Löhle Matthias, Storch Alexander
Technische Universität Dresden, Department of Neurology, Fetscherstrasse 74, 01307 Dresden, Germany.
Expert Opin Pharmacother. 2008 Nov;9(16):2881-91. doi: 10.1517/14656566.9.16.2881.
The selective monoamine oxidase type B inhibitor selegiline is commonly administered as medical treatment to patients suffering from Parkinson's disease. The clinical value of conventional selegiline is, however, compromised by extensive first-pass metabolism, which reduces its bioavailability and leads to the production of possibly harmful methamfetamine metabolites. This review aims to evaluate a novel, orally disintegrating formulation of selegiline by examining scientific evidence from previous pharmacological and clinical studies. As a result of improved bioavailability, orally disintegrating selegiline can be administered at lower doses than conventional selegiline with similar clinical effect. It also leads to less variable selegiline blood concentrations and produces significantly less methamfetamine metabolites. We conclude that this novel formulation offers an interesting treatment option, especially for patients who report adverse events after initial treatment with conventional selegiline or who suffer from swallowing difficulties.
选择性单胺氧化酶B型抑制剂司来吉兰通常作为药物用于治疗帕金森病患者。然而，传统司来吉兰的临床价值因广泛的首过代谢而受到影响，这降低了其生物利用度，并导致可能有害的甲基苯丙胺代谢物的产生。本综述旨在通过研究以往药理学和临床研究的科学证据来评估司来吉兰的一种新型口腔崩解制剂。由于生物利用度提高，口腔崩解司来吉兰可以以低于传统司来吉兰的剂量给药，临床效果相似。它还能使司来吉兰的血药浓度变化较小，并产生明显较少的甲基苯丙胺代谢物。我们得出结论，这种新型制剂提供了一个有趣的治疗选择，特别是对于那些在初始使用传统司来吉兰治疗后报告有不良事件或有吞咽困难的患者。
