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Cholinergic neurotransmission, REM sleep and depression.

It is known from animal experiments that the regulation of REM and Non-REM sleep is governed by cholinergic and serotonergic/adrenergic neurons in the brain stem. Cholinergic neurons in the gigantocellular field of the tegmentum seem to be responsible for the triggering and maintenance of REM sleep. These findings are of special interest for interpreting abnormalities of REM sleep in depression. Psychiatric sleep research in the last two decades has demonstrated that an early onset of REM sleep and heightened REM density frequently occurs in patients suffering from depression. Extrapolating fr

Symptomatic and nonamyloid/tau based pharmacologic treatment for Alzheimer disease.

In this work we consider marketed drugs for Alzheimer disease (AD) including acetylcholinesterase inhibitors (AChE-Is) and antiglutamatergic treatment involving the N-methyl-d-aspartate (NMDA) receptor. We discuss medications and substances available for use as cognitive enhancers that are not approved for AD or cognitive impairment, and other neurotransmitter-related therapies in development or currently being researched. We also review putative therapies that aim to slow disease progression by mechanisms not directly related to amyloid or tau.

[Current therapy of patients with dementia].

In recent years, the efficacy of symptomatic treatment in patients with Alzheimer's disease has repeatedly been demonstrated in a number of multicenter studies. Such treatment aims both to improve the patient's cognitive abilities and to preserve his or her quality of life and ability to cope with the activities of daily life. In this way the burden on relatives and caregivers is reduced, and the need for home or institutionalized care delayed. Causally effective therapeutic strategies resulting in a cure or the delaying of pathophysiological progression are currently not available, but are be

Recent Advances in Therapeutics for the Treatment of Alzheimer's Disease.

The most prevalent chronic neurodegenerative illness in the world is Alzheimer's disease (AD). It results in mental symptoms including behavioral abnormalities and cognitive impairment, which have a substantial financial and psychological impact on the relatives of the patients. The review discusses various pathophysiological mechanisms contributing to AD, including amyloid beta, tau protein, inflammation, and other factors, while emphasizing the need for effective disease-modifying therapeutics that alter disease progression rather than merely alleviating symptoms. This review mainly covers m

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… Donepezil, galantamine, and rivastigmine are the cholinesterase inhibitors that are most frequently prescribed [ 102 , 103 , 104 , 105 , 106 ]. … Galantamine: A Review Update J. Drug Deliv. Ther. 2022 12 167 173 113. Santos G.S. Sinoti S.B.P. De Almeida F.T.C. Silveira D. Simeoni L.A. Gomes-Copeland K.K.P. …

Cholinergic medication for antipsychotic-induced tardive dyskinesia.

BACKGROUND: Tardive dyskinesia (TD) remains a troublesome adverse effect of conventional antipsychotic (neuroleptic) medication. It has been proposed that TD could have a component of central cholinergic deficiency. Cholinergic drugs have been used to treat TD. OBJECTIVES: To determine the effects of cholinergic drugs (arecoline, choline, deanol, lecithin, meclofenoxate, physostigmine, RS 86, tacrine, metoxytacrine, galantamine, ipidacrine, donepezil, rivastigmine, eptastigmine, metrifonate, xanomeline, cevimeline) for treating antipsychotic-induced TD in people with schizophrenia or other ch…

Marine Natural Products, Multitarget Therapy and Repurposed Agents in Alzheimer's Disease.

Alzheimer's disease (AD) is a multifactorial disease characterized by the presence of amyloid plaques, neurofibrillary tangles, and nerve cell death that affects, mainly, older people. After decades of investigation, the search for an efficacious treatment for AD remains and several strategies can be and are being employed in this journey. In this review, four of the most promising strategies, alongside with its most promising agents under investigation or development are highlighted. Marine natural products (MNP) are a source of unique chemical structures with useful biological activities for

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… Donepezil, when compared to rivastigmine and galantamine, presents less adverse gastrointestinal adverse effects [ 13 ]. … In current treatment for AD, an example of a repurposed drug is galantamine ( Figure 3 ). Galantamine is an alkaloid present in Galanthus sp. with a complex chemical structure possessing three chiral centers. …

The Movement Disorder Society Evidence-Based Medicine Review Update: Treatments for the non-motor symptoms of Parkinson's disease.

