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Rivastigmine

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https://www.readbyqxmd.com/read/29135926/proline-based-carbamates-as-cholinesterase-inhibitors
#1
Hana Pizova, Marketa Havelkova, Sarka Stepankova, Andrzej Bak, Tereza Kauerova, Violetta Kozik, Michal Oravec, Ales Imramovsky, Peter Kollar, Pavel Bobal, Josef Jampilek
Series of twenty-five benzyl (2S)-2-(arylcarbamoyl)pyrrolidine-1-carboxylates was prepared and completely characterized. All the compounds were tested for their in vitro ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and the selectivity of compounds to individual cholinesterases was determined. Screening of the cytotoxicity of all the compounds was performed using a human monocytic leukaemia THP-1 cell line, and the compounds demonstrated insignificant toxicity. All the compounds showed rather moderate inhibitory effect against AChE; benzyl (2S)-2-[(2-chlorophenyl)carbamoyl]pyrrolidine-1-carboxylate (IC50 = 46...
November 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29131306/comparative-effectiveness-and-safety-of-cognitive-enhancers-for-treating-alzheimer-s-disease-systematic-review-and-network-metaanalysis
#2
Andrea C Tricco, Huda M Ashoor, Charlene Soobiah, Patricia Rios, Areti Angeliki Veroniki, Jemila S Hamid, John D Ivory, Paul A Khan, Fatemeh Yazdi, Marco Ghassemi, Erik Blondal, Joanne M Ho, Carmen H Ng, Brenda Hemmelgarn, Sumit R Majumdar, Laure Perrier, Sharon E Straus
BACKGROUND/OBJECTIVES: To examine the comparative effectiveness and safety of cognitive enhancers for Alzheimer's disease (AD). DESIGN: Systematic review and Bayesian network metaanalysis (NMA). SETTING: MEDLINE, EMBASE, Cochrane Library, CINAHL, Ageline (inception-March 2016). PARTICIPANTS: Individuals with AD in randomized controlled trials (RCTs), quasi-RCTs, and nonrandomized studies. INTERVENTION: Any combination of donepezil, rivastigmine, galantamine, or memantine...
September 29, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/29119798/a-very-low-dose-of-rivastigmine-induced-pisa-syndrome-in-a-clozapine-treated-patient
#3
Pei-Chun Chao, Juo-Chi Li, Ta-Chuan Yeh, Chin-Bin Yeh
No abstract text is available yet for this article.
November 1, 2017: Australian and New Zealand Journal of Psychiatry
https://www.readbyqxmd.com/read/29102759/preclinical-profile-of-a-dopamine-d1-potentiator-suggests-therapeutic-utility-in-neurological-and-psychiatric-disorders
#4
Robert F Bruns, Stephen N Mitchell, Keith A Wafford, Alex J Harper, Elaine A Shanks, Guy Carter, Michael J O'Neill, Tracey K Murray, Brian J Eastwood, John M Schaus, James P Beck, Junliang Hao, Jeffrey M Witkin, Xia Li, Eyassu Chernet, Jason S Katner, Hong Wang, John W Ryder, Meghane E Masquelin, Linda K Thompson, Patrick L Love, Deanna L Maren, Julie F Falcone, Michelle M Menezes, Linli Zhang, Charles R Yang, Kjell A Svensson
DETQ, an allosteric potentiator of the dopamine D1 receptor, was tested in therapeutic models that were known to respond to D1 agonists. Because of a species difference in affinity for DETQ, all rodent experiments used transgenic mice expressing the human D1 receptor (hD1 mice). When given alone, DETQ reversed the locomotor depression caused by a low dose of reserpine. DETQ also acted synergistically with L-DOPA to reverse the strong hypokinesia seen with a higher dose of reserpine. These results indicate potential as both monotherapy and adjunct treatment in Parkinson's disease...
October 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29034195/protective-effect-of-hydro-alcoholic-extract-of-salvia-haematodes-wall-root-on-cognitive-functions-in-scopolamine-induced-amnesia-in-rats
#5
Mohammad Shawwal, Badruddeen, Mohammad Khushtar, Md Azizur Rahman
Diminished cholinergic transmission may be responsible for development of amnesia. Hence, the present study was undertaken to investigate the possible protective effect of hydro-alcoholic extract of Salvia haematodes Wall root (HESH) on cognitive functions in scopolamine-induced amnesia in adult Sprague Dawley rats. The rats were divided randomly into five groups each consisting of five rats (n = 5). Rats of the groups I, II, III, IV, and V received orally normal saline (10 ml/kg b. wt.), normal saline (10 ml/kg), standard drug rivastigmine (1...
