scholarly journals Sertindole in the Management of Schizophrenia

2011 ◽  
Vol 3 ◽  
pp. JCNSD.S5729 ◽  
Author(s):  
Mario F. Juruena ◽  
Eduardo Ponde00C9; De Sena ◽  
Irismar Reis De Oliveira
Keyword(s):  
Atypical Antipsychotics ◽  
Second Generation ◽  
Antipsychotic Agents ◽  
Comparable Efficacy ◽  
Psychotic Symptoms ◽  
Alternative Treatment Option ◽  
Second Generation Antipsychotics

Nowadays, new schizophrenia treatments are more ambitious than ever, aiming not only to improve psychotic symptoms, but also quality of life and social reinsertion. Our objective is to briefly but critically review the diagnosis of schizophrenia, the atypical antipsychotics sertindole's pharmacology, safety and status, and mainly evaluate the effects of sertindole compared with other second generation antipsychotics for people with schizophrenia and schizophrenia-like psychosis. In vitro studies showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole offers an alternative treatment option for refractory patients given its good EPS profile, favorable metabolic profile, and comparable efficacy to risperidone. Due to cardiovascular safety concerns, sertindole is available as a second-line choice for patients intolerant to other antipsychotic agents. Further clinical studies, mainly comparisons with other second-generation antipsychotic agents, are needed to define the role of sertindole in the treatment of schizophrenia.

Second-generation taxanes effectively suppress subcutaneous rat lymphoma: role of disposition, transport, metabolism, in vitro potency and expression of angiogenesis genes

2011 ◽  
Vol 30 (3) ◽  
pp. 991-1002 ◽  
Author(s):  
Berta Otová ◽  
Iwao Ojima ◽  
Radka Václavíková ◽  
Jiří Hrdý ◽  
Marie Ehrlichová ◽  
...  
Keyword(s):  
Second Generation

Metabolic and Cardiac Side Effects of Second-generation Antipsychotics: What Every Clinician Should Know

2009 ◽  
Vol 22 (5) ◽  
pp. 478-488 ◽  
Author(s):  
Ericka L. Breden ◽  
Mei T. Liu ◽  
Stacey R. Dean ◽  
Toyin S. Tofade
Keyword(s):  
Cardiovascular Disease ◽  
Health Care ◽  
Adverse Effects ◽  
Second Generation ◽  
Antipsychotic Agents ◽  
The United States ◽  
Natural Death ◽  
Cardiac Side Effects ◽  
Second Generation Antipsychotics ◽  
Physical Health Care

In 2007, 5 of the 7 second-generation antipsychotics were listed in the Top 200 Drugs prescribed by retail sales in the United States. Cardiovascular disease is the leading cause of natural death in individuals with schizophrenia. Second-generation antipsychotics have been implicated with metabolic and cardiovascular adverse effects, and it is important for nonpsychiatric practitioners to be familiar with the monitoring parameters recommended for these agents. This article discusses the risk of weight gain, hyperglycemia, hyperlipidemia, hyperprolactinemia, and cardiovascular concerns associated with second-generation antipsychotic agents. It also discusses the proposed mechanisms for each of these adverse effects. Furthermore, it reviews suggested monitoring parameters to help manage cardiovascular disease in this patient population, and to improve the gap that exists between mental health care and physical health care in the schizophrenic population.

Quality of life in individuals with attenuated psychotic symptoms: Possible role of anxiety, depressive symptoms, and socio-cognitive impairments

2017 ◽  
Vol 257 ◽  
pp. 431-437 ◽  
Author(s):  
Tsutomu Takahashi ◽  
Yuko Higuchi ◽  
Yuko Komori ◽  
Shimako Nishiyama ◽  
Mihoko Nakamura ◽  
...  
Keyword(s):  
Quality Of Life ◽  
Depressive Symptoms ◽  
Cognitive Impairments ◽  
Psychotic Symptoms

scholarly journals Antioxidant Therapy in Graves’ Orbitopathy

2020 ◽  
Vol 11 ◽  
Author(s):  
Giulia Lanzolla ◽  
Claudio Marcocci ◽  
Michele Marinò
Keyword(s):  
Ros Generation ◽  
Related Condition ◽  
Orbital Radiotherapy ◽  
Antioxidant Agents ◽  
Graves Orbitopathy ◽  
High Doses

