scholarly journals Progress in Clinical Neurosciences: Treatment of Alzheimer’s Disease and Other Dementias - Review and Comparison of the Cholinesterase Inhibitors

2002 ◽  
Vol 29 (4) ◽  
pp. 306-314 ◽  
Author(s):  
David B. Hogan ◽  
Christopher Patterson
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Side Effect ◽  
Cholinesterase Inhibitors ◽  
Mechanisms Of Action ◽  
Convincing Evidence ◽  
Clinical State ◽  
Moderate Dementia ◽  
Alzheimer’S Pathology ◽  
Clinical Trails

Background:Alzheimer’s disease (AD) is the most common cause of dementia in older adults. Acceptance of the cholinergic hypothesis led to a search for medications which could enhance central cholinergic activity in this condition. There are now three cholinesterase inhibitors available for the treatment of AD in Canada.Objectives:To review the currently available cholinesterase inhibitors approved for the treatment of AD in Canada and to provide guidance on who and how to treat with these agents.Results:Donepezil, rivastigmine, and galantamine are approved for the treatment of AD in Canada. In clinical trails, patients with mild to moderate AD treated with these agents experienced modest improvements in cognition, function, behaviour, and/or global clinical state. The magnitude of benefits seen with each agent appeared to be similar. While to date, there is no convincing evidence that one is more efficacious or effective, they do differ in their pharmacokinetics, additional mechanisms of action, and side effect profiles. Therefore, the selection of agent will be based on considerations such as side effect profiles, ease of administration, personal familiarity/experience, and beliefs about the importance of the noted differences in their pharmacokinetics and additional mechanisms of action.Conclusion:We believe that these agents should be offered to all individuals with a mild to moderate dementia where Alzheimer’s pathology is felt to be a contributing factor. We view all three available cholinesterase inhibitors as first-line drugs.

scholarly journals Good rate of clinical response to cholinesterase inhibitors in mild and moderate Alzheimer's disease after three months of treatment: An open-label study

2013 ◽  
Vol 7 (2) ◽  
pp. 190-196 ◽  
Author(s):  
Luis Felipe José Ravic de Miranda ◽  
Marilourdes do Amaral Barbosa ◽  
Patrícia Regina Henrique Peles ◽  
Patrícia Hilar Pôças ◽  
Pedro Augusto Lopes Tito ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cerebrovascular Disease ◽  
Clinical Response ◽  
Cholinesterase Inhibitors ◽  
Rating Scale ◽  
The Elderly ◽  
Open Label ◽  
Age Related ◽  
Moderate Dementia

ABSTRACT Life expectancy in Brazil has increased markedly over the last 30 years. Hence, age-related disorders, such as Alzheimer's disease (AD), warrant special attention due to their high prevalence in the elderly. Pharmacologic treatment of AD is based on cholinesterase inhibitors (ChEI) and memantine, leading to modest clinical benefits both in the short and long-term. However, clinical response is heterogeneous and needs further investigation. Objective: To investigate the rate of response to ChEI in AD after three months of treatment. Methods: Patients with mild or moderate dementia due to probable AD or to AD associated with cerebrovascular disease were included in the study. The subjects were assessed at baseline and again after three months of ChEI treatment. Subjects were submitted to the Mini-Mental State Examination (MMSE), Mattis Dementia Rating Scale, Katz Basic Activities of Daily Living, Pfeffer Functional Activities Questionnaire, Neuropsychiatric Inventory and Cornell Scale for Depression in Dementia. Good response was defined by a gain of ≥2 points on the MMSE after three months of treatment in relation to baseline. Results: Seventy-one patients, 66 (93%) with probable AD and five (7%) with AD associated with cerebrovascular disease, were evaluated. The good response rate at three months was 31.0%, being 37.2% and 21.4% in mild and moderate dementia, respectively. There were no significant differences on most tests, except for improvement in hallucinations, agitation and dysphoria in moderate dementia patients. Conclusion: The rate of good clinical response to ChEI was higher than usually reported. Specific behavioral features significantly improved in the subgroup of moderate dementia.

Drug Design of Inhibitors of Alzheimer’s Disease (AD): POM and DFT Analyses of Cholinesterase Inhibitory Activity of β-amino di-Carbonyl Derivatives

2019 ◽  
Vol 19 (8) ◽  
pp. 688-705
Author(s):  
Taibi Ben Hadda ◽  
Abdur Rauf ◽  
Hsaine Zgou ◽  
Fatma Sezer Senol ◽  
Ilkay Erdogan Orhan ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
Metal Accumulation ◽  
Microtiter Plate ◽  
Metal Chelation ◽  
Carbonyl Derivatives ◽  
Cholinesterase Inhibitory Activity ◽  
Inhibitory Potential

Background:Since deficit of acetylcholine has been evidenced in the Alzheimer’s disease (AD) patients, cholinesterase inhibitors are currently the most specified drug category for the remediation of AD.Method:In the present study, 16 compounds (1-16) with dicarbonyl skeletons have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 100 μg/mL. Since metal accumulation is related to AD, the compounds were also tested for their metal-chelation capacity.Results and Conclusion:All the investigated dicarbonyl compounds exerted none or lower than 30% inhibition against both cholinesterases, whereas compounds 2, 8 and 11 showed 37, 42, 41% of inhibition towards BChE, being the most active. The highest metal-chelation capacity was observed with compound 8 (53.58 ± 2.06%). POM and DFT analyses are in good harmonization with experimental data.

scholarly journals Virtual Reality-Based Cognitive Stimulation on People with Mild to Moderate Dementia due to Alzheimer’s Disease: A Pilot Randomized Controlled Trial

