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https://www.readbyqxmd.com/read/29319910/reversal-of-mecamylamine-induced-effects-in-healthy-subjects-by-nicotine-receptor-agonists-cognitive-and-electro-physiological-responses
#1
Ricardo Alvarez-Jimenez, Ellen P Hart, Samantha Prins, Marieke de Kam, Joop M A van Gerven, Adam F Cohen, Geert Jan Groeneveld
AIM: Establishing a pharmacologic challenge model could yield an important tool to understand the complex role of the nicotinic cholinergic system in cognition and to develop novel compounds acting on the nicotinic acetylcholine receptor. METHODS: This randomized, double-blind, double-dummy, placebo-controlled, four way cross-over study examined the effects of the nicotinic antagonist mecamylamine on a battery of cognitive and neurophysiologic test with co-administration of a placebo, nicotine or galantamine in order to reverse the cognitive impairment caused by mecamylamine...
January 10, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29318278/effect-of-idalopirdine-as-adjunct-to-cholinesterase-inhibitors-on-change-in-cognition-in-patients-with-alzheimer-disease-three-randomized-clinical-trials
#2
Alireza Atri, Lutz Frölich, Clive Ballard, Pierre N Tariot, José Luis Molinuevo, Neli Boneva, Kristian Windfeld, Lars L Raket, Jeffrey L Cummings
Importance: New therapeutic approaches for Alzheimer disease (AD) are needed. Objective: To assess whether idalopirdine, a selective 5-hydroxytryptamine-6 receptor antagonist, is effective for symptomatic treatment of mild to moderate AD. Design, Setting, and Participants: Three randomized clinical trials that included 2525 patients aged 50 years or older with mild to moderate AD (study 1: n = 933 patients at 119 sites; study 2: n = 858 at 158 sites; and study 3: n = 734 at 126 sites)...
January 9, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29286595/galantamine-and-computerized-cognitive-behavioral-therapy-for-cocaine-dependence-a-randomized-clinical-trial
#3
Kathleen M Carroll, Charla Nich, Elise E DeVito, Julia M Shi, Mehmet Sofuoglu
OBJECTIVE: To examine whether galantamine, a cognitive-enhancing medication that is both acetylcholinesterase inhibitor and agonist at nicotinic acetylcholine receptors, is effective at improving cocaine use outcomes and cognitive functioning, alone and in combination with computerized cognitive behavioral therapy (CBT). METHOD: A 12-week, randomized 2 × 2, factorial trial was conducted to evaluate galantamine versus placebo (double-blind) and computerized CBT plus standard methadone treatment versus standard methadone treatment alone in a community-based methadone maintenance program (September 2009-April 2015)...
December 26, 2017: Journal of Clinical Psychiatry
https://www.readbyqxmd.com/read/29258890/serotonergic-and-cholinergic-modulation-of-functional-brain-connectivity-a-comparison-between-young-and-older-adults
#4
Bernadet L Klaassens, Joop M A van Gerven, Erica S Klaassen, Jeroen van der Grond, Serge A R B Rombouts
Aging is accompanied by changes in neurotransmission. To advance our understanding of how aging modifies specific neural circuitries, we examined serotonergic and cholinergic stimulation with resting state functional magnetic resonance imaging (RS-fMRI) in young and older adults. The instant response to the selective serotonin reuptake inhibitor citalopram (30 mg) and the acetylcholinesterase inhibitor galantamine (8 mg) was measured in 12 young and 17 older volunteers during a randomized, double blind, placebo-controlled, crossover study...
December 16, 2017: NeuroImage
https://www.readbyqxmd.com/read/29250815/current-and-emerging-pharmacotherapies-for-cessation-of-tobacco-smoking
#5
Nieves Gómez-Coronado, Adam J Walker, Michael Berk, Seetal Dodd
Tobacco use disorder is a chronic illness. With its high comorbidity rate, it is a major cause of years of life lost or years lived with disability; however, is also considered the most preventable cause of death in developed countries. Since the development of nicotine replacement therapy (NRT) in 1978, treatment options have continued to evolve and expand. Despite this, currently available treatments remain insufficient, with less than 25% of smokers remaining abstinent after one year after treatment. In this article, we review existing and emerging smoking cessation pharmacotherapies, affording a special emphasis on the most promising agents that are currently being investigated...
