Historical overview of the rationale for the pharmacological use of prolonged-release fampridine in multiple sclerosis

作者：Fernandez Oscar^*; Berger Thomas; Hartung Hans Peter; Putzki Norman

来源：Expert Review of Clinical Pharmacology, 2012, 5(6): 649-665.

DOI：10.1586/ECP.12.59

• 4-aminopyridine
• dalfampridine
• FAMPYRA (R)
• immediate-release fampridine
• multiple sclerosis
• prolonged-release fampridine
• walking impairment
• walking speed

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.

• 出版日期2012-11
• 单位Biogen Idec