scholarly journals New drugs for Alzheimer's disease and other dementias

2002 ◽  
Vol 180 (2) ◽  
pp. 135-139 ◽  
Author(s):  
Roger Bullock
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Observational Studies ◽  
Cholinesterase Inhibitors ◽  
Treatment Options ◽  
Clinical Excellence ◽  
Good Evidence ◽  
New Drugs ◽  
Drug Treatments ◽  
Review Current

BackgroundAlzheimer's disease management involves symptomatic drug treatments passed by the National Institute for Clinical Excellence. Disease modification is now the goal.AimsTo review current and developmental drugs for Alzheimer's disease, their usage, and the clinical context of known facts and proposed specific models.MethodA brief evidence-based review was made, using literature where available, or evidence from consensus groups where it was absent.ResultsThere is good evidence to support the use of cholinesterase inhibitors, and perhaps vitamin E. Oestrogen and anti-inflammatory agents show possibility, but there is not enough evidence to support routine use.ConclusionsSymptomatic treatments exist for Alzheimer's disease. Observational studies and increasing knowledge of brain biology are leading towards further treatment options. Old age psychiatrists have valuable treatments they now have to learn to use.

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 Non-Alkaloid Cholinesterase Inhibitory Compounds from Natural Sources

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5582
Author(s):  
Alfred Ngenge Tamfu ◽  
Selcuk Kucukaydin ◽  
Balakyz Yeskaliyeva ◽  
Mehmet Ozturk ◽  
Rodica Mihaela Dinica
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
High Efficiency ◽  
Neurodegenerative Disorder ◽  
Therapeutic Potential ◽  
New Drugs ◽  
Cholinesterase Inhibition ◽  
Natural Sources ◽  
Long Term Treatment

Alzheimer’s disease (AD) is a severe neurodegenerative disorder of different brain regions accompanied by distresses and affecting more than 25 million people in the world. This progressive brain deterioration affects the central nervous system and has negative impacts on a patient’s daily activities such as memory impairment. The most important challenge concerning AD is the development of new drugs for long-term treatment or prevention, with lesser side effects and greater efficiency as cholinesterases inhibitors and the ability to remove amyloid-beta(Aβ) deposits and other related AD neuropathologies. Natural sources provide promising alternatives to synthetic cholinesterase inhibitors and many have been reported for alkaloids while neglecting other classes with potential cholinesterase inhibition. This review summarizes information about the therapeutic potential of small natural molecules from medicinal herbs, belonging to terpenoids, coumarins, and phenolic compounds, and others, which have gained special attention due to their specific modes of action and their advantages of low toxicity and high efficiency in the treatment of AD. Some show superior drug-like features in comparison to synthetic cholinesterase inhibitors. We expect that the listed phytoconstituents in this review will serve as promising tools and chemical scaffolds for the discovery of new potent therapeutic leads for the amelioration and treatment of Alzheimer’s disease.

Evaluation of rivastigmine in Alzheimer's disease

2021 ◽  
Vol 11 (1) ◽  
pp. 35-48
Author(s):  
Kevin Nguyen ◽  
Heidi Hoffman ◽  
Binu Chakkamparambil ◽  
George T Grossberg
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Observational Studies ◽  
Cholinesterase Inhibitors ◽  
Randomized Clinical Trials ◽  
Mortality And Morbidity ◽  
Post Marketing ◽  
Dual Inhibition ◽  
The Brain ◽  
Oral Capsule

Dementia is the major cause of mortality and morbidity in older adults, with Alzheimer's disease (AD) being the most common cause. AD has a significant impact on economic and psychosocial status. Cholinesterase inhibitors (ChEIs) are currently the mainstay in the management of AD. Rivastigmine is the only ChEI that inhibits both acetylcholinesterase and butyrylcholinesterase enzymes in the brain. This dual inhibition makes it potentially more effective for AD patients. Its availability as both a transdermal formulation and oral capsule, may improve adherence rates and care giver satisfaction compared with other ChEIs. To date, the data from randomized clinical trials and post marketing observational studies have shown evidence for an impact on cognitive functions in AD with good safety and tolerability.

scholarly journals Neuroprotective Strategies Using Vegetal Compounds in the Treatment of Alzheimer’s Disease

2015 ◽  
Vol 45 ◽  
pp. 56-62
Author(s):  
Loredana Sandu ◽  
Alin Ciobica ◽  
Radu Lefter ◽  
Daniel Timofte ◽  
Emil Anton
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Research Effort ◽  
Treatment Options ◽  
Therapeutic Strategies ◽  
New Drugs ◽  
Simultaneous Application ◽  
Starting Point ◽  
Neuroprotective Strategies ◽  
Therapy Strategies

