舒马曲坦是否能穿过动物和人类的血脑屏障？
Does sumatriptan cross the blood-brain barrier in animals and man?
机构信息
Department of Neurology, Faculty of Health Sciences, Danish Headache Center, Glostrup Hospital, University of Copenhagen, Glostrup, 2600 Copenhagen, Denmark.
出版信息
J Headache Pain. 2010 Feb;11(1):5-12. doi: 10.1007/s10194-009-0170-y. Epub 2009 Dec 10.
Abstract
Sumatriptan, a relatively hydrophilic triptan, based on several animal studies has been regarded to be unable to cross the blood-brain barrier (BBB). In more recent animal studies there are strong indications that sumatriptan to some extent can cross the BBB. The CNS adverse events of sumatriptan in migraine patients and normal volunteers also indicate a more general effect of sumatriptan on CNS indicating that the drug can cross the BBB in man. It has been discussed whether a defect in the BBB during migraine attacks could be responsible for a possible central effect of sumatriptan in migraine. This review suggests that there is no need for a breakdown in the BBB to occur in order to explain a possible central CNS effect of sumatriptan.
摘要
舒马曲坦是一种相对亲水的曲坦类药物，基于几项动物研究，它被认为不能穿过血脑屏障 (BBB)。在最近的一些动物研究中，有强有力的迹象表明舒马曲坦在某种程度上可以穿过 BBB。舒马曲坦在偏头痛患者和正常志愿者中的中枢神经系统不良反应也表明舒马曲坦对中枢神经系统有更广泛的影响，表明该药可以在人体内穿过 BBB。有人曾讨论偏头痛发作期间 BBB 的缺陷是否可能导致舒马曲坦在偏头痛中产生可能的中枢作用。这篇综述表明，没有必要发生 BBB 的破坏来解释舒马曲坦可能对中枢神经系统的影响。
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