The Movement Disorder Society (MDS) Task Force on Evidence-Based Medicine (EBM) Review of Treatments for Parkinson's Disease (PD) was first … nil for the treatment of fatigue; amantadine for the treatment of pathological gambling; donepezil, galantamine, and memantine for the treatment of dementia; quetiapine for the treatment of psychosis; fludrocortisone and domperidone for the treatment of orthostatic hypotension; sildenafil for the treatment of erectile dysfunction, ipratropium bromide spray fo …

Mechanisms to medicines: navigating drug repurposing strategies in Alzheimer's disease.

Alzheimer's disease (AD) represents a continuously advancing neurodegenerative condition distinguished by the unremitting deterioration of cognitive abilities and memory impairment, which significantly hampers daily functioning of life. In the absence of disease modifying treatments, it continues to pose a significant global challenge. Though symptomatic treatment exists, the inherent complexity involved with AD pathogenesis related to Aβ plaques, neurofibrillary tangles, neuroinflammation, oxidative stress, etc. poses a tremendous challenge to developing drugs. With the incidence of AD increa

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… Key drugs include Donepezil, Galantamine, Rivastigmine, and Aducanumab. Alternative approaches (e.g., Vitamin E, Melatonin) and new approaches (e.g., Anti-inflammatory treatments) are highlighted. … Galantamine is indicated for the treatment of the same but not for PD. The drug has been demonstrated to improve cognitive functions and overall quality of life. …

Comparison of the Utility of Amplitude-Spectral and Coherence Features of Psychotropic Drugs' Action on ECoG Signal for Pharmaco-EEG Based Drug Screening in Rats.

A naive Bayesian classifier (NBC) combined with principal component analysis (PCA) effectively differentiates the dose-dependent effects of … linergic tropicamide, the H1/5HT2A receptor blocker hydroxyzine, the acetylcholinesterase inhibitor galantamine, the alpha-2 adrenergic agonist dexmedetomidine, the alpha-2 adrenergic antagonist atipamezole, the adenosine receptor blocker caffeine and the GABA-mimetics aminophenylbutyric acid (phenibut), bromdihydrochlorophenylbenzodiazepine (phenazepam) and …

Predictors of institutionalization of dementia patients in mild and moderate stages: a 4-year prospective analysis.

BackgroundInstitutionalization is the most important milestone in the care of dementia patients. This study was aimed at identifying relevant predictors of institutionalization in a broad empirical context and interpreting them on the basis of the predictor model proposed by Luppa et al. [Dement Geriatr Cogn Disord 2008;26:65-78].MethodsAt the start of this study, 357 patients with mild to moderate dementia were examined by their general practitioners, and a telephone interview was conducted with their caregivers. Four years later, the outcomes 'institutionalization' and 'death' were determine

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… A systematic review of randomized, placebo-controlled trials of donepezil, rivastigmine and galantamine Int Psychogeriatr 2009 21 813 824 19538824 10.1017/S1041610209990354 97 Takeda A Loveman E Clegg A Kirby J Picot J Payne E Green C A systematic review of the clinical effectiveness of donepezil, rivastigmine … and galantamine on cognition, quality of life and adverse events in Alzheimer's disease Int J Geriatr Psychiatry 2006 21 17 28 16323253 10.1002/gps.1402 98 Pinquart M Sörensen S Helping caregivers of persons with dementia: which interventions work and how large are their effects? …

Trazodone in the Management of Major Depression Among Elderly Patients with Dementia: A Narrative Review and Clinical Insights.

