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Rivastigmine

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https://www.readbyqxmd.com/read/28626484/cognitive-enhancing-of-pineapple-extract-and-juice-in-scopolamine-induced-amnesia-in-mice
#1
Amir Abbas Momtazi-Borojeni, Hojjat Sadeghi-Aliabadi, Mohammed Rabbani, Alireza Ghannadi, Elham Abdollahi
The objective of the present study was to evaluate the cognitive enhancing of pineapple juice and ethanolic extract in scopolamine-induced cognitive deficit mice. The ethanolic extract of pineapple (Ananas comosus (L.) Merr.) was prepared by maceration method and its juice was obtained by a homogenizer. Object recognition task was used to evaluate the mice memory. Exploration time in the first and second trial was recorded. The differences in exploration time between a familiar and a novel object in the second trial were taken as a memory index...
June 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28617100/discovery-of-potent-and-selective-acetylcholinesterase-ache-inhibitors-acacetin-7-o-methyl-ether-mannich-base-derivatives-synthesised-from-easy-access-natural-product-naringin
#2
Hao-Ran Liu, Xue Men, Xiao-Hui Gao, Lin-Bo Liu, Hao-Qun Fan, Xin-Hua Xia, Qiu-An Wang
Naringin, as a component universal existing in the peel of some fruits or medicinal plants, was usually selected as the material to synthesise bioactive derivates since it was easy to gain with low cost. In present investigation, eight new acacetin-7-O-methyl ether Mannich base derivatives (1-8) were synthesised from naringin. The bioactivity evaluation revealed that most of them exhibited moderate or potent acetylcholinesterase (AChE) inhibitory activity. Among them, compound 7 (IC50 for AChE = 0.82 ± 0...
June 15, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28601231/factors-affecting-therapeutic-response-to-rivastigmine-in-alzheimer-s-disease-patients-in-taiwan
#3
Tzu-Hua Chen, Mei-Chuan Chou, Chiou-Lian Lai, Shyh-Jong Wu, Chia-Ling Hsu, Yuan-Han Yang
Rivastigmine has been widely used in mild-to-moderate Alzheimer's disease (AD), but the therapeutic response rate varies from 20 to 60%. A dose-dependent effect has been suggested, but the plasma concentration of rivastigmine and its metabolite, NAP 226-90, were not measured in previous studies. The influencing factors of therapeutic response are complicated and discordant in various studies among different ethnic groups. Hence, we analyzed the therapeutic responses of rivastigmine, measured by neuropsychological assessments, among 63 clinically diagnosed AD patients taking a daily dosage of 6-9 mg in relation to their plasma concentration of rivastigmine and NAP 226-90, apolipoprotein E (APOE) genotype and demographic characteristics...
June 2017: Kaohsiung Journal of Medical Sciences
https://www.readbyqxmd.com/read/28594244/acute-cholinergic-syndrome-in-a-patient-with-mild-alzheimer-s-type-dementia-who-had-applied-a-large-number-of-rivastigmine-transdermal-patches-on-her-body
#4
Yoshiki Suzuki, Yoshito Kamijo, Tomohiro Yoshizawa, Yuji Fujita, Kiyotaka Usui, Tohru Kishino
CASE PRESENTATION: A 91-year-old woman was transferred to our Emergency Medical Center and Poison Center with somnolence, hypertension (186/61 mm Hg), and repeated vomiting. Three hours later, 10 transdermal patches, each containing 18 mg of rivastigmine (9.5 mg/24 h), were found on her lower back and both thighs, when miosis, facial and trunk sweating, enhanced bowel sound, hypertension, and sinus tachycardia were noted. She was diagnosed with acute cholinergic syndrome due to rivastigmine poisoning...
June 8, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28588366/neurocognitive-effect-of-nootropic-drug-brahmi-bacopa-monnieri-in-alzheimer-s-disease
#5
REVIEW
Kaustubh S Chaudhari, Nishant R Tiwari, Rakesh R Tiwari, Rohan S Sharma
Alzheimer's disease (AD) is a progressive neurodegenerative disease of the elderly. The rapid increase in its incidence has necessitated development of newer drugs. Ayurvedic herbal medications are increasingly researched due to their biosafety profile and usefulness in cognitive impairment. In this article, we critically reviewed one such Medhya Rasayana (nootropic drug) Brahmi-derived from extract of Bacopa monnieri (EBm). Studies have shown that EBm promotes free radical scavenger mechanisms and protects cells in prefrontal cortex, hippocampus, and striatum against cytotoxicity and DNA damage implicated in AD...
May 2017: Annals of Neurosciences
https://www.readbyqxmd.com/read/28553835/pharmacological-manipulation-of-cortical-inhibition-in-the-dorsolateral-prefrontal-cortex
#6
Bahar Salavati, Tarek K Rajji, Reza Zomorrodi, Daniel M Blumberger, Robert Chen, Bruce G Pollock, Zafiris J Daskalakis
Cortical inhibition (CI) occurs largely through GABA receptor mediated inhibitory neurotransmission, which can be modulated by cholinergic, dopaminergic, and glutamatergic inputs. Transcranial magnetic stimulation (TMS) can be used to index CI through a paradigm known as long interval cortical inhibition (LICI). When TMS is combined with electroencephalography (EEG), LICI can index GABA receptor mediated inhibitory neurotransmission in the dorsolateral prefrontal cortex (DLPFC). We conducted a hypothesis-driven pharmacological study to assess the role of cholinergic, dopaminergic, GABAergic, and glutamatergic neurotransmission on LICI from the DLPFC using TMS-EEG...
