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Cariprazine

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https://www.readbyqxmd.com/read/29729086/the-novel-atypical-antipsychotic-cariprazine-demonstrates-dopamine-d-2-receptor-dependent-partial-agonist-actions-on-rat-mesencephalic-dopamine-neuronal-activity
#1
Sarah Delcourte, Charles R Ashby, Renaud Rovera, Béla Kiss, Nika Adham, Bence Farkas, Nasser Haddjeri
AIM: Cariprazine, a dopamine D3 -preferring D3 /D2 receptor partial agonist, is FDA approved for the treatment of schizophrenia and acute manic or mixed episodes of bipolar disorder. This study used in vivo electrophysiological techniques in anesthetized rats to determine cariprazine's effect on dopaminergic cell activity in the ventral tegmental area (VTA) and substantia nigra pars compacta (SNc). METHODS: Extracellular recordings of individual dopaminergic neurons were performed after oral or intravenous administration of cariprazine, the D3 receptor antagonist SB 277011A, the D2 receptor antagonist L741,626, and/or the D3 receptor agonist PD 128,907...
May 4, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29722587/the-preclinical-discovery-and-development-of-cariprazine-for-the-treatment-of-schizophrenia
#2
Anna Wesołowska, Anna Partyka, Magdalena Jastrzębska-Więsek, Marcin Kołaczkowski
Cariprazine is approved in the United States and Europe for the treatment of manic or mixed episodes associated with bipolar I disorder and for the treatment of schizophrenia in adult patients. It is typically administered orally once a day (a dose range 1.5 - 6 mg/day), does require titration, and may be given with or without food. It has a half-life of 2 - 4 days with an active metabolite that has a terminal half-life of 2 - 3 weeks. Areas covered: This review article focuses on the preclinical discovery of cariprazine providing details regarding its pharmacological, behavioral, and neurochemical mechanisms and its contribution to clinical therapeutic benefits...
May 3, 2018: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29698737/dichlorophenyl-piperazines-including-a-recently-approved-atypical-antipsychotic-are-potent-inhibitors-of-dhcr7-the-last-enzyme-in-cholesterol-biosynthesis
#3
Thiago C Genaro-Mattos, Keri A Tallman, Luke B Allen, Allison Anderson, Karoly Mirnics, Zeljka Korade, Ned A Porter
While antipsychotic medications provide important relief from debilitating psychotic symptoms, they also have significant adverse side effects, which might have relevant impact on human health. Several research studies, including ours, have shown that commonly used antipsychotics such as haloperidol and aripiprazole affect cholesterol biosynthesis at the conversion of 7-dehydrocholesterol (7-DHC) to cholesterol. This transformation is promoted by the enzyme DHCR7 and its inhibition causes increases in plasma and tissue levels of 7-DHC...
April 23, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29694244/cost-effectiveness-of-long-acting-injectable-aripiprazole-once-monthly-400-mg-in-bipolar-i-disorder-in-the-usa
#4
Margarida Augusto, Mallik Greene, Maëlys Touya, Samantha Min Sweeney, Heidi Waters
AIM: To evaluate the cost-effectiveness of aripiprazole once-monthly 400/300 mg (AOM 400) in maintenance monotherapy treatment of bipolar I disorder (BP-I). METHODS: A de novo lifetime Markov model was developed for BP-I using available data for AOM 400 and relevant comparators. Base-case analysis considered costs and outcomes from the US payer perspective. RESULTS: The cost per quality-adjusted life year gained with AOM 400 versus comparators ranged from US$2007 versus oral asenapine to dominance (i...
