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https://www.readbyqxmd.com/read/29684390/lack-of-dopamine-supersensitivity-in-rats-after-chronic-administration-of-blonanserin-comparison-with-haloperidol
#1
Takashi Hashimoto, Satoko Baba, Hiroko Ikeda, Yasunori Oda, Kenji Hashimoto, Isao Shimizu
Long-term treatment with antipsychotic drugs in patients with schizophrenia can lead to dopamine supersensitivity psychosis. It is reported that repeated administration of haloperidol caused dopamine supersensitivity in rats. Blonanserin is an atypical antipsychotic drug with high affinity for dopamine D2 , D3 and serotonin2A receptors. In this study, we investigated whether chronic administration of blonanserin leads to dopamine supersensitivity. Following oral treatment with blonanserin (0.78mg/kg) or haloperidol (1...
April 20, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29670504/clozapine-induced-cardiovascular-side-effects-and-autonomic-dysfunction-a-systematic-review
#2
Jessica W Y Yuen, David D Kim, Ric M Procyshyn, Randall F White, William G Honer, Alasdair M Barr
Background: Clozapine is the antipsychotic of choice for treatment-resistant schizophrenia and has minimal risk for extrapyramidal symptoms. Therapeutic benefits, however, are accompanied by a myriad of cardiometabolic side-effects. The specific reasons for clozapine's high propensity to cause adverse cardiometabolic events remain unknown, but it is believed that autonomic dysfunction may play a role in many of these. Objective: This systematic review summarizes the literature on autonomic dysfunction and related cardiovascular side effects associated with clozapine treatment...
2018: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/29663882/key-updates-on-the-chemistry-and-biological-roles-of-thiazine-scaffold-a-review
#3
Shalki Choudhary, Pankaj Kumar Singh, Om Silakari
Nitrogen and sulphur based heterocyclic molecules have gained significant attention owing to their broad spectrum pharmacological profiles. Thiazine is one of such promising scaffolds which has been widely utilized in the synthesis of compounds that possess interesting biological profile including anti-proliferative, anti-bacterial, antipsychotic, analgesic, anti-inflammatory, antifungal and antiviral activities. The current review focus on the chemistry of thiazine and its derivatives along with potential pharmacological activities reported for them in scientific literature...
April 16, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29648618/inflammation-in-schizophrenia-pathogenetic-aspects-and-therapeutic-considerations
#4
Norbert Müller
This paper discusses the current evidence from animal and human studies for a central role of inflammation in schizophrenia. In animal models, pre- or perinatal elicitation of the immune response may increase immune reactivity throughout life, and similar findings have been described in humans. Levels of pro-inflammatory markers, such as cytokines, have been found to be increased in the blood and cerebrospinal fluid of patients with schizophrenia. Numerous epidemiological and clinical studies have provided evidence that various infectious agents are risk factors for schizophrenia and other psychoses...
April 10, 2018: Schizophrenia Bulletin
https://www.readbyqxmd.com/read/29614416/repositioning-of-the-antipsychotic-trifluoperazine-synthesis-biological-evaluation-and-in-silico-study-of-trifluoperazine-analogs-as-anti-glioblastoma-agents
#5
Seokmin Kang, Jung Moo Lee, Borami Jeon, Ahmed Elkamhawy, Sora Paik, Jinpyo Hong, Soo-Jin Oh, Sun Ha Paek, C Justin Lee, Ahmed H E Hassan, Sang Soo Kang, Eun Joo Roh
Repositioning of the antipsychotic drug trifluoperazine for treatment of glioblastoma, an aggressive brain tumor, has been previously suggested. However, trifluoperazine did not increase the survival time in mice models of glioblastoma. In attempt to identify an effective trifluoperazine analog, fourteen compounds have been synthesized and biologically in vitro and in vivo assessed. Using MTT assay, compounds 3dc and 3dd elicited 4-5 times more potent inhibitory activity than trifluoperazine with IC50  = 2...
