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Chinese Journal of Chemistry 2006年第10期24卷 1384-1387页

作者：王兆彦许杏祥胡之德康经武 College of Chemistry and Chemical Engineering Lanzhou University Lanzhou Gansu 730000 China Shanghai Institute of Organic Chemistry Chinese Academy of Sciences Shanghai 200032 China

A sensitive method for enantioseparation of a basic drug rivastigmine and determination of its optical impurity by capillary electrophoresis with highly sulfated β-cyclodextrin （HS-β-CD） as the chiral selector is described. In general, enantioseparation of basic chiral compounds is carried out in acidic condition （pH 2.5） to prevent analytes from adsorption on the capillary wall. However, in the case of rivastigmine, the detection sensitivity was too limited to determine the optical impurity of S-rivastigmine lower than 1% when buffer pH was 2.5. It was found that the detection sensitivity was improved 1.6 times just by raising the buffer pH value from 2.5 to 5.8. The poor column efficiency due to the adsorption of the analytes on the capillary wall was resolved by using dynamical coating of the capillary wall with the linear polyacrylamide solution. The experimental parameters such as the concentration of HS-β-CD, buffer pH and buffer ionic strength were optimized, respectively. The method was validated in terms of repeatability, linearity, limit of detection （LOD） and limit of quantitation （LOQ）. Using the present method, the optical purity of nonracemic rivastigmine with the enantiomeric excess （ee） value of 99.14% was determined.

关键词： rivastigmine enantioseparation capillary electrophoresis highly sulfated β-cyclodextrin

Third degree atrioventricular block associated with treatment with rivastigmine transdermal patch

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Journal of Geriatric Cardiology 2013年第1期10卷 113-115页

作者： Fredrikke C. Knudtzen Thomas B. Christophersen Department of Internal Medicine OUH Svendborg Hospital Valdemarsgade 53 5700 Svendborg Denmark

rivastigmine transdermal patch is indicated for patientswithAlzheimer’s disease and dementia with Parkinson’s disease. rivastigmine, an acetylcholinesterase inhibitor, has several common adverse effects, mainly involving the gastrointestinal tract, but few cardiovascular adverse effects have been reported. This report presents two cases of patients presenting with 3rd degree atrioventricular block. Both patients were treated with the acetylcholinesterase inhibitor, rivastigmine. In one case, the patient reverted to normal sinus rhythm following the discontinuation of rivastigmine, and the atrioventricular block reappeared after rivastigmine was reinstated. In the other case, the atrioventricular block did not revert and the patient required a permanent pacemaker. Both bradycardia and syncope have previously been reported as adverse events in patients treated with acetylcholinesterase inhibitors. However, the type of bradycardia and the etiology of the syncope are rarely specified. rivastigmine, and other acetylcholinesterase inhibitors, are widely used in the pharmacological treatment of Alzheimer��s disease. We recommend that physicians are vigilant of possible warning signs, such as dizziness, syncope and bradycardia.

关键词： Acetylcholinesterase inhibitors Alzheimer's disease Atrioventricular block rivastigmine

rivastigmine Restores 5-HT<sub>1A</sub>Receptor Levels in the Hippocampus of Olfactory Bulbectomized Mice

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Advances in Alzheimer's Disease 2014年第3期3卷 128-136页

作者： Muhammad Rashedul Islam Shigeki Moriguchi Hideaki Tagashira Kohji Fukunaga Department of Pharmacology Graduate School of Pharmaceutical Sciences Tohoku University Sendai Japan

