scholarly journals Alzheimer’s Disease Pharmacotherapy in Relation to Cholinergic System Involvement

Biomolecules ◽  
2019 ◽  
Vol 10 (1) ◽  
pp. 40 ◽  
Author(s):  
Gabriela Dumitrita Stanciu ◽  
Andrei Luca ◽  
Razvan Nicolae Rusu ◽  
Veronica Bild ◽  
Sorin Ioan Beschea Chiriac ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Global Health ◽  
Disease Progression ◽  
Cholinergic System ◽  
Cholinesterase Inhibitors ◽  
Current Understanding ◽  
Brain Functioning ◽  
System Involvement ◽  
Global Health Challenge

Alzheimer’s disease, a major and increasing global health challenge, is an irreversible, progressive form of dementia, associated with an ongoing decline of brain functioning. The etiology of this disease is not completely understood, and no safe and effective anti-Alzheimer’s disease drug to prevent, stop, or reverse its evolution is currently available. Current pharmacotherapy concentrated on drugs that aimed to improve the cerebral acetylcholine levels by facilitating cholinergic neurotransmission through inhibiting cholinesterase. These compounds, recognized as cholinesterase inhibitors, offer a viable target across key sign domains of Alzheimer’s disease, but have a modest influence on improving the progression of this condition. In this paper, we sought to highlight the current understanding of the cholinergic system involvement in Alzheimer’s disease progression in relation to the recent status of the available cholinesterase inhibitors as effective therapeutics.

Physicians' Efficacy Requirements for Prescribing Medications to Persons with Alzheimer's Disease

2007 ◽  
Vol 26 (2) ◽  
pp. 139-148 ◽  
Author(s):  
Mark Oremus ◽  
Christina Wolfson ◽  
Howard Bergman ◽  
Alain C Vandal
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Disease Progression ◽  
Odds Ratio ◽  
Daily Living ◽  
Cholinesterase Inhibitors ◽  
Postal Survey ◽  
Drug Treatments ◽  
Efficacy Measures ◽  
Cent Level

ABSTRACTPhysicians (N = 803) were contacted via postal survey and given two sets of efficacy measures for drug treatments in Alzheimer's disease: (a) the time that patients spend in a mild or moderate state of disease; (b) levels of modification to disease progression in the areas of cognition, behaviour, and mood, and ability to perform basic activities of daily living. Physicians reported that they would prescribe a hypothetical, new Alzheimer's disease medication if it would allow patients to remain in their current disease state for 15 (mild) or 11 (moderate) additional months. Most physicians required a permanent halt to, or some reversal of, disease progression as a prerequisite for prescribing; a few required substantial reversal. More stringent efficacy requirements were negatively associated with physicians' current prescribing of cholinesterase inhibitors to persons with Alzheimer's disease, although the effects were either small (odds ratio = 0.99) or not statistically significant at the 5 per cent level. The results suggest that physicians with stringent efficacy requirements for clinically relevant efficacy measures are less likely to prescribe cholinesterase inhibitors.

scholarly journals Defeating dementia: Current approaches to potential amyloid-based Alzheimer's disease therapies

2008 ◽  
Vol 30 (5) ◽  
pp. 14-17 ◽  
Author(s):  
Ayesha Khan ◽  
Clive Ballard
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Receptor Antagonist ◽  
Disease Progression ◽  
Cholinesterase Inhibitors ◽  
Neurodegenerative Disorder ◽  
The Uk

Alzheimer's disease (AD) is a progressive neurodegenerative disorder, accounting for 700000 people in the UK and 25 million people worldwide with dementia1. Already licensed treatments, cholinesterase inhibitors and an NMDA (Nmethyldaspartate) receptor antagonist, confer important symptomatic benefits2, but at present, there are no treatments that can delay or halt the disease progression. This review outlines one of the main mechanisms currently thought to underpin the development of AD, and the treatments that are being developed based upon it.

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.

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