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Rivastigmine

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https://www.readbyqxmd.com/read/28415883/electrosteric-stealth-rivastigmine-loaded-liposomes-for-brain-targeting-preparation-characterization-ex-vivo-bio-distribution-and-in-vivo-pharmacokinetic-studies
#1
Sara Nageeb El-Helaly, Ahmed Abd Elbary, Mohamed A Kassem, Mohamed A El-Nabarawi
Being one of the highly effective drugs in treatment of Alzheimer's disease, Rivastigmine brain targeting is highly demandable, therefore liposomal dispersion of Rivastigmine was prepared containing 2 mol% PEG-DSPE added to Lecithin, Didecyldimethyl ammonium bromide (DDAB), Tween 80 in 1:0.02:0.25 molar ratio. A major challenge during the preparation of liposomes is maintaining a stable formulation, therefore the aim of our study was to increase liposomal stability by addition of DDAB to give an electrostatic stability and PEG-DSPE to increase stability by steric hindrance, yielding what we called an electrosteric stealth (ESS) liposomes...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28409049/rivastigmine-as-a-symptomatic-treatment-for-apathy-in-parkinson-s-dementia-complex-new-aspects-for-this-riddle
#2
Rita Moretti, Paola Caruso, Matteo Dal Ben
Over 90% of PDD patients show at least one neuropsychiatric symptom (NPS); in the 60-70% two or more NPS are present. Their incidence is important in terms of prognosis and severity of pathology. However, among all NPS, apathy is often the most disturbing, associated with greater caregiver's burden. Similar to other NPS, apathy may be due to a dysfunction of the nigrostriatal pathway, even though, not all the PD patients become apathetic, indicating that apathy should not entirely be considered a dopamine-dependent syndrome, and in fact it might also be related to acetylcholine defects...
2017: Parkinson's Disease
https://www.readbyqxmd.com/read/28387023/simultaneous-usage-of-dementia-medications-and-anticholinergics-among-asians-and-pacific-islanders
#3
Brian R Schultz, Junji Takeshita, Deborah Goebert, Steven Takeshita, Brett Y Lu, Alexandre Guilloux, Joy Higa
BACKGROUND: The simultaneous use of dementia medications and anticholinergic medications occurs frequently. Cholinesterase inhibitors and anticholinergic medications likely counteract one another, potentially exposing patients to medications with decreased benefit, more adverse effects, and higher cost of care. We identified the rate of concurrent prescriptions of cholinesterase inhibitors/memantine with anticholinergics in an urban hospital setting with a large Asian and Pacific Islander population...
April 7, 2017: Psychogeriatrics: the Official Journal of the Japanese Psychogeriatric Society
https://www.readbyqxmd.com/read/28386767/increased-quinolinic-acid-in-peripheral-mononuclear-cells-in-alzheimer-s-dementia
#4
Mandy Busse, Vanessa Hettler, Victoria Fischer, Christian Mawrin, Roland Hartig, Henrik Dobrowolny, Bernhard Bogerts, Thomas Frodl, Stefan Busse
The role of monocytes and macrophages in the pathogenesis of neurodegenerative disorders such as Alzheimer's disease (AD) is poorly understood. Recently, we have shown that the number of CD14+ monocytes remained constant during healthy aging and in AD patients. Although only little is known about the function of activated macrophages and microglia in AD, one important mechanism involves the expression of quinolinic acid (QUIN), an endogenous N-methyl-D-aspartate glutamate receptor (NMDA-R) agonist which mediates excitotoxicity especially in the hippocampus...
April 6, 2017: European Archives of Psychiatry and Clinical Neuroscience
https://www.readbyqxmd.com/read/28381516/randomized-controlled-trials-in-mild-cognitive-impairment-sources-of-variability
#5
Ronald C Petersen, Ronald G Thomas, Paul S Aisen, Richard C Mohs, Maria C Carrillo, Marilyn S Albert
OBJECTIVE: To examine the variability in performance among placebo groups in randomized controlled trials for mild cognitive impairment (MCI). METHODS: Placebo group data were obtained from 2 National Institute on Aging (NIA) MCI randomized controlled trials, the Alzheimer's Disease Cooperative Study (ADCS) MCI trial and the Alzheimer's Disease Neuroimaging Initiative (ADNI), which is a simulated clinical trial, in addition to industry-sponsored clinical trials involving rivastigmine, galantamine, rofecoxib, and donepezil...
