Román Gustavo C, Rogers Susan J
Medicine/Neurology, Mail Code 7883, University of Texas HSC, 7703 Floyd Curl Drive, San Antonio, TX 78229-3900, USA.
Expert Opin Pharmacother. 2004 Jan;5(1):161-80. doi: 10.1517/14656566.5.1.161.
This article reviews the piperidine derivative, donepezil hydrochloride (E2020, Aricept), a reversible central acetylcholinesterase inhibitor currently approved for treatment of mild-to-moderate Alzheimer's disease. Donepezil is well absorbed orally, unaffected by food or by time of administration; it reaches therapeutic levels in doses of 5-10 mg/day and peak plasma concentrations are obtained 3-4 h after oral administration. A single bedtime dose is recommended due to the long elimination half-life of the drug (70 h). Donepezil does not cause liver toxicity or significant drug interactions and is relatively well-tolerated. Initial side effects include nausea, vomiting, diarrhoea, insomnia, muscle cramps, fatigue, anorexia and syncope. Caution is advised in patients with bradycardia. Long-term use of donepezil in AD has been found to delay nursing-home placement and to result in caregiver respite. Donepezil also slows deterioration of cognition and global function in patients with moderate-to-severe AD, with improvement of abnormal behaviours. In addition to AD, donepezil demonstrates significant improvement in cognition, global function and activities of daily living in comparison with placebo-treated patients with vascular dementia and has potential therapeutic benefit for other neurological conditions.
本文综述了哌啶衍生物盐酸多奈哌齐（E2020，安理申），一种目前已被批准用于治疗轻至中度阿尔茨海默病的可逆性中枢乙酰胆碱酯酶抑制剂。多奈哌齐口服吸收良好，不受食物或给药时间的影响；每日剂量为5 - 10毫克时可达到治疗水平，口服给药后3 - 4小时达到血浆峰值浓度。由于该药消除半衰期长（70小时），建议睡前单次给药。多奈哌齐不会引起肝毒性或显著的药物相互作用，耐受性相对良好。初始副作用包括恶心、呕吐、腹泻、失眠、肌肉痉挛、疲劳、厌食和晕厥。心动过缓患者需谨慎使用。已发现长期使用多奈哌齐治疗阿尔茨海默病可延迟入住养老院，并使照料者得到缓解。多奈哌齐还可减缓中度至重度阿尔茨海默病患者认知和整体功能的恶化，并改善异常行为。除阿尔茨海默病外，与安慰剂治疗的血管性痴呆患者相比，多奈哌齐在认知、整体功能和日常生活活动方面有显著改善，对其他神经系统疾病也有潜在治疗益处。