The balance of the cell redox state is a key point for the maintenance of cellular homeostasis. Increased reactive oxygen species (ROS) generation leads to oxidative damage of tissues, which is involved in the development of several diseases, including autoimmune diseases. Graves’ Orbitopathy (GO) is a disfiguring autoimmune-related condition associated with Graves’ Disease (GD). Patients with active, moderate-to-severe GO, are generally treated with high doses intravenous glucocorticoids (ivGCs) and/or orbital radiotherapy. On the contrary, up to recently, local ointments were the treatment most frequently offered to patients with mild GO, because the risks related to ivGCs does not justify the relatively poor benefits expected in mild GO. However, a medical treatment for these patients is heavily wanted, considering that GO can progress into more severe forms and also patients with mild GO complain with an impairment in their quality of life. Thus, based on the role of oxidative stress in the pathogenesis of GO, a therapy with antioxidant agents has been proposed and a number of studies have been performed, both in vitro and in vivo, which is reviewed here.

scholarly journals Targeting Wnt/β-Catenin Pathway for Developing Therapies for Hair Loss

2020 ◽  
Vol 21 (14) ◽  
pp. 4915 ◽  
Author(s):  
Bu Young Choi
Keyword(s):  
Hair Loss ◽  
Hair Growth ◽  
In Vivo Studies ◽  
Intracellular Targets ◽  
Remarkable Progress ◽  
Made In

Persistent hair loss is a major cause of psychological distress and compromised quality of life in millions of people worldwide. Remarkable progress has been made in understanding the molecular basis of hair loss and identifying valid intracellular targets for designing effective therapies for hair loss treatment. Whereas a variety of growth factors and signaling pathways have been implicated in hair cycling process, the activation of Wnt/β-catenin signaling plays a central role in hair follicle regeneration. Several plant-derived chemicals have been reported to promote hair growth by activating Wnt/β-catenin signaling in various in vitro and in vivo studies. This mini-review sheds light on the role of Wnt/β-catenin in promoting hair growth and the current progress in designing hair loss therapies by targeting this signaling pathway.

Quality of monitoring for metabolic effects associated with second generation antipsychotics in patients with schizophrenia on public insurance

2011 ◽  
Vol 126 (1-3) ◽  
pp. 117-123 ◽  
Author(s):  
Karen E. Moeller ◽  
Sally K. Rigler ◽  
Angela Mayorga ◽  
Niaman Nazir ◽  
Theresa I. Shireman
Keyword(s):  
Second Generation ◽  
Metabolic Effects ◽  
Public Insurance ◽  
Second Generation Antipsychotics

Anchoring of FLT3 in the endoplasmic reticulum alters signaling quality

Blood ◽  
2009 ◽  
Vol 113 (15) ◽  
pp. 3568-3576 ◽  
Author(s):  
Dirk Schmidt-Arras ◽  
Sylvia-Annette Böhmer ◽  
Sina Koch ◽  
Jörg P. Müller ◽  
Lutz Blei ◽  
...  
Keyword(s):  
Endoplasmic Reticulum ◽  
Cell Transformation ◽  
Intracellular Location ◽  
Er Retention ◽  
Transforming Activity ◽  
Signaling Quality

Abstract The mechanism of cell transformation by Fms-like tyrosine kinase 3 (FLT3) in acute myeloid leukemia (AML) is incompletely understood. The most prevalent activated mutant FLT3 ITD exhibits an altered signaling quality, including strong activation of the STAT5 transcription factor. FLT3 ITD has also been found partially retained as a high-mannose precursor in an intracellular compartment. To analyze the role of intracellular retention of FLT3 for transformation, we have generated FLT3 versions that are anchored in the perinuclear endoplasmic reticulum (ER) by appending an ER retention sequence containing a RRR (R3) motif. ER retention of R3, but not of corresponding A3 FLT3 versions, is shown by biochemical, fluorescence-activated cell sorting, and immunocytochemical analyses. ER anchoring reduced global autophosphorylation and diminished constitutive activation of ERK1/2 and AKT of the constitutively active FLT3 versions. ER anchoring was, however, associated with elevated signaling to STAT3. Transforming activity of the FLT3 D835Y mutant was suppressed by ER anchoring. In contrast, ER-anchored FLT3 ITD retained STAT5-activating capacity and was transforming in vitro and in vivo. The findings highlight another aspect of the different signaling quality of FLT3 ITD: It can transform cells from an intracellular location.

