- |||||||||| Comtan (entacapone) / Novartis, Orion Corp
Review, Journal: Mushroom Polysaccharides as Potential Candidates for Alleviating Neurodegenerative Diseases. (Pubmed Central) - Nov 27, 2022
Some have been demonstrated to exhibit neuroprotective effects via their antioxidant, anti-amyloidogenic, anti-neuroinflammatory, anticholinesterase, anti-apoptotic, and anti-neurotoxicity activities, which have potential in the treatment of NDs. This review focuses on the different processes involved in ND development and progression, highlighting the neuroprotective activities and potential role of mushroom polysaccharides and summarizing the limitations and future perspectives of mushroom polysaccharides in the prevention and treatment of NDs.
- |||||||||| galantamine hydrobromide / Generic mfg.
Review, Journal: A systematic review of new empirical data on lucid dream induction techniques. (Pubmed Central) - Nov 22, 2022
As hypothesised, the overall methodological quality of the studies included in the present review was higher than that of the studies included the previous review. In all, 17 studies had moderate methodological quality, whereas only three studies had poor methodological quality.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., rivastigmine / Generic mfg.
Journal, Real-world evidence: Real-world effects of anti-dementia treatment on mortality in patients with Alzheimer´s dementia. (Pubmed Central) - Nov 19, 2022
Patients were primarily exposed to donepezil (65.8%) with rivastigmine (19.8%) and galantamine (14.4%) being used less often. These findings underscore the effect of AChEI on not only reducing speed of cognitive decline but also directly prolonging life, which could result in changes in treatment recommendation for when to stop treatment.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Retrospective data, Review, Journal: The efficacy of pharmacological interventions to improve cognitive and behavior symptoms in people with dementia: A systematic review and meta-analysis. (Pubmed Central) - Nov 19, 2022
The study subjects who received donepezil 5 mg/day, donepezil 10 mg/day, and galantamine 24 mg/day had improved cognition symptoms (ADAS-cog) score of -1.46 (95% CI = -2.24, -0.68, z = 3.67, p < 0.001), -2.31 (95% CI = -3.30, -1.31, z = 5.45, p < 0.001) and -3.04 (95% CI = -4.16, -1.92, z = 5.31, p < 0.001) respectively. The current meta-analysis suggests significant benefits of cholinesterase inhibitors such as donepezil (5 and 10 mg/day) and galantamine on cognitive symptoms.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: New amides derived from sclareolide as anticholinesterase agents. (Pubmed Central) - Nov 16, 2022
Five amides (9, 13, 14, 15 and 17) caused inhibition of one of the enzymes greater than 60%; thereby those that inhibited BuChE were more active than positive control galantamine, and they showed better K values (1.07 to 8.49)...Of special note is compound 15, as it presented the second-best K value for BuChE (1.71), was not cytotoxic (EC > 30 μM). Compound 15 also does not violate Lipinski rules, and showed permeability in the blood brain barrier, indicating that it can be considered a lead for the development of new drugs to treat Alzheimer's disease.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Therapeutic effects of carvacrol on beta-amyloid-induced impairments in in-vitro and in-vivo models of Alzheimer's disease. (Pubmed Central) - Nov 16, 2022
SH-SY5Y cells differentiated into neurons by retinoic acid were pretreated with carvacrol or galantamine before Aβ1-42 administration...However, none of the treatments changed in-vitro SOD and tau-peptide levels, or in-vivo serum levels of MDA, H2O2, SOD, CAT, Tau peptide, Aβ1-40, or Aβ1-42. Our results suggest that multi-target pharmacological agent carvacrol may be promising in treatment of AD by preventing beta-amyloid-induced neurotoxicity, oxidative stress, and memory deficits.
