Institute of Clinical Neurosciences, Hospital Regional Universitario Carlos Haya, Spain.
Expert Rev Clin Pharmacol. 2012 Nov;5(6):649-65. doi: 10.1586/ecp.12.59. Epub 2012 Nov 13.
Multiple sclerosis is a progressive demyelinating neurological disease resulting in long-term disability, commonly manifesting in walking impairment and reduced quality of life. The use of the potassium channel blocker fampridine, chemically 4-aminopyridine, as an immediate-release formulation to improve action potential conduction in demyelinated axons was hampered by adverse events, including seizures. The prolonged-release formulation of fampridine (known as modified- or sustained-release fampridine in some countries and dalfampridine extended release in the USA) has a longer apparent half-life and a lower peak plasma concentration versus immediate-release fampridine formulations, sustaining its duration of action and reducing the incidence of adverse events. Prolonged-release fampridine is the first drug specifically licensed to improve walking in patients with multiple sclerosis, and has been shown to consistently improve walking ability in a third of patients. Prolonged-release fampridine Timed-Walk Responders showed both clinically significant improvements in walking speed and in patient-reported walking ability.
多发性硬化症是一种进行性脱髓鞘神经疾病，导致长期残疾，常见表现为行走障碍和生活质量下降。钾通道阻滞剂 4-氨基吡啶（化学名：氨吡啶）作为一种即时释放制剂，用于改善脱髓鞘轴突中的动作电位传导，但由于不良反应（包括癫痫发作）而受到限制。氨吡啶的缓释制剂（在某些国家称为改良或持续释放氨吡啶，在美国称为 dalfampridine 延长释放）具有更长的表观半衰期和更低的峰血浆浓度，与即时释放制剂相比，可延长其作用持续时间并降低不良反应发生率。缓释氨吡啶是第一种专门获准用于改善多发性硬化症患者行走能力的药物，已被证明可使三分之一的患者持续改善行走能力。缓释氨吡啶定时行走应答者在行走速度和患者报告的行走能力方面均表现出临床显著改善。
