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https://www.readbyqxmd.com/read/28721057/safety-tolerability-and-risks-associated-with-first-and-second-generation-antipsychotics-a-state-of-the-art-clinical-review
#1
REVIEW
Marco Solmi, Andrea Murru, Isabella Pacchiarotti, Juan Undurraga, Nicola Veronese, Michele Fornaro, Brendon Stubbs, Francesco Monaco, Eduard Vieta, Mary V Seeman, Christoph U Correll, André F Carvalho
Since the discovery of chlorpromazine (CPZ) in 1952, first-generation antipsychotics (FGAs) have revolutionized psychiatric care in terms of facilitating discharge from hospital and enabling large numbers of patients with severe mental illness (SMI) to be treated in the community. Second-generation antipsychotics (SGAs) ushered in a progressive shift from the paternalistic management of SMI symptoms to a patient-centered approach, which emphasized targets important to patients - psychosocial functioning, quality of life, and recovery...
2017: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/28716608/opioidergic-and-dopaminergic-modulation-of-cost-benefit-decision-making-in-long-evans-rats
#2
Ileana Morales, Paul J Currie, Timothy D Hackenberg, Raúl Pastor
Eating disorders are associated with impaired decision-making and dysfunctional reward-related neurochemistry. The present study examined the potential contributions of dopamine and opioid signaling to these processes using two different decision-making tasks. In one task, Long Evans Rats chose between working for a preferred food (high-carbohydrate banana-flavored sucrose pellets) by lever pressing on a progressive-ratio schedule of reinforcement vs. obtaining less preferred laboratory chow that was concurrently available...
July 14, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28716589/the-role-of-dopamine-d2-receptors-in-the-nucleus-accumbens-during-taste-aversive-learning-and-memory-extinction-after-long-term-sugar-consumption
#3
María Isabel Miranda, José Alejandro Rangel-Hernández, Gabriela Vera-Rivera, Nadia Edith García-Medina, Gerardo Soto-Alonso, Gabriela Rodríguez-García, Luis Núñez-Jaramillo
The nucleus accumbens (NAcc) is a forebrain region that may significantly contribute to the integration of taste and visceral signals during food consumption. Changes in dopamine release in the NAcc have been observed during consumption of a sweet taste and during compulsive consumption of dietary sugars, suggesting that NAcc dopaminergic transmission is strongly correlated with taste familiarity and the hedonic value content. NAcc core and shell nuclei are differentially involved during and after sugar exposure and, particularly, previous evidence suggests that dopamine D2 receptors could be related with the strength of the latent inhibition (LI) of conditioned taste aversion (CTA), which depends on the length of the taste stimulus pre-exposure...
July 14, 2017: Neuroscience
https://www.readbyqxmd.com/read/28712880/the-role-of-oxidative-stress-in-antipsychotics-induced-ovarian-toxicity
#4
Ekramy Elmorsy, Ayat Al-Ghafari, Amal Misbah Aggour, Raheela Khan, Saad Amer
This study tested the hypothesis that oxidative stress could be an underlying mechanism for APs-induced ovarian cytotoxicity and reproductive dysfunction. Rat ovarian theca interstitial cells (TICs) were isolated and treated with four APs [chlorpromazine (CPZ), haloperidol (HAL), risperidone (RIS) and clozapine (CLZ)]. MTT assay was used to test the effects of these antipsychotics on TICs viability and to estimate their 50% inhibitory concentrations (IC50s). The effects of APs (IC50s and 1μM concentrations) on the activities of caspases-3, -8 and -9, reactive oxygen species (ROS) production, total intracellular glutathione and lipid peroxidation (LPO) in TICs were assessed...
July 13, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28710881/an-ethanolic-extract-of-desmodium-adscendens-exhibits-antipsychotic-like-activity-in-mice
#5
Patrick Amoateng, Samuel Adjei, Dorcas Osei-Safo, Kennedy K E Kukuia, Thomas K Karikari, Alexander K Nyarko
BACKGROUND: Desmodium adscendens extract (DAE) is used traditionally in Ghana for the management of psychosis. The present study aimed at providing pharmacological evidence for its ethnomedical use by testing the hypothesis that an ethanolic extract of Desmodium adscendens may possess antipsychotic properties. METHODS: The primary behavioral effects of DAE on the central nervous system of mice were investigated using Irwin's test paradigm. Novelty-induced and apomorphine-induced locomotor and rearing behaviors in mice were explored in an open-field observational test system...
