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Donepezil

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https://www.readbyqxmd.com/read/28808833/long-acting-ionically-paired-embonate-based-nanocrystals-of-donepezil-for-the-treatment-of-alzheimer-s-disease-a-proof-of-concept-study
#1
Naresh Mittapelly, Maharshi Thalla, Gitu Pandey, Venkatesh Teja Banala, Shweta Sharma, Abhishek Arya, Sandeep Mishra, Kalyan Mitra, Shubha Shukla, Prabhat Ranjan Mishra
PURPOSE: The aim of the present study was to prepare a patient friendly long acting donepezil (D) nanocrystals (NCs) formulation, with a high payload for i.m administration. As the native D hydrochloride salt has high aqueous solubility it is necessary to increase its hydrophobicity prior to the NCs formation. METHODS: D was ionically paired with embonic acid (E) in aqueous media and was successfully characterized using techniques like DSC, PXRD, FT-IR, NMR etc...
August 14, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28806057/rational-design-and-multi-biological-profiling-of-novel-donepezil-trolox-hybrids-against-alzheimer-s-disease-with-cholinergic-antioxidant-neuroprotective-and-cognition-enhancing-properties
#2
Pei Cai, Si-Qiang Fang, Xue-Lian Yang, Jia-Jia Wu, Qiao-Hong Liu, Hao Hong, Xiao-Bing Wang, Lingyi Kong
A novel series of donepezil-trolox hybrids were designed, synthesized and evaluated as multifunctional ligands against Alzheimer's disease (AD). Biological assays showed that these derivatives possessed moderate to good inhibitory activities against acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) as well as remarkable antioxidant effects. The optimal compound 6d exhibited balanced functions with good inhibition against hAChE (IC50 = 0.54 μM) and hMAO-B (IC50 = 4.3 μM), significant antioxidant activity (41...
August 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28789886/an-advanced-technique-using-an-electronic-taste-sensing-system-to-evaluate-the-bitterness-of-orally-disintegrating-films-and-the-evaluation-of-model-films
#3
Yoshiko Takeuchi, Rina Usui, Hidekazu Ikezaki, Kohei Tahara, Hirofumi Takeuchi
Taste detection systems using electronic sensors are needed in the field of pharmaceutical design. The aim of this study was to propose an advanced technique using a taste-sensing system to evaluate the bitterness of an orally disintegrating film (ODF) samples. In this system, a solid film sample is kept in the test medium with stirring, and the sensor output is recorded. Model films were prepared using a solution-casting method with a water-soluble polymer such as pullulan, HPMC, HPC or PVP as film formers, and donepezil hydrochloride and quinine hydrochloride as model bitter-tasting active pharmaceutical ingredients (APIs)...
August 5, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28783933/improvement-of-visuo-spatial-function-assessed-by-raven-s-colored-progressive-matrices-in-dementia-with-lewy-bodies-by-donepezil-treatment
#4
Yuta Yoshino, Takaaki Mori, Taku Yoshida, Yasutaka Toyota, Hideaki Shimizu, Jun-Ichi Iga, Shusaku Nishitani, Shu-Ichi Ueno
Objective: Donepezil is used to improve cognitive impairment of dementia with Lewy bodies (DLB). Visuo-spatial dysfunction is a well-known symptom of DLB. Non-verbal Raven's Colored Progressive Matrices (RCPM) were used to assess both visual perception and reasoning ability in DLB subjects treated with donepezil. Methods: Twenty-one DLB patients (mean age, 78.7±4.5 years) were enrolled. RCPM assessment was performed at the time of starting donepezil and within one year after starting donepezil...
August 31, 2017: Clinical Psychopharmacology and Neuroscience: the Official Scientific Journal of the Korean College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28751142/design-synthesis-and-biological-evaluation-of-dual-acetylcholinesterase-and-phosphodiesterase-5a-inhibitors-in-treatment-for-alzheimer-s-disease
#5
Li-Yun Zhou, Yao Zhu, Yu-Ren Jiang, Xiong-Jie Zhao, Dong Guo
With the recent research advances in molecular biology and technology, multiple credible hypotheses about the progress of Alzheimer's disease (AD) have been proposed; multi-target drugs have emerged as an innovative therapeutic approach for AD. Current clinical therapy for AD patients is mainly palliative treatment targeting acetylcholinesterase (AChE). Inhibition of phosphodiesterase 5A (PDE5A) has recently been validated as a potentially novel therapeutic approach for Alzheimer's disease (AD). In this work, series of new compounds were designed, synthesized and evaluated as dual cholinesterase and PDE5A inhibitor...