April 25, 2018: Journal of Comparative Effectiveness Research
https://www.readbyqxmd.com/read/29694243/budget-impact-analysis-of-long-acting-injectable-aripiprazole-once-monthly-400-mg-in-bipolar-i-disorder-in-the-usa
#5
Margarida Augusto, Mallik Greene, Maëlys Touya, Samantha Min Sweeney, Heidi Waters
AIM: To estimate the budget impact (BI) of introducing aripiprazole once-monthly 400 mg/300 mg (AOM 400) in the maintenance monotherapy treatment of bipolar I disorder versus long-acting injectables, oral antipsychotics and best supportive care. METHODS: A BI model was developed from a US-payer perspective using treatment-related, hospitalization and adverse event management cost estimates for a hypothetical 1,000,000-member health plan over a 5-year period. RESULTS: Market share of AOM 400 was predicted to increase from 0...
April 25, 2018: Journal of Comparative Effectiveness Research
https://www.readbyqxmd.com/read/29564481/correction-to-the-effects-of-cariprazine-and-aripiprazole-on-pcp-induced-deficits-on-attention-assessed-in-the-5-choice-serial-reaction-time-task
#6
Samuel A Barnes, Jared W Young, Athina Markou, Nika Adham, István Gyertyán, Béla Kiss
The article The Effects of Cariprazine and Aripiprazole on PCP-Induced Deficits on Attention Assessed in the 5-Choice Serial Reaction Time Task, written by Samuel A. Barnes, Jared W. Young, Athina Markou, Nika Adham, István Gyertyán, Béla Kiss, was originally published electronically.
March 21, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29559781/novel-treatment-options-in-depression-and-psychosis
#7
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/29543103/meta-analysis-and-review-of-dopamine-agonists-in-acute-episodes-of-mood-disorder-efficacy-and-safety
#8
Bruno Romeo, Lisa Blecha, Katia Locatelli, Amine Benyamina, Catherine Martelli
The objective of this meta-analysis is to assess the efficacy and safety of partial and complete dopamine agonists in the treatment of acute mood disorder episodes. Randomized, double-blind and placebo-controlled trials of dopamine agonists in the treatment of acute mood disorder episodes were identified in the MEDLINE and PsycINFO databases and included in the meta-analysis. In monotherapy of mania, improved remission rates were found for cariprazine (odds ratio (OR): 2.08, P < 0.01) and for high-dose aripiprazole (OR: 3...
April 2018: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/29536616/canadian-network-for-mood-and-anxiety-treatments-canmat-and-international-society-for-bipolar-disorders-isbd-2018-guidelines-for-the-management-of-patients-with-bipolar-disorder
#9
Lakshmi N Yatham, Sidney H Kennedy, Sagar V Parikh, Ayal Schaffer, David J Bond, Benicio N Frey, Verinder Sharma, Benjamin I Goldstein, Soham Rej, Serge Beaulieu, Martin Alda, Glenda MacQueen, Roumen V Milev, Arun Ravindran, Claire O'Donovan, Diane McIntosh, Raymond W Lam, Gustavo Vazquez, Flavio Kapczinski, Roger S McIntyre, Jan Kozicky, Shigenobu Kanba, Beny Lafer, Trisha Suppes, Joseph R Calabrese, Eduard Vieta, Gin Malhi, Robert M Post, Michael Berk
The Canadian Network for Mood and Anxiety Treatments (CANMAT) previously published treatment guidelines for bipolar disorder in 2005, along with international commentaries and subsequent updates in 2007, 2009, and 2013. The last two updates were published in collaboration with the International Society for Bipolar Disorders (ISBD). These 2018 CANMAT and ISBD Bipolar Treatment Guidelines represent the significant advances in the field since the last full edition was published in 2005, including updates to diagnosis and management as well as new research into pharmacological and psychological treatments...
