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Rivastigmine

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https://www.readbyqxmd.com/read/29777723/effect-of-acetylcholinesterase-inhibitors-donepezil-and-rivastigmine-on-the-activity-and-expression-of-cyclooxygenases-in-a-model-of-the-inflammatory-action-of-fluoride-on-macrophages-obtained-from-thp-1-monocytes
#1
Marta Goschorska, Irena Baranowska-Bosiacka, Izabela Gutowska, Maciej Tarnowski, Katarzyna Piotrowska, Emilia Metryka, Krzysztof Safranow, Dariusz Chlubek
Inflammation is an important factor in the development of many diseases of the central nervous system, including Alzheimer's disease and other types of dementia. ‪Given that acetylcholinesterase inhibitors are also currently believed to have anti-inflammatory properties, the purpose of this study was to investigate the effect of acetylcholinesterase inhibitors (rivastigmine, donepezil) on cyclooxygenase activity and expression using the proinflammatory action of fluoride (F- ) on cultured macrophages obtained from THP-1 monocytes...
May 16, 2018: Toxicology
https://www.readbyqxmd.com/read/29772289/nose-to-brain-drug-delivery-an-update-on-clinical-challenges-and-progress-towards-approval-of-anti-alzheimer-drugs
#2
REVIEW
Mukta Agrawal, Swarnlata Saraf, Shailendra Saraf, Sophia G Antimisiaris, Mahavir Chougule, Sunday A Shoyele, Amit Alexander
According to the Alzheimer Association Report (2017), Alzheimer's disease (AD) is the 6th primary cause of death in the USA, which affects nearly 5.5 million people. In the year 2017 itself, the cost of AD treatment in the USA has been reported to rise to $259 billion. This statistic shows the severity of the disease in the USA which is very much similar across the globe. On the other hand, the treatment remains limited to a few conventional oral medications (approved by FDA). These are mainly acting superficially from mild to the moderate AD...
May 14, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29768996/a-systematic-review-on-donepezil-based-derivatives-as-potential-cholinesterase-inhibitors-for-alzheimer-s-disease
#3
Jan Korabecny, Katarina Spilovska, Eva Mezeiova, Ondrej Benek, Radomir Juza, Daniel Kaping, Ondrej Soukup
Alzheimer's disease (AD) is a multifactorial progressive neurodegenerative disorder characterized by memory loss, disorientation, and gradual deterioration of intellectual capacity. Its etiology has not been elucidated yet. To date, only one therapeutic approach has been approved for the treatment of AD. The pharmacotherapy of AD has relied on non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist - memantine, and acetylcholinesterase (AChE) inhibitors (AChEIs) - tacrine, donepezil, rivastigmine and galantamine...
May 16, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29762677/anti-dementia-drugs-for-psychopathology-and-cognitive-impairment-in-schizophrenia-a-systematic-review-and-meta-analysis
#4
Taro Kishi, Toshikazu Ikuta, Kazuto Oya, Shinji Matsunaga, Yuki Matsuda, Nakao Iwata
Background: We conducted a systematic review and meta-analysis of double-blind, randomized, placebo-controlled trials of anti-dementia drugs plus antipsychotics (ADD+AP) for schizophrenia. Methods: Primary outcomes of efficacy and safety included improving overall symptoms (Positive and Negative Syndrome Scale and Brief Psychiatric Rating Scale scores) and all-cause discontinuation, respectively. Other outcomes included psychopathology subscales (positive, negative, general, and anxiety/depressive symptoms), cognitive function (attention/vigilance, reasoning/problem solving, social cognition, speed of processing, verbal learning, visual learning, working memory, and cognitive control/executive function), Mini-Mental State Examination (MMSE) scores, treatment discontinuation due to adverse events and inefficacy, and individual adverse events...
May 14, 2018: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29742912/the-impact-of-a-long-term-rivastigmine-and-donepezil-treatment-on-all-cause-mortality-in-patients-with-alzheimer-s-disease
#5
Jakub Kazmierski, Chaido Messini-Zachou, Mara Gkioka, Magda Tsolaki
Cholinesterase inhibitors (ChEIs) are the mainstays of symptomatic treatment of Alzheimer's disease (AD); however, their efficacy is limited, and their use was associated with deaths in some groups of patients. The aim of the current study was to assess the impact of the long-term use of ChEIs on mortality in patients with AD. This observational, longitudinal study included 1171 adult patients with a diagnosis of AD treated with donepezil or rivastigmine. Each patient was observed for 24 months or until death...
