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Haloperidol

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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
#1
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
#2
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
https://www.readbyqxmd.com/read/28641484/protective-effect-of-hesperetin-against-haloperidol-induced-orofacial-dyskinesia-and-catalepsy-in-rats
#3
Dinesh Dhingra, Shikha Goswami, Nidhi Gahalain
OBJECTIVES: The present study was designed to evaluate the effect of hesperetin on haloperidol-induced orofacial dyskinesia and catalepsy in Wistar male albino rats. METHODS: Haloperidol (1 mg/kg, ip) was administered for 21 successive days to induce orofacial dyskinesia and catalepsy. Hesperetin (50 and 100 mg/kg, po) was administered 10 min prior to the injection of haloperidol for 21 successive days. Vacuous chewing movements (VCMs), tongue protrusions, catalepsy, and locomotor activity scores were recorded on 7th, 14th, and 22nd day of drug treatment...
June 22, 2017: Nutritional Neuroscience
https://www.readbyqxmd.com/read/28636569/diabetic-ketoacidosis-associated-with-antipsychotic-drugs-case-reports-and-a-review-of-literature
#4
Antonia Vuk, Martina Rojnic Kuzman, Maja Baretic, Martina Matovinovic Osvatic
BACKGROUND: Second generation antipsychotics (SGAs) are associated with metabolic disturbances. Diabetic ketoacidosis (DKA) is a rare, but potentially fatal sign of acute glucose metabolism dysregulation linked to the use of SGAs. The aims of this article are to present patients with a history of psychotic disorders and of severe metabolic diabetic ketoacidosis, possibly associated with the use of antipsychotics, and to review the current literature on the topic of antipsychotic-induced DKA...
June 2017: Psychiatria Danubina
https://www.readbyqxmd.com/read/28629145/synthesis-and-evaluation-of-phenylxanthine-derivatives-as-potential-dual-a2ar-antagonists-mao-b-inhibitors-for-parkinson-s-disease
#5
Xuebao Wang, Chao Han, Yong Xu, Kaiqi Wu, Shuangya Chen, Mangsha Hu, Luyao Wang, Yun Ye, Faqing Ye
The aim of this research was to prove the speculation that phenylxanthine (PX) derivatives possess adenosine A2A receptor (A2AR)-blocking properties and to screening and evaluate these PX derivatives as dual A2AR antagonists/MAO-B inhibitors for Parkinson's disease. To explore this hypothesis, two series of PX derivatives were prepared and their antagonism against A2AR and inhibition against MAO-B were determined in vitro. In order to evaluate further the antiparkinsonian properties, pharmacokinetic and haloperidol-induced catalepsy experiments were carried out in vivo...
June 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28627267/%C3%AE-cyclodextrin-based-ternary-complexes-of-haloperidol-and-organic-acids-the-effect-of-organic-acids-on-the-drug-solubility-enhancement
#6
Prisada Rakkaew, Jiraphong Suksiriworapong, Doungdaw Chantasart
Haloperidol (HALO) is a weak base with very low aqueous solubility that is used as an antipsychotic drug. This study aimed to improve its solubility by forming HALO/β-cyclodextrin (β-CD) based ternary complexes with organic acids. The solubility of HALO/β-CD binary and HALO/β-CD/organic acid ternary complexes in different media (i.e., citrate buffer pH 3 and 6) was explored. The stoichiometric ratio between the drug and β-CD was 1:1 in all complexes formed. The solubility of HALO/β-CD binary complexes significantly increased in citrate buffer pH 3 compared to citrate buffer pH 6...