May 29, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28544619/design-and-synthesis-of-some-acridine-piperazine-hybrids-for-the-improvement-of-cognitive-dysfunction
#7
Anuradha Sharma, Poonam Piplani
A novel series of hybrid molecules (5a-5m) was designed, synthesized and evaluated as multifunctional cholinesterase (ChE) inhibitors against cognitive dysfunction. Heterocyclic moieties acridine and piperazine were conjugated with suitable linkers in a single scaffold and the structures of the target compounds were confirmed by IR, (1) H NMR, (13) C NMR and LC-MS analysis. The pharmacological activity of synthesized compounds was evaluated using behavioral models of amnesia viz. step down passive avoidance and elevated plus maze at a dose 0...
May 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28536360/coconut-cocos-nucifera-ethanolic-leaf-extract-reduces-amyloid-%C3%AE-1-42-aggregation-and-paralysis-prevalence-in-transgenic-caenorhabditis-elegans-independently-of-free-radical-scavenging-and-acetylcholinesterase-inhibition
#8
Rafael Vincent Manalo, Maries Ann Silvestre, Aza Lea Anne Barbosa, Paul Mark Medina
Virgin coconut oil (VCO) has been the subject of several studies which have aimed to alleviate Alzheimer's disease (AD) pathology, focusing on in vitro antioxidant and acetylcholinesterase (AChE) inhibitory activities. Here, we studied an underutilized and lesser-valued part of the coconut tree, specifically the leaves, using in vitro and in vivo approaches. Coconut leaf extract (CLE) was screened for antioxidant and AChE inhibitory properties in vitro and therapeutic effects in two strains of transgenic Caenorhabditis elegans expressing amyloid-β1-42 (Aβ1-42) in muscle cells...
April 21, 2017: Biomedicines
https://www.readbyqxmd.com/read/28506583/synthesis-of-enantiomerically-enriched-drug-precursors-and-an-insect-pheromone-via-reduction-of-ketones-using-commercially-available-carbonyl-reductase-screening-kit-chiralscreen%C3%A2-oh
#9
Toshiya Nagai, Saki Sakurai, Naoki Natori, Manaka Hataoka, Takako Kinoshita, Hiroyoshi Inoue, Kengo Hanaya, Mitsuru Shoji, Takeshi Sugai
Commercially available "Chiralscreen® OH" starter kit containing five types of carbonyl reductases (E001, E007, E031, E039, and E078) was used for the reduction of several aromatic and aliphatic ketones to obtain enantiomerically enriched drug precursors and an insect pheromone. Almost stereochemically pure secondary alcohols, used in the synthesis of drugs such as (R)-rasagiline mesylate, (S)-rivastigmine, (R)-chlorphenesin carbamate, and (R)-mexiletine, and the insect pheromone (4S,5R)-sitophilure, were conveniently obtained...
April 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28498150/effect-of-insulin-on-spatial-memory-in-aluminum-chloride-induced-dementia-in-rats
#10
Madhavan Nampoothiri, Nitesh Kumar, Grandhi Venkata Ramalingayya, Nampurath Gopalan Kutty, Nandakumar Krishnadas, Chamallamudi Mallikarjuna Rao
Latest reports suggest the involvement of insulin in modulating memory. A few published in-vitro studies favor the antidementia effect of insulin. Thus, the present study aimed to evaluate the prophylactic role of insulin and its combination with glucose and its possible mechanism(s) in an aluminum chloride (AlCl3)-induced cognitive dysfunction model in rodents, with a special focus on memory centers namely, the hippocampus and the frontal cortex. Male Wistar rats were exposed to AlCl3 (175 mg/kg orally) for 60 days...
June 14, 2017: Neuroreport
https://www.readbyqxmd.com/read/28458525/rivastigmine-the-advantages-of-dual-inhibition-of-acetylcholinesterase-and-butyrylcholinesterase-and-its-role-in-subcortical-vascular-dementia-and-parkinson-s-disease-dementia
#11
REVIEW
Nagaendran Kandiah, Ming-Chyi Pai, Vorapun Senanarong, Irene Looi, Encarnita Ampil, Kyung Won Park, Ananda Krishna Karanam, Stephen Christopher
Several studies have demonstrated clinical benefits of sustained cholinesterase inhibition with rivastigmine in Alzheimer's disease (AD) and Parkinson's disease dementia (PDD). Unlike donepezil and galantamine that selectively inhibit acetylcholinesterase (AChE; EC 3.1.1.7), rivastigmine is a unique cholinesterase inhibitor with both AChE and butyrylcholinesterase (BuChE; EC 3.1.1.8) inhibitory activity. Rivastigmine is also available as transdermal patch that has been approved by the US Food and Drug Administration for the treatment of mild, moderate, and severe AD as well as mild-to-moderate PDD...
2017: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/28452906/reversible-pisa-syndrome-induced-by-rivastigmine-in-a-patient-with-early-onset-alzheimer-disease
#12
Chih-Wei Hsu, Yu Lee, Chun-Yi Lee, Pao-Yen Lin
Pisa syndrome (PS) is a state of dystonic muscle contraction with a marked truncal deviation to one side. It is an uncommon adverse effect of antipsychotic drugs, but is rarely reported in patients receiving acetylcholinesterase inhibitors, especially rivastigmine. We present a 57-year-old female patient with Alzheimer disease who began to develop symptoms of dementia at the age of 51 years. She was observed to have symptoms of PS after continuous use of rivastigmine (9 mg/d) for nearly 2 years. The PS symptoms improved after the dose of rivastigmine was reduced but recurred when the dose was added back to 9 mg/d...
May 2017: Clinical Neuropharmacology
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
#13
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
#14
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
#15
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
#16
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
#17
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...
May 2, 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
#18
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...
May 12, 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
#19
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...
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
#20
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
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