Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala-147002, India.
Curr Neuropharmacol. 2014 Jan;12(1):44-56. doi: 10.2174/1570159X1201140117162802.
Pregabalin is an antagonist of voltage gated Ca2+ channels and specifically binds to alpha-2-delta subunit to produce antiepileptic and analgesic actions. It successfully alleviates the symptoms of various types of neuropathic pain and presents itself as a first line therapeutic agent with remarkable safety and efficacy. Preclinical studies in various animal models of neuropathic pain have shown its effectiveness in treating the symptoms like allodynia and hyperalgesia. Clinical studies in different age groups and in different types of neuropathic pain (peripheral diabetic neuropathy, fibromyalgia, post-herpetic neuralgia, cancer chemotherapy-induced neuropathic pain) have projected it as the most effective agent either as monotherapy or in combined regimens in terms of cost effectiveness, tolerability and overall improvement in neuropathic pain states. Preclinical studies employing pregabalin in different neuropathic pain models have explored various molecular targets and the signaling systems including Ca2+ channel-mediated neurotransmitter release, activation of excitatory amino acid transporters (EAATs), potassium channels and inhibition of pathways involving inflammatory mediators. The present review summarizes the important aspects of pregabalin as analgesic in preclinical and clinical studies as well as focuses on the possible mechanisms.
普瑞巴林是电压门控钙通道的拮抗剂，特别与α-2-δ亚基结合产生抗癫痫和镇痛作用。它成功地缓解了各种类型的神经性疼痛症状，并作为一种具有显著安全性和疗效的一线治疗药物。在各种神经性疼痛动物模型的临床前研究中，它在治疗痛觉过敏和痛觉过强等症状方面显示出了有效性。在不同年龄组和不同类型的神经性疼痛（周围性糖尿病性神经病、纤维肌痛、疱疹后神经痛、癌症化疗引起的神经性疼痛）的临床研究中，它作为单药治疗或联合治疗方案，在成本效益、耐受性和神经性疼痛状态的整体改善方面，都被认为是最有效的药物。在不同神经性疼痛模型中使用普瑞巴林的临床前研究已经探索了各种分子靶点和信号转导系统，包括钙通道介导的神经递质释放、兴奋性氨基酸转运体（EAATs）的激活、钾通道和抑制涉及炎症介质的途径。本综述总结了普瑞巴林作为临床前和临床研究中的镇痛剂的重要方面，并重点介绍了可能的机制。