2021 ◽  
Vol 18 (10) ◽  
pp. 5290
Author(s):  
Jorge Oliveira ◽  
Pedro Gamito ◽  
Teresa Souto ◽  
Rita Conde ◽  
Maria Ferreira ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Randomized Controlled Trial ◽  
Virtual Reality ◽  
Cognitive Function ◽  
Controlled Trial ◽  
Cognitive Stimulation ◽  
Randomized Controlled ◽  
Moderate Dementia ◽  
Pilot Randomized Controlled Trial

The use of ecologically oriented approaches with virtual reality (VR) depicting instrumental activities of daily living (IADL) is a promising approach for interventions on acquired brain injuries. However, the results of such an approach on dementia caused by Alzheimer’s disease (AD) are still lacking. This research reports on a pilot randomized controlled trial that aimed to explore the effect of a cognitive stimulation reproducing several IADL in VR on people with mild-to-moderate dementia caused by AD. Patients were recruited from residential care homes of Santa Casa da Misericórdia da Amadora (SCMA), which is a relevant nonprofit social and healthcare provider in Portugal. This intervention lasted two months, with a total of 10 sessions (two sessions/week). A neuropsychological assessment was carried out at the baseline and follow-up using established neuropsychological instruments for assessing memory, attention, and executive functions. The sample consisted of 17 patients of both genders randomly assigned to the experimental and control groups. The preliminary results suggested an improvement in overall cognitive function in the experimental group, with an effect size corresponding to a large effect in global cognition, which suggests that this approach is effective for neurocognitive stimulation in older adults with dementia, contributing to maintaining cognitive function in AD.

scholarly journals Marine-Derived Compounds with Anti-Alzheimer’s Disease Activities

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 410
Author(s):  
Salar Hafez Ghoran ◽  
Anake Kijjoa
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Thinking Skills ◽  
Mechanisms Of Action ◽  
Brain Disorder ◽  
Brain Functioning ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds

Alzheimer’s disease (AD) is an irreversible and progressive brain disorder that slowly destroys memory and thinking skills, and, eventually, the ability to perform simple tasks. As the aging population continues to increase exponentially, AD has become a big concern for society. Therefore, neuroprotective compounds are in the spotlight, as a means to tackle this problem. On the other hand, since it is believed—in many cultures—that marine organisms in an individual diet cannot only improve brain functioning, but also slow down its dysfunction, many researchers have focused on identifying neuroprotective compounds from marine resources. The fact that the marine environment is a rich source of structurally unique and biologically and pharmacologically active compounds, with unprecedented mechanisms of action, marine macroorganisms, such as tunicates, corals, sponges, algae, as well as microorganisms, such as marine-derived bacteria, actinomycetes, and fungi, have been the target sources of these compounds. Therefore, this literature review summarizes and categorizes various classes of marine-derived compounds that are able to inhibit key enzymes involved in AD, including acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), β-secretase (BACE-1), and different kinases, together with the related pathways involved in the pathogenesis of AD. The compounds discussed herein are emerging as promising anti-AD activities for further in-depth in vitro and in vivo investigations, to gain more insight of their mechanisms of action and for the development of potential anti-AD drug leads.

Pharmacotherapies for Alzheimer's disease: Beyond cholinesterase inhibitors

2012 ◽  
Vol 134 (1) ◽  
pp. 8-25 ◽  
Author(s):  
Haythum O. Tayeb ◽  
Hyun Duk Yang ◽  
Bruce H. Price ◽  
Frank I. Tarazi
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors

scholarly journals Efficacy of SSRIs on cognition of Alzheimer's disease patients treated with cholinesterase inhibitors

2009 ◽  
Vol 22 (1) ◽  
pp. 114-119 ◽  
Author(s):  
Luca Rozzini ◽  
Barbara Vicini Chilovi ◽  
Marta Conti ◽  
Erik Bertoletti ◽  
Marina Zanetti ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
Mmse Score ◽  
Joint Effect ◽  
Negative Effects ◽  
Multidimensional Assessment ◽  
Degree Of Protection ◽  
Depressed Patients ◽  
The Mean

ABSTRACTBackground: This study examines the joint effect on cognition of selective serotonin re-uptake inhibitors (SSRIs) and cholinesterase inhibitors (AChEIs) in depressed patients affected by Alzheimer's disease (AD) living at home.Methods: The study was conducted in two different outpatient neurological clinics. 338 patients with probable AD were treated with ChEis (donepezil, rivastigmine and galantamine) as per the clinician's judgment and were observed for nine months. At study entry, participants underwent a multidimensional assessment evaluating cognitive, functional and psychobehavioral domains. All patients were evaluated at baseline, after one (T1), three (T2) and nine months (T3). Patients were grouped in three different categories (patients not depressed and not treated with SSRIs, patients depressed and treated with SSRIs, and patients depressed but not treated with SSRIs).Results: At baseline 182 were diagnosed as not depressed and not treated with SSRIs, 66 as depressed and treated with SSRIs, and 90 as depressed but not treated with SSRIs. The mean change in MMSE score from baseline to nine months showed that depressed patients not treated worsened in comparison with those not depressed and not treated with SSRIs (mean change −0.8 ± 2.3 vs 0.04 ± 2.9; p = 0.02) and patients depressed and treated with SSRI (mean change −0.8 ± 2.3 vs 0.1 ± 2.5; p = 0.03).Conclusions: In AD patients treated with AChEIs, SSRIs may exert some degree of protection against the negative effects of depression on cognition.

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