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prolactin antipsychotic

Kazunori Suzuki, Akina Harada, Hirobumi Suzuki, Clizia Capuani, Annarosa Ugolini, Mauro Corsi, Haruhide Kimura
Activation of indirect pathway medium spiny neurons (MSNs) via promotion of cAMP production is the principal mechanism of action of current antipsychotics with dopamine D2 receptor antagonism. TAK-063 [1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one] is a novel phosphodiesterase 10A inhibitor that activates both direct and indirect pathway MSNs through increasing both cAMP and cGMP levels by inhibition of their degradation. The activation of indirect pathway MSNs through the distinct mechanism of action of these drugs raises the possibility of augmented pharmacological effects by combination therapy...
February 2018: Pharmacology Research & Perspectives
Baris Olten, Michael H Bloch
Our objective was to examine the association between antipsychotic receptor binding profiles and the magnitude of common side-effects. We used regression analysis to examine the association between the receptor binding affinities of antipsychotic agents (log Ki) and degree of specific antipsychotic side-effects. Data on magnitude of weight gain, prolactin increase and QTc prolongation (in Standardized Mean Difference) and risk of sedation and extrapyramidal symptoms (in Odds Ratio) between individual antipsychotic medications as compared to placebo was based on a recent network meta-analysis examining the treatment of schizophrenia...
February 1, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
Dhanya Raveendranthan, Naren P Rao, Mukund G Rao, Ajish G Mangot, Shivaram Varambally, Muralidharan Kesavan, Ganesan Venkatasubramanian, Bangalore N Gangadhar
Background: Antipsychotic treatment-induced hyperprolactinemia is a highly distressing and disabling side effect for patients. The use of add-on aripiprazole has been identified as a possible treatment strategy in this situation. However, data on prolactin changes with add-on aripiprazole in a real-world naturalistic clinical setting from India are sparse. Materials and Methods: The retrospective chart review was conducted at the specialty metabolic clinic at the National Institute of Mental Health and Neurosciences, Bengaluru, India...
January 2018: Indian Journal of Psychological Medicine
Hugo Geerts, Athan Spiros, Patrick Roberts, Larry Alphs
Long-acting injectable (LAI) antipsychotic formulations are increasingly used for improving patient compliance and long-term outcomes. Transitioning to LAIs raises questions regarding how optimum efficacy can be rapidly achieved while minimizing potential efficacy and safety concerns related to overlapping plasma levels of prior treatments and the new LAI. Ideally, randomized clinical trials would provide guidance regarding transition algorithms, but the number of studies and sample size required to address relevant questions makes this approach unachievable...
January 25, 2018: Schizophrenia Research
Robin Emsley, Sanja Kilian
The course of schizophrenia is characterized by multiple relapses, incomplete remission of symptoms, enduring cognitive deficits, and social and occupational functional impairments. Nonadherence to antipsychotic medication is a major determinant of this poor outcome. Long-acting injectable antipsychotics were developed specifically to address the nonadherence problem and are increasingly considered as an early treatment option, in an attempt to prevent accruing morbidity. This review focuses on paliperidone palmitate, the long-acting injectable (LAI) formulation of paliperidone...
2018: Neuropsychiatric Disease and Treatment
Błażej Misiak, Dorota Frydecka, Olga Loska, Ahmed A Moustafa, Jerzy Samochowiec, Justyna Kasznia, Bartłomiej Stańczykiewicz
Neuroactive steroids, including testosterone, dehydroepiandrosterone (DHEA) and its sulfate (DHEA-S) might play an important role in the pathophysiology of schizophrenia. Therefore, we performed a systematic review and meta-analysis of studies comparing the levels of testosterone, DHEA and DHEA-S in patients with schizophrenia and healthy controls. We searched electronic databases from their inception until Oct 29, 2017. Effect size (ES) estimates were calculated as Hedges' g. Data analysis was performed using random-effects models...
January 9, 2018: Psychoneuroendocrinology
Fahad D Alosaimi, Ebtihaj O Fallata, Mohammed Abalhassan, Abdulhadi Alhabbad, Nasser Alzain, Bandar Alhaddad, Mohammed Z Alassiry
OBJECTIVES: Hyperprolactinemia is a common adverse event associated with psychotropic medications (mainly antipsychotics) used in the management of schizophrenia and bipolar disorders. The aim of this study was to estimate the prevalence of hyperprolactinemia in psychiatric patients and to evaluate its association with various psychiatric diagnoses and the use of various psychotropic medications. METHODS: A cross-sectional observational study was conducted between July 2012 and June 2014...