January 1, 2018: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/29742314/benzofuran-and-indole-a-promising-scaffold-for-drug-development-in-alzheimer-s-disease
#6
Deepti Goyal, Amandeep Kaur, Bhupesh Goyal
Alzheimer's disease (AD) is a progressive neurodegenerative disease with no clinically accepted treatment to cure or halt its progression. The Food and Drug Administration (FDA) approved drugs (rivastigmine, donepezil, galantamine and memantine) at best provide marginal benefits thus emphasize the urgent need to explore other molecular entities as future drug candidates for AD. Looking at the wide pharmaceutical applications of heterocyclic compounds and particularly those containing benzofuran and indole ring system; these molecular frameworks draw special attention of the medicinal chemists for further evaluation in numerous diseases...
May 9, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29740299/pharmacological-modulation-of-long-term-potentiation-like-activity-in-the-dorsolateral-prefrontal-cortex
#7
Bahar Salavati, Zafiris J Daskalakis, Reza Zomorrodi, Daniel M Blumberger, Robert Chen, Bruce G Pollock, Tarek K Rajji
Background : Long-term potentiation (LTP) depends on glutamatergic neurotransmission and is modulated by cholinergic, dopaminergic and GABAergic inputs. Paired associative stimulation (PAS) is a neurostimulation paradigm that, when combined with electroencephalography (EEG), assesses LTP-like activity (PAS-induced LTP) in the dorsolateral prefrontal cortex (DLPFC). Thus, we conducted a study to assess the role of cholinergic, dopaminergic, GABAergic and glutamatergic neurotransmission on PAS-induced LTP in the DLPFC...
2018: Frontiers in Human Neuroscience
https://www.readbyqxmd.com/read/29739252/evaluation-of-the-rivastigmine-role-against-botulinum-toxin-a-induced-osteoporosis-in-albino-rats-a-biochemical-histological-and-immunohistochemical-study
#8
D M Ali, W Y Abdelzaher, Smn Abdel-Hafez
The present study aimed to evaluate the role of rivastigmine against the effect of a single unilateral botulinum toxin-A (BTX-A) injection on the bone and bone marrow of adult albino rats 4 weeks after injection. Twenty-four Wistar albino rats were divided into four equal groups: group I, which received distilled water; group II, which received rivastigmine (0.3 mg/kg daily, intraperitoneally for 4 weeks); group III, which received BTX-A (4 IU in 0.2 mL physiological saline) single dose, intramuscularly; and group IV, which received BTX-A + rivastigmine...
January 1, 2018: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/29739128/evaluation-of-acute-and-chronic-effects-of-d-galactose-on-memory-and-learning-in-wistar-rats
#9
Bharti Chogtu, Avinash Arivazhahan, Sushil Kiran Kunder, Amod Tilak, Ravi Sori, Amruta Tripathy
Objective: D-galactose has been commonly used in rodent models to induce accelerated effects of aging, including those on learning, memory, and muscular tone and coordination. This is normally seen on chronic administration of D-galactose. However, there is minimal suggestive evidence on the short-term effects of the same. The aim of the study was to study the acute and chronic effects of D-galactose on learning and memory in Wistar rats. Methods: Twenty four male Wistar rats were randomly assigned to the control, standard (rivastigmine), oral D-galactose (200 mg/kg/day) and subcutaneous D-galactose (200 mg/kg/day) for a total duration of 8 weeks...
May 31, 2018: Clinical Psychopharmacology and Neuroscience: the Official Scientific Journal of the Korean College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29717478/monotherapy-is-good-enough-for-patients-with-mild-to-moderate-alzheimer-s-disease-a-network-meta-analysis-of-76-randomized-controlled-trials
#10
Kelvin Kf Tsoi, Joyce Yc Chan, Felix Ch Chan, Hoyee W Hirai, Timothy Cy Kwok, Samuel Ys Wong
Memantine and the Acetylcholinesterase inhibitors (AChEIs) are two classes of drugs that are used to treat patients with Alzheimer's disease. We conducted a network meta-analysis of randomized controlled trials to compare the treatment effectiveness of monotherapy or combination therapy A total of 23,707 AD patients in 76 randomized trials were identified. In patients with mild-to-moderate AD, monotherapy with donepezil, galantamine or rivastigmine were superior to placebo in enhancing cognitive functions and activities of daily living (ADL), whereas monotherapy with donepezil or memantine were superior to placebo in improving behavioral symptoms...
