- |||||||||| galantamine hydrobromide / Generic mfg.
Biomarker, PK/PD data, Review, Journal: The Pharmacogenetics of Natural Products: A Pharmacokinetic and Pharmacodynamic Perspective. (Pubmed Central) - May 23, 2020
This review covers the effects of genetic variations in drug metabolizing enzymes, drug transporters, and direct and indirect interactions with the pharmacological targets/pathways on the individual response to natural products, and provides suggestions on dosing regimen adjustments of natural products based on their pharmacokinetic and pharmacogenetic paratmeters. Finally, we provide our viewpoints on the importance and necessity of pharmacogenetic and pharmacogenomic research of natural products in natural medicine's rational development and clinical application of precision medicine.
- |||||||||| Preclinical, Journal: Spatial memory deficits in mice induced by chemotherapeutic agents are prevented by acetylcholinesterase inhibitors. (Pubmed Central) - May 13, 2020
Therefore, fangchinoline-coptisine/berberine pairs, or their parental herbal mixtures, may potentially be developed as a possible therapeutic strategy for Alzheimer's patients. Results indicate that chemotherapy-induced spatial memory deficits in mice can be prevented, but not reversed by the use of acetylcholinesterase inhibitors concomitant with chemotherapy, suggesting that these agents should be investigated further for the prevention of chemobrain.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., rivastigmine / Generic mfg.
Clinical, Journal: Effect of Rivastigmine (Acetyl Cholinesterase Inhibitor) versus Placebo on Manic Episodes in Patients with Bipolar Disorders: Results from a Double Blind, Randomized, Placebo-Controlled Clinical Trial. (Pubmed Central) - May 1, 2020
The pattern of results from the present randomized, placebo-controlled, double-blind study suggests that adjuvant rivastigmine, a cholinesterase inhibitor, improved symptoms of mania among a larger sample of inpatients with BPD and in the acute manic state. However, the improvements were modest, and the results should be replicated and above all balanced against side effects.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Phytoconstituents and their possible mechanistic profile for Alzheimer's Disease - A Literature Review. (Pubmed Central) - Apr 22, 2020
So far some AChE inhibitors and NMDA receptor antagonists are the only approved medications and moreover western medicine is concentrating in isolation of moieties from the extracts that are responsible for therapeutic action. Even though several herbals have shown neuroprotective actions, we have mentioned about the phytoconstituents that have been tested experimentally against different Alzheimer's pathology models.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Design of natural-product-inspired multi-target ligands by machine learning. (Pubmed Central) - Apr 19, 2020
A virtual screening protocol based on machine learning models was used to identify mimetics of the natural product (-)-galantamine...Two of the computer-generated hits possess an expanded spectrum of bioactivity on targets relevant to the treatment of Alzheimer's disease and are suitable for hit-to-lead expansion. These results advocate multi-target drug design by advanced virtual screening protocols based on chemically-informed machine learning models.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Meta-Analyses of Randomized Controlled Trials and Potential Novel Combination Treatments in Schizophrenia (Americas Hall I & II) - Apr 17, 2020 - Abstract #SOBP2020SOBP_777;
All the major symptoms and biomarkers of schizophrenia (brain-derived neurotrophic factor, mismatch negativity, prepulse inhibition, gamma oscillations, and kynurenic acid) are based on nicotinic and NMDA receptors. To date, only one receptor has been targeted at a time with partial response.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Synthesis, molecular docking studies, and biological evaluation of novel alkyl bis(4-amino-5-cyanopyrimidine) derivatives. (Pubmed Central) - Apr 10, 2020
Molecular modeling study revealed that compounds 7c, 7f, and 7b showed a higher inhibitory activity than that of galantamine against both AChE and BChE...Taking into account the results of biological evaluation, further modifications will be designed to increase potency on different targets. In this study, the obtained results can be a new starting point for further development of multifunctional agents for the treatment of Alzheimer's disease.