April 5, 2017: Neurology
https://www.readbyqxmd.com/read/28381360/introduction-of-agarose-gel-as-a-green-membrane-in-electromembrane-extraction-an-efficient-procedure-for-the-extraction-of-basic-drugs-with-a-wide-range-of-polarities
#6
Hadi Tabani, Sakine Asadi, Saeed Nojavan, Mitra Parsa
Developing green methods for analyte extraction is one of the most important topics in the field of sample preparation. In this study, for the first time, agarose gel was used as membrane in electromembrane extraction (EME) without using any organic solvent, for the extraction of four model basic drugs (rivastigmine (RIV), verapamil (VER), amlodipine (AML), and morphine (MOR)) with a wide polarity window (log P from 0.43 to 3.7). Different variables playing vital roles in the proposed method were evaluated and optimized...
March 29, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28372337/association-between-anti-dementia-treatment-persistence-and-daily-dosage-of-the-first-prescription-a-retrospective-analysis-in-neuropsychiatric-practices-in-germany
#7
Jens Bohlken, Louis Jacob, Karel Kostev
BACKGROUND: High adherence and persistence are important for the efficacy of anti-dementia treatments. OBJECTIVE: The goal of this study was to analyze the association between anti-dementia treatment persistence and daily dosage of the first prescription in patients treated in neuropsychiatric practices in Germany. METHODS: This study included patients aged 60 years or over who were diagnosed with Alzheimer's disease and received anti-dementia prescriptions (galantamine, donepezil, memantine, and rivastigmine) for the first time between 2005 and 2014...
March 29, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28351483/surface-modified-nano-lipid-drug-conjugates-of-positive-allosteric-modulators-of-m1-muscarinic-acetylcholine-receptor-for-the-treatment-of-alzheimer-s-disease
#8
Pavan Kumar Chintamaneni, Praveen T Krishnamurthy, Pachava Vengal Rao, SaiKiran S S Pindiprolu
Acetyl Cholinesterase (AChE) inhibitors such as Donepezil, Rivastigmine and Galantamine are approved by US-FDA as first line drugs to treat the cognitive symptoms of Alzheimer's disease (AD). Their beneficial effects are attributed to their ability to elevate endogenous acetylcholine (ACh) at the M1 muscarinic receptor in the brain. However, their side effects such as nausea, vomiting, dizziness, insomnia, loss of appetite and altered heart rate are related to non-specific activation of M2-M5 muscarinic subtypes in various tissues...
April 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/28328690/the-first-use-of-pralidoxime-in-a-child-with-rivastigmine-poisoning
#9
Eylem Ulaş Saz, Ali Yurtseven, Mehmet Arda Kilinç, Yusuf Sari, Hasan Ağin
The aim of this report is to describe the successful use of pralidoxime in a pediatric patient who accidentally ingested 12 mg of rivastigmine and presented to the emergency department with weakness, drowsiness, hyporeactivity to environmental stimuli, and full cholinergic syndrome. CASE: The patient presented to the emergency department 2 hours after a suspected ingestion of rivastigmine. He was sleepy but oriented and cooperative, hypotonic, and hyporeflexic and has a Glasgow Coma Scale score of 13 (E3M6V4)...
March 21, 2017: Pediatric Emergency Care
https://www.readbyqxmd.com/read/28315690/prediction-of-human-pharmacokinetic-profile-after-transdermal-drug-application-using-excised-human-skin
#10
Syunsuke Yamamoto, Masatoshi Karashima, Yuta Arai, Kimio Tohyama, Nobuyuki Amano
Although several mathematical models have been reported for the estimation of human plasma concentration profiles of drug substances after dermal application, the successful cases that can predict human pharmacokinetic profiles are limited. Therefore, the aim of this study is to investigate the prediction of human plasma concentrations after dermal application using in vitro permeation parameters obtained from excised human skin. The in vitro skin permeability of 7 marketed drug products was evaluated. The plasma concentration-time profiles of the drug substances in humans after their dermal application were simulated using compartment models and the clinical pharmacokinetic parameters...
March 16, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28301952/correction-to-karimzadeh-mahmonir-rashidi-ladan-ganji-fariba-mesoporous-silica-nanoparticles-for-efficient-rivastigmine-hydrogen-tartrate-delivery-into-sy5y-cells
#11
(no author information available yet)
No abstract text is available yet for this article.
June 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28295141/adherence-and-tolerability-of-alzheimer-s-disease-medications-a-pragmatic-randomized-trial
#12
Noll L Campbell, Anthony J Perkins, Sujuan Gao, Todd C Skaar, Lang Li, Hugh C Hendrie, Nicole Fowler, Christopher M Callahan, Malaz A Boustani
BACKGROUND/OBJECTIVES: Post-marketing comparative trials describe medication use patterns in diverse, real-world populations. Our objective was to determine if differences in rates of adherence and tolerability exist among new users to acetylcholinesterase inhibitors (AChEI's). DESIGN: Pragmatic randomized, open label comparative trial of AChEI's currently available in the United States. SETTING: Four memory care practices within four healthcare systems in the greater Indianapolis area...