- |||||||||| Cognex (tacrine) / Shionogi
Journal: Phytochemicals-based Therapeutics against Alzheimer's Disease: An Update. (Pubmed Central) - Nov 16, 2022
Phyto-chemicals derived from plants exhibit neuroprotection via targeting apoptosis, neurotrophic factor deficit, mitochondrial dysfunction, oxidative stress, and abnormal accumulation of proteins. Here, we discussed some of the neuroprotective phytochemicals used for the treatment of neurodegenerative diseases like AD and dementia.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: In Silico and In Vitro Studies of Benzothiazole-Isothioureas Derivatives as a Multitarget Compound for Alzheimer's Disease. (Pubmed Central) - Nov 16, 2022
In silico studies showed that 3f, 3r and 3t had a delta G (ΔG) value better than curcumin and galantamine on Aβ and AChE, respectively...Compound 3t showed the best anti-Aβ aggregation and inhibitory AChE activity and, despite that predictor, showed that it could be cytotoxic; in vitro with PC12 cell was negative. Therefore, 3t could be employed as a scaffold to develop new molecules with multitarget activity for AD and, due to physicochemical and pharmacokinetics predictions, it could be administered in vivo using liposomes due to is not able to cross the BBB.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
FDA event, Review, Journal: Drug Delivery Systems as a Strategy to Improve the Efficacy of FDA-Approved Alzheimer's Drugs. (Pubmed Central) - Nov 15, 2022
As a result, the pharmacological therapeutic effectiveness is raised, while the unwanted side effects induced by the unspecific distribution decrease. This article reviews the recently developed DDSs to increase the efficacy of Food and Drug Administration-approved AD drugs.
- |||||||||| galantamine hydrobromide / Generic mfg., pyridostigmine Bromide / Generic mfg.
Trial completion date, Trial primary completion date, Reflex: Vagal Stimulation in POTS (clinicaltrials.gov) - Oct 31, 2022
P1, N=11, Active, not recruiting,
Responsiveness to galantamine may be related to co-morbid AD pathology. Trial completion date: Dec 2022 --> Jun 2023 | Trial primary completion date: Jul 2022 --> Feb 2023
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Evaluation of anti-Alzheimer activity of synthetic coumarins by combination of in vitro and in silico approaches. (Pubmed Central) - Oct 26, 2022
The IC50 value of compound 16 for BChE inhibition (IC50=126.56 ± 11.96 µM) was slightly higher than galantamine...The three inhibitory coumarins (9, 13, 16) were next tested for their effects on the genes associated with AD using human neuroblastoma (SH-SY5Y) cell line. Our data indicate that they could be considered for further evaluation as new anti-Alzheimer drug candidates.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Pathology and prevention of brain microvascular and neuronal dysfunction induced by a high-fructose diet in rats. (Pubmed Central) - Oct 23, 2022
The aim of this study was to evaluate i) the involvement of microvascular disorders and neuronal plasticity in the deleterious effects of a high-fructose diet on the rat brain and ii) a comparative assessment of the effectiveness of Phytocollection therapy (with antidiabetic, antioxidant, and acetylcholinesterase inhibitory activities) compared to Galantamine as first-line therapy for dementia and Diabeton as first-line therapy for hyperglycemia...Differences in the parameters of spike background activity and expression of excitatory and inhibitory responses of cortical neurons have been discovered, allowing for flexibility and neuronal function stabilization in pathology and pharmacological prevention. Integration of the coupling mechanism between microvascular function and neuronal spike activity could delay the progressive decline in cognitive function in rats fed a high fructose diet.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Novel Morpholine-Bearing Quinoline Derivatives as Potential Cholinesterase Inhibitors: The Influence of Amine, Carbon Linkers and Phenylamino Groups. (Pubmed Central) - Oct 22, 2022