- |||||||||| Kinaction (masitinib) / AB Science
Trial completion date, Trial primary completion date: Masitinib in Patients With Mild to Moderate Alzheimer's Disease (clinicaltrials.gov) - Apr 7, 2020
P3, N=721, Active, not recruiting,
In this study, the obtained results can be a new starting point for further development of multifunctional agents for the treatment of Alzheimer's disease. Trial completion date: Sep 2020 --> Jun 2020 | Trial primary completion date: Sep 2020 --> Dec 2019
- |||||||||| Kinaction (masitinib) / AB Science
Trial completion date, Trial primary completion date: Masitinib in Patients With Mild to Moderate Alzheimer's Disease (clinicaltrials.gov) - Apr 1, 2020
P3, N=721, Active, not recruiting,
Further studies should explore whether treating schizophrenia is a potentially modifiable risk factor for dementia. Trial completion date: Dec 2019 --> Sep 2020 | Trial primary completion date: Dec 2019 --> Sep 2020
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Novel regulatory systems for acetylcholine release in rat striatum and anti-Alzheimer's disease drugs. (Pubmed Central) - Mar 15, 2020
[ H]efflux was also enhanced by ACh uptake inhibitors (100 μM hemicholinium-3 and physostigmine), regardless of ACh hydrolysis. The present study shows that synaptic ACh concentrations in striatal cholinergic neurons are regulated in a complex manner by many factors such as release probability, presynaptic M /M /M mAChRs, AChE, and postsynaptic ACh uptake, and provides important information about cholinergic neurotransmission for future exploration of therapeutic strategies for Alzheimer's and other central nervous system diseases.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., rivastigmine / Generic mfg.
Clinical, Journal: An update on the utility and safety of cholinesterase inhibitors for the treatment of Alzheimer's disease. (Pubmed Central) - Mar 2, 2020
The authors have reviewed all recent literature including review articles, meta-analyses, clinical trials and more.Expert opinion: These ChEIs differ subtly in their mechanisms of action, in their tolerability and safety and FDA-approved indications. All are considered first-line, symptomatic treatments of the various phases of AD and may even have potentially disease-modifying effects.
- |||||||||| citalopram / Generic mfg., galantamine hydrobromide / Generic mfg.
Journal: Cholinergic and serotonergic modulation of resting state functional brain connectivity in Alzheimer's disease. (Pubmed Central) - Feb 28, 2020
Since AD has previously been characterized by reduced connectivity between the default mode network and the precuneus and posterior cingulate cortex, the effects of citalopram on the default mode network suggest a restoring potential of selective serotonin reuptake inhibitors in AD. The results of this study also confirm a change in cerebellar connections in AD, which is possibly related to cholinergic decline.
- |||||||||| galantamine hydrobromide / Generic mfg., dronabinol oral / Generic mfg.
Journal: Feasibility and effects of galantamine on cognition in humans with cannabis use disorder. (Pubmed Central) - Feb 26, 2020
The findings of this pilot study support the feasibility of the administration of galantamine for individuals with CUD. Adequately powered, randomized, placebo-controlled trials are required to investigate the potential of galantamine to improve cognitive deficits associated with CUD.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Ursolic and oleanolic acid derivatives with cholinesterase inhibiting potential. (Pubmed Central) - Feb 14, 2020
An ursolic acid derived hydroxyl-propinyl derivative 10 was a competitive inhibitor for butyrylcholinesterase with an inhibition constant of K = 4.29 μM, and therefore being twice as active as gold standard galantamine hydrobromide. The best inhibitor for acetylcholinesterase, however, was 2-methyl-3-oxo-methyl-ursoloate (18), acting as a mixed-type inhibitor showing K = 1.72 µM and K' = 1.28 μM, respectively.
- |||||||||| Medication-Induced QTc Prolongation in Parkinson’s Disease-Related Psychosis: A Literature Review (Biscayne Ballroom) - Feb 14, 2020 - Abstract #MDSPAS2020MDS_PAS_77;
While PD patients exhibiting psychotic symptoms are treated with medications targeting multiple neurotransmitters, it is possible that PD patients exhibit different QTc prolongation profiles following antipsychotic use as compared to other patient populations. Neuroimaging evidence from a 1997 paper demonstrated cardiac sympathetic denervation in PD, which has been confirmed by many studies since, (23) and additional studies are needed to determine whether these changes could affect QTc intervals in PD patients treated with antipsychotics.
- |||||||||| galantamine hydrobromide / Generic mfg., pyridostigmine Bromide / Generic mfg.
