Department of Anaesthesia, Section Pain Clinic, Ghent University Hospital, Ghent, Belgium.
CNS Drugs. 2010 Oct;24(10):867-81. doi: 10.2165/11536230-000000000-00000.
Flupirtine is a centrally acting, non-opioid analgesic that is available in a number of European countries for the treatment of a variety of pain states. The therapeutic benefits seen with flupirtine relate to its unique pharmacological properties. Flupirtine displays indirect NDMA receptor antagonism via activation of potassium channels and is the first representative of a pharmacological class denoted the 'selective neuronal potassium channel openers'. The generation of the M-current is facilitated by flupirtine via the opening of neuronal Kv7 potassium channels. The opening of these channels inhibits exaggerated neuronal action potential generation and controls neuronal excitability. Neuronal hyperexcitability is a physiological component of many pain states such as chronic pain, migraine and neurogenic pain. Although large-scale clinical trials are lacking, the clinical trial database available to date from smaller-scale studies, together with extensive clinical experience, indicate that flupirtine effectively reduces chronic musculoskeletal pain, migraine and neuralgias, amongst other types of pain. In addition, flupirtine produces, at recommended clinical doses, muscle-relaxing effects in the presence of abnormally increased muscle tension. Its analgesic and muscle-relaxant properties were comparable to tramadol and chlormezanone, respectively, in two prospective trials in patients with lower back pain. Cytoprotective, anti-apoptotic and antioxidant properties have also been associated with flupirtine use in a small number of studies to date. When provided as combination therapy with morphine, flupirtine increases the antinociceptive activity of morphine 4-fold. Flupirtine displays superior tolerability when compared with tramadol and pentazocine. The most common adverse effects associated with flupirtine use are drowsiness, dizziness, heartburn, dry mouth, fatigue and nausea. With respect to its molecular structure, mechanism of action and adverse event profile, flupirtine is a unique drug. Flupirtine is an analgesic with many potential therapeutic benefits that may prove useful in the treatment of many disease states.
氟吡汀是一种中枢作用的非阿片类镇痛药，在许多欧洲国家被用于治疗多种疼痛状态。氟吡汀的治疗益处与其独特的药理学特性有关。氟吡汀通过激活钾通道显示出间接的 NMDA 受体拮抗作用，是药理学上第一个被称为“选择性神经元钾通道开放剂”的代表药物。氟吡汀通过打开神经元 Kv7 钾通道促进 M 电流的产生。这些通道的开放抑制了过度的神经元动作电位产生，并控制了神经元的兴奋性。神经元的过度兴奋是许多疼痛状态的生理组成部分，如慢性疼痛、偏头痛和神经性疼痛。尽管缺乏大规模的临床试验，但迄今为止，来自较小规模研究的临床试验数据库以及广泛的临床经验表明，氟吡汀有效地减轻了慢性肌肉骨骼疼痛、偏头痛和神经痛等其他类型的疼痛。此外，在存在异常增加的肌肉张力的情况下，氟吡汀在推荐的临床剂量下产生肌肉松弛作用。在两项针对腰痛患者的前瞻性试验中，氟吡汀的镇痛和肌肉松弛作用分别与曲马多和氯美扎酮相当。迄今为止，少数研究还将细胞保护、抗细胞凋亡和抗氧化作用与氟吡汀的使用联系起来。当与吗啡联合治疗时，氟吡汀使吗啡的镇痛作用增加 4 倍。与曲马多和喷他佐辛相比，氟吡汀具有更好的耐受性。与氟吡汀使用相关的最常见不良反应是嗜睡、头晕、胃灼热、口干、疲劳和恶心。就其分子结构、作用机制和不良反应谱而言，氟吡汀是一种独特的药物。氟吡汀是一种具有许多潜在治疗益处的镇痛药，可能对治疗许多疾病状态有用。
