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Sample records for olanzapine quetiapine risperidone

  1. Pregnancy exposure to olanzapine, quetiapine, risperidone, aripiprazole and risk of congenital malformations. A systematic review

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    Ennis, Zandra Nymand; Damkier, Per

    2015-01-01

    To review available data on first-trimester exposure to olanzapine, quetiapine, risperidone and aripiprazole and risk of congenital malformations. We performed a systematic literature search in accordance with PRISMA guidelines identifying studies containing original data on first......-trimester exposure and pregnancy outcome with respect to congenital malformations. Cumulated data for olanzapine were 1090 first-trimester-exposed pregnancies with 38 malformations resulting in a malformation rate of 3.5%. The corresponding numbers for quetiapine, risperidone and aripiprazole were 443/16 (3.6%), 432...... of congenital malformation. Data for quetiapine and risperidone do not suggest a substantially increased risk, while the risk estimate for aripiprazole remains imprecise owing to a low amount of data....

  2. Ziprasidone versus olanzapine, risperidone or quetiapine in patients with chronic schizophrenia: a 12-week open-label, multicentre clinical trial

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    Lublin, Henrik; Haug, Hans-Joachim; Koponen, Hannu

    2009-01-01

    The efficacy, safety and tolerability of ziprasidone versus the comparators olanzapine, risperidone or quetiapine were investigated in adult patients with chronic schizophrenia, schizoaffective and schizophreniform disorders, with lack of efficacy or intolerance to their previous antipsychotic tr...

  3. Atypical antipsychotics olanzapine, quetiapine, and risperidone and risk of acute major cardiovascular events in young and middle-aged adults

    DEFF Research Database (Denmark)

    Pasternak, Björn; Svanström, Henrik; Ranthe, Mattis F

    2014-01-01

    risperidone (n = 14,134). The primary outcome was any major cardiovascular event (composite of cardiovascular mortality, acute coronary syndrome, or ischemic stroke) within 1 year following treatment initiation. Cox regression was used to estimate hazard ratios (HRs) while on current antipsychotic monotherapy......BACKGROUND: A number of serious cardiovascular safety concerns related to the use of atypical antipsychotics, compared with no use, have emerged, but nearly all reports are from studies of older patients. We aimed to compare the risk of cardiovascular events between the three most commonly used...... in the outpatient setting, adjusting for an outcome-specific disease risk score. RESULTS: The crude rate of any major cardiovascular event was 5.3 per 1,000 person-years among olanzapine users, 3.4 in quetiapine users, and 5.2 in risperidone users. Compared with risperidone, the risk of any major cardiovascular...

  4. Frequency of sexual dysfunction and other reproductive side-effects in patients with schizophrenia treated with risperidone, olanzapine, quetiapine, or haloperidol: the results of the EIRE study.

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    Bobes, J; Garc A-Portilla, M P; Rejas, J; Hern Ndez, G; Garcia-Garcia, M; Rico-Villademoros, F; Porras, A

    2003-01-01

    Atypical antipsychotics seem to differ mainly in their tolerability profile. The aim of this cross-sectional study, the Estudio de Investigaci n de Resultados en Esquizofrenia (Outcomes Research Study in Schizophrenia; EIRE study), was to assess in a clinical setting the frequency of several side-effects related to haloperidol, risperidone, olanzapine, and quetiapine. This article addresses sexual dysfunction and other reproductive side-effects (gynecomastia, menorrhage, amenorrhea, and galactorrhea). We recruited outpatients diagnosed with schizophrenia according to Diagnostic and Statistical Manual of Mental Disorders (DSM-IV; American Psychiatric Association, 1994) criteria and who had received a single antipsychotic (risperidone, olanzapine, quetiapine, or haloperidol) for at least 4 weeks. During a single visit, we collected data, including demographic and clinical characteristics, current antipsychotic and concomitant treatment, and adverse effects listed in a modified version of the UKU Scale. We used a Chi-squared test to determine pairs comparisons of the frequency of adverse reactions between treatments. To estimate risk of a given adverse reaction with a given treatment, we used a logistic regression method. We assessed 636 evaluable patients out of 669 recruited. Frequency of sexual dysfunction was high with haloperidol (38.1%) and also with olanzapine (35.3%), quetiapine (18.2%), and risperidone (43.2%). We found the frequency of other reproductive side-effects to be relatively low with all four drugs: haloperidol (6.9%), olanzapine (6.4%), quetiapine (2.7%), and risperidone (11.7%). Sexual dysfunction appeared to be dose-related with haloperidol, risperidone, and olanzapine. Risperidone and olanzapine showed a higher risk of sexual dysfunction and other reproductive sideeffects than haloperidol. Quetiapine showed a lower risk of sexual dysfunction during short-term treatment ( 12 weeks) are lacking. Our results suggest that none of the atypical

  5. One-year, randomized, open trial comparing olanzapine, quetiapine, risperidone and ziprasidone effectiveness in antipsychotic-naive patients with a first-episode psychosis.

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    San, Luis; Arranz, Belen; Perez, Victor; Safont, Gemma; Corripio, Iluminada; Ramirez, Nicolas; Dueñas, Rosa; Alvarez, Enric

    2012-12-30

    The aim of this study was to compare the 12-month effectiveness of several second-generation antipsychotic drugs, with that of haloperidol in never-treated patients with first-episode psychosis. In total, 114 patients without life time exposure to any psychotropic medication were randomized to haloperidol, olanzapine, risperidone, quetiapine or ziprasidone. Primary outcome was time to all-cause discontinuation. Secondary outcomes included discontinuation rates and symptom change as measured by the Positive and Negative Syndrome Scale (PANSS). The overall discontinuation rate 64%. At 12 months, the proportion of patients discontinuing treatment was 40.0% for olanzapine, 56.5% for quetiapine, 64.0% for risperidone, 80.0% for ziprasidone and 85.7% for haloperidol. Mean time to antipsychotic discontinuation was higher in patients randomized to second-generation antipsychotics than in those taking haloperidol. Significantly lower discontinuation was noted in patients on olanzapine than on haloperidol, or ziprasidone. Our results suggest that olanzapine might lead to longer treatment continuation in treatment naïve FEP patients than haloperidol and, possibly ziprasidone. Global psychopathology was significantly less reduced by haloperidol than with each individual SGA in this earliest phase of treatment. Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.

  6. Olanzapine-induced neuroleptic malignant syndrome in a patient with bipolar affective disorder: Does quetiapine holds the solution?

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    Praveen Tripathi

    2013-01-01

    Full Text Available Neuroleptic Malignant Syndrome (NMS is a rare, severe and life threatening condition induced by antipsychotic medications. It is commonly encountered with the use of first generation antipsychotics, however cases of NMS have been reported with the use of second generation antipsychotics like Olanzapine, Risperidone, Paliperidone, Aripiprazole, Ziprasidone, Amisulpride, Quetiapine and Clozapine, though the incidence of such reports is rare. Due to decreased use of first generation antipsychotics, NMS is reported less frequently now a days. In this case report- we highlight the management issues of a patient suffering from bipolar affective disorder, who had developed NMS following intramuscular injection of haloperidol, which was withdrawn and olanzapine was given later on. The patient had again developed NMS with olanzapine. Finally the patient was managed with modified electroconvulsive therapy and discharged on Lithium carbonate and Quetiapine.

  7. Risk of extrapyramidal syndromes with haloperidol, risperidone, or olanzapine

    NARCIS (Netherlands)

    Schillevoort, I; de Boer, A; Herings, R M; Roos, R A; Jansen, P A; Leufkens, H G

    2001-01-01

    OBJECTIVE: To compare the risk of extrapyramidal syndrome (EPS) between risperidone, olanzapine, and haloperidol, taking into account patients' past antipsychotic drug use and past EPS. METHODS: Data were obtained from the PHARMO-database, containing filled prescriptions of 450,000

  8. Risk of extrapyramidal syndromes with haloperidol, risperidone, or olanzapine

    NARCIS (Netherlands)

    Schillevoort, I; de Boer, A; Herings, R M; Roos, R A; Jansen, P A; Leufkens, H G

    2001-01-01

    OBJECTIVE: To compare the risk of extrapyramidal syndrome (EPS) between risperidone, olanzapine, and haloperidol, taking into account patients' past antipsychotic drug use and past EPS. METHODS: Data were obtained from the PHARMO-database, containing filled prescriptions of 450,000 community-dwellin

  9. Switching to quetiapine for risperidone-induced amenorrhea: Report of two cases

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    P K Pardal

    2010-01-01

    Full Text Available Almost all the antipsychotics can cause hyperprolactinemia-related side-effects like amenorrhea. Quetiapine has been reported to have minimal propensity to cause hyperprolactinemia. We report here two cases of risperidone-induced amenorrhea, who resumed their normal cycle on switching over the medication to quetiapine.

  10. A randomized open-label comparison of the impact of olanzapine versus risperidone on sexual functioning

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    Knegtering, H; Boks, M; Blijd, C; Castelein, S; Van den Bosch, RJ; Wiersma, D

    2006-01-01

    The objective of this study was to compare sexual functioning in patients treated with olanzapine or risperidone. This open-label trial included 46 patients randomized to olanzapine (5-15mg/d) or risperidone (1-6mg/d) for 6 weeks. We used sexual dysfunction was assessed by a semistructured interview

  11. A Comparative Study between Olanzapine and Risperidone in the Management of Schizophrenia

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    Saeed Shoja Shafti

    2014-01-01

    Full Text Available Introduction. Since a variety of comparisons between risperidone and olanzapine have resulted in diverse outcomes, so safety and efficacy of them were compared again in a new trial. Method. Sixty female schizophrenic patients entered into one of the assigned groups for random allocation to olanzapine or risperidone (n=30 in each group in a double-blind, 12-week clinical trial. Scale for Assessment of Positive Symptoms (SAPS and Scale for Assessment of Negative Symptoms (SANS were used as the primary outcome measures. Clinical Global Impressions-Severity Scale (CGI-S, Schedule for Assessment of Insight (SAI, and finally Simpson Angus Scale (SAS as well were employed as secondary scales. Results. While both of olanzapine and risperidone were significantly effective for improvement of positive symptoms (P<0.0001, as regards negative symptoms, it was so only by means of olanzapine (P<0.0003. CGI-S and SAI, as well, were significantly improved in both of the groups. SAS increment was significant only in the risperidone group (P<0.02. Conclusion. While both of olanzapine and risperidone were equally effective for improvement of positive symptoms and insight, olanzapine showed superior efficacy with respect to negative symptoms, along with lesser extrapyramidal side effects, in comparison with risperidone.

  12. Comparison of neuropsychological effects of adjunctive risperidone or quetiapine in euthymic patients with bipolar I disorder.

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    Kozicky, Jan-Marie; Torres, Ivan J; Bond, David J; Lam, Raymond W; Yatham, Lakshmi N

    2012-03-01

    Although associations between antipsychotic use and neuropsychological impairment in bipolar I disorder have been observed, there is a lack of studies comparing the effects of specific agents used in this population. We compared performance between patients receiving maintenance treatment with mood stabilizer monotherapy (n=15), adjunctive risperidone (n=15) or quetiapine (n=17), and a group of demographically matched healthy controls (n=28) on tests of executive function (working memory, set shifting, and inhibition) and verbal learning. Despite having a similar clinical profile, patients being treated with risperidone showed significantly impaired working memory, set-shifting, and verbal learning (Pdisorder, preliminary results indicate that addition of risperidone to a mood stabilizer has a negative impact on executive function and verbal learning, an effect not shared with quetiapine.

  13. Predominant role of the 9-hydroxy metabolite of risperidone in elevating blood prolactin levels

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    Knegtering, R; Baselmans, P; Castelein, S; Bosker, F; Bruggeman, R; van den Bosch, RJ

    2005-01-01

    Objective: The atypical antipsychotic risperidone significantly raises plasma prolactin levels in patients, but clozapine, olanzapine, and quetiapine do not. The differences in neuroendocrine response may be connected with the metabolism of the medications. The authors examined the contributory role

  14. Risperidone versus olanzapine in the acute treatment of Persistent Delusional Disorder: A retrospective analysis.

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    Kulkarni, Karishma; Arasappa, Rashmi; Prasad M, Krishna; Zutshi, Amit; Chand, Prabhat K; Murthy, Pratima; Philip, Mariamma; Muralidharan, Kesavan

    2017-07-01

    There is a dearth of prospective trials studying treatment response in Persistent Delusional Disorder (PDD) to guide clinical practice. Available retrospective data indicate good response to second-generation antipsychotics (SGAs). We selected the data of patients prescribed either olanzapine or risperidone from a retrospective chart review of PDD (n=455) at our centre. We compared the two groups olanzapine (n =86) versus risperidone (n =280) on dose, drug adherence, response and adverse effects. The two groups were comparable on socio-demographic and clinical characteristics of PDD. There was no statistically significant difference between the two groups on adherence (>80%) and response to treatment (>52% good response). Olanzapine was effective at lower mean chlorpromazine equivalents than risperidone. Logistic regression analysis identified shorter mean duration of illness, good adherence and absence of substance dependence as predictors of good response to both drugs. Our study indicates that acute PDD responds well to treatment with both risperidone and olanzapine, provided adherence can be ensured. In the absence of specific treatment guidelines and randomized controlled trials for PDD, our analysis reaffirms the efficacy of SGAs. Copyright © 2017. Published by Elsevier B.V.

  15. Physiogenomic comparison of weight profiles of olanzapine- and risperidone-treated patients.

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    Ruaño, G; Goethe, J W; Caley, C; Woolley, S; Holford, T R; Kocherla, M; Windemuth, A; de Leon, J

    2007-05-01

    Atypical antipsychotics induce pre-diabetic symptoms in some but not all patients, characterized most notably by elevated weight. The side effect profiles of the various drugs in the class differ, however, raising the possibility of drug-specific mechanisms for similar side effects. We used physiogenomic analysis, an approach previously employed to study the genetics of drug and diet response, to discover and compare genetic associations with weight profiles observed in patients treated with olanzapine and risperidone as an approach to unraveling contrasting mechanistic features of both drugs. A total of 29 single nucleotide polymorphisms (SNPs) were selected from 13 candidate genes relevant to two potential pharmacological axes of psychotropic-related weight profiles, appetite peptides and peripheral lipid homeostasis. We applied physiogenomic analysis to a cross-section of 67 and 101 patients being treated with olanzapine and risperidone, respectively, and assessed genetic associations with the weight profiles. Weight profiles in patients treated with olanzapine were significantly associated with SNPs in the genes for apolipoprotein E, apolipoprotein A4 and scavenger receptor class B, member 1. Weight profiles in patients treated with risperidone were significantly associated with SNPs in the genes for leptin receptor, neuropeptide Y receptor Y5 and paraoxonase 1. These results are consistent with contrasting mechanisms for the weight profile of patients treated with these drugs. Genes associated with olanzapine weight profiles may be related to peripheral lipid homeostatic axes, whereas those associated with risperidone's may be related to brain appetite peptide regulation. Future physiogenomic studies will include neurotransmitter receptor SNPs and validation in independent samples.

  16. Quetiapine

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    ... of bed slowly, resting your feet on the floor for a few minutes before standing up.you should know that quetiapine may cause an increase in blood pressure in children and teenagers taking quetiapine. When ...

  17. Effects of quetiapine and olanzapine in patients with psychosis and violent behavior: a pilot randomized, open-label, comparative study

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    Gobbi G

    2014-05-01

    Full Text Available Gabriella Gobbi,1,2 Stefano Comai,1 Guy Debonnel1,2,† 1Neurobiological Psychiatric Unit, Department of Psychiatry, McGill University and McGill University Health Center, 2Institut Philippe Pinel, Department of Psychiatry, Université de Montréal, Montréal, QC, Canada †Guy Debonnel passed away on November 4, 2006 Objective: Patients suffering from psychosis are more likely than the general population to commit aggressive acts, but the therapeutics of aggressive behavior are still a matter of debate. Methods: This pilot randomized, open-label study compared the efficacy of quetiapine versus olanzapine in reducing impulsive and aggressive behaviors (primary endpoints and psychotic symptoms (secondary endpoints from baseline to days 1, 7, 14, 28, 42, 56, and 70, in 15 violent schizophrenic patients hospitalized in a maximum-security psychiatric hospital. Results: Quetiapine (525±45 mg and olanzapine (18.5±4.8 mg were both efficacious in reducing Impulsivity Rating Scale from baseline to day 70. In addition, both treatments reduced the Brief Psychiatric Rating Scale, Positive and Negative Syndrome Scale, and Clinical Global Impression Scale scores at day 70 compared to baseline, and no differences were observed between treatments. Moreover, quetiapine, but not olanzapine, yielded an improvement of depressive symptoms in the items “depression” in Brief Psychiatric Rating Scale and “blunted affect” in Positive and Negative Syndrome Scale. Modified Overt Aggression Scale scores were also decreased from baseline to the endpoint, but due to the limited number of patients, it was not possible to detect a significant difference. Conclusion: In this pilot study, quetiapine and olanzapine equally decreased impulsive and psychotic symptoms after 8 weeks of treatment. Double-blind, large studies are needed to confirm the validity of these two treatments in highly aggressive and violent schizophrenic patients. Keywords: schizophrenia, aggression

  18. Report of a Rare Case of Olanzapine and Risperidone Induced Hypomania

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    AR Zahiroddin

    2006-07-01

    Full Text Available Introduction & Objective: Hypomania is a mood disorder with symptoms of constantly high expansive or irritable mood. After a 4-day period, the patient feels to be in need of less sleep, being talkative, or feeling pressure if not treated kindly, having flight of ideas, distractibility, and increase in goal oriented activities (including social, occupational, educational or sexual activities and being extravagant. Hypomania could be a mood episode of bipolar I and II mood disorder or cyclothymia and could be resulted from consumption of drugs, materials, Electro Convulsive Therapy (ECT or photo therapy. Case: The present report is the case of a 57-year old married woman, who has had a record of bipolar I mood disorder since 30 years ago. The patient was hospitalized once in psychiatry hospital and referred to psychiatry office 2 years ago. She has been under medication therapy by lithium 600 mg, nortriptyline 75 mg, and colonazpam 1 mg. She has taken risperidone 2 mg, the symptoms of hypomania have revealed. After stopping the consumption of risperidone, the treatment continued by lithium tablet 900 mg, eskazina tablet 4 mg, nortriptyline 75 mg for one day. She was under care for 15 months and then due to muscle complications of lithium, pessimism, auditory and visual hallucination, she was recommended to take olanzapine tablet 5 mg once every night. Two days after taking olanzapine the symptoms of hypomania revealed. Consumption of olanzapine was then stopped and the symptoms disappeared and she was brought under control after taking sodiumvalproate tablet. Conclusion: Rarely could Hypomania be a mood episode induced by consuming atypical antipsychotics such as risperidone and olanzapine.

  19. Risperidone, quetiapine and chlorpromazine may have induced priapism in an adolescent.

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    Baytunca, Muharrem Burak; Kose, Sezen; Ozbaran, Burcu; Erermis, Serpil

    2016-01-01

    Priapism is the prolonged, painful erection of penile tissue not accompanied by sexual arousal. Priapism has been established as a rare adverse drug reaction to drugs such as antipsychotics, psychostimulants, antidepressants, and mood stabilizers. Immediate intervention is needed to prevent destructive and irreversible complications, such as erectile dysfunction, disfigurement, inability of the penis to stay erect, and related social/emotional problems. Antipsychotic-induced priapism may result from the alpha receptor occupancy property of those drugs. We report the case of a 13-year-old suffering from attention deficit-hyperactivity disorder plus conduct disorder with priapism related to antipsychotics. Episodes occurred with risperidone plus methylphenidate, quetiapine plus methylphenidate, and chlorpromazine alone. © 2015 Japan Pediatric Society.

  20. A comparison between augmentation with olanzapine and increased risperidone dose in acute schizophrenia patients showing early non-response to risperidone.

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    Hatta, Kotaro; Otachi, Taro; Sudo, Yasuhiko; Kuga, Hironori; Takebayashi, Hiroshi; Hayashi, Hideaki; Ishii, Ryusuke; Kasuya, Masataka; Hayakawa, Tatsuro; Morikawa, Fumiyoshi; Hata, Kazuya; Nakamura, Mitsuru; Usui, Chie; Nakamura, Hiroyuki; Hirata, Toyoaki; Sawa, Yutaka

    2012-07-30

    We examined whether augmentation with olanzapine would be superior to increased risperidone dose among acute schizophrenia patients showing early non-response to risperidone. We performed a rater-blinded, randomized controlled trial at psychiatric emergency sites. Eligible patients were newly admitted patients with acute schizophrenia. Early response was defined as Clinical Global Impressions-Improvement Scale score ≤3 following 2 weeks of treatment. Early non-responders were allocated to receive either augmentation with olanzapine (RIS+OLZ group) or increased risperidone dose (RIS+RIS group). The 78 patients who completed 2 weeks of treatment were divided into 52 early responders to risperidone and 26 early non-responders to risperidone (RIS+OLZ group, n=13; RIS+RIS group, n=13). No difference in the achievement of ≥50% improvement in Positive and Negative Syndrome Scale total score was observed between RIS+OLZ and RIS+RIS groups. Although time to treatment discontinuation for any cause was significantly shorter in the RIS+RIS group (6.8 weeks [95% confidence interval, 5.2-8.4]) than in early responders to risperidone (8.6 weeks [7.9-9.3]; P=0.018), there was no significant difference between the RIS+OLZ group (7.9 weeks [6.3-9.5]) and early responders to risperidone. Secondary outcomes justify the inclusion of augmentation arms in additional, larger studies comparing strategies for early non-responders.

  1. Subjective response to antipsychotic treatment and compliance in schizophrenia. A naturalistic study comparing olanzapine, risperidone and haloperidol (EFESO Study

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    Sacristán Jose A

    2001-12-01

    Full Text Available Abstract Background In order to compare the effectiveness of different antipsychotic drugs in the treatment of schizophrenia it is very important to evaluate subjective response and compliance in patient cohorts treated according to routine clinical practice. Method Outpatients with schizophrenia entered this prospective, naturalistic study when they received a new prescription for an antipsychotic drug. Treatment assignment was based on purely clinical criteria, as the study did not include any experimental intervention. Patients treated with olanzapine, risperidone or haloperidol were included in the analysis. Subjective response was measured using the 10-item version of the Drug Attitude Inventory (DAI-10, and treatment compliance was measured using a physician-rated 4 point categorical scale. Results A total of 2128 patients initiated treatment (as monotherapy with olanzapine, 417 with risperidone, and 112 with haloperidol. Olanzapine-treated patients had significantly higher DAI-10 scores and significantly better treatment compliance compared to both risperidone- and haloperidol-treated patients. Risperidone-treated patients had a significantly higher DAI-10 score compared to haloperidol-treated patients. Conclusion Subjective response and compliance were superior in olanzapine-treated patients, compared to patients treated with risperidone and haloperidol, in routine clinical practice. Differences in subjective response were explained largely, but not completely, by differences in incidence of EPS.

  2. Gabapentin adjunctive to risperidone or olanzapine in partially responsive schizophrenia: an open-label pilot study

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    Adel Gabriel

    2010-10-01

    Full Text Available Adel GabrielDepartments of Psychiatry and Community Health Sciences, University of Calgary, Alberta, CanadaBackground: There is a great need in the treatment of schizophrenia for a drug, or drug ­combinations, to improve clinical response with fewer serious side effects. The objective of this study was to explore the therapeutic effects and tolerability of the anticonvulsant gabapentin as an adjunctive in the treatment of patients with partially responsive schizophrenia.Methods: Ten consenting patients with a confirmed Diagnostic and Statistical Manual of Mental Disorders, 4th Edition, Text Revision diagnosis of schizophrenia were identified. All patients failed at least one 12-week treatment trial with risperidone or olanzapine. Gabapentin was added to ongoing antipsychotic treatment with olanzapine or risperidone for eight weeks. The primary outcome measure was the Positive and Negative Syndrome Scale (PANSS. Other scales included the Calgary Depression Scale (CDSS and the Abnormal Involuntary Movement Scale (AIMS. Repeated-measures multivariate analysis of variance was utilized to examine changes in outcome measures over time with adjunctive treatment with gabapentin.Results: There was a significant drop in the PANSS and CDSS scores at endpoint (week 8. There were no significant differences between the two treatment groups with regard to changes in all outcome measures or in AIMS score. The adjunctive treatments were well tolerated and side effects were transient.Conclusion: Gabapentin could be used successfully as an adjunct to novel antipsychotics in partially responsive schizophrenia. However, large controlled studies are needed to examine the effectiveness of gabapentin in psychotic disorders.Keywords: schizophrenia, refractory, adjunctive treatment, gabapentin, risperidone, olanzapine

  3. Switch to quetiapine in antipsychotic agent-related hyperprolactinemia.

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    Keller, R; Mongini, F

    2002-12-01

    Novel antipsychotics (clozapine, risperidone, olanzapine, quetiapine) are effective in treating psychotic symptoms, also in neurological disease. Hyperprolactinemia is a side effect related to antipsychotics that can cause galactorrhea, gynecomastia, amenorrhea, anovulation, impaired spermatogenesis, decreased libido and sexual arousal, impotence, and anorgasmia, consequent to removal of tonic dopaminergic inhibition of prolactin secretion via hypothalamic dopaminergic receptor blockade in the tuberoinfundibolar tract. Hyperprolactinemia occurs more frequently during treatment with risperidone and olanzapine compared with clozapine and quetiapine. The therapeutic algorithm to antipsychotic-relatedhyperprolactinemia is the following: reduction in antipsychotic dose, addition of cabergoline, bromocriptine, amantadine, and/or switch to another antipsychotic. We propose switching to quetiapine in symptomatic hyperprolactinemia related to antipsychotics and describe five cases.

  4. Effects of lactational exposure of olanzapine and risperidone on hematology and lymphoid organs histopathology: a comparative study in mice neonates.

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    Mishra, Akash C; Mohanty, Banalata

    2010-05-25

    Body weight gain, sexual/reproductive dysfunction and hematological abnormalities are serious consequences of atypical antipsychotics treatment. No attempts however have been made preclinically to elucidate the adverse hematological impacts. Presently, effects of lactational exposure of olanzapine (4, 8 and 10 mg/kg) and risperidone (1 and 2 mg/kg) on hematology as well as lymphoid organ histopathology of mice neonates were investigated. Both olanzapine and risperidone transfers through milk and make the neonates susceptible to their adverse side effects. Corticosterone elevation tendency of both the drugs further enhance the susceptibility for immune dysfunction. Analysis of total and differential leukocytes counts revealed neutropenia with all the doses of olanzapine but only with risperidone 2mg/kg. Weight analysis and histopathology of thymus and spleen indicated a state of suppression; less in the risperidone-exposed groups. Significant plasma corticosterone elevation occurred on 4 and 8 mg/kg olanzapine exposures but not with 10 mg/kg as well as with both the risperidone doses. Elevation of plasma prolactin levels occurred dose-dependently for both the drugs. Hematological toxicity (neutropenia) might be the direct toxic effects of the drugs/unstable metabolites on circulating neutrophils and/or on the bone marrow hemopoietic cells. Direct toxicity of the drugs might also have suppressed the lymphoid organs thymus and spleen. Further, it could be associated to hormonal imbalance induced by adverse pharmacological effects of the drugs on the endocrine system. Suppression of lymphoid organs in olanzapine groups might have resulted because of corticosteronemia and hyperprolactinemia, while in risperidone it could be mediated by pronounced hyperprolactinemic effect alone.

  5. Efficacy and safety of atypical antipsychotic drugs (quetiapine, risperidone, aripiprazole and paliperidone compared with placebo or typical antipsychotic drugs for treating refractory schizophrenia: overview of systematic reviews

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    Tamara Melnik

    Full Text Available CONTEXT AND OBJECTIVE: According to some cohort studies, the prevalence of refractory schizophrenia (RS is 20-40%. Our aim was to evaluate the effectiveness and safety of aripiprazole, paliperidone, quetiapine and risperidone for treating RS. METHODS: This was a critical appraisal of Cochrane reviews published in the Cochrane Library, supplemented with reference to more recent randomized controlled trials (RCTs on RS. The following databases were searched: Medical Literature Analysis and Retrieval System Online (Medline (1966-2009, Controlled Trials of the Cochrane Collaboration (2009, Issue 2, Embase (Excerpta Medica (1980-2009, Literatura Latino-Americana e do Caribe em Ciências da Saúde (Lilacs (1982-2009. There was no language restriction. Randomized controlled trials, systematic reviews and meta-analyses evaluating atypical antipsychotics for treating RS were included. RESULTS: Seven Cochrane systematic reviews and 10 additional RCTs were included in this review. The data generally showed minor differences between the atypical antipsychotics evaluated and typical antipsychotics, regarding improvement in disease symptoms, despite better adherence to treatment with atypical antipsychotics. Risperidone was specifically evaluated in patients with RS in one of the systematic reviews included, with favorable outcomes, but without definitive superiority compared with other drugs of proven efficacy, like amisulpride, clozapine and olanzapine. CONCLUSIONS: The findings underscore the difficulty in treating these patients, with high dropout rates and treatment patterns of modest improvement in assessments of effectiveness. Atypical antipsychotics have advantages over typical antipsychotics mainly through their better safety profile, which leads to better adherence to treatment. A combination of antipsychotics may also be an option for some refractory patients.

  6. Quetiapine versus other atypical antipsychotics for schizophrenia

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    Komossa, Katja; Rummel-Kluge, Christine; Schmid, Franziska; Hunger, Heike; Schwarz, Sandra; Srisurapanont, Manit; Kissling, Werner; Leucht, Stefan

    2014-01-01

    Background In many countries of the industrialised world second generation (’atypical’) antipsychotic drugs have become the first line drug treatment for people with schizophrenia. It is not clear how the effects of the various second generation antipsychotic drugs differ. Objectives To evaluate the effects of quetiapine compared with other second generation antipsychotic drugs for people with schizophrenia and schizophrenia-like psychosis. Search methods We searched the Cochrane Schizophrenia Group Trials Register (April 2007), inspected references of all identified studies, and contacted relevant pharmaceutical companies, drug approval agencies and authors of trials for additional information. Selection criteria We included all randomised control trials comparing oral quetiapine with oral forms of amisulpride, aripiprazole, clozapine, olanzapine, risperidone, sertindole, ziprasidone or zotepine in people with schizophrenia or schizophrenia-like psychosis. Data collection and analysis We extracted data independently. For dichotomous data we calculated relative risks (RR) and their 95% confidence intervals (CI) on an intention-to-treat basis based on a random-effects model. We calculated numbers needed to treat/harm (NNT/NNH) where appropriate. For continuous data, we calculated weighted mean differences (WMD) again based on a random-effects model. Main results The review currently includes 21 randomised control trials (RCTs) with 4101 participants. These trials provided data on four comparisons - quetiapine versus clozapine, olanzapine, risperidone or ziprasidone. A major limitation to all findings is the high number of participants leaving studies prematurely (57.6%) and the substantial risk of biases in studies. Efficacy data favoured olanzapine and risperidone compared with quetiapine (PANSS total score versus olanzapine:10 RCTs, n=1449, WMD 3.66 CI 1.93 to 5.39; versus risperidone: 9 RCTs, n=1953, WMD 3.09 CI 1.01 to 5.16), but clinical meaning is unclear

  7. Improvement of dumping syndrome and oversecretion of glucose-dependent insulinotropic polypeptide following a switch from olanzapine to quetiapine in a patient with schizophrenia.

    Science.gov (United States)

    Watanabe, Aiko; Fukui, Naoki; Suzuki, Yutaro; Motegi, Takaharu; Igeta, Hirofumi; Tsuneyama, Nobuto; Someya, Toshiyuki

    2015-01-01

    Among the most important adverse effects of antipsychotics is abnormal glucose metabolism, which includes not only hyperglycemia but hyperinsulinemia and hypoglycemia. We have previously described five patients who experienced hypoglycemia during treatment with antipsychotics. Thus, an anamnesis of gastric surgery, which often causes dumping syndrome, and treatment with antipsychotics may synergistically induce hypoglycemia. We describe here a patient with schizophrenia under treatment of olanzapine and an anamnesis of gastric surgery, who experienced late dumping syndrome, hyperinsulinemia and overactivation of glucose-dependent insulinotropic polypeptide. Dumping syndrome, however, was improved after the patient was switched from olanzapine to quetiapine.

  8. Schizophrenic patients treated with clozapine or olanzapine perform better on theory of mind tasks than those treated with risperidone or typical antipsychotic medications.

