- |||||||||| risperidone / Generic mfg., galantamine hydrobromide / Generic mfg., rivastigmine / Generic mfg.
Review, Journal: Acetylcholinesterase inhibitors for autistic spectrum disorders. (Pubmed Central) - Jun 6, 2023
There is a need for more evidence of improvement in outcomes of relevance to clinical care, autistic people, and their families. There are a number of ongoing studies involving acetylcholinesterase inhibitors, and future updates of this review may add to the current evidence.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Review, Journal: Alzheimer's disease: Molecular aspects and treatment opportunities using herbal drugs. (Pubmed Central) - May 24, 2023
Herbal and food intake is also important as preventive strategy and recently focus has also been placed on herbal drugs for treatment. This review focuses on the molecular aspects, pathogenesis and recent studies that signifies the potential of medicinal plants and their extracts or chemical constituents for the treatment of degenerative symptoms related to AD.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Journal: Anti-Dementia Drugs (Anti-Alzheimer's Disease Drugs) (Pubmed Central) - May 21, 2023
In Japan, DMTs have not yet been approved for treating AD; however, four drugs are currently available for symptomatic therapies, including cholinesterase inhibitors (ChEIs) such as donepezil for mild-to-severe dementia, galantamine and rivastigmine for mild-to-moderate dementia, and memantine, an N-methyl-D-aspartate (NMDA) receptor antagonist, for moderate-to-severe dementia. In this review, we describe the use of four symptomatic anti-AD drugs in clinical practice for AD.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Journal, Adverse events: Adverse Drug Event Profile Associated with Anti-dementia Drugs: Analysis of a Spontaneous Reporting Database. (Pubmed Central) - May 20, 2023
Bradycardia, loss of consciousness, falls, and syncope incidence were significantly diverse. The Kaplan-Meier curve results for the cumulative ADEs incidence showed that donepezil had the slowest onset, while galantamine, rivastigmine, and memantine had approximately the same timing of onset.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Azole derivatives inhibit wildtype butyrylcholinesterase and its common mutants. (Pubmed Central) - May 8, 2023
In the current study, an azole library of 1-aryl-2-(1H-imidazol-1-yl)ethanol/ethanone oxime esters were tested against AChE and BChE, which yielded derivates more potent than the positive control, galantamine, against both isoforms...Molecular modeling confirmed these kinetic data and provided further insights regarding molecular basis of BChE inhibition by the active derivatives. Thus, current study suggests new azole derivatives with promising cholinesterase inhibitory effects and reveals the first set of information to promote our understanding for the inhibitory behavior of this class against the mutant BChE forms.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Preclinical, Journal: Myricetin improves pathological changes in 3 (Pubmed Central) - May 7, 2023
Our results revealed the therapeutic efficacy of Myr in experimental AD, and implied that the associated mechanism is possibly associated with inhibiting tmitochondrial dysfunction, activating NLRP3 inflammasome, and neuroinflammation which was mediated by P38 MAPK pathway. Myr is the drug candidate in AD therapy via targeting P38 MAPK pathway.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., queuine (STEL-101) / Stellate Therap
Journal: Proposing novel natural compounds against Alzheimer's disease targeting acetylcholinesterase. (Pubmed Central) - May 1, 2023
The results showed that the selected doses were effective with half inhibitory concentrations estimated to be: Queuine (IC50 = 70,90 ?M), Etoperidone (IC50 = 712,80 ?M), Thiamine (IC50 = 18780,34 ?M), Galantamine (IC50 = 556,01 ?M) and Donepezil (IC50 = 222,23 ?M), respectively. The promising results for these molecules suggest the development of the next step in vivo animal testing and provide hope for natural therapeutic aids in the treatment of AD.
- |||||||||| galantamine hydrobromide / Generic mfg.
Review, Journal: Phytochemicals: A Promising Alternative for the Prevention of Alzheimer's Disease. (Pubmed Central) - Apr 28, 2023
These plants possess anti-inflammatory, antioxidant, anticholinesterase, and anti-amyloid properties and are safe for consumption. This paper focuses on the taxonomic details of the plants, the mode of action of their phytochemicals, their safety, future prospects, limitations, and sustainability criteria for the effective treatment of AD.
- |||||||||| lithium carbonate ER / Generic mfg.