December 17, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/29248451/features-and-outcomes-of-drugs-for-combination-therapy-as-multi-targets-strategy-to-combat-alzheimer-s-disease
#6
REVIEW
Atish Kumar Sahoo, Jagnehswar Dandapat, Umesh Chandra Dash, Satish Kanhar
ETHNOPHARMACOLOGICAL RELEVANCE: Alzheimer's disease (AD), a deleterious neurodegenerative disorder that impairs memory, cognitive functions and may lead to dementia in late stage of life. The pathogenic cause of AD remains incompletely understood and FDA approved drugs are partial inhibitors rather than curative. Most of drugs are synthetic or natural products as galanthamine is an alkaloid obtained from Galanthus spp. Huperzine A, an alkaloid found in Huperzia spp., gingkolides a diterpenoids from Gingko biloba and many ethnobotanicals like Withania somnifera (L...
December 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29247294/rcbf-and-cognitive-impairment-changes-assessed-by-spect-and-adas-cog-in-late-onset-alzheimer-s-disease-after-18%C3%A2-months-of-treatment-with-the-cholinesterase-inhibitors-donepezil-or-galantamine
#7
Yukihiko Shirayama, Michio Takahashi, Yasunori Oda, Kouhei Yoshino, Koichi Sato, Toshiyuki Okubo, Masaomi Iyo
Late-onset Alzheimer's disease (AD) differs substantially from early-onset AD. In this cross sectional study we investigated brain perfusion changes after 18 months of treatment with cholinesterase inhibitors (ChEIs) donepezil or galantamine. Twenty-five drug-naïve late-onset AD patients were recruited from outpatient clinics. We examined brain perfusion using single photon emission computed tomography (SPECT) and used three-dimensional stereotactic surface projection (3D-SSP) and the stereotactic extraction estimation method (SEE) level 3 to analyze classified gyrus level segments...
December 15, 2017: Brain Imaging and Behavior
https://www.readbyqxmd.com/read/29239495/comparisons-between-traditional-medicines-and-pharmacotherapies-for-alzheimer-disease-a-systematic-review-and-meta-analysis-of-cognitive-outcomes
#8
REVIEW
Brian H May, Mei Feng, Anna J Hyde, Helmut Hügel, Su-Yueh Chang, Lin Dong, Xinfeng Guo, Anthony L Zhang, Chuanjian Lu, Charlie C Xue
OBJECTIVES: To evaluate the clinical evidence for traditional medicines (TMs) used in East Asia on measures of cognition in Alzheimer disease, determine the effect sizes at different time points for the TMs and pharmacotherapies, and assess the tolerability of the TMs. METHODS: We searched 12 databases in English, Chinese, and Japanese for eligible randomised controlled trials that compared orally administered TMs with pharmacotherapy and reported cognitive outcomes...
December 14, 2017: International Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/29179999/phytochemicals-as-inhibitors-of-nf-%C3%AE%C2%BAb-for-treatment-of-alzheimer-s-disease
#9
REVIEW
Ean-Jeong Seo, Nicolas Fischer, Thomas Efferth
Alzheimer's disease (AD) is the most prevalent form of dementia. The exact pathophysiology of this disease remains incompletely understood and safe and effective therapies are required. AD is highly correlated with neuroinflammation and oxidative stress in brain causing neuronal loss. Nuclear factor of activated B-cells (NF-κB) is involved in physiological inflammatory processes and thus representing a promising target for inflammation-based AD therapy. Phytochemicals are able to interfere with the NF-κB pathway...
November 24, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29168128/enhancement-of-galantamine-hbr-skin-permeation-using-sonophoresis-and-limonene-containing-pegylated-liposomes
#10
Worranan Rangsimawong, Yasuko Obata, Praneet Opanasopit, Tanasait Ngawhirunpat, Kozo Takayama
This study aimed to investigate the effect of low-frequency sonophoresis (SN) and limonene-containing PEGylated liposomes (PL) on the transdermal delivery of galantamine HBr (GLT). To evaluate the skin penetration mechanism, confocal laser scanning microscopy (CLSM), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were employed. The application of SN led to more GLT penetration into and through the skin than GLT solution alone. The liposomes also improved GLT permeation, and 2% limonene-containing PL (PL-LI2%) exhibited the highest GLT permeation, followed by PL-LI1%, PL-LI0...