    Science.gov (United States)

    Savina, Ioulia; Beninger, Richard J

    2007-08-01

    Theory of mind (ToM), the ability to attribute mental states to others, is associated with medial prefrontal cortical (mPFC) activity and is impaired in schizophrenia. Olanzapine or clozapine but not typical antipsychotics or risperidone preferentially affect c-fos expression in mPFC in animals. We tested the hypothesis that schizophrenic patients treated with different antipsychotics would perform differently on ToM tasks. Groups receiving Typicals (n=23), Clozapine (n=18), Olanzapine (n=20) or Risperidone (n=23) and a Control group of healthy volunteers (n=24) were matched for age, gender, handedness and education. ToM functioning was assessed with picture sequence, second-order belief and faux-pas tests. Schizophrenic groups performed similarly to controls on non-ToM conditions. The Olanzapine and Clozapine groups performed similarly to Controls on ToM tasks. The Typicals and Risperidone groups performed worse than the other groups on ToM tasks. We concluded that ToM performance of schizophrenic patients is influenced by the antipsychotic they are taking. Our results suggest that olanzapine or clozapine but not typicals or risperidone may improve or protect ToM ability.

  9. Atypicality in presentation of neuroleptic malignant syndrome caused by olanzapine

    Directory of Open Access Journals (Sweden)

    Mishra Biswaranjan

    2007-10-01

    Full Text Available Neuroleptic malignant syndrome (NMS is the most serious of acute neurological side effects produced by antipsychotic medication, characterized by hyperthermia, rigidity, altered consciousness and autonomic dysfunction, the prevalence of which varies from 0.4-1.4%. NMS is usually seen in treatment with high potency typical antipsychotics and very rarely with atypical antipsychotics. However, NMS cases have been reported with risperidone, clozapine, olanzapine and quetiapine. The presentations of NMS have often varied, and we report another atypicality in presentation of NMS due to olanzapine use.

  10. Comparison of the effect of lithium plus quetiapine with lithium plus risperidone in children and adolescents with bipolar I disorder: a randomized clinical trial.

    Science.gov (United States)

    Habibi, Nastaran; Dodangi, Nasrin; Nazeri, Ali

    2017-01-01

    Background: In the treatment of bipolar disorder in youths, often more than one medication should be prescribed. In the current study, we compared the efficacy and tolerability of the combination of lithium and quetiapine with lithium and risperidone in the treatment of manic or mixed episodes in children and adolescents. Methods: Thirty patients (aged 10-18 years) who were hospitalized for a manic or mixed episode were recruited from consecutive inpatient admissions to the Child and Adolescent Psychiatric Unit at Razi Psychiatric Hospital (University of Social Welfare and Rehabilitation Sciences, Tehran, Iran) from June 2012 to September. They were randomly treated with lithium (with the usual dose to achieve blood levels 0.8-1) and quetiapine (400-600 mg per day) or risperidone (0.5-6 mg per day). The primary outcome measure with respect to efficacy was the mean decrease in Young Mania Rating Scale (YMRS) score. Side effects were also assessed. The independent t test and two-factor repeated measure analysis of variance (ANOVA) was used for data analysis. P-value of less than 0.05 was considered statistically significant. Results: The reduction in YMRS scores was similar in both groups. The remission rate (YMRS lithium in manic or mixed episodes of bipolar I disorder in children and adolescents was not superior to lithium and risperidone, but was associated with fewer complications.

  11. Development and validation of a HPLC-UV method for the simultaneous determination of the antipsychotics clozapine, olanzapine and quetiapine, several beta-blockers and their metabolites.

    Science.gov (United States)

    Gracia, Margarete Silva; Köppl, Alexandra; Unholzer, Sandra; Haen, Ekkehard

    2017-03-07

    A simple, accurate and selective column-switching high performance liquid chromatography (HPLC) method was developed and validated for simultaneous quantification of six beta-blockers (metoprolol MET, timolol TIM, bisoprolol BIS, propranolol PRO, carvedilol CAR and nebivolol NEB), three of their metabolites (α-hydroxy metoprolol α-HMET, N-desisopropyl propranolol DIPRO and 4'-hydroxy carvedilol 4-HCAR), three antipsychotics (olanzapine OLA, clozapine CLO and quetiapine QUE) and three of their metabolites (N-desmethyl olanzapine DMOLA, N-desmethyl clozapine DMCLO and N-desalkyl quetiapine DAQUE) in human serum. After pretreatment on a Merck LiChrospher RP-4 ADS column (25 μm) drugs were separated on a Phenomenex Gemini Phenyl Hexyl 110 A column (250 mm x 4.6 mm, 5 μm) using a gradient mixture of acetonitrile and potassium dihydrogen phosphate buffer pH 3.1 (containing 10 % methanol) as a mobile phase at a flow rate of 1ml/min. The total analysis time was 40 min. For detection of the analytes, four different UV wavelengths were used: 215 nm, 226 nm, 242 nm and 299 nm. The method was validated according to the guidelines of the Society of Toxicology and Forensic Chemistry (GTFCh) in terms of selectivity, linearity, accuracy, precision and stability and successfully applied for the analysis of the 15 described analytes in human serum.

  12. Olanzapine

    Science.gov (United States)

    ... bipolar disorder (manic depressive disorder; a disease that causes episodes of depression, episodes of mania, and other abnormal moods) in ... Olanzapine may cause side effects. Tell your doctor if any of these ... difficulty walking constipation weight gain dry mouth pain in arms, legs, ...

  13. 利培酮联合喹硫平治疗老年痴呆精神行为症状的研究%Study on risperidone combined with quetiapine for treating psychiatric and behavioral disturbances in senile dementia

    Institute of Scientific and Technical Information of China (English)

    赵新民; 李远

    2016-01-01

    Objective To investigate the efficacy and safety of risperidone combined with quetiapine in the treatment behavioral and psychiatric symptoms of dementia (BPSD). Methods Ninety cases of BPSD in the geriatric department of our hospital from January 2013 to December 2015 were randomly divided into the combination group , risperidone group and quetiap-ine group according to the completely random method ,30 cases in each group. The combination group was given risperidone com-bined with quetiapine, the risperidone group was given the risperidone therapy and quetiapine group received the quetiapine therapy. The treatment effects were evaluated by using the BEHAVE-AD before treatment and after 2-,4-,8-week treatment. The side effects scale(TESS) was used to evaluate the adverse reactions occurrence situation. Results The AD-BEHAVE scores after 2-,4-,8-week treatment in 3 groups were significantly lower than those before treatment ,the difference was statistically significant (P0.05),but the effect in the combination group was significantly superior to that in the quetiapine group(χ2=15.39,P0.05),但明显优于喹硫平组,差异有统计学意义(χ2=15.39,P<0.01)。利培酮组不良反应发生率明显高于联合组、喹硫平组,差异均有统计学意义(P<0.05)。结论利培酮联合喹硫平治疗老年痴呆BPSD具有较好疗效,不良反应小,更适于老年痴呆患者的治疗。

  14. Olanzapine versus other atypical antipsychotics for schizophrenia

    Science.gov (United States)

    Komossa, Katja; Rummel-Kluge, Christine; Hunger, Heike; Schmid, Franziska; Schwarz, Sandra; Duggan, Lorna; Kissling, Werner; Leucht, Stefan

    2014-01-01

    Background In many countries of the industrialised world second generation (“atypical”) antipsychotics have become the first line drug treatment for people with schizophrenia. The question as to whether, and if so how much, the effects of the various second generation antipsychotics differ is a matter of debate. In this review we examined how the efficacy and tolerability of olanzapine differs from that of other second generation antipsychotics. Objectives To evaluate the effects of olanzapine compared to other atypical antipsychotics for people with schizophrenia and schizophrenia-like psychosis. Search methods 1. Electronic searching We searched the Cochrane Schizophrenia Group Trials Register (April 2007) which is based on regular searches of BIOSIS, CENTRAL, CINAHL, EMBASE, MEDLINE and PsycINFO. 2. Reference searching We inspected the reference of all identified studies for more trials. 3. Personal contact We contacted the first author of each included study for missing information. 4. Drug companies We contacted the manufacturers of all atypical antipsychotics included for additional data. Selection criteria We included all randomised trials that used at least single-blind (rater-blind) design, comparing oral olanzapine with oral forms of amisulpride, aripiprazole, clozapine, quetiapine, risperidone, sertindole, ziprasidone or zotepine in people with schizophrenia or schizophrenia-like psychosis. Data collection and analysis We extracted data independently. For dichotomous data we calculated relative risks (RR) and their 95% confidence intervals (CI) on an intention-to-treat basis based on a random effects model. We calculated numbers needed to treat/harm (NNT/NNH) where appropriate. For continuous data, we calculated weighted mean differences (WMD) again based on a random effects model. Main results The review currently includes 50 studies and 9476 participants which provided data for six comparisons (olanzapine compared to amisulpride, aripiprazole

  15. Haloperidol induces higher Homer1a expression than risperidone, olanzapine and sulpiride in striatal sub-regions.

    Science.gov (United States)

    Iasevoli, Felice; Fiore, Germano; Cicale, Maria; Muscettola, Giovanni; de Bartolomeis, Andrea

    2010-05-15

    Homer1a and Yotiao are two post-synaptic density proteins at the crossroad of dopamine-glutamate neurotransmission. Homer1a has been implicated in the pathophysiology of schizophrenia and is differentially induced by typical and atypical antipsychotics, perhaps according to their dopaminergic profile. Yotiao has been involved in glutamate and dopamine post-synaptic signalling. Here, we seek to determine whether Homer1a and Yotiao might be implicated in post-synaptic response to antipsychotics with affinity to different dopamine D(2) receptors: haloperidol (0.8mg kg(-1)), risperidone (3mg kg(-1)), olanzapine (2.5mg kg(-1)) and (-)-sulpiride (50mg kg(-1)). Homer1a expression was significantly induced by haloperidol compared to vehicle and to atypical antipsychotics in almost all striatal sub-regions. Atypical antipsychotics induced the gene in the lateral putamen and in the core of the accumbens only. All antipsychotics, with the exclusion of sulpiride, elicited a dorsolateral-to-ventromedial distribution pattern of Homer1a expression. No significant induction was detected for Yotiao. These results suggest that the quantitative and topographical pattern of Homer1a expression may putatively be related to antipsychotics affinity and/or occupancy at dopamine D(2) receptors.

  16. Risperidone

    Science.gov (United States)

    ... bipolar disorder (manic depressive disorder; a disease that causes episodes of depression, episodes of mania, and other abnormal moods). Risperidone is also used to treat behavior problems such as aggression, self-injury, and ... repetitive behavior, difficulty interacting with others, and problems ...

  17. Effects of cigarette smoking on priapism induced by quetiapine: a case report

    Directory of Open Access Journals (Sweden)

    Hosseini Seyed

    2012-10-01

    Full Text Available Abstract Priapism is defined as an unwanted, prolonged, and painful erection which is unrelated to sexual stimulation. Some case studies suggest that priapism is an adverse effect of antipsychotic medications. In our case study a 30 year-old Iranian male with schizophrenia was experiencing recurrent priapism associated with quetiapine use. There are three interesting facts about this case: Firstly, the patient suffered priapism after even low dose consumption of quetiapine. Secondly, this case had experienced priapism with risperidone, olanzapine, and even clozapine in the past, suggesting a possible pharmacodynamic interaction of antipsychotics and inner biological traits in this particular case. Thirdly, priapism induced by low dose quetiapine was resolved after cigarette smoking.

  18. Economic consequences of the adverse reactions related with antipsychotics: an economic model comparing tolerability of ziprasidone, olanzapine, risperidone, and haloperidol in Spain.

    Science.gov (United States)

    Bobes, Julio; Cañas, Fernando; Rejas, Javier; Mackell, Joan

    2004-12-01

    Frequency of adverse reactions (ARs) related with antipsychotics usage is high. Along with clinical implications, economic impact might be important. The purpose of this study was to model the economic consequences of ARs related with ziprasidone, olanzapine, risperidone, and haloperidol in Spain, by means of a cost-effectiveness model developed using a Markov modeling approach. The model simulated treatment of a cohort of 1000 schizophrenics for 12 months, initiating treatment with one of four antipsychotic drugs; haloperidol, risperidone, olanzapine and ziprasidone. Conditional probabilities of developing any of four adverse events were calculated. Treatment was modified (decrease dose, switch medication) according to incidence of ARs and physician judgments, obtained from a local cross-sectional study and clinical trials previously published. The analysis was conducted in year 2002 from a third party payer perspective. Results are shown as annual cost per month with psychotic symptoms controlled and included univariate sensitivity analysis. The therapeutic strategy starting with ziprasidone showed the lower costs and the greater number of months with symptoms controlled in most scenarios evaluated versus the other options considered, although the differences were weak: 9.6, 9.3, 9.5 and 9.5 controlled months per patient in base scenario, with annual cost per patient per month with symptoms controlled of 1035 Euros, 1084 Euros, 1087 Euros and 1090 Euros for ziprasidone, haloperidol, risperidone and olanzapine, respectively. Results were robust to one-way sensitivity analysis. Despite the unlike drug prices of antipsychotics, a considerable economic impact due to adverse reactions was seen in our setting. These results should be taken into account by health decision makers and clinicians in the management of patients with schizophrenia.

  19. Risperidone versus other atypical antipsychotics for schizophrenia

    Science.gov (United States)

    Komossa, Katja; Rummel-Kluge, Christine; Schwarz, Sandra; Schmid, Franziska; Hunger, Heike; Kissling, Werner; Leucht, Stefan

    2014-01-01

    Background In many countries of the industrialised world second-generation (“atypical”) antipsychotics (SGAs) have become the first line drug treatment for people with schizophrenia. The question as to whether and if so how much the effects of the various SGAs differ is a matter of debate. In this review we examined how the efficacy and tolerability of risperidone differs from that of other SGAs. Objectives To evaluate the effects of risperidone compared with other atypical antipsychotics for people with schizophrenia and schizophrenia-like psychosis. Search methods 1. Electronic searching We searched the Cochrane Schizophrenia Group Trials Register (April 2007) which is based on regular searches of BIOSIS, CENTRAL, CINAHL, EMBASE, MEDLINE and PsycINFO. 2. Reference searching We inspected the references of all identified studies for more trials. 3. Personal contact We contacted the first author of each included study for missing information. 4. Drug companies We contacted the manufacturers of all atypical antipsychotics included for additional data. Selection criteria We included all randomised, blinded trials comparing oral risperidone with oral forms of amisulpride, aripiprazole, clozapine, olanzapine, quetiapine, sertindole, ziprasidone or zotepine in people with schizophrenia or schizophrenia-like psychosis. Data collection and analysis We extracted data independently. For dichotomous data we calculated risk ratio (RR) and their 95% confidence intervals (CI) on an intention-to-treat basis based on a random-effects model. We calculated numbers needed to treat/harm (NNT/NNH) where appropriate. For continuous data, we calculated mean differences (MD), again based on a random-effects model. Main results The review currently includes 45 blinded RCTs with 7760 participants. The number of RCTs available for each comparison varied: four studies compared risperidone with amisulpride, two with aripiprazole, 11 with clozapine, 23 with olanzapine, eleven with

  20. Incidence of tardive dyskinesia with risperidone or olanzapine in the elderly: results from a 2-year, prospective study in antipsychotic-naïve patients.

    Science.gov (United States)

    Woerner, Margaret G; Correll, Christoph U; Alvir, Jose Ma J; Greenwald, Blaine; Delman, Howard; Kane, John M

    2011-07-01

    Tardive dyskinesia (TD) rates with second-generation antipsychotics (SGAs) are considered to be low relative to first-generation antipsychotics (FGAs), even in the particularly vulnerable elderly population. However, risk estimates are unavailable for patients naïve to FGAs. Therefore, we aimed to determine the TD incidence in particularly vulnerable, antipsychotic-naïve elderly patients treated with the SGA risperidone or olanzapine. The present work describes a prospective inception cohort study of antipsychotic-naïve elderly patients aged 55 years identified at New York Metropolitan area in-patient and out-patient geriatric psychiatry facilities and nursing homes at the time of risperidone or olanzapine initiation. At baseline, 4 weeks, and at quarterly periods, patients underwent assessments of medical and medication history, abnormal involuntary movements, and extra-pyramidal signs. TD was classified using Schooler-Kane criteria. Included in the analyses were 207 subjects (age: 79.8 years, 70.0% female, 86.5% White), predominantly diagnosed with dementia (58.9%) or a major mood disorder (30.9%), although the principal treatment target was psychosis (78.7%), with (59.4%) or without (19.3%) agitation. With risperidone (n=159) the cumulative TD rate was 5.3% (95% confidence interval (CI): 0.7, 9.9%) after 1 year (mean dose: 1.0±0.76 mg/day) and 7.2% (CI: 1.4, 12.9%) after 2 years. With olanzapine (n=48) the cumulative TD rate was 6.7% (CI: 0, 15.6%) after 1 year (mean dose: 4.3±1.9 mg/day) and 11.1% (CI: 0, 23.1%) after 2 years. TD risk was higher in females, African Americans, and patients without past antidepressant treatment or with FGA co-treatment. The TD rates for geriatric patients treated with risperidone and olanzapine were comparable and substantially lower than previously reported for similar patients in direct observation studies using FGAs. This information is relevant for all patients receiving antipsychotics, not just the especially

  1. Cost-effectiveness model comparing olanzapine and other oral atypical antipsychotics in the treatment of schizophrenia in the United States

    Directory of Open Access Journals (Sweden)

    Smolen Lee J

    2009-04-01

    Full Text Available Abstract Background Schizophrenia is often a persistent and costly illness that requires continued treatment with antipsychotics. Differences among antipsychotics on efficacy, safety, tolerability, adherence, and cost have cost-effectiveness implications for treating schizophrenia. This study compares the cost-effectiveness of oral olanzapine, oral risperidone (at generic cost, primary comparator, quetiapine, ziprasidone, and aripiprazole in the treatment of patients with schizophrenia from the perspective of third-party payers in the U.S. health care system. Methods A 1-year microsimulation economic decision model, with quarterly cycles, was developed to simulate the dynamic nature of usual care of schizophrenia patients who switch, continue, discontinue, and restart their medications. The model captures clinical and cost parameters including adherence levels, relapse with and without hospitalization, quality-adjusted life years (QALYs, treatment discontinuation by reason, treatment-emergent adverse events, suicide, health care resource utilization, and direct medical care costs. Published medical literature and a clinical expert panel were used to develop baseline model assumptions. Key model outcomes included mean annual total direct cost per treatment, cost per stable patient, and incremental cost-effectiveness values per QALY gained. Results The results of the microsimulation model indicated that olanzapine had the lowest mean annual direct health care cost ($8,544 followed by generic risperidone ($9,080. In addition, olanzapine resulted in more QALYs than risperidone (0.733 vs. 0.719. The base case and multiple sensitivity analyses found olanzapine to be the dominant choice in terms of incremental cost-effectiveness per QALY gained. Conclusion The utilization of olanzapine is predicted in this model to result in better clinical outcomes and lower total direct health care costs compared to generic risperidone, quetiapine, ziprasidone, and

  2. 喹硫平与利培酮对女性精神分裂症患者血清泌乳素水平的影响%Effects of quetiapine and risperidone on serum prolactin levels of female schizophrenia

    Institute of Scientific and Technical Information of China (English)

    孙海华; 杨焕

    2013-01-01

    Objective To explore the effects of quetiapine and risperidone in the treatmemt of female schizophrenic patients and the effect of levels on serum prolactin. Methods 76 female schizophrenic patients were treated with quetiapine and risperidone randomly. The serum prolactin were measured and the scores of PANSS were evaluated before treatment and at the 1st、2nd、4th、8th week respectively. TESS was used to evaluate side effect. Results There were no significant differences in PANSS basal scores and the decreased scores after the treatment in two groups. The level of serum prolactin in risperidone group increased markedly than quetiapine group, and the serum prolactin level in quetiapine group were not increase significantly. Conclusion Quetiapine and risperidone have similar efficacy in the treatment of femal patients with schizophrenia. Risperidone produced increases in plasma prolactin levels in femal patients.%目的:评价喹硫平与利培酮对女性精神分裂症患者疗效和血清泌乳素水平的影响。方法选择女性精神分裂症患者76例,随机分为喹硫平与利培酮组治疗8周。采用阳性和阴性症状量表(PANSS)在治疗前及治疗第1周、2周、4周、8周末分别评定疗效,检测血清泌乳素水平,同时精神药物副反应量表(TESS)评定药物副反应。结果治疗前和治疗8周,两组在PANSS总分无显著差异。利培酮组血清泌乳素水平显著升高,并显著高于喹硫平组。喹硫平组血清泌乳素水平治疗前后无显著变化。结论喹硫平与利培酮对女性精神分裂症的疗效相似,利培酮对女性精神病患者的血清泌乳素水平有较大影响。

  3. Comparison of clinical effects of quetiapine and risperidone in the treatment of senile schizophrenia%喹硫平与利培酮治疗老年精神分裂症的临床效果对比

    Institute of Scientific and Technical Information of China (English)

    刘春容

    2015-01-01

    目的:比较喹硫平与利培酮治疗老年精神分裂症的临床效果。方法:回顾性分析170例老年精神分裂症患者的临床资料,根据治疗方法不同将其分为喹硫平组与利培酮组,其中喹硫平组74人,利培酮组96人,比较两组治疗前后的PANSS评分及不良反应情况。结果:喹硫平组与利培酮组治疗后2周、4周、6周、8周其各项指标较治疗前均有显著改善,差异具统计学意义(P0.05);喹硫平组锥体外系反应、恶主呕吐、停经泌乳等不良反应发生率显著低于利培酮组,而嗜睡发生率显著高于利培酮组,差异具统计学意义(P0.05)。结论:喹硫平与利培酮对老年精神分裂症均有确切疗效,且安全性较高;喹硫平对症状的改善相对更好。%Objective: To compare the clinical effects of quetiapine and risperidone in the treatment of senile schizophrenia. Methods:retrospective analysis of the clinical data of 170 cases of elderly patients with schizophrenia, according to the different treatment methods were divided into quetiapine group and risperidone group, wherein the quetiapine group of 74 people, 96 people of risperidone group, PANSS scores and adverse reactions were compared between two groups before and after treatment. Results:the quetiapine group and risperidone group after treatment for 2 weeks, 4 weeks, 6 weeks, 8 weeks, the indicators were significantly improved than before treatment, the difference was statistically significant ( P0.05) ;quetiapine flat group extrapyramidal adverse reactions, the evil Lord vomiting, stopping lactation was significantly lower than the risperidone group, and the incidence of somnolence was significantly higher than the risperidone group, the difference was statistically signif-icant (P0.05) . Conclusion: quetiapine and risperidone in schizophrenia have exact curative ef-fect on senile spirit, and high safety;the improvement of symptom of quetiapine is relatively

  4. 喹硫平与利培酮治疗精神分裂症的疗效与安全性研究%Study on efficacy and safety of Quetiapine and Risperidone in treatment of schizophrenia

    Institute of Scientific and Technical Information of China (English)

    吴雪娥

    2015-01-01

    Objective To observe efficacy and safety of quetiapine and risperidone to patients with schizophrenia.Methods Participants included 80 patients with schizophrenia ,accepted quetiapine(496 ±65) mg/d and risperidone ( 3.1 ±0.3 ) mg/d respectively for eight weeks, and curative effect and safety were observed.Results The total efficiency rate of quetiapine group and risperidone group was 72.5% and 75%respectively, the effects of quetiapine and risperidone in schizophrenic patients had no significantly difference( p>0.05).The incidence of postural hypotension in quetiapine group was higher than that in risperidone group, but the incidence of extrapyramidal side effects and weight gain in quetiapine group was lower than that in risperidone group, there was significantly difference (P<0.05).Conclusions Quetiapine and risperidone have similar efficiency in the treatment of schizophrenic patients, and are safe and generally well-tolerated.%目的:研究喹硫平与利培酮治疗精神分裂症的疗效及安全性。方法按随机数字表法将2013年在本院精神病科住院的精神分裂症患者随机分为喹硫平组和利培酮组,每组各40例。喹硫平组给予喹硫平(496±65) mg/d治疗,利培酮组给予利培酮(3.1±0.3) mg/d治疗。疗程8周,从PANSS减分率评价其疗效,同时以不良反应症状量表(TESS)评定副反应。结果喹硫平组总有效率为72.5%,利培酮组总有效率为75.0%,两组疗效差异无统计学意义( P>0.05)。喹硫平组体位性低血压发生率明显高于利培酮组,利培酮组体重增加及锥体外系反应发生率显著高于喹硫平组,组间比较差异有统计学意义( P<0.05)。结论喹硫平与利培酮治疗精神分裂症疗效相当,安全性良好。

  5. Cognitive effects of olanzapine treatment in schizophrenia.

    Science.gov (United States)

    McGurk, Susan R; Lee, M A; Jayathilake, K; Meltzer, Herbert Y

    2004-05-10

    Improvement in some but not all domains of cognition during treatment with the atypical antipsychotic drugs clozapine, quetiapine, olanzapine, and risperidone has been reported in some but not all studies. It has been recently suggested that these reports are an artifact, related to lessening of the impairment due to typical neuroleptic drugs and anticholinergic agents. The purpose of this study was to further test the hypothesis that olanzapine, an atypical antipsychotic drug reported to have anticholinergic properties, improves cognition in patients with schizophrenia, including domains of cognition related closely to work and social function (ie, verbal learning and memory) and that this improvement is independent of improvement in psychopathology. Thirty-four patients with schizophrenia who were partial responders to typical antipsychotic drug treatment were evaluated with a comprehensive neurocognitive battery, including measures of executive functioning; verbal and visual learning and memory; working memory; immediate, selective, and sustained attention; perceptual/motor processing; and motor skills prior to and following treatment with olanzapine for 6 weeks. The Brief Psychiatric Rating Scale (BPRS) was used to assess psychopathology in patients treated with typical antipsychotic drugs. Subjects were switched to olanzapine (average dose 13.4 mg, range 5-20 mg) and reassessed following 6 weeks and 6 months of treatment. Significant improvement was noted in 9 of 19 cognitive tests, including measures of selective attention, verbal learning and memory, and verbal fluency. No cognitive test was worsened by olanzapine treatment. Improvements in the BPRS Total and Positive Symptom Subscale scores were noted. Improvements in verbal learning and memory, sustained attention, and psychomotor tracking were independent of improvement in psychopathology. These data suggest that olanzapine improved some but not all cognitive deficits in schizophrenia, including verbal

  6. A control study of olanzapine and risperidone in the treatment of senile delirium%奥氮平与利培酮治疗老年期谵妄患者的对照研究

    Institute of Scientific and Technical Information of China (English)

    冼易平; 王英

    2011-01-01

    Objective; To compare the efficacy and safety of olanzapine and risperidone in the treatment of senile delirium. Method: Fifty patients with senile delirium were randomly divided into olanzapine treatment group (n = 25 ) and risperidone treatment group ( n = 25). They were prospectively observed and assessed with the Chinese revision of confusion assessment method (CAM-CR) .clinical global impression severity scale (CGI-SI) and treatment emergent symptom scales (TESS). Results:The effective rate of olanzapine treatment group and risperidone treatment group were 64. 0% and 68. 0% respectively (P > 0. 05). CGI-SI total scores of olanzapine treatmeng group and that of risperidone treatmen group were both reduced significantly after treatment (t=5. 19,6. 95 ;P 0.05 ). The total incidence rate of side effects in the risperidone group was significantly higher than that in olanzapine group ( χ2 = 5. 88, P < 0. 05). Conclusion; Olanzapine and risperidone have similar effects in treating senile delirium,ahd has fewer side effects.%目的:比较奥氮平和利培酮治疗老年期谵妄的疗效和安全性. 方法:将50例老年期谵妄患者随机分成奥氮平治疗组(n=25),利培酮治疗组(n=25),疗程2周.治疗前后以谵妄评定方法中文修订版(CAM-CR)及临床疗效总评量表-病情严重程度(CGI-SI)评定疗效;以治疗中出现的症状量表(TESS)评定药物不良反应. 结果:奥氮平组和利培酮组显效率分别为64.0%和68.0% (P >0.05).两组CGI-SI总分治疗后均较治疗前明显降低(t=5.19、6.95,P均<0.01);两组间比较,差异无统计学意义(P>0.05).利培酮组不良反应明显高于奥氮平组(x2=5.88,P<0.05). 结论:奥氮平和利培酮治疗老年期谵妄疗效相当,不良反应轻.

  7. Clinical consequences of switching from olanzapine to risperidone and vice versa in outpatients with schizophrenia: 36-month results from the worldwide schizophrenia outpatients health outcomes (W-SOHO study

    Directory of Open Access Journals (Sweden)

    Hong Jihyung

    2012-12-01

    Full Text Available Abstract Background With many atypical antipsychotics now available in the market, it has become a common clinical practice to switch between atypical agents as a means of achieving the best clinical outcomes. This study aimed to examine the impact of switching from olanzapine to risperidone and vice versa on clinical status and tolerability outcomes in outpatients with schizophrenia in a naturalistic setting. Methods W-SOHO was a 3-year observational study that involved over 17,000 outpatients with schizophrenia from 37 countries worldwide. The present post hoc study focused on the subgroup of patients who started taking olanzapine at baseline and subsequently made the first switch to risperidone (n=162 and vice versa (n=136. Clinical status was assessed at the visit when the first switch was made (i.e. before switching and after switching. Logistic regression models examined the impact of medication switch on tolerability outcomes, and linear regression models assessed the association between medication switch and change in the Clinical Global Impression-Schizophrenia (CGI-SCH overall score or change in weight. In addition, Kaplan-Meier survival curves and Cox-proportional hazards models were used to analyze the time to medication switch as well as time to relapse (symptom worsening as assessed by the CGI-SCH scale or hospitalization. Results 48% and 39% of patients switching to olanzapine and risperidone, respectively, remained on the medication without further switches (p=0.019. Patients switching to olanzapine were significantly less likely to experience relapse (hazard ratio: 3.43, 95% CI: 1.43, 8.26, extrapyramidal symptoms (odds ratio [OR]: 4.02, 95% CI: 1.49, 10.89 and amenorrhea/galactorrhea (OR: 8.99, 95% CI: 2.30, 35.13. No significant difference in weight change was, however, found between the two groups. While the CGI-SCH overall score improved in both groups after switching, there was a significantly greater change in those who

  8. Improvement in hyperprolactinemia and reproductive comorbidities in patients with schizophrenia switched from conventional antipsychotics or risperidone to olanzapine.