Among them, compounds 11a, 11g, 11h, 11j, 11l, and 12a had comparable inhibition activities to reference galantamine in AChE...Besides, compounds 11f and 11l showed excellent ABTS radical-scavenging activities, with IC values of 9.07 ± 1.34 μM and 6.05 ± 1.17 μM, respectively, which were superior to the control, Trolox (IC = 11.03 ± 0.76 μM). It is worth noting that 3-aminoquinoline derivatives 12a-12d exhibited better drug-like properties.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Resveratrol-Maltol and Resveratrol-Thiophene Hybrids as Cholinesterase Inhibitors and Antioxidants: Synthesis, Biometal Chelating Capability and Crystal Structure. (Pubmed Central) - Oct 21, 2022
While resveratrol-thiophene hybrids have excellent inhibitory and antioxidant properties (similar to the activity of reference drug galantamine), maltols have been proven to be weaker inhibitors and antioxidants...The crystal structures of two new resveratrol-maltol hybrids were recorded, giving additional information on the molecules' intermolecular hydrogen bonds and packing. In this way, several functionalities of these new resveratrol hybrids were examined as a necessary approach to finding more effective drugs for complicated neurodegenerative diseases.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: L-Cysteine Modified Chitosan Nanoparticles and Carbon-Based Nanostructures for the Intranasal Delivery of Galantamine. (Pubmed Central) - Oct 15, 2022
Finally, in vitro dissolution release studies revealed that the prepared NPs could prolong GAL's release for up to 12 days. In sum, regarding the most promising system, the results of the present study clearly suggest that the preparation of NPs using both Cys-CS and CDs results in a more thermodynamically stable drug dispersion, while a zero-order release profile was achieved, which is essential to attain a stable in vivo pharmacokinetic behavior.
- |||||||||| risperidone / Generic mfg., galantamine hydrobromide / Generic mfg.
Validating the use of PCP as a model of schizophrenia in rodents (SDCC Halls B-H) - Oct 10, 2022 - Abstract #Neuroscience2022NEUROSCIENCE_7813;
Mice treated with subchronic PCP showed no difference in time spent with either object suggesting a deficit in object recognition memory. The results indicate that subchronic treatment with PCP is a valid model for inducing schizophrenia-like phenotype in a rodent model.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., rivastigmine / Generic mfg.
Review: Predictors of response to acetylcholinesterase inhibitors in dementia: A systematic review. (Pubmed Central) - Oct 8, 2022
Short-term response may predict subsequent cognitive response, while higher education might correlate with short-term good response (months), and long-term poor response (years). Age, gender, baseline cognitive and functional levels, and APOE relationship with treatment outcome is controversial.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
TREATMENT STATUS OF ALZHEIMER’S DEMENTIA USING COMMON DATA MODEL IN SOUTH KOREA. () - Oct 5, 2022 - Abstract #CTAD2022CTAD_181;
Age, gender, baseline cognitive and functional levels, and APOE relationship with treatment outcome is controversial. There were differences in persistence and the prescribing pattern among anti-dementia medications from database using the Observational Medical Outcome Partnership Common Data Model in South Korea.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: GC-MS Chemical Profiling, Biological Investigation of Three Salvia Species Growing in Uzbekistan. (Pubmed Central) - Sep 18, 2022
AChE enzyme was more sensitive to S. officinalis EO (4.2 ± 0.01 mg galantamine equivalent (GALAE)/g oil), rather than S. virgata EO, which was ineffective...Partial least squares regression (PLS-R) models showed that there is an excellent correlation between the antioxidant activity and the volatile profile when being compared to that of enzyme inhibitory activity. Thus, the studied Salvia essential oils are interesting candidates that could be used in drug discovery for the management of Alzheimer's and hyperpigmentation conditions.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: A General Electro-Synthesis Approach to Amaryllidaceae Alkaloids. (Pubmed Central) - Sep 10, 2022
The biomimetic syntheses start with the readily available, inexpensive biogenic starting materials methyl gallate, O-methyl tyramine, and vanillin derivatives. Through known dynamic resolutions, this technology provides access to both enantiomeric series of martidine, (epi-)crinine, siculine, and galantamine, clinically prescribed for the treatment of Alzheimer's disease.
- |||||||||| dexamethasone / Generic mfg., galantamine hydrobromide / Generic mfg.
