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Rivastigmine

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https://www.readbyqxmd.com/read/28224389/development-of-a-discriminative-in-vitro-release-test-for-rivastigmine-transdermal-patches-using-pharmacopeial-apparatuses-usp-5-and-usp-6
#1
Alice Simon, Maria Inês Amaro, Anne Marie Healy, Lucio Mendes Cabral, Valeria Pereira de Sousa
The aim of this study was to develop and validate a discriminating in vitro release test to evaluate rivastigmine transdermal patches. The Exelon® Patch was chosen as a model transdermal product. The studies of in vitro release were designed to determine the impact of the official apparatus chosen (USP apparatus 5 and USP apparatus 6), the rotation speed, and the dissolution medium characteristics on the rivastigmine release profile from transdermal patches. Patches with different drug release profiles were tested in order to evaluate the discriminating power of the in vitro release test developed and validated...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28164767/nanotechnology-for-alzheimer-disease
#2
Jerzy Leszek, Wai Hei Tse, Jin Zhang, Marco Fidel Ávila-Rodriguez, Vadim V Tarasov, George E Barreto, Sergey O Bachurin, Gjumrakch Aliev
Dementia of Alzheimer disease (AD) type affects memory, thinking and behavior. Researchers believe that changes in the brain may begin 10-20 years before symptoms appear and AD is diagnosed. The need to diagnose and treat the devastating disease at an early stage is critical to manage and treat AD. Unfortunately, the lack of validated biomarkers limits the possibility of the earlier stages of AD. The advance of nanotechnology could offer huge opportunities in early-stage diagnosis and well treatment of AD. Biocompatible nanoparticles with diameter in the range of 1-100 nm could be used as targeted delivery system for drugs (e...
February 3, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/28143625/potential-benefits-of-phytochemicals-against-alzheimer-s-disease
#3
Emma L Wightman
Our current therapeutic drugs for Alzheimer's disease are predominantly derived from the alkaloid class of plant phytochemicals. These drugs, such as galantamine and rivastigmine, attenuate the decline in the cholinergic system but, as the alkaloids occupy the most dangerous end of the phytochemical spectrum (indeed they function as feeding deterrents and poisons to other organisms within the plant itself), they are often associated with unpleasant side effects. In addition, these cholinesterase inhibiting alkaloids target only one system in a disorder, which is typified by multifactorial deficits...
February 1, 2017: Proceedings of the Nutrition Society
https://www.readbyqxmd.com/read/28138912/tolerability-of-cholinesterase-inhibitors-a-population-based-study-of-persistence-adherence-and-switching
#4
Anat Fisher, Greg Carney, Ken Bassett, Colin R Dormuth
BACKGROUND: Cholinesterase inhibitors (ChEIs) are prescribed to dementia patients despite their poor tolerance. Low tolerability potentially reduces persistence and adherence, while inducing switching between medications. Comparisons of these utilization measures contribute to knowledge of the relative tolerability of these medications. AIM: The aim was to compare persistence, adherence, and switching between donepezil, galantamine, oral rivastigmine, and rivastigmine patch...
January 30, 2017: Drugs & Aging
https://www.readbyqxmd.com/read/28130773/identification-of-substandard-medicines-via-disproportionality-analysis-of-individual-case-safety-reports
#5
Zahra Anita Trippe, Bruno Brendani, Christoph Meier, David Lewis
INTRODUCTION: The distribution and use of substandard medicines (SSMs) is a public health concern worldwide. The detection of SSMs is currently limited to expensive large-scale assay techniques such as high-performance liquid chromatography (HPLC). Since 2013, the Pharmacovigilance Department at Novartis Pharma AG has been analyzing drug-associated adverse events related to 'product quality issues' with the aim of detecting defective medicines using spontaneous reporting. The method of identifying SSMs with spontaneous reporting was pioneered by the Monitoring Medicines project in 2011...
January 28, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/28129887/a-left-lateral-accessory-pathway-unmasked-by-rivastigmine
#6
Charles Guenancia, Marie Fichot, Fabien Garnier, Mathieu Montoy, Gabriel Laurent
A 75-year-old woman was referred for advice regarding surface electrocardiographic modifications after the initiation of rivastigmine. In our patient, the baseline ECGs appeared perfectly normal. However, the initiation of a cholinesterase inhibitor unmasked a left lateral accessory pathway that had never been diagnosed before. Although cholinesterase inhibitors are known to increase vagal tone, the PR interval was shortened after rivastigmine administration, thus excluding this hypothesis to explain the appearance of the accessory pathway...
