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Rivastigmine

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https://www.readbyqxmd.com/read/28923321/nose-to-brain-delivery-of-rivastigmine-by-in-situ-gelling-cationic-nanostructured-lipid-carriers-enhanced-brain-distribution-and-pharmacodynamics
#1
Preeti Wavikar, Rohan Pai, Pradeep Vavia
Present investigation explores the potential of Nanostructured Lipid Carriers (NLCs) for nose to brain delivery of Rivastigmine (RV), which is further enhanced by incorporating into an in-situ gelling system, increasing retention in nasal cavity. NLC's having particle size of 123.2±2.3 nm, entrapment efficiency of 68.3±3.4% and zeta potential of 32±1.2 mV was fabricated by a scalable method. Pharmacokinetics showed sustained release of intranasal (IN) and intravenous (IV) NLC's compared to RV solution by same route, with significantly higher AUC and Thalf...
September 15, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28901528/beyond-symptomatic-effects-donepezil-s-potential-for-neuroprotection-and-disease-modification-in-alzheimer-s-disease
#2
REVIEW
Seung Hyun Kim, Nagaendran Kandiah, Jung-Lung Hsu, Chuthamanee Suthisisang, Chesda Udommongkol, Amitabh Dash
Alzheimer's disease (AD) is associated with neurodegenerative changes resulting clinically in progressive cognitive and functional deficits. The only therapies are the cholinesterase inhibitors (ChEIs) donepezil, galantamine, and rivastigmine and the N-methyl-D-aspartate-receptor antagonist memantine. Donepezil acts primarily on the cholinergic system as symptomatic treatment, but it also has potential for disease modification and may reduce the rate of progression of AD. This review explores the potential for a disease modifying effect of donepezil...
September 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28865359/thermosensitive-in-situ-nanocomposite-of-rivastigmine-hydrogen-tartrate-as-an-intranasal-delivery-system-development-characterization-ex-vivo-permeation-and-cellular-studies
#3
S Salatin, J Barar, M Barzegar-Jalali, Kh Adibkia, M Jelvehgari
Intranasal administration of pharmaceutical compounds is gaining considerable attention as an alternative route for localized/systemic drug delivery. However, insufficient therapeutic efficacy of drugs via this route seems to be a major challenge for development of de novo intranasal formulations. This shortcoming can be overcome by simultaneous utilization of a nanoparticulate delivery system with a polymeric gel network. Therefore, the main aim of the present study was to develop erodible in-situ gel forming systems of poloxamer 407(®) (P407) as a promising platform, capable of prolonging rivastigmine hydrogen tartrate (RHT) release from the embedded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs)...
August 24, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28855009/ache-inhibitors-and-nmda-receptor-antagonists-in-advanced-alzheimer-s-disease
#4
Brianna E Glynn-Servedio, Trisha Seys Ranola
OBJECTIVE: The objective of this article is to review the available evidence for duration of treatment with, and considerations for discontinuation of, acetylcholinesterase inhibitors and N-methyl-<small>d</small>-aspartate receptor antagonists in Alzheimer's disease. DATA SOURCES: Literature searches of clinical trials and meta-analyses were conducted using PubMed with the search terms Alzheimer's, dementia, donepezil, galantamine, memantine, and rivastigmine...
September 1, 2017: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
https://www.readbyqxmd.com/read/28854283/transdermal-rivastigmine-for-hiv-associated-cognitive-impairment-a-randomized-pilot-study
#5
Jose A Muñoz-Moreno, Anna Prats, José Moltó, Maite Garolera, Núria Pérez-Álvarez, Crisanto Díez-Quevedo, Cristina Miranda, Carmina R Fumaz, Maria J Ferrer, Bonaventura Clotet
OBJECTIVE: To assess the efficacy and safety of transdermal rivastigmine for the treatment of HIV-associated cognitive impairment. METHODS: We recruited HIV-infected patients with cognitive impairment on stable antiretroviral therapy in a randomized controlled pilot trial with a 48-week follow-up. An additional assessment was held at 12 weeks. Participants received transdermal rivastigmine (9.5 mg daily), lithium (400 mg twice daily, titrated progressively), or remained in a control group (no new medication)...
2017: PloS One
https://www.readbyqxmd.com/read/28832937/systematic-review-of-sex-specific-reporting-of-data-cholinesterase-inhibitor-example
#6
Nishila Mehta, Craig Rodrigues, Manpreet Lamba, Wei Wu, Susan E Bronskill, Nathan Herrmann, Sudeep S Gill, An-Wen Chan, Robin Mason, Suzanne Day, Jerry H Gurwitz, Paula A Rochon
OBJECTIVES: To improve the value of research for older adults, we examine sex-specific reporting of data from drug trials for the management of dementia. These data are important because they may influence considerations ranging from the health of populations to shared decision-making by individual patient and caregiver about the risk and benefit of a drug therapy. METHODS: Randomized controlled trials of cholinesterase inhibitors (i.e., donepezil, rivastigmine, or galantamine) with clinical outcomes were identified from searches of MEDLINE, EMBASE, and the Cochrane Library...
August 18, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/28829178/rivastigmine-for-treatment-resistant-post-traumatic-stress-disorder
#7
Alexander Murray, Duncan Wallace, Olav Nielssen
No abstract text is available yet for this article.
September 2017: Australian and New Zealand Journal of Psychiatry
https://www.readbyqxmd.com/read/28827871/cognitive-effects-with-rivastigmine-augmentation-of-risperidone-a-12-month-randomized-double-blind-placebo-controlled-study-in-schizophrenia
#8
Pattath Narayanan Suresh Kumar, Seema P Mohemmedali, P K Anish, Chittaranjan Andrade
OBJECTIVE: An important challenge in schizophrenia therapeutics is to develop an efficacious treatment for cognitive impairment. Acetylcholinesterase inhibitors, such as rivastigmine, have been studied for improving cognitive performance in these patients. MATERIALS AND METHODS: Rivastigmine (uptitrated to 6 mg/day) was given as an add-on therapy to risperidone-treated stable schizophrenia patients in a randomized, double-blind, placebo-controlled design. Of 67 patients who met eligibility criteria, 55 were recruited into the study...
April 2017: Indian Journal of Psychiatry
https://www.readbyqxmd.com/read/28782481/rational-approaches-design-strategies-structure-activity-relationship-and-mechanistic-insights-for-esterase-inhibitors
#9
Harbinder Singh, Jatinder Vir Singh, Navdeep Kaur, Mohit Sanduja, Gurpreet Singh, Preet Mohinder Singh Bedi, Sahil Sharma
BACKGROUND: Esterase is an enzyme that splits esters into an acid and alcohol. Varieties of esterases are present in human body to control diverse set of cellular processes and execute their specific functions. It can be seen that any increase in metabolites produced by these enzymes lead to severe pathological conditions like Alzheimer disease, hypercholesterolemia etc. OBJECTIVE: Numerous esterase inhibitors have been developed and reported by the researchers around the globe, but not systematically summarized yet...
August 7, 2017: Mini Reviews in Medicinal Chemistry
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
#10
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/28733154/community-pharmacists-knowledge-of-alzheimer-disease-care-in-high-and-low-income-chicago
#11
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
#12
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
#13
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
#14
REVIEW
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...
September 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
#15
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/28670949/preparation-and-optimization-of-rivastigmine-loaded-tocopherol-succinate-based-solid-lipid-nanoparticles
#16
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
#17
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
#18
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
#19
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...
August 2017: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/28626484/cognitive-enhancing-of-pineapple-extract-and-juice-in-scopolamine-induced-amnesia-in-mice
#20
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
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