rivastigmine, a dual acetylcholinesterase and butyrylcholinesterase inhibitor, is used for symptomatic treatment of patients with mild to moderately severe dementia in Alzheimer’s disease (AD) patients. In the present study, we found that 5-HT1A receptor (5-HT1AR) is downregulated, whereas 5-HT2A receptor (5-HT2AR) is upregulated in the hippocampal dentate gyrus (DG) and CA1 region by olfactory bulbectomy (OBX) in mice. Furthermore, chronic treatment with rivastigmine (1.0 mg/kg) for 2 weeks starting 2 weeks after OBX operation restored the decreased 5-HT1AR and the increased 5-HT2AR levels. To determine whether cholinergic receptor stimulation by rivastigmine is involved in the rivastigmine-induced regulation of 5-HTR levels, we treated the mice with mecamylamine (2.5 mg/kg), or atropine (5.0 mg/kg) with rivastigmine (1.0 mg/kg) once a day for 2 weeks. Notably, the rivastigmine-induced 5-HT1AR upregulation was eliminated by mecamylamine but not by atropine treatments. On the other hand, the restored 5-HT2AR level by rivastigmine was not affected by either mecamylamine or atropine. Treatment with 8-OH-DPAT, a selective 5-HT1AR agonist improved the decreased 5-HT1AR and the increased 5-HT2AR levels in OBX mice. On the other hand, treatment with TCB-2, a potent 5-HT2AR agonist had no effects on the 5-HT1AR and 5-HT2AR dysregulation in OBX mice. Taken together, nicotinic acetylcholine receptor (nAChR) stimulation mediates rivastigmine-induced upregulation of 5-HT1AR. Therefore, we speculate that the increased ACh levels by rivastigmine can stimulate nAChR located on serotonergic nerve terminals and stimulate 5-HT1AR by the enhanced 5-HT release in the hippocampus. The 5-HT1AR stimulation likely mediates the improvement of 5-HT1AR levels as auto-receptor in OBX hippocampus.

关键词： rivastigmine 5-HT1A Receptor 5-HT2A Receptor Nicotinic Acetylcholine Receptor Olfactory Bulbectomized Mice

Comparative studies of huperzine A,donepezil,and rivastigmine on brain acetylcholine,dopamine,norepinephrine,and 5-hydroxytryptamine lev-els in freely-moving rats

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Acta Pharmacologica Sinica 2006年第9期27卷 1127-1136页

作者： Yan-qi LIANG Xi-can TANG~2 State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Shanghai Instituties for Biological Sciences,Graduate School of the Chinese Academy of Sciences,Chinese Academy of Sciences,Shanghai 201203.China State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Instituties for Biological Sciences Graduate School of the Chinese Academy of Sciences Chinese Academy of Sciences Shanghai 201203 China. eds.ufl.edu

Aim:To assess the effects of cholinesterase inhibitors huperzine A,donepeziland rivastigmine on cerebral neurotransmitters in the cortex and hippocampus infreely-moving ***:Double-probe cerebral microdialysis and HPLC withelectrochemical detection were used to detect ***:Ourresults showed that huperzine A(0.***.0.5,and 0.75μmol/kg,po)dose-depen-dently elevated extracellular acetylcholine(ACh)levels in the medial prefrontalcortex(mPFC)and *** administration of donepezil(5.4μmol/kg)orrivastigmine(1μmol/kg)also elicited significant increases in ACh in the mPFC *** time course of cortical acetylcholinesterase(ACHE)inhibitionwith the 3 inhibitors minored the increases of ACh at the same *** markedelevation of ACh after oral administration of huperzine A(0.5μmol/kg)anddonepezil(5.4μmol/kg)was associated with a significantly increased release ofdopamine(DA)in the mPFC or *** of the 3 inhibitors affectednorepinephrine(NE)and 5-hydroxytryptamine(5-HT)levels in the mPFC *** effects of huperzine A and rivastigmine did not depend on theroute of administration,but donepezil was less efficacious by the oral route thanby ip *** ability of huperzine A to increase ACh levels was unchangedwhen tests were performed after multiple oral administration of the drug at 0.5μmol/kg,once per day for 30 ***:The present findings showed that,inmolar terms,huperzine A had similar potency on increasing mPFC ACh and DAlevels as compared to the 11-and 2-fold dosages of donepezil and rivastigmine,respectively,and had longer lasting effects after oral dosing.

关键词： huperzine A donepezil rivastigmine acetylcholine dopamine norepinephrine 5-hydroxy tryptamine Alzheimer’s disease rats

rivastigmine inhibits voltage-activated potassium currents in rat hippocampal pyramidal neurons

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Rivastigmine inhibits voltage-activated potassium currents i...

