- |||||||||| galantamine hydrobromide / Generic mfg., rivastigmine / Generic mfg.
Isatin-linked heterocycles for inhibition of acetylcholinesterase and butyrylcholinesterase | Poster Board #2769 (Hall F2 (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_12928;
This series of molecules shows selective inhibition of butyrylcholinesterase (BChE) with low micromolar IC50 values. Subsequent studies are exploring the SAR and mode of interaction of these selective compounds with BChE, and additional synthetic and enzymatic inhibition results of these ongoing studies will be presented.
- |||||||||| risperidone / Generic mfg., galantamine hydrobromide / Generic mfg.
Journal: Neuropsychiatric Symptoms in Dementia: Considering a Clinical Role for Electroencephalography. (Pubmed Central) - Aug 7, 2022
No other consistent and significant relationships were observed between NPSD and EEG at baseline, after NPSD treatment, or in the change in EEG from baseline to follow-up. The limited informative findings in this study suggest that there exists a complex relationship between NPSD and EEG; hence, it is difficult to evaluate and use EEG for clinical assessment of pharmacological NPSD treatment.
- |||||||||| galantamine hydrobromide / Generic mfg.
Treatment With Galantamine in 15q13.3 Deletions: Genomically-Informed Precision Medicine Strategies in Neurodevelopmental Disorders. (Spadolini Pavilion Main Floor) - Jul 31, 2022 - Abstract #WCPG2022WCPG_248;
In all cases, behavioral outbursts diminished as reported by clinicians or family members, allowing in some cases for a reduction in the frequency of hospitalizations, and/or in the dose or number of medications prescribed, including the antipsychotics that are often used to treat irritability in ASD and which also confer increased risk for metabolic side effects. This case series serves as preliminary support for future clinical trials focusing on galantamine as a feasible pharmacological strategy with an indication for targeting aggression and irritability in people with 15q13.3 deletion, continuing to pave the way for genomically-informed precision medicine interventions in neurodevelopmental disorders.
- |||||||||| Cerebrolysin (porcine brain-derived proteolytic peptide fraction) / Novartis, EVER Pharma
Review, Journal: Pharmacotherapy of Alzheimer's disease: an overview of systematic reviews. (Pubmed Central) - Jul 27, 2022
The use of ChEIs, including rivastigmine, galantamine, and donepezil, as well as memantine has demonstrated a positive impact on improving cognitive outcomes of AD patients, but no considerable effects were found for immunotherapies. Melatonin, statins, antihypertensive drugs, antidiabetic agents, Cerebrolysin, psychostimulants, and some herbal drugs such as Danggui-Shaoyao-San and Ginkgo biloba seem to be effective in improving cognitive function of AD patients, but the evidence in this regard is limited.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: New 1,2,3-Triazole-genipin Analogues and Their Anti-Alzheimer's Activity. (Pubmed Central) - Jul 27, 2022
The molecular docking studies of these genipin analogues showed good binding energy and interact well with the key amino acids of BuChE via hydrogen-bonding and hydrophobic interactions. Triazole genipins might be promising lead compounds as anti-Alzheimer's agents.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Journal: A single-molecule with multiple investigations: Synthesis, characterization, computational methods, inhibitory activity against Alzheimer's disease, toxicity, and ADME studies. (Pubmed Central) - Jun 25, 2022
The calculated docking score of the title compound is not better than the AChE inhibitors known as galantamine and donepezil (positive control group). The binding energies of the complexes, title compound-AChE, donepezil-AChE, and galantamine-AChE, were calculated to be -7.80, -10.41, and -8.16 kcal/mol, respectively.
- |||||||||| Aduhelm (aducanumab) / Eisai, Biogen
Review, Journal: Therapeutic Approach to Alzheimer's Disease: Current Treatments and New Perspectives. (Pubmed Central) - Jun 25, 2022
In the therapeutic approach to AD, we can identify three important fronts: the approved drugs currently available for the treatment of the disease, which include aducanumab, donepezil, galantamine, rivastigmine, memantine, and a combination of memantine and donepezil; therapies under investigation that work mainly on Aβ pathology and tau pathology, and which include γ-secretase inhibitors, β-secretase inhibitors, α-secretase modulators, aggregation inhibitors, metal interfering drugs, drugs that enhance Aβ clearance, inhibitors of tau protein hyperphosphorylation, tau protein aggregation inhibitors, and drugs that promote the clearance of tau, and finally, other alternative therapies designed to improve lifestyle, thus contributing to the prevention of the disease. Therefore, the aim of this review was to analyze and describe current treatments and possible future alternatives in the therapeutic approach to AD.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Journal: In Silico Design of Dual-Binding Site Anti-Cholinesterase Phytochemical Heterodimers as Treatment Options for Alzheimer's Disease. (Pubmed Central) - Jun 22, 2022
In silico molecular docking of heterodimers with the target enzymes, AChE and butyrylcholinesterase (BuChE), were performed, and anti-cholinesterase binding affinities were compared with donepezil...Computational pharmacokinetic and pharmacodynamic screening suggested that phytochemical heterodimers would display useful gastrointestinal absorption and with relatively low predicted toxicity. Collectively, the present study suggests that phytochemicals could be garnered for the provision of novel ChEIs with enhanced drug efficacy and low toxicity.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., fluoxetine / Generic mfg.
