López-Trigo J, Sancho Rieger J
Servicio de Neurología, Consorcio Hospital General Universitario, Valencia. neurofisiologia_hgva@es
Neurologia. 2006 Mar;21(2):96-103.
Neuropathic pain is a condition affecting a significant proportion of the world's population. Many therapeutic drugs have been used. They achieve less than satisfactory results and are associated to common side effects that affect the daily life of patients. Pregabalin is a new drug that has been shown to be effective for treating partial epilepsy and peripheral neuropathic pain in clinical trials. It is a structural, but not functional, analogue of GABA. It acts as a ligand of the alpha2-delta subunit, a protein associated to the voltage-dependent calcium channels. Modulation of these channels decreases calcium entry into nerve endings, resulting in a decreased release of several excitatory neurotransmitters. Pregabalin had a linear pharmacokinetics with little variability between the different subjects. It does not bind to plasma proteins, has no liver metabolism, and is excreted trough the kidneys. Few interactions with other drugs may be expected based on these characteristics. In clinical trials, pregabalin has been shown to be effective in postherpetic neuralgia and painful diabetic neuropathy at doses ranging from 150-600 mg/day. The analgesic effects of pregabalin occur in the first few days of treatment and are sustained over time. Side effects are few; most are transient and well-tolerated by patients, and the treatment discontinuation rate is minimal.
神经性疼痛是一种影响着世界上相当一部分人口的疾病。人们已经使用了许多治疗药物。但这些药物的效果并不理想，而且还伴有影响患者日常生活的常见副作用。普瑞巴林是一种新药，在临床试验中已显示出对治疗部分癫痫和周围神经性疼痛有效。它是γ-氨基丁酸（GABA）的结构类似物，但不是功能类似物。它作为α2-δ亚基的配体发挥作用，α2-δ亚基是一种与电压依赖性钙通道相关的蛋白质。对这些通道的调节可减少钙进入神经末梢，从而导致几种兴奋性神经递质的释放减少。普瑞巴林具有线性药代动力学，不同个体之间的变异性很小。它不与血浆蛋白结合，没有肝脏代谢，通过肾脏排泄。基于这些特性，预计它与其他药物的相互作用很少。在临床试验中，普瑞巴林已显示出在150 - 600毫克/天的剂量范围内对带状疱疹后神经痛和糖尿病性神经痛有效。普瑞巴林的镇痛作用在治疗的最初几天就会出现，并会持续一段时间。副作用很少；大多数是短暂的，患者耐受性良好，停药率极低。