January 16, 2017: Journal of Electrocardiology
https://www.readbyqxmd.com/read/28103749/clinical-practice-with-anti-dementia-drugs-a-revised-third-consensus-statement-from-the-british-association-for-psychopharmacology
#7
John T O'Brien, Clive Holmes, Matthew Jones, Roy Jones, Gill Livingston, Ian McKeith, Peter Mittler, Peter Passmore, Craig Ritchie, Louise Robinson, Elizabeth L Sampson, John-Paul Taylor, Alan Thomas, Alistair Burns
The British Association for Psychopharmacology coordinated a meeting of experts to review and revise its previous 2011 guidelines for clinical practice with anti-dementia drugs. As before, levels of evidence were rated using accepted standards which were then translated into grades of recommendation A-D, with A having the strongest evidence base (from randomised controlled trials) and D the weakest (case studies or expert opinion). Current clinical diagnostic criteria for dementia have sufficient accuracy to be applied in clinical practice (B) and both structural (computed tomography and magnetic resonance imaging) and functional (positron emission tomography and single photon emission computerised tomography) brain imaging can improve diagnostic accuracy in particular situations (B)...
February 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28100075/urinary-incontinence-in-alzheimer-s-disease
#8
Hsiang-Ying Lee, Ching-Chia Li, Yung-Shun Juan, Yu-Han Chang, Hsin-Chih Yeh, Chia-Chun Tsai, Kuang-Shun Chueh, Wen-Jeng Wu, Yuan-Han Yang
OBJECTIVES: Urinary incontinence (UI) is more prevalent in the elderly populations with dementia than without dementia, and Alzheimer's disease (AD) is the most common cause of dementia. Urinary incontinence may complicate AD morbidity and mortality. Therefore, this study aimed to evaluate the prevalence and annual incidence and determine the risk possibility of UI, which is the main type of incontinence in patients with AD in Taiwan. METHODS: A total of 933 patients with AD were included in the study cohort, and a total of 2799 patients without AD by 1:3 proportion compared to the study cohort were used as a matched cohort...
February 2017: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/28078633/benzodiazepine-use-and-risk-of-developing-alzheimer-s-disease-a-case-control-study-based-on-swiss-claims-data
#9
Fabienne A Biétry, Alena M Pfeil, Oliver Reich, Matthias Schwenkglenks, Christoph R Meier
BACKGROUND: A possible association between benzodiazepine use and Alzheimer's disease (AD) has been hypothesized in previous studies. OBJECTIVES: Using claims data from the Helsana Group, a large Swiss health insurance provider, we examined the association between previous benzodiazepine use and the risk of AD. METHODS: We conducted a matched case-control study and identified 1438 incident AD cases between 2013 and 2014 based on recorded first-time use of drugs used to treat AD [i...
January 11, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28076987/antioxidant-activity-and-cholinesterase-inhibition-studies-of-four-flavouring-herbs-from-alentejo
#10
Sílvia Arantes, Andreia Piçarra, Fátima Candeias, A Teresa Caldeira, M Rosário Martins
Essential oils (EOs) and aqueous extracts of aerial parts of four aromatic species, Calamintha nepeta, Foeniculum vulgare, Mentha spicata and Thymus mastichina, from southwest of Portugal were characterised chemically and analysed in order to evaluate their antioxidant potential and cholinesterase inhibitory activities. The main components of EOs were oxygenated monoterpenes, and aqueous extracts were rich in phenol and flavonoid compounds. EOs and aqueous extracts presented a high antioxidant potential, with ability to protect the lipid substrate, free radical scavenging and iron reducing power...
January 11, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28060449/therapeutic-effects-of-drug-switching-between-acetylcholinesterase-inhibitors-in-patients-with-alzheimer-s-disease
#11
Yasuyuki Ohta, Mohamed Darwish, Nozomi Hishikawa, Toru Yamashita, Kota Sato, Mami Takemoto, Koji Abe
AIM: To evaluate the therapeutic effects of switching from one acetylcholinesterase inhibitor (ChEI), donepezil, galantamine or rivastigmine, to another in Alzheimer's disease patients. METHODS: We retrospectively enrolled 171 Alzheimer's disease patients, whose ChEI medication was changed. The patients were evaluated on three major aspects of dementia - cognitive, affective and activities of daily living (ADL) measures - at 6 months (M) before the drug switch, at the time of drug switch (baseline), and at 3 M and 6 M after the drug switch...