March 23, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29609929/red-yeast-rice-ryr-supplementation-in-patients-treated-with-second-generation-antipsychotics
#6
Antonio Bruno, Gianluca Pandolfo, Manuela Crucitti, Giulia Maria Troili, Edoardo Spina, Rocco Antonio Zoccali, Maria Rosaria Anna Muscatello
OBJECTIVE: Second-generation antipsychotics (SGAs) have a negative impact on metabolic syndrome (MetS) risk factors for their effects on body weight and on metabolic parameters. Statins are widely used in the treatment of dyslipidemia; less is known on the ability of statins to treat SGAs-induced dyslipidemia, and nutraceutical approaches may represent promising strategies in SGAs-treated patients. Red Yeast Rice (RYR), the fermented product of the Aspergillaceae mold Monascus purpureus (red yeast) grown on white rice, has been shown to have a cholesterol-lowering effect which can be ascribed to monacolin K, although other active compounds may play a role management of hyperlipidemia...
April 2018: Complementary Therapies in Medicine
https://www.readbyqxmd.com/read/29605970/withdrawal-versus-continuation-of-long-term-antipsychotic-drug-use-for-behavioural-and-psychological-symptoms-in-older-people-with-dementia
#7
REVIEW
Ellen Van Leeuwen, Mirko Petrovic, Mieke L van Driel, An Im De Sutter, Robert Vander Stichele, Tom Declercq, Thierry Christiaens
BACKGROUND: Antipsychotic agents are often used to treat neuropsychiatric symptoms (NPS) in people with dementia although there is uncertainty about the effectiveness of their long-term use for this indication and concern that they may cause harm, including higher mortality. When behavioural strategies have failed and treatment with antipsychotic drugs is instituted, regular attempts to withdraw them have been recommended in guidelines. Physicians, nurses and families of older people with dementia may be reluctant to stop antipsychotics, fearing deterioration of NPS...
March 30, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29590590/modulation-of-deg-enacs-by-amphiphiles-suggests-sensitivity-to-membrane-alterations
#8
Axel Schmidt, Rick J Alsop, Rahul Rimal, Pia Lenzig, Sylvia Joussen, Natalie N Gervasi, Adree Khondker, Stefan Gründer, Maikel C Rheinstädter, Dominik Wiemuth
The bile acid-sensitive ion channel is activated by amphiphilic substances such as bile acids or artificial detergents via membrane alterations; however, the mechanism of membrane sensitivity of the bile acid-sensitive ion channel is not known. It has also not been systematically investigated whether other members of the degenerin/epithelial Na+ channel (DEG/ENaC) gene family are affected by amphiphilic compounds. Here, we show that DEG/ENaCs ASIC1a, ASIC3, ENaC, and the purinergic receptor P2X2 are modulated by a large number of different, structurally unrelated amphiphilic substances, namely the detergents N-lauroylsarcosine, Triton X-100, and β-octylglucoside; the fenamate flufenamic acid; the antipsychotic drug chlorpromazine; the natural phenol resveratrol; the chili pepper compound capsaicin; the loop diuretic furosemide; and the antiarrythmic agent verapamil...
March 27, 2018: Biophysical Journal
https://www.readbyqxmd.com/read/29582250/opposite-interplay-between-the-canonical-wnt-%C3%AE-catenin-pathway-and-ppar-gamma-a-potential-therapeutic-target-in-gliomas
#9
REVIEW
Alexandre Vallée, Yves Lecarpentier, Rémy Guillevin, Jean-Noël Vallée
In gliomas, the canonical Wingless/Int (WNT)/β-catenin pathway is increased while peroxisome proliferator-activated receptor gamma (PPAR-γ) is downregulated. The two systems act in an opposite manner. This review focuses on the interplay between WNT/β-catenin signaling and PPAR-γ and their metabolic implications as potential therapeutic target in gliomas. Activation of the WNT/β-catenin pathway stimulates the transcription of genes involved in proliferation, invasion, nucleotide synthesis, tumor growth, and angiogenesis...
