Levy A, Brandeis R, Treves T A, Meshulam Y, Mawassi F, Feiler D, Wengier A, Glikfeld P, Grunwald J, Dachir S
Israel Institute for Biological Research, Ness Ziona, Israel.
Alzheimer Dis Assoc Disord. 1994 Spring;8(1):15-21. doi: 10.1097/00002093-199408010-00004.
Physostigmine has been reported to improve the memory function of some patients with Alzheimer's Disease (AD). However, the drug has a short half-life and a narrow therapeutic window. To overcome these impediments, we developed a continuous transdermal delivery system and tested it for 2 weeks in 12 AD inpatients, using a single-blind design. No major adverse effects were recorded in any of the patients. Physostigmine plasma concentrations were relatively stable (0.56 +/- 0.10 ng/ml) and correlated well with blood acetylcholinesterase inhibition. Six of the 12 patients reported improved vigilance and concentration, and also had higher scores in all four neuropsychological tests employed (Mini Mental State examination, Short Mental Test [SMT], Wechsler's Memory Scale [WMS], and Buschke's Selective Reminding Test). The performance of two additional patients improved in only two tests (SMT and WMS). Transdermal delivery of physostigmine appears to be safe and may be useful for the treatment of a subset of AD patients.
据报道，毒扁豆碱可改善部分阿尔茨海默病（AD）患者的记忆功能。然而，该药物半衰期短，治疗窗窄。为克服这些障碍，我们开发了一种持续透皮给药系统，并采用单盲设计，在12名AD住院患者中进行了为期2周的测试。所有患者均未记录到重大不良反应。毒扁豆碱血浆浓度相对稳定（0.56±0.10 ng/ml），且与血液乙酰胆碱酯酶抑制作用相关性良好。12名患者中有6名报告警觉性和注意力有所改善，并且在所有四项神经心理学测试（简易精神状态检查、简短精神测试[SMT]、韦氏记忆量表[WMS]和布施克选择性提醒测试）中的得分也更高。另外两名患者仅在两项测试（SMT和WMS）中表现有所改善。毒扁豆碱的透皮给药似乎是安全的，可能对一部分AD患者的治疗有用。