October 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/29032750/longitudinal-neuropsychological-outcome-in-taiwanese-alzheimer-s-disease-patients-treated-with-medication
#6
Yuan-Han Yang, Meng-Ni Wu, Ping-Song Chou, Hui-Chen Su, Sheng-Hsiang Lin, Pi-Shan Sung
Background The longitudinal change of neuropsychological tests (NPTs) in treated Alzheimer's disease (AD) is essential to understand the interplay of a therapeutic response from medication and a disease decline due to degenerative processes. The aim of our study is to investigate the annual cognitive progression as measured by commonly used NPTs in treated AD patients and to assess the potential predictors of disease progression. Methods Participants (N=455) diagnosed with AD and treated with cholinesterase inhibitors (ChEIs) or memantine at memory clinics in three hospitals in southern Taiwan from January 2009 to December 2014 were enrolled in this prospectively registered study...
October 10, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/29031070/nature-based-molecules-combined-with-rivastigmine-a-symbiotic-approach-for-the-synthesis-of-new-agents-against-alzheimer-s-disease
#7
Giulia Nesi, Qiuhe Chen, Simona Sestito, Maria Digiacomo, Xiaohong Yang, Shengnan Wang, Rongbiao Pi, Simona Rapposelli
Starting from nature as original source, new potential agents with pleiotropic activities have been synthesized and evaluated as neuroprotective agents. In this work, novel nature-based hybrids, combining antioxidant motifs with rivastigmine, have been designed and synthesized. The biological results revealed that the new compounds inhibit both AChE and BuChE. In particular, lipoic acid hybrids LA1, LA2, LA3 resulted to be the most potent inhibitors of BuChE showing IC50 values ranging from 340 to 378 nM. Analogously, all the compounds were able to inhibit the self β-amyloid1-42 aggregation...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28978455/the-present-and-future-of-pharmacotherapy-of-alzheimer-s-disease-a-comprehensive-review
#8
REVIEW
Abhinav Anand, Albert Anosi Patience, Neha Sharma, Navneet Khurana
Alzheimer's disease (AD) is a generalized term used for the loss in memory and other intellectual abilities on levels serious enough to interfere with daily life. It accounts for 60-80% of dementia cases. The characteristic features include aggregation of Amyloid-Beta (Aβ) plaques and Tau Protein Tangles in the nervous tissue of brain. Another important aspect associated with development of AD is the decrease in levels of Acetylcholine (ACh) in brain. The conventional pharmacotherapy of AD employs the use of compounds that inhibit the enzyme acetylcholinesterase (e...
November 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28974110/acetylcholinesterase-inhibitors-beneficial-effects-on-comorbidities-in-patients-with-alzheimer-s-disease
#9
Vinod Kaushik, Sarah Toombs Smith, Emmanuel Mikobi, Mukaila A Raji
Elderly patients with Alzheimer's disease (AD) and other dementias are at high risk of polypharmacy and excessive polypharmacy for common coexisting medical conditions. Polypharmacy increases the risk of drug-drug and drug-disease interactions in these patients who may not be able to communicate early symptoms of adverse drug events. Three acetylcholinesterase inhibitors (ACHEIs) have been approved for AD: donepezil (Aricept), rivastigmine (Exelon), and galantamine (Razadyne). They are also used off-label for other causes of dementia such as Lewy body and vascular dementia...
January 1, 2017: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/28970454/community-pharmacists-knowledge-regarding-donepezil-averse-effects-and-self-care-recommendations-for-insomnia-for-persons-with-ad
#10
Marketa Marvanova, Paul Jacob Henkel
Alzheimer's disease (AD) impacts millions of individuals worldwide. Since no cure is currently available, acetylcholinesterase inhibitors are symptomatic therapy. This study assessed community pharmacists' knowledge regarding donepezil adverse effects (AEs) and self-care recommendations for insomnia management for persons with AD treated with rivastigmine. This is a cross-sectional, standardized telephone survey of community pharmacists (n = 862) in three study areas: West Virginia, North Dakota/South Dakota, and Southern Oregon/Northern California...
July 28, 2017: Pharmacy (Basel, Switzerland)
https://www.readbyqxmd.com/read/28966636/heterocyclic-compounds-as-key-structures-for-the-interaction-with-old-and-new-targets-in-alzheimer-s-disease-therapy
#11
REVIEW
Asha Hiremathad, Luca Piemontese
Nowadays, Alzheimer's disease (AD) is widely recognized as a real social problem. In fact, only five drugs are FDA approved for the therapy of this widespread neurodegenerative disease, but with low results so far. Three of them (rivastigmine, donepezil and galantamine) are acetylcholinesterase inhibitors, memantine is a N-methyl-D-aspartate receptor antagonist, whereas the fifth formulation is a combination of donepezil with memantine. The prevention and treatment of AD is the new challenge for pharmaceutical industry, as well as for public institutions, physicians, patients, and their families...
August 2017: Neural Regeneration Research
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
#12
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. NLCs 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) NLCs compared with 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
#13
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
#14
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
#15
REVIEW
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
#16
RANDOMIZED CONTROLLED TRIAL
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
#17
REVIEW
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...
October 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/28829178/rivastigmine-for-treatment-resistant-post-traumatic-stress-disorder
#18
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
#19
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
#20
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
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