March 26, 2018: Neuroscience Bulletin
https://www.readbyqxmd.com/read/29581153/aicar-prevents-acute-olanzapine-induced-disturbances-in-glucose-homeostasis
#10
Natasha D Bush, Logan K Townsend, David C Wright
Olanzapine (OLZ) is an antipsychotic drug used in the treatment of schizophrenia. While effective in reducing psychoses, OLZ causes acute increases in blood glucose. The acute effects of OLZ on hyperglycaemia are likely caused by reductions in insulin secretion, insulin resistance and increased hepatic glucose production. 5'AMP-activated protein kinase (AMPK) is an energy sensor activated during exercise that can increase insulin sensitivity and insulin-independent glucose uptake in muscle. 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) is a pharmacological agent that, among other effects, can activate AMPK in vivo...
March 26, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29575568/association-between-serotonin-syndrome-and-second-generation-antipsychotics-via-pharmacological-target-adverse-event-analysis
#11
Rebecca Racz, Theodoros G Soldatos, David Jackson, Keith Burkhart
Case reports suggest an association between second-generation antipsychotics (SGAs) and serotonin syndrome (SS). The US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS) was analyzed to generate hypotheses about how SGAs may interact with pharmacological targets associated with SS. FAERS was integrated with additional sources to link information about adverse events with drugs and targets. Using Proportional Reporting Ratios, we identified signals that were further investigated with the literature to evaluate mechanistic hypotheses formed from the integrated FAERS data...
March 25, 2018: Clinical and Translational Science
https://www.readbyqxmd.com/read/29569082/long-acting-injectable-second-generation-antipsychotics-an-update-and-comparison-between-agents
#12
REVIEW
Michael W Jann, Scott R Penzak
Schizophrenia is a chronic medical condition with periods of remission and relapses over a patient's lifetime. Antipsychotic medications represent the mainstay of treatment for this disease. Long-acting injectable (LAI) formulations of antipsychotics are an attractive alternative to their oral counterparts, as they enhance patient adherence. A number of second-generation antipsychotics (SGAs) are available in LAI formulations. These include paliperidone, aripiprazole, olanzapine, and risperidone. This article reviews the most recently developed and approved of these formulations-aripiprazole monohydrate, aripiprazole lauroxil, and paliperidone palmitate...
March 22, 2018: CNS Drugs
https://www.readbyqxmd.com/read/29568275/neurosteroids-in-schizophrenia-pathogenic-and-therapeutic-implications
#13
REVIEW
HuaLin Cai, Ting Cao, Xiang Zhou, Jeffrey K Yao
Neurosteroids are a group of important endogenous molecules affecting many neural functions in the brain. Increasing evidence suggests a possible role of these neurosteroids in the pathology and symptomatology of schizophrenia (SZ) and other mental disorders. The aim of this review is to summarize the current knowledge about the neural functions of neurosteroids in the brain, and to evaluate the role of the key neurosteroids as candidate modulators in the etiology and therapeutics of SZ. The present paper provides a brief introduction of neurosteroid metabolism and distribution, followed by a discussion of the mechanisms underlying neurosteroid actions in the brain...
2018: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29559781/novel-treatment-options-in-depression-and-psychosis
#14
REVIEW
Eva Ceskova, Petr Silhan
In spite of tremendous development in central nervous system research, current treatment is suboptimal, especially in severe mental disorders. In medicine, there are two main methods of improving the health care provided: seeking new treatment procedures and perfecting (optimizing) the existing ones. Optimization of treatment includes not only practical tools such as therapeutic drug monitoring but also implementation of general trends in the clinical practice. New pharmacological options include new more sophisticated forms of monoaminergic drugs, old drugs rediscovered on the base of a better understanding of pathophysiology of mental illnesses, and drugs aimed at new treatment targets...
2018: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/29556812/getting-it-right-the-first-time-recent-progress-in-optimizing-antiemetic-usage
#15
Lee Schwartzberg
Recent years have witnessed significant improvements in the prevention and management of chemotherapy-induced nausea and vomiting (CINV), allowing patients to complete their prescribed chemotherapy regimens without compromising quality of life. This reduction in the incidence of CINV can be primarily attributed to the emergence of effective, well-tolerated antiemetic therapies, including serotonin (5-hydroxytryptamine or 5-HT3) receptor antagonists, neurokinin-1 (NK-1) receptor antagonists, and the atypical antipsychotic olanzapine...