    Science.gov (United States)

    Kinon, Bruce J; Ahl, Jonna; Liu-Seifert, Hong; Maguire, Gerald A

    2006-06-01

    This open-label, prospective, 4-month study in hyperprolactinemic patients with schizophrenia explored whether prolactin levels decrease after switching antipsychotic therapy to olanzapine. A secondary objective was to determine if reproductive morbidities and sexual dysfunction occurring with hyperprolactinemia improved with prolactin normalization. Clinically stable patients with schizophrenia, who had hyperprolactinemia defined as >18.8 ng/ml for males and >24.2 ng/ml for females, were randomized to: remain on current therapy (n=27) or switch to olanzapine, 5-20 mg/day, (n=27). Baseline prolactin levels in female patients randomized to receive olanzapine (n=14) were 66.3+/-38.7 ng/ml and were 82.0+/-37.6 (p=.32) in those remaining on their pre-study antipsychotic medication (n=14). In male patients, baseline prolactin levels were 33.7+/-12.1 and 33.5+/-13.8 ng/ml (p=.97), respectively, for those randomized to olanzapine (n=13) or remaining on pre-study treatment (n=13). At study end, patients switched to olanzapine experienced significant reductions in mean serum prolactin levels of 19.8+/-18.1 ng/ml in males (p=.02), and 32.3+/-47.5 ng/ml in females (p=.01), but prolactin continued to be elevated in patients who remained on pre-study antipsychotic treatment. After switching to olanzapine treatment, male patients experienced significantly (p=.03) increased free testosterone levels but there were no significant improvements in total testosterone levels; some female patients experienced improved menstrual cycling, as well as resolution of galactorrhea and gynecomastia, and sexual functioning was significantly improved in both genders. Patients switched to olanzapine, as well as those remaining on their pre-study medication, maintained clinical stability, their symptoms continued to improve, although there were no significant between-treatment differences in improvement. Treatment-emergent adverse events did occur in both treatment groups; however, they were not

  9. Effect of quetiapine and olanzapine on cognitive function in patients with chronic schizophrenia%喹硫平和奥氮平对慢性精神分裂症患者认知功能的影响

    Institute of Scientific and Technical Information of China (English)

    王美玲

    2014-01-01

    目的:比较喹硫平和奥氮平对慢性精神分裂症患者认知功能的影响。方法:80例慢性精神分裂症患者随机分配接受喹硫平、奥氮平治疗。分别在入组时、12周、24周末测定PANSS、WCST、言语流畅性测验、成人言语学习测验、CPT、WMS、WAIS、连线试验测定、手指叩击试验。结果:喹硫平组患者在言语流畅性、CPT和执行功能方面优于奥氮平组,有统计学差异(P<0.05);认知功能的改善与PANSS量表总分、阴性症状的改善之间有显著的相关性(r=-0.33, P<0.05)。结论:喹硫平、奥氮平均可不同程度改善慢性精神分裂症患者的认知功能,喹硫平在某些方面优于奥氮平。%Objective:To compare effects of quetiapine and olanzapine on cognitive function in patients with chronic schizo-phrenia. Methods:A total of 80 patients with chronic schizophrenia were randomly divided into quetiapine group and olanzapine group. The cognitive function was assessed at baseline,12th weekend and 24th weekend with positive and negative syndrome scale (PANSS), Wisconsin card sorting test (WCST), verbal fluency test, adult verbal learning test, continuous performance test (CPT), Wechsler memory scale ( WMS) , Wechsler adult intelligence scale ( WAIS) , trail marking test ( TMT) and finger tapping test ( FIT) . Results:Quetiapine had more significant improvement on executive function, CPT and verbal fluency than olanzapine (P<0. 05). The cognitive function change was related to change of total score and negative symptoms score in PANSS (r=-0. 33, P<0. 05). Conclusions:Que-tiapine and olanzapine could improve the cognitive function for the patients with chronic schizophrenia, and the former is better in some aspects.

  10. 喹硫平、奥氮平在治疗老年痴呆患者精神行为障碍的效果研究%Study on the Effect of Quetiapine and Olanzapine in the Treatment of Senile Dementia Patients With Behavioral and Psychological Disorders

    Institute of Scientific and Technical Information of China (English)

    赵永明

    2015-01-01

    Objective Observation of quetiapine, olanzapine treatment with mental behavior disorder symptoms of alzheimer's patients clinical effect. Methods Compared with quetiapine lfat and olanzapine group two groups of therapeutic effect. Results Two groups of curative effect and adverse reaction rate was no signiifcant difference (P>0.05). Conclusion Quetiapine and the nitrogen average is safe and effective.%目的:观察喹硫平、奥氮平治疗有精神行为障碍症状的老年痴呆患者的临床效果。方法对比喹硫平组和奥氮平组两组治疗效果。结果两组疗效和不良反应发生率比较无显著差异(P>0.05)。结论喹硫平和奥氮平均安全有效。

  11. Disease Burden Research of Quetiapine and Olanzapine in the treatment of Schizophrenia%喹硫平与奥氮平治疗精神分裂症患者的疾病负担研究

    Institute of Scientific and Technical Information of China (English)

    路亚洲; 白羽霞; 李虹耀; 韩晟

    2016-01-01

    Objective Based on real world data, this study explores disease burden of schizophrenia and evaluates the impacts of quetiapine and olanzapine on economic burden.Methods Included data were extracted from urban basic medical insurance database.Then statistical analyses were used to analyze the data.Results Study included 26 patients with schizophrenia hospitalized patients,the average hospitalization time (116±56)d,average hospital- lization expenses for (8899±11,748) yuan.Quetiapine group patients hospitalization time was significantly lower than that in the olanzapine group,average hospitalization expenses and average daily hospitalization expenses were significantly lower than those of olanzapine group,average and daily drug cost,drug accounted for were significantly lower than the olanzapine group,differences were statisticaly significant(P<0.05).Conclusion Our mental division patients in hospital for a long time,burden of disease.Compared to the olanzapine,quetiapine can save medical resources and quetiapine economy better.%目的:基于真实世界数据,对中国精神分裂症进行疾病负担研究,并以奥氮平和喹硫平为例探讨该疾病的经济负担情况。方法提取2011年中国医疗保险研究会《全国城镇基本医疗保险参保患者药品医疗器械和诊疗项目利用情况调查》数据库中精神分裂症住院患者的相关数据,进行统计分析。结果研究纳入了2600例精神分裂症住院患者,平均住院时间为(116±56)d,次均住院费用为(8899±11748)元;喹硫平组患者的次均住院时间显著低于奥氮平组,次均住院费用和日均住院费用均显著低于奥氮平组,次均及日均药品费用、药占比均显著低于奥氮平组,差异均有统计学意义(均P<0.05)。结论我国精神分裂症患者住院时间长,疾病负担重;相比于奥氮平,使用喹硫平能节约医疗服务资源,且经济性更佳。

  12. Analyzing effect and safety of quetiapine and risperidone on mental and behavioral of alzheimer disease%喹硫平与利培酮治疗阿尔茨海默病精神行为异常的临床疗效及安全性

    Institute of Scientific and Technical Information of China (English)

    许晓英; 曾媛媛; 张易

    2013-01-01

    目的 探讨喹硫平与利培酮治疗阿尔茨海默病精神行为异常的临床疗效及安全性.方法 将86例阿尔茨海默病患者随机分为喹硫平组和利培酮组,分别给予喹硫平及利培酮口服治疗,疗程8周.采用痴呆病理行为评定量表评估临床疗效,并比较2组不良反应发生率.结果 喹硫平组与利培酮组治疗有效率分别为79.5%和76.2%,差异无统计学意义(P>0.05);治疗后8周,喹硫平组痴呆病理行为评定量表昼夜节律紊乱及攻击行为因子显著优于利培酮组(P<0.05);2组不良反应发生率无显著差异(P>0.05).结论 喹硫平与利培酮治疗阿尔茨海默精神行为异常临床疗效相当,但喹硫平抗焦虑及镇静的作用优于利培酮.%Objective To explore the effect and safety of quetiapine and risperidone on mental and behavioral of alzheimer disease.Methods Eighty-six patients with alzheimer disease were randomly divided into quetiapine group and risperidone group.The two groups received quetiapine and risperidone treatment respectively.The course of treatment was 8 weeks.BEHAVE-AD scale was used to evaluate the clinical effect.Adverse rates were compared between two groups.Results The effectiveness rates of treatment were 79.5 % and 76.2 % in quetiapine group and risperidone group without significant difference (P >0.05).Aggressiveness and diurnal rhythm disturbances of BEHAVE-AD 8 weeks after treatment in quetiapine group were superior to risperidone group (P < 0.0 5).There was no significant difference of adverse reactions between the two groups (P >0.05).Conclusion Quetiapine and risperidone have equivalent effects on mental and behavioral of alzheimer disease,while the anti-anxiety effects and sedative effect of quetiapine is superior to risperidone.

  13. Prediction of long-term metabolic effects of olanzapine and risperidone treatment from baseline body mass index in schizophrenia and bipolar disorder.

    Science.gov (United States)

    Bobo, William Victor; Bonaccorso, Stefania; Jayathilake, Karuna; Meltzer, Herbert Yale

    2011-09-30

    Baseline body mass index (BMI), baseline BMI status (normal, overweight, obese) and early (1 month) BMI increases were tested as predictors of 6- and 12-month increases in glucose and lipid measures in 82 olanzapine (OLZ)- and 78 risperidone (RIS)-treated patients with schizophrenia, schizoaffective disorder, or bipolar disorder who participated in a 12-month randomized, prospective metabolic effects study. Baseline BMI predicted greater fasting glucose and HgbA1c levels at 12 months for both treatments. Early BMI change predicted fasting glucose levels at 6 months, but not HgbA1c or BMI, at either time point. For patients who received no concomitant mood stabilizers, early BMI change predicted 12 month HgbA1c values in the OLZ group, and 6- (but not 12-) month fasting glucose and HgbA1c values in the RIS group. Neither baseline BMI nor early BMI change consistently predicted increases in lipids with either drug. OLZ-treated patients with normal baseline BMI had greater increases in total cholesterol, triglycerides, and non-HDL-cholesterol than those who were overweight or obese. In conclusion, higher baseline BMI predicted adverse glycemic changes after 12 months with OLZ and RIS. Individuals with normal baseline BMI may be most susceptible to OLZ-induced hyperlipidosis. Frequency of metabolic screening should be independent of baseline BMI or rapid increases in BMI.

  14. Concurrent determination of olanzapine, risperidone and 9-hydroxyrisperidone in human plasma by ultra performance liquid chromatography with diode array detection method: application to pharmacokinetic study.

    Science.gov (United States)

    Siva Selva Kumar, M; Ramanathan, M

    2016-02-01

    A simple and sensitive ultra-performance liquid chromatography (UPLC) method has been developed and validated for simultaneous estimation of olanzapine (OLZ), risperidone (RIS) and 9-hydroxyrisperidone (9-OHRIS) in human plasma in vitro. The sample preparation was performed by simple liquid-liquid extraction technique. The analytes were chromatographed on a Waters Acquity H class UPLC system using isocratic mobile phase conditions at a flow rate of 0.3 mL/min and Acquity UPLC BEH shield RP18 column maintained at 40°C. Quantification was performed on a photodiode array detector set at 277 nm and clozapine was used as internal standard (IS). OLZ, RIS, 9-OHRIS and IS retention times were found to be 0.9, 1.4, .1.8 and 3.1 min, respectively, and the total run time was 4 min. The method was validated for selectivity, specificity, recovery, linearity, accuracy, precision and sample stability. The calibration curve was linear over the concentration range 1-100 ng/mL for OLZ, RIS and 9-OHRIS. Intra- and inter-day precisions for OLZ, RIS and 9-OHRIS were found to be good with the coefficient of variation <6.96%, and the accuracy ranging from 97.55 to 105.41%, in human plasma. The validated UPLC method was successfully applied to the pharmacokinetic study of RIS and 9-OHRIS in human plasma.

  15. Doses of olanzapine, risperidone, and haloperidol used in clinical practice: results of a prospective pharmacoepidemiologic study. EFESO Study Group. Estudio Farmacoepidemiologico en la Esquizofrenia con Olanzapina.

    Science.gov (United States)

    Sacristán, J A; Gómez, J C; Montejo, A L; Vieta, E; Gregor, K J

    2000-05-01

    The objectives of this study were to determine the doses of olanzapine (OLZ), risperidone (RIS), and haloperidol (HAL) used in clinical practice in outpatients with schizophrenia and the rates of occurrence of extrapyramidal symptoms (EPS) and other adverse events, clinical response, and use of concomitant medications. The present study involved a subset of patients from a 6-month, open-label, prospective observational study. Data were collected by 293 psychiatrists at mental health centers and other outpatient treatment facilities in Spain. Medications and doses used, occurrence of EPS and other adverse events, and scores on the Clinical Global Impression (CGI) of Severity Scale and Global Assessment of Function (GAF) were recorded. Clinical response was defined as a decrease of > or = 2 points on the CGI, with a final CGI score or = 5 received significantly higher overall mean daily doses than did patients with an initial CGI score < 5 (P < 0.001). A significantly lower proportion of OLZ-treated patients (10.2%) were receiving concomitant anticholinergic medication at the end of the study (month 6) compared with RIS-treated (19.9%) and HAL-treated (44.0%) patients (P < 0.001). The mean daily doses recorded in this analysis based on data from a naturalistic setting are consistent with recommendations based on clinical trials. Compared with both RIS- and HAL-treated patients, OLZ-treated patients were less likely to experience EPS or other adverse events, and less likely to use concomitant anticholinergic medications. OLZ-treated patients were also more likely to respond to treatment than were RIS-treated patients.

  16. Cost effectiveness of paliperidone palmitate versus risperidone long-acting injectable and olanzapine pamoate for the treatment of patients with schizophrenia in Sweden.

    Science.gov (United States)

    Mehnert, Angelika; Nicholl, Deborah; Pudas, Hanna; Martin, Monique; McGuire, Alistair

    2012-01-01

    To model the cost effectiveness of paliperidone palmitate (paliperidone long-acting injectable; PLAI), a new once-monthly long-acting antipsychotic therapy, compared with risperidone long-acting injectable (RLAI) and olanzapine pamoate (OLAI), in multi-episode patients (two or more relapses) with schizophrenia in Sweden. A Markov decision analytic model was developed to simulate the history of a cohort of multi-episode patients transitioning through different health states on a monthly basis over a 5-year time horizon from the perspective of the Swedish healthcare system. Therapeutic strategies consisted of starting treatment with RLAI (mean dose 37.5 mg every 2 weeks), PLAI (mean dose 75 mg equivalent (eq.) every month) or OLAI (150 mg every 2 weeks or 300 mg every 4 weeks). Probability of relapse, level of adherence, side-effects (extrapyramidal symptoms, tardive dyskinesia, weight gain and diabetes) and treatment discontinuation (switch) were derived from long-term observational data when feasible. Incremental cost-effectiveness outcomes, discounted at 3% annually, included cost per quality-adjusted life-year (QALY) and cost per relapse avoided (expressed in 2009 Swedish Krona SEK). Relative to RLAI and OLAI, PLAI is economically dominant: more effective (additional QALYs, less relapses) and less costly treatment option over a 5-year time horizon. The results were robust when tested in sensitivity analysis. The impact of once-monthly treatment on adherence levels is not yet known, and not all variables that could impact on real-world outcomes and costs were included in this model. PLAI was cost saving from a Swedish payer perspective compared with RLAI and OLAI in the long-term treatment of multi-episode (two or more relapses) schizophrenia patients.

  17. CONTROL STUDY BETWEEN RISPERIDONE ORAL SOLUTION AND OLANZAPINE FOR ALCOHOL -INDUCED MENTAL DISORDER%利培酮口服液与奥氮平治疗酒精所致精神障碍对照研究

    Institute of Scientific and Technical Information of China (English)

    王丽莉; 吕浩; 杨建立

    2012-01-01

    目的:探讨利培酮口服液与奥氮平治疗酒精所致精神障碍的疗效和安全性.方法:将68例男性酒精所致精神障碍患者随机分为利培酮口服液治疗组和奥氮平治疗组.采用阳性与阴性症状量表( PANSS)评定临床疗效;采用治疗副反应量表( TESS)评定药物不良反应.结果:利培酮口服液与奥氮平两组疗效差异无显著性.利培酮口服液主要不良反应为锥外系反应,奥氮平为体重增加.结论:利培酮口服液与奥氮平治疗酒精所致精神障碍疗效及耐受性均好,可根据用药对象对不良反应的耐受等情况进行选择.%Objective: To compare the efficacy and safety of risperidone oral solution and olanzapine in the treatment of alcohol - induced mental disorder. Methods: Sixty - eight male patients with alcohol - induced mental disorder were randomly divided into risperidone oral solution group and olanzapine group. Clinical effect was evaluated by Positive and Negative Syndrome Scale (PANSS) ,and the adverse drug reactions were assessed with Treatment Emergent Symptom Scale ( TESS) . Results: No significant differences were observed in the clinical effect of the two groups. The main side effect experienced by the olanzapine group was body weight gain, while the resperidone oral solution group showed extrapyramidal responses. Conclusion: Both olanzapine and risperidone oral solution are safe and effective for the treatment of alcohol - induced mental disorder,and can be clinically selected according to patients' tolerance of the side effects.

  18. 60例脑血管疾病所致精神障碍奥氮平与利培酮治疗效果对比%Effect of olanzapine and risperidone in the treatment of 60 cases of mental disorder caused by cerebrovascular disease comparison

    Institute of Scientific and Technical Information of China (English)

    高晨

    2015-01-01

    Objective To observe the effect of mental disorder caused by olanzapine and risperidone in the treatment of cerebral vascular disease. Methods will randomly olanzapine group and risperidone group. According to the grouping of olanzapine in the treatment group received olanzapine treatment of risperidone in treatment group were given risperidone, treatment. Results In the total effective rate of treatment group was 96.66%, treatment with olanzapine, risperidone group 93.33%, two groups are basically the same. However, olanzapine has fewer adverse effects of the treatment group was 16.66%, risperidone in treatment group was 30%, statistically significant difference contrast. Conclusion Olanzapine can significantly reduce the incidence of adverse reaction of patients, more worthy of clinical promotion and practice of strengthening the.%目的:分析奥氮平与利培酮治疗脑血管疾病所致精神障碍的疗效。方法将该院于2013年1月—2013年12月选取的60例患者随机划分为奥氮平治疗组与利培酮治疗组。根据分组对奥氮平治疗组患者予以奥氮平进行治疗,对利培酮治疗组予以利培酮进行治疗。结果在治疗的总有效率方面,奥氮平治疗组为96.66%,利培酮治疗组为93.33%,两组基本一致,对比差异不具有统计学意义。但奥氮平治疗组患者的不良反应更少为16.66%,利培酮治疗组为30%,对比差异具有统计学意义。结论奥氮平治疗脑血管疾病所致精神障碍的效果与利培酮基本一致,但是却能够明显降低患者的不良反应发生率,更加值得加强临床推广与实践。

  19. Clinical comparison and investigation of curative effects by olanzapine and risperidone in the treatment of behavioral and psychological symptoms of Alzheimer’s disease%奥氮平、利培酮治疗老年痴呆精神行为症状疗效的临床比较探讨

    Institute of Scientific and Technical Information of China (English)

    慕经纬

    2016-01-01

    Objective To compare clinical effects by olanzapine and risperidone in the treatment of behavioral and psychological symptoms of Alzheimer’s disease. Methods A total of 102 patients with Alzheimer’s disease were randomly divided into olanzapine group and risperidone group, with 51 cases in each group. The olanzapine group received olanzapine tablets for treatment, and the risperidone group received risperidone tablets for treatment. Improvements of clinical symptoms were observed in 2, 4, and 8 weeks of treatment. Mini mental state examination (MMSE), dementia pathological behavior score (BE-HAVE) and positive and negative syndrome scale (PANSS) were taken. Condition of adverse drug reactions was evaluated. Results The olanzapine group had total effective rate as 92.2%, and the risperidone group had that as 90.2%. Their difference had no statistical significance (P>0.05). There was no statistically significant difference of scores in hostile suspicion, disturbance of thought, behavior disorders, anxiety-depression, and bigotry between the two groups after 2, 4 and 8 weeks of treatment (P>0.05). The olanzapine group had lower PANSS score in 2 and 4 weeks of treatment than the risperidone group, and the difference had statistical significance (P0.05)。两组治疗后2、4、8周敌对猜疑、思维障碍、行为紊乱、焦虑抑郁、偏执等评分比较差异均无统计学意义(P>0.05)。奥氮平组在治疗2、4周时 PANSS 评分低于利培酮组,差异有统计学意义(P<0.05)。利培酮组发生锥体外系反应和恶心例数多于奥氮平组,差异有统计学意义(P<0.05)。结论奥氮平和利培酮治疗老年痴呆精神行为症状均有较好的疗效,但奥氮平起效更快,不良反应较少,患者耐受性更好。

  20. Contrast study of synergistic effect of Quetiapine and Olanzapine on patients with depression combined with anxiety disorder treated with Paroxetine%喹硫平与奥氮平对帕罗西汀治疗抑郁症伴焦虑障碍患者增效作用的比较

    Institute of Scientific and Technical Information of China (English)

    王学燕; 周玉珍; 杨红梅; 孙克峰; 梁家騋

    2015-01-01

    Objective: To compare efficacy and safety of Paroxetine combined with Quetiapine or Olanzapine in treatment of patients with depression combined with anxiety disorder. Methods:60 patients suffering from depression with anxiety disorder were randomly divided into Paroxetine combined with Quetiapine group (n=30, combined Quetiapine group) and Paroxetine combined with Olanzapine group ( n=30, combined Olanzapine group). The treatment continued for eight weeks. Hamilton depression scale ( HAMD) , Hamilton anxiety scale ( HAMA) , and treatment emergent symptom scale ( TESS) were used to evaluate efficacy and ad-verse reactions. Results:One week after the treatment, the scores of HAMD and HAMA of the two groups decreased compared with those before the treatment, the differences of the same group were significant (P0. 05). No big difference between the two groups in the obvious effective rate (P>0. 05). For the ad-verse reactions ( nausea, dry mouth, constipation, tachycardia, loss of appetite and weight gain):the occurrence rates of increased ap-petite and body mass gain of combined Olanzapine group were higher than those of combined Quetiapine group, and the differences had statistical significance (P0.05)。两组患者显效率无明显差异(P>0.05)。对于不良反应(如恶心、口干、便秘、心动过速、食欲和体质量增加等),合并奥氮平组患者除了食欲和体质量增加发生率高于合并喹硫平组,差异有统计学意义(P<0.05)外,余项无明显差异。结论:帕罗西汀合并喹硫平和合并奥氮平治疗抑郁症伴焦虑障碍疗效相当,起效快,不良反应少,依从性好,均为较好增效策略。肥胖者合并喹硫平治疗更安全。

  1. Clinical Efficacy of Risperidone and Olanzapine in the Treatment of first Episode Schizophrenia%利培酮与奥氮平治疗首发精神分裂症患者的临床疗效与安全性

    Institute of Scientific and Technical Information of China (English)

    任丽

    2015-01-01

    Objective To investigate the effect of risperidone and olanzapine in the treatment of first-episode clinical eficacy and safety in patients with schizophrenia.Methods Methods 68 patients with first episode schizophrenia were randomly divided into risperidone group in 34 cases and 34 cases of olanzapine group, risperidone group were treated with oral risperidone treatment,olanzapine group were treated with oral olanzapine treatment,after 8 weeks of treatment with PANSS reduction rate of curative effect evaluation.Results Risperidone group of patients,the total effective rate was 94.1%(32/34),olanzapine group of patients,the total effective rate was 91.2%(31/34),the difference between the two groups had no statistical significance(P>0.05).Olanzapine group drowsiness,dry mouth and body mass increase adverse effects than risperidone group,risperidone group akathisia, insomnia and headache adverse reactions than olanzapine group(P<0.05).Conclusion Equivalent efficacy of olanzapine and risperidone on schizophrenia,but the adverse reactions of two different,clinicians should take according to the regimen of according to the clinical characteristics of the patients with.%目的:探讨利培酮与奥氮平治疗首发精神分裂症患者的临床疗效与安全性。方法将68例首发精神分裂症患者随机分为利培酮组34例及奥氮平组34例,利培酮组患者给予口服利培酮进行治疗,奥氮平组患者给予口服奥氮平进行治疗,治疗8周后采用阳性和阴性症状量表(PANSS)减分率评估疗效。结果利培酮组患者总有效率为94.1%(32/34),奥氮平组患者总有效率为91.2%(31/34),两组比较差异无统计学意义(P>0.05)。奥氮平组嗜睡、口干和体质量增加不良反应多于利培酮组,利培酮组静坐不能、失眠和头痛不良反应多于奥氮平组(P<0.05)。结论奥氮平与利培酮对首发精神分裂症的疗效相当,但二者不良反应不同,临床

  2. Quetiapine monotherapy for bipolar depression

    Directory of Open Access Journals (Sweden)

    Michael E Thase

    2008-03-01

    Full Text Available Michael E ThaseDepartments of Psychiatry, University of Pennsylvania School of Medicine, Philadelphia, PA, USA; the Philadelphia Veterans Affairs Medical Center, Philadelphia, PA, USA; and the University of Pittsburgh Medical Center, Pittsburgh, PA, USAAbstract: Bipolar depression is more common, disabling, and difficult-to-treat than the manic and hypomanic phases that define bipolar disorder. Unlike the treatment of so-called “unipolar” depressions, antidepressants generally are not indicated as monotherapies for bipolar depressions and recent studies suggest that - even when used in combination with traditional mood stabilizers – antidepressants may have questionable value for bipolar depression. The current practice is that mood stabilizers are initiated first as monotherapies; however, the antidepressant efficacy of lithium and valproate is modest at best. Within this context the role of atypical antipsychotics is being evaluated. The combination of olanzapine and the antidepressant fluoxetine was the first treatment to receive regulatory approval in the US specifically for bipolar I depression. Quetiapine was the second medication to be approved for this indication, largely as the result of two pivotal trials known by the acronyms of BOLDER (BipOLar DEpRession I and II. Both studies demonstrated that two doses of quetiapine (300 mg and 600 mg given once daily at bedtime were significantly more effective than placebo, with no increased risk of patients switching into mania. Pooling the two studies, quetiapine was effective for both bipolar I and bipolar II depressions and for patients with (and without a history of rapid cycling. The two doses were comparably effective in both studies. Although the efficacy of quetiapine monotherapy has been established, much additional research is necessary. Further studies are needed to more fully investigate dose-response relationships and comparing quetiapine monotherapy to other mood stabilizers

  3. Efficacy and executive function of olanzapine and risperidone in the treatment of elderly patients with schizophrenia%奥氮平与利培酮治疗老年精神分裂症患者疗效及执行功能比较

    Institute of Scientific and Technical Information of China (English)

    杭荣华; 程万良; 王瑞权; 吴明飞

    2012-01-01

    AIM: To explore the difference on efficacy and executive function between olanzapine and risperidone in treatment of elderly patients with schizophrenia. METHODS: 84 eider-ly patients with schizophrenia were randomly divided into olanzapine group (43 cases) and ris-peridon group (41 cases) treated for 8 weeks. The efficacy was assessed with the positive and negative symptoms scale (PANSS) and the executive function was evaluated with Wisconsin Card Sorting Test (WCST) in baseline and after 8 weeks of treatment. RESULTS: After 8 weeks of treatment, the efficacy rate of olanzapine was 90. 6 % . in which 67. 4% was improved markedly. The efficacy rate of risperidon was 92. 6%, in which 68.3% were improved markedly. There were no differences between two groups (P>0. 01). The score of negative symptom of olanzapine group was significantly lower than that of risperidon group(P<0. 05). The score of categories control in risperidon group was significantly lower than that in olanzapine group, persistent errors and response error were higher than that in olanzapine group(P<0. 01). CONCLUSION; Both olanzapine and risperidon can improve the symptom and executive function of elderly patients with schizophrenia. Olanzapine is better than risperidon in improving negative symptom and executive function.%目的:比较奥氮平与利培酮治疗老年精神分裂症的疗效及对执行功能的影响.方法:84例老年精神分裂症患者随机分为奥氮平组(43例)和利培酮组(41例),于治疗前及治疗后第8周末采用阳性与阴性症状量表(PANSS)和威斯康星卡片分类测验( WCST)评定疗效和执行功能,分别比较每组治疗前后及两组间的结果.结果:治疗后奥氮平组的有效率及显效率分别为90.6%和67.4%,利培酮组的有效率及显效率分别为92.6%和68.3%,两者差异无统计学意义(P>0.05).治疗后奥氮平组的阴性症状分低于利培酮组(P<0.01).利培酮组WCST的完成分类数低于奥氮平组,

  4. 奥氮平与喹硫平治疗以阴性症状为主精神分裂症的对照研究%A comparative study of olanzapine and quetiapine in the treatment of negative symptoms of schizophrenia

    Institute of Scientific and Technical Information of China (English)

    张香云; 李广田; 刘忠; 李亚忠; 栗克清; 狄亚琴; 韩彦超; 于雪竹; 高月霞; 黄静; 余红; 梁汝沛

    2012-01-01

    Objective To compare the efficacy and safety of olanzapine in the treatment of negative symptoms of schizophrenia. Methods Eighty patients diagnosed negative symptoms of schizophrenia by DSM -IV were randomly allocated to two groups and treated with olanzapine or quetiapine for 8 weeks, respectively. The efficacy and side effects were evaluated by PANSS, CGI and TESS. Results The significant efficacy rates for the olanzapine and quetiapine groups were 87. 2% and 81. 1%. There was no significant difference in efficacy between the two groups. The rates of side effects were similar in two groups, including lethargy and weight gain. Conclusion The results suggest that olanzapine is as effective and safe as quetiapine for patients with negative symptoms of schizophrenia.%目的 评价国产奥氮平治疗以阴性症状为主的精神分裂症的疗效和安全性.方法 将80例符合DSM-Ⅳ精神分裂症患者随机分为2组,分别给予奥氮平和喹硫平治疗,疗程共8周,用阳性症状与阴性症状量表(PANSS)、临床疗效总评量表(CGI)评定疗效,药物副反应量表(TESS)评定不良反应.结果 奥氮平组显效率87.2%、喹硫平组显效率为81.1%,两药对阴性症状的疗效无显著性差异(P>0.05).2组在治疗过程中出现较多的不良反应是嗜睡、体质量增加,但两者之间无显著性差异(P>0.05).结论 奥氮平对以阴性症状为主的精神分裂症有较好的疗效,与喹硫平的疗效和不良反应相当.

  5. Influences of risperidone,quetiapine,or ziprasidone on metabolic parameters of first-episode schizophrenics%利培酮喹硫平齐拉西酮对首发精神分裂症患者代谢指标的影响

    Institute of Scientific and Technical Information of China (English)

    王明进; 张宗顺; 寻广磊

    2016-01-01

    Objective To explore the influences of risperidone ,quetiapine ,or ziprasidone on metabolic parameters of first‐episode schizophrenics .Methods A total of 120 first‐episode schizophrenics were ran‐domly divided into 3 groups taking orally risperidone ,quetiapine or ziprasidone for 12 weeks .Efficacies were assessed with the Positive and Negative Syndrome Scale (PANSS) before and after treatment ,the changes of blood pressure (BP) ,waist circumference (WC) ,fasting plasma glucose (FPG) ,triacylglycer‐ol (TG) and high density lipoprotein cholesferol (HDL‐c) detected at the same time ,and the incidences of metabolism syndrome at each time point were added up .Results After treatment the total effective rate was respectively 89 .2% in risperidone ,88 .9% in quetiapine and 86 .5% in ziprasidone group ,which showed no significant group differences (P> 0 .05) .Since the end of the 4th week WC ,TG and FPG levels heightened more significantly in risperidone and quetiapine group compared with pretreatment ,so did those of the 3 groups at the end of the 12th week (P<0 .05 or 0 .01) ,HDL‐c levels lowered more significantly in risperidone and quetiapine group compared with pretreatment (P<0 .05);WCs ,TGs and the incidences of metabolic syndrome were significantly higher in risperidone and quetiapine than in ziprasidone group at each time point (P<0 .05 or 0 .01) .Conclusion Risperidone ,quetiapine and ziprasidone are all effective in first‐epi‐sode schizophrenia ,their total efficacies equivalent ,but have different influences on metabolism , risperidone and quetiapine influences are obvious .%目的:探讨利培酮、喹硫平、齐拉西酮对首发精神分裂症患者代谢指标的影响。方法将120例首发精神分裂症患者按随机数字表法分为3组,分别口服利培酮、喹硫平、齐拉西酮治疗,观察12周。于治疗前后采用阳性与阴性症状量表评定临床疗效,同时检测血压、腰围及空腹血糖、三酰

  6. Focus on olanzapine.

    Science.gov (United States)

    Green, B

    1999-01-01

    Olanzapine (2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine) is a novel antipsychotic agent of the theinobenzodiazepine class developed by Eli Lilly & Co. It has a pleotrophic pharmacology and affects the dopaminergic, serotonergic, muscarinic and adrenergic systems. The therapeutic advantage of recent antipsychotics (so-called atypical antipsychotics) has been attributed to additional serotonergic effects. Clinical studies and trials suggest that olanzapine is comparable or superior to haloperidol and may be superior to risperidone in terms of efficacy and side-effect profiles. The starting dose of olanzapine is a single dose of 10 mg. The drug reaches peak plasma levels in 5-8 h, and has a half-life of about 35 h, depending on metabolism. The recommended maximum dose is 20 mg daily, but higher doses have been employed. Abnormalities of the QTc interval on ECG are unlikely to occur and so there is no need for a baseline ECG as with sertindole, which has recently been withdrawn. The most common side-effects are somnolence and weight gain. About 40% of patients in clinical trials gain weight--especially if they are on a high starting dose and if they were underweight pre-treatment. Reported evidence to date suggests that olanzapine is relatively less likely to produce sexual dysfunction. In general, weight gain and sexual dysfunction are of great concern to people taking antipsychotics and the side-effect profile of any antipsychotic may affect compliance. Olanzapine's general efficacy and side-effect profile suggest that, unforeseen post-marketing complications notwithstanding, olanzapine deserves a major place in the first-line management of psychotic disorders.