January 15, 2018: International Journal of Psychiatry in Clinical Practice
Min Jhon, Taeyoung Yoo, Ju-Yeon Lee, Seon-Young Kim, Jae-Min Kim, Il-Seon Shin, Lana Williams, Michael Berk, Jin-Sang Yoon, Sung-Wan Kim
OBJECTIVE: This study examined clinical and gender-specific risk factors for low bone mineral density (BMD) in adult patients with psychotic disorders. METHODS: The study included 285 community-dwelling patients with psychotic disorders. Dual-energy X-ray absorptiometry was used to measure BMD. Clinical characteristics associated with low BMD were identified with logistic regression analysis in total population and each gender. RESULTS: Fifty-eight (20...
January 8, 2018: Human Psychopharmacology
Robert Krysiak, Witold Szkróbka, Bogusław Okopień
Metformin was found to reduce elevated serum thyrotropin levels, and this effect was partially determined by endogenous dopaminergic tone. The aim of this study was to compare the effect of metformin treatment on hypothalamic-pituitary-thyroid axis activity in elderly women with subclinical hypothyroidism treated with antipsychotic agents and not receiving this drug. The study population consisted of 34 elderly women with subclinical hypothyroidism, 16 of whom received antipsychotic drugs. Because of coexistent type 2 diabetes, these women were treated with metformin (2...
December 18, 2017: Journal of Clinical Pharmacology
Itziar Montalvo, Roser Nadal, Antonio Armario, Alfonso Gutiérrez-Zotes, Marta Creus, Ángel Cabezas, Montse Solé, Maria José Algora, Vanessa Sánchez-Gistau, Elisabet Vilella, Javier Labad
INTRODUCTION: Hyperprolactinaemia is commonly observed in people with psychotic disorders due to D2 receptor blockade by antipsychotic drugs, although it may also exist in drug-naïve patients with first-episode psychosis. Recent studies suggest that hyperprolactinaemia may have a negative impact on cognitive function in people with early psychosis. We aimed to explore whether there are sex differences in the association between prolactin levels and cognitive performance in early psychosis patients...
December 1, 2017: Australian and New Zealand Journal of Psychiatry
Amit Taneja, An Vermeulen, Dymphy R H Huntjens, Meindert Danhof, Elizabeth C M De Lange, Johannes H Proost
Prolactin release is a side effect of antipsychotic therapy with dopamine antagonists, observed in rats as well as humans. We examined whether two semimechanistic models could describe prolactin response in rats and subsequently be translated to predict pituitary dopamine D2 receptor occupancy and plasma prolactin concentrations in humans following administration of paliperidone or remoxipride. Data on male Wistar rats receiving single or multiple doses of risperidone, paliperidone, or remoxipride was described by two semimechanistic models, the precursor pool model and the agonist-antagonist interaction model...
December 2017: Pharmacology Research & Perspectives
Eiji Kirino
Objectives: Antipsychotics, even atypical ones, can induce hyperprolactinemia. Aripiprazole (APZ), a dopamine D2 partial agonist, has a unique pharmacological profile and few side effects. We investigated the incidence of hyperprolactinemia in patients with schizophrenia treated with APZ and other antipsychotics. Methods: Serum prolactin levels were measured by ELISA (enzyme-linked immunosorbent assay). A questionnaire survey was used to evaluate subjective sexual dysfunction...
2017: Annals of General Psychiatry
Chadi A Calarge, James A Mills, Ekhard E Ziegler, Janet A Schlechte
BACKGROUND: The chronic use of antipsychotics has been associated with impaired bone mineralization, partially mediated by hyperprolactinemia. We examined if calcium and vitamin D supplementation promote bone mineral accrual in boys with risperidone-induced hyperprolactinemia. METHODS: Between February 2009 and November 2013, medically healthy, 5- to 17-year-old boys were enrolled in a 36-week double-blind, placebo-controlled study, examining the skeletal effects of supplementation with 1250 mg calcium carbonate and 400 IU of vitamin D3 in risperidone-induced hyperprolactinemia...
November 7, 2017: Journal of Child and Adolescent Psychopharmacology
Manli Huang, Liang Yu, Fen Pan, Shaojia Lu, Shaohua Hu, Jianbo Hu, Jinkai Chen, Pingbo Jin, Hongli Qi, Yi Xu
BACKGROUND: This study was conducted to evaluate the efficacy and metabolic effects of paliperidone palmitate (PP) injections against oral olanzapine in first-episode schizophrenia (FES) patients. METHODS: Eligible patients were randomized to receive PP or olanzapine. Efficacy assessments and weight-related parameters were assessed at baseline, weeks 1, 5, 9, and endpoint or at early withdrawal. Lipid, glucose, insulin and prolactin were evaluated at baseline and endpoint or at early withdrawal...