June 19, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28619471/oral-haloperidol-or-olanzapine-intake-produces-distinct-and-region-specific-increase-in-cannabinoid-receptor-levels-that-is-prevented-by-high-fat-diet
#7
Foteini Delis, Lauren Rosko, Aditya Schroff, Kenneth E Leonard, Panayotis K Thanos
Clinical studies show higher levels of cannabinoid CB1 receptors (CB1R) in the brain of schizophrenic patients while preclinical studies report a significant functional interaction between dopamine D2 receptors and CB1Rs as well as an upregulation of CB1Rs after antipsychotic treatment. These findings prompted us to study the effects of chronic oral intake of a first and a second generation antipsychotic, haloperidol and olanzapine, on the levels and distribution of CB1Rs in the rat brain. Rats consumed either regular chow or high-fat food and drank water, haloperidol drinking solution (1...
June 12, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28614404/treatment-continuation-of-four-long-acting-antipsychotic-medications-in-the-netherlands-and-belgium-a-retrospective-database-study
#8
Flore Decuypere, Jan Sermon, Paul Geerts, Tom R Denee, Cedric De Vos, Bart Malfait, Mark Lamotte, Cornelis L Mulder
Achieving greater continuation of treatment is a key element to improve treatment outcomes in schizophrenia patients. However, reported treatment continuation can differ markedly depending on the study design. In a retrospective setting, treatment continuation remains overall poor among patients using antipsychotics. This study aimed to document the difference in treatment continuation between four long-acting injectable antipsychotics based on the QuintilesIMS LRx databases, national, longitudinal, panel based prescription databases of retail pharmacies, in the Netherlands and Belgium...
2017: PloS One
https://www.readbyqxmd.com/read/28612134/ketamine-induced-behavioural-and-brain-oxidative-changes-in-mice-an-assessment-of-possible-beneficial-effects-of-zinc-as-mono-or-adjunct-therapy
#9
Olakunle James Onaolapo, Olayemi Quyyom Ademakinwa, Temitayo Opeyemi Olalekan, Adejoke Yetunde Onaolapo
RATIONALE: We studied the influence of zinc, haloperidol or olanzapine on neurobehaviour (open-field, radial arm maze and elevated plus maze) and brain antioxidant status in vehicle- or ketamine-treated mice, with the aim of ascertaining the potentials of zinc in counteracting ketamine's effects. OBJECTIVES: Experiment 1 assessed the effects of zinc in healthy animals and the relative degrees of modulation of ketamine's effects by zinc, haloperidol or olanzapine, respectively...
June 14, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28611376/allopregnanolone-mediates-the-exacerbation-of-tourette-like-responses-by-acute-stress-in-mouse-models
#10
Laura J Mosher, Sean C Godar, Marianela Nelson, Stephen C Fowler, Graziano Pinna, Marco Bortolato
Tourette syndrome (TS) is a neuropsychiatric disorder characterized by multiple tics and sensorimotor abnormalities, the severity of which is typically increased by stress. The neurobiological underpinnings of this exacerbation, however, remain elusive. We recently reported that spatial confinement (SC), a moderate environmental stressor, increases tic-like responses and elicits TS-like sensorimotor gating deficits in the D1CT-7 mouse, one of the best-validated models of TS. Here, we hypothesized that these adverse effects may be mediated by neurosteroids, given their well-documented role in stress-response orchestration...
June 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28601965/event-related-potentials-reflect-impaired-temporal-interval-learning-following-haloperidol-administration
#11
Sarah E Forster, Patrick Zirnheld, Anantha Shekhar, Stuart R Steinhauer, Brian F O'Donnell, William P Hetrick
BACKGROUND: Signals carried by the mesencephalic dopamine system and conveyed to anterior cingulate cortex are critically implicated in probabilistic reward learning and performance monitoring. A common evaluative mechanism purportedly subserves both functions, giving rise to homologous medial frontal negativities in feedback- and response-locked event-related brain potentials (the feedback-related negativity (FRN) and the error-related negativity (ERN), respectively), reflecting dopamine-dependent prediction error signals to unexpectedly negative events...