  7. 奥氮平与利培酮治疗痴呆患者精神行为症状的对照研究%The comparative study of olanzapine and risperidone in the treatment of dementia patients with behavioral and psychological symptoms

    Institute of Scientific and Technical Information of China (English)

    黄文平; 赵祖安; 白玉红; 曾丽苹

    2012-01-01

    Objective To observe the efficacy and safety of Olanzapine and Risperidone in the treatment of dementia patients with behavioral and psychological symptoms. Methods 80 senile dementia patients were selected and divided into two groups randomly, Olanzapine group (40 cases) and Risperidone group (40 cases). Before the treatment and the treatment for two, four and eight weeks, the two groups were both given the BEHAVE-AD scale to evaluate the efficacy and TESS scale to evaluate the adverse reactions. Results In the treatment of the 8th week, the differences of all the BE-HAVE-AD scales compared with before the treatment in the two groups were statistically significant (P < 0.01). In the treatment of the 2nd week, the difference of total scales compared with before the treatment in the Olanzapine group was statistically significant (P < 0.01), the Risperidone group was not; but at the 8th week the difference of efficiency rate between the two groups was not statistically significant. In security, the difference of total adverse reactions rate was not statistically significant, but the incidence of extrapyramidal side effects (EPS) in the Risperidone group was higher than in the Olanzapine group(P < 0.05). Conclusion The efficacy of Olanzapine and Risperidone in the treatment of dementia patients with behavioral and psychological symptoms are equal, but Olanzapine works faster, side effects are less, so Olanzapine is more suitable to treat dementia patients with behavioral and psychological symptoms.%目的 观察奥氮平和利培酮治疗老年痴呆患者精神行为症状的疗效和安全性.方法 将80例老年痴呆患者随机分为奥氮平组和利培酮组,每组各40例,共观察8周.治疗前及治疗第2、4、8周末分别用BEHAVE-AD量表评定疗效,用TESS量表评定不良反应.结果 奥氮平组和利培酮组在治疗第8周末,BEHAVE-AD量所有项目评分与治疗前比较,差异均有高度统计学意义(均P < 0.01),

  8. Movement disorders in elderly users of risperidone and first generation antipsychotic agents: a Canadian population-based study.

    Directory of Open Access Journals (Sweden)

    Irina Vasilyeva

    Full Text Available BACKGROUND: Despite concerns over the potential for severe adverse events, antipsychotic medications remain the mainstay of treatment of behaviour disorders and psychosis in elderly patients. Second-generation antipsychotic agents (SGAs; e.g., risperidone, olanzapine, quetiapine have generally shown a better safety profile compared to the first-generation agents (FGAs; e.g., haloperidol and phenothiazines, particularly in terms of a lower potential for involuntary movement disorders. Risperidone, the only SGA with an official indication for the management of inappropriate behaviour in dementia, has emerged as the antipsychotic most commonly prescribed to older patients. Most clinical trials evaluating the risk of movement disorders in elderly patients receiving antipsychotic therapy have been of limited sample size and/or of relatively short duration. A few observational studies have produced inconsistent results. METHODS: A population-based retrospective cohort study of all residents of the Canadian province of Manitoba aged 65 and over, who were dispensed antipsychotic medications for the first time during the time period from April 1, 2000 to March 31, 2007, was conducted using Manitoba's Department of Health's administrative databases. Cox proportional hazards models were used to determine the risk of extrapyramidal symptoms (EPS in new users of risperidone compared to new users of FGAs. RESULTS: After controlling for potential confounders (demographics, comorbidity and medication use, risperidone use was associated with a lower risk of EPS compared to FGAs at 30, 60, 90 and 180 days (adjusted hazard ratios [HR] 0.38, 95% CI: 0.22-0.67; 0.45, 95% CI: 0.28-0.73; 0.50, 95% CI: 0.33-0.77; 0.65, 95% CI: 0.45-0.94, respectively. At 360 days, the strength of the association weakened with an adjusted HR of 0.75, 95% CI: 0.54-1.05. CONCLUSIONS: In a large population of elderly patients the use of risperidone was associated with a lower risk of EPS

  9. Quetiapine treatment in youth is associated with decreased insulin secretion.

    Science.gov (United States)

    Ngai, Ying Fai; Sabatini, Paul; Nguyen, Duc; Davidson, Jana; Chanoine, Jean-Pierre; Devlin, Angela M; Lynn, Francis C; Panagiotopoulos, Constadina

    2014-06-01

    Second-generation antipsychotics (SGAs) are commonly prescribed to youth but are associated with metabolic effects including obesity and diabetes. The mechanisms underlying diabetes development are unclear. The purpose of this study was to compare glucose homeostasis, insulin sensitivity, insulin secretion, and overall β-cell function in risperidone-treated, quetiapine-treated, and SGA-naive youth with mental illness. We conducted a cross-sectional study in which youth aged 9 to 18 years underwent a 2-hour oral glucose tolerance test. Indices for insulin sensitivity (Matsuda index), insulin secretion (insulinogenic index), and β-cell function (insulin secretion-sensitivity index-2 [ISSI-2]) were calculated. A total of 18 SGA-naive, 20 risperidone-treated, and 16 quetiapine-treated youth participated. The 3 groups were similar in age, sex, ethnicity, body mass index standardized for age and sex, pubertal status, degree of psychiatric illness, psychiatric diagnoses, and other medications. The median treatment duration was 17 months (range, 3-91 months) for risperidone-treated youth and 10 months (range, 3-44 months) for quetiapine-treated youth. The quetiapine-treated group had lower insulinogenic index (P youth. Quetiapine treatment was negatively associated with insulinogenic index (β = -0.426, P = 0.007) and ISSI-2 (β = -0.433, P = 0.008). Quetiapine reduced the insulin expression in isolated mouse islets suggesting a direct β-cell effect. Our results suggest that quetiapine treatment in youth is associated with impaired β-cell function, specifically lower insulin secretion. Prospective longitudinal studies are required to understand the progression of β-cell dysfunction after quetiapine initiation.

  10. A controlled study on effect of olanzapine and risperidone on quality of life in first-episode schizophrenia patients%奥氮平与利培酮治疗精神分裂症首次发病患者的疗效

    Institute of Scientific and Technical Information of China (English)

    徐彩; 李美银; 邓文

    2012-01-01

    目的:探讨奥氮平与利培酮治疗首发精神分裂症的疗效以及对生活质量的影响. 方法:68例首发精神分裂症患者随机分为奥氮平组和利培酮组各34例,分别给予奥氮平和利培酮治疗8周,随访6个月.于治疗前后采用阳性与阴性症状量表(PANSS)及治疗中出现的症状量表(TESS)评定疗效及不良反应;于治疗6个月前后,采用生活质量综合评定问卷(GQOLI)评定生活质量. 结果:两组PANSS评分治疗后均有显著下降(P<0.05或P<0.01).奥氮平组GQOLI总分及各维度与利培酮组GQOLI总分及躯体功能、心理功能维度治疗前后差异均有统计学意义(P均<0.01);两组间比较,治疗前两组GQOLI评分差异无统计学意义,6个月后随访,在躯体功能及社会功能差异有统计学意义(P均<0.01). 结论:奥氮平与利培酮治疗首发精神分裂症疗效相当,但奥氮平在提高生活质量方面略优于利培酮.%Objective: To study the curative powers and effect of olanzapine and risperidone on quality of life in the treatment of first onset schizophrenia patients. Method: 68 first onset schizophrenia patients were randomly divided into olanzapine group and risperidone group, each of which (n = 34 ) received the olanzapine or risperidone treatment respectively for 8 weeks and 6 months follow-up. The efficacy was assessed using positive and negative syndrome scales (PANSS) , and the adverse reaction using treatment emergent symptom scale (TESS). Generic quality of life inventory (GQOLI) was conducted before and 6 months after the treatment for assessmet of patients quality of life. Results: PANSS score of two groups decreased singnificanty after the treatment ( P < 0.05 or P < 0.01). The significant differences were found on GQOLI total score and each dimension score in olanzeoine group and GQOLI total score, physical function,psychological function in risperidone group between before and after treatment (all P<0.01). After 6

  11. A control of schizophrenia ’ s metabolic syndrome caused by olanzapine and risperidone%奥氮平与利培酮治疗精神分裂症所致代谢综合征对照研究

    Institute of Scientific and Technical Information of China (English)

    于君; 郝增平; 徐鹏波; 王志敏; 林晓东; 孙军伟; 李红梅

    2014-01-01

    Objective To explore schizophrenia’s metabolic syndromes caused by olanzapine and risperi-done .Methods Eighty-six schizophrenics were randomly assigned to two groups taking orally olanzapine or risperidone for 12 weeks .Mental symptoms were assessed with the Positive and Negative Syndrome Scale (PANSS) before and after treatment and changes of BP ,body height (BH) ,body mass (BM) ,waist circumference (WC) ,fasting blood sugar (FBS) and blood fit (BF) detected simultaneously .Results Af-ter treatment the PANSS scores of both groups lowered more significantly compared with pretreatment (P0 .05) .Af-ter treatment BM and BMI of both groups increased more significantly ,FBS ,triacylglycerol ,total choles-terol (TC) ,LDL levels heightened and HDL lowered ,and differences had significances since the end of the 8th week (P0 .05) .There were no significant group differences in over-standard WC ,the elevation of FBS ,tria-cylglycerol .TC and LDL ,the reduction of HDL and the detection rate of metabolic syndrome (P>0 .05) . Conclusion Olanzapine and risperidone have therapeutic equivalence in schizophrenia ,different influences on patients’ glucose and lipid metabolism and the risk of causing metabolic syndromes ,so clinically all metabolic indexes should be closely watched .%目的:探讨奥氮平与利培酮治疗精神分裂症导致代谢综合征的发生状况。方法将86例精神分裂症患者随机分成两组,分别口服奥氮平及利培酮治疗,观察12周。于治疗前后采用阳性与阴性症状量表评定精神症状,同时检测血压、身高、体质量、腰围及空腹血糖、血脂水平的变化。结果治疗后两组阳性与阴性症状量表评分均较治疗前显著下降( P<0.05或0.01),治疗各时段两组评分比较差异均无显著性(P>0.05)。治疗后两组体质量及体质量指数均较治疗前显著增加,空腹血糖、三酰甘油、总胆固醇、低密度脂

  12. 奥氮平与利培酮治疗老年痴呆伴精神行为症状对照观察%A control study of olanzapine vs .risperidone in senile demen-tia with behavioral and psychological symptoms

    Institute of Scientific and Technical Information of China (English)

    韩曙林; 孟红凤

    2015-01-01

    目的:比较奥氮平与利培酮治疗老年痴呆伴精神行为症状患者的疗效及安全性。方法将52例老年痴呆伴精神行为症状患者随机分为奥氮平组与利培酮组,分别予以奥氮平与利培酮治疗,观察8周。治疗前后采用痴呆病理行为评定量表、副反应量表评定临床疗效及不良反应。结果奥氮平组治疗第2周末起,利培酮组治疗第4周末起痴呆病理行为评定量表评分较治疗前显著降低(P<0.01),治疗第2周末奥氮平组显著低于利培酮组(P<0.05或0.01);奥氮平组有效率为92.3%,利培酮组为88.5%,两组比较差异无显著性( P>0.05);奥氮平组不良反应发生率显著低于利培酮组(P<0.05)。结论奥氮平与利培酮治疗老年痴呆伴精神行为症状患者疗效显著且相当,但奥氮平起效更快,安全性更高。%Objective To compare the efficacy and safety between olanzapine and risperidone in senile de‐mentia with behavioral and psychological symptoms (BPS) .Methods Fifty‐two senile dementia patients with BPS were randomly assigned to olanzapine and risperidone group treated with olanzapine or risperi‐done for 8 weeks .Efficacies were assessed with the Rating Scale of the Behavioral Pathology in Alzheime‐r′s Disease (BEHAVE‐AD) before and after treatment and adverse reactions with the Treatment Emergent Symptom Scale (TESS) .Results The BEHAVE‐AD score lowered more significantly since the end of the 2nd week in olanzapine group and since the 4th in risperidone group compared with pretreatment (P0 .05);the incidence of adverse reactions was significantly lower in olanzapine than in ris‐peridone group (P<0 .05) .Conclusion Both olanzapine and risperidone have an equivalent and evident effect in senile dementia with BPS ,but the former takes effect more rapidly and has higher safety .

  13. Comparative analysis of treatment with Olanzapine and Quetiapine on behavioral and psychological symptoms of patients with Alzheimer's%奥氮平和喹硫平治疗老年期痴呆患者精神行为症状的对比分析

    Institute of Scientific and Technical Information of China (English)

    徐燕

    2015-01-01

    目的:探讨奥氮平和喹硫平治疗老年期痴呆患者精神行为症状的临床疗效与不良反应。方法将我院收治的120例老年期痴呆患者随机分为奥氮平组与喹硫平组,每组60例,奥氮平组使用奥氮平,初始剂量2.5 mg/d,4周内逐渐增至5~15 mg/d;喹硫平组应用喹硫平,初始剂量25 mg/d,4周内逐渐增至200~400 mg/d。比较2组患者治疗前后的BEHAVE-AD、MMSE。结果2组患者治疗后BEHAVE-AD、MMSE及ADL评分均较治疗前明显改善(P0.05);2组患者的嗜睡、头晕、便秘、震颤、静坐不能、直立性低血压、失眠比较无统计学差异(P>0.05),奥氮平组患者的口干、体重增加、锥体外系反应明显多于喹硫平组,2组比较差异显著(P0.05);there was no significant difference in somnolence, dizziness,constipation,tremor,akathisia,orthostatic hypotension and between the two groups (P>0.05);the dry mouth, weight gain and extrapyramidal reactions of the patients of Olanzapine Group were significantly more that of the Quetiapine Group,there was significant difference between the two groups (P<0.01).Conclusions Both of Olanzapine and quetiapine can achieve satisfactory results on treatment for patients with Alzheimer's,with fewer adverse reactions, therefore they are worthy of clinical application.

  14. Change in level of productivity in the treatment of schizophrenia with olanzapine or other antipsychotics

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    Osuntokun Olawale

    2011-05-01

    Full Text Available Abstract Background When treating schizophrenia, improving patients' productivity level is a major goal considering schizophrenia is a leading cause of functional disability. Productivity level has been identified as the most preferred treatment outcome by patients with schizophrenia. However, little has been done to systematically investigate productivity levels in schizophrenia. We set out to better understand the change in productivity level among chronically ill patients with schizophrenia treated with olanzapine compared with other antipsychotic medications. We also assessed the links between productivity level and other clinical outcomes. Methods This post hoc analysis used data from 6 randomized, double-blind clinical trials of patients with schizophrenia or schizoaffective disorder, with each trial being of approximately 6 months duration. Change in productivity level was compared between olanzapine-treated patients (HGBG, n = 172; HGHJ, n = 277; HGJB, n = 171; HGLB, n = 281; HGGN, n = 159; HGDH, n = 131 and patients treated with other antipsychotic medications (separately vs. haloperidol [HGGN, n = 97; HGDH, n = 132], risperidone [HGBG, n = 167; HGGN, n = 158], quetiapine [HGJB, n = 175], ziprasidone [HGHJ, n = 271] and aripiprazole [HGLB, n = 285]. Productivity was defined as functional activities/work including working for pay, studying, housekeeping and volunteer work. Productivity level in the prior 3 months was assessed on a 5-point scale ranging from no useful functioning to functional activity/work 75% to 100% of the time. Results Chronically ill patients treated with olanzapine (OLZ experienced significantly greater improvement in productivity when compared to patients treated with risperidone (RISP (OLZ = 0.22 ± 1.19, RISP = -0.03 ± 1.17, p = 0.033 or ziprasidone (ZIP (OLZ = 0.50 ± 1.38, ZIP = 0.25 ± 1.27, p = 0.026, but did not significantly differ from the quetiapine, aripiprazole or haloperidol treatment groups. Among

  15. Efficacy and safety study of Olanzapine or Quetiapine joint Donepezil in the treatment of behavioral and psychological symptoms of dementia%奥氮平或喹硫平联合多奈哌齐治疗老年痴呆精神行为症状的疗效和安全性研究

    Institute of Scientific and Technical Information of China (English)

    张玉琦; 徐文炜; 程灶火; 吴越; 顾君; 汤莉; 季萍; 李桂林

    2012-01-01

    目的 探讨奥氮平或喹硫平联合多奈哌齐治疗老年痴呆精神行为症状的疗效和安全性.方法 将103例伴精神行为症状的痴呆患者随机分为奥氮平联合多奈哌齐组(A组)与喹硫平联合多奈哌齐组(B组).治疗前和研究结束时进行简易智力状态检查(MMSE)评分.在治疗后的第2、4、6、8周末以痴呆病理行为评定量表(BEHAVE-AD)减分率评定疗效,以副反应量表(TESS)记录治疗中各项药物不良反应.结果 两组MMSE评分均较治疗前提高2分以上,治疗结束后两组组内比较,差异均有统计学意义(均P < 0.05).治疗前后BEHAVE-AD量表评分两组组内比较,至第4周末时均明显下降,差异有高度统计学意义(均P < 0.01).A组有效率为88.46%(46/52),显著有效率为67.31%(35/52);B组有效率为86.27%(44/51),显著有效率为64.71%(33/51),两组疗效比较差异无统计学意义(P > 0.05).两组均无不能耐受的不良药物反应.结论 奥氮平或喹硫平联合多奈哌齐治疗老年痴呆精神行为症状安全有效.%Objective To investigate the efficacy and safety of Olanzapine or Quetiapine joint Donepezil in the treatment of Alzheimer's behavioral and psychological symptoms. Methods 103 patients with behavioral and psychological symptoms of dementia patients were randomly divided into a combination of Olanzapinewith Donepezil group (group A) and the Quetiapine with Donepezil group (group B). The mini-mental state examination (MMSE) scores were evaluated before treatment and the end of the study. The efficacies were evaluated in 2, 4, 6, 8 weekend of the treatment by reduced rate of the behavioral pathology in Alzheimer's disease scale (BEHAVE-AD), the treatment emergent symptom scale (TESS) was used to record the adverse reactions. Results Two sets of MMSE scores than before treatment, increased by more than two scores after the end of the treatment within the two groups were statistically significant different (all P 0

  16. Effect comparison of olanzapine and risperidone treating patients with Alzheimer disease associated with psychiatric symptom%奥氮平与利培酮治疗阿尔茨海默病患者伴精神行为症状的效果比较

    Institute of Scientific and Technical Information of China (English)

    钟华; 刘少华

    2015-01-01

    Objective To compare the effect of olanzapine and risperidone treating patients with Alzheimer disease as-sociated with psychiatric symptom. Methods 68 patients with Alzheimer disease received by our hospital from January 2013 to January 2015 of our hospital were selected as study object and were randomly divided into observation group and control group.Observation group was treated by olanzapine and control group was treated by risperidone. Clinical effect of patients in two groups was compared. Results The total effective rate of observation group was 91.2% and the control group was 88.2%,and there was no statistical difference (P>0.05).After treatment,the total score of BEHAVE-AD and BPRS of patients in two groups had no statistical difference when compared with before treatment (P0.05).The incidence rate of adverse reaction in observation group was 20.6% and the control group was 50.0%,and there was a statistical difference (P0.05)。治疗后,两组患者的痴呆病理行为评定量表(BEHAVE-AD)总分、简明神经精神量表(BPRS)总分与治疗前比较,差异有统计学意义(P0.05)。观察组的不良反应发生率为20.6%,对照组为50.0%,两组的不良反应发生率比较,差异有统计学意义(P<0.05)。结论奥氮平与利培酮治疗阿尔茨海默病伴精神行为症状患者具有良好效果,但奥氮平药物起效快,且安全性高。

  17. Costs and efficacy ofolanzapine and risperidone in schizophrenia

    Directory of Open Access Journals (Sweden)

    Vittorio Mapelli

    2007-06-01

    Full Text Available Introduction: schizophrenia is a serious and long lasting psychiatric disease. The new “atypical” antipsychotic drugs, introduced in the 90s, have substantially improved the effectiveness of medical treatments, compared to previous neuroleptic drugs. Nowadays they tend to be used as first choice drugs. The ddd cost of atypicals may differ by 20% and health authorities may have an incentive to deliver the less costly drug, especially if they are generic. However the various drugs show differential effectiveness rates and a rational choice should consider both cost and effectiveness.
Objective: the purpose of this analysis is to review the existing evidence on cost-effectiveness studies of olanzapine and risperidone, the two most prescribed drugs in Italy. Six published studies were identified, but attention was focused on two articles that reported consistent and methodologically sound results.
Results: most reviewed studies are cost-minimization analyses, since effectiveness indicators show no significant statistical difference between the two drugs, and are inconclusive since the results depend on the evaluation setting. However one observational retrospective study showed a significant severity reduction over 12 months for patients treated with olanzapine (-2.46 on HoNOS scale; p<0.05, compared to a smaller non significant reduction of the risperidone group (-0.57. Despite the higher drug cost, the average total cost per reduced severity score was lower for olanzapine than for risperidone patients (€ 4,554 vs. € 10,897. The only medical and related health care costs for risperidone patients were higher than total costs for olanzapine patients. Another study comparing cohorts of patients with similar starting severity showed a significant severity reduction and global functioning increase over 12 months for olanzapine but no significant increase for risperidone patients (-0.35, p<0.01 on CGI scale; +3.66, p <0.05 on GAF scale

  18. [Quetiapine-induced leucopenia].

    Science.gov (United States)

    Penninga, Elisabeth I; Dalhoff, Kim Peder; Lykkegaard, Signe E

    2008-09-08

    We describe the case of a 20-year-old man with schizophrenia who was treated with the dibenzothiazepine antipsychotic drug quetiapine in oral doses of 900 mg daily. At admission the patient had a normal blood count. 15 weeks after initiation of treatment asymptomatic cytopenia was discovered with leucocytes of 2.2 billion/l and thrombocytes of 114 billion/l. Two weeks after discontinuation of quetiapine the leucopenia subsided. Physicians should be aware of leucopenia as a potential adverse effect to quetiapine, especially in patients with symptoms of infections or cytopenia.

  19. 利培酮和氯氮平、喹硫平对精神分裂症患者脂代谢影响比较%Risperidone and clozapine, quetiapine impact on lipid metabolism in patients with schizophrenia

    Institute of Scientific and Technical Information of China (English)

    胡红霞; 赵倩; 白天山; 崔素华; 任玉红; 王旭红; 李小全

    2012-01-01

    Objective: To study the influence of risperdal, clozapine and quetiapine on blood -lipid level of patients with schizophrenia. Methods:178 cases of schizophrenia patients were randomly divided into risperdal group ( 90 cases ) , clozapine group ( 68 cases) , quetiapine group ( 20 cases ). Before treatment and treatment at the fourth and eighth, weekend, the levels of total cholesterol (TC) , triglycerides (TG), high - density iipoprotein (HDL), low density Iipoprotein (LDL) , apolipoprotein A ( ApoA) , apolipoprotein B ( ApoB) in the fasting plasma were determined. Results: CHOL level had statistical difference in clozapine group before and after treatment(P 0,05). Other indicators had no significant difference before and after treatment(P > 0.05 ) . The effect of clozapine on TG and CHOL were greater than that of risperdal. Conclusion: Risperdal and clozapine both had effect on blood - lipid of patients with schizophrenia, and clozapine had greater effect on lipid metabolism than risperdal, while quetiapine had the least effect.%目的:探讨利培酮、氯氮平与喹硫平对精神分裂症患者血脂的影响.方法:将178例精神分裂症患者随机分为利培酮组90例,氯氮平组68例,喹硫平组20例;于治疗前及治疗第4、8周末晨间空腹采血,测定总胆固醇(TC)、甘油三脂(TG)、高密度脂蛋白(HDL)、低密度脂蛋白(LDL)、载脂蛋白A(ApoA)、载脂蛋白B(ApoB).结果:治疗前后氯氮平组的CHOL差异均有统计学意义(P<0.05),TG较治疗前显著升高(P<0.01);利培酮组TG浓度差值(0.58 ±0.41) mmol/L,差异有统计学意义(P<0.05).喹硫平组TG浓度差值(0.16 ±0.20) mmol/L,无统计学差异(P>0.05).其他各项指标与治疗前比较差异无显著性(P>0.05).氯氮平和利培酮对TG、CHOL的影响程度氯氮平大于利培酮.结论:利培酮与氯氮平对精神分裂症患者血脂均有影响,氯氮平对脂代谢的影响大于利培酮,喹硫平最低.

  20. Clinical observation of aripiprazole orally disintegrating tablets in the improvement of women's weight,prolactin increase caused by risperidone,sulpiride,olanzapine%阿立哌唑口腔崩解片改善利培酮、舒必利、奥氮平致女性体重、泌乳素增加的临床观察

    Institute of Scientific and Technical Information of China (English)

    卓子禄; 王群英; 熊英; 胡俊英

    2015-01-01

    目的:探讨阿立哌唑口腔崩解片改善利培酮、舒必利、奥氮平等精神类药物所致体重、泌乳素增加的临床效果。方法:收治因服用利培酮、舒必利、奥氮平等精神类药物后引起体重增加及高催乳素血症患者60例,所有患者均维持原抗精神类药物的治疗方案,根据随机数字表将患者分为阿立哌唑口腔崩解片组(观察组)30例和安慰剂组(对照组)30例,两组患者干预12周后测量患者体质指数(BMI)变化及催乳素(PRI)的水平,同时采用不良反应量表(TESS)评定阿立哌唑口腔崩解片治疗的不良反应。结果:与对照组相比,观察组治疗后 BMI 及PRL 显著下降,差异有统计学意义(P<0.01)。观察组总有效率93.33%,对照组总有效率76.67%,两组比较有统计学意义(P<0.05)。TESS 评分观察组(5.12±1.12)分,对照组(4.98±1.08)分,两组比较差异无统计学意义(P>0.05)。结论:阿立哌唑口腔崩解片能有效改善利培酮、舒必利、奥氮平等抗精神病药所致体重、泌乳素增加症状,且安全、可靠,值得临床应用和推广。%Objective:To explore the clinical effect of aripiprazole orally disintegrating tablets in the improvement of women's weight,prolactin increase caused by sulpiride,risperidone,olanzapine.Methods:60 cases of weight gain and hyperprolactinemic patients caused by sulpiride,risperidone,olanzapine were selected.All patients maintained antipsychotic drug treatment scheme of the original.According to the random number table,they were divided into the aripiprazole orally disintegrating tablets group(observation group) with 30 cases and the placebo group(control group) with 30 cases.After 12 weeks of treatment,we measured body mass index patients(BMI) changes and prolactin(PRI) level.At the same time,we evaluated the adverse reactions of aripiprazole orally disintegrating tablets treatment using side effects scale

  1. Comparison of the Effcacy of Olanzapine and Risperidone in the Treatment of Behavioral and Psychological Symptoms of Dementia%奥氮平与利培酮治疗老年痴呆精神行为症状的疗效比较

    Institute of Scientific and Technical Information of China (English)

    孙玮

    2016-01-01

    Objective To comparison of olanzapine and risperidone in the treatment of the clinical effcacy of behavioral and psychological symptoms of dementia, study of olanzapine clinical value.MethodsFrom March 2010 to May 2015, 92 cases of senile dementia patients were selected, according to the order of admission, the patients were divided into observation group and control group, 46 cases in each group. Patients in the control group were given risperidone in the treatment, experimental group given olanzapine for the treatment of drug and using Tess analysis of two groups in the treatment process of adverse reactions occurred, and compared between the two groups of patients for half a month, one month and two months after treatment.Results The scores of PANSS in observation group and 1 months after treatment, the total effective rate was signiifcantly higher than that of the control group, the difference was statistically significant (P<0.05). The incidence of adverse reactions in the observation group was lower than that in the control group, which had statistical signiifcance (P<0.05).Conclusion Olanzapine treatment effect better, fast effect, clinical adverse reactions less for elderly behavioral and psychological symptoms of dementia treatment.%目的:对比奥氮平与利培酮治疗老年痴呆精神行为症状的临床疗效,探讨奥氮平的临床治疗价值。方法从我院2010年3月~2015年5月收治的老年痴呆症患者中选择92例,根据入院顺序将患者平分为观察组和对照组各46例。对照组给予利培酮药物治疗,实验组给予奥氮平药物治疗,使用TESS量表分析两组在治疗过程中的不良反应发生情况,并比较两组患者的半个月、一个月和2个月后的治疗效果。结果观察组治疗半个月和1个月后的PANSS量表评分、治疗总有效率高于对照组,对比差异具有统计学意义(P<0.05)。观察组各项不良反应发生率均低于对照组,对

  2. Olanzapine-induced ischemic colitis

    Directory of Open Access Journals (Sweden)

    Esteban Sáez-González

    Full Text Available Background: Ischemic colitis (IC is an uncommon adverse event associated with antipsychotic agents, more commonly found with phenothiazine drugs and atypical neuroleptics such as clozapine. The risk of developing ischemic colitis increases when anticholinergic drugs are associated. Case report: We report the case of a 38-year-old woman with a history of schizoaffective disorder who had been on chronic quetiapine for 3 years, and presented to the ER because of diarrhea for 5 days. Four months previously, olanzapine had been added to her psychiatric drug regimen. Physical examination revealed abdominal distension with abdominal tympanic sounds and tenderness. Emergency laboratory tests were notable for increased acute phase reagents. Tomography revealed a concentric thickening of the colonic wall in the transverse, descending and sigmoid segments, with no signs of intestinal perforation. Colonoscopy demonstrated severe mucosal involvement from the sigmoid to the hepatic flexure, with ulcerations and fibrinoid exudate. Biopsies confirmed the diagnosis of ischemic colitis. The only relevant finding in her history was the newly added drug to her baseline regimen. An adverse effect was suspected because of its anticholinergic action at the intestinal level, and the drug was withdrawn. After 6 months of follow-up clinical, laboratory and endoscopic recovery was achieved. Discussion: Antipsychotic medication should be considered as a potential cause of ischemic colitis, particularly atypical antipsychotics such as clozapine and olanzapine; despite being uncommon, this adverse event may result in high morbidity and mortality.

  3. Risperidone Injection

    Science.gov (United States)

    ... control slow movements or shuffling walk falling painful erection of the penis that lasts for hours Risperidone extended-release injection may cause other side effects. Call your doctor if you have any unusual problems while receiving this medication.If you experience a ...