July 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28746664/what-do-cochrane-systematic-reviews-say-about-non-pharmacological-interventions-for-treating-cognitive-decline-and-dementia
#6
Vitória Carvalho Vilela, Rafael Leite Pacheco, Carolina Oliveira Cruz Latorraca, Daniela Vianna Pachito, Rachel Riera
BACKGROUND: Dementia is a highly prevalent condition worldwide. Its chronic and progressive presentation has an impact on physical and psychosocial characteristics and on public healthcare. Our aim was to summarize evidence from Cochrane reviews on non-pharmacological treatments for cognitive disorders and dementia. DESIGN AND SETTING: Review of systematic reviews, conducted in the Discipline of Evidence-Based Medicine, Escola Paulista de Medicina, Universidade Federal de São Paulo...
May 2017: São Paulo Medical Journal, Revista Paulista de Medicina
https://www.readbyqxmd.com/read/28744942/utilization-of-western-medicine-and-traditional-chinese-medicine-among-patients-with-alzheimer-s-disease-in-taiwan-a-nationwide-population-based-study
#7
C-Y Lai, M-Y Wu, J-H Chiang, M-F Sun, Y-H Chen, C-T Chang, J-G Lin, H-R Yen
BACKGROUND AND PURPOSE: Large-scale studies of utilization of medical services among patients with Alzheimer's disease (AD) are lacking. We aimed to investigate the usage of Western medicine and traditional Chinese medicine (TCM) among these patients in Taiwan. METHODS: We analyzed one million samples from the National Health Insurance Research Database in Taiwan. Patients (n = 1814) newly diagnosed with AD in 2001-2010 were divided into TCM users (n = 528) and non-TCM users (n = 1286)...
July 26, 2017: European Journal of Neurology: the Official Journal of the European Federation of Neurological Societies
https://www.readbyqxmd.com/read/28737885/classics-in-chemical-neuroscience-memantine
#8
Shahrina Alam, Kaelyn Skye Lingenfelter, Aaron M Bender, Craig W Lindsley
Memantine was the first breakthrough medication for the treatment of moderate to severe Alzheimer's disease (AD) patients, and represents a fundamentally new mechanism of action (moderate-affinity, uncompetitive, voltage-dependent, N-methyl-D-aspartate (NMDA) receptor antagonist that exhibits fast on/off kinetics) to modulate glutamatergic dysfunction. Since its approval by the FDA in 2003, memantine, alone, and in combination with donepezil, has improved patient outcomes in terms of cognition, behavioral disturbances, daily functioning and delaying time to institutionalization...
July 24, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28734741/beneficial-effects-of-tqrf-and-tq-nano-and-conventional-emulsions-on-memory-deficit-lipid-peroxidation-total-antioxidant-status-antioxidants-genes-expression-and-soluble-a%C3%AE-levels-in-high-fat-cholesterol-diet-induced-rats
#9
Norsharina Ismail, Maznah Ismail, Nur Hanisah Azmi, Muhammad Firdaus Abu Bakar, Zhang Yida, Johnson Stanslas, Dahiru Sani, Hamidon Basri, Maizaton Atmadini Abdullah
The study determined the effect of thymoquinone rich fraction (TQRF) and thymoquinone (TQ) in the forms of nano- and conventional emulsions on learning and memory, lipid peroxidation, total antioxidant status, antioxidants genes expression and soluble β-amyloid (Aβ) levels in rats fed with a high fat-cholesterol diet (HFCD). The TQRF was extracted from Nigella sativa seeds using a supercritical fluid extraction system and prepared into nanoemulsion, which later named as TQRF nanoemulsion (TQRFNE). Meanwhile, TQ was acquired commercially and prepared into thymoquinone nanoemulsion (TQNE)...
July 20, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28733154/community-pharmacists-knowledge-of-alzheimer-disease-care-in-high-and-low-income-chicago
#10
Marketa Marvanova, Paul Jacob Henkel
OBJECTIVES: This pilot study examined community pharmacists' knowledge to provide care and services for persons with Alzheimer disease (AD) and area income-based disparities in knowledge and availability of cognitive enhancers. METHODS: A cross-sectional telephone survey of pharmacies (n = 137) in high- and low-income areas in Chicago was conducted on pharmacists' degree, experience, and continuing education, as well as knowledge of AD disease and treatment expectations, adverse effects (AEs) of donepezil, and self-care recommendations for insomnia...