Review, Journal: Medicinal nicotine in COVID-19 acute respiratory distress syndrome, the new corticosteroid. (Pubmed Central) - Sep 3, 2022
Direct agonists like nicotine and GTS-1 have also demonstrated anti-inflammatory properties in models of sepsis and acute respiratory distress syndrome, as have acetylcholinesterase inhibitors like Galantamine and Physostigmine...Dexamethasone is the only medication currently in use that has shown to improve clinical outcomes...Nicotine transdermal patch activates CAP and harvests its anti-inflammatory potential by means of an easily administered depot delivery mechanism. It could prove to be a promising, safe and inexpensive additional tool in the currently limited armamentarium at our disposal for management of COVID-19 induced acute hypoxic respiratory failure.
- |||||||||| Aduhelm (aducanumab) / Eisai, Biogen, Nine Phase One (mannote sodium) / Shanghai Greenvalley
Review, Journal: Symptomatic and Disease-Modifying Therapy Pipeline for Alzheimer's Disease: Towards a Personalized Polypharmacology Patient-Centered Approach. (Pubmed Central) - Sep 3, 2022
Small molecules, mAbs, or multimodal strategies showing promise in animal studies have not confirmed that promise in the clinic (where small to moderate changes in clinical efficacy have been observed), and therefore, there is a significant unmet need for a better understanding of the AD pathogenesis and the exploration of alternative etiologies and therapeutic effective disease-modifying therapies strategies for AD. Therefore, a critical review of the disease-modifying therapy pipeline for Alzheimer's disease is needed.
- |||||||||| An Evaluation of Health Technology Assessment (HTA) Requirements for Emerging Therapies in Alzheimer’s Disease (AD) (In-person; Virtual) - Sep 1, 2022 - Abstract #ISPOREU2022ISPOR_EU_756;
Then we mapped the identified requirements from the HTA reports with endpoints used in clinical trials of emerging therapies (identified through clinicaltrials.gov), namely aducanumab, donanemab, gantenerumab, and lecanemab...Donepezil, galantamine, rivastigmine, and memantine are reimbursed in Germany, England, and Wales but not in France... Although clinical trials on new AD agents include HTA- and payer-relevant endpoints, it is highly recommended to also assess time to institutionalisation, HRQoL, and caregiver burden to generate a compelling HTA and payer evidence package.
- |||||||||| Journal: Drugs for cognitive loss and dementia. (Pubmed Central) - Aug 28, 2022
Although clinical trials on new AD agents include HTA- and payer-relevant endpoints, it is highly recommended to also assess time to institutionalisation, HRQoL, and caregiver burden to generate a compelling HTA and payer evidence package. No abstract available
- |||||||||| Aduhelm (aducanumab) / Eisai, Biogen, Namzaric (memantine ER/donepezil) / AbbVie, Supernus Pharma, Adlarity (donepezil transdermal system) / Corium
Journal: Comparison table: Drugs for Alzheimer's disease. (Pubmed Central) - Aug 28, 2022
No abstract available No abstract available
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Review, Journal: Advances on Therapeutic Strategies for Alzheimer's Disease: From Medicinal Plant to Nanotechnology. (Pubmed Central) - Aug 22, 2022
We have discussed pathophysiology, various targets, FDA-approved drugs, and various drugs in clinical trials against AD. The goal of this study is to shed light on current developments and treatment options, utilizing phytopharmaceuticals, nanomedicines, nutraceuticals, and gene therapy.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Isolation, derivatization, in-vitro, and in-silico studies of potent butyrylcholinesterase inhibitors from Berberis parkeriana Schneid. (Pubmed Central) - Aug 17, 2022
Among them, compound 15 was a potent BChE inhibitor (IC = 5.5 ± 0.3 μM), as compared to the standard drug galantamine hydrobromide (IC = 40.83 ± 0.37 μM)...In addition, these compounds were found to be non-cytotoxic against human fibroblast (BJ) cell line, except 9 (IC = 17.1 ± 1.0 μM), and 10 (IC = 18.4 ± 0.3 μM). Inhibition of cholinesterases is an important approach for development of drugs against Alzheimer's disease, and thus discoveries presented here deserve further investigation.
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