  4. Cognitive effectiveness of risperidone and olanzapine in first-episode schizophrenia%利培酮和奥氮平对首发精神分裂症患者治疗前后认知功能的对比观察

    Institute of Scientific and Technical Information of China (English)

    赵瑾; 吕路线; 张燕; 晁阳阳; 马骏; 杨勇锋; 赵晶媛; 杜云红; 李文强; 宋学勤

    2016-01-01

    目的:观察首发精神分裂症患者部分认知功能领域损害情况以及利培酮和奥氮平对其治疗前后认知功能的潜在作用。方法选取2015年1—10月在新乡医学院第二附属医院住院治疗的57例首发精神分裂症患者和周边社区年龄、性别匹配的30名健康人(健康对照组),采用随机数字表法将患者分为2组,分别给予利培酮和奥氮平单一治疗。因不良反应难以耐受、药物疗效不佳、换用药物共脱落4例,53例患者完成研究。患者组分别于治疗前和治疗8周后评估患者临床症状(PANSS)和认知功能(连线测试、符号编码、言语记忆、工作记忆、Stroop 测试),健康对照组仅评估一次。结果 PANSS 减分率对比两组并无显著差异。治疗前,利培酮组和奥氮平组均较健康对照组表现出显著的操作速度、言语记忆(t =3.191,t =3.743)、工作记忆(t =2.151,t =2.602)和执行功能领域的差异(P <0.05);经过8周的抗精神病药物治疗,利培酮治疗组表现出连线测试(t =3.862, P <0.05)、言语记忆领域(t =-3.073,P <0.05)功能的改善,奥氮平治疗组表现出连线测试(t =3.587,P <0.05)和工作记忆(t =-2.891,P <0.05)功能的改善。抗精神病药物剂量与认知功能减分率相关分析发现利培酮服用剂量与患者连线测试减分率呈负相关(r =-0.391,P =0.048)。结论利培酮和奥氮平对首发精神分裂症患者临床症状和整体认知功能在8周内作用差异无统计学意义,首发精神分裂症患者存在显著的认知功能损害,利培酮和奥氮平能够在改善精神症状的同时一定程度上改善患者的某些认知领域损害,利培酮服用剂量越大,操作速度领域改善情况越差。%Objective To study the impairments of cognitive function in first-episode schizophrenia and the potential effectiveness of risperidone and olanzapine

  5. Long-acting injectable antipsychotics: focus on olanzapine pamoate

    Directory of Open Access Journals (Sweden)

    JP Lindenmayer

    2010-05-01

    Full Text Available JP LindenmayerDepartment of Psychiatry, New York University School of Medicine, New York NY, USAAbstract: Medication non-adherence in patients with schizophrenia continues to be a significant problem and threatens successful treatment outcomes. Medication non-adherence is often associated with negative consequences, including symptom exacerbation, more frequent emergency room visits, re-hospitalizations and relapse. Long-acting injectable (LAI forms of antipsychotics allow for rapid identification of non-adherence, obviate the need for the patient to take the medication on a daily basis and increase adherence to some significant degree. Eli Lilly has developed a long-acting depot formulation of olanzapine, olanzapine pamoate, which has recently been approved by the FDA for the US market, and which will be reviewed here. Olanzapine LAI appears to be an effective antipsychotic at dosages of 210 mg every 2 weeks, 300 mg every 2 weeks and 405 mg every 4 weeks in patients with acute schizophrenia, and at 150 mg every 2 weeks, 300 mg every 2 weeks and at 405 mg every 4 weeks for the maintenance treatment of stable patients. Oral supplementation appears not to be needed, particularly not at the onset of treatment with the LAI as is necessary with risperidone LAI. Its efficacy is in general comparable to the efficacy seen with oral olanzapine at a corresponding dose. The side effect profile is also comparable to the side effects observed with oral olanzapine, including lower rates of extrapyramidal symptoms, prolactin elevation and cardiovascular side effects, but significant metabolic effects. The latter include significant weight gain, lipid abnormalities and glucose dysregulation. While the injection site adverse events are overall mild, the most significant serious adverse event is the post-injection delirium sedation syndrome (PDSS. While rare, this syndrome results from inadvertent intravascular injection of olanzapine LAI and can cause a range of

  6. Comparative Study on the Efficacy and Safety of Olanzapine and Risperidone in the Treatment of Behavioral and Psychological Symptoms of Dementia%奥氮平与利培酮治疗痴呆精神行为症状的疗效及安全性比较研究

    Institute of Scientific and Technical Information of China (English)

    梁静涛; 吴丽娟

    2016-01-01

    目的探讨奥氮平与利培酮治疗痴呆精神行为症状的临床效果以及安全性。方法将我院2013年1月~2014年1月收治的70例患有痴呆精神行为症状的患者随机分成对照组和治疗组,对照组行利培酮进行治疗,治疗组行奥氮平进行治疗,比较两组患者的治疗效果。结果治疗后,治疗组总有效率为85.71%,对照组为91.43%,对比显示差异无统计学意义(>0.05);与治疗前相比,两组患者治疗2、4、8w后的BEHAVE-AD评分均有明显改善,且差异显示具有统计学意义(0.05);治疗组不良反应率为11.43%,明显低于对照组的31.43%,且差异显示具有统计学意义( 0.05); compared with before treatment, the two groups of patients after treatment BEHAVE 2,4,8w -AD scores showed significant improvement, and show a statistically significant difference ( 0.05); adverse reaction rate was 11.43% in treatment group was significantly 31.43% lower than the control group, and the difference was statistically significant display ( <0.05). Conclusion Olanzapine and risperidone behavioral and psychological symptoms of dementia have some clinical effect, but Olanzapine security even more significant, can reduce the incidence of adverse events, help patients get better treatment, worthy of promotion.

  7. Potentiating effect of fluphenazine decanoate and risperidone on development of neuroleptic malignant syndrome.

    Science.gov (United States)

    Liu, Pang-Yen; Wu, Pei-Chuan; Chen, Chun-Yen; Chen, Yi-Chyan

    2011-01-01

    We present the case of a woman with paranoid schizophrenia who was receiving oral risperidone. She developed neuroleptic malignant syndrome (NMS) following the addition of depot fluphenazine for the treatment of refractory delusions. NMS subsided and psychotic features were controlled after both antipsychotics were discontinued and the patient was treated instead with olanzapine.

  8. 利培酮口服液与奥氮平治疗老年痴呆精神行为症状的疗效比较%Comparison efficacy of risperidone oral solution and olanzapine in the treatment of elderly dementia behavioral and psychological symptoms

    Institute of Scientific and Technical Information of China (English)

    曲春晖; 孙平; 孙忠国

    2016-01-01

    Objective To discuss the clinical value and safety of risperidone oral solution and olanzapine in treatment of elderly dementia behavioral and psychological symptoms (BPSD).Methods 120 patients with BPSD were randomly divided into research group and control group ,each of 60 cases.Research group were treated with risperidone oral solution ,control group were treated with olanzapine ,the treatment course was 8 weeks.Used BEHAVE-AD to evaluate the efficacy ,evaluated the agitated behavior improvement by CMAI , assessed the adverse drug reactions by TESS assessment , observed the medication compliance by self compliance scale .Results 4 weeks after treatment ,the BEHAVE-AD score and CMAI scores of two groups than before treatment decreased ,but the difference was not statistically significant (P>0.05),8 weeks after treatment,the BE-HAVE-AD score and CMAI scores of two groups decreased significantly ,compared with before treatment difference was statisti-cally significant(P0.05).The incidence rate of weight gain,lethargy in research group were lower than control group ,the difference was statistically significant (P0.05),4 weeks,8 weeks after treatment the compliance of research group was better than control group ,the difference was statistically significant(P<0.05).Conclusion Risperidone oral solu-tion is applied to the clinical treatment of elderly dementia with BPSD effective and relatively safe ,patients with better compli-ance .%目的:比较利培酮口服液与奥氮平治疗老年痴呆精神行为症状( BPSD )的疗效和安全性。方法将120例BPSD患者随机分为研究组和对照组各60例。研究组患者给予利培酮口服液治疗,对照组患者给予奥氮平治疗,疗程为8周。2组患者均采用痴呆病理行为评定量表(BEHAVE-AD)评定疗效,Cohan Mansfield 激越行为量表(CMAI)评定激越行为的改善程度,副反应量表(TESS)评定药物不良反应,自编依从性量表观察患者服药

  9. Misuse and abuse of quetiapine

    Directory of Open Access Journals (Sweden)

    Agnieszka Piróg-Balcerzak

    2015-02-01

    Full Text Available Quetiapine is an atypical antipsychotic agent, frequently used in psychiatry, often for symptomatic treatment against a number of mental disorders differing from the registration indications. One of the use is to soothe the clinical conditions caused by the use of various psychoactive substances. The paper presents and discusses the reports of quetiapine misuse, abuse, and even mental addiction, as well as symptoms similar to the so-called discontinuation syndrome, often mixed with withdrawal syndrome occurring in the course of addiction. Most reports concern males, and especially those with a history of other psychoactive substance abuse, and personality disorders, often in conflict with the law. Therefore, clinicians should be cautious when prescribing quetiapine to such patients. The article discusses potential mechanisms responsible for quetiapine abuse. This is probably related to its sedative and anxiolytic activity which results in the frequent use with stimulants. Also, high affinity for the H1 receptor, as antihistamines agents causes rewarding action.

  10. Pharmacogenetics of olanzapine metabolism.

    Science.gov (United States)

    Söderberg, Mao Mao; Dahl, Marja-Liisa

    2013-08-01

    The pharmacokinetics of the atypical antipsychotic, olanzapine, display large interindividual variation leading to multiple-fold differences in drug exposure between patients at a given dose. This variation in turn gives rise to the need for individualized dosing in order to avoid concentration-dependent adverse effects or therapeutic failure. Genetically determined differences in olanzapine metabolism represent a less studied source of variability in comparison to environmental and physiological factors. In this review, we summarize available in vitro and in vivo data addressing the influence of polymorphisms in drug-metabolizing enzymes on olanzapine serum exposure. The polymorphic CYP2D6 enzyme appears to have no significant influence on olanzapine steady-state serum concentrations. The formation of the various olanzapine metabolites is influenced by polymorphisms in the genes coding for CYP1A2, CYP1A expression regulator AHR, UGT1A4 and UGT2B10, as well as FMO3. An impact on steady-state olanzapine serum concentrations has been suggested for variants of CYP1A2 and UGT1A4, with somewhat conflicting findings. The potential involvement of FMO1 and CYP3A43 in olanzapine disposition has also been suggested but needs future validation.

  11. Dose-dependent galactorrhea with quetiapine

    OpenAIRE

    Sethi, Sujata; Sharma, Manisha; Malik, Amit

    2010-01-01

    Quetiapine is an atypical antipsychotic agent with minimal propensity to induce hyperprolactinemia in standard therapeutic dosages. Despite that quetiapine is considered to be a prolactin-sparing atypical antipsychotic, hyperprolactinemia with related side effects may rarely be encountered in susceptible individuals. We report a case of quetiapine-induced hyperprolactinemia and galactorrhea in an adult female, which was dose-dependent.

  12. Interpreting serum risperidone concentrations.

    Science.gov (United States)

    Boerth, Joel M; Caley, Charles F; Goethe, John W

    2005-02-01

    Risperidone is an atypical antipsychotic commonly used for treatment of schizophrenia and other psychotic disorders. Although therapeutic drug monitoring is not routine for any of the atypical antipsychotics, serum antipsychotic concentrations are measured routinely to assess treatment nonadherence. In humans, risperidone is metabolized by cytochrome P450 2D6 to 9-hydroxyrisperidone; together these constitute the active moiety. Dose-proportional increases in serum concentrations have not been reported for the parent drug, but have been reported for 9-hydroxyrisperidone and the active moiety (i.e., the combined concentrations of risperidone and 9-hydroxyrisperidone). We describe a 34-year-old Caucasian man of Sicilian descent with a history of schizophrenia, disorganized type. He was suspected to be noncompliant with his risperidone therapy. Initially, active moiety risperidone concentrations increased linearly with prescribed dosage increases. However, with continued increases, active moiety concentrations adjusted downward and remained 17-36% below anticipated levels. We propose a method for estimating target active moiety concentrations of risperidone based on dosage-a method that may be used to guide clinicians in assessing nonadherence to risperidone treatment.

  13. Cost-effectiveness of olanzapine long-acting injection in the treatment of patients with schizophrenia in the United States: a micro-simulation economic decision model.

    Science.gov (United States)

    Furiak, Nicolas M; Ascher-Svanum, Haya; Klein, Robert W; Smolen, Lee J; Lawson, Anthony H; Montgomery, William; Conley, Robert R

    2011-04-01

    To compare, from the perspective of third-party payers in the United States health care system, the cost-effectiveness of olanzapine long-acting injection (LAI, depot) with alternative antipsychotic agents including risperidone-LAI, paliperidone-LAI, haloperidol-LAI, and oral olanzapine, in the treatment of patients with schizophrenia who have been non-adherent or partially adherent with oral antipsychotics. A 1-year micro-simulation economic decision model was developed to simulate the dynamics of usual care of patients with schizophrenia who continue, discontinue, switch, or restart their medication. The model uses a range of clinical and cost parameters including adherence levels, relapse with and without hospitalization, quality-adjusted life years (QALYs), treatment discontinuation rates by reason, treatment-emergent adverse events, suicide, health care resource utilization, and direct health care costs. Published medical literature and a clinical expert panel were used to develop baseline model assumptions. Key model outputs include annual total direct cost (US$) per treatment and incremental cost-effectiveness values per additional QALY gained. Model results found that the olanzapine-LAI treatment strategy was more effective (greater QALYs) and less costly than risperidone-LAI, paliperidone-LAI, and haloperidol-LAI. In addition, olanzapine-LAI was both more effective and more costly, with an estimated incremental cost/QALY of $26,824 compared to oral olanzapine. The base-case and multiple sensitivity analyses found olanzapine-LAI to remain within acceptable cost-effective ranges (micro-simulation model finds the olanzapine-LAI treatment strategy to result in better effectiveness and to be a cost-effective alternative compared to oral olanzapine and the LAI formulations of risperidone, paliperidone, and haloperidol in the treatment of non-adherent and partially adherent patients with schizophrenia in the United States. A key limitation is the assumption how

  14. Acute camptocormia induced by olanzapine: a case report

    Directory of Open Access Journals (Sweden)

    Boyer Stéphane

    2010-06-01

    Full Text Available Abstract Introduction Camptocormia refers to an abnormal posture with flexion of the thoraco-lumbar spine which increases during walking and resolves in supine position. This symptom is an increasingly recognized feature of parkinsonian and dystonic disorders, but may also be caused by neuromuscular diseases. There is recent evidence that both central and peripheral mechanisms may be involved in the pathogenesis of camptocormia. We report a case of acute onset of camptocormia, a rare side effect induced by olanzapine, a second-generation atypical anti-psychotic drug with fewer extra-pyramidal side-effects, increasingly used as first line therapy for schizophrenia, delusional disorders and bipolar disorder. Case presentation A 73-year-old Caucasian woman with no history of neuromuscular disorder, treated for chronic delusional disorder for the last ten years, received two injections of long-acting haloperidol. She was then referred for fatigue. Physical examination showed a frank parkinsonism without other abnormalities. Routine laboratory tests showed normal results, notably concerning creatine kinase level. Fatigue was attributed to haloperidol which was substituted for olanzapine. Our patient left the hospital after five days without complaint. She was admitted again three days later with acute back pain. Examination showed camptocormia and tenderness in paraspinal muscles. Creatine kinase level was elevated (2986 UI/L. Magnetic resonance imaging showed necrosis and edema in paraspinal muscles. Olanzapine was discontinued. Pain resolved quickly and muscle enzymes were normalized within ten days. Risperidone was later introduced without significant side-effect. The camptocormic posture had disappeared when the patient was seen as an out-patient one year later. Conclusions Camptocormia is a heterogeneous syndrome of various causes. We believe that our case illustrates the need to search for paraspinal muscle damage, including drug

  15. A Case of Olanzapine-Induced Fever

    Science.gov (United States)

    Yang, Cho-Hsiang; Chen, Ying-Yeh

    2017-01-01

    Olanzapine, a frequently used second-generation antipsychotic, has rarely been implicated as a cause of drug-induced fever in the absence of neuroleptic malignant syndrome. We describe a patient who developed isolated fever following olanzapine monotherapy, which subsided after discontinuation of olanzapine. Blockade of dopaminergic receptors and elevated cytokines concentration are possible mechanisms of fever development during treatment with olanzapine. This case calls for attention to olanzapine-induced fever in clinical practice. PMID:28138204

  16. Olanzapine-induced cerebral metabolic changes related to symptom improvement in schizophrenia.

    Science.gov (United States)

    Molina, Vicente; Gispert, Juan D; Reig, Santiago; Pascau, Javier; Martínez, Raúl; Sanz, Javier; Palomo, Tomás; Desco, Manuel

    2005-01-01

    The pattern of brain metabolic changes produced by olanzapine has yet to be described, despite the theoretical and clinical interest of this new antipsychotic. We studied a group of 17 schizophrenic patients who underwent two fluoro-deoxyglucose-positron emission tomography (FDG-PET) studies under two different conditions: a baseline scan during treatment with either conventional antipsychotics (n=15) or risperidone (n=2) and a second scan performed 17-24 weeks after switching to olanzapine. PET scans were obtained while performing a standard cognitive paradigm (Continuous Performance Test) and analysed by means of Statistical Parametric Mapping. No significant metabolic changes were found in the comparison between pre- and post-olanzapine conditions. A brain map of the statistical power of our design showed that changes up to 3% in the frontal and up to 8% in the occipital region were not likely to exist (1-beta=0.8). The degree of improvement in positive symptoms was related to the amount of activity decrease in the right orbital region and to the amount of activity increase in the primary visual area. Improvement in negative symptoms was associated with an activity increase in the dorsal prefrontal cortex, and a higher baseline activity in both temporal poles. These correlation patterns suggest that the functional mechanism of action of olanzapine may share traits from both typical and atypical neuroleptics.

  17. Olanzapine-high potency antipsychotic drug inducing significant weight gain: A case report

    Directory of Open Access Journals (Sweden)

    Marić Nađa P.

    2008-01-01

    Full Text Available INTRODUCTION Olanzapine is a second generation antipsychotic (SGA with a high level of therapeutic effectiveness in schizophrenia and other psychotic disorders. Along with the positive therapeutic effects, an increase of the body weight frequently occurs. According to the literature, the average weight gain is about 6-7 kg during several months of treatment. This could be valued as a moderate weight increase. CASE OUTLINE This article presents a case of a young female with schizophrenia, without clinical improvement with several antipsychotics (clozapine, risperidone, haloperidol and with the occurrence of significant neurological side effects. The treatment started with olanzapine (baseline was associated with good initial response (PANSS reduction 20% in the first two weeks and the improvement was maintained further on (PANSS reduction 50% after 16 weeks. Significant increase (20 kg, 40% in weight appeared during the following 16 weeks (BMI at baseline 17.9 kg/m2; BMI 16 weeks later 25.1 kg/m2. CONCLUSION High effectiveness of olanzapine in schizophrenia symptoms reduction was accompanied by a significant weight gain. However, this drug leads to impaired glucoregulation, dyslipidaemia etc. It also increases the risk of diabetes and cardio-vascular diseases, i.e. the main causes of mortality in schizophrenia after a suicide. Therefore, clinicians are suggested to focus on possible predictors of weight gain during olanzapine therapy, and act accordingly in order to prevent serious health consequences.

  18. Development of diabetes mellitus associated with quetiapine

    Science.gov (United States)

    Nanasawa, Hideki; Sako, Akahito; Mitsutsuka, Tomohiko; Nonogaki, Kaori; Kondo, Tadayuki; Mishima, Shuichi; Uju, Yoriyasu; Ito, Toshihiko; Enomoto, Tetsuro; Hayakawa, Tatsuro; Yanai, Hidekatsu

    2017-01-01

    Abstract We aimed to describe the characteristics and clinical course of patients who developed diabetes associated with the use of quetiapine. This study included patients who received quetiapine for over a month between April 2008 and November 2013, and were diagnosed as having new-onset diabetes after initiation of quetiapine. We excluded patients who developed diabetes more than 1 year after discontinuation of quetiapine. We identified new-onset diabetes by hemoglobin A1c or prescriptions of antidiabetic drugs. Among 1688 patients who received quetiapine, hemoglobin A1c had been measured in 595 (35.2%) patients at least once during the observation period, and 33 (2.0%) patients had received hypoglycemic drugs. Eighteen (1.1%) patients were considered to have developed new-onset diabetes associated with quetiapine after a median of 1.6 years following initiation of quetiapine. Median (interquartile range) age was 54.5 (29.8) years, 8 patients were male, and median (interquartile range) duration of mental illness was 15.3 (13.8) years. Median hemoglobin A1c and body mass index (BMI) were 7.1 (1.4) % and 28.4 (7.0) kg/m2, respectively. Seventeen patients had dyslipidemia when diabetes was discovered. All of these discontinued quetiapine within 3 months after the diagnosis of diabetes, and the diabetes in 4 patients had ameliorated without hypoglycemic drugs. Of 13 patients who had received either oral hypoglycemic drugs or insulin, 2 patients achieved well-controlled hemoglobin A1c without hypoglycemic drugs, and 10 patients had hemoglobin A1c 5.0% to 7.7% with the continued use of hypoglycemic drugs. We demonstrated that almost all patients who developed quetiapine-associated diabetes had dyslipidemia and increased BMI. There was no life-threatening hyperglycemia and diabetes was ameliorated just by discontinuation of quetiapine in several patients. The monitoring of metabolic parameters during antipsychotic treatment is important to diagnose and treat diabetes

  19. Use of quetiapine in children and adolescents.

    Science.gov (United States)

    Masi, Gabriele; Milone, Annarita; Veltri, Stefania; Iuliano, Raffaella; Pfanner, Chiara; Pisano, Simone

    2015-04-01

    The atypical antipsychotic quetiapine has been used in different psychotic and non-psychotic disorders in children and adolescents in randomized clinical trials, open-label studies and chart reviews. Most of these studies suggest that quetiapine may be a promising agent with a potential for use in young patients. The aim of this paper is to critically review available literature on quetiapine in the treatment of children and adolescents with a variety of psychiatric disorders, including psychotic disorders, bipolar disorders (manic and depressive episodes), conduct disorder, autism spectrum disorder, Tourette's syndrome and personality disorders. Furthermore, we report on possible neurochemical pathways involved during treatment with quetiapine, and discuss some issues that are clinically relevant in daily practice, such as titration strategies, safety and tolerability, and monitoring possible side effects. Controlled studies support the short-term efficacy for treating psychosis, mania, and aggression within certain diagnostic categories. However, although quetiapine seems well tolerated in various pediatric populations during acute and intermediate treatments, and hyper-prolactinemia and extra-pyramidal side effects are consistently low among studies, weight gain and alterations in lipid profile need to be closely monitored. Furthermore, the distal benefit/risk ratio during long-term treatment remains to be determined.

  20. Update on quetiapine in the treatment of bipolar disorder: results from the BOLDER studies

    Directory of Open Access Journals (Sweden)

    Prashant Gajwani

    2007-01-01

    Full Text Available Prashant Gajwani1, David J Muzina2, David E Kemp3, Keming Gao1, Joseph R Calabrese11Case Western Reserve University (CWRU School of Medicine, 2Cleveland Clinic Lerner College of Medicine of CWRU, 3Case Western Reserve University, Cleveland OH, USAAbstract: The essential features of bipolar affective disorder involve the cyclical occurrence of high (manic or hypomanic episodes and low mood states. Depressive episodes in both bipolar I and II disorder are more numerous and last for longer duration than either manic or hypomanic episodes. In addition depressive episodes are associated with higher morbidity and mortality. While multiple agents, including all 5 atypical antipsychotics, have demonstrated efficacy and earned US FDA indication for manic phase of bipolar illness, the acute treatment of bipolar depression is less well-studied. The first treatment approved by the US FDA for acute bipolar depression was the combination of the atypical antipsychotic olanzapine and the antidepressant fluoxetine. Recently, quetiapine monotherapy has demonstrated efficacy in the treatment of depressive episodes associated with both bipolar I and II disorder and has earned US FDA indication for the same.Keywords: bipolar disorder, quetiapine, BOLDER studies

  1. Olanzapine-induced eosinophilic pleuritis

    Directory of Open Access Journals (Sweden)

    Matthew Evison

    2015-01-01

    Eosinophilic pleural fluid is not a marker of non-malignant aetiology and eosinophilic pleural effusions require a careful and systematic diagnostic work-up. This is the second case report to identify olanzapine as a causative agent in eosinophilic pleural effusion.

  2. The quetiapine active metabolite N-desalkylquetiapine and the neurotensin NTS₁ receptor agonist PD149163 exhibit antidepressant-like effects on operant responding in male rats.

    Science.gov (United States)

    Hillhouse, Todd M; Shankland, Zachary; Matazel, Katelin S; Keiser, Ashley A; Prus, Adam J

    2014-12-01

    Major depressive disorder is the most common mood disorder in the United States and European Union; however, the limitations of clinically available antidepressant drugs have led researchers to pursue novel pharmacological treatments. Clinical studies have reported that monotherapy with the atypical antipsychotic drug quetiapine produces a rapid reduction in depressive symptoms that is apparent after 1 week of treatment, and it is possible that the active metabolite N-desalkylquetiapine, which structurally resembles an antidepressant drug, produces antidepressant effects. Neuropharmacological evaluations of the neurotensin NTS1 receptor agonist PD149163 suggest antidepressant efficacy, but the effects of a NTS₁ receptor agonist in an antidepressant animal model have yet to be reported. The present study examined the antidepressant-like effects of N-desalkylquetiapine, PD14916, quetiapine, the tricyclic antidepressant drug imipramine, the atypical antipsychotic drug risperidone, and the typical antipsychotic drug raclopride on responding in male Sprague-Dawley rats trained on a differential-reinforcement-of-low-rate 72-s operant schedule, a procedure used for screening antidepressant drugs. Quetiapine, PD149163, risperidone, and imipramine exhibited antidepressant-like effects by increasing the number of reinforcers earned, decreasing the number of responses emitted, and shifting the interresponse time (IRT) distributions to the right. N-Desalkylquetiapine produced a partial antidepressant-like effect by decreasing the number of responses emitted and producing a rightward shift in the IRT distributions, but it did not significantly alter the number of reinforcers earned. Raclopride decreased reinforcers and responses. These data suggest that N-desalkylquetiapine likely contributes to quetiapine's antidepressant efficacy and identify NTS₁ receptor activation as a potential novel pharmacologic strategy for antidepressant drugs.

  3. Cardiac effects of sertindole and quetiapine

    DEFF Research Database (Denmark)

    Nielsen, Jimmi; Matz, Jørgen; Mittoux, Aurelia;

    2015-01-01

    The QT interval is the most widely used surrogate marker for predicting TdP; however, several alternative surrogate markers, such as Tpeak-Tend (TpTe) and a quantitative T-wave morphology combination score (MCS) have emerged. This study investigated the cardiac effects of sertindole and quetiapin...

  4. Olanzapine approved for the acute treatment of schizophrenia or manic/mixed episodes associated with bipolar I disorder in adolescent patients

    Directory of Open Access Journals (Sweden)

    Ann E Maloney

    2010-11-01

    Full Text Available Ann E Maloney1,2, Linmarie Sikich31Maine Medical Center Research Institute, Scarborough, ME, USA; 2Department of Psychiatry, Tufts University School of Medicine, Boston, MA, USA; 3Department of Psychiatry, University of North Carolina at Chapel Hill, Chapel Hill, NC, USABackground: Severe and persistent mental illnesses in children and adolescents, such as early-onset schizophrenia spectrum (EOSS disorders and pediatric bipolar disorder (pedBP, are increasingly recognized. Few treatments have demonstrated efficacy in rigorous clinical trials. Enduring response to current medications appears limited. Recently, olanzapine was approved for the treatment of adolescents with schizophrenia or acute manic/mixed episodes in pedBP.Methods: PubMed searches were conducted for olanzapine combined with pharmacology, schizophrenia, or bipolar disorder. Searches related to schizophrenia and bipolar disorder were limited to children and adolescents. The bibliographies of the retrieved articles were hand-checked for additional relevant studies. The epidemiology, phenomenology, and treatment of EOSS and pedBP, and olanzapine’s pharmacology are reviewed. Studies of olanzapine treatment in youth with EOSS and pedBP are examined.Results: Olanzapine is efficacious for EOSS and pedBP. However, olanzapine is not more efficacious than risperidone, molindone, or haloperidol in EOSS and is less efficacious than clozapine in treatment-resistant EOSS. No comparative trials have been done in pedBP. Olanzapine is associated with weight gain, dyslipidemia, and transaminase elevations in youth. Extrapyramidal symptoms, neuroleptic malignant syndrome, and blood dyscrasias have also been reported but appear rare.Conclusions: The authors conclude that olanzapine should be considered a second-line agent in EOSS and pedBP due to its risks for significant weight gain and lipid dysregulation. Awareness of the consistent weight and metabolic changes observed in olanzapine

  5. Control study of quetiapine in the treatment of alzheimer's disease(AD) with behavioral and psychological symptoms%奎硫平治疗阿尔茨海默病精神行为症状对照研究

    Institute of Scientific and Technical Information of China (English)

    孙锦红

    2014-01-01

    Objective:To compare the efficacy and safety of quetiapine and risperidone in the treatment of alzheimer's disease(AD) patients with behavioral and psychological symptoms(BPSD).Methods:60 cases of AD patients with behavioral and psychological symptoms were selected,they were randomly divided into two groups.The two groups were respectively treated with quetiapine and risperidone for 6 weeks.Treatment effects were assessed with the behavioral pathology in alzheimer's disease rating scale(BEHAVE-AD) and mini mental state examination(MMSE).Adverse reactions were assessed with treatment emergent symptom scale(TESS).Results:In the quetiapine group,the effective rate was 84.5%;in the risperidone group,the effective rate was 83%.Conclusion:The safety of quetiapine is higher.%目的:比较奎硫平和利培酮对阿尔茨海默病(AD)患者精神行为症状(BPSD)的疗效和安全性。方法:收治具有精神行为症状的AD患者60例,随机分为两组,分别给予奎硫平和利培酮治疗,疗程6周。采用痴呆病理行为评定量表(BEHAVE-AD)、简易智力状态检查(MMSE)评定疗效。采用副反应量表(TESS)评定不良反应。结果:奎硫平组的有效率84.5%;利培酮组的有效率83%。结论:奎硫平的安全性更高。

  6. Postmortem redistribution of olanzapine following intramuscular administration of olanzapine pamoate in dogs.

    Science.gov (United States)

    Johnson, Jason T; Everly, Amy G; Kpakima, Felicia E Frazier; Detke, Holland C

    2015-12-01

    The potential for postmortem redistribution of olanzapine was investigated in beagle dogs. Olanzapine pamoate monohydrate was administered once every 14 days by intramuscular injection for 3 months to fed male dogs (n=15) at a dose of 20 mg/kg olanzapine (equivalent to 46 mg/kg olanzapine pamoate monohydrate). Blood samples were collected after the fifth (Day 57) and sixth (Day 71) doses to determine olanzapine and N-oxide olanzapine concentrations. On Day 71 at 72 h postdose, dogs were euthanized and placed on their backs without additional manipulation and held for postmortem blood, urine, and tissue collection at room temperature for up to 168 h postdose (96 h after euthanasia). Concentrations of olanzapine and N-oxide olanzapine were determined by liquid chromatography-mass spectroscopy/mass spectroscopy (LC-MS/MS). Postmortem olanzapine concentrations in blood increased up to seven-fold compared to the last quantified antemortem blood concentration. Olanzapine concentrations in vein tissue samples (surrogates for peripheral blood) also increased, whereas other tissue concentrations, such as myocardium, lung, liver, and kidney decreased over the postmortem period. An increase in blood concentration of olanzapine after death was observed in all but one animal, suggesting that postmortem redistribution may occur in dogs following biweekly intramuscular administration of olanzapine pamoate monohydrate. The rise in olanzapine concentrations in blood after death in this study may potentially be attributed to diffusion from multiple tissues to blood and, to a lesser extent, reduction of the N-oxide olanzapine metabolite back to olanzapine. However, the generalizability of these results to humans cannot be confirmed by the present study.

  7. Olanzapine induced neuroleptic malignant syndrome.

    Science.gov (United States)

    Patra, Bichitra Nanda; Khandelwal, Sudhir K; Sood, Mamta

    2013-01-01

    An 18 year old male diagnosed as a case of bipolar affective disorder (BPAD), developed neuroleptic malignant syndrome (NMS) following treatment with olanzapine (20 mg per day), an atypical antipsychotic drug. NMS is usually seen with typical antipsychotic drugs. The patient was diagnosed as a case of NMS, offending agent was immediately withdrawn and prompt treatment with bromocriptine and levodopa produced a good recovery. The various features of the case are discussed in view of the potential mortality of the syndrome.

  8. A suspected case of olanzapine induced hyponatremia

    Directory of Open Access Journals (Sweden)

    Ajay Kumar Bakhla

    2014-01-01

    Full Text Available Here we report a case of a 63-year-old male diagnosed with recurrent depressive disorder and current episode of severe depression with psychotic symptoms, developed hyponatremia soon after addition of olanzapine and increasing the dose of escitalopram. A possible causality association was established with olanzapine, and the possible etiological reasons of this clinically significant risk were discussed.

  9. A literature review of quetiapine for generalized anxiety disorder.

    Science.gov (United States)

    Kreys, Tiffany-Jade M; Phan, Stephanie V

    2015-02-01

    To evaluate the efficacy and tolerability of quetiapine for the treatment of generalized anxiety disorder (GAD), a literature search of the Medline database was conducted from inception to May 2014. The search was not restricted by language. Keywords used in the search were quetiapine and generalized anxiety disorder or anxiety. All studies assessing the use of quetiapine as monotherapy or adjunct therapy for the primary management of GAD in adults 18-65 years of age were included in this review. The nine studies included in this review were three studies evaluating the use of quetiapine extended release (XR) as monotherapy for acute GAD treatment, one study evaluating quetiapine XR monotherapy for maintenance treatment of GAD, and five studies evaluating quetiapine (2 XR, 3 immediate release) as adjunct therapy for acute GAD treatment. Quetiapine displayed both efficacy and tolerability in all monotherapy trials evaluating its use for acute and long-term treatment of GAD. Despite some limitations to and heterogeneity among the five adjunct therapy studies, three studies showed that quetiapine resulted in statistically significant changes in the Hamilton Anxiety Rating Scale or Clinical Global Impressions-Severity of Illness Scale scores. Although future studies of longer duration with broader inclusion criteria are needed to further evaluate the benefits and risks of quetiapine for GAD, in patients failing to respond to conventional antidepressant therapy, quetiapine may be a potential treatment option. With appropriate monitoring and management of adverse effects, the potential benefits of quetiapine in patients with treatment-refractory GAD may outweigh the risks associated with its use.