July 15, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28710219/comparison-of-propofol-and-dexmedetomidine-infused-overnight-to-treat-hyperactive-and-mixed-icu-delirium-a-protocol-for-the-basel-prodex-clinical-trial
#6
Alexa Hollinger, Katrin Ledergerber, Stefanie von Felten, Raoul Sutter, Stephan Rüegg, Lukas Gantner, Sibylle Zimmermann, Andrea Blum, Luzius A Steiner, Stephan Marsch, Martin Siegemund
BACKGROUND/OBJECTIVES: Delirium is a neurobehavioural disturbance that frequently develops particularly in the intensive care unit (ICU) population. It was first described more than half a century ago, where it was already discovered as a state that might come along with serious complications such as prolonged ICU and hospital stay, reduced quality of life and increased mortality. However, in most cases, there is still lack of proof for causal relationship. Its presence frequently remains unrecognised due to suggested predominance of the hypoactive form...
July 13, 2017: BMJ Open
https://www.readbyqxmd.com/read/28705742/an-acute-oral-intoxication-with-haloperidol-decanoate-a-case-report
#7
Bart G J Dekkers, Ruben J Eck, Jan C Ter Maaten, Daniël J Touw
Haloperidol decanoate is a typical antipsychotic drug used as maintenance therapy for schizophrenia and mood disorders formulated as an ester for intramuscular injection. Cases of oral haloperidol decanoate intoxications have not been described in literature. In this report, we present for the first time a case of an oral ingestion of haloperidol decanoate of a young woman who presented to the emergency department following an intentional oral ingestion of 1 ampoule of haloperidol decanoate 100mg. At presentation, she had a bilateral rest tremor of both hands and mild hypothermia...
July 5, 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28704276/effects-of-d1-and-d2-receptor-antagonists-on-the-discriminative-stimulus-effects-of-methylendioxypyrovalerone-and-mephedrone-in-male-sprague-dawley-rats-trained-to-discriminate-d-amphetamine
#8
Eric L Harvey, Rachel L Burroughs, Lisa E Baker
Psychopharmacology research has amassed substantial evidence for similarities between synthetic cathinones and other commonly abused psychostimulants. Few studies have utilized drug discrimination methods to investigate synthetic cathinones, and the precise neurochemical substrates underlying their interoceptive effects have not been examined. The present study assessed the involvement of D1 and D2 dopaminergic receptors in the stimulus effects of 3,4-methylenedioxypyrovalerone (MDPV) and mephedrone (MEPH) in rats trained to discriminate D-amphetamine...
July 12, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28698031/comparable-impediment-of-cognitive-function-in-female-and-male-rats-subsequent-to-daily-administration-of-haloperidol-after-traumatic-brain-injury
#9
Kristin E Free, Anna M Greene, Corina O Bondi, Naima Lajud, Patricia B de la Tremblaye, Anthony E Kline
Antipsychotic drugs, such as haloperidol (HAL), are prescribed in the clinic to manage traumatic brain injury (TBI)-induced agitation. While preclinical studies have consistently shown that once-daily administration of HAL hinders functional recovery after TBI in male rats, its effects in females are unknown. Hence, the objective of this study was to directly compare neurobehavioral and histological outcomes in both sexes to determine whether the reported deleterious effects of HAL extend to females. Anesthetized adult female and male rats received either a controlled cortical impact (CCI) or sham injury and then were randomly assigned to a dosing regimen of HAL (0...
July 8, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28697832/-efficacy-of-clonidine-transdermal-patch-in-treatment-of-moderate-to-severe-tic-disorders-in-children
#10
Jing-Min Guo, Xiao-Xi Shi, Shi-Wei Yang, Qin-Fang Qian, Yan Huang, Yan-Qin Xie, Ping Ou
OBJECTIVE: To investigate the difference in the efficacy between clonidine transdermal patch and haloperidol tablets in the treatment of moderate to severe tic disorders in children. METHODS: A total of 134 children with moderate to severe tic disorders were randomly divided into clonidine group (n=70) and haloperidol group (n=64). The clonidine and haloperidol groups were treated with clonidine transdermal patch and haloperidol tablets respectively, and the treatment lasted for 8 weeks in both groups...