Journal: An update on potential pharmacotherapies for cognitive impairment in bipolar disorder. (Pubmed Central) - Apr 17, 2023
Traditional treatments, such as lithium, anticonvulsants (lamotrigine), antipsychotics (aripiprazole, asenapine, cariprazine, lurasidone, and olanzapine), antidepressants (vortioxetine, fluoxetine, and tianeptine) and psychostimulants (modafinil), and emerging interventions, such as acetylcholinesterase inhibitors (galantamine and donepezil), dopamine agonists (pramipexole), erythropoietin, glucocorticoid receptor antagonists (mifepristone), immune modulators (infliximab, minocycline and doxycycline), ketamine, metabolic agents (insulin, metformin, and liraglutide), probiotic supplements, and Withania somnifera are discussed...In the past, methodological pitfalls in BD cognition trials have also been a critical limiting factor. Expanding on the existing literature and identifying novel pharmacological and non-pharmacological treatments for cognitive impairment in BD should be a priority.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal, IO biomarker: Diagnoses and new therapeutic strategy focused on physiological alteration of tryptophan metabolism (Pubmed Central) - Mar 30, 2023
Taken together, depletion of 5-HT by induction of IDO1 and ?7nAChR antagonism by KA via decreased KMO expression cause depression-like behavior, suggesting that metabolic alterations in TRP-KYN pathway are highly involved in the pathophysiology of MDD. Therefore, TRP-KYN pathway is expected to be an attractive target for the development of novel diagnosis of MDD and antidepressants.
- |||||||||| galantamine hydrobromide / Generic mfg., pyridostigmine Bromide / Generic mfg.
Trial completion date, Trial primary completion date, Reflex: Vagal Stimulation in POTS (clinicaltrials.gov) - Mar 17, 2023
P1, N=11, Active, not recruiting,
GH release profiles in PBS at 37 Trial completion date: Jun 2023 --> Dec 2024 | Trial primary completion date: Feb 2023 --> Jun 2024
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Natural products as bioactive agents in the prevention of dementia. (Pubmed Central) - Mar 16, 2023
In contrast, despite the existence of a large library of natural products, only a few of them (galantamine, huperzine A, etc.) have been approved as drugs against dementia...Despite an efficient role of natural products in dementia prevention, their direct application as drugs are still limited due to some controversial results obtained from their clinical trials however bioassay guided drug development studies can prove them potential drugs against dementia and related diseases. This review provides useful information for a researcher working in the field, pharmacologists, medical doctors, and for the pharmaceutical industry.
- |||||||||| galantamine hydrobromide / Generic mfg.
Review, Journal, IO biomarker: Targeting Persistent Changes in Neuroimmune and Epigenetic Signaling in Adolescent Drinking to Treat Alcohol Use Disorder in Adulthood. (Pubmed Central) - Feb 13, 2023
Inhibition of HMGB1 neuroimmune signaling, histone methylation enzymes, and galantamine, the cholinesterase inhibitor, both prevent and reverse AIE pathology...Preclinical studies find the underage binge drinking adolescent intermittent ethanol (AIE) model causes lasting changes in adults that increase risks of developing adult alcohol problems. Loss of hippocampal neurogenesis and loss of basal forebrain cholinergic neurons provide examples of how AIE-induced epigenetic and neuroimmune signaling provide novel therapeutic targets for adult AUD.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Galantamine Based Novel Acetylcholinesterase Enzyme Inhibitors: A Molecular Modeling Design Approach. (Pubmed Central) - Feb 12, 2023
In conclusion, this study shows that in silico modeling can be used to create new drug candidate inhibitors for hAChE. The compounds ZINC16951574-LMQC2, and ZINC08342556-LMQC5 are particularly promising for oral administration because they have a favorable drug-likeness profile, excellent lipid solubility, high bioavailability, and adequate pharmacokinetics.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Journal: Investigation of Cannabis sativa Phytochemicals as Anti-Alzheimer's Agents: An In Silico Study. (Pubmed Central) - Feb 11, 2023
On the other hand, Cannabinol C2 (BA = -9.2 kcal/mol, Ki = 4.32 mM) significantly inhibits Butyrylcholinesterase (BuChE) in comparison to Memantine (BA = -6.8 kcal/mol, Ki = 0.54 mM). This study sheds new light and opens new avenues for elucidating the role of bioactive compounds present in Cannabis sativa in treating Alzheimer's disease.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Synthesis, characterization, and in vitro anti-cholinesterase screening of novel indole amines. (Pubmed Central) - Jan 24, 2023
These ligands interacted with the PAS site in the enzyme, and their binding may disrupt the activity. The in vitro acetylcholinesterase inhibition studies revealed that the IC values for indole amines 25 and 24 (4.28 and 4.66 μM, respectively) were comparable to that of galantamine (4.15 μM) and may be studied further as cost-effective acetylcholinesterase inhibitors.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Butenolide derivatives from Aspergillus terreus selectively inhibit butyrylcholinesterase. (Pubmed Central) - Jan 10, 2023
All compounds were evaluated for cholinesterase inhibitory effects with galantamine as a positive control...The structure-activity relationship was discussed. Molecular docking and dynamic simulation of the inhibitor-enzyme complex were performed to better understand the interactions.