March 19, 2018: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/29553158/cholinergic-medication-for-antipsychotic-induced-tardive-dyskinesia
#16
REVIEW
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
https://www.readbyqxmd.com/read/29548911/involvement-of-gabaergic-bdnf-and-nox-2-mechanisms-in-the-prevention-and-reversal-of-ketamine-induced-schizophrenia-like-behavior-by-morin-in-mice
#17
Benneth Ben-Azu, Adegbuyi Oladele Aderibigbe, Abayomi Mayowa Ajayi, Aya-Ebi Okubo Eneni, Solomon Umukoro, Ezekiel O Iwalewa
GABAergic (Gamma-aminobutyric acid) and neurotrophic derangements have important implication in schizophrenia, a neuropsychiatric disease. Previous studies have shown that nicotinamide adenine dinucleotide phosphate oxidase (NADPH-oxidase) alters GABAergic and neurotrophic activities via inflammatory and oxidative pathways. Thus, it has been proposed that agents with anti-oxidant and anti-inflammatory properties might be beneficial for the treatment of the disease. Morin is neuroactive bioflavonoid compound, which has been reported to demonstrate antipsychotic and anti-oxidant/anti-inflammatory activities...
March 13, 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29540132/royal-australian-and-new-zealand-college-of-psychiatrists-clinical-practice-guidelines-for-mood-disorders-bipolar-disorder-summary
#18
Gin S Malhi, Tim Outhred, Grace Morris, Philip M Boyce, Richard Bryant, Paul B Fitzgerald, Malcolm J Hopwood, Bill Lyndon, Roger Mulder, Greg Murray, Richard J Porter, Ajeet B Singh, Kristina Fritz
In December 2015, the Royal Australian and New Zealand College of Psychiatrists published a comprehensive set of mood disorder clinical practice guidelines for psychiatrists, psychologists and mental health professionals. This guideline summary, directed broadly at primary care physicians, is an abridged version that focuses on bipolar disorder. It is intended as an aid to the management of this complex disorder for primary care physicians working in collaboration with psychiatrists to implement successful long term management...
March 19, 2018: Medical Journal of Australia
https://www.readbyqxmd.com/read/29519687/reprint-of-clinical-management-of-tardive-dyskinesia-five-steps-to-success
#19
REVIEW
Leslie Citrome
Tardive dyskinesia (TD) has long been thought to be a generally irreversible consequence of the use of dopamine receptor blocking agents. There is now an opportunity to successfully manage this condition with agents approved by the US Food and Drug Administration. This is important because TD has not been eliminated with the use of second-generation antipsychotics, and the expansion of antipsychotics to treat conditions other than schizophrenia has resulted in millions of additional individuals at risk for developing TD...
February 28, 2018: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/29516413/interplay-between-adenosine-receptor-antagonist-and-cyclooxygenase-inhibitor-in-haloperidol-induced-extrapyramidal-effects-in-mice
#20
Devinder Arora, Jayesh Mudgal, Madhavan Nampoothiri, Sanchari Basu Mallik, Manas Kinra, Susan Hall, Shailendra Anoopkumar-Dukie, Gary D Grant, Chamallamudi Mallikarjuna Rao
Antipsychotic drugs are the mainstay of psychotic disorders. The 'typical' antipsychotic agents are commonly employed for the positive symptoms of schizophrenia, though at an expense of extrapyramidal side effects (EPS). In the present study, we employed haloperidol (HP)-induced catalepsy model in mice to evaluate the role of adenosine receptor antagonist and cyclooxygenase (COX) enzyme inhibitor in the amelioration of EPS. HP produced a full blown catalepsy, akinesia and a significant impairment in locomotion and antioxidant status...
March 7, 2018: Metabolic Brain Disease
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