May 1, 2018: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29706984/rivastigmine-improves-appetite-by-increasing-the-plasma-acyl-des-acyl-ghrelin-ratio-and-cortisol-in-alzheimer-disease
#11
Yoshiko Furiya, Takami Tomiyama, Tesseki Izumi, Naoki Ohba, Satoshi Ueno
Background: Weight loss accelerates cognitive decline and increases mortality in patients with dementia. While acetylcholinesterase (AChE) inhibitors are known to cause appetite loss, we sometimes encounter patients in whom switching from donepezil (AChE inhibitor) to rivastigmine (AChE and butyrylcholinesterase [BuChE] inhibitor) improves appetite. Since BuChE inactivates ghrelin, a potent orexigenic hormone, we speculated that rivastigmine improves appetite by inhibiting BuChE-mediated ghrelin inactivation...
January 2018: Dementia and Geriatric Cognitive Disorders Extra
https://www.readbyqxmd.com/read/29686925/a-stability-indicating-hplc-assay-method-for-analysis-of-rivastigmine-hydrogen-tartrate-in-dual-ligand-nanoparticle-formulation-matrices-and-cell-transport-medium
#12
Naz Hasan Huda, Bhawna Gauri, Heather A E Benson, Yan Chen
The objective of this study was to develop and validate a method for quantitative analysis of rivastigmine hydrogen tartrate (RHT) in dual-ligand polymeric nanoparticle formulation matrices, drug release medium, and cellular transport medium. An isocratic HPLC analysis method using a reverse phase C18 column and a simple mobile phase without buffer was developed, optimised, and fully validated. Analyses were carried out at a flow rate of 1.5 mL/min at 50°C and monitored at 214 nm. This HPLC method exhibited good linearity, accuracy, and selectivity...
2018: Journal of Analytical Methods in Chemistry
https://www.readbyqxmd.com/read/29667758/synthesis-of-enantiomerically-enriched-drug-precursors-by-lactobacillus-paracasei-bd87e6-as-a-biocatalyst
#13
Selda Öksüz, Engin Şahin, Enes Dertli
Global sales of single enantiomeric drug products are growing at an alarming rate every year. A total of 7 bacterial strains were screened for their ability to reduce acetophenones to its corresponding alcohol. Among these strain Lactobacillus paracasei BD87E6 was found to be the most successful biocatalyst to reduce the ketones to the corresponding alcohols. The reaction conditions were systematically optimized for the reducing agent Lactobacillus paracasei BD87E6, which showed high enantioselectivity and conversion for the bioreduction...
April 18, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29666099/collapse-in-the-elderly-rivastigmine-induced-heart-block-and-a-literature-review-of-the-pharmacology-of-acetylcholinesterase-inhibitors-used-in-alzheimer-s-disease
#14
Olushola Alonge, Fahad Mujtaba Iqbal, Elzbieta Cifonelli
Falls resulting in neck of femur fractures are common in the elderly. Often multiple comorbidities can make management and diagnosis of such a polyfactorial condition difficult, particularly with Alzheimer's dementia (AD). Indeed, poorly managed AD may contribute to falls. We present our management of an 87-year-old woman, on rivastigmine for AD, who presented with a collapse episode-attributed to rivastigmine-resulting in a neck of femur fracture. Furthermore, we perform a literature review of the pharmacology of acetylcholinesterase inhibitors and how their use in AD may contribute to bradyarrhythmias...