ObjectiveMajor depressive disorder (MDD) often co-occurs with dementia and other neurological disorders, and treatment with antidepressants can improve symptoms, quality of life, and survival in these patients. This narrative review provides an expert opinion about the role and effectiveness of trazodone in the treatment of older adults with MDD and cognitive impairment due to physical illnesses, such as dementia.ResultsBecause of its mechanism of action, trazodone can treat several depression symptoms often seen in people with dementia, including insomnia, agitation, anxiety, cognitive impair

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… The US Food and Drug Administration (FDA) has approved galantamine and rivastigmine for mild-to-moderate dementia, memantine for moderate-to-severe dementia, and donepezil for mild-to-severe dementia. … Considering that donepezil and galantamine are metabolized in the liver through CYP2D6 and CYP3A4, their hepatic metabolism may be affected by specific substrates, inhibitors, or enhancers of the same enzymes. 89 Trazodone is primarily metabolized to meta-chlorophenylpiperazine (mCPP) by the isoenzyme …

Role of Nanomedicine-Based Therapeutics in the Treatment of CNS Disorders.

Central nervous system disorders, especially neurodegenerative diseases, are a public health priority and demand a strong scientific response. Various therapy procedures have been used in the past, but their therapeutic value has been insufficient. The blood-brain barrier (BBB) and the blood-cerebrospinal fluid barrier is two of the barriers that protect the central nervous system (CNS), but are the main barriers to medicine delivery into the CNS for treating CNS disorders, such as brain tumors, Parkinson's disease, Alzheimer's disease, and Huntington's disease. Nanotechnology-based medicinal

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… Pharmaceutical treatments include donepezil, rivastigmine, galantamine, tacrine (acetylcholinesterase (Ache) inhibitors), and memantine (N-methyl-aspartate (NMDA) receptor antagonist) [ 69 ]. … Existing AD treatments include cholinesterase inhibitors like donepezil, rivastigmine, galantamine, and N-methyl-d-aspartate receptor antagonists (memantine) [ 100 ]. …

Mechanisms and effects of metformin on skeletal muscle disorders.

Skeletal muscle disorders are mostly genetic and include several rare diseases. With disease progression, muscle fibrosis and adiposis occur, resulting in limited mobility. The long course of these diseases combined with limited treatment options affect patients both psychologically and economically, hence the development of novel treatments for neuromuscular diseases is crucial to obtain a better quality of life. As a widely used hypoglycemic drug in clinical practice, metformin not only has anti-inflammatory, autophagy-regulating, and mitochondrial biogenesis-regulating effects, but it has a

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… Tezze et al. found that the combination of metformin and galantamine (RJx-01) can prolong the lifespan, exercise ability, and beneficial effects on muscle structure and function of C. elegans . … A combination of metformin and galantamine exhibits synergistic benefits in the treatment of sarcopenia. JCI Insight. (2023) 8:e168787. doi: 10.1172/jci.insight.168787 151. Romanello V. The interplay between mitochondrial morphology and Myomitokines in aging sarcopenia. …

Withdrawal or continuation of cholinesterase inhibitors or memantine or both, in people with dementia.

BACKGROUND: Dementia is a progressive syndrome characterised by deterioration in memory, thinking and behaviour, and by impaired ability to perform daily activities. Two classes of drug - cholinesterase inhibitors (donepezil, galantamine and rivastigmine) and memantine - are widely licensed for dementia due to Alzheimer's disease, and rivastigmine is also licensed for Parkinson's disease dementia. These drugs are prescribed to alleviate symptoms and delay disease progression in these and sometimes in other forms of dementia. There are uncertainties about the benefits and adverse effects of the…

Роль воспаления в нейродегенеративных болезнях: болезнь Паркинсона, болезнь Альцгеймера и множественный склероз.

Нейродегенеративные заболевания представляют собой группу заболеваний, которые, как правило, характеризуются постепенным повреждением и дегенерацией нейронов в центральной нервной системе. В эту группу входят болезнь Паркинсона, болезнь Альцгеймера и множественный склероз. В последние годы все больше фактов указывает на важную роль воспаления в патогенезе этих условий. Происхождение воспаления в мозге, которое часто вызывается провоспалительной активацией микроглий или астроцитов, может, следовательно, привести к хронической провокационной реакции, способствующей развитию нейродегенеративных п

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… Current symptomatic treatments include only two classes of approved medications for the treatment of Alzheimer’s disease; i /inhibitors of the enzyme cholinesterase, i.e., donepezil, rivastigmine, or galantamine, and ii /N-methyl-D-aspartate antagonists, i.e., memantine, which are only effective in …

Cholinesterase inhibitors for rarer dementias associated with neurological conditions.