July 2017: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/28681176/population-pharmacokinetics-of-haloperidol-in-terminally-ill-adult-patients
#11
L G Franken, R A A Mathot, A D Masman, F P M Baar, D Tibboel, T van Gelder, B C P Koch, B C M de Winter
PURPOSE: Over 80% of the terminally ill patients experience delirium in their final days. In the treatment of delirium, haloperidol is the drug of choice. Very little is known about the pharmacokinetics of haloperidol in this patient population. We therefore designed a population pharmacokinetic study to gain more insight into the pharmacokinetics of haloperidol in terminally ill patients and to find clinically relevant covariates that may be used in developing an individualised dosing regimen...
July 5, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28675258/narcolepsy-cataplexy-and-psychosis-a-case-study
#12
F Canellas-Dols, C Delgado, C Arango-Lopez, R Peraita-Adrados
AIMS: To report a challenging patient a girl who developed narcolepsyy with cataplexy (NT1) and a psychosis during adolescence. To discuss diagnostic and therapeutic challenges of the comorbid cases. CASE REPORT: A 14-year-old girl was referred to Sleep and Epilepsy Unit for excessive daytime sleepiness, impaired nocturnal sleep, binge eating and weight gain, over the last year. After being diagnosed with a NT1 the patient was treated with modafinil and sodium oxybate...
July 16, 2017: Revista de Neurologia
https://www.readbyqxmd.com/read/28674870/heart-rate-response-to-alpha2-adrenergic-receptor-antagonism-by-antipsychotics
#13
David D Kim, Donna J Lang, Darren E R Warburton, Melissa L Woodward, Randall F White, Alasdair M Barr, William G Honer, Ric M Procyshyn
PURPOSE: To explore the relationship between antipsychotic-associated antagonism of alpha2-adrenergic receptors and resting heart rate in individuals with schizophrenia. METHODS: Thirty-one inpatients treated with antipsychotics were included in this exploratory analysis. Antipsychotic doses were converted to haloperidol equivalents for alpha2-adrenergic receptor antagonism. Resting heart rate was measured with the patient in the seated upright posture. RESULTS: After controlling for confounding variables, the relationship between alpha2-adrenergic receptor antagonism and resting heart rate demonstrated a positive linear effect (P = 0...
July 3, 2017: Clinical Autonomic Research: Official Journal of the Clinical Autonomic Research Society
https://www.readbyqxmd.com/read/28674852/effects-of-long-term-treatment-with-haloperidol-clozapine-and-aripiprazole-on-mice-isolated-vas-deferens
#14
Mehmet Hanifi Tanyeri, Mehmet Emin Buyukokuroglu, Pelin Tanyeri, Oguz Mutlu, Füruzan Yildiz Akar, Güner Ulak, Bekir Faruk Erden
PURPOSE: Sexual dysfunction is a common condition in patients taking antipsychotics and is the most bothersome symptom and adverse drug effect, resulting in a negative effect on treatment compliance. Pharmacology research into human ejeculatory disorders is limited to clinical studies with registered drugs affecting the ejaculation process; therefore, animal research has become the need. We aimed to investigate the effects of haloperidol, clozapine and aripiprazole on serotonin, noradrenaline, adenosine triphosphate (ATP) and potassium chloride (KCl)-induced contractions of the vas deferens in order to evaluate the effect of haloperidol, clozapine and aripiprazole on the contraction of the vas deferens...
July 3, 2017: International Urology and Nephrology
https://www.readbyqxmd.com/read/28671605/glycine-binding-site-stimulants-of-nmda-receptors-alleviate-extrapyramidal-motor-disorders-by-activating-the-nigrostriatal-dopaminergic-pathway
#15
Saki Shimizu, Shunsaku Sogabe, Ryoto Yanagisako, Akiyoshi Inada, Megumi Yamanaka, Higor A Iha, Yukihiro Ohno
Dysfunction of the N-methyl-d-aspartate (NMDA) receptor has been implicated in the pathogenesis of schizophrenia. Although agonists for the glycine-binding sites of NMDA receptors have potential as new medication for schizophrenia, their modulation of antipsychotic-induced extrapyramidal side effects (EPS) has not yet been clarified. We herein evaluated the effects of glycine-binding site stimulants of NMDA receptors on antipsychotic-induced EPS in mice and rats. d-cycloserine (DCS) and d-serine significantly improved haloperidol (HAL)-induced bradykinesia in mice, whereas glycine showed no effects...