July 18, 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28728106/multipotent-ache-and-bace-1-inhibitors-for-the-treatment-of-alzheimer-s-disease-design-synthesis-and-bio-analysis-of-7-amino-1-4-dihydro-2h-isoquilin-3-one-derivates
#11
Xiong-Jie Zhao, Da-Min Gong, Yu-Ren Jiang, Dong Guo, Yao Zhu, You-Chao Deng
In this paper, the preparation of a new class of multi-target-directed ligands (MTDLs) based on a 7-amino-1,4-dihydro-2H-isoquilin-3-one, whose lead (compound I) showed promising properties in acetylcholinesterase (AChE) inhibitory activity [1], is described. The results of in vitro activities and molecular docking demonstrated that the target molecule (compounds 10a-n) with three parts of aromatic moieties and appropriate structural length can interact with aromatic residues in catalytic active site (CAS), peripheral anionic site (PAS) and the channel of AChE...
July 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28713915/concurrent-administration-of-thyroxine-and-donepezil-induces-plastic-changes-in-the-prefrontal-cortex-of-adult-hypothyroid-rats
#12
Fen Wang, Zhangbi Wu, Xiaoxue Zha, Yaojun Cai, Bo Wu, Xuemei Jia, Defa Zhu
The aim of the present study was to observe the effects of the concurrent administration of thyroxine (T4) and an acetylcholinesterase (AChE) inhibitor, donepezil (DON), on the hypothyroidism‑induced ultrastructural changes of the prefrontal cortex (PFC) in adult rats. The acetylcholine (ACh) content and AChE activity was assessed, as well as the expressions of synaptotagmin‑1 (syt‑1) and SNAP‑25 were analyzed in the rats. Adding 0.05% propylthiouracil to rats' drinking water induced a hypothyroid rat model...
September 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28711758/assessing-the-binding-of-cholinesterase-inhibitors-by-docking-and-molecular-dynamics-studies
#13
M Rejwan Ali, Mostafa Sadoqi, Simon G Møller, Allal Boutajangout, Mihaly Mezei
In this report we assessed by docking and molecular dynamics the binding mechanisms of three FDA-approved Alzheimer drugs, inhibitors of the enzyme acetylcholinesterase (AChE): donepezil, galantamine and rivastigmine. Dockings by the softwares Autodock-Vina, PatchDock and Plant reproduced the docked conformations of the inhibitor-enzyme complexes within 2Å of RMSD of the X-ray structure. Free-energy scores show strong affinity of the inhibitors for the enzyme binding pocket. Three independent Molecular Dynamics simulation runs indicated general stability of donepezil, galantamine and rivastigmine in their respective enzyme binding pocket (also referred to as gorge) as well as the tendency to form hydrogen bonds with the water molecules...
June 29, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28705297/the-diagnosis-and-treatment-of-behavioral-disorders-in-dementia
#14
Torsten Kratz
BACKGROUND: Behavioral disorders such as aggressiveness, agitation, delusions, disinhibition, affect lability, and apathy arise in more than 90% of patients with dementia. Behavioral disorders are a major challenge and the greatest stress factor in everyday life for nursing personnel and for family members caring for the patient. METHODS: This review is based on relevant publications retrieved by a selective literature search in the PubMed, Cochrane Library, and German S3 guideline databases with the search terms "behavioral disorders," "non-cognitive disorders," and "challenging behavior," in conjunction with "dementia" and "behavioral and psychological symptoms of dementia...
June 30, 2017: Deutsches Ärzteblatt International
https://www.readbyqxmd.com/read/28699213/acetamide-derivatives-of-chromen-2-ones-as-potent-cholinesterase-inhibitors
#15
Suchita Prasad, Bipul Kumar, Shiv Kumar, Karam Chand, Shashank S Kamble, Hemant K Gautam, Sunil K Sharma
Alzheimer's disease (AD), a neurodegenerative disorder, is a serious medical issue worldwide with drastic social consequences. Inhibition of cholinesterase is one of the rational and effective approaches to retard the symptoms of AD and, hence, consistent efforts are being made to develop efficient anti-cholinesterase agents. In pursuit of this, a series of 19 acetamide derivatives of chromen-2-ones were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potential...
