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Irina Tammenmaa-Aho, Rosie Asher, Karla Soares-Weiser, Hanna Bergman
BACKGROUND: Tardive dyskinesia (TD) remains a troublesome adverse effect of conventional antipsychotic (neuroleptic) medication. It has been proposed that TD could have a component of central cholinergic deficiency. Cholinergic drugs have been used to treat TD. OBJECTIVES: To determine the effects of cholinergic drugs (arecoline, choline, deanol, lecithin, meclofenoxate, physostigmine, RS 86, tacrine, metoxytacrine, galantamine, ipidacrine, donepezil, rivastigmine, eptastigmine, metrifonate, xanomeline, cevimeline) for treating antipsychotic-induced TD in people with schizophrenia or other chronic mental illness...
March 19, 2018: Cochrane Database of Systematic Reviews
Maju Mathew Koola, Ajay K Parsaik
No abstract text is available yet for this article.
June 2018: Schizophrenia Research. Cognition
Eva Mezeiova, Katarina Spilovska, Eugenie Nepovimova, Lukas Gorecki, Ondrej Soukup, Rafael Dolezal, David Malinak, Jana Janockova, Daniel Jun, Kamil Kuca, Jan Korabecny
Alzheimer's disease is debilitating neurodegenerative disorder in the elderly. Current therapy relies on administration of acetylcholinesterase inhibitors (AChEIs) -donepezil, rivastigmine, galantamine, and N-methyl-d-aspartate receptor antagonist memantine. However, their therapeutic effect is only short-term and stabilizes cognitive functions for up to 2 years. Given this drawback together with other pathological hallmarks of the disease taken into consideration, novel approaches have recently emerged to better cope with AD onset or its progression...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Hisanao Izumi, Yasuharu Shinoda, Takashi Saito, Takaomi C Saido, Keita Sato, Yasushi Yabuki, Yotaro Matsumoto, Yoshitomi Kanemitsu, Yoshihisa Tomioka, Nona Abolhassani, Yusaku Nakabeppu, Kohji Fukunaga
Alzheimer's disease (AD) is a progressive neurodegenerative disease and the most common form of elderly dementia in the world. At present, acetylcholine inhibitors, such as donepezil, galantamine and rivastigmine, are used for AD therapy, but the therapeutic efficacy is limited. We recently proposed T-type voltage-gated Ca2+ channels' (T-VGCCs) enhancer as a new therapeutic candidate for AD. In the current study, we confirmed the pharmacokinetics of SAK3 in the plasma and brain of mice using ultra performance liquid chromatography-tandem mass spectrometry...
March 3, 2018: Neuroscience
Rita Khoury, Jayashree Rajamanickam, George T Grossberg
Alzheimer's disease (AD) is the most common cause of major neurocognitive disorders worldwide. Despite all research efforts, therapeutic options for AD are still limited to two drug classes: cholinesterase inhibitors (ChEIs) and the NMDA-receptor antagonist memantine. Donepezil, rivastigmine and galantamine are the three ChEIs FDA-approved as first-line treatment for AD. Although they share the same mode of action, they differ in terms of their pharmacologic characteristics and route of administration, which can impact their safety and tolerability profile...
March 2018: Therapeutic Advances in Drug Safety
Mahboob Alam, Mohammad Jane Alam, Shaista Azaz, Mehtab Parveen, Soonheum Park, Shabbir Ahmad
The quantum chemical study, spectroscopic characterization and biological activity of the pharmaceutically active 7-benzoyloxycoumarin (2) molecule have been presented. Potential energy surface (PES) scanning has been performed to search for the most stable molecular geometry of the present compound. The stable geometry in the ground state, IR, UV-Vis absorption and NMR ( 13 C, 1 H) spectra of the title compound were theoretically obtained and compared with the experimental one. Various theoretical molecular parameters like molecular energy, atomic charges, dipole moment, thermodynamic parameters, donor-acceptor natural bond orbital (NBO) hyperconjugative interaction energies, frontier molecular orbitals energies, HOMO-LUMO gap, molecular electrostatic potential, chemical reactivity descriptors, molecular polarizability and non-linear optical (NLO) properties are presented...
February 8, 2018: Computational Biology and Chemistry
Zaahira Aumeeruddy-Elalfi, Namrita Lall, Bianca Fibrich, Analike Blom van Staden, Muzzammil Hosenally, Mohamad Fawzi Mahomoodally
Essential oils (EOs) extracted from six medicinal herbs and food plants [Cinnamomum zeylanicum (CZ), Psiadia arguta (PA), Psiadia terebinthina (PT), Citrus grandis (CGp), Citrus hystrix (CH), and Citrus reticulata (CR)] were studied for any inhibitory potential against key physiological enzymes involved in diabetes (α-glucosidase), skin aging (collagenase and elastase), and neurodegenerative disorders (acetylcholinesterase). Kinetic studies of the active EOs on the aforementioned enzymes were determined using Lineweaver-Burk plots...
January 2018: Journal of Food and Drug Analysis
Olufemi D Akilo, Pradeep Kumar, Yahya E Choonara, Priyamvada Pradeep, Lisa C du Toit, Viness Pillay
Alzheimer's disease (AD) is known to be caused by the accumulation of deformed beta amyloid and hyperphosphorylated tau proteins resulting into formation and aggregation of senile plaques and neurofibrillary tangles in the brain. Additionally, AD is associated with the accumulation of iron or metal ions in the brain which causes oxidative stress. Galantamine (Gal) is one of the therapeutic agents that has been approved for the treatment of AD, but still saddled with numerous side effects and could not address the issue of iron accumulation in the brain...
January 29, 2018: Journal of Cellular and Molecular Medicine
Bohang Zhou, Bingyu Zhang, Xingqiang Li, Xiuxiu Liu, Hui Li, Ding Li, Zhiming Cui, Huiling Geng, Le Zhou
A series of 2-aryl-9-methyl-β-carbolinium bromides (B) were synthesized and explored for anti-acetylcholinesterase (AChE) activities in vitro, action mechanism and structure-activity relationship. All the compounds B along with their respective 3,4-dihydro intermediates (A) presented anti-AChE activity at 10 μM. Thirteen compounds B showed the excellent activity with IC50 values of 0.11-0.76 μM and high selectivity toward AChE relative to butyrylcholinesterase (BChE), superior to galantamine (IC50 = 0...
January 24, 2018: Scientific Reports
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
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
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
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
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, it 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 1 year after treatment. In this article, we review existing and emerging smoking cessation pharmacotherapies, with a special emphasis on the most promising agents that are currently being investigated...
February 2018: Pharmacotherapy
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
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
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
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...
March 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
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
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
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