  10. Typical neuroleptic malignant syndrome presented in patient on maintenance quetiapine

    Directory of Open Access Journals (Sweden)

    Chintan Madhusudan Raval

    2014-01-01

    Full Text Available Neuroleptic malignant syndrome is an acute, life-threatening medical complication caused by antipsychotics. It is commonly seen with typical antipsychotics and very rare with atypicals. Cases have been reported with quetiapine also, but this case is of special interest because it occurred in patient who was stable on maintenance quetiapine 200 mg/day for last 5 years.

  11. Postmortem Femoral Blood Reference Concentrations of Aripiprazole, Chlorprothixene, and Quetiapine

    DEFF Research Database (Denmark)

    Skov, Louise; Johansen, Sys Stybe; Linnet, Kristian

    2015-01-01

    Postmortem femoral blood concentrations of the antipsychotic drugs aripiprazole, chlorprothixene and its metabolite, and quetiapine were determined by LC-MS-MS in 25 cases for aripiprazole and 60 cases each for chlorprothixene and quetiapine. For cases where the cause of death was not related to ...

  12. Olanzapine induced neuroleptic malignant syndrome

    Directory of Open Access Journals (Sweden)

    Bichitra Nanda Patra

    2013-01-01

    Full Text Available An 18 year old male diagnosed as a case of bipolar affective disorder (BPAD, developed neuroleptic malignant syndrome (NMS following treatment with olanzapine (20 mg per day, an atypical antipsychotic drug. NMS is usually seen with typical antipsychotic drugs. The patient was diagnosed as a case of NMS, offending agent was immediately withdrawn and prompt treatment with bromocriptine and levodopa produced a good recovery. The various features of the case are discussed in view of the potential mortality of the syndrome.

  13. Olanzapine use in a manic patient during second and third trimester pregnancy

    Directory of Open Access Journals (Sweden)

    Choi L

    2014-02-01

    Full Text Available Lynn Choi, Soo-Hyun Joo, Jong-Hyun Jeong Department of Psychiatry, St Vincent's Hospital, College of Medicine, The Catholic University of Korea, Suwon, Korea Abstract: Women with bipolar disorder have a high risk for symptom exacerbation during pregnancy and the risk is elevated further when mood stabilizers are discontinued. This report describes a 31-year-old bipolar woman who discontinued medication before pregnancy but had to resume her pharmacotherapy due to manic episodes that recurred during the second trimester. Olanzapine, an atypical antipsychotic, was administered from week 25 of gestation and then replaced with quetiapine in week 35 of gestation. Even though a consensus on clinical interventions for pregnant patients with symptom relapse has not been reached, clinicians should still discuss pregnancy and therapeutic management with every female bipolar patient of childbearing age. This discussion is important because treatment can be managed most effectively in these individuals if pregnancy is planned. Ultimately, clinical decisions should be made on a case-by-case basis, weighing the risks to the mother and fetus between the disorder itself and the teratogenicity of pharmacotherapy. Keywords: pregnancy, bipolar disorder, olanzapine, manic

  14. Active metabolites as antidepressant drugs: The role of norquetiapine in the mechanism of action of quetiapine in the treatment of mood disorders

    Directory of Open Access Journals (Sweden)

    Francisco eLopez-Munoz

    2013-09-01

    Full Text Available Active metabolites of some antipsychotic drugs exhibit pharmacodynamic and pharmacokinetic properties that may be similar to or differ from the original compound and that can be translated by a different profile of responses and interactions to clinical level. Some of these antipsychotics’ active metabolites might participate in mechanisms of antidepressant activity, as m-chlorophenylpiperazine (aripiprazole, 9-OH-risperidone and norquetiapine. Norquetiapine exhibits distinct pharmacological activity from quetiapine and plays a fundamental role in its antidepressant efficacy. In this review, we analyze the differential pharmacological aspects between quetiapine and norquetiapine, both from the pharmacokinetic and pharmacodynamic perspectives (affinity for dopaminergic, noradrenegic and/or serotonergic receptors, etc., as well as differential neuroprotective role. The pharmacological differences between the two drugs could explain the differential clinical effect, as well as some differences in tolerability profile and drug interactions. The available data are sufficient to arrive at the conclusion that antidepressant activity of quetiapine is mediated, at least in part, by the active metabolite norquetiapine, which selectively inhibits noradrenaline reuptake, is a partial 5-HT1A receptor agonist, and acts as an antagonist at presynaptic α2, 5-HT2C and 5-HT7 receptors.

  15. Eosinophilic myocarditis during treatment with olanzapine

    DEFF Research Database (Denmark)

    Vang, Torkel; Rosenzweig, Mary; Bruhn, Christina Hedegaard

    2016-01-01

    -mortem toxicological examination demonstrated presence of olanzapine, morphine, venlafaxine and oxazepam. Syringes indicating substance abuse were found in his home. Case 2 was a 36-year-old Caucasian man diagnosed with schizophrenia was found dead unexpectedly. There was no history of substance abuse. Current...... fatal cases of eosinophilic myocarditis associated with the use of olanzapine. CASE PRESENTATION: Case 1 was a 39-year-old Caucasian man with known substance abuse and schizophrenia. He was found dead in his home. Olanzapine was prescribed at day -54, and dose at time of death was 40 mg/day. Post...

  16. Olanzapine-induced tardive oculogyric crises

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    Amar D Bavle

    2013-01-01

    Full Text Available Tardive syndromes are much lower in prevalence in second generation antipsychotics (SGA than in the typical antipsychotics. Although, olanzapine, which is an SGA, has a high risk of causing weight gain, metabolic syndrome, raised blood sugar, and dyslipidemias; it is widely used as the risk of developing extrapyramidal syndromes (EPS is low. Among the various forms of EPS, tardive syndromes are the most feared, tardive dyskinesia, tardive akathisia, and tardive dystonia are the commonest tardive syndromes, the others being less common. Tardive oculogyric crises (TOC are a rare form of tardive dystonia. This patient had TOC with prolonged unsupervised treatment with low-dose olanzapine. Added to that, she developed weight gain that was alarmingly high and such high gain in weight with olanzapine, to our knowledge, has not been reported. She responded to a low dose of trihexiphenydyl, and on stopping olanzapine and adding aripiprazole, has started losing weight.

  17. Eosinophilic myocarditis during treatment with olanzapine

    DEFF Research Database (Denmark)

    Vang, Torkel; Rosenzweig, Mary; Bruhn, Christina Hedegaard;

    2016-01-01

    BACKGROUND: Drug-induced eosinophilic myocarditis is a life-threatening and frequently overlooked condition. The prevalence of myocarditis in clozapine-treated patients may be as high as 3 %. An association between olanzapine and myocarditis has not previously been described, but given the chemical...... fatal cases of eosinophilic myocarditis associated with the use of olanzapine. CASE PRESENTATION: Case 1 was a 39-year-old Caucasian man with known substance abuse and schizophrenia. He was found dead in his home. Olanzapine was prescribed at day -54, and dose at time of death was 40 mg/day. Post......-mortem toxicological examination demonstrated presence of olanzapine, morphine, venlafaxine and oxazepam. Syringes indicating substance abuse were found in his home. Case 2 was a 36-year-old Caucasian man diagnosed with schizophrenia was found dead unexpectedly. There was no history of substance abuse. Current...

  18. Olanzapine discontinuation emergent recurrence in bipolar disorder

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    Manu Arora

    2014-01-01

    Full Text Available Objective: The efficacy of atypical antipsychotics including olanzapine in acute treatment of manic episode has been established, whereas its role in maintenance treatment is not clear. Materials and Methods: Thirteen patients of bipolar disorder who were on regular treatment with mood stabilizer and subsequently relapsed into mania or depressive episode after discontinuation of olanzapine were studied for various socio-demographic and clinical factors using retrospective chart review. Results: There was no correlation found between the period of tapering olanzapine, time to recurrence of episode after discontinuation, and the dosage of olanzapine at the time of discontinuation. The predominant early signs of relapse after discontinuation of olanzapine included sleep disturbance (72.7%, lack of insight for change in behavior (72.7%, irritability (54.5%, and elevated mood (45.5%. Conclusion: Mood stabilizer alone as a maintenance therapy of bipolar disorder may be inadequate for long-term management. A low dose of olanzapine along with mood stabilizers might be useful for prevention of recurrence in bipolar disorder.

  19. Postmortem Femoral Blood Concentrations of Risperidone

    DEFF Research Database (Denmark)

    Linnet, Kristian; Johansen, Sys Stybe

    2014-01-01

    Postmortem femoral blood concentrations of the antipsychotic drug risperidone and the active metabolite 9-hydroxyrisperidone were determined by an achiral LC-MS/MS method in 38 cases. The cause of death was classified as unrelated to risperidone in 30 cases, in which the sum of the concentration ...

  20. Olanzapine versus haloperidol: Which can control stuttering better?

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    Vahid Shaygannejad

    2013-01-01

    Conclusions: It seems that olanzapine does have better impact in controlling stuttering, and it may be recommended to prescribe olanzapine for stutters as the first choice to control the stuttering under a careful follow-up.

  1. Branch retinal vein occlusion associated with quetiapine fumarate

    Directory of Open Access Journals (Sweden)

    Siang Lim

    2011-08-01

    Full Text Available Abstract Background To report a case of branch retinal vein occlusion in a young adult with bipolar mood disorder treated with quetiapine fumarate. Case Presentation A 29 years old gentleman who was taking quetiapine fumarate for 3 years for bipolar mood disorder, presented with sudden vision loss. He was found to have a superior temporal branch retinal vein occlusion associated with hypercholesterolemia. Conclusion Atypical antipsychotic drugs have metabolic side effects which require regular monitoring and prompt treatment.

  2. Short-term treatment with olanzapine does not modulate gut hormone secretion: olanzapine disintegrating versus standard tablets

    DEFF Research Database (Denmark)

    Vidarsdottir, Solrun; Roelfsema, Ferdinand; Streefland, Trea;

    2009-01-01

    BACKGROUND: Treatment with olanzapine (atypical antipsychotic drug) is frequently associated with various metabolic anomalies, including obesity, dyslipidemia, and diabetes mellitus. Recent data suggest that olanzapine orally disintegrating tablets (ODT), which dissolve instantaneously in the mouth...

  3. Costs and effects of long-acting risperidone compared with oral atypical and conventional depot formulations in Germany.

    Science.gov (United States)

    Laux, Gerd; Heeg, Bart; van Hout, Ben A; Mehnert, Angelika

    2005-01-01

    Schizophrenia is one of the most expensive psychiatric conditions because of high direct and indirect costs associated with the nature of the illness, its resistance to treatment and the consequences of relapse. Long-acting risperidone is a new formulation of an atypical antipsychotic drug that also offers the improvements in compliance associated with haloperidol depot. The aim of this simulation study was to compare the benefits and costs of three pharmacological treatment strategies comprising first-line treatment with long-acting risperidone injection, a haloperidol depot or an oral atypical antipsychotic agent, over a 5-year period in Germany. A discrete event simulation model was developed to compare three treatment scenarios from the perspective of major third-party payers (sickness funds and social security 'Sozialversicherung'). The scenarios comprised first-line treatment with haloperidol depot (scenario 1), long-acting risperidone (scenario 2) and oral olanzapine (scenario 3). Switches to second or third-line options were allowed when side-effects occurred or a patient suffered more than a fixed number of relapses. The model accounted for fixed patient characteristics, and on the basis of these, simulated patient histories according to several time-dependent variables. The time horizon for this model was limited to 5 years, and in accordance with German guidelines, costs and effects were discounted by between 3 and 10%. Direct costs included medication, type of physician visits and treatment location. Indirect costs were not included. Information on treatment alternatives, transition probabilities, model structure and healthcare utilization were derived from the literature and an expert panel. Outcomes were expressed in terms of the number and duration of psychotic episodes, cumulative symptom scores, costs, and quality-adjusted life-years (QALY). Univariate sensitivity analyses were carried out, as were subgroup analyses based on disease severity and

  4. Development of Risperidone PLGA Microspheres

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    Susan D’Souza

    2014-01-01

    Full Text Available The aim of this study was to design and evaluate biodegradable PLGA microspheres for sustained delivery of Risperidone, with an eventual goal of avoiding combination therapy for the treatment of schizophrenia. Two PLGA copolymers (50 : 50 and 75 : 25 were used to prepare four microsphere formulations of Risperidone. The microspheres were characterized by several in vitro techniques. In vivo studies in male Sprague-Dawley rats at 20 and 40 mg/kg doses revealed that all formulations exhibited an initial burst followed by sustained release of the active moiety. Additionally, formulations prepared with 50 : 50 PLGA had a shorter duration of action and lower cumulative AUC levels than the 75 : 25 PLGA microspheres. A simulation of multiple dosing at weekly or 15-day regimen revealed pulsatile behavior for all formulations with steady state being achieved by the second dose. Overall, the clinical use of Formulations A, B, C, or D will eliminate the need for combination oral therapy and reduce time to achieve steady state, with a smaller washout period upon cessation of therapy. Results of this study prove the suitability of using PLGA copolymers of varying composition and molecular weight to develop sustained release formulations that can tailor in vivo behavior and enhance pharmacological effectiveness of the drug.

  5. Development of diabetes mellitus associated with quetiapine: A case series.

    Science.gov (United States)

    Nanasawa, Hideki; Sako, Akahito; Mitsutsuka, Tomohiko; Nonogaki, Kaori; Kondo, Tadayuki; Mishima, Shuichi; Uju, Yoriyasu; Ito, Toshihiko; Enomoto, Tetsuro; Hayakawa, Tatsuro; Yanai, Hidekatsu

    2017-01-01

    We aimed to describe the characteristics and clinical course of patients who developed diabetes associated with the use of quetiapine.This study included patients who received quetiapine for over a month between April 2008 and November 2013, and were diagnosed as having new-onset diabetes after initiation of quetiapine. We excluded patients who developed diabetes more than 1 year after discontinuation of quetiapine. We identified new-onset diabetes by hemoglobin A1c or prescriptions of antidiabetic drugs.Among 1688 patients who received quetiapine, hemoglobin A1c had been measured in 595 (35.2%) patients at least once during the observation period, and 33 (2.0%) patients had received hypoglycemic drugs. Eighteen (1.1%) patients were considered to have developed new-onset diabetes associated with quetiapine after a median of 1.6 years following initiation of quetiapine. Median (interquartile range) age was 54.5 (29.8) years, 8 patients were male, and median (interquartile range) duration of mental illness was 15.3 (13.8) years. Median hemoglobin A1c and body mass index (BMI) were 7.1 (1.4) % and 28.4 (7.0) kg/m, respectively. Seventeen patients had dyslipidemia when diabetes was discovered. All of these discontinued quetiapine within 3 months after the diagnosis of diabetes, and the diabetes in 4 patients had ameliorated without hypoglycemic drugs. Of 13 patients who had received either oral hypoglycemic drugs or insulin, 2 patients achieved well-controlled hemoglobin A1c without hypoglycemic drugs, and 10 patients had hemoglobin A1c 5.0% to 7.7% with the continued use of hypoglycemic drugs.We demonstrated that almost all patients who developed quetiapine-associated diabetes had dyslipidemia and increased BMI. There was no life-threatening hyperglycemia and diabetes was ameliorated just by discontinuation of quetiapine in several patients. The monitoring of metabolic parameters during antipsychotic treatment is important to diagnose and treat diabetes earlier.

  6. Efficacy of risperidone, olanzapine and clozapine in the treatment of therapy resistant schizophrenia

    NARCIS (Netherlands)

    Wardenier, M; Slooff, CJ; Arends, J

    2000-01-01

    Therapy-resistance for positive symptoms is one of the most important problems that occurs with the medical treatment of schizophrenia. In the past years, clozapine has proven its effectiveness in this area and has been included in the treatment protocols and guidelines, Because of the risk of agran

  7. Differences in craving for cannabis between schizophrenia patients using risperidone, olanzapine or clozapine

    NARCIS (Netherlands)

    Machielsen, Marise; Beduin, Albertine Scheltema; Dekker, Nienke; Kahn, Rene S.; Linszen, Don H.; van Os, Jim; Wiersma, Durk; Bruggeman, Richard; Cahn, Wiepke; de Haan, Lieuwe; Krabbendam, Lydia; Myin-Germeys, Inez

    2012-01-01

    Substance abuse and psychotic disorders have a high rate of comorbidity. Both disorders are associated with changes in the dopaminergic transmission in the mesocorticolimbic pathways of the brain. Since antipsychotic medications interact with the dopamine receptors in these pathways, these medicatio

  8. Differential effects of olanzapine and risperidone on cognition in schizophrenia? A saccadic eye movement study

    NARCIS (Netherlands)

    Broerse, A; Crawford, TJ; den Boer, JA

    2002-01-01

    Recent studies suggest that novel antipsychotics have positive effects on certain cognitive functions in schizophrenia. The present study investigated this claim by means of saccadic paradigms, which provide a selective index of cognitive function. Thirty-three first-episode schizophrenic patients w

  9. Risperidone for Aggressive Behavior in ADHD

    Directory of Open Access Journals (Sweden)

    J Gordon Millichap

    2007-05-01

    Full Text Available The effects of risperidone augmentation for treatment-resistant aggression in children with ADHD were evaluated in a placebo-controlled pilot study at the University of Miami Miller School of Medicine, FL.

  10. 奥氮平治疗首发精神分裂症的随访对照研究%A compartive Study of Olanzapine in the treatment of first-episode schizophrenia

    Institute of Scientific and Technical Information of China (English)

    谭余龙

    2011-01-01

    Objective To investigate the olanzapine and risperidone in treatm ent of first-episode schizophrenia curative effect and the security.M ethods 148 patients w ith first-episode schizophrenia patients w ere random ly divided into study group (olanzapine group) in 75 cases and the control group (73 cases,risperidone group) respectively taking olanzapine,risperidone treatm ent.T o evaluate clinicalefficacy,positive and negative sym ptom s scale (P A N SS) form s have been used before the treatm ent and afte the treatm ent at the the end of the second,the forth,the eighth and tw elveth m onth,asw ell as using the social dysfunction screening scale (SD SS ) form to assess the social function.R esults the olanzapine and risperidone groups in cure rate,significant efficiency,P A N SS score and SD SS score difference does not have statistical significance (P>0.05),the olanzapine group in extrapyram idal reactions,endocrine disorders,less than risperidone group,the increase in the body w eight than risperidone group,the difference w as statistically significant (P<0.05).C onclusion B oth O lanzapine and risperidone in the treatm ent of first-episode schizophrenia curative effect are good;but olanzapine less adverse reaction,high safety,high com pliance.%目的 探讨奥氮平与利培酮治疗首发精神分裂症的疗效及安全性.方法 将148例首发精神分裂症患者随机分为研究组(奥氮平组)75例和对照组(利培酮组)73例,分别服用奥氮平、利培酮治疗.于治疗前及治疗第2月、4月、8月及12个月末采用阳性症状与阴性症状量表(PANsS)评定临床疗效,同时以社会功能缺陷筛选表(SDSS)评定社会功能;以副反应量表(TESS)评定不良反应.结果 奥氮平组与利培酮组在痊愈率、显效率、PANSS评分与SDSS评分差异无统计学意义(P>0.05),奥氮平组在锥体外系反应、内分泌失调等方面少于利培酮组,在体质量增加方面多于利培酮组,差异具有统计学意

  11. 奥氮平治疗阿尔茨海默病精神行为症状对照研究%Comparative study of olanzapine in treatment of behavioral and psychological symptoms of Alzheimer's disease

    Institute of Scientific and Technical Information of China (English)

    吴忠海; 王洪娟

    2015-01-01

    Objective To compare the effect and adverse reaction of olanzapine and risperidone in the treatment of behavioral and psychological symptoms of Alzheimer's disease.Methods 70 cases with Alzheimer's disease were randomly divided into 2 groups, being treated with olanzapine and risperidone seperately for 8 weeks.The Alzheimer's disease pathology behavioral assessment scale ( BEHAVE-AD) and Treatment Emergent Symptom Scale ( TESS) were used to assess the efficacy and adverse reactions.Results Scores of BEHAV-AD decreased significantly after treatment (P0.05).The incidence of extrapyramidal system reaction ( EPS) and insomnia in risperidone group was higher than that of olanzapine group (P <0.05).Conclusions Olanzapine and risperidone had considerable effect in the treatment of behavioral and psychological symptoms of Alzheimer's disease, but olanzapine had better safety.%目的:探讨奥氮平与利培酮治疗老年期痴呆患者的精神行为症状的疗效及不良反应。方法对70例老年痴呆患者随机分为奥氮平组和利培酮组进行治疗,疗程8周。采用阿尔茨海默病病理行为评定表( BEHAVE-AD )及不良反应症状量表( TESS )评定疗效和不良反应。结果治疗后两组BEHAV-AD评分均显著下降(P<0.05或P<0.01);4周时以奥氮平组BEHAV-AD总分及行为紊乱、抑郁、焦虑评分降低明显(P<0.05);奥氮平组有效率91.43%,利培酮组有效率88.57%(P>0.05);在锥体外系反应(EPS)、失眠的发生率利培酮组高于奥氮平组(P<0.05)。结论奥氮平和利培酮用于治疗阿尔茨海默病精神行为症状的临床疗效相当,但奥氮平的安全性更好。

  12. Risperidone-induced symptomatic hyperprolactinaemia in adolescents.

    Science.gov (United States)

    Holzer, Laurent; Eap, Chin B

    2006-04-01

    Studies performed in adult patients unambiguously demonstrate a marked effect of risperidone on prolactin blood levels, with possible clinical effects related to hyperprolactinemia, such as gynecomastia and galactorrhea. However, the largest study performed in children and adolescents showed a weak effect of risperidone on prolactin concentrations during short-term treatment and a negligible effect during long-term treatment, which was probably because of the relatively low dosages of risperidone used [approximately 0.04 mg/(kg x d)]. Among the 10 psychotic adolescents treated with risperidone in our unit, we had 3 cases of gynecomastia in 3 male patients and 2 cases of galactorrhea in 2 female patients. The prolactin blood levels in these cases and in 3 other patients without apparent prolactin-related side effects were all above the normal range (median, 59 ng/mL; range, 30-123 ng/mL). Thus, risperidone administered to adolescents at doses commonly used for the treatment of psychotic symptoms can strongly increase prolactin levels, with clinical consequences such as gynecomastia and/or galactorrhea. Given that the long-term effects of antipsychotic drug-induced hyperprolactinemia are not well documented, especially regarding osteopenia, infertility, growth, and pubertal delay, risperidone should be administered with caution to children and adolescents.

  13. Postmortem Quetiapine Reference Concentrations in Brain and Blood

    DEFF Research Database (Denmark)

    Skov, Louise; Johansen, Sys Stybe; Linnet, Kristian

    2015-01-01

    and related to concentrations in postmortem blood. For cases, where quetiapine was unrelated to the cause of death (N 5 36), the 10–90 percentiles for quetiapine concentrations in brain tissue were 0.030 – 1.54 mg/kg (median 0.48 mg/kg, mean 0.79 mg/kg). Corresponding blood 10 –90 percentile values were 0.......007 – 0.39 mg/kg (median 0.15 mg/kg, mean 0.19 mg/kg), giving brain –blood ratio 10 –90 percentiles of 2.31 – 6.54 (median 3.87, mean 4.32). Both correspond well to the limited amount of data found in the literature. For cases where quetiapine was a contributing factor to death (N 5 5), the median value.......08 –6.05, which correspond to those of the nontoxic concentrations. A single case, where quetiapine was ruled as the sole cause of death, a suicide by quetiapine overdose, had an even higher value of 25.74 mg/kg in brain tissue. The blood concentration was 8.99 mg/kg, giving a brain–blood ratio of 2...

  14. Quetiapine: recent developments in preclinical research

    Directory of Open Access Journals (Sweden)

    Marco Orsetti

    2010-03-01

    Full Text Available Quetiapine (QTP is an atypical antipsychotic labelled for the treatment of patients with schizophrenia, bipolar mania and bipolar depression. Nevertheless, QTP has been tried across multiple diagnosis categories and seems to be used, among other atypical antipsychotics, in clinical practice for an expanding range of disorders such as major depression, substance abuse disorders, anxiety disorders, and borderline personality disorders. The present review focuses on papers which investigated the molecular mechanism(s of QTP antidepressant effect. In particular, preclinical studies performed by coupling the chronic mild stress, an animal model of human depression with Affymetrix microarray technology, revealed that chronic QTP administration prevented the stress-induced up- or down-regulation of 42 genes involved in the central nervous system development or having a crucial role for viability of neural cells, like regulation of signal transduction, inorganic ion transport, membrane organisation, and neurite morphogenesis. Among these, Ptgs2, Hes5, Plcb1, Senp2, Gad1, and Marcks are presumably the effectors of the QTP clinical efficacy.

  15. In vivo effects of olanzapine on striatal dopamine D{sub 2}/D{sub 3} receptor binding in schizophrenic patients: an iodine-123 iodobenzamide single-photon emission tomography study

    Energy Technology Data Exchange (ETDEWEB)

    Dresel, S.; Rossmueller, B.; Hahn, K.; Tatsch, K. [Department of Nuclear Medicine, University of Munich (Germany); Mager, T.; Meisenzahl, E.; Moeller, H.J. [Department of Psychiatry, University of Munich (Germany)

    1999-08-01

    Olanzapine is a new atypical antipsychotic agent that belongs to the same chemical class as clozapine. The pharmacological efficacy of olanzapine (in contrast to that of risperidone) has been shown to be comparable to that of clozapine, but olanzapine has the advantage of producing a less pronounced bone marrow depressing effect than clozapine. The specific aims of this study were (a) to assess dopamine D{sub 2}/D{sub 3} receptor availability in patients treated with olanzapine by means of iodine-123 iodobenzamide [{sup 123}I]IBZM single-photon emission tomography (SPET), (b) to compare the results with findings of [{sup 123}I]IBZM SPET in patients under treatment with risperidone and (c) to correlate the results with the occurrance of extrapyramidal side-effects (EPMS). Brain SPET scans were performed in 20 schizophrenic patients (DSM III R) at 2 h after i.v. administration of 185 MBq [{sup 123}I]IBZM. Images were acquired using a triple-head gamma camera (Picker Prism 3000 XP). For semiquantitative evaluation of D{sub 2}/D{sub 3} receptor binding, transverse slices corrected for attenuation were used to calculate specific uptake values [STR-BKG]/BKG (STR=striatum; BKG=background). The mean daily dose of olanzapine ranged from 0.05 to 0.6 mg/kg body weight. The dopamine D{sub 2}/D{sub 3} receptor binding was reduced in all patients treated with olanzapine. Specific IBZM binding [STR-BKG]/BKG ranged from 0.13 to 0.61 (normal controls >0.95). The decreased D{sub 2}/D{sub 3} receptor availability revealed an exponential dose-response relationship (r=-0.85, P<0.001). The slope of the curve was similar to that of risperidone and considerably higher than that of clozapine as compared with the results of a previously published study. EPMS were observed in only one patient, presenting with the lowest D{sub 2}/D{sub 3} availability. The frequency of EPMS induced by olanzapine (5%) was considerably lower than the frequency under risperidone treatment (40%). Our findings

  16. In vivo effects of olanzapine on striatal dopamine D[sub 2]/D[sub 3] receptor binding in schizophrenic patients: an iodine-123 iodobenzamide single-photon emission tomography study

    Energy Technology Data Exchange (ETDEWEB)

    Dresel, S.; Rossmueller, B.; Hahn, K.; Tatsch, K. (Department of Nuclear Medicine, University of Munich (Germany)); Mager, T.; Meisenzahl, E.; Moeller, H.J. (Department of Psychiatry, University of Munich (Germany))

    1999-08-01

    Olanzapine is a new atypical antipsychotic agent that belongs to the same chemical class as clozapine. The pharmacological efficacy of olanzapine (in contrast to that of risperidone) has been shown to be comparable to that of clozapine, but olanzapine has the advantage of producing a less pronounced bone marrow depressing effect than clozapine. The specific aims of this study were (a) to assess dopamine D[sub 2]/D[sub 3] receptor availability in patients treated with olanzapine by means of iodine-123 iodobenzamide [[sup 123]I]IBZM single-photon emission tomography (SPET), (b) to compare the results with findings of [[sup 123]I]IBZM SPET in patients under treatment with risperidone and (c) to correlate the results with the occurrance of extrapyramidal side-effects (EPMS). Brain SPET scans were performed in 20 schizophrenic patients (DSM III R) at 2 h after i.v. administration of 185 MBq [[sup 123]I]IBZM. Images were acquired using a triple-head gamma camera (Picker Prism 3000 XP). For semiquantitative evaluation of D[sub 2]/D[sub 3] receptor binding, transverse slices corrected for attenuation were used to calculate specific uptake values [STR-BKG]/BKG (STR=striatum; BKG=background). The mean daily dose of olanzapine ranged from 0.05 to 0.6 mg/kg body weight. The dopamine D[sub 2]/D[sub 3] receptor binding was reduced in all patients treated with olanzapine. Specific IBZM binding [STR-BKG]/BKG ranged from 0.13 to 0.61 (normal controls >0.95). The decreased D[sub 2]/D[sub 3] receptor availability revealed an exponential dose-response relationship (r=-0.85, P<0.001). The slope of the curve was similar to that of risperidone and considerably higher than that of clozapine as compared with the results of a previously published study. EPMS were observed in only one patient, presenting with the lowest D[sub 2]/D[sub 3] availability. The frequency of EPMS induced by olanzapine (5%) was considerably lower than the frequency under risperidone treatment (40%). Our findings

  17. Treatment of bipolar disorder: Review of evidence regarding quetiapine and lithium.

    Science.gov (United States)

    Ketter, Terence A; Miller, Shefali; Dell'Osso, Bernardo; Wang, Po W

    2016-02-01

    Lithium, the prototypical mood stabilizer, and quetiapine, a second-generation antipsychotic, are widely used acute and maintenance pharmacotherapies for bipolar disorder. The Clinical and Health Outcomes Initiative in Comparative Effectiveness for Bipolar Disorder (Bipolar CHOICE) study was the first comparative effectiveness assessment of lithium versus quetiapine (in combination with adjunctive personalized treatment), and found no overall significant differences in efficacy and safety/tolerability outcomes between lithium and quetiapine. Completion of Bipolar CHOICE offers a timely opportunity to review the evidence regarding lithium and quetiapine for bipolar disorder. Controlled clinical trials and real-world observational studies that included quetiapine and lithium as monotherapy or as combination therapy were identified by literature search. Selected studies were reviewed in detail. Review of the available trials suggested comparable efficacy of quetiapine and lithium in acute mania, and possibly greater efficacy for quetiapine compared with lithium in acute bipolar depression and in prevention of recurrent (particularly depressive) episodes. Combination therapy including quetiapine and lithium was generally more effective than either agent alone in acute mania and bipolar maintenance, although adding lithium to quetiapine did not increase efficacy in acute bipolar depression. Safety data for quetiapine and lithium were consistent with the established profiles of the two treatments. Limitations include those of the available efficacy and effectiveness trial data. Quetiapine and lithium have overlapping but distinctive roles in different phases of bipolar disorder, and further studies of these agents (particularly in combination with one another) are warranted. Copyright © 2015 Elsevier B.V. All rights reserved.

  18. RISPERIDONE IN INDIAN PATIENTS WITH SCHIZOPHRENIA

    Science.gov (United States)

    Agarwal, A.K.; Bashyam, V.S.P; Channabasavanna, S.M.; Dhavale, H.S.; Khan, M.A.M.; Khanna, Sumant; Pradhan, P.V.; Katiyar, M.; Rajkumar, R.; Niazi, Faiz R.; Jalali, R.K.; Gowrishankar, R.; Mishra, S.K.; Sood, O.P.