Possible Oxcarbazepine Inductive Effects on Aripiprazole Metabolism: A Case Report

2017 ◽  
Vol 31 (3) ◽  
pp. 361-363 ◽  
Author(s):  
Ian R. McGrane ◽  
Joshua G. Loveland ◽  
Jose de Leon
Keyword(s):  
Metabolic Pathway ◽  
Atypical Antipsychotics ◽  
Case Reports ◽  
Autism Spectrum ◽  
Therapeutic Drug ◽  
Second Generation Antipsychotics ◽  
Inductive Effects ◽  
Cyp3a4 Induction ◽  
Low Serum

Oxcarbazepine is a cytochrome P450 (CYP) 3A4 inducer, which is structurally similar to carbamazepine. Although lacking Food and Drug Administration approval, oxcarbazepine is sometimes prescribed to treat aggressive behavior in youth with autism spectrum disorder (ASD). These youths may also be taking second-generation antipsychotics, some of which are substrates of the CYP3A4 metabolic pathway. The combination of these medications may result in decreased serum antipsychotic concentrations, potentially reducing effectiveness. A limited number of reports are available which discuss reduced atypical antipsychotic concentrations secondary to oxcarbazepine CYP3A4 induction. We report a young boy taking oxcarbazepine (1200 mg/d) who presented with an unexpectedly low serum aripiprazole concentration. Utilizing therapeutic drug monitoring, pharmacogenetic testing, and a tool to evaluate drug-drug interactions, we estimate that oxcarbazepine possibly reduced his serum aripiprazole concentration by 68%. Our report is important, as it is the first to describe a drug–drug interaction between oxcarbazepine and aripiprazole. This report should encourage the completion of in vitro and clinical studies and the publication of case reports describing the possible inductive effects of oxcarbazepine on atypical antipsychotics (including cariprazine, lurasidone, quetiapine, aripiprazole, brexpiprazole, iloperidone, and risperidone) mediated by induction of the CYP3A4 metabolic pathway.

scholarly journals Comparative effectiveness of second-generation antipsychotics and haloperidol in acute schizophrenia

2006 ◽  
Vol 189 (5) ◽  
pp. 433-440 ◽  
Author(s):  
Robert E. McCue ◽  
Rubina Waheed ◽  
Leonel Urcuyo ◽  
Geraldine Orendain ◽  
Michel D. Joseph ◽  
...  
Keyword(s):  
Schizoaffective Disorder ◽  
Comparative Effectiveness ◽  
Second Generation ◽  
Rating Scale ◽  
Antipsychotic Agents ◽  
Schizophreniform Disorder ◽  
Open Label ◽  
Hospitalised Patients ◽  
Second Generation Antipsychotics ◽  
Psychiatric Rating Scale

BackgroundThere is little information on the comparative effectiveness of second-generation antipsychotic agents.AimsTo determine if any of five second-generation antipsychotics or haloperidol is more effective in treating acutely ill patients with schizophrenia, schizoaffective disorder or schizophreniform disorder.MethodA sample of 327 newly admitted patients were randomised to open-label treatment with aripiprazole, haloperidol, olanzapine, quetiapine, risperidone or ziprasidone for a minimum of 3 weeks. Measures of effectiveness were improvement in mental status so that the patient no longer required acute in-patient care, and changes in Brief Psychiatric Rating Scale (BPRS) scores.ResultsBy the first measure, haloperidol (89%), olanzapine (92%) and risperidone (88%) were significantly more effective than aripiprazole (64%), quetiapine (64%) and ziprasidone (64%). Changes in BPRS ratings were not significant among treatments.ConclusionsHaloperidol, olanzapine and risperidone are superior to aripiprazole, quetiapine and ziprasidone for the acute treatment of psychosis in hospitalised patients with schizophrenia, schizoaffective disorder or schizophreniform disorder.

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