June 10, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28589693/antipsychotic-prescription-and-mortality-in-hospitalized-older-persons
#12
Deborah Chiesa, Alessandra Marengoni, Alessandro Nobili, Mauro Tettamanti, Luca Pasina, Carlotta Franchi, Codjo D Djade, Salvatore Corrao, Francesco Salerno, Maura Marcucci, Giuseppe Romanelli, Pier Mannuccio Mannucci
BACKGROUND: Recent scientific reports have shown that older persons treated with antipsychotics for dementia-related behavioural symptoms have increased mortality. However, the impact of these drugs prescribed during hospitalization has rarely been assessed. We aimed to investigate whether antipsychotics are associated with an increased risk of mortality during hospitalization and at 3-month follow-up in elderly inpatients. METHODS: We analyzed data gathered during two waves (2010 and 2012) by the REPOSI (Registro Politerapie Società Italiana Medicina Interna)...
June 6, 2017: Psychogeriatrics: the Official Journal of the Japanese Psychogeriatric Society
https://www.readbyqxmd.com/read/28587776/pharmacological-characterization-of-a-novel-potent-selective-and-orally-active-phosphodiesterase-2a-inhibitor-pdm-631
#13
Shunsuke Maehara, Keita Arakawa, Kotaro Hoshida, Hiroshi Nagasue, Noboru Chida, Kazunari Nakao, Shoji Furusako
Recently, we identified a novel phosphodiesterase 2A (PDE2A) inhibitor, PDM-631 ((S)-3-cyclopropyl-6-methyl-1-(1-(4-(trifluoromethoxy)phenyl)propan-2-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one). PDM-631 showed potent inhibitory activities for human and rat PDE2A with IC50 values of 1.5 and 4.2nM, respectively and more than 2000-fold selectivity against other phosphodiesterases. In rat studies, PDM-631 showed oral bioavailability and good brain penetration, and increased the cGMP levels in the cortex...
June 3, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28585931/the-modulation-of-adult-neuroplasticity-is-involved-in-the-mood-improving-actions-of-atypical-antipsychotics-in-an-animal-model-of-depression
#14
M Morais, P Patrício, A Mateus-Pinheiro, N D Alves, A R Machado-Santos, J S Correia, J Pereira, L Pinto, N Sousa, J M Bessa
Depression is a prevalent psychiatric disorder with an increasing impact in global public health. However, a large proportion of patients treated with currently available antidepressant drugs fail to achieve remission. Recently, antipsychotic drugs have received approval for the treatment of antidepressant-resistant forms of major depression. The modulation of adult neuroplasticity, namely hippocampal neurogenesis and neuronal remodeling, has been considered to have a key role in the therapeutic effects of antidepressants...
June 6, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28577995/equilibrium-solubility-measurement-of-compounds-with-low-dissolution-rate-by-higuchi-s-facilitated-dissolution-method-a-validation-study
#15
Krisztina Takács-Novák, Maria Urac, Péter Horváth, Gergely Völgyi, Bradley D Anderson, Alex Avdeef
Incubation time plays a critical role in the accurate measurement of equilibrium solubility of compounds. Substances which dissolve very slowly generally need long incubation times (days or weeks) to reach equilibrium. However, long times may pose several problems, such as decomposition of solute, molding of buffer, and drifting of pH. Higuchi in 1979 proposed the Facilitated Dissolution Method (FDM) to dramatically reduce incubation time. It employs a small volume of water-immiscible organic solvent to partly solubilize the sample and thereby increase the surface area available for dissolution...
May 31, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28567698/incidence-and-risk-factors-of-acute-akathisia-in-493-individuals-with-first-episode-non-affective-psychosis-a-6-week-randomised-study-of-antipsychotic-treatment
#16
Maria Juncal-Ruiz, Mariluz Ramirez-Bonilla, Jorge Gomez-Arnau, Victor Ortiz-Garcia de la Foz, Paula Suarez-Pinilla, Obdulia Martinez-Garcia, Karl David Neergaard, Rafael Tabares-Seisdedos, Benedicto Crespo-Facorro
INTRODUCTION: Acute akathisia is a neuropsychiatric syndrome with a negative effect on illness outcome. Its incidence in patients treated with antipsychotics has shown to be highly variable across studies. OBJECTIVES: Our goals were to investigate prevalence, risk factors for the development of acute akathisia, and differences in incidence between antipsychotics in a sample of 493 first episode non-affective psychosis patients. METHODS: This is a pooled analysis of three prospective, randomized, flexible-dose, and open-label clinical trials...