    1998-01-01

    Conventional antipsychotic agents are not effective against negative symptoms of schizophrenia and are also noted for their extrapyramidal side effects. Risperidone is a noval antipsychotic agent whose dual antagonism of dopamine and serotonin receptors is believed to underlie its efficacy against negative symptoms and the low incidence of extrapyramidal side effects. An open, non-comparative study of seven weeks duration was performed to evaluate risperidone in the treatment of schizophrenia in Indian patients. Previous antipsychotic therapy was discontinued for a week before risperidone therapy was initiated. At the end of six weeks of risperidone therapy, clinical improvement (≥ 20% reduction in total score on positive and negative syndrome scale for schizophrenia (PANSS;; was shown by 128 (87.7%) of the 146 evaluable patients. Statistically significant reduction (p < 0.05) occurred in the total score of this scale and in the subscale scores for positive, negative and general psychopathology symptoms and in the clinical global impression severity score. The number of patients with adverse experiences were 108 (65.5%) at baseline and 120 (72.7%) at the end of risperidone therapy. Extrapyramidal symptoms, seen in 65 (39.4%) patients compared to 22 (13.3%) patients at baseline, were largely mild to moderate in intensity. PMID:21494480

  19. Olanzapine-Induced Hypertriglyceridemia Resulting in Necrotizing Pancreatitis

    Science.gov (United States)

    Roy-Chaudhury, Prabir; Yadlapalli, Ganesh

    2016-01-01

    Olanzapine is an atypical antipsychotic agent that was approved by the Food and Drug Administration in 1996 for treatment of psychotic disorders, bipolar disorder, and schizophrenia. Since that time, numerous case reports have been published that describe the association of olanzapine and the development of pancreatitis. Furthermore, 3 reports suggest the mechanism of olanzapine-induced hypertriglyceridemia as the etiology of this progression. We report a case of a 36-year-old man who developed necrotizing pancreatitis secondary to olanzapine-induced hypertriglyceridemia. This case, to our knowledge, is the most severe case of this progression and the first case requiring plasmapheresis for acute management.

  20. Risperidone associated paralytic ileus in schizophrenia

    Directory of Open Access Journals (Sweden)

    Parthasarathy Ramamourthy

    2013-01-01

    Full Text Available A 32-year-old man, diagnosed with catatonic schizophrenia, was treated with risperidone and lorazepam in the general hospital psychiatry setup. He developed signs of intestinal obstruction, which was diagnosed as paralytic ileus and was treated conservatively along with stopping the offending drug. Risperidone is said to be devoid of anticholinergic side effects, but prevalence of these varies from 7% to 13% in patients receiving treatment for schizophrenia. Constipation has been reported but fatal adverse effect like paralytic ileus with risperidone is rarely reported. Timely diagnosis can save the need for surgical interventions and fatal complications. This predisposition in schizophrenia could be due to neurodevelopmentally shared abnormality of brain and gut nervous system.

  1. Gynecomastia with risperidone-fluoxetine combination.

    Science.gov (United States)

    Benazzi, F

    1999-01-01

    Gynecomastia (breast enlargement) is a side effect of neuroleptic antipsychotic drugs, related to prolactin elevation caused by dopamine D2 receptor blockade (Richelson, 1996). The atypical antipsychotic risperidone is less likely to cause gynecomastia at low doses (Casey, 1996). It can cause a dose-dependent increase in serum prolactin concentration (Peuskens, 1995), by blocking dopamine D2 receptors (Richelson, 1996). I would like to describe a patient who did not have gynecomastia with risperidone at a dose of 3 mg/day, but had it when risperidone, at a dose of 0.5 mg/day, was combined with fluoxetine. A MEDLINE search failed to find any reports about such an interaction.

  2. Quetiapine and clarithromycin-induced neuroleptic malignant syndrome.

    Science.gov (United States)

    Christodoulou, Christos; Margaritis, Dimitris; Makris, Gerasimos; Kavatha, Dimitra; Efstathiou, Vasiliki; Papageorgiou, Charalabos; Douzenis, Athanasios

    2015-01-01

    We report a case of neuroleptic malignant syndrome possibly caused by the combined administration of quetiapine and clarithromycin in a 75-year-old male patient. He was receiving quetiapine regularly. Two days before his admission to the hospital, he had been feverish and started receiving clarithromycin without consulting a doctor. Clarithromycin administration was interrupted 3 days after his admission because it was ineffective and because his clinical state was deteriorating. The patient presented altered level of consciousness and excessive muscular rigidity on his limbs, while he remained feverish (38.7 °C). Laboratory abnormalities included elevated serum creatine phosphokinase level (5.387 U/L), leukocytosis, and low serum iron. The patient was diagnosed with neuroleptic malignant syndrome, and quetiapine was immediately discontinued. After the following days, his muscle rigidity and mental status ameliorated, his fever withdrew, and his laboratory findings improved. The various features of the case are discussed in view of the fact that the concomitant administration of cytochrome 3A4 inhibitors, such as clarithromycin, is suggested to cause an increase of plasma concentrations of quetiapine. Thus, physicians should have a high index of suspicion of the interactions of commonly administered medications.

  3. The management of schizophrenia: focus on extended-release quetiapine fumarate

    Directory of Open Access Journals (Sweden)

    Peuskens J

    2011-09-01

    Full Text Available Joseph Peuskens Universitair Psychiatrisch Centrum KU Leuven, Campus St Jozef Kortenberg, Kortenberg, Belgium Abstract: Effective management of schizophrenia remains a significant clinical challenge. While antipsychotic medications have proven efficacy in this disease, there remains an opportunity to further improve symptom control and long-term relapse prevention. Also, a number of factors, including tolerability and complex dosing regimens, can result in nonadherence to medication. Quetiapine is an atypical antipsychotic with proven efficacy and an established tolerability profile in schizophrenia. The once-daily extended-release formulation (quetiapine XR offers a simplified dosing regimen and titration schedule. Short-term clinical studies have shown that quetiapine XR (400–800 mg/d is efficacious in the acute treatment of schizophrenia, while a long-term study has shown that quetiapine XR was significantly more effective than placebo at preventing relapse. Furthermore, an investigation in which stable patients switched from the immediate-release formulation (quetiapine IR to quetiapine XR showed that quetiapine XR is generally well tolerated and has no loss of efficacy compared with quetiapine IR. In patients who experienced insufficient efficacy or poor tolerability on their previous antipsychotic, switching to quetiapine XR significantly improved efficacy compared with the previous treatment. In conclusion, quetiapine XR is an effective and generally well tolerated treatment for schizophrenia. Furthermore, once-daily dosing may improve patient adherence, which may impact positively on patient outcomes. Keywords: adherence, atypical antipsychotics, adverse events

  4. Olanzapine-Induced Neuroleptic Malignant Syndrome

    Directory of Open Access Journals (Sweden)

    Seyedhamze Hosseini

    2017-05-01

    Full Text Available Neuroleptic malignant syndrome (NMS is a rare but life-threatening idiosyncratic side effect resulting from neuroleptic drugs. NMS mainly occurs in patients treated with high-potency typical antipsychotics, but rarely caused by atypical antipsychotics. Although NMS is less common with atypical antipsychotic, but it seems that its incidence is rising due to increased administration of such drugs. We present the case of a 27-year-old man with a history of paranoid schizophrenia that showed signs consistent with NMS that occurred after treatment with olanzapine. The patient was adherent to treatment. He had decreased level of consciousness, muscle rigidity, diaphoresis, fever, drooling, urinary incontinence, and high blood pressure. This patient illustrates that NMS can occur due to treatment with atypical antipsychotic drugs like olanzapine, particularly in the presence of risk factors. This phenomenon is often unrecognized, underdiagnosed, or not treated properly. Physicians should be aware that NMS with extrapyramidal syndrome could occur with olanzapine at steady state doses without recent dosage adjustments or titration. It is essential that adequate and safe dose of medication is chosen and the patient is monitored by the signs and symptoms of this lethal syndrome.

  5. Costi ed effetti di Risperidone Long Acting (RLA rispetto ad antipsicotici atipici nel trattamento dei soggetti schizofrenici in Italia

    Directory of Open Access Journals (Sweden)

    Lorenzo G. Mantovani

    2004-03-01

    Full Text Available Objective: to estimate the costs and effects of long-acting risperidone (LAR in the treatment of schizophrenic patients in Italy, as compared to conventional and oral atypical antipsychotics. Methods: a discrete event model was used. The model simulates patients. history for every single therapeutic alternative and selects incident events, on the basis of pre-defined probability distribution-powered, randomized repetitions. The model operates on two types of parameters: patient characteristics and time-dependent variables. Patient characteristics (age, sex, illness profile and severity, probability of incurring in an adverse event and potential dangerousness remain fixed during the 5 simulated years. Time-dependent variables are subject to changes and include outpatient visits, severity of psychotic episodes, symptom-scores, compliance, incidence of adverse effects, site of treatment and dangerousness. Three treatments have been selected: scenario 1 begins with LAR, switches to olanzapine and then to clozapine; scenario 2 starts with olanzapine, switches to oral risperidone and ends with clozapine. Direct medical costs have been computed on the basis of psychiatric visits, drug costs and costs of the institution in which the patient is treated (hospital, rehabilitation clinic, etc. Outcome measures were number of psychotic episodes in 5 years, total time spent during these episodes and cumulative score of positive and negative symptoms at 5 years. Information on alternatives, transition probabilities, model structure and health resources utilization were derived from the literature and from a panel of experts. Results: it has been estimated that LAR is economically dominant (more effective at lower cost respect to oral atypical antipsychotics, being able to prevent 0.87 psychotic episodes per patient, with a net cost saving of 4,773 euro per patient. Sub-group analysis indicate that LAR is always more effective than the considered alternatives

  6. Risperidone for the treatment of delusional disorder.

    Science.gov (United States)

    Fear, Christopher F; Libretto, Susan E

    2002-01-01

    The overlap between diagnostic criteria for schizophrenia and delusional disorder (DD) may cause diagnostic confusion. This is important if response to treatment differs. Risperidone, an atypical antipsychotic, is established in the treatment of schizophrenia, although less so in other psychotic conditions. We report the case of a woman who developed DD, persecutory type, at the age of 50 years. Treatment with sulpiride 200-800 mg daily caused side-effects of drowsiness and 'hangover' and, consequently, non-compliance. Written informed consent was gained for a 24-week, randomized, double-blind, placebo-controlled, crossover trial of risperidone, initiated at 1 mg daily and increasing to 2 mg daily. Significant improvement was found, as assessed by the Brief Psychiatric Rating Scale, Positive and Negative Symptom Schedule and Maudsley Assessment of Delusions Schedule. We believe that this is the first case study reporting the resolution of persecutory DD with risperidone. A controlled clinical trial of risperidone in the treatment of patients with DD is warranted. (Int J Psych Clin Pract 2002; 6: 113-116).

  7. Olanzapine affects locomotor activity and meal size in male rats

    NARCIS (Netherlands)

    van der Zwaal, Esther M.; Luijendijk, Mieneke C. M.; Evers, Simon S.; la Fleur, Susanne E.; Adan, Roger A. H.

    2010-01-01

    Olanzapine is an antipsychotic drug that frequently induces weight gain accompanied by increased fat deposition as a side effect To investigate how olanzapine affects different aspects of energy balance we used male rats to determine effects on meal patterns food preference locomotor activity and

  8. Tolerability and efficacy of paliperidone ER compared to olanzapine in the treatment of schizophrenia: A randomized, double-blind, multicentric trial

    Directory of Open Access Journals (Sweden)

    Sandip Shah

    2011-01-01

    Full Text Available Background: Paliperidone is an active metabolite of risperidone and actss through a combination of central dopamine Type 2 (D2 and serotonin Type 2 (5HT2A receptor antagonism. Aim: The present randomized, double-blind, multicentric trial was designed to determine the safety and efficacy of paliperidone extended release (ER compared to olanzapine in the treatment of acute schizophrenia. Materials and Methods: A total of 214 patients with diagnosis of schizophrenia were randomized to paliperidone ER (n=109 and olanzapine (n=106 treatment groups. Totally 206 patients were evaluated for efficacy parameters using Positive and negative syndrome scale (PANSS score and Clinical Global Impression-severity of illness (CGI-S and Clinical Global Impression-improvement of illness (CGI-I scales. Safety was assessed by treatment-emergent adverse events and movement disorders. Results: All patients showed significant reduction in PANSS scores at the end of treatment. However, the results were comparable and there was no significant difference at the end of the trial between paliperidone ER group and olanzapine group. Both the treatment groups showed decrease in the severity of illness and improvement in symptomatology. The most common adverse events reported in paliperidone ER versus olanzapine group were Extra Pyramidal Syndrome (EPS (13.7% vs. 15.6%, headache (12.7% vs. 8.9%, increased appetite (8.8% vs. 10.0% and drowsiness (4.9% vs. 303%. There was no clinically relevant difference in change from baseline to the end of the trial in abnormal involuntary movement scale (AIMS and barnes akathisia rating scale (BARS total scores between both the groups. Conclusion: Paliperidone ER is effective in controlling schizophrenic symptoms as well as exhibits comparable tolerability profile. Thus, paliperidone ER has the potential to be a useful new treatment option for patients with schizophrenia.

  9. Aggravation of Hypertriglyceridemia and Acute Pancreatitis in a Bipolar Patient Treated with Quetiapine

    OpenAIRE

    Liou, Li-Syue; Hung, Yi-Jen; Hsieh, Chang-Hsun; Hsiao, Fone-Ching

    2014-01-01

    Pancreatitis is a very rare adverse effect of quetiapine treatment, with only 5 cases of quetiapine-associated pancreatitis reported in the English literature to date. Herein, we report one patient who developed severe hypertriglyceridemia (>1000 mg/dL) after quetiapine administration, resulting in acute pancreatitis. An analysis of the underlying pathogenic mechanisms and a review of relevant literature are also presented. Clinicians should be aware of the potentially life-threatening metabo...

  10. Adverse events in children and adolescents treated with quetiapine

    DEFF Research Database (Denmark)

    Jakobsen, Klaus D; Wallach-Kildemoes, Helle; Bruhn, Christina H

    2017-01-01

    Quetiapine is a low-affinity dopamine D2 receptor antagonist, approved for the treatment of bipolar disorder and schizophrenia in children and adolescents by the Food and Drug Administration, but not by European Medicine Agency. Although knowledge of adverse drug reactions in children and adolesc......Quetiapine is a low-affinity dopamine D2 receptor antagonist, approved for the treatment of bipolar disorder and schizophrenia in children and adolescents by the Food and Drug Administration, but not by European Medicine Agency. Although knowledge of adverse drug reactions in children...... 10–17 years) and six patients were boys. The main reported ADEs were (i) endocrine, for example, hyperprolactinemia and hyperthyroidism, (ii) cardiac, for example, tachycardia and QT prolongation, (iii) neurological, for example, seizures and cerebral hemorrhage, and (iv) psychiatric, for example...

  11. Restless Legs Syndrome After Single Low Dose Quetiapine Administration.

    Science.gov (United States)

    Soyata, Ahmet Z; Celebi, Fahri; Yargc, Lutfi I

    2016-01-01

    Restless legs syndrome is an underdiagnosed sensori-motor disorder and psychotropic drugs are one of the main secondary causes of the illness. The most common psychotropic agents that cause restless legs syndrome are antidepressants; however, antipsychotics have also been reported to induce restless legs syndrome. The prevalence, vulnerability factors and the underlying mechanism of antipsychotic-induced restless legs syndrome are unclear. A possible explanation is that dopaminergic blockade is the main precipitator of the syndrome. Quetiapine-induced restless legs syndrome is another point of interest because of its low binding to D2 receptors. We herein report the case of a restless legs syndrome that emerged after a single low dose quetiapine administration.

  12. Quetiapine modulates functional connectivity in brain aggression networks.

    Science.gov (United States)

    Klasen, Martin; Zvyagintsev, Mikhail; Schwenzer, Michael; Mathiak, Krystyna A; Sarkheil, Pegah; Weber, René; Mathiak, Klaus

    2013-07-15

    Aggressive behavior is associated with dysfunctions in an affective regulation network encompassing amygdala and prefrontal areas such as orbitofrontal (OFC), anterior cingulate (ACC), and dorsolateral prefrontal cortex (DLPFC). In particular, prefrontal regions have been postulated to control amygdala activity by inhibitory projections, and this process may be disrupted in aggressive individuals. The atypical antipsychotic quetiapine successfully attenuates aggressive behavior in various disorders; the underlying neural processes, however, are unknown. A strengthened functional coupling in the prefrontal-amygdala system may account for these anti-aggressive effects. An inhibition of this network has been reported for virtual aggression in violent video games as well. However, there have been so far no in-vivo observations of pharmacological influences on corticolimbic projections during human aggressive behavior. In a double-blind, placebo-controlled study, quetiapine and placebo were administered for three successive days prior to an fMRI experiment. In this experiment, functional brain connectivity was assessed during virtual aggressive behavior in a violent video game and an aggression-free control task in a non-violent modification. Quetiapine increased the functional connectivity of ACC and DLPFC with the amygdala during virtual aggression, whereas OFC-amygdala coupling was attenuated. These effects were observed neither for placebo nor for the non-violent control. These results demonstrate for the first time a pharmacological modification of aggression-related human brain networks in a naturalistic setting. The violence-specific modulation of prefrontal-amygdala networks appears to control aggressive behavior and provides a neurobiological model for the anti-aggressive effects of quetiapine.

  13. Immunosuppressant-Associated Neurotoxicity Responding to Olanzapine

    Directory of Open Access Journals (Sweden)

    James A. Bourgeois

    2014-01-01

    Full Text Available Immunosuppressants, particularly tacrolimus, can induce neurotoxicity in solid organ transplantation cases. A lower clinical threshold to switch from tacrolimus to another immunosuppressant agent has been a common approach to reverse this neurotoxicity. However, immunosuppressant switch may place the graft at risk, and, in some cases, continuation of the same treatment protocol may be necessary. We report a case of immunosuppressant-associated neurotoxicity with prominent neuropsychiatric manifestation and describe psychiatric intervention with olanzapine that led to clinical improvement while continuing tacrolimus maintenance.

  14. Il trattamento dei disturbi psicotici con olanzapina, risperidone e neurolettici tipici: una valutazione comparativa di costo/efficacia in una realtà psichiatrica locale

    Directory of Open Access Journals (Sweden)

    Egidio Filippelli

    2005-09-01

    Full Text Available BACKGROUND: Several clinical trials demonstrated that atypical antipsychotics are more effective but also more expensive (as drug cost compared with the typical neuroleptics by treating psychotic disorders. The present study aimed to evaluate this result using an observational approach which better reflects the real clinical practice. OBJECTIVE: To evaluate clinical effectiveness (including work and social functioning and overall direct costs in a group of patients affected by psychotic disorders (schizophrenia and bipolar and treated with typical and atypical (olanzapine and risperidone antipsychotics. METHODS: With a multicentre observational design - two years long - 89 patients (in charge by Psychiatric Centers of Regione Campania - Italy were assessed using CGI (Clinical Global Impression and GAF (Global Assessment of Functioning scales. Moreover economic data were collected with reference to pharmacological and non-pharmacological (hospitalization, medical/nurse visits, etc. resources consumption. The pharmacoeconomic analysis were conducted choosing the perspective of the local Psychiatric Services for costs attribution. RESULTS: Considering the treatment outcomes, the use of the atypical drugs provided better performances with reference to the patients quality of life. The results in terms of work and social functioning indicated an advantage in the olanzapine group of patients. Overall direct costs of treatment (drugs and healthcare resources didn’t generate significant differences among the groups of therapy despite the pharmacological cost evidentiated an economic advantage (p<0,05 in the typical group due to the cheaper cost of these drugs. The use of olanzapine was associated to a lower number of hospitalizations and showed a general reduction (- 16% of total treatment costs between 1st and 2nd year of observation. CONCLUSIONS: The lack of side effects, the improvement in work and social functioning, associated to a more efficient

  15. Combination quetiapine therapy in the long-term treatment of patients with bipolar I disorder

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    Calabrese JR

    2005-07-01

    Full Text Available Abstract Objective Determine the long-term effectiveness of quetiapine in combination with standard treatments in preventing relapses for patients with bipolar I disorders Method Twenty-one outpatients with type I bipolar disorder who had inadequate responses to ongoing standard therapies were treated with add-on quetiapine in an open-label study. The quetiapine dose was increased until clinical response occurred. Illness response was assessed using the Clinical Global Impression (CGI scale. Relapse rates before and during quetiapine treatment were compared by calculating incidence risk ratios. Results Quetiapine was added to ongoing standard therapy for 26 to 78 weeks. Thirteen patients received combination therapy for at least 52 weeks. The mean quetiapine dose received was 518 ± 244 mg/day. There were highly significant improvements in overall relapse rate, manic/mixed relapse rate, and depression relapse rate in the period during quetiapine treatment compared with the period before quetiapine was initiated. The calculated relative risk of relapse in the absence of quetiapine treatment was 2.9 overall (95% confidence interval, 1.5~5.6, 3.3 for manic/mixed relapse (95% confidence interval, 1.5~7.1, and 2.4 for depressive relapse (95% confidence interval, 1.3~4.4. The mean Clinical Global Impression scores improved significantly from baseline during 26 weeks of quetiapine treatment in 21 patients (p = 0.002 and remained significantly better during a 52-week treatment period in 13 patients (p = 0.036. Conclusion Long-term treatment with quetiapine combination therapy reduced the probability of manic/mixed and depressive relapses and improved symptoms in patients with bipolar I disorder who had inadequate responses to ongoing standard treatment.

  16. Update on extended release quetiapine fumarate in schizophrenia and bipolar disorders

    Directory of Open Access Journals (Sweden)

    El-Khalili N

    2012-11-01

    Full Text Available Nizar El-KhaliliAlpine Clinic, Lafayette, IN, USAAbstract: The atypical antipsychotic quetiapine fumarate is available both as an immediate release (IR and as an extended release (XR formulation allowing flexibility of dosing for individual patients. Approved uses of quetiapine XR include the treatment of schizophrenia (including maintenance therapy for prevention of relapse, the treatment of bipolar disorder (manic and depressive episodes, and the prevention of recurrence in patients with bipolar disorder who respond to quetiapine XR. This narrative review provides an update on quetiapine XR in these indications. The pharmacological profile of quetiapine, including a moderate affinity for dopamine D2 receptors and higher affinity for serotonin 5-hydroxytryptophan (5-HT2A receptors, may explain its broad efficacy and low propensity for extrapyramidal symptoms (EPS. The XR formulation has similar bioavailability but prolonged plasma levels compared with the IR formulation, allowing for less frequent (once-daily dosing. Clinical studies have confirmed the efficacy of quetiapine XR in relieving the acute symptoms of schizophrenia during short-term trials, and reducing the risk for relapse in long-term studies. Direct switching from the IR formulation to the same dose of the XR formulation did not reveal any loss of efficacy or tolerability issues, and switching patients to quetiapine XR from conventional or other atypical antipsychotics (for reasons of insufficient efficacy or tolerability also proved to be beneficial and generally well tolerated. In bipolar disorder, quetiapine XR has also proven effective in relieving acute depressive and manic symptoms. Adverse events with quetiapine XR in patients with either schizophrenia or bipolar disorder are similar to those associated with the IR formulation, the most common being sedation, dry mouth, somnolence, dizziness, and headache. The low propensity for EPS is maintained with the XR formulation

  17. Multiple dose pharmacokinetics of quetiapine and some of its metabolites in Chinese suffering from schizophrenia

    Institute of Scientific and Technical Information of China (English)

    Kun-yan LI; Xin LI; Ze-neng CHENG; Wen-xing PENG; Bi-kui ZHANG; Huan-de LI

    2004-01-01

    AIM: To study the multiple dose pharmacokinetics of quetiapine and its sulfoxide-, 7-hydroxy-, 7-hydroxy-Ndealkyl-metabolites in Chinese suffering from schizophrenia. METHODS: Twenty-one patients (11 females and 10males) were given quetiapine twice daily to control the symptoms. After the dose reached 200 mg twice daily,blood were sampled to study the pharmacokinetics. The plasma concentrations of quetiapine and its metabolites were assayed by HPLC-MS. RESULTS: The main pharmacokinetic parameters of quetiapine, 7-hydroxy-N-dealkylquetiapine, quetiapine sulfoxide, and 7-hydroxy-quetiapine were as follows: tmax were 2.0 (0.3-5.0), 4.0 (1.5-6.0),3.0 (0.5-5.0), and 3.0 (0.5-5.0) h respectively; t1/2 were (7±3), (9.4±2.7), (7±3), and (8±5) h, respectively; CSSmaxwere (678±325), (19±5), (451±216), and (58±22) μg/L, respectively; CSSmin were (51±68), (3.3±1.6), (35±36), and (5±4) μg/L, respectively; CSSav were (295±144), (13±4), (209±71), and (28±9) μg/L, respectively; AUCSS0-12 were (0.103±0.028) h-1, respectively; CL/F and V/F of quetiapine were (67±25) L.h-1 and (672±394) L, respectively.The plasma concentrations for the four compounds reached a steady state within 48 h at the dose of 200 mg initiation. These parameters were not statistically different between genders. CONCLUSIONS: Quetiapine was absorbed quickly, distributed widely, and metabolized mainly to be quetiapine sulfoxide. The elimination speeds of quetiapine and its three metabolites were similar. Gender had no effect on the pharmacokinetics of quetiapine and its metabolites. The clinical dosage regime caused no drug accumulation.

  18. Preparation, Characterization and Evaluation of Quetiapine Fumarate Solid Lipid Nanoparticles to Improve the Oral Bioavailability

    Directory of Open Access Journals (Sweden)

    Arjun Narala

    2013-01-01

    Full Text Available Quetiapine fumarate is an antipsychotic drug with poor oral bioavailability (9% due to first-pass metabolism. Present work is an attempt to improve oral bioavailability of quetiapine fumarate by incorporating in solid lipid nanoparticles (SLN. Six quetiapine fumarate SLN formulations were developed using three different lipids by hot homogenisation followed by ultrasonication. The drug excipient compatibility was studied by differential scanning calorimetry (DSC. Stable quetiapine fumarate SLNs having a mean particle size of 200–250 nm with entrapment efficiency varying in between 80% and 92% were developed. The physical stability of optimized formulation F3 was checked at room temperature for 2 months. Comparative bioavailability studies were conducted in male Wistar rats after oral administration of quetiapine fumarate suspension and SLN formulation. The relative bioavailability of quetiapine fumarate from optimized SLN preparation was increased by 3.71 times when compared with the reference quetiapine fumarate suspension. The obtained results are indicative of SLNs as potential lipid carriers for improving the bioavailability of quetiapine fumarate by minimizing first-pass metabolism.

  19. Effects of Green Tea Extracts on the Pharmacokinetics of Quetiapine in Rats

    Directory of Open Access Journals (Sweden)

    Essam Ezzeldin

    2015-01-01

    Full Text Available Quetiapine is an atypical antipsychotic, used clinically in the treatment of schizophrenia, acute mania in bipolar disorders, and bipolar depression in adults. In this study, the effect of green tea extracts (GTE on the pharmacokinetics of quetiapine (substrate of CYP3A4 was investigated in rats. Male Wistar albino rats received GTE (175 mg/kg or saline (control by oral gavage for 7 days before a single intragastric administration of 25 mg/kg quetiapine. Plasma concentrations of quetiapine were measured up to 12 h after its administration by a validated ultraperformance liquid chromatography-tandem mass spectroscopy. Pretreatment with GTE produced significant reductions in the maximum plasma concentration and area under the curve of quetiapine by 45% and 35%, respectively, compared to quetiapine alone. However, GTE did not produce significant change in elimination half-life and oral clearance of quetiapine. This study concluded that GTE may decrease the bioavailability of quetiapine when coadministered.

  20. Plasma quetiapine in relation to prescribed dose and other factors: data from a therapeutic drug monitoring service, 2000–2011

    Science.gov (United States)

    Bowskill, Sally V.J.; Patel, Maxine X.; Flanagan, Robert J.

    2013-01-01

    Objective: Suggested predose plasma quetiapine target ranges for effective therapy in schizophrenia lie between 50 and 500 µg/l. We aimed to examine data from a quetiapine therapeutic drug monitoring (TDM) service to assess the plasma quetiapine concentrations attained at specified doses in clinical practice. Method: We studied TDM data from patients given immediate-release quetiapine in the period 2000–2011. Results: There were 946 samples from 487 patients (257 males, age at time of first sample, median [range] 34 [14–87] years, and 230 females, age at time of first sample, median [range] 38 [10–92] years). The plasma quetiapine concentration was <50 and <100 µg/l in 30% and 50% of samples, respectively (no quetiapine detected in 9% of samples). The relationship between dose and plasma quetiapine was poor. The mean (95% confidence interval [CI]) quetiapine dose was higher (t = 3.6, df = 446, p <0.01) in males versus females (641 [600–1240] and 548 [600–943] mg/day, respectively), although there was no difference in median dose (600 mg/day) or in the mean (95% CI) plasma quetiapine concentrations attained. Smoking habit had no discernible effect on plasma quetiapine concentration. Conclusions: There was a poor relationship between dose and plasma quetiapine concentration in this study, as found by others. This is probably because of the short plasma half-life of the drug, at least in part. Nevertheless, quetiapine TDM can help assess adherence and measurement of quetiapine metabolites, notably N-desalkylquetiapine, as well as quetiapine itself may enhance the value of quetiapine TDM in future. PMID:24167685

  1. Naturalistic study of olanzapine in treatment-resistaant ...

    African Journals Online (AJOL)

    Naturalistic study of olanzapine in treatment-resistaant schizophrenia and acute mania, depression and obsessional disorder. ... depression, four obsessive compulsive disorder (OCD), one each had schizo-affective and delusional disorders, ...

  2. Effects of repeated quetiapine treatment on conditioned avoidance responding in rats.

    Science.gov (United States)

    Gao, Jun; Feng, Min; Swalve, Natashia; Davis, Collin; Sui, Nan; Li, Ming

    2015-12-15

    The present study characterized the behavioral mechanisms of avoidance-disruptive effect of quetiapine in the conditioned avoidance response test under two behavioral testing (2 warning signals vs. 1 warning signal) and two drug administration conditions (subcutaneous vs. intravenous). In Experiments 1 and 2, well-trained adult male Sprague-Dawley rats were tested under the subcutaneous (s.c.) quetiapine treatment (5.0, 15.0, 25.0, 50.0mg/kg) for 7 days in a novel procedure consisting of two conditioned stimuli (CS) (white noise serving as CS1 and pure tone as CS2). Only the highest dose (50.0mg/kg) produced a persistent suppression of the avoidance response without impairing the escape response. The magnitude of suppression of the CS1 avoidance was similar to that of CS2 avoidance. No significant group difference was found in the quetiapine (15.0mg/kg, s.c.) challenge test, indicating a lack of a long-term quetiapine effect. In Experiment 3, well-trained rats were tested under the intravenous (i.v.) quetiapine treatment (3.0, 9.0, 15.0mg/kg) for 5 days and challenged with quetiapine (6.0mg/kg, i.v. followed by 9.0mg/kg, s.c.). Only the white noise was used as the CS. Similar to what was being observed in Experiments 1 and 2, intravenously administered quetiapine dose-dependently suppressed avoidance responding during the drug test days, but did not alter drug sensitivity in the challenge days. Thus, quetiapine does not appear to show a preferential inhibition of the avoidance response to a less salient stimulus; and prior quetiapine treatment (s.c. and i.v.) does not cause a sensitization or tolerance to quetiapine.

  3. RISPERIDONE - INDUCED TARDIVE DYSKINESIA : CASE REPORT AND REVIEW OF LITERATURE

    OpenAIRE

    Kumar, P.N. Suresh; Andrade, Chittaranjan

    2001-01-01

    Risperidone is an atypical antipsychotic with broad spectrum of antipsychotic activity and lower potential for extrapyramidal side effects at therapeutic doses. This case report illustrates the development of tardive dyskinesia with therapeutic dose of risperidone in a paranoid schizophrenic patient who was not on any antipsychotic medication previously.

  4. Euprolactinemic gynecomastia and galactorrhea with risperidone-fluvoxamine combination.

    Science.gov (United States)

    Pratheesh, P J; Praharaj, Samir Kumar; Srivastava, Ashish

    2011-01-01

    Risperidone is associated with hyperprolactinemia and its consequent symptoms such as gynecomastia, galactorrhea and sexual dysfunction in adults, and less so in adolescents. Rarely, serotonin reuptake inhibitors are also associated with such adverse effects. We report a case of gynecomastia and galactorrhea in an adolescent male while on a combination of risperidone and fluvoxamine, although the serum prolactin was within normal range.