July 3, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28666858/potent-haloperidol-derivatives-covalently-binding-to-the-dopamine-d2-receptor
#16
Tobias Schwalbe, Jonas Kaindl, Harald Hübner, Peter Gmeiner
The dopamine D2 receptor (D2R) is a common drug target for the treatment of a variety of neurological disorders including schizophrenia. Structure based design of subtype selective D2R antagonists requires high resolution crystal structures of the receptor and pharmacological tools promoting a better understanding of the protein-ligand interactions. Recently, we reported the development of a chemically activated dopamine derivative (FAUC150) designed to covalently bind the L94C mutant of the dopamine D2 receptor...
June 20, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28654186/haloperidol-decreases-hyperalgesia-and-allodynia-induced-by-chronic-constriction-injury
#17
Josué Vidal Espinosa-Juárez, Osmar Antonio Jaramillo-Morales, Francisco Javier López-Muñoz
Neuropathic pain has proven to be a difficult condition to treat, so investigational therapy has been sought that may prove useful, such as the use of sigma-1 antagonists. Haloperidol (HAL) is a compound that shows a high affinity with these receptors, acting as an antagonist. Therefore, the objective of this study was to demonstrate its effect in an experimental model of neuropathic pain and corroborate its antagonistic action of the sigma-1 receptors under these conditions. BD-1063 was used as a sigma-1 antagonist control and gabapentin was used as a positive control...
June 27, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28651936/efficacy-safety-and-tolerability-of-aripiprazole-in-bipolar-disorder-an-updated-systematic-review-and-meta-analysis-of-randomized-controlled-trials
#18
Dian-Jeng Li, Ping-Tao Tseng, Brendon Stubbs, Che-Sheng Chu, Han-Yung Chang, Eduard Vieta, Michele Fornaro, Andre F Carvalho, Marco Solmi, Nicola Veronese, Tien-Yu Chen, Yen-Wen Chen, Pao-Yen Lin, Philip Chik-Keung Chow
Numerous studies have investigated aripiprazole as a treatment for bipolar disorder (BD). therefore we conducted this comprehensive meta-analysis to investigate the efficacy and safety profile of aripiprazole in treating BD. Two authors conducted systematic searches of PubMed and ScienceDirect from inception until May 14th, 2017. Randomized controlled trials (RCTs) of people with BD who received aripiprazole were included. A total of 20 RCTs met the eligibility criteria, including two which investigated the efficacy of aripiprazole versus haloperidol (aripiprazole=340; haloperidol=337), three which compared aripiprazole versus lithium (aripiprazole=208; lithium=212), and 15 with multiple comparisons of aripiprazole versus a placebo (aripiprazole=1923; placebo=1499)...
June 23, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28646590/randomized-controlled-double-blind-trial-comparing-haloperidol-combined-with-conventional-therapy-to-conventional-therapy-alone-in-patients-with-symptomatic-gastroparesis
#19
Carlos J Roldan, Kimberly A Chambers, Linda Paniagua, Sonali Patel, Marylou Cardenas-Turanzas, Yashwant Chathampally
OBJECTIVE: Gastroparesis is a debilitating condition that causes nausea, vomiting, and abdominal pain. Management includes analgesics and antiemetics, but symptoms are often refractory. Haloperidol has been utilized in the palliative care setting for similar symptoms. The study objective was to determine whether haloperidol as an adjunct to conventional therapy would improve symptoms in gastroparesis patients presenting to the emergency department. METHODS AND TRIAL DESIGN: This was a randomized, double-blind, placebo-controlled trial of adult emergency department patients with acute exacerbation of previously diagnosed gastroparesis...
June 24, 2017: Academic Emergency Medicine: Official Journal of the Society for Academic Emergency Medicine
https://www.readbyqxmd.com/read/28643331/treatment-with-antipsychotics-in-pregnancy-changes-in-drug-disposition
#20
Andreas Austgulen Westin, Malin Brekke, Espen Molden, Eirik Skogvoll, Ingrid Castberg, Olav Spigset
Although pregnancy is known to cause changes in drug pharmacokinetics, little is known about its impact on serum levels of antipsychotics. In this study, we retrospectively assessed 201 routine serum antipsychotic therapeutic drug monitoring concentration measurements obtained from a total of 110 pregnancies in 103 women, and 512 measurements from the same women before and after pregnancy. Serum concentrations in the third trimester were significantly lower than baseline for quetiapine (-76%; CI, -83%, -66%; p<0...
June 23, 2017: Clinical Pharmacology and Therapeutics
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