Journal: Unraveling the Binding Mechanism of Alzheimer's Drugs with Irisin: Spectroscopic, Calorimetric, and Computational Approaches. (Pubmed Central) - Jun 19, 2022
Molecular docking further validated the fluorescence and ITC results and unfolded the mechanism that hydrogen bonding governs the binding of fluoxetine to irisin with a significant binding score, i.e., -6.3 kcal/mol. We believe that these findings provide a promising solution to fight against AD as well as a platform for further research to utilize irisin in the drug-delivery system for an effective therapeutic strategy.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Inhibitory Effects of Cannabinoids on Acetylcholinesterase and Butyrylcholinesterase Enzyme Activities. (Pubmed Central) - Jun 18, 2022
The inhibitory effects of these cannabinoids (with IC values ranging from 85.2 to >200 µM for AChE and 107.1 to >200 µM for BChE) were less potent as compared to the positive control galantamine (IC 1.21 and 6.86 µM for AChE and BChE, respectively)...Cannabinoids showed moderate inhibitory effects on the activities of AChE and BChE enzymes, which may contribute to their modulatory effects on the cholinergic system. Further studies using cell-based and in vivo models are warranted to evaluate whether cannabinoids' neuroprotective effects are associated with their anti-cholinesterase activities.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Retrospective data, Journal: Targeting the Beta-2-Adrenergic Receptor and the Risk of Developing Alzheimer's Disease: A Retrospective Inception Cohort Study. (Pubmed Central) - Jun 9, 2022
Conclusions are limited by paucity of research; but fortunately, a large randomized controlled trial is ongoing, and more are needed to truly determine the efficacy of AChEIs in helping with recovery from TBI. These findings suggest that exposure to non-selective βAR antagonists is associated with an increased risk for developing AD whereas there may be a decreased risk for developing AD after exposure to selective β2AR agonists.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Enhanced parasympathetic cholinergic activity with galantamine inhibited lipid-induced oxidative stress in obese African Americans. (Pubmed Central) - Jun 8, 2022
P1/2
These findings suggest that exposure to non-selective βAR antagonists is associated with an increased risk for developing AD whereas there may be a decreased risk for developing AD after exposure to selective β2AR agonists. In this pilot, proof-of-concept study, enhancing parasympathetic nervous system (PNS) cholinergic activity with galantamine inhibited lipid-induced oxidative stress and inflammation induced by lipid infusion in obese AAs.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Journal: A comprehensive computational perspective in drug discovery for Alzheimer's disease. (Pubmed Central) - Jun 8, 2022
This chapter considers a wide range targets for Alzheimer's disease and current advances in the discovery of disease inhibitors. And also brief in-silico studies were highlighted and included to know how the theoretical lead is achievable in AD medication discovery.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Virtual Screening and Hit Selection of Natural Compounds as Acetylcholinesterase Inhibitors. (Pubmed Central) - Jun 5, 2022
The achieved success of plant-based natural drugs acting as AChE inhibitors, such as galantamine (GAL) from Galanthus genus and huperzine A from Huperzia serrate (approved drug in China), in the treatment of AD, and the fact that natural compounds (NCs) are considered as safer and less toxic compared to synthetic drugs, led us to screen the available NCs (almost 150,000) in the ZINC12 database for AChE inhibitory activity...They were tested for AChE inhibitory and antioxidant activity. Five compounds showed weak AChE inhibition and three of them exhibited high antioxidant activity.
