Department of Physical Medicine and Rehabilitation, The University of Western Ontario, London, ON, Canada.
Neuropsychiatr Dis Treat. 2011;7:229-39. doi: 10.2147/NDT.S10469. Epub 2011 Apr 28.
Dalfampridine extended release (ER) 10 mg is an oral tablet form of the potassium (K(+)) channel-blocking compounded dalfampridine, also known as fampridine, and chemically 4-aminopyridine or 4-AP, which received regulatory approval in the United States for the treatment of walking in patients with multiple sclerosis (MS) in January 2010. Two pivotal Phase 3 clinical trials demonstrated significant improvements in walking in patients with the four primary forms of MS following administration of dalfampridine ER tablets 10 mg twice daily. The drug is thought to act by restoring conduction in focally demyelinated axons and by enhancing neurotransmission, thereby leading to improved neurological function. This review describes how dalfampridine represents a new pharmacotherapeutic approach to the clinical management of mobility impairment. It describes the mechanism of action and chemistry of dalfampridine ER, its pharmacokinetics, tolerability, and side effects, and the outcomes of multicenter trials showing its efficacy in improving walking speed. Clinician and patient global assessments, as well as patient self-assessment of the impact of MS on their gait disability, confirm clinically relevant benefit from the therapy. Patients tolerate the drug well and their improvement in terms of household and community ambulation, inferred from analysis of pooled data from several studies, is likely to translate into benefits in the performance of instrumental activities of daily living and a reduction in the neuropsychiatric burden of disease.
地夫可特缓释片(ER)10 毫克是一种钾(K(+))通道阻断化合物地夫可特的口服片剂,也称为奋乃静,化学上称为 4-氨基吡啶或 4-AP,于 2010 年 1 月在美国获得监管批准,用于治疗多发性硬化症(MS)患者的行走。两项主要的 3 期临床试验表明,每日两次服用地夫可特 ER 片剂 10 毫克后,四种主要形式的 MS 患者的行走能力有显著改善。该药物被认为通过恢复局部脱髓鞘轴突的传导和增强神经传递而起作用,从而改善神经功能。这篇综述描述了地夫可特如何代表一种新的药物治疗方法来管理移动障碍。它描述了地夫可特 ER 的作用机制和化学性质、药代动力学、耐受性和副作用,以及多项临床试验的结果表明其在提高行走速度方面的疗效。临床医生和患者的整体评估,以及患者对 MS 对其步态障碍影响的自我评估,都证实了该治疗的临床相关益处。患者对药物耐受良好,从几项研究的汇总数据分析推断,他们在家庭和社区活动中的改善可能转化为日常生活活动工具性能力的提高,并减轻神经精神疾病负担。