April 17, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29621640/synthesis-and-characterization-of-new-inhibitors-of-cholinesterases-based-on-n-phenylcarbamates-in-vitro-study-of-inhibitory-effect-type-of-inhibition-lipophilicity-and-molecular-docking
#15
Katarína Vorčáková, Magdaléna Májeková, Eva Horáková, Pavel Drabina, Miloš Sedlák, Šárka Štěpánková
Based on current treatment of Alzheimer's disease, where the carbamate inhibitor Rivastigmine is used, two series of carbamate derivatives were prepared: (i) N-phenylcarbamates with additional carbamate group (1-12) and (ii) N-phenylcarbamates with monosaccharide moiety (13-24). All compounds were tested for the inhibitory effect on both of the cholinesterases, electric eel acetylcholinesterase (eeAChE) and butyrylcholinesterase from equine serum (eqBChE) and the inhibitory activity (expressed as IC50 values) was compared with that of the established drugs Galanthamine and Rivastigmine...
March 28, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29620690/angioedema-caused-by-rivastigmine-patch-a-rare-case
#16
Mehmet Ilkin Naharci, Ilker Tasci
No abstract text is available yet for this article.
April 3, 2018: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29570866/international-parkinson-and-movement-disorder-society-evidence-based-medicine-review-update-on-treatments-for-the-motor-symptoms-of-parkinson-s-disease
#17
REVIEW
Susan H Fox, Regina Katzenschlager, Shen-Yang Lim, Brandon Barton, Rob M A de Bie, Klaus Seppi, Miguel Coelho, Cristina Sampaio
OBJECTIVE: The objective of this review was to update evidence-based medicine recommendations for treating motor symptoms of Parkinson's disease (PD). BACKGROUND: The Movement Disorder Society Evidence-Based Medicine Committee recommendations for treatments of PD were first published in 2002 and updated in 2011, and we continued the review to December 31, 2016. METHODS: Level I studies of interventions for motor symptoms were reviewed. Criteria for inclusion and quality scoring were as previously reported...
March 23, 2018: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/29553158/cholinergic-medication-for-antipsychotic-induced-tardive-dyskinesia
#18
REVIEW
Irina Tammenmaa-Aho, Rosie Asher, Karla Soares-Weiser, Hanna Bergman
BACKGROUND: Tardive dyskinesia (TD) remains a troublesome adverse effect of conventional antipsychotic (neuroleptic) medication. It has been proposed that TD could have a component of central cholinergic deficiency. Cholinergic drugs have been used to treat TD. OBJECTIVES: To determine the effects of cholinergic drugs (arecoline, choline, deanol, lecithin, meclofenoxate, physostigmine, RS 86, tacrine, metoxytacrine, galantamine, ipidacrine, donepezil, rivastigmine, eptastigmine, metrifonate, xanomeline, cevimeline) for treating antipsychotic-induced TD in people with schizophrenia or other chronic mental illness...
March 19, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29550337/paeonol-promotes-hippocampal-synaptic-transmission-the-role-of-the-kv2-1-potassium-channel
#19
Chin-Tsang Yang, Guan-Ling Lu, Sheng-Feng Hsu, Iona MacDonald, Lih-Chu Chiou, Shih-Ya Hung, Yi-Hung Chen
Paeonol is a major constituent of the Chinese herb Moutan cortex radices. Recent studies report that paeonol has neuroprotective effects and improves impaired learning and memory. However, its underlying mechanisms by which paeonol contributes to synaptic transmission remain unclear. In this study, we found that paeonol increased the frequency of miniature excitatory postsynaptic currents (mEPSCs) and spontaneous excitatory postsynaptic currents (sEPSCs), but had no effect on the amplitude in rat hippocampal CA1 neurons...
March 14, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29537978/a-randomized-trial-of-oral-and-transdermal-rivastigmine-for-postural-instability-in-parkinson-disease-dementia
#20
Jaime McDonald, Emmanuelle Pourcher, Alexandra Nadeau, Philippe Corbeil
OBJECTIVES: The objective of this study was to compare the efficacy and safety of oral and transdermal rivastigmine for postural instability in patients with Parkinson disease dementia (PDD) who were candidates for a cholinesterase inhibitor. The primary outcome was the change in mean velocity of the center of pressure (CoP) after 6 months. Secondary outcomes included structural parameters of dynamic posturography, clinical rating scales, and adverse events requiring dose reduction. METHODS: Patients with PDD were randomized in a 1:1 ratio to oral or transdermal rivastigmine with target doses of 6 mg twice daily and 9...
March 13, 2018: Clinical Neuropharmacology
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