November 22, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29165092/synthesis-characterization-and-biological-activities-of-new-symmetric-bis-1-2-3-triazoles-with-click-chemistry
#11
Fatih Celik, Yasemin Unver, Burak Barut, Arzu Ozel, Kemal Sancak
BACKGROUND: 1,2,3-Triazole and its derivatives have important biological activities such as antimicrobial, anti-allergic, analgesic, anti-HIV, antiinflammatory, anticancer, antimalarial and antituberculosis. Other significant triazole derivatives are 1,2,4-triazoles which play a very important role in the medicinal chemistry due to the antiinflammatory, antimicrobial, antimigraine, anticancer, antimicrobial and antimycotic activities. In this study, we aimed to synthesize a new series of bis-1,2,3-triazole derivatives including 1,2,4-triazole to obtain more effective biological activities METHODS: In this study, a new series of bis-1,2,3-triazole compounds (9,10,11) were synthesized...
November 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29143695/an-overview-of-systematic-reviews-of-pharmacological-and-non-pharmacological-interventions-for-the-treatment-of-behavioral-and-psychological-symptoms-of-dementia
#12
Suzanne M Dyer, Stephanie L Harrison, Kate Laver, Craig Whitehead, Maria Crotty
BACKGROUND: This systematic overview reports findings from systematic reviews of randomized controlled trials of pharmacological and non-pharmacological interventions for behavioural and psychological symptoms of dementia (BPSD). METHODS: The Cochrane Database of Systematic Reviews, DARE, Medline, EMBASE, and PsycINFO were searched to September 2015. RESULTS: Fifteen systematic reviews of eighteen different interventions were included. A significant improvement in BPSD was seen with: functional analysis-based interventions (GRADE quality of evidence moderate; standardized mean difference (SMD) -0...
November 16, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/29131306/comparative-effectiveness-and-safety-of-cognitive-enhancers-for-treating-alzheimer-s-disease-systematic-review-and-network-metaanalysis
#13
Andrea C Tricco, Huda M Ashoor, Charlene Soobiah, Patricia Rios, Areti Angeliki Veroniki, Jemila S Hamid, John D Ivory, Paul A Khan, Fatemeh Yazdi, Marco Ghassemi, Erik Blondal, Joanne M Ho, Carmen H Ng, Brenda Hemmelgarn, Sumit R Majumdar, Laure Perrier, Sharon E Straus
BACKGROUND/OBJECTIVES: To examine the comparative effectiveness and safety of cognitive enhancers for Alzheimer's disease (AD). DESIGN: Systematic review and Bayesian network metaanalysis (NMA). SETTING: MEDLINE, EMBASE, Cochrane Library, CINAHL, Ageline (inception-March 2016). PARTICIPANTS: Individuals with AD in randomized controlled trials (RCTs), quasi-RCTs, and nonrandomized studies. INTERVENTION: Any combination of donepezil, rivastigmine, galantamine, or memantine...
September 29, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/29130805/rehabilitative-success-after-brain-trauma-by-augmenting-a-subtherapeutic-dose-of-environmental-enrichment-with-galantamine
#14
Patricia B de la Tremblaye, Jody L Wellcome, Benjamin Wells de Witt, Jeffrey P Cheng, Elizabeth R Skidmore, Corina O Bondi, Anthony E Kline
BACKGROUND: Environmental enrichment (EE) confers benefits after traumatic brain injury (TBI) when provided daily for > 6 hours, but not 2 or 4 hours, which more accurately reflects the daily amount of clinical rehabilitation. The lack of benefit with sub-therapeutic EE suggests that augmentation with galantamine (GAL), which enhances cognition after TBI, may be indicated to confer benefits. OBJECTIVE: To test the hypothesis that 2 and 4 hours of EE paired with GAL will provide benefits comparable to 24 hours of EE alone...
November 1, 2017: Neurorehabilitation and Neural Repair
https://www.readbyqxmd.com/read/29126732/2-arylbenzofurans-from-artocarpus-lakoocha-and-methyl-ether-analogs-with-potent-cholinesterase-inhibitory-activity
#15
Umalee Namdaung, Anan Athipornchai, Thongchai Khammee, Mayuso Kuno, Sunit Suksamrarn
In vitro screening for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the Artocarpus lakoocha root-bark extracts revealed interesting results. Bioassay-guided fractionation resulted in the isolation of two new (1 and 2) and six known 2-arylbenzofurans 3-8, along with one stilbenoid 9 and one flavonoid 10. The structures of the isolated compounds were elucidated by UV, IR, 1D- and 2D-NMR and MS spectroscopic data analysis. Compounds 4, 6 and 7 exhibited more potent AChE inhibitory activity (IC50 = 0...
