Department of Neurology, Kaohsiung Municipal Ta-Tung Hospital, Kaohsiung, Taiwan.
J Alzheimers Dis. 2012;31(4):857-64. doi: 10.3233/JAD-2012-120109.
The aim of this small pilot study was to evaluate the association between plasma concentrations of rivastigmine and its metabolite, NAP 226-90, and cognitive function in patients with Alzheimer's disease (AD). Rivastigmine-treated AD patients, who had been maintained on a fixed regimen of twice daily rivastigmine (6 to 12 mg/d) for ≥6 months, were eligible for evaluation. The assessments included cognitive assessment screening instrument (CASI) and clinical dementia rating scale, conducted at baseline and at 6-month follow-up. The 9 subdomains of CASI at baseline and follow-up were analyzed in relation to the plasma concentrations of rivastigmine and NAP 226-90, as measured by capillary electrophoresis. Logistic regression was performed to adjust for age, gender, education level, apolipoprotein E ε4 genotype status, and baseline CASI score to investigate the association between plasma rivastigmine and NAP 226-90 concentrations and the cognitive response. The total sample consisted of 53 clinically diagnosed AD patients taking rivastigmine only at doses of 6 mg to 9 mg/d because of intolerability at 12 mg/d. Higher rivastigmine concentration was significantly associated with improved or preserved short-term memory and worsened abstraction/judgment (p < 0.05), but not with changes in other domains (p > 0.05). Higher NAP 226-90 concentration was significantly associated with worsened abstraction/judgment (p < 0.05), but not with changes in other domains. Higher plasma rivastigmine concentration was significantly associated with improved or preserved short-term memory but worsened abstraction/judgment. An optimal concentration of rivastigmine should be quantified for each patient because of differential cognitive responses.
本小型先导研究旨在评估阿尔茨海默病(AD)患者中利伐斯的明及其代谢物 NAP 226-90 的血浆浓度与认知功能之间的关系。符合条件的患者为接受利伐斯的明治疗的 AD 患者,他们已接受固定的每日两次利伐斯的明(6 至 12 毫克/天)治疗至少 6 个月。评估包括认知评估筛选工具(CASI)和临床痴呆评定量表,在基线和 6 个月随访时进行。基线和随访时的 CASI 的 9 个亚域与通过毛细管电泳测量的利伐斯的明和 NAP 226-90 的血浆浓度相关,采用逻辑回归来调整年龄、性别、教育水平、载脂蛋白 E ε4 基因型状态和基线 CASI 评分,以调查血浆利伐斯的明和 NAP 226-90 浓度与认知反应之间的关系。总样本由 53 名仅接受 6 毫克至 9 毫克/天剂量的利伐斯的明治疗的临床诊断为 AD 的患者组成,因为 12 毫克/天的剂量不耐受。较高的利伐斯的明浓度与短期记忆改善或保持和抽象/判断恶化显著相关(p < 0.05),但与其他领域的变化无关(p > 0.05)。较高的 NAP 226-90 浓度与抽象/判断恶化显著相关(p < 0.05),但与其他领域的变化无关。较高的血浆利伐斯的明浓度与短期记忆改善或保持相关,但与抽象/判断恶化相关。由于认知反应的差异,应针对每个患者确定利伐斯的明的最佳浓度。