BACKGROUND: Rarer dementias include Huntington's disease (HD), cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy (CADASIL), frontotemporal dementia (FTD), dementia in multiple sclerosis (MS) and progressive supranuclear palsy (PSP). Cholinesterase inhibitors, including donepezil, galantamine and rivastigmine, are considered to be the first-line medicines for Alzheimer's disease and some other dementias, such as dementia in Parkinson's disease. Cholinesterase inhibitors are hypothesised to work by inhibiting the enzyme acetylcholinesterase (AChE) which b…

NDP52 и его новая роль в патогенезе.

Автофагика - это процесс, способствующий выживанию, который регулирует деградацию и обновление клеточных компонентов, что делает его важнейшим механизмом для клеточного гомеостазиза. Существуют выборочные формы автофагии, характерные для ряда субстратов, таких, как патогены (бактерии или вирусы), белковые агрегаты или излишние/поврежденные органеллы. Эти процессы включают в себя в качестве ключевых игроков автофагичные рецепторы, которые связывают груз, подлежащий деградации, с автофагическим оборудованием. Среди них NDP52 (известный также как КАКПО2) был охарактеризован как «бридж» между авто

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… Such agents belong to two families: acetyl cholinesterase inhibitors (Donepezil, Galantamine, Rivastigmine), and anti-glutaminergics (Memantine). …

Окисляющий стресс в функции мозга.

Окисляющий стресс (OS) является важным фактором в патофизиологии многочисленных нейродегенеративных расстройств, таких, как болезнь Паркинсона, множественный склероз, цереброваскулярная патология или болезнь Альцгеймера. OS также оказывает значительное влияние на прогресс между различными нейродегенеративными расстройствами. Несбалансированность между образованием реактивных видов кислорода (РОС) и способностью организма нейтрализовать эти токсичные побочные продукты делает мозг подверженным окислительным повреждениям. Увеличение количества ROS может привести к сбоям в клетке, апоптозу и нейро

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… Cholinesterase inhibitors, including donepezil, rivastigmine and galantamine, are formulated to augment cholinergic neurotransmission by blocking the enzyme acetylcholinesterase, which is responsible for the degradation of acetylcholine in the synaptic cleft [ 103 ]. …

Persistent lactic acidosis in ALK-positive anaplastic large cell lymphoma: a case report and literature review.

Lactic acidosis is common in the ICU, but malignancy-associated type B lactic acidosis mediated by the clinical Warburg effect (CWE) is uncommon and easily missed when infection or organ dysfunction dominates the presentation. We report a 35-year-old man with a month of fever and progressive dyspnea who presented with persistent hyperlactatemia (peak 15.46 mmol/L) and markedly elevated LDH despite stable hemodynamics. Imaging revealed generalized lymphadenopathy, multifocal osteolytic lesions, and bilateral pleural effusions; infectious studies were unrevealing apart from chronic hepatitis B.

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… Treatment included mecobalamin (Beijing Sunho Pharmaceutical Co., Ltd.) for neuroprotection, ambroxol combined with galantamine (Hubei Meilin) to enhance neuromuscular transmission, and early passive joint mobilization exercises in collaboration with rehabilitation services. …

Alzheimer's Disease: Cellular and Pharmacological Aspects.

Alzheimer's disease was described more than 100 years ago and despite the fact that several molecules are being tested for its treatment, which are in phase III trials, the disease continues to progress. The main problem is that these molecules function properly in healthy neurons, while neuronal pathology includes plasma membrane disruption, malfunction of various organelles, and hyperphosphorylation of Tau and amyloid plaques. The main objective of this article is the discussion of a neuronal restoration therapy, where molecules designed for the treatment of Alzheimer's disease would probabl

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… Among the five FDA-approved drugs, donepezil, galantamine, rivastigmine, tacrine, and memantine, unfortunately none of them work, as patients at first seem to recover cognitive ability, but then that ability is lost over time [ 10 ]. …