Lately, different therapy strategies for treating or slowing the progression of Alzheimer's disease are being analyzed. Moreover, the last two decades have seen a considerable research effort directed towards discovering the causes of Alzheimer's disease with the ultimate hope of developing safe and effective pharmacological treatments. In addition to the therapeutic strategies based on targeted drugs, the regimens will require the simultaneous application of neuroprotective drugs. Therefore, although there is currently no "cure" for Alzheimer's disease, a large number of potential therapeutic strategies emerged lately. In this small mini-review we will selectively describe some of the compounds derived from plants that could have a great potential in the treatment of various diseases, including Alzheimer's disease. In this way, there are many plant species that have been traditionally used for memory disorders. The differentiated results and powerful activity of these extracts are making these neuroprotective strategies to be somehow plausible for the treatment of Alzheimer's disease. In addition, these plants can be examined in order to isolate and identify their active ingredients and this can serve as a starting point to find safer and more effective agents for therapeutic use. On thing is certain: as the effective treatment options are limited, there is a demand for new drugs. Thus, plant extracts or vegetal compounds could represent an important part in this equation.

Natural Anti-inflammatory compounds as Drug candidates in Alzheimer’s disease

2020 ◽  
Vol 27 ◽  
Author(s):  
Reyaz Hassan Mir ◽  
Abdul Jalil Shah ◽  
Roohi Mohi-ud-din ◽  
Faheem Hyder Potoo ◽  
Mohd. Akbar Dar ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Natural Products ◽  
Protective Action ◽  
New Drugs ◽  
Huperzine A ◽  
Brain Disorder ◽  
Anti Inflammatory

: Alzheimer's disease (AD) is a chronic neurodegenerative brain disorder characterized by memory impairment, dementia, oxidative stress in elderly people. Currently, only a few drugs are available in the market with various adverse effects. So to develop new drugs with protective action against the disease, research is turning to the identification of plant products as a remedy. Natural compounds with anti-inflammatory activity could be good candidates for developing effective therapeutic strategies. Phytochemicals including Curcumin, Resveratrol, Quercetin, Huperzine-A, Rosmarinic acid, genistein, obovatol, and Oxyresvertarol were reported molecules for the treatment of AD. Several alkaloids such as galantamine, oridonin, glaucocalyxin B, tetrandrine, berberine, anatabine have been shown anti-inflammatory effects in AD models in vitro as well as in-vivo. In conclusion, natural products from plants represent interesting candidates for the treatment of AD. This review highlights the potential of specific compounds from natural products along with their synthetic derivatives to counteract AD in the CNS.

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.

[18F]-florbetaben PET/CT Imaging in the Alzheimer’s Disease Mouse Model APPswe/PS1dE9

2018 ◽  
Vol 16 (1) ◽  
pp. 49-55 ◽  
Author(s):  
J. Stenzel ◽  
C. Rühlmann ◽  
T. Lindner ◽  
S. Polei ◽  
S. Teipel ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Mouse Model ◽  
New Drugs ◽  
Imaging Data ◽  
Wild Type ◽  
Preclinical Research ◽  
Standardized Uptake Values ◽  
Pet Ct

Background: Positron-emission-tomography (PET) using 18F labeled florbetaben allows noninvasive in vivo-assessment of amyloid-beta (Aβ), a pathological hallmark of Alzheimer’s disease (AD). In preclinical research, [<sup>18</sup>F]-florbetaben-PET has already been used to test the amyloid-lowering potential of new drugs, both in humans and in transgenic models of cerebral amyloidosis. The aim of this study was to characterize the spatial pattern of cerebral uptake of [<sup>18</sup>F]-florbetaben in the APPswe/ PS1dE9 mouse model of AD in comparison to histologically determined number and size of cerebral Aβ plaques. Methods: Both, APPswe/PS1dE9 and wild type mice at an age of 12 months were investigated by smallanimal PET/CT after intravenous injection of [<sup>18</sup>F]-florbetaben. High-resolution magnetic resonance imaging data were used for quantification of the PET data by volume of interest analysis. The standardized uptake values (SUVs) of [<sup>18</sup>F]-florbetaben in vivo as well as post mortem cerebral Aβ plaque load in cortex, hippocampus and cerebellum were analyzed. Results: Visual inspection and SUVs revealed an increased cerebral uptake of [<sup>18</sup>F]-florbetaben in APPswe/ PS1dE9 mice compared with wild type mice especially in the cortex, the hippocampus and the cerebellum. However, SUV ratios (SUVRs) relative to cerebellum revealed only significant differences in the hippocampus between the APPswe/PS1dE9 and wild type mice but not in cortex; this differential effect may reflect the lower plaque area in the cortex than in the hippocampus as found in the histological analysis. Conclusion: The findings suggest that histopathological characteristics of Aβ plaque size and spatial distribution can be depicted in vivo using [<sup>18</sup>F]-florbetaben in the APPswe/PS1dE9 mouse model.

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