March 14, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/28276131/different-clinical-effect-of-four-antidementia-drugs-for-alzheimer-s-disease-patients-depending-on-white-matter-severity
#13
Yusuke Fukui, Nozomi Hishikawa, Jin Ichinose, Kota Sato, Yumiko Nakano, Ryuta Morihara, Yasuyuki Ohta, Toru Yamashita, Koji Abe
AIM: To examine the clinical effect of four antidementia drugs (donepezil, galantamine, rivastigmine and memantine) in Alzheimer's disease patients who were divided into subgroups based on their periventricular hyperintensity (PVH) severity. METHODS: A total of 551 Alzheimer's disease patients (201 men and 350 women) were divided into four subgroups based on their PVH severity (0-III). They received monotherapy for 12 months. We compared the clinical effects at the baseline, and at 3, 6 and 12 months after initiation...
March 9, 2017: Geriatrics & Gerontology International
https://www.readbyqxmd.com/read/28271317/cholinergic-anti-inflammatory-pathway-does-not-contribute-to-prevention-of-ulcerative-colitis-by-novel-indoline-carbamates
#14
Helena Shifrin, Odelia Mouhadeb, Nathan Gluck, Chen Varol, Marta Weinstock
Indoline carbamates, AN680 and AN917 decrease cytokines, TNF-α and IL-6 in peritoneal macrophages activated by lipopolysaccharide (LPS) and in mouse tissues after LPS injection. They prevent nuclear translocation of nuclear factor κB (NF-κB) and activator protein 1. Only AN917 inhibits cholinesterase (ChE) at relevant concentrations. ChE inhibitors decrease NF-κB by activating α7 nicotinic acetylcholine receptors (α7nAChR). The current study compared the effect of rivastigmine, a ChE inhibitor, AN680 and AN917 on ulcerative colitis induced in mice by ingestion of dextran sodium sulfate (4...
March 7, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28260511/clinically-relevant-drug-interactions-with-anti-alzheimer-s-drugs
#15
Filippo Caraci, Janet Sultana, Filippo Drago, Edoardo Spina
The aging world population had led to an increase in the prevalence of Alzheimer's disease (AD). The drugs used to slow down the onset of AD, galantamine, donepezil, rivastigmine and memantine, are generally well-tolerated. However, drug interactions between these drugs and other drugs are an important aspect of patient safety that should be borne in mind, particularly given the high burden of polypharmacy in the elderly. The aim of this review is to provide an updated review of clinically significant drug-drug interactions concerning drugs approved for AD...
March 3, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28255308/development-of-a-nanoprecipitation-method-for-the-entrapment-of-a-very-water-soluble-drug-into-eudragit-rl-nanoparticles
#16
Sara Salatin, Jaleh Barar, Mohammad Barzegar-Jalali, Khosro Adibkia, Farhad Kiafar, Mitra Jelvehgari
Rivastigmine hydrogen tartrate (RHT), one of the potential cholinesterase inhibitors, has received great attention as a new drug candidate for the treatment of Alzheimer's disease. However, the bioavailability of RHT from the conventional pharmaceutical forms is low because of the presence of the blood brain barrier. The main aim of the present study was to prepare positively charged Eudragit RL 100 nanoparticles as a model scaffold for providing a sustained release profile for RHT. The formulations were evaluated in terms of particle size, zeta potential, surface morphology, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC)...
February 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28245905/synthesis-of-readily-available-fluorophenylalanine-derivatives-and-investigation-of-their-biological-activity
#17
Martin Krátký, Šárka Štěpánková, Katarína Vorčáková, Lucie Navrátilová, František Trejtnar, Jiřina Stolaříková, Jarmila Vinšová
A series of thirty novel N-acetylated fluorophenylalanine-based aromatic amides and esters was synthesized using N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide or phosphorus trichloride in pyridine. They were characterized by spectral methods and screened against various microbes (Mycobacterium tuberculosis, non-tuberculous mycobacteria, other bacteria, fungi), for their inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and cytotoxicity. All amino acids derivatives revealed a moderate inhibition of both cholinesterases with IC50 values for AChE and BChE of 57...
February 21, 2017: Bioorganic Chemistry
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
#18
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
#19
Jerzy Leszek, G M Ashraf, Wai Hei Tse, Jin Zhang, K Gasiorowski, Marco Fidel Ávila-Rodriguez, Vadim V Tarasov, George E Barreto, S G Klochkov, 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
#20
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
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