  5. [Olanzapine improves chorea in patients with Huntington's disease].

    Science.gov (United States)

    Jiménez-Jiménez, F J; de Toledo, M; Puertas, I; Barón, M; Zurdo, M; Barcenilla, B

    The main treatment for choreatic movements associated to Huntington s disease are the neuroleptic drugs, however, its use causes long term troubles. We describe two patients with a predominantly choreic Huntington s disease, who experience improvement of choreatic movements after introduction of olanzapine to their treatment, being this drug well tolerated. The improvement of chorea suggests that olanzapine has a dopaminergic D2 receptors blocking action.

  6. Intramuscular Olanzapine – a UK case series of early cases

    Directory of Open Access Journals (Sweden)

    Taylor Mark

    2007-04-01

    Full Text Available Abstract Background Clinical trials assessing efficacy and safety of Intramuscular (IM Olanzapine in acute schizophrenia and acute mania have previously been undertaken in studies required for drug registration in patients who were required to give informed consent. These patients may have less severe forms of psychosis than patients treated in routine practice. Data derived from naturalistic practice following the launch of IM olanzapine may be helpful for clinicians in assessing efficacy and safety of IM olanzapine. The PANSS-EC scale used in the clinical studies may represent a tool that could be used in routine clinical practice. Case presentation We report on an early unselected case series of 7 patients who received IM olanzapine in routine clinical practice settings in the UK. In this case series, olanzapine IM was generally effective, and no adverse events were reported. Adjunctive benzodiazepines were given concomitantly in 1 of the 7 subjects. This is relevant as concomitant benzodiazepines are not recommended for a minimum of 1 hour post IM olanzapine administration. PANSS-EC data was collected in 2 of the 7 subjects. Conclusion Although patients had greater severity of psychosis than clinical trial patients there were no unexpected findings. In addition the PANSS-EC scale is a scale that may be useful in assessing the efficacy of IM antipsychotics in routine clinical practice.

  7. LC–MS/MS assay for olanzapine in human plasma and its application to a bioequivalence study

    Directory of Open Access Journals (Sweden)

    Dinesh S. Patel

    2012-10-01

    Full Text Available This paper describes a selective and sensitive assay for the determination of olanzapine (OLZ in human plasma based on liquid chromatography–tandem mass spectrometry (LC–MS/MS. The analyte and quetiapine as internal standard (IS were extracted from 200 μL plasma via solid phase extraction on Waters Oasis HLB cartridges. Chromatographic separation was achieved on an ACE 5C18-300 column (100 mm×4.6 mm, 5 μm under isocratic conditions in a run time of 3.5 min. Mass spectrometric detection involved electrospray ionization in the positive ion mode followed by multiple reaction monitoring (MRM of the transitions at m/z 313/256 for OLZ and m/z 384/253 for the IS. The assay was linear in the range 0.10–40.0 ng/mL with a lower limit of quantitation and limit of detection of 0.10 and 0.012 ng/mL, respectively. Intra- and inter-day precision (as coefficient of variation and relative recovery were 90%, respectively. The method was successfully applied to a bioequivalence study of 5 and 10 mg OLZ disintegrating tablets in 40 healthy Indian males with reproducibility by incurred sample reanalysis in the range −7.43 to 8.07%.

  8. Preventing olanzapine-induced weight gain using betahistine: a study in a rat model with chronic olanzapine treatment.

    Science.gov (United States)

    Lian, Jiamei; Huang, Xu-Feng; Pai, Nagesh; Deng, Chao

    2014-01-01

    Olanzapine is the one of first line antipsychotic drug for schizophrenia and other serious mental illness. However, it is associated with troublesome metabolic side-effects, particularly body weight gain and obesity. The antagonistic affinity to histamine H1 receptors (H1R) of antipsychotic drugs has been identified as one of the main contributors to weight gain/obesity side-effects. Our previous study showed that a short term (2 weeks) combination treatment of betahistine (an H1R agonist and H3R antagonist) and olanzapine (O+B) reduced (-45%) body weight gain induced by olanzapine in drug-naïve rats. A key issue is that clinical patients suffering with schizophrenia, bipolar disease and other mental disorders often face chronic, even life-time, antipsychotic treatment, in which they have often had previous antipsychotic exposure. Therefore, we investigated the effects of chronic O+B co-treatment in controlling body weight in female rats with chronic and repeated exposure of olanzapine. The results showed that co-administration of olanzapine (3 mg/kg, t.i.d.) and betahistine (9.6 mg/kg, t.i.d.) significantly reduced (-51.4%) weight gain induced by olanzapine. Co-treatment of O+B also led to a decrease in feeding efficiency, liver and fat mass. Consistently, the olanzapine-only treatment increased hypothalamic H1R protein levels, as well as hypothalamic pAMPKα, AMPKα and NPY protein levels, while reducing the hypothalamic POMC, and UCP1 and PGC-1α protein levels in brown adipose tissue (BAT). The olanzapine induced changes in hypothalamic H1R, pAMPKα, BAT UCP1 and PGC-1α could be reversed by co-treatment of O+B. These results supported further clinical trials to test the effectiveness of co-treatment of O+B for controlling weight gain/obesity side-effects in schizophrenia with chronic antipsychotic treatment.

  9. The efficacy and safety of quetiapine for treatment of geriatric psychosis.

    Science.gov (United States)

    Yang, Cheng-Hung; Tsai, Shih-Jen; Hwang, Jen-Ping

    2005-11-01

    Quetiapine, an atypical antipsychotic, is effective for psychosis in younger patients, with limited adverse effects reported. This open-label naturalistic study was conducted to assess the 4-week efficacy and safety of quetiapine for treatment of geriatric psychosis. Clinical efficacy was evaluated using the Brief Psychiatric Rating Scale (BPRS) and Clinical Global Impression Improvement (CGI-I) instruments before and after 4 weeks of quetiapine treatment. The sample population consisted of 100 geropsychiatric inpatients with psychosis, with the therapeutic evaluation completed by 91. Eighty-one of these 91 patients (89.0%) experienced mild-to-substantial improvement, as determined from the CGI-I. Further, a mean reduction in BPRS score of 39.5% (from baseline) was also determined. The mean daily dose of quetiapine for the fourth week was 276.1 177.2mg/day (range 50-800). Higher quetiapine dosages were administered for patients with functional psychoses compared to an analogous group with organic mental disorders. The most common adverse effects were somnolence (30.0%), lower-limb weakness (28.0%) and dizziness (27.0%). Body weight and fasting triglyceride were significantly elevated after quetiapine treatment (2.2% and 8.9% from baseline, respectively). Based on the results of this study, it appears that quetiapine is an efficacious and safe treatment for geriatric inpatients with psychosis, however, there is a wide dosing range and optimal dosage is diagnosis-dependent.

  10. Discovering risperidone: the LSD model of psychopathology.

    Science.gov (United States)

    Colpaert, Francis C

    2003-04-01

    In the 1970s and 1980s, Janssen Pharmaceutica Research, which had a broad interest in central nervous system disorders and nurtured intellectual freedom, developed original, and at times heretical, concepts. It took decades for the scientific community to endorse some of these concepts. Among them were such notions as an elementary particle of behaviour, the introduction of response quality in receptor theory, and the idea that tolerance does not develop to opioids. These concepts enabled the discovery of the antipsychotic risperidone, a unique full antagonist of the interoceptive effects of LSD.

  11. The antipsychotics clozapine and olanzapine increase plasma glucose and corticosterone levels in rats: comparison with aripiprazole, ziprasidone, bifeprunox and F15063.

    Science.gov (United States)

    Assié, Marie-Bernadette; Carilla-Durand, Elisabeth; Bardin, Laurent; Maraval, Mireille; Aliaga, Monique; Malfètes, Nathalie; Barbara, Michèle; Newman-Tancredi, Adrian

    2008-09-11

    Several novel antipsychotics activate serotonin 5-HT1A receptors as well as antagonising dopamine D2/3 receptors. Such a pharmacological profile is associated with a lowered liability to produce extrapyramidal side effects and enhanced efficacy in treating negative and cognitive symptoms of schizophrenia. However, 5-HT1A receptor agonists increase plasma corticosterone and many antipsychotics disturb the regulation of glucose. Here, we compared the influence on plasma glucose and corticosterone of acute treatments with 'new generation' antipsychotics which target dopamine D2/3 receptors and 5-HT1A receptors, with that of atypical antipsychotics, and with haloperidol. Olanzapine and clozapine, antipsychotics that are known to produce weight gain and diabetes in humans, both at 10 mg/kg p.o., substantially increased plasma glucose (from 0.8 to 1.7 g/l) at 1 h after administration, an effect that returned to control levels after 4 h. In comparison, F15063 (40 mg/kg p.o.) was without effect at any time point. Olanzapine and clozapine dose-dependently increased plasma glucose concentrations as did SLV313 and SSR181507. Haloperidol and risperidone had modest effects whereas aripiprazole, ziprasidone and bifeprunox, antipsychotics that are not associated with metabolic dysfunction in humans, and F15063 had little or no influence on plasma glucose. The same general pattern of response was found for plasma corticosterone levels. The present data provide the first comparative study of conventional, atypical and 'new generation' antipsychotics on glucose and corticosterone levels in rats. A variety of mechanisms likely underlie the hyperglycemia and corticosterone release observed with clozapine and olanzapine, whilst the balance of dopamine D2/3/5-HT1A interaction may contribute to the less favourable impact of SLV313 and SSR181507 compared with that of bifeprunox and F15063.

  12. Quetiapine for acute bipolar depression: a systematic review and meta-analysis.

    Science.gov (United States)

    Suttajit, Sirijit; Srisurapanont, Manit; Maneeton, Narong; Maneeton, Benchalak

    2014-01-01

    Precise estimated risks and benefits of quetiapine for acute bipolar depression are needed for clinical practice. To systematically review the efficacy and the tolerability of quetiapine, either as monotherapy or combination therapy, for acute bipolar depression. We included all randomized, controlled trials (RCTs) comparing quetiapine with other treatments, including placebo, in patients with acute bipolar depression (bipolar I or II disorder, major depressive episode). Published and unpublished RCTs were identified using the Cochrane Central Register of Controlled Trials, MEDLINE, Web of Knowledge, CINAHL, PsycINFO, the EU Clinical Trials Register database, and ClinicalTrials.gov. The primary outcome was the change scores of depression rating scales. Eleven RCTs (n=3,488) were included. Two of them were conducted in children and adolescents. The change in depression scores was significantly greater in the quetiapine group compared with the placebo group (mean difference, [MD] =-4.66, 95% confidence interval [CI] -5.59 to -3.73). The significant difference was observed from week 1. Compared with placebo, quetiapine had higher incidence rates of extrapyramidal side effects, sedation, somnolence, dizziness, fatigue, constipation, dry mouth, increased appetite, and weight gain but lower risks of treatment-emergent mania and headache. Quetiapine treatment was associated with significant improvement of clinical global impression, quality of life, sleep quality, anxiety, and functioning. Quetiapine monotherapy is effective for acute bipolar depression and the prevention of mania/hypomania switching. Its common adverse effects are extrapyramidal side effects, sedation, somnolence, dizziness, fatigue, constipation, dry mouth, increased appetite, and weight gain. The lower risk of headache in quetiapine-treated patients with acute bipolar depression should be further investigated. The evidence for the use of quetiapine combined with mood stabilizers in children and

  13. Prolactin levels and adverse events in patients treated with risperidone.

    Science.gov (United States)

    Kleinberg, D L; Davis, J M; de Coster, R; Van Baelen, B; Brecher, M

    1999-02-01

    Hyperprolactinemia is a common clinical disorder that may lead to sexual dysfunction or galactorrhea. It may arise from a variety of etiologies, including the use of antipsychotic agents, presumably because of a dopamine receptor blockade. This analysis was designed to characterize the relationship between risperidone, serum prolactin levels, and possible clinical sequelae. All data from randomized, double-blind studies of risperidone in patients with chronic schizophrenia were analyzed. The two largest studies (the North American and multinational trials) included 841 patients (259 women, 582 men) with paired prolactin level data and 1,884 patients (554 women, 1,330 men) with data on six adverse events possibly associated with increased prolactin levels (amenorrhea, galactorrhea, and decreased libido in women; erectile dysfunction, ejaculatory dysfunction, gynecomastia, and decreased libido in men). Both risperidone and haloperidol produced dose-related increases in plasma prolactin levels in men and women. Among women, the risperidone dose was not correlated with adverse events, nor were the adverse events correlated with endpoint prolactin levels. Among men, the incidence of adverse events was positively correlated with risperidone dose; however, at risperidone doses of 4 to 10 mg/day the incidence of adverse events was not significantly higher than that observed in patients receiving placebo. Furthermore, adverse events in men were unrelated to plasma prolactin levels. Risperidone-associated increase in serum prolactin levels was not significantly correlated to the emergence of possible prolactin-related side effects.

  14. P-glycoprotein interaction with risperidone and 9-OH-risperidone studied in vitro, in knock-out mice and in drug-drug interaction experiments

    DEFF Research Database (Denmark)

    Ejsing, Thomas B.; Pedersen, Anne D.; Linnet, Kristian

    2005-01-01

    P-glycoprotein, risperidone, nortriptyline, cyclosporine A, drug-drug interaction, blood-brain barrier, knock-out mice......P-glycoprotein, risperidone, nortriptyline, cyclosporine A, drug-drug interaction, blood-brain barrier, knock-out mice...

  15. The extended-release formulation of quetiapine fumarate (quetiapine XR) adjunctive treatment in partially responsive generalized anxiety disorder (GAD): An open label naturalistic study.

    Science.gov (United States)

    Gabriel, A

    2011-01-01

    To assess the effect of adjunctive treatment with extended-release formulation of quetiapine fumarate (quetiapine XR) to other antidepressants in the treatment of partially responsive, poorly functioning patients with generalized anxiety disorder was assessed. Twenty four consenting adult outpatients with confirmed DSM-IV diagnosis of generalized disorder were identified. All patients failed at least one 8-week treatment trial with SSRI or SNRI antidepressant. All were treated with quetiapine XR as an add on treatment to citalopram or vanlafaxine antidepressant for at least 12 weeks. The primary efficacy measure was the Clinical Global Impression Scale (CGI-S). Other scales included; the Hamilton Anxiety Scale (HAM-A) scale, Sheehan Disability Scale, and the Abnormal Involuntary Movement Scale (AIMS). Baseline measures prior to adding quetiapine XR were compared to those at 4, 8 and 12 weeks with the adjunctive treatment. Twenty three patients completed the trial. There was significant rapid resolution of the anxiety symptoms in all effectiveness measures, including the symptoms of anxiety as shown by changes from baseline in HAM-A, and CGI at four weeks. Improvement was maintained to week twelve. Impairments in work, social, and home responsibilities were also reduced significantly, and there were no significant changes in weight at 12 weeks. Patients tolerated the adjunctive treatment well. Quetiapine XR may have anxiolytic properties and could be used effectively as adjunctive treatment with SSRIs in GAD patients with partial response to SSRs or SNRISs. However double blind randomized trials are needed to support these results.

  16. Effects of once-daily extended release quetiapine fumarate (quetiapine XR) on quality of life and sleep in elderly patients with major depressive disorder.

    Science.gov (United States)

    Locklear, Julie C; Svedsäter, Henrik; Datto, Catherine; Endicott, Jean

    2013-07-01

    Major depressive disorder (MDD) is frequently associated with reduced quality of life (QoL) and sleep disturbance. We investigated the effects of once-daily extended release quetiapine fumarate (quetiapine XR) monotherapy on QoL and sleep in elderly patients with MDD. Prospectively planned analysis of patient-reported data from an 11-week (9-week randomized; 2-week post-treatment), double-blind, placebo-controlled, Phase III study. Elderly patients (≥66 years; DSM-IV MDD; Hamilton Rating Scale for Depression [HAM-D] total score ≥22, HAM-D Item 1 score ≥2) were randomized to quetiapine XR (flexible dosing 50-300 mg/day) or placebo. MADRS total score change from randomization at Week 9. Patient-reported outcomes: Quality of Life, Enjoyment and Satisfaction Questionnaire Short Form (Q-LES-Q-SF) % of maximum total score (Items 1-14), Q-LES-Q-SF Item 15 ('satisfaction with medication'), Q-LES-Q-SF Item 16 ('overall life satisfaction'), and Pittsburgh Sleep Quality Index (PSQI) global score. In total, 338 patients were randomized (166 quetiapine XR; 172 placebo). At Week 9, quetiapine XR significantly reduced MADRS total score (-16.33; difference: -7.54; 95% CI: -9.23, -5.85; pelderly patients with MDD. Copyright © 2013. Published by Elsevier B.V.

  17. Case reports of neuroleptic malignant syndrome in context of quetiapine use.

    Science.gov (United States)

    Detweiler, Mark B; Sullivan, Kelly; Sharma, Taral R; Kim, Kye Y; Detweiler, Jonna G

    2013-12-01

    A retrospective analysis was followed on 20 case reports covering the possible correlation between the atypical antipsychotic, quetiapine, and neuroleptic malignant syndrome (NMS), determined by the study of 7 different NMS criteria guidelines. A great majority (19) of the case studies did not meet the requirements of all 7 guidelines, frequently due to unreported information. Nor was quetiapine proven to be the sole cause of the possible NMS in the two age groups investigated. Only one case was found to have no other medication or medical conditions confounding the relationship of quetiapine and NMS symptoms, and that case was in the context of a significant quetiapine overdose. The other 19 cases demonstrated the difficulty of identifying the cause of NMS when polypharmacy and other medical conditions are involved. The authors note the need for caution in deciding both the presence of NMS and the causal factors of the symptoms.

  18. Intoxication after Extreme Oral Overdose of Quetiapine to Attempt Suicide: Pharmacological Concerns of Side Effects

    Directory of Open Access Journals (Sweden)

    C. Müller

    2009-01-01

    Full Text Available Quetiapine is an atypical antipsychotic approved for the treatment of patients with psychotic disorders. Since approvement several case reports about intoxication with quetiapine were linked mainly with tachycardia, QTc-prolongation, somnolence, and hyperglycemia. Here, we present the first case report of an intoxication with an extreme overdose of quetiapine (36 g, ingested by a 32-year-old female (62 kg bodyweight to attempt suicide. Symptoms associated with intoxication were coma without arterial hypotension, persistent tachycardia, hyperglycemia, and transient hypothyreoidism. QTc-interval was moderately extended. Management consisted of intubation for airway protection, gastric lavage, the use of activated charcoal, i.v. saline, and observation for 17 hours on an intensive care unit. Despite the extremely high dose of quetiapine, the patient recovered completely without residual symptoms.

  19. Efficacy and electrocardiogram abnormality of olanzapine in the treatment of old schizophrenic patients%奥氮平治疗老年精神分裂症患者的疗效观察及对心电图的影响

    Institute of Scientific and Technical Information of China (English)

    袁国锋; 俞玉礼

    2011-01-01

    AIM: To explore the efficacy and the electrocardiogram abnormality of olanzapine or risperidon in the treatment of old schizophrenic patients.METHODS: 120 patients with old schizophrenia were randomly divided into olanzapine group (60 cases) and risperidon group(60 cases) treated for 8 weeks.The efficacy was measured with the positive and negative symptoms scale (PANSS) and PANSS and the electrocardiogram test was used to evaluate the efficacy and adverse effects respectively before and at the ends of 2,4,6,8 weeks of treatment.The amount and information of electrocardiogram abnormality were analyzed.RESULTS:The efficacy rate of olanzapine was 78.3%, in which 56.7% was improved markedly.The efficacy rate of risperidon was 75.0%, in which 51.7% were improved markedly.There were no difference between two groups (P> 0.05 ).There were significant differences on extrapyramidal side effect and liver function between them.At the 2nd week, the efficacy of olanzapine was more than that of the risperidon (P < 0.05 ).There were significant difference in electrocardiogram abnormality between olanzapine group and risperidon group ( P < 0.05).CONCLUSION: There are no significant differences in the efficacy and the electrocardiogram abnormality between two groups.Olanzapine has less sideeffect especially.The two drugs adapt to old schizophrenic.%目的:比较奥氮平与利培酮治疗老年精神分裂症患者的疗效及对心电图的影响.方法:选取120例老年精神分裂症患者,随机分为奥氮平组(研究组)和利培酮组(对照组),各60例,分别于治疗前及治疗后第2、4、6、8周末采用阳性与阴性症状量表(PANSS)评定疗效,并进行心电图检查,统计异常心电图的数目和相关信息.结果:两组PANSS评分治疗后均较治疗前明显下降(P0.05).奥氮平组以嗜睡为主,利培酮组以锥体外系副反应和转氨酶升高为主,两组在锥体外系副反应和转氨酶升高两方面有统计学差异(P<0

  20. Effects of quetiapine on sleep architecture in patients with unipolar or bipolar depression

    Directory of Open Access Journals (Sweden)

    Laura Gedge

    2010-08-01

    Full Text Available Laura Gedge1, Lauren Lazowski1, David Murray2, Ruzica Jokic2,3, Roumen Milev2,31Centre for Neuroscience Studies, 2Department of Psychiatry, Queen’s University, Kingston, 3Providence Care-Mental Health Services, Kingston, Ontario, CanadaObjective: To determine the effect of adjunctive quetiapine therapy on the sleep architecture of patients with bipolar or unipolar depression.Methods: This is a prospective, single-blind, repeated measures polysomnographic study. Sleep architecture was analyzed by overnight polysomnography, and subjective sleep quality was measured using the Pittsburgh Sleep Quality Index. The Hamilton Rating Scale for Depression, Montgomery Asberg Depression Rating Scale, Young Mania Rating Scale, and Clinical Global Impression-Severity Scale were employed to quantify changes in illness severity with adjunctive quetiapine treatment. Polysomnographs and clinical measures were administered at baseline, after 2–4 days of treatment, and after 21–28 days of quetiapine treatment. The average dose of quetiapine was 155 mg, ranging from 100–200 mg.Results: Adjunctive quetiapine therapy did not significantly alter sleep efficiency, sleep continuity, or Pittsburgh Sleep Quality Index scores. Respiratory Disturbance Index and percentage of total time in rapid eye movement (REM sleep significantly decreased and the percentage of total time in non-REM sleep, and duration of Stage 2 and non-REM sleep significantly increased after 2–4 days of quetiapine treatment. Illness severity significantly decreased over time.Conclusions: Adjunctive quetiapine treatment alters sleep architecture in patients with major depressive disorder or bipolar disorder, which may partially explain its early antidepressant properties. Changes in sleep architecture are more robust and significant within two to four days of starting treatment.Keywords: quetiapine, sleep architecture, depression, bipolar disorder

  1. Efficacy of Quetiapine Monotherapy in Posttraumatic Stress Disorder: A Randomized, Placebo-Controlled Trial.

    Science.gov (United States)

    Villarreal, Gerardo; Hamner, Mark B; Cañive, José M; Robert, Sophie; Calais, Lawrence A; Durklaski, Valerie; Zhai, Yusheng; Qualls, Clifford

    2016-12-01

    This was a 12-week randomized, placebo-controlled trial to assess the efficacy of quetiapine monotherapy in the treatment of posttraumatic stress disorder (PTSD). Eighty patients were randomly assigned to treatment with either quetiapine or placebo. The primary outcome measure was the Clinician-Administered PTSD Scale (CAPS). Secondary efficacy measures included the CAPS subscales, the Davidson Trauma Scale, the Positive and Negative Syndrome Scale (PANSS), the Clinical Global Impressions (CGI) scales for severity of Illness and improvement, the Hamilton Depression Rating Scale (HAM-D), and the Hamilton Anxiety Rating Scale (HAM-A). Safety measurements included adverse events, vital signs, the Abnormal Involuntary Movement Scale, the Barnes Akathisia Scale, the Simpson-Angus Scale, and the Arizona Sexual Experiences Scale. After a 1-week placebo run-in, quetiapine was started at a daily dosage of 25 mg and increased to a maximum of 800 mg; the average was 258 mg (range, 50-800 mg). Reductions in CAPS total, re-experiencing, and hyperarousal scores were significantly greater for the quetiapine group than for the placebo group. Greater improvements were also observed for quetiapine in scores on the Davidson Trauma Scale, CGI severity and improvement ratings, PANSS positive symptom and general psychopathology subscales, HAM-A, and HAM-D than for placebo. Adverse events were generally mild and expected based on prior studies of quetiapine in this and other patient population. There were no differences in safety measures between groups. Quetiapine monotherapy was efficacious in the treatment of PTSD. These findings suggest quetiapine as a single agent is effective in treating military PTSD.

  2. Peripheral Edema Occurring during Treatment with Risperidone Combined with Citalopram

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    Seyed Hamzeh Hosseini

    2012-01-01

    Full Text Available An 80-year-old female presented with symptoms of depression, worthlessness, hopelessness, loss of energy, insomnia, impatience, and forgetfulness associated with persecutory delusion that had begun about one year before her visit. She was diagnosed with major depression with psychotic signs and began treatment with risperidone (2 mg/night and citalopram (20 mg/day. After 20 days, she returned and reported partial improvement in her symptoms, although she had developed severe swelling of the hands and feet. The results of liver and renal function tests and rheumatologic tests were found to be within normal limits. Risperidone was discontinued for a week, and the swelling resolved completely. Risperidone was then administered again, and the swelling returned so that the patient had to discontinue taking the drug. The reappearance of edema on rechallenge is strong evidence implicating risperidone as the cause of the swelling.

  3. Risperidone treatment increases CB1 receptor binding in rat brain

    DEFF Research Database (Denmark)

    Secher, Anna; Husum, Henriette; Holst, Birgitte

    2010-01-01

    BACKGROUND/AIMS: Body weight gain is a common side effect of treatment with antipsychotics, but the mechanisms underlying this weight gain are unknown. Several factors may be involved in antipsychotic-induced body weight gain including the cannabinoid receptor 1 (CB(1)), the serotonin receptor 2C...... positively correlated with visceral fat mass. Risperidone treatment increased CB(1) receptor binding in the arcuate nucleus (40%), hippocampus (25-30%) and amygdala (35%) without concurrent alterations in the CB(1) receptor mRNA. Risperidone treatment increased adiponectin mRNA. CONCLUSION: The present study...... showed that risperidone treatment altered CB(1) receptor binding in the rat brain. Risperidone-induced adiposity and metabolic dysfunction in the clinic may be explained by increased CB(1) receptor density in brain regions involved in appetite and regulation of metabolic function....

  4. Formulation and characterization of nanoemulsion of olanzapine for intranasal delivery.

    Science.gov (United States)

    Kumar, Mukesh; Misra, Ambikanandan; Pathak, Kamla

    2009-01-01

    The objective was to formulate an olanzapine nanoemulsion that could potentially deliver the drug directly to the brain following intranasal administration. The nanoemulsions were prepared using the water titration method. The mucoadhesive character was imparted by the addition of 0.5%w/w chitosan and 0.5%w/w polycarbophil and was characterized for drug content, pH, percentage transmittance, globule size, zeta potential, and PDI. The composition (%w/w) of the optimized olanzapine nanoemulsion was capmul MCM, tween 80, and a mixture of 1:1 ratio of polyethylene glycol 400 and ethanol, and aqueous phase in a ratio of 15:35:17.5:32.5. The optimized olanzapine nanoemulsion exhibited a high diffusion coefficient and no nasal cilio-toxicity. The drug release followed the Higuchi model. The optimized nanoemulsions were found to be stable for 3 months.

  5. Effect of quetiapine vs. placebo on response to two virtual public speaking exposures in individuals with social phobia.

    Science.gov (United States)

    Donahue, Christopher B; Kushner, Matt G; Thuras, Paul D; Murphy, Tom G; Van Demark, Joani B; Adson, David E

    2009-04-01

    Clinical practice and open-label studies suggest that quetiapine (an atypical anti-psychotic) might improve symptoms for individuals with social anxiety disorder (SAD). The purpose of this study was to provide a rigorous test of the acute impact of a single dose of quetiapine (25mg) on SAD symptoms. Individuals with SAD (N=20) were exposed to a 4-min virtual reality (VR) public speaking challenge after having received quetiapine or placebo (double-blind) 1h earlier. A parallel VR challenge occurred 1 week later using a counter-balanced cross-over (within subject) design for the medication-placebo order between the two sessions. There was no significant drug effect for quetiapine on the primary outcome measures. However, quetiapine was associated with significantly elevated heart rate and sleepiness compared with placebo. Study findings suggest that a single dose of 25mg quetiapine is not effective in alleviating SAD symptoms in individuals with fears of public speaking.

  6. Quetiapine treatment reverses depressive-like behavior and reduces DNA methyltransferase activity induced by maternal deprivation.

    Science.gov (United States)

    Ignácio, Zuleide M; Réus, Gislaine Z; Abelaira, Helena M; Maciel, Amanda L; de Moura, Airam B; Matos, Danyela; Demo, Júlia P; da Silva, Júlia B I; Gava, Fernanda F; Valvassori, Samira S; Carvalho, André F; Quevedo, João

    2017-03-01

    Stress in early life has been appointed as an important phenomenon in the onset of depression and poor response to treatment with classical antidepressants. Furthermore, childhood trauma triggers epigenetic changes, which are associated with the pathophysiology of major depressive disorder (MDD). Treatment with atypical antipsychotics such as quetiapine, exerts therapeutic effect for MDD patients and induces epigenetic changes. This study aimed to analyze the effect of chronic treatment with quetiapine (20mg/kg) on depressive-like behavior of rats submitted to maternal deprivation (MD), as well as the activity of histone acetylation by the enzymes histone acetyl transferases (HAT) and deacetylases (HDAC) and DNA methylation, through DNA methyltransferase enzyme (DNMT) in the prefrontal cortex (PFC), nucleus accumbens (NAc) and hippocampus. Maternally deprived rats had a depressive-like behavior in the forced swimming test and an increase in the HDAC and DNMT activities in the hippocampus and NAc. Treatment with quetiapine reversed depressive-like behavior and reduced the DNMT activity in the hippocampus. This is the first study to show the antidepressant-like effect of quetiapine in animals subjected to MD and a protective effect by quetiapine in reducing epigenetic changes induced by stress in early life. These results reinforce an important role of quetiapine as therapy for MDD. Copyright © 2016 Elsevier B.V. All rights reserved.

  7. Neurofunctional effects of quetiapine in patients with bipolar mania.

    Science.gov (United States)

    Davis, Andrew K; DelBello, Melissa P; Eliassen, James; Welge, Jeffrey; Blom, Thomas J; Fleck, David E; Weber, Wade A; Jarvis, Kelly B; Rummelhoff, Emily; Strakowski, Stephen M; Adler, Caleb M

    2015-06-01

    Several lines of evidence suggest that abnormalities within portions of the extended limbic network involved in affective regulation and expression contribute to the neuropathophysiology of bipolar disorder. In particular, portions of the prefrontal cortex have been implicated in the appearance of manic symptomatology. The effect of atypical antipsychotics on activation of these regions, however, remains poorly understood. Twenty-two patients diagnosed with bipolar mania and 26 healthy subjects participated in a baseline functional magnetic resonance imaging scan during which they performed a continuous performance task with neutral and emotional distractors. Nineteen patients with bipolar disorder were treated for eight weeks with quetiapine monotherapy and then rescanned. Regional activity in response to emotional stimuli was compared between healthy and manic subjects at baseline; and in the subjects with bipolar disorder between baseline and eight-week scans. At baseline, functional activity did not differ between subjects with bipolar disorder and healthy subjects in any region examined. After eight weeks of treatment, subjects with bipolar disorder showed a significant decrease in ratings on the Young Mania Rating Scale (YMRS) (p < 0.001), and increased activation in the right orbitofrontal cortex (OFC) (p = 0.002); there was a significant association between increased right OFC activity and YMRS improvement (p = 0.003). These findings are consistent with suggestions that mania involves a loss of emotional modulatory activity in the prefrontal cortex--restoration of the relatively greater elevation in prefrontal activity widely observed in euthymic patients is associated with clinical improvement. It is not clear, however, whether changes are related to quetiapine treatment or represent a non-specific marker of affective change. © 2014 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  8. Antipsychotic medication in children and adolescents: a descriptive review of the effects on prolactin level and associated side effects.

    OpenAIRE

    Roke, Y.; van Harten, P. N.; Boot, A M; Buitelaar, J K

    2009-01-01

    OBJECTIVE: This review reports the incidence of hyperprolactinemia, its relