部分中文多奈哌齐处方资料（仅供参考）
药品英文名
Donepezil
药品别名
盐酸多奈哌齐、安理申、Aricept、Donepezil Hydrochloride
药物剂型
片剂：3mg、5mg 10mg。
药理作用
本药是多奈哌齐的盐酸盐，为第二代胆碱酯酶抑制药，是一种长效的阿尔茨海默病(AD)的对症治疗药物。近30年的研究表明：AD胆碱能神经元的进行性蜕变是记忆力减退、定向力丧失、行为和个性改变的原因，这种胆碱能理论已被组织学研究证实。本药作用机制是可逆性地抑制乙酰胆碱酯酶(AchE)，使乙酰胆碱水解减少，增加受体部位的乙酰胆碱含量。可能还有其他机制，包括对肽的作用、对神经递质受体或Ca2＋通道的直接作用。
药动学
口服后吸收良好，相对生物利用度为100%，达峰时间为3～4h。每天口服1～10mg，血药浓度与剂量呈线性相关。在多剂量服药后，血浆中浓度蓄积4～7倍，在连服14天后达到稳态。进食和服药时间均不影响药物的吸收程度。血浆蛋白结合率为96%，血药浓度达稳态时分布容积为12L/kg。药物基本上以代谢产物形式从尿中排出，部分代谢产物仍具有胆碱酯酶抑制活性。以14C标记的药物动力学研究表明，服药后10天内，57%从尿中排出，15%从粪便排出，但有28%仍未排出。此后可发现约17%以原药形式从尿中排出。半衰期约为70h，平均血浆清除率为每小时0.13L/kg。
适应证
适用于轻至中度认知障碍的阿尔茨海默病的治疗。
禁忌证
1.对本药或哌啶衍生物高度敏感的患者；
2.哺乳期妇女。
注意事项
1.慎用：
(1)胃肠道疾病活动期或有溃疡病史的患者；
(2)接受非甾体类抗炎药治疗的患者；
(3)哮喘或阻塞性肺病患者；
(4)病窦综合征或室上性心脏传导阻滞患者(本药可能引起心动过缓)；
(5)有癫痫发作史者；
(6)外科大手术患者(多奈哌齐可以增加氯琥珀胆碱型肌肉的松弛)；
(7)妊娠妇女。
2.过量会引起胆碱能危象，重者危及生命，当出现明显中毒反应时静推阿托品1～2mg。
不良反应
最常见的是腹泻、恶心和失眠，通常是轻微和短暂的，无需停药，在1～2天内可缓解。
用法用量
口服给药：每次5mg或10mg，每天1次，睡前服用。3～6个月为一个疗程。
药物相应作用
1.与拟胆碱药(如氨甲酰甲基胆碱)和其他胆碱酯酶抑制药有协同作用。
2.酮康唑、伊曲康唑、奎尼丁可抑制本药代谢，升高其血药浓度。
3.与氯琥珀胆碱类肌松药、抗胆碱药有拮抗作用，故不能合用。
4.苯妥英、苯巴比妥、卡马西平、地塞米松、利福平等药物，可增加本药的清除率，降低本药的血药浓度。
5.与洋地黄、华法林联用时，要注意调节剂量。
专家点评
本品为第二代胆碱酯酶抑制剂。抑制乙酰胆碱酯酶活性的强度是抑制丁酰胆碱酯酶的570倍，具有较高的选择性。而且只对脑内胆碱酯酶产生抑制作用，因此是一种长效的阿尔茨海默病(AD)的对症治疗药物。
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アリセプト内服ゼリー３mg／アリセプト内服ゼリー５mg／アリセプト内服ゼリー10mg

有効成分に関する理化学的知見
商標名
Aricept
一 般 名
ドネペジル塩酸塩（Donepezil Hydrochloride）
化 学 名
(2RS)‐2‐［(1‐Benzylpiperidin‐4‐yl)methyl］‐5,6‐dimethoxy‐2,3‐dihydro‐1H‐inden‐1‐one monohydrochloride
分 子 式
C24H29NO3・HCl
分 子 量
415.95
構 造 式

