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https://www.readbyqxmd.com/read/28733154/community-pharmacists-knowledge-of-alzheimer-disease-care-in-high-and-low-income-chicago
#1
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/28711758/assessing-the-binding-of-cholinesterase-inhibitors-by-docking-and-molecular-dynamics-studies
#2
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
#3
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/28678552/acetylcholinesterase-inhibitors-for-treating-dementia-symptoms-a-safety-evaluation
#4
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
#5
REVIEW
Jan Korábečný, Eugenie Nepovímová, 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/28670949/preparation-and-optimization-of-rivastigmine-loaded-tocopherol-succinate-based-solid-lipid-nanoparticles
#6
Fariba Malekpour-Galogahi, Ashrafalasadat Hatamian-Zarmi, Fariba Ganji, Bahman Ebrahimi-Hosseinzadeh, Fahimeh Nojoki, Razi Sahraeian, Zahra Beagom Mokhtari-Hosseini
Rivastigmine hydrogen tartrate (RHT) is a pseudo-irreversible inhibitor of cholinesterase, and is used for the treatment of Alzheimer's. However, RHT delivery to the brain is limited by the Blood-Brain Barrier (BBB). The purpose of this study was to improve the brain-targeting delivery of RHT by producing and optimizing rivastigmine hydrogen tartrate-loaded tocopherol succinate-based solid lipid nanoparticles (RHT-SLNs). RHT-SLNs were prepared using the microemulsion technique. The impact of significant variables such as surfactant concentration and drug/lipid ratio on the size of RHT-SLNs and their drug loading and encapsulation efficiency was analyzed using a five-level central composite design (CCD)...
July 2, 2017: Journal of Liposome Research
https://www.readbyqxmd.com/read/28670911/bioequivalence-study-of-rivastigmine-6-mg-capsules-single-dose-in-healthy-volunteers
#7
Dhiraj Abhyankar, Ashish Shedage, Milind Gole, Preeti Raut
OBJECTIVE: To assess the bioequivalence of generic formulation of rivastigmine (test) and Exelon (reference). METHODS: This randomized, open-label, 2-period, single-dose, 2-treatment, 2-sequence, crossover study was conducted in 40 healthy men under fed condition. Participants were randomized to receive a single dose of Exelon or rivastigmine capsule. RESULTS: A total of 31 participants completed the study. Area under the concentration-time curve from time zero to time t (AUC0- t) and area under the concentration-time curve from time zero to infinity (AUC0-∞) for Exelon (mean [standard deviation], h·ng/mL) were 126...
January 1, 2017: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/28665099/improvement-in-behavioral-and-psychological-symptoms-of-dementia-by-rivastigmine-patch-in-a-group-of-italian-elderly-patients-with-alzheimer-s-disease
#8
Adriana Servello, Evaristo Ettorre, Mauro Cacciafesta
No abstract text is available yet for this article.
September 2017: Panminerva Medica
https://www.readbyqxmd.com/read/28645134/-arterial-hyper-and-hypotension-associated-with-psychiatric-medications-a-risk-assessment-based-on-the-summaries-of-product-characteristics-smpcs
#9
Roland W Freudenmann, Ninja Freudenmann, Bartosz Zurowski, Carlos Schönfeldt-Lecuona, Ludwig Maier, Roland E Schmieder, Christian Lange-Asschenfeldt, Maximilian Gahr
Introduction Psychiatric medications are well-known triggers of clinically relevant blood pressure changes. Therefore, we aimed at creating ranking lists for their risk of causing arterial hyper- or hypotension. Methods We analyzed 784 Summaries of Product characteristics (SmPCs, available online from "Rote Liste" or "Gelbe Liste" websites) from 105 psychiatric medications registered in adult psychiatry in Germany and extracted the standardized reported risks of increasing or decreasing arterial blood pressure...
June 23, 2017: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/28626484/cognitive-enhancing-of-pineapple-extract-and-juice-in-scopolamine-induced-amnesia-in-mice
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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