta-1 subunit of voltage-gated calcium (Ca2+) channels (VGCCs) on the dorsal root ganglion resulting in more sustained analgesia compared with traditional gabapentinoids. Additionally, mirogabalin has a superior adverse events (AEs) profile due to a rapid dissociation from the a2delta-2 subunit of VGCCs potentially implicated in central nervous system-specific AEs. The most common AEs for mirogabalin are dizziness (approximately 8-16%), somnolence (approximately 6-24%) and headache (approximately 6-14%), with a lower incidence of constipation, nausea, diarrhea, vomiting, edema, fatigue and weight gain. Postmarketing studies are required to evaluate its analgesic durability and efficacy when combined with other antineuropathic agents such as tricyclics, duloxetine and tramadol/tapentadol.
神经性疼痛（NeP）是导致痛苦和身体衰弱的全球性病因，会引发严重的发病率并降低生活质量。需要新的治疗方法来应对NeP日益增长的患病率及其对睡眠、情绪和功能的影响。甲磺酸米罗加巴（米罗加巴，Tarlige）是由第一三共公司研发的一种加巴喷丁类药物，在日本被批准用于治疗带状疱疹后神经痛和疼痛性糖尿病周围神经病变。米罗加巴对背根神经节电压门控钙（Ca2+）通道（VGCCs）的α2δ-1亚基具有强大的疼痛调节作用，具有独特的高亲和力和延长的解离速率，与传统加巴喷丁类药物相比，可产生更持久的镇痛效果。此外，米罗加巴具有更好的不良事件（AEs）谱，因为它能迅速从可能与中枢神经系统特异性AEs有关的VGCCs的α2δ-2亚基上解离。米罗加巴最常见的AEs是头晕（约8-16%）、嗜睡（约6-24%）和头痛（约6-14%），便秘、恶心、腹泻、呕吐、水肿、疲劳和体重增加的发生率较低。需要进行上市后研究，以评估其与其他抗神经病变药物（如三环类药物、度洛西汀和曲马多/他喷他多）联合使用时的镇痛持久性和疗效。