物理化学的性状
ドネペジル塩酸塩は白色の結晶性の粉末である。
本品は水にやや溶けやすく、エタノール（99.5）に溶けにくい。
本品の水溶液（１→100）は旋光性を示さない。
融　　点
223.5℃（分解）
分配係数
log P＝4.27（1－オクタノール／水）
取扱い上の注意
1. 誤用を避けるため他の容器に移し替えて保存しないこと。
2. 小児等の手の届かないところに保存すること。
3. 高温を避けて保存すること。
4. 包装に表示している上下の向きに注意して保存すること。
5. アルミ袋の状態で保存すること（アルミ袋内に脱酸素剤を封入している）。
6. ゼリー表面に水分がみられることがあるが、製剤由来のものである。
承認条件
**レビー小体型認知症における認知症症状の進行抑制
レビー小体型認知症を対象に、本剤の有効性の検証及び安全性の確認を目的とした臨床試験を実施し、終了後速やかに試験成績及び解析結果を提出すること。
包装规格[安理申口腔果冻]为
3mg*14件

5mg*14件

10mg*14件

生产厂商
卫材有限公司

完整处方资料附件：http://www.info.pmda.go.jp/go/pack/1190012Q1027_1_09/1
ARICEPT® (donepezil hydrochloride) is a reversible inhibitor of the enzyme acetylcholinesterase
ARICEPT® is available for oral administration in film-coated tablets containing 5 or 10 mg of donepezil hydrochloride.
INDICATIONS
ARICEPT® is indicated for the treatment of dementia of the Alzheimer's type. Efficacy has been demonstrated in patients with mild to moderate Alzheimer's Disease, as well as in patients with severe Alzheimer's Disease.
Mild to Moderate Alzheimer's Disease
The dosages of ARICEPT® shown to be effective in controlled clinical trials are 5 mg and 10 mg administered once per day.
Severe Alzheimer's Disease
ARICEPT® has been shown to be effective in controlled clinical trials at a dose of 10 mg administered once daily.
>GENERALLY WELL TOLERATED
>NOT HEPATOTOXIC
Most Frequent Adverse Clinical Events Seen in Association with the Use of ARICEPT®
These include diarrhea, anorexia, vomiting, nausea, and ecchymosis. These adverse events were often of mild intensity and transient, resolving during continued ARICEPT® treatment without the need for dose modification.
PRECAUTIONS
Carcinogenesis, Mutagenesis, Impairment of Fertility
No evidence of a carcinogenic potential was obtained in an 88-week carcinogenicity study of donepezil hydrochloride conducted in CD-1 mice at doses up to 180 mg/kg/day (approximately 90 times the maximum recommended human dose on a mg/m² basis), or in a 104-week carcinogenicity study in Sprague-Dawley rats at doses up to 30mg/kg/day (approximately 30 times the maximum recommended human dose on a mg/m² basis).
Donepezil was not mutagenic in the Ames reverse mutation assay in bacteria, or in a mouse lymphoma forward mutation assay in vitro. In the chromosome aberration test in cultures of Chinese hamster lung (CHL) cells, some clastogenic effects were observed. Donepezil was not clastogenic in the in vivo mouse micronucleus test and was not genotoxic in an in vivo unscheduled DNA synthesis assay in rats.
Donepezil had no effect on fertility in rats at doses up to 10 mg/kg/day (approximately 8 times the maximum recommended human dose on a mg/m² basis).
Pregnancy
Pregnancy Category C: Teratology studies conducted in pregnant rats at doses up to 16 mg/kg/day (approximately 13 times the maximum recommended human dose on a mg/m² basis) and in pregnant rabbits at doses up to 10 mg/kg/day (approximately 16 times the maximum recommended human dose on a mg/m² basis) did not disclose any evidence for a teratogenic potential of donepezil. However, in a study in which pregnant rats were given up to 10 mg/kg/day (approximately 8 times the maximum recommended human dose on a mg/m² basis) from day 17 of gestation through day 20 postpartum, there was a slight increase in still births and a slight decrease in pup survival through day 4 postpartum at this dose; the next lower dose tested was 3 mg/kg/day. There are no adequate or well-controlled studies in pregnant women. ARICEPT® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers
It is not known whether donepezil is excreted in human breast milk. ARICEPT® has no indication for use in nursing mothers.
Pediatric Use
There are no adequate and well-controlled trials to document the safety and efficacy of ARICEPT® in any illness occurring in children.
Geriatric Use
Alzheimer's disease is a disorder occurring primarily in individuals over 55 years of age. The mean age of patients enrolled in the clinical studies with ARICEPT® was 73 years; 80% of these patients were between 65 and 84 years old and 49% of patients were at or above the age of 75. The efficacy and safety data presented in the clinical trials section were obtained from these patients. There were no clinically significant differences in most adverse events reported by patient groups ≥ 65 years old and < 65 years old.