- |||||||||| Cognex (tacrine) / Shionogi
Review, Journal: Determination of Anti-Alzheimer's Disease Activity of Selected Plant Ingredients. (Pubmed Central) - Jun 5, 2022
This study also aims to highlight species with assessed efficacy, usable plant parts and the most active plant components in order to identify species and compounds of interest for further study. Future research directions are suggested and recommendations made to expand the use of medicinal plants, their formulations and plant-derived active compounds to prevent, mitigate and treat Alzheimer's disease.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Biomarker, Review, Journal: Pharmacogenetic studies in Alzheimer disease. (Pubmed Central) - May 29, 2022
Potential pharmacogenetic biomarkers for AD have been identified; however, it is still necessary to conduct further research into other populations and to identify new biomarkers. This information could assist in predicting patient response to these drugs and contribute to better treatment decision-making in a context as complex as ageing.
- |||||||||| galantamine hydrobromide / Generic mfg.
Clinical, Journal: Acute response to cholinergic challenge predicts long-term response to galantamine treatment in patients with Alzheimer's Disease. (Pubmed Central) - May 19, 2022
Thus, the mechanisms by which ChEI can promote neuroprotective effects and prospects for the development of new drug candidates for the treatment of AD are discussed in this review. This study demonstrates that acute PD effects after single dose of galantamine are correlated with long-term treatment effects and that patients who demonstrate a reduction in EEG power in the alpha and theta frequency after a single administration of galantamine 16 mg will most likely respond to treatment.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Central Activation of the Cholinergic Anti-Inflammatory Pathway Improves Outcome in a Murine Model of Systemic Lupus Erythematosus. (Pubmed Central) - May 14, 2022
Previous studies from our group demonstrated that the pharmacological potentiation of the efferent vagus nerve via systemic administration of galantamine reduces renal inflammation and blood pressure in systemic lupus erythematosus (SLE), suggesting an impairment in the cholinergic anti-inflammatory pathway in this model...In addition, selective activation of DMV neurons decreased urinary leukocytes (62.5% vs 50%) and blood in the urine (50% vs 16%) in SLE mice. The present study showed that boosting the cholinergic anti-inflammatory pathway via selective activation of vagal efferents lowered splenic inflammation and protected the kidney without altering blood pressure suggesting an important role of the cholinergic anti-inflammatory pathway in regulating inflammation and renal injury in SLE.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Amelioration of Cardiac Autonomic Dysfunction Mitigates Perivascular and Perirenal Adipose Inflammation and Cardiorenal Involvement in Prediabetes. (Pubmed Central) - May 14, 2022
The present study showed that boosting the cholinergic anti-inflammatory pathway via selective activation of vagal efferents lowered splenic inflammation and protected the kidney without altering blood pressure suggesting an important role of the cholinergic anti-inflammatory pathway in regulating inflammation and renal injury in SLE. Pharmacological interventions to reverse sympathetic predominance could be of therapeutic value treating perivascular and perirenal adipose inflammation that cause early cardiorenal manifestations of prediabetes.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Journal: Structural Fractal Analysis of the Active Site of Acetylcholinesterase in Complexes with Huperzine A, Galantamine, and Donepezil. (Pubmed Central) - May 6, 2022
When analyzing FMSCs, we found that the most significant structural changes are related to the Glu202 amino acid residue. No structural perturbations are revealed in the case of Trp86, Gly122, Ala204, Phe338, Tyr341, Gly448, and Ile451.
- |||||||||| Cognex (tacrine) / Shionogi
Journal: Acetylcholinesterase Enzyme Inhibitor Molecules with Therapeutic Potential for Alzheimer's Disease. (Pubmed Central) - May 6, 2022
This review comprises the many hybrids and non-hybrid forms of heteroaromatic and non-heteroaromatic compounds that were designed and evaluated for AchE inhibition by Ellman's method of assay. These novel compounds may assist the future perspectives in the discovery of novel moieties against Alzheimer's disease by the inhibition of AchE.
- |||||||||| Myrbetriq (mirabegron) / Astellas
Journal: Risk of overactive bladder associated with cholinesterase inhibitors in dementia. (Pubmed Central) - May 6, 2022
The study found that the risk of OAB varies across individual ChEIs with an increased risk of OAB with donepezil compared to rivastigmine. The study findings suggest the need to understand and manage medication-related morbidity in older adults with dementia.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Observational data, Journal: Analysis of treatment pattern of anti-dementia medications in newly diagnosed Alzheimer's dementia using OMOP CDM. (Pubmed Central) - May 6, 2022
A 12-month persistence analysis showed values of approximately 50% for donepezil and memantine and approximately 40% for rivastigmine and galantamine. There were differences in the prescribing pattern and persistence among anti-dementia medications from database using the Observational Medical Outcome Partnership Common Data Model on the Federated E-health Big Data for Evidence Renovation Network platform in Korea.
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