January 6, 2017: Geriatrics & Gerontology International
https://www.readbyqxmd.com/read/28060207/brain-cholinergic-function-and-response-to-rivastigmine-in-patients-with-chronic-sequels-of-traumatic-brain-injury-a-pet-study
#12
Anna Östberg, Jere Virta, Juha O Rinne, Vesa Oikonen, Pauliina Luoto, Kjell Någren, Eveliina Arponen, Olli Tenovuo
OBJECTIVE: To investigate quantitative positron emission tomography (PET) findings and to study whether the cholinergic function differs between respondents to cholinergic medication versus nonrespondents. SETTING: Outpatient clinic and university PET imaging center. PARTICIPANTS: We studied 17 subjects for more than 1 year after at least moderate traumatic brain injury. Ten of the subjects were respondents and 7 nonrespondents to cholinergic medication...
January 5, 2017: Journal of Head Trauma Rehabilitation
https://www.readbyqxmd.com/read/28049888/influence-of-memantine-on-continuous-treatment-with-rivastigmine-patches-retrospective-study-using-the-logistic-regression-analysis
#13
Yuki Yasutaka, Shinsuke Fujioka, Mariko Terasawa, Hirotomo Shibaguchi, Koujiro Futagami, Shinji Ouma, Yoshio Tsuboi, Hidetoshi Kamimura
 Rivastigmine patches exhibit stable effects when attached once a day, and may reduce Alzheimer's disease (AD) patient's or caregiver's burden. On the other hand, it was reported that adverse events, such as dermal disorder, frequently appeared after the start of rivastigmine administration. We retrospectively investigated medical records in 120 patients with moderate or mild AD in whom rivastigmine administration was started in the Department of Neurology, Fukuoka University Hospital between July 2011 and June 2014 (43 males, 77 females, mean age: 76...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28043167/mesoporous-silica-nanoparticles-for-efficient-rivastigmine-hydrogen-tartrate-delivery-into-sy5y-cells
#14
Mahmonir Karimzadeh, Ladan Rashidi, Fariba Ganji
Rivastigmine hydrogen tartrate (RT) is a molecule with both hydrophilic and hydrophobic properties used for the treatment of the Alzheimer's disease. In this work, the larger pore size of mesoporous silica nanoparticles (P1-MSN) was synthesized and then, P1-MSN were functionalized by succinic anhydride (S-P1-MSN) and 3-aminopropyltriethoxysilane (APTES) (AP-CO-P1-MSN) using the grafting and co-condensation methods, respectively. A new method was used for the functionalization of P1-MSN by succinic anhydride at room temperature...
April 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28034279/inhibition-of-a%C3%AE-1-42-oligomerization-fibrillization-and-acetylcholinesterase-activity-by-some-anti-inflammatory-drugs-an-in-vitro-study
#15
Hamendra Singh Parmar, Anshul Assaiya, Renuka Agrawal, Shalini Tiwari, Iram Mufti, Neha Jain, Elangovan Manivannan, Tushar Banerjee, Anil Kumar
Background-Number of contradictory reports are available on the effects of anti-inflammatory drugs on Alzheimer's disease (AD) including beneficial, adverse and stage dependent effects. We provide insights of the effects exert by some anti-inflammatory drugs on the chemistry of AD. Methods-Three different doses of dexamethasone (0.015, 0.030, 0.060 µM), piroxicam (5, 7.5, 10 µM), indomethacin (1, 1.25, 1.50 µM), diclofenac (0.6, 0.8, 1.0 µM), aspirin (90, 120, 150 µM) and celecoxib (30, 45, 60 µM) were used...
December 29, 2016: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28011206/design-synthesis-and-biological-evaluation-of-4-aminochalcone-rivastigmine-hybrids-as-multifunctional-agents-for-the-treatment-of-alzheimer-s-disease
#16
Ganyuan Xiao, Yan Li, Xiaoming Qiang, Rui Xu, Yunxiaozhu Zheng, Zhongcheng Cao, Li Luo, Xia Yang, Zhipei Sang, Fu Su, Yong Deng
A series of 4'-aminochalcone-revastigmine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease. The results showed that most of these compounds exhibited good multifunctional activities. In particular, compound 6c displayed the best inhibitory potency on acetylcholinesterase (IC50=4.91μM), and significant antioxidative activity with a value 2.83-fold of Trolox. The kinetic analysis of AChE inhibition revealed that 6c showed mixed-type inhibition, binding simultaneously to the catalytic active site and peripheral anionic site of AChE...
