Tzellos T G, Papazisis G, Toulis K A, Sardeli Ch, Kouvelas D
Department of Pharmacology, School of Medicine, Aristotle University of Thessaloniki, Greece.
Hippokratia. 2010 Apr;14(2):71-5.
Gabapentin (GP) and pregabalin (PB) are structurally related compounds and their predominant mechanism of action is the inhibition of calcium currents via high-voltage-activated channels containing the a2d-1 subunit. A2delta ligands are approved for the treatment of pain of diabetic neuropathy and post-herpetic neuralgia in adults and as adjunctive therapy of partial seizures in children. Recently, pregabalin has been approved for treatment of anxiety disorders in Europe. Besides their already approved indications both drugs are promising treatment options for a number of different serious and debilitating diseases, as fibromyalgia, neuropathic pain of spinal cord injury, hot flushes, and essential tremor. In the present review, the unique mechanism of action of the above drugs is critically analyzed and evidence for their future use is provided. Gabapentin and pregabalin can be treatment options for these disorders, however, a clear comparison between the two drugs can not be performed, since there is no direct comparison study. The most common side effects are dizziness and somnolence which are also the most frequent reasons for withdrawal. Recommendations for future studies should include assessment of ideal titration period for GP and PB to reduce incidence of somnolence and dizziness and increase tolerability, cost-effectiveness and dose-response analysis of PB and GP and direct comparison of the two drugs.
加巴喷丁（GP）和普瑞巴林（PB）是结构相关的化合物，它们的主要作用机制是通过含有α2δ-1亚基的高电压激活通道抑制钙电流。α2δ配体已被批准用于治疗成人糖尿病性神经病变疼痛和带状疱疹后神经痛，并作为儿童部分性癫痫发作的辅助治疗。最近，普瑞巴林在欧洲已被批准用于治疗焦虑症。除了它们已获批的适应症外，这两种药物对于许多不同的严重和使人衰弱的疾病，如纤维肌痛、脊髓损伤性神经病理性疼痛、潮热和特发性震颤，都是有前景的治疗选择。在本综述中，对上述药物独特的作用机制进行了批判性分析，并提供了它们未来应用的证据。加巴喷丁和普瑞巴林可以作为这些疾病的治疗选择，然而，由于没有直接比较研究，无法对这两种药物进行明确比较。最常见的副作用是头晕和嗜睡，这也是停药的最常见原因。未来研究的建议应包括评估加巴喷丁和普瑞巴林的理想滴定期，以降低嗜睡和头晕的发生率，提高耐受性、成本效益以及对普瑞巴林和加巴喷丁进行剂量反应分析，并对这两种药物进行直接比较。