May 31, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28556305/hypothalamic-dopamine-is-required-for-salsolinol-induced-prolactin-secretion-in-goats
#17
Tsutomu Hashizume, Ryunosuke Watanabe, Yuki Inaba, Ken Sawai, Ferenc Fülöp, György Miklos Nagy
The aim of the present study was to clarify the relationship between hypothalamic dopamine (DA) and salsolinol (SAL) for the secretion of prolactin (PRL) in goats. SAL or thyrotropin-releasing hormone (TRH) was intravenously injected into female goats treated with or without the D2 DA receptor antagonist haloperidol (Hal), which crosses the blood-brain barrier, and the PRL-releasing response to SAL was compared with that to TRH. PRL-releasing responses to SAL, Hal, and Hal plus SAL were also examined after a pretreatment to augment central DA using carbidopa (Carbi) and L-dopa...
May 29, 2017: Animal Science Journal, Nihon Chikusan Gakkaihō
https://www.readbyqxmd.com/read/28555076/comparative-genomic-evidence-for-the-involvement-of-schizophrenia-risk-genes-in-antipsychotic-effects
#18
Y Kim, P Giusti-Rodriguez, J J Crowley, J Bryois, R J Nonneman, A K Ryan, C R Quackenbush, M D Iglesias-Ussel, P H Lee, W Sun, F P-M de Villena, P F Sullivan
Genome-wide association studies (GWAS) for schizophrenia have identified over 100 loci encoding >500 genes. It is unclear whether any of these genes, other than dopamine receptor D2, are immediately relevant to antipsychotic effects or represent novel antipsychotic targets. We applied an in vivo molecular approach to this question by performing RNA sequencing of brain tissue from mice chronically treated with the antipsychotic haloperidol or vehicle. We observed significant enrichments of haloperidol-regulated genes in schizophrenia GWAS loci and in schizophrenia-associated biological pathways...
May 30, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28554133/melatonin-attenuates-behavioural-deficits-and-reduces-brain-oxidative-stress-in-a-rodent-model-of-schizophrenia
#19
Adejoke Y Onaolapo, Olufemi A Aina, Olakunle James Onaolapo
Melatonin is a neurohormone that is linked to the aetiopathogenesis of schizophrenia. The aim of this study was to assess the potentials of oral melatonin supplement in the management of induced schizophrenia-like behavioural and brain oxidative status changes, using an animal model. The relative degrees of modulation of ketamine-induced behaviours by haloperidol, olanzapine or melatonin were assessed in the open-field, Y-maze, elevated plus maze and the social interaction tests. 12-week old, male mice were assigned to six groups of ten each (n=10)...
May 26, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28553116/comparative-efficacy-and-safety-of-antipsychotics-in-the-treatment-of-schizophrenia-a-network-meta-analysis-in-a-japanese-population
#20
Taro Kishi, Toshikazu Ikuta, Shinji Matsunaga, Yuki Matsuda, Kazuto Oya, Nakao Iwata
BACKGROUND: The relative efficacy and tolerability of antipsychotics for schizophrenia are considerably well studied. This study aimed to examine whether previous findings could be replicated in a genetically distinct and homogenous group (ie, Japanese patients with schizophrenia) and whether previous findings could be extended to a broader range of antipsychotics with previously unclear relative efficacy and tolerability. METHODS: Bayesian network meta-analysis was performed in which randomized trials comparing any of the following interventions were included: second-generation antipsychotics, haloperidol, or placebo...
2017: Neuropsychiatric Disease and Treatment
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