December 9, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28003750/baicalein-improves-behavioral-dysfunction-induced-by-alzheimer-s-disease-in-rats
#17
Li Zhou, Sha Tan, Yi-Long Shan, Yu-Ge Wang, Wei Cai, Xue-Hong Huang, Xi-Yuan Liao, Hai-Yan Li, Lei Zhang, Bing-Jun Zhang, Zheng-Qi Lu
BACKGROUND: Alzheimer's disease (AD) is considered to be a neurodegenerative disorder that is characterized by increased oxidative stress. Medicinal plants, with their antioxidant properties, have been used to cure several human diseases. The aim of the current study was to explore the protective and therapeutic effect of baicalein on AD-induced rats. MATERIALS AND METHODS: Swiss Wistar rats were used in the study. The rats were divided into five groups. Group I: normal control group treated with water; Group II: disease control treated with AlCl3 to induce the mimicking AD for 4 successive weeks (SW); Group III: normal control group treated with baicalein (5 mg/kg) for 2 SW followed by combination of baicalein and AlCl3 for 4 SW; Group IV: normal control group treated with baicalein (10 mg/kg) for 2 SW followed by combination of baicalein and AlCl3 for 4 SW; Group V: normal control group treated with rivastigmine (0...
2016: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28000168/caregiver-preference-and-treatment-compliance-in-patients-with-mild-to-moderate-alzheimer-s-disease-in-south-korea-recap-study-results
#18
Kang Joon Lee, Seong-Jin Cho, Byeong Chae Kim, Minseok Park, Jae-Hong Lee
INTRODUCTION: The aim of this study was to assess caregiver preference and treatment compliance with oral and transdermal medications in a "real-world" setting in patients with mild-to-moderate Alzheimer's disease (AD) in South Korea. METHODS: Real-world evaluation of compliance and preference in Alzheimer's disease treatment (RECAP) was a 24-week, multicenter, prospective, non-interventional study in patients with AD treated with oral or transdermal therapy. Here, we report data from patients living in South Korea...
December 20, 2016: Advances in Therapy
https://www.readbyqxmd.com/read/27984078/anti-inflammatory-and-protective-effects-of-mt-031-a-novel-multitarget-mao-a-and-ache-buche-inhibitor-in-scopolamine-mouse-model-and-inflammatory-cells
#19
Wei Liu, Alon Rabinovich, Yuval Nash, Dan Frenkel, Yuqiang Wang, Moussa B H Youdim, Orly Weinreb
Previous study demonstrated that the novel multitarget compound, MT-031 preserved in one molecule entity the beneficial properties of its parent drugs, rasagiline and rivastigmine, and exerted high dual potencies of monoamine oxidase-A (MAO-A) and cholinesterase (ChE) inhibition in acute-treated mice and neuroprotective effects against H2O2-induced neurotoxicity in human neuroblastoma SH-SY5Y cells. The present study aimed to further investigate the anti-inflammatory and protective effects of MT-031 in scopolamine mouse model and inflammatory cell cultures...
October 28, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27951489/novel-ferulic-amide-derivatives-with-tertiary-amine-side-chain-as-acetylcholinesterase-and-butyrylcholinesterase-inhibitors-the-influence-of-carbon-spacer-length-alkylamine-and-aromatic-group
#20
Haoran Liu, Linbo Liu, Xiaohui Gao, Yingzi Liu, Wanjun Xu, Wei He, Hong Jiang, Jingjing Tang, Haoqun Fan, Xinhua Xia
Based on our recent investigations on chalcone derivatives as AChE inhibitors, a series of ferulic acid (FA) tertiary amine derivatives similar to chalcone compounds were designed and synthesized. The results of bioactivity evaluation revealed that most of new synthesized compounds had comparable or more potent AChE inhibitory activity than the control drug Rivastigmine. The alteration of carbon chain linking tertiary amine groups and ferulic acid scaffold markedly influenced the inhibition activity against AChE...
January 27, 2017: European Journal of Medicinal Chemistry
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