- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Clinical, Review, Journal: Efficacy of acetylcholinesterase inhibitors in Alzheimer's disease. (Pubmed Central) - Jan 12, 2022 Other approaches in which ChE-Is were investigated is in their use in combination with other classes of drugs such as cholinergic precursors, N-methyl-d-aspartate (NMDA) receptor antagonists and antioxidant agents. After many years from the introduction in therapy of ChE-Is, the combination with other classes of drugs may represent the chance for a renewed interest of ChE-Is in the treatment of adult-onset dementia disorders.
- |||||||||| rivastigmine / Generic mfg.
Preclinical, Journal: Synthesis, characterization and pharmacological evaluation of quinoline derivatives and their complexes with copper(ΙΙ) in in vitro cell models of Alzheimer's disease. (Pubmed Central) - Jan 11, 2022 Molecular docking simulations, using the crystal structure of the acetylcholinesterase (AChE)-rivastigmine complex as a template, indicated a strong interaction of the metal chelator Hdqpyca, followed by Hbqch, with both the peripheral anionic site and the catalytic active site of AChE. In conclusion, the sufficient neuroprotection provided by the metal chelator Hdqpyca and the copper(II) complex [Cu(Hbqch)Cl]3HO along with the evidence for interaction between Hdqpyca and AChE, indicate that these compounds have the potential and should be further investigated in the framework of preclinical studies employing animal models of AD as candidate multifunctional lead compounds for the treatment of the disease.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Review, Journal: Multitarget Directed Ligand Approaches for Alzheimer's Disease: A Complete Review. (Pubmed Central) - Dec 22, 2021 Using cholinesterase inhibitor therapy may benefit AD patients through attenuation of oxidative stress and manipulation of the mtCN. The review might be helpful for researchers working on multi target directed ligands against AD.
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7,8-dihydroxyflavone attenuates cognitive deficit in icv-stz rat model of alzheimer's disease reversing oxidative stress, mitochondrial dysfunction, and insulin resistance (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_2143; Conclusively, 7,8-DHF was found to be neuroprotective in the ICV-STZ rat model of SAD by ameliorating oxidative stress, mitochondrial dysfunction, and insulin resistance, thereby improving cognitive functions evident with the behavioral results. Hence, these results can further have clinical relevance in human AD.
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Journal, Adverse events: The Association Between Use of Rivastigmine and Pneumonia: Systematic Analysis of FDA Adverse Event Reporting System. (Pubmed Central) - Dec 16, 2021 The observed elevated frequency of aspiration pneumonia in patients prescribed rivastigmine may be due to an induced cholinergic crisis that is selective for the medulla oblongata, resulting in gastrointestinal distress, impaired swallowing, heightened salivation, and labored breathing. The observed elevated frequency of infectious pneumonia in patients prescribed rivastigmine may also be linked to overstimulation of neurons in the medulla oblongata and downstream suppression of localized inflammatory responses.
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Trial completion date, Trial initiation date, Trial primary completion date: Telerehabilitation Alzheimer's Disease Feasibility (TADF) (clinicaltrials.gov) - Dec 10, 2021 P=N/A, N=14, Not yet recruiting, The observed elevated frequency of infectious pneumonia in patients prescribed rivastigmine may also be linked to overstimulation of neurons in the medulla oblongata and downstream suppression of localized inflammatory responses. Trial completion date: Feb 2022 --> Dec 2022 | Initiation date: Sep 2021 --> Dec 2021 | Trial primary completion date: Dec 2021 --> Dec 2022
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Preclinical, Journal: Current Quest in Natural Bioactive Compounds for Alzheimer's Disease: Multi-Targeted-Designed-Ligand Based Approach with Preclinical and Clinical Based Evidence. (Pubmed Central) - Nov 29, 2021 Computational studies (molecular docking) have been used to predict the binding affinity of these natural bioactive as well as synthetic compounds derived from natural sources for the acetylcholine esterase, α/β secretase Nuclear Factor kappa-light-chain-enhancer of activated B cells(NF-kB),Nuclear factor erythroid 2-related factor 2(Nrf2) and other neurological targets. Thus, in this review, we have discussed molecular etiology of AD, focused on the pharmacotherapeutics of natural product, chemical and pharmacological aspects and multi-targeted designed ligands (MTDLs) of synthetic and semisynthetic molecules derived from the natural sources along with some important on-going clinical trials.