March 2018: Bipolar Disorders
https://www.readbyqxmd.com/read/29473089/the-effects-of-cariprazine-and-aripiprazole-on-pcp-induced-deficits-on-attention-assessed-in-the-5-choice-serial-reaction-time-task
#10
Samuel A Barnes, Jared W Young, Athina Markou, Nika Adham, István Gyertyán, Béla Kiss
RATIONALE: Attentional processing deficits are a core feature of schizophrenia, likely contributing to the persistent functional and occupational disability observed in patients with schizophrenia. The pathophysiology of schizophrenia is hypothesized to involve dysregulation of NMDA receptor-mediated glutamate transmission, contributing to disruptions in normal dopamine transmission. Preclinical investigations often use NMDA receptor antagonists, such as phencyclidine (PCP), to induce cognitive disruptions relevant to schizophrenia...
May 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29368205/antipsychotic-drugs-for-patients-with-schizophrenia-and-predominant-or-prominent-negative-symptoms-a-systematic-review-and-meta-analysis
#11
Marc Krause, Yikang Zhu, Maximilian Huhn, Johannes Schneider-Thoma, Irene Bighelli, Adriani Nikolakopoulou, Stefan Leucht
BACKGROUND: Negative symptoms are the core of schizophrenia, but whether antipsychotics are efficacious for their treatment is unclear. Moreover, there is debate whether patients in relevant trials should have predominant negative symptoms or whether prominent negative symptoms are also acceptable. METHODS: We systematically reviewed randomised, blinded antipsychotic drug trials in patients with schizophrenia and either predominant or prominent negative symptoms (last search Dec 12, 2017)...
January 24, 2018: European Archives of Psychiatry and Clinical Neuroscience
https://www.readbyqxmd.com/read/29119668/global-improvement-with-cariprazine-in-the-treatment-of-bipolar-i-disorder-and-schizophrenia-a-pooled-post-hoc-analysis
#12
Suresh Durgam, Willie Earley, Kaifeng Lu, György Németh, István Laszlovszky, Stephen Volk, Robert E Litman
INTRODUCTION: Global rating scale measures are useful for assessing the clinical relevance of patient change. Cariprazine, a dopamine D3 and D2 receptor partial agonist, is FDA-approved for the adult treatment of acute manic/mixed episodes of bipolar I disorder and schizophrenia. Post hoc evaluations of Clinical Global Impressions-Severity (CGI-S) scores from the cariprazine pivotal trials in both indications were conducted. METHODS: Data from 3 bipolar mania and 3 schizophrenia trials were pooled by indication (bipolar disorder = 1033; schizophrenia = 1466)...
December 2017: International Journal of Clinical Practice
https://www.readbyqxmd.com/read/29090086/the-prospects-of-cariprazine-in-the-treatment-of-schizophrenia
#13
EDITORIAL
Jonathan R Scarff
No abstract text is available yet for this article.
November 2017: Therapeutic Advances in Psychopharmacology
https://www.readbyqxmd.com/read/29017067/clinically-relevant-response-and-remission-outcomes-in-cariprazine-treated-patients-with-bipolar-i-disorder
#14
RANDOMIZED CONTROLLED TRIAL
Willie Earley, Suresh Durgam, Kaifeng Lu, Adam Ruth, György Németh, István Laszlovszky, Lakshmi N Yatham
BACKGROUND: Rates of response and remission are measures that endorse the clinical significance of treatment. Cariprazine is FDA approved for the acute treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder in adults. Post hoc analyses of pooled data from 3 pivotal trials of cariprazine in manic/mixed episodes associated with bipolar I disorder were conducted to investigate the effect of cariprazine on various criteria of response and remission. METHODS: The constituent studies were 3-week randomized, double-blind, placebo-controlled, multicenter, parallel-group phase II/III studies in adult patients (age 18-65 years) with bipolar I disorder (NCT00488618, NCT01058096, NCT01058668)...