July 12, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28698078/chitosan-nanofilm-and-electrospun-nanofiber-for-quick-drug-release-in-the-treatment-of-alzheimer-s-disease-in-vitro-and-in-vivo-evaluation
#16
Keshireddy AnjiReddy, Subramanian Karpagam
Chitosan micro sized ODF (CBF), chitosan nano sized ODF (CNF) and chitosan nanofiber (CNfib) were prepared to release the donepezil drug quickly for Alzheimer's disease. CNF and CNfib were prepared from ionic gelation technique and electro-spinning process which were further examined under in vitro and in vivo animal model studies. Good thermal stability of CNfib (450°C) when compared to CBF (325°C) and CNF (305°C). The particle size was below 150nm in diameter for CNfib and 250nm in diameter for CNF4 from TEM technique...
July 8, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28690138/chinese-herbal-medicine-for-alzheimer-s-disease-clinical-evidence-and-possible-mechanism-of-neurogenesis
#17
Wen-Ting Yang, Xia-Wei Zheng, Shuang Chen, Chun-Shuo Shan, Qing-Qing Xu, Jia-Zhen Zhu, Xiao-Yi Bao, Yan Lin, Guo-Qing Zheng, Yan Wang
Currently, there is lack of cure or disease-modifying treatment for Alzheimer's disease (AD). Chinese herbal medicine (CHM) is purported to ameliorate AD progression, perhaps by promoting hippocampal neurogenesis. Here, we conducted an updated systematic review to investigate the efficacy and safety of CHM for AD based on high-quality randomized controlled trials (RCTs) and reviewed its possible mechanisms of neurogenesis according to animal-based researches. Twenty eligible studies with 1,767 subjects were identified in eight database searches from inception to February 2017...
July 6, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28678552/acetylcholinesterase-inhibitors-for-treating-dementia-symptoms-a-safety-evaluation
#18
Dana Mohammad, Parco Chan, Janelle Bradley, Krista Lanctôt, Nathan Herrmann
The prevalence of Alzheimer's disease (AD) continues to rise, while treatment options for cognitive impairment are limited. Acetylcholinesterase inhibitors (AChEIs) aim to provide symptomatic benefit for cognitive decline, however these drugs are not without adverse events (AEs). The safety profile of each drug must be taken carefully into consideration before being prescribed, as new dosages and formulations have recently been approved. Areas Covered: Donepezil, galantamine and rivastigmine are the three AChEIs approved for the treatment of varying stages of AD...
July 5, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28673719/newly-developed-drugs-for-alzheimer-s-disease-in-relation-to-energy-metabolism-cholinergic-and-monoaminergic-neurotransmission
#19
REVIEW
Jan Korábečný, Eugenie Nepovimová, Tereza Cikánková, Katarína Špilovská, Lucie Vašková, Eva Mezeiová, Kamil Kuča, Jana Hroudová
Current options for Alzheimer's disease (AD) treatment are based on administration of cholinesterase inhibitors (donepezil, rivastigmine, galantamine) and/or memantine, acting as an N-methyl-D-aspartate (NMDA). Therapeutic approaches vary and include novel cholinesterase inhibitors, modulators of NMDA receptors, monoamine oxidase (MAO) inhibitors, immunotherapeutics, modulators of mitochondrial permeability transition pores (mPTP), amyloid-beta binding alcohol dehydrogenase (ABAD) modulators, antioxidant agents, etc...
July 1, 2017: Neuroscience
https://www.readbyqxmd.com/read/28673322/the-effect-of-electroacupuncture-combined-with-donepezil-on-cognitive-function-in-alzheimer-s-disease-patients-study-protocol-for-a-randomized-controlled-trial
#20
Weina Peng, Jing Zhou, Min Xu, Qing Feng, Lulu Bin, Zhishun Liu
BACKGROUND: Alzheimer's disease is a progressive neurodegenerative disease. Although some of the current treatments offer some symptomatic relief, this disease cannot be cured at present. Electroacupuncture may be effective for Alzheimer's disease for cognitive function, but the evidence for its effectiveness is still limited. The aim of this study is to evaluate the add-on effect of electroacupuncture to donepezil for improving the cognitive function of Alzheimer's disease. METHODS/DESIGN: A total of 334 participants with Alzheimer's disease will be randomly assigned to either an electroacupuncture combined with donepezil group or a donepezil group with a ratio of 1:1...
July 3, 2017: Trials
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