Randomized, Placebo-Controlled Trial of Transdermal rivastigmine for the Treatment of Encephalopathy in Liver Cirrhosis (TREC Trial)

2002全国青年药理学英文学术会议

作者： PAN Ya-Ping, XU Xiang-Hua, WANG Xiao-Liang(Department of Pharmacology, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China)

AIM: rivastigmine is a new acetylcholinesterase (ACHE) inhibitor following tacrine and donepezil. It displays specificity for central ACHE. Potassium channels in the brain has been found in close relationship with learning and memory. While no research about the action of rivastigmine on central potassium currents has been reported up to date. In the present study, we examined the effects of rivastigmine on two main voltage-activated outward potassium currents including transient outward potassium current (I) and delayed rectifier potassium current (I) in rat hippocampal neurons. METHODS: Hippocampal

关键词： rivastigmine hippocampus pyramidal neurons potassium currents patch clamp technique

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Open Journal of Gastroenterology 2014年第6期4卷 255-264页

作者： Patrick P. Basu Niraj James Shah Mark M. Aloysius Robert S. Brown Columbia University College of Physicians & Surgeons New York USA James J. Peters VA Medical Center New York USA King’s County Hospital New York USA

Objectives: Cognitive dysfunction in patients with hepatic encephalopathy (HE) may be caused by alterations in cholinergic neurotransmission. The objective of the study was to evaluate the efficacy and safety of transdermal rivastigmine in improving cognitive function in patients with overt HE. Design: Randomized, controlled pilot study in which patients with grade 2 or 3 HE were treated with lactulose and randomized to receive either transdermal rivastigmine or placebo for 21 days. The modified encephalopathy scale (MES), object recognition test (ORT), trail test (TT), and serum ammonia were assessed at baseline weekly. Electroencephalography was performed at baseline and the final week of the study. Results: Patients were treated with lactulose (20 g/30 mL three times per day) and either transdermal rivastigmine (4.6 mg/d;n = 15) or placebo (n = 15). Transdermal rivastigmine significantly improved MES, ORT, and TT results compared with placebo (P ≤ 0.0001 at all 3 weeks for all 3 assessments). Serum ammonia improved in both treatment groups, although there was significantly greater improvement with placebo than rivastigmine after 2 weeks of treatment (P What is already known about this subject? ? Current approaches to the management of HE are primarily designed to reduce the levels of ammonia and other gut-derived toxins. ? Traditional strategies for HE treatment have included non-absorbable disaccharides (to decrease bowel transit time) or rifamixin (non-absorbable antibiotics to reduce ammoniogenic flora). ? No transdermal cholinomimetic agents have been used with oral lactulose to date, in HE. What are the new findings? ? Transdermal rivastigmine is safe for use in patients with grade 2 & 3 HE. ? Transdermal rivastigmine in combination with oral lactulose in this study is far superior to lactulose alone in improving cognitive function. How might it impact on clinical practice in the foreseeable future? ? Transdermal rivastigmine in combination with oral lactulo

关键词： Acetylcholinesterase Cholinergic Function Hepatic Encephalopathy rivastigmine

Effects of rivastigmine Combined with Reinhartdt and Sea Cucumber Capsule in Patients with Mild-to-Moderate Parkinson’s Disease Dementia: A Pilot Study

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Chinese Medicine 2014年第2期5卷 94-103页

作者： Yongxing Yan Lizhen Liang Tao Xie Yonghui Shen Yanjing Cao Department of Neurology The Third People’s Hospital of Hangzhou Hangzhou China Department of Neurology University of Chicago Medicine Chicago USA