October 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29088998/post-injury-administration-of-galantamine-reduces-traumatic-brain-injury-pathology-and-improves-outcome
#16
Jing Zhao, Michael J Hylin, Nobuhide Kobori, Kimberly N Hood, Anthony N Moore, Pramod K Dash
Acetylcholine is an excitatory neurotransmitter in the central nervous system that plays a key role in cognitive function, including learning and memory. Previous studies have shown that experimental traumatic brain injury (TBI) reduces cholinergic neurotransmission, decreases evoked release of acetylcholine, and alters cholinergic receptor levels. Galantamine (U.S. Food and Drug Administration approved for the treatment of vascular dementia and Alzheimer's disease) has been shown to inhibit acetylcholinesterase activity and allosterically potentiate nicotinic receptor signaling...
December 18, 2017: Journal of Neurotrauma
https://www.readbyqxmd.com/read/29074413/galantamine-attenuates-n-n-dimethyl-hydrazine-induced-neoplastic-colon-damage-by-inhibiting-acetylcholinesterase-and-bimodal-regulation-of-nicotinic-cholinergic-neurotransmission
#17
Shreesh Raj Sammi, Jitendra K Rawat, Neetu Raghav, Ajay Kumar, Subhadeep Roy, Manjari Singh, Swetlana Gautam, Rajnish K Yadav, Uma Devi, Rakesh Pandey, Gaurav Kaithwas
The present study reveals the effect of galantamine (GAL) against 1, 2-dimethylhydrazine (DMH) induced colon cancer. Wistar albino rats were arbitrarily divided into four groups (n = 8). Group 1 served as normal control (normal saline, 3ml/kg/day, p.o.); group 2, 3 and 4 received DMH (20mg/kg/week, s.c.), for 6 weeks; groups 3 and 4 also received GAL (2 and 4mg/kg/day, p.o) for 6 weeks. DMH treated rats showed decreased heart rate variability (HRV) factors, increased incidence of aberrant crypt foci (ACF), increased thiobarbituric acid reactive substances (TBARs) along with the decrease in the enzymatic activity of superoxide dismutase (SOD) and catalase...
October 23, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28974110/acetylcholinesterase-inhibitors-beneficial-effects-on-comorbidities-in-patients-with-alzheimer-s-disease
#18
Vinod Kaushik, Sarah Toombs Smith, Emmanuel Mikobi, Mukaila A Raji
Elderly patients with Alzheimer's disease (AD) and other dementias are at high risk of polypharmacy and excessive polypharmacy for common coexisting medical conditions. Polypharmacy increases the risk of drug-drug and drug-disease interactions in these patients who may not be able to communicate early symptoms of adverse drug events. Three acetylcholinesterase inhibitors (ACHEIs) have been approved for AD: donepezil (Aricept), rivastigmine (Exelon), and galantamine (Razadyne). They are also used off-label for other causes of dementia such as Lewy body and vascular dementia...
January 1, 2017: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/28966636/heterocyclic-compounds-as-key-structures-for-the-interaction-with-old-and-new-targets-in-alzheimer-s-disease-therapy
#19
REVIEW
Asha Hiremathad, Luca Piemontese
Nowadays, Alzheimer's disease (AD) is widely recognized as a real social problem. In fact, only five drugs are FDA approved for the therapy of this widespread neurodegenerative disease, but with low results so far. Three of them (rivastigmine, donepezil and galantamine) are acetylcholinesterase inhibitors, memantine is a N-methyl-D-aspartate receptor antagonist, whereas the fifth formulation is a combination of donepezil with memantine. The prevention and treatment of AD is the new challenge for pharmaceutical industry, as well as for public institutions, physicians, patients, and their families...
August 2017: Neural Regeneration Research
https://www.readbyqxmd.com/read/28929435/neuroprotective-effects-of-galantamine-on-nerve-agent-induced-neuroglial-and-biochemical-changes
#20
RamaRao Golime, Meehir Palit, J Acharya, D K Dubey
Neuroprotection from nerve agent such as soman-induced neural damage is a major challenge for existing drugs. Nerve agent exposure can cause many neural effects in survivors arising mainly due to acetylcholinesterase (AChE) inhibition or death within minutes. Unraveling the mechanisms underlying the nerve agent-induced multiple neurological effects is useful to develop better and safe drugs. The present study aimed to understand the molecular response during soman exposure and to evaluate the neuroprotective efficacy of galantamine on nerve agent-induced neurotoxic changes...
September 19, 2017: Neurotoxicity Research
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