Enrollment closed, Enrollment change, Reflex: Vagal Stimulation in POTS (clinicaltrials.gov) - Feb 10, 2020
P1, N=11, Active, not recruiting,
Neuroimaging evidence from a 1997 paper demonstrated cardiac sympathetic denervation in PD, which has been confirmed by many studies since, (23) and additional studies are needed to determine whether these changes could affect QTc intervals in PD patients treated with antipsychotics. Recruiting --> Active, not recruiting | N=16 --> 11
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Chemical profiling of Centaurea bornmuelleri Hausskn. aerial parts by HPLC-MS/MS and their pharmaceutical effects: From nature to novel perspectives. (Pubmed Central) - Feb 7, 2020
Ethyl acetate extract of C. bornmuelleri inhibited both acetylcholinesterase (1.14 mg galantamine equivalent [GALAE]/g extract), butyrylcholinesterase (0.63 mg GALAE/g extract), tyrosinase (69.84 mg kojic acid equivalent/g extract), amylase (19.90 mg acarbose equivalent [ACAE]/g extract), and glucosidase (33.12 mg ACAE/g extract). The phytochemical profile of C. bornmuelleri has been characterized and the main components quantified in order to provide scientific base to design innovative products including pharmaceuticals, cosmetics or nutraceuticals although further investigation concerning the isolation of the main bioactive compounds would be required.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Journal: Synthesis of 2-(2-oxo-2H-chromen-4-yl)acetamides as potent acetylcholinesterase inhibitors and molecular insights into binding interactions. (Pubmed Central) - Jan 23, 2020
The most active compound in this series, 5a (IC 0.04 ± 0.01 µM), noncompetitively inhibited AChE with a higher potency than tacrine and galantamine...Molecular docking was applied to postulate the selectivity toward AChE of 5a in comparison with donepezil and tacrine...ADMET analysis suggested that the 2-(2-oxo-2H-chromen-4-yl)acetamides showed a good pharmacokinetic profile and no hepatotoxicity. These coumarin derivatives showed high potential for further development as anti-Alzheimer agents.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Clinical, Journal, Real-World Evidence: Comparison of cholinesterase inhibitor safety in real-world practice. (Pubmed Central) - Jan 11, 2020
Compared with low-dose donepezil, galantamine use was associated with a lower risk of mortality (adjusted hazard ratio: 0.84, 95% confidence interval: 0.60-1.18), cardiovascular serious adverse events (adjusted hazard ratio: 0.78, 95% confidence interval: 0.62-0.98), and entry into a residential care facility (adjusted hazard ratio: 0.72, 95% confidence interval: 0.59-0.89). Given the absence of randomized trial data showing clinically meaningful benefit of ChEI therapy in Alzheimer's disease, our study suggests preferential use of galantamine may at least be associated with fewer adverse events than treatment with donepezil or rivastigmine.
- |||||||||| galantamine hydrobromide / Generic mfg.
Trial completion date, Trial primary completion date: Effects of Galantamine on Cognition (clinicaltrials.gov) - Jan 7, 2020
P2, N=24, Active, not recruiting,
Given the absence of randomized trial data showing clinically meaningful benefit of ChEI therapy in Alzheimer's disease, our study suggests preferential use of galantamine may at least be associated with fewer adverse events than treatment with donepezil or rivastigmine. Trial completion date: Dec 2019 --> Dec 2020 | Trial primary completion date: Dec 2019 --> Dec 2020
- |||||||||| galantamine hydrobromide / Generic mfg.
[VIRTUAL] NEW PEPTIDE DERIVATIVES OF GALANTAMINE WITH ACETYLCHOLINE ESTERASE INHIBITORY EFFECT (EXHIBITION HALL) - Jan 6, 2020 - Abstract #AATADPD2020AAT_ADPD_753;
Present studies confirmed preliminary data of our team about improving memory effect of compounds on scopolamine AD mouse model and gives some details on the mechanism of their action. Conclusions We consider that four newly synthesized GalD have significant AChE inhibitory activity (especially GalD 43) and are potentially active agents for AD prevention and treatment.
- |||||||||| galantamine hydrobromide / Generic mfg.
[VIRTUAL] EFFECT OF MYRTENAL IN EXPERIMENTAL DEMENTIA – NEUROMODULATORY AND HISTOLOGICAL EXAMINATIONS (EXHIBITION HALL) - Jan 6, 2020 - Abstract #AATADPD2020AAT_ADPD_752;
Methods Male Wistar rats (180-210 g) were divided into groups and treated i.p.: Control (saline), Scopolamine (Scop., 0.1 mg/kg for 8 days and 20 mg/kg on the 9th day), Galantamine as a reference for anti-cholinesterase activity (Gal, 1 mg/kg b.wt.) and Myrtenal (M, 40 mg/kg b.wt.)...Conclusions The neuromodulatory effects of M confirmed the results of our previous studies on its potential to improve cognitive abilities in experimental animals and manifested anxiolytic properties. Histological studies (qualitative and quantitative) of different regions of the rat brain suggest the brain cortex as the main site of M’s neuroprotective action.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., rivastigmine / Generic mfg.
