Fazekas Franz, Berger Thomas, Fabjan Tanja Hojs, Ledinek Alenka Horvat, Jakab Gábor, Komoly Samuel, Kraus Jörg, Kurča Egon, Kyriakides Theodoros, Lisý L'ubomír, Milanov Ivan, Panayiotou Panayiotis, Jazbec Sasa Sega, Taláb Radomír, Traykov Latchezar, Turčáni Peter, Vass Karl, Vella Norbert, Havrdová Eva
Department of Neurology, Medical University of Graz, Auenbruggerplatz 22, 8036 Graz, Austria.
Wien Med Wochenschr. 2012 Aug;162(15-16):354-66. doi: 10.1007/s10354-012-0123-y. Epub 2012 Aug 16.
Fingolimod is the first oral treatment of multiple sclerosis. It is the first-in-class sphingosine 1-phosphate receptor modulator that binds to sphingosine 1-phophate receptors on lymphocytes and via downregulation of the receptor prevents lymphocyte egress from lymphoid tissues into the circulation. This mechanism reduces the infiltration of potentially auto-aggressive lymphocytes into the central nervous system. Two large phase III studies with fingolimod have shown superior efficacy of the drug in two dosages compared to placebo and to weekly intramuscular injections of Interferon beta-1a. Among possible side effects of the drug is a transient bradycardia after the first dose of fingolimod including possible AV blockade and therefore monitoring of pulse rate and blood pressure for 6 h following the first application is needed. During treatment, attention has to be given to specific infections, elevated liver enzymes, and ophthalmologic changes. Recommendations on the use of fingolimod including safety aspects are given in this article.
芬戈莫德是第一种用于治疗多发性硬化症的口服药物。它是同类首创的鞘氨醇-1-磷酸受体调节剂,可与淋巴细胞上的鞘氨醇-1-磷酸受体结合,并通过受体下调阻止淋巴细胞从淋巴组织进入循环系统。这种机制减少了潜在的自身攻击性淋巴细胞向中枢神经系统的浸润。两项针对芬戈莫德的大型III期研究表明,与安慰剂以及每周一次肌肉注射干扰素β-1a相比,该药物在两种剂量下均具有更高的疗效。该药物可能的副作用包括首次服用芬戈莫德后出现短暂性心动过缓,包括可能的房室传导阻滞,因此首次用药后需要监测脉搏率和血压6小时。在治疗期间,必须关注特定感染、肝酶升高和眼科变化。本文给出了关于芬戈莫德使用的建议,包括安全方面。