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首页> 外文期刊>CNS drug reviews >The use of 4-aminopyridine (fampridine) in demyelinating disorders.
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The use of 4-aminopyridine (fampridine) in demyelinating disorders.

机译：4-氨基吡啶（fampridine）在脱髓鞘疾病中的用途。

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摘要

4-Aminopyridine (4-AP or fampridine) is a potassium channel-blocking agent that has been shown to restore conduction in focally demyelinated axons. A sustained-release matrix tablet form of 4-AP (fampridine-SR) is currently undergoing multicenter clinical trials in patients with multiple sclerosis or chronic spinal cord injury. This review describes the pharmacology and mechanisms of action of 4-AP, its pharmacokinetics in human subjects, and the outcomes of clinical trials employing either immediate-release or sustained-release formulations of the drug. The randomized clinical trials that have been completed to date indicate that K(+) channel blockade may prove to be a useful strategy for ameliorating central conduction deficits due to demyelination. Diverse neurological gains have been reported for both motor and sensory domains. At the present time, however, the clinical trials have not provided sufficiently robust or definitive evidence of efficacy to gain regulatory approval for the symptomatic management of patients with either multiple sclerosis or spinal cord injury.
机译：4-氨基吡啶（4-AP或fampridine）是一种钾通道阻滞剂，已显示可恢复局灶性脱髓鞘轴突的传导。目前正在对患有多发性硬化症或慢性脊髓损伤的患者进行4-AP缓释基质片剂（fampridine-SR）的多中心临床试验。这篇综述描述了4-AP的药理学和作用机理，其在人类受试者中的药代动力学以及采用药物的立即释放或持续释放制剂的临床试验结果。迄今为止已完成的随机临床试验表明，K（+）通道阻滞可能被证明是缓解因脱髓鞘而引起的中央传导不足的有用策略。据报道，运动和感觉领域都有不同的神经功能。但是，目前，临床试验尚未提供足够有力的或确凿的疗效证据，无法获得监管部门批准对多发性硬化症或脊髓损伤患者进行对症治疗。

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