- |||||||||| solanezumab (LY2062430) / Eli Lilly
Review, Journal: Review of Alzheimer's disease drugs and their relationship with neuron-glia interaction. (Pubmed Central) - Jan 4, 2023
This review focused on existing medications used in treating AD amongst which include Donepezil, Choline Alphoscerate, Galantamine, Dextromethorphan, palmitoylethanolamide, citalopram, resveratrol, and solanezumab. This review summarizes the effects of these drugs on neurons, astrocytes, and microglia interactions based on their pharmacokinetic properties, mechanism of action, dosing, and clinical presentations.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg., rivastigmine / Generic mfg.
Review, Journal: Role of multi-targeted bioactive natural molecules and their derivatives in the treatment of Alzheimer's disease: an insight into structure-activity relationship. (Pubmed Central) - Dec 30, 2022
This review summarises the structural properties required for bioactive natural molecules to show anti-Alzheimer's activity by emphasizing on SAR of several bioactive natural molecules targeting various AD pathologies, their key molecular interactions that are critical for target specificity, their role as multitargeted ligands, used with adjunctive therapy for AD followed by related US patents granted recently. This article highlights the significance of the structural features of natural bioactive molecules in the treatment of AD and establishes a connection between them.Communicated by Ramaswamy H. Sarma.
- |||||||||| galantamine hydrobromide / Generic mfg.
AN ASSESSMENT OF CERTAIN PHYTOCHEMICALS AS POSSIBLE THERAPEUTIC OPTIONS TO TREAT ALZHEIMER'S DISEASE (EXHIBITION) - Dec 23, 2022 - Abstract #ADPD2023ADPD_1791;
Since 2001, the FDA -approved second -generation ChEI galantamine hydrobromide has been one of the mainstay treatments for mi ld-to-moderate AD, and little has changed regarding the drug therapy for AD. Along with phytochemical ChEIs, the potential of Gala was also examined and observed to be the most potent of the natural products.PhTs, most notably 4 -O-CQA, Q3 -?-D-G, Rutin and Ber are potentially useful ChEIs with the additional benefits of potent antioxidant and free radical scavenging capacity, and low cytotoxicity may therefore prove valuable compounds for the development as the next -generation ChEIs for the treatment of AD.
- |||||||||| galantamine hydrobromide / Generic mfg.
SYNERGISTIC MODULATION OF THE CHOLINERGIC SYSTEM IN A TRANSGENIC RAT MODEL OF AD (EXHIBITION) - Dec 23, 2022 - Abstract #ADPD2023ADPD_1382;
This co -treatment effect can be achieved by AChEIs such as galantamine, which increases the synaptic concentration of ACh. Not only cholinergic deficits but also amyloid plaques and neuroinflammation represent neuropathological origins of cognitive decline and disease burden in AD.
- |||||||||| imipramine / Generic mfg., galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Methanolic Extract of Aerva javanica Leaves Prevents LPS-Induced Depressive Like Behavior in Experimental Mice. (Pubmed Central) - Dec 16, 2022
While imipramine and Aj.Cr (100, 300, and 500 mg/kg) treated groups significantly (p<0.05) improved the depressive-like behavior and biomarkers when compared to the LPS group. The mitigation of LPS-induced depressive-like behavior by Aj.Cr may be linked to the modulation of oxidative stress, neuro-inflammation and catecholamines due to the presence of potent bioactive compounds exerting anti-depressant effects.
- |||||||||| Aduhelm (aducanumab) / Eisai, Biogen
Review, Journal: Conventional Versus New Treatment: Comparing the Effects of Acetylcholinesterase Inhibitors and N-Methyl-D-Aspartate Receptor Antagonist With Aducanumab. (Pubmed Central) - Dec 8, 2022
Furthermore, memantine, an NMDA receptor antagonist, is authorized for moderate-to-severe dementia...Unfortunately, at this time, aducanumab's risks outweigh the benefits with a questionable approval process by the Food and Drug Administration (FDA). However, given the potential disease-modifying capabilities of aducanumab, other disease-modifying options may become available by possibly reducing inflammation, preventing Aβ plaques from clumping, or keeping tau proteins from tangling.
- |||||||||| Cognex (tacrine) / Shionogi
Journal: Recent developments in tacrine-based hybrids as a therapeutic option for Alzheimer's disease. (Pubmed Central) - Dec 6, 2022
Here, tacrine-based derivatives including heterocyclic structures such as dihydroxypyridine, chromene, coumarin, pyrazole, triazole, tetrahydroquinolone, dipicolylamine, arylisoxazole were reported with promising anti-AD effects compared to tacrine. In vitro and in vivo assays showed that new tacrine-based hybrids, which are selective, neuroprotective, and non-hepatotoxic, might be considered as remarkable anti-AD drug candidates for further clinical studies.
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