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Biomarker, Clinical, Journal: Pharmacogenetic and Association Studies on the Influence of HLA Alleles and Rivastigmine on the Iranian Patients with Late-Onset Alzheimer's Disease. (Pubmed Central) - Nov 29, 2021 The PcPPV of testing for DQB1*06:00/x in the Iranian LOAD patients was 1.17% which means that people carrying this genotype have half of the probability of the absolute risk for developing LOAD, whereas the PcPPV of testing for B*07:00/x was 4.45% for SAD, which can be interpreted as a doubling chance for developing LOAD among the Iranian population carrying this genotype. These results also suggest that DQβ1 peptide containing positively charged AAs histidine and arginine and HLA class I β chain containing negatively charges aspartic acid and glutamic acid in their binding groove plays important roles in protection against and susceptibility for LOAD respectively.
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Clinical, Review, Journal: Current Treatment Options for REM Sleep Behaviour Disorder. (Pubmed Central) - Nov 29, 2021 The development of potential preventive therapies against the phenoconversion of isolated RBD to synucleinopathies should be another important aim of RBD therapy. The design of long-term, multicentre, randomized, placebo-controlled clinical trials involving a large number of patients diagnosed with isolated RBD with polysomnographic confirmation, directed towards both symptomatic and preventive therapy for RBD, is warranted.
- |||||||||| rivastigmine / Generic mfg.
Journal: Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies. (Pubmed Central) - Nov 17, 2021 Finally, the intranasal ciliotoxicity study on sheep nasal mucosa revealed that the exposure of developed nanoparticles was similar to the negative control group, while destruction of normal architecture was noticed in the positive control test group. Overall, from the in vitro results it could be summarized that the optimization of nanoparticles' formulation of rivastigmine for intranasal application would be retained at the application site for a prolonged duration to release the entrapped drug without producing any local toxicity at the mucosal region.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Journal: Current Strategies and Novel Drug Approaches for Alzheimer Disease. (Pubmed Central) - Nov 17, 2021 Phytopharmaceuticals and nutraceuticals are also gaining attention in overcoming the symptoms related to AD. The present review article concludes that novel and traditional therapies simultaneously promise future hope for AD treatment.
- |||||||||| donepezil one-month depot (GB-5001) / G2GBIO
Journal: Donepezil Regulates LPS and Aβ-Stimulated Neuroinflammation through MAPK/NLRP3 Inflammasome/STAT3 Signaling. (Pubmed Central) - Nov 10, 2021 In a mouse model of AD (5xFAD mice), donepezil significantly reduced Aβ-induced microglial and astrocytic activation, density, and morphology. Taken together, our findings indicate that donepezil significantly downregulates LPS- and Aβ-evoked neuroinflammatory responses in vitro and in vivo and may be a therapeutic agent for neuroinflammation-associated diseases such as AD.
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Journal: Therapeutic Potential Of Multifunctional Derivatives Of Cholinesterase Inhibitors. (Pubmed Central) - Nov 7, 2021 In this account we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant, decreasing β-amyloid plaque aggregation, nitric oxide production, pro-inflammatory cytokines release, monoamine oxidase-B activity, cytotoxicity and oxidative stress in vitro and in animal model that classify these hybrids as potential multifunctional therapeutic agents for Alzheimer's disease. Moreover, herein, we have described the cholinergic hypothesis, mechanisms of neurodegeneration and current pharmacotherapy of Alzheimer's disease which is based on the restoration of cholinergic function through blocking enzymes that break down acetylcholine.
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Journal: Multiple gastric ulcers due to rivastigmine. (Pubmed Central) - Nov 5, 2021 If cost-effective, it will alter current management guidelines by offering a new therapeutic option in this high-risk population. No abstract available
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PK/PD data, Preclinical, Journal: Dermal Pharmacokinetics of rivastigmine-loaded liposomes: an Ex vivo- in vivo correlation study. (Pubmed Central) - Oct 30, 2021 A point-to-point significant linear correlation was found between ex vivo- in vivo parameters, meaning in vivo pharmacokinetic parameters can be predicted by Ex vivo permeation parameters. These data suggest that a liposomal formulation could be an effective carrier to enhance rivastigmine permeation through the skin and maintain plasma levels within the therapeutic window.
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