January 15, 2018: Journal of Affective Disorders
https://www.readbyqxmd.com/read/28843918/the-safety-and-tolerability-of-cariprazine-in-patients-with-manic-or-mixed-episodes-associated-with-bipolar-i-disorder-a-16-week-open-label-study
#15
Terence A Ketter, Gary S Sachs, Suresh Durgam, Kaifeng Lu, Anju Starace, István Laszlovszky, György Németh
BACKGROUND: We evaluated the safety/tolerability of longer-term open-label treatment with cariprazine in patients who had responded to cariprazine for acute bipolar mania. METHODS: In this multinational, multicenter study, open-label, flexible-dose, cariprazine 3-12mg/d was administered for up to 16 weeks to patients (18-65 years) with bipolar mania. Safety evaluations included adverse events (AEs), laboratory values, vital signs, and extrapyramidal symptom (EPS) scales...
January 1, 2018: Journal of Affective Disorders
https://www.readbyqxmd.com/read/28836957/the-safety-and-tolerability-of-cariprazine-in-long-term-treatment-of-schizophrenia-a-post-hoc-pooled-analysis
#16
Henry A Nasrallah, Willie Earley, Andrew J Cutler, Yao Wang, Kaifeng Lu, István Laszlovszky, György Németh, Suresh Durgam
BACKGROUND: Schizophrenia is a chronic and debilitating neuropsychiatric disorder that often requires long-term pharmacotherapy to manage symptoms and prevent relapse. Cariprazine is a potent dopamine D3 and D2 receptor partial agonist that is FDA-approved in the US for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder in adults; the recommended dose range is 1.5-6 mg/d. METHODS: To further characterize the long-term safety of cariprazine, data from two 48-week open-label, flexible-dose extension studies were pooled for post hoc analyses...
August 24, 2017: BMC Psychiatry
https://www.readbyqxmd.com/read/28782490/unmet-needs-in-schizophrenia
#17
Maurizio Pompili, Gloria Giordano, Mario Luciano, Dorian A Lamis, Valeria Del Vecchio, Gianluca Serafini, Gaia Sampogna, Denise Erbuto, Peter Falkai, Andrea Fiorillo
BACKGROUND: Schizophrenia is a complex psychiatric disorder that represents a challenge for all clinicians. Although treatment must address both positive and negative symptoms, several authors have reported the importance of managing unmet needs among patients with schizophrenia. Unmet needs in schizophrenia include difficulties at various clinical, psychosocial, relational, economic, and occupational levels. An important unmet need is represented by insight into the illness that is associated with treatment adherence and compliance with medical prescriptions...
2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28758583/new-trends-in-the-treatment-of-schizophrenia
#18
Herbert Y Meltzer
OBJECTIVES: This article are to describe current trends in the treatment of schizophrenia and the most interesting new approaches to optimizing outcome and fostering the development of new schizophrenia treatments. RESULTS: Increasing utilization of diverse types of atypical antipsychotic drugs (AAPDs), e.g. clozapine- type serotonin (5-HT)2A and weak dopamine (DA) D2 antagonist, amisulpride, a D2/D3/5-HT7 antagonist, and cariprazine, a D3 partial agonist with additional neurotransmitter targets, is occurring as their advantages in efficacy, especially for cognitive impairment and mood symptoms, and side effects are becoming appreciated...
2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28727644/cariprazine-specificity-profile-in-the-treatment-of-acute-schizophrenia-a-meta-analysis-and-meta-regression-of-randomized-controlled-trials
#19
Filippo Corponi, Alessandro Serretti, Stuart Montgomery, Chiara Fabbri
Cariprazine is a new dopamine D2 and D3 receptor partial agonist antipsychotic. Meta-analytic evidence of efficacy in acute schizophrenia and specific groups of patients is lacking. We carried out a meta-analysis in patients with acute schizophrenia to evaluate the efficacy of cariprazine over placebo and active comparators in overall symptoms, positive and negative symptoms and quality of life. Low and high (≥6 mg/day) doses were tested separately. The possible effect of clinical-demographic modulators was also tested...
November 2017: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28721057/safety-tolerability-and-risks-associated-with-first-and-second-generation-antipsychotics-a-state-of-the-art-clinical-review
#20
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
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