Stump Patrick
Médico fisiatra do Instituto Lauro De Souza Lima de Bauru. Médico fisiatra do Grupo de Dor da Neurologia do HC da FMUSP.
Drugs Today (Barc). 2009 Oct;45 Suppl C:19-27.
Pregabalin (PGB), like its predecessor gabapentin, is a structural analogue (but not functional) of the gammaaminobutyric acid (GABA). PGB has analgesic, antoconvulsivant, and ansiolytic activities. Neuropathic pain (NP) initial recommended dose is 150 mg per day. Depending on the patient response or bodily resistance to the drug the initial dose can be increased up to 300 mg per day (divided in 2-3 daily doses) during a one-week period. PGB is quickly absorbed in the digestive system with high oral biodisponibility. The drug is eliminated almost exclusively by renal excretion (98%). PGB efficacy was evaluated by several studies by means of visual analog scales (VAS) in several NP conditions such as post-herpetic neuropathy (PHN) or painful diabetic neuropathy (PDN). When compared with placebo, PGB provided significant benefit with 150 mg doses in the treatment of PHN pain. In studies developed in patients with PDN, the significant difference between placebo and treatment group only was achieved in individuals with daily doses of 300 mg/day, and the response was clearly dose-dependent. Tolerability information obtained from a number of studies has shown that the drug has a very good safety and tolerability profile. Side effects were mild to moderate and dose-dependent. Based on controlled studies, the main adverse effects observed with PGB are dizziness (23.1%), drowsiness (14.6%), and peripheral aedema (10.4%). As these side effects are dosedependent, they can be easily managed by a simple dose reduction, with no need to discontinue the therapy. Thus, according to efficacy and tolerability data, PGB is an important therapeutic option in NP treatment.
普瑞巴林(PGB)与其前身加巴喷丁一样,是γ-氨基丁酸(GABA)的结构类似物(但非功能性类似物)。PGB具有镇痛、抗惊厥和抗焦虑活性。神经性疼痛(NP)的初始推荐剂量为每日150毫克。根据患者的反应或身体对药物的耐受性,初始剂量可在一周内增至每日300毫克(分2 - 3次服用)。PGB在消化系统中吸收迅速,口服生物利用度高。该药物几乎完全通过肾脏排泄(98%)。多项研究通过视觉模拟量表(VAS)在多种NP病症中评估了PGB的疗效,如疱疹后神经痛(PHN)或糖尿病性疼痛性神经病变(PDN)。与安慰剂相比,PGB在治疗PHN疼痛时,150毫克剂量可带来显著益处。在针对PDN患者开展的研究中,仅每日剂量为300毫克的个体中,安慰剂组与治疗组之间存在显著差异,且反应明显呈剂量依赖性。从多项研究中获得的耐受性信息表明,该药物具有非常良好的安全性和耐受性。副作用为轻度至中度且呈剂量依赖性。基于对照研究,使用PGB观察到的主要不良反应为头晕(23.1%)、嗜睡(14.6%)和外周水肿(10.4%)。由于这些副作用呈剂量依赖性,可通过简单减少剂量轻松控制,无需中断治疗。因此,根据疗效和耐受性数据,PGB是NP治疗中的重要治疗选择。