[VIRTUAL] USING CHOLINESTERASE INHIBITORS TO TREAT ALZHEIMER PATIENTS AT DIFFERENT STAGES OF THE DISEASE. WHAT WE HAVE LEARNED IN 25Y EXPERIENCE! (Hall E) - Jan 6, 2020 - Abstract #AATADPD2020AAT_ADPD_153;
ChEI are clinically efficacious at mild to moderate , as well as at severe stages of AD.2 Female MCI with APOE4 + respond better than male MCI.3 generally, higher doses are more effective in severe cases.4 there are positive clinical therapeutic dose-response effects at any stage of the disease.5 rapidly progressing patients in moderate stages are more likely to respond .6 the three most used ChEI (donepezil, rivastigmine, galantamine) do not show clinically significant differences .7 beneficial, symptomatic effects may persist over 1-2 years and their administration should be continued as long as the patients are benefiting.8 valuable indications for ChEI therapy are : Lewy body dementia ; Parkinson dementia, Mixed AD and Vascular Dementia.9 female and male AD patients show differences in disease progression and do not respond similarly to CEIhhhEI. Conclusions a remarkable progress in our knowledge has been obtained regarding the use of ChEI in AD ,allowing for a more personalized treatment.
- |||||||||| galantamine hydrobromide / generics
Preclinical, Journal: Ameliorative effect of galantamine on acetic acid-induced colitis in rats. (Pubmed Central) - Dec 8, 2019
Thus the antioxidant and anti-inflammatory effects may account for its anti-inflammatory and anti-ulcerative properties. Nevertheless, further detailed studies are warranted for exact elucidation of GAL mechanism on inflammation and colitis.
- |||||||||| galantamine hydrobromide / generics
Journal: Aporphines and Alzheimer's disease: Towards a Medical Approach Facing the Future. (Pubmed Central) - Dec 6, 2019
In this review, the use of aporphines in nature is showed for treating Alzheimer's disease, alkaloids isolated from natural and/or synthetic sources have been used principally as cholinesterase inhibitors (acetyl- and butyrylcholinesterase) as galantamine, for instance, though its use has been questioned for being slightly effective or marginal. The use of aporphines give the possibility of generating new treatments with nitrogenous chemical structures of diverse complexity and that are focused in this review comparatively and with real therapeutic scopes.
- |||||||||| galantamine hydrobromide / Generic mfg.
Trial completion: SAHRANG: Subarachnoid Hemorrhage Recovery And Galantamine (clinicaltrials.gov) - Dec 5, 2019
P1/2, N=60, Completed,
The use of aporphines give the possibility of generating new treatments with nitrogenous chemical structures of diverse complexity and that are focused in this review comparatively and with real therapeutic scopes. Recruiting --> Completed
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Journal: Cholinesterase as a Target for Drug Development in Alzheimer's Disease. (Pubmed Central) - Nov 28, 2019
Herein, we describe the role of acetylcholine sterase (AChE) and related hypothesis in AD along with the pharmacological and chemical aspects of the available cholinesterase inhibitors. This chapter discusses the development of several congeners and hybrids of available cholinesterase inhibitors along with their binding patterns in enzyme active sites.
- |||||||||| galantamine hydrobromide / generics
Preclinical, Journal: Activation of α7 Nicotinic Acetylcholine Receptor Ameliorates Zymosan-Induced Acute Kidney Injury in BALB/c Mice. (Pubmed Central) - Nov 21, 2019
Furthermore, the reno-curattive effect of galantamine was associated by a reduction in plasma creatinine (Cr), cystatin (Cys)-C, IL-18, and renal neutrophil gelatinase-associated lipocalin (NGAL), as well as an improved histopathological structure. Blocking the α7 nAChR by methyllycaconitine abolished the beneficial effect of galantamine to document the involvement of this receptor and the CAP in the amelioration of AKI induced by zymosan.
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