October 31, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
Han-Yung Chang, Ping-Tao Tseng, Brendon Stubbs, Che-Sheng Chu, Dian-Jeng Li, Michele Fornaro, Andre Carvalho, Marco Solmi, Nicola Veronese, Eduard Vieta, Tien-Yu Chen, Yen-Wen Chen, Pao-Yen Lin, Philip Chik-Keung Chow
Paliperidone may be effective for the treatment of bipolar disorder (BD); however, the evidence has been mixed. This is the first meta-analysis to evaluate the efficacy, safety, and tolerability of paliperidone for the treatment of BD. We performed a systematic search of the literature using major electronic databases from inception to January 27, 2017. Randomized control trials (RCTs) investigating paliperidone treatment among patients with BD versus a placebo or other second-generation antipsychotics were included...
October 2017: Experimental and Clinical Psychopharmacology
Judy Hope, David Castle, Nicholas A Keks
OBJECTIVES: Brexpiprazole is a new dopamine partial agonist antipsychotic in the same class as aripiprazole. This paper will briefly review brexpiprazole and compare it with aripiprazole. CONCLUSIONS: Brexpiprazole and aripiprazole are both partial agonists at dopamine D2, and serotonin 5-HT1A and antagonists at serotonin 5-HT2A and noradrenergic α1B receptors. However, the two drugs are significantly different in potencies at various receptors; neurochemical profiles predict that brexpiprazole may be comparable with aripiprazole in its antipsychotic efficacy but may cause less akathisia, extrapyramidal side effects (EPS) and activation...
October 1, 2017: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
Emilia Tarland, Robert T Franke, Heidrun Fink, Heinz H Pertz, Jan Brosda
RATIONALE: 2-Bromoterguride, a dopamine D2 receptor partial agonist with antagonist properties at serotonin 5-HT2A receptors and α2C-adrenoceptors, meets the prerequisites of a putative atypical antipsychotic drug (APD). We recently showed that 2-bromoterguride is effective in tests of positive symptoms of schizophrenia in rats without inducing extrapyramidal side effects or metabolic changes. OBJECTIVE: In continuation of our recent work, we now investigated the effect of 2-bromoterguride on apomorphine and phencyclidine (PCP)-induced disruptions of prepulse inhibition (PPI) of the acoustic startle response, a measure of sensory gating...
October 3, 2017: Psychopharmacology
David A Sykes, Holly Moore, Lisa Stott, Nicholas Holliday, Jonathan A Javitch, J Robert Lane, Steven J Charlton
Atypical antipsychotic drugs (APDs) have been hypothesized to show reduced extrapyramidal side effects (EPS) due to their rapid dissociation from the dopamine D2 receptor. However, support for this hypothesis is limited to a relatively small number of observations made across several decades and under different experimental conditions. Here we show that association rates, but not dissociation rates, correlate with EPS. We measured the kinetic binding properties of a series of typical and atypical APDs in a novel time-resolved fluorescence resonance energy transfer assay, and correlated these properties with their EPS and prolactin-elevating liabilities at therapeutic doses...
October 2, 2017: Nature Communications
Kenshi Takechi, Yurika Yoshioka, Hitoshi Kawazoe, Mamoru Tanaka, Shingo Takatori, Miwako Kobayashi, Ichiro Matsuoka, Hiroaki Yanagawa, Yoshito Zamami, Masaki Imanishi, Keisuke Ishizawa, Akihiro Tanaka, Hiroaki Araki
Treatment with antipsychotic drugs has been associated with hyperprolactinemia. The same antipsychotic drugs have also been associated with side effects such as menstruation disorders. The aim of this study was to evaluate the prevalence of hyperprolactinemia and menstruation disorders in women undergoing antipsychotic treatment. We performed a retrospective chart review study of psychiatric patients who underwent laboratory testing for serum prolactin (PRL) level between March 2011 and March 2015 in Ehime University Hospital...
2017: Biological & Pharmaceutical Bulletin
Simon S Evers, Gretha J Boersma, Kellie Lk Tamashiro, Anton Jw Scheurink, Gertjan van Dijk
Olanzapine, an antipsychotic agent mainly used for treating schizophrenia, is frequently associated with body weight gain and diabetes mellitus. Nonetheless, studies have shown that not every individual is equally susceptible to olanzapine's weight-gaining effect. Therefore, Roman high and low avoidance rat strains were examined on their responsiveness to olanzapine treatment. The Roman high avoidance rat shares many behavioral and physiological characteristics with human schizophrenia, such as increased central dopaminergic sensitivity, whereas the Roman low avoidance rat has been shown to be prone to diet-induced obesity and insulin resistance...
August 1, 2017: Journal of Psychopharmacology
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