Many patients with Parkinson’s disease suffer cognitive impairment or dementia. Cholinesterase inhibitors (ChEIs) have positive effects on patients with Parkinson’s Disease Dementia (PDD). But it is only improve symptoms. There is no etiological cure for PDD. So, In order to achieve the best outcomes, the combination of ChEIs and other therapeutic strategies is needed to study.?In the present study, we investigate the efficacy and safety of rivastigmine combined with Reinhartdt and Sea Cucumber Capsule (RSC) in patients with mild-to-moderate PDD, and its effect on thyroid function.?There were 52 patients were randomly assigned to receive either rivastigmine (3 mg/ day) or rivastigmine plus RSC (2.7 g/day) treatment for 24 weeks. Efficacy was investigated by the change of the scores of Alzheimer’s Disease Assessment Scale cognitive subscale (ADAS-Cog), Activities of Daily Life (ADL) and Unified Parkinson’s Disease Rating Scale (UPDRS) part III (motor scale). Meanwhile, thyroid hormone levels were detected before and after 12 weeks, 24 weeks treatment in all patients. Results showed that?the patients treated with rivastigmine plus RSC showed more improvement in the cognition and the daily life activities compared to those treated with rivastigmine alone. Significant difference was present after being treated for 12 weeks or more. However, no group difference was found on UPDRS part III, thyroid hormone level change and the incidence of adverse events (11.1% vs 16.0%) between the two groups of treatment. Adverse effects were nausea and vomiting which were the main reasons for the dropout. The finding suggests that rivastigmine plus RSC may improves the treatment effects in cognition and the ADL of the patients with mild-to-moderate PDD, compared with the rivastigmine treatment alone. However, no effect was observed on the motor symptoms and thyroid hormone levels. In addition, this joint treatment is safe.

关键词： Parkinson’s Disease Cognitive Function rivastigmine Reinhartdt and Sea Cucumber

rivastigmine对大鼠海马锥体神经元电压依赖性外向钾电流的影响

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Rivastigmine对大鼠海马锥体神经元电压依赖性外向钾电流的影响

阿尔茨海默症治疗药rivastigmine

2002全国青年药理学英文学术会议

作者：潘雅萍徐向华王晓良中国医学科学院

目的:rivastigmine是继tacrine和donepezil之后的一个新型胆碱酯酶抑制剂,有中枢胆碱酯酶选择性,目前已用于临床治疗AD。中枢神经系统钾离子通道与学习记忆关系密切,而有关rivastigmine对中枢神经元钾通道的影响尚未见报道。本实验研究... 详细信息

目的:rivastigmine是继tacrine和donepezil之后的一个新型胆碱酯酶抑制剂,有中枢胆碱酯酶选择性,目前已用于临床治疗AD。中枢神经系统钾离子通道与学习记忆关系密切,而有关rivastigmine对中枢神经元钾通道的影响尚未见报道。本实验研究了rivastigmine对大鼠急性分离海马锥体神经元瞬间外向钾电流(I)和延迟整流钾电流(I)的影响。方法:采用酶解和机械方法急性分离2-3周龄大鼠的海马锥体神经元,用全细胞膜片钳技术记录神经元I和I,分别观察1,3,和10μmol·L

关键词： rivastigmine 海马锥体神经元钾电流膜片钳技术

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国外医药（合成药．生化药．制剂分册） 1999年第1期20卷 20-21页

作者：马卫东

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rivastigmine透皮贴剂用于AD

国外药讯 2006年第5期 21-21页

作者：王卫（摘）

小野公司有意在日本帮助Novartis公司开发和上市阿尔茨海默病（AD）治疗药rivastigmine（Ⅰ）的透皮贴剂。这种乙酰胆碱酯酶抑制剂在日本已处于Ⅱ期试验中，小野公司将协助完成剩下的临床项目以加速开发。这家中等规模的日本公司将获得... 详细信息

小野公司有意在日本帮助Novartis公司开发和上市阿尔茨海默病（AD）治疗药rivastigmine（Ⅰ）的透皮贴剂。这种乙酰胆碱酯酶抑制剂在日本已处于Ⅱ期试验中，小野公司将协助完成剩下的临床项目以加速开发。这家中等规模的日本公司将获得在日本的共同上市权。（Ⅰ）有望成为第一个用于AD的透皮治疗药物，它可抑制乙酰胆碱酯酶和丁酰胆碱酯酶。这两家公司指出，在AD的疾病进程中丁酰胆碱酯酶的含量是增加的。

关键词： rivastigmine 透皮贴剂 Novartis公司 AD 乙酰胆碱酯酶抑制剂丁酰胆碱酯酶阿尔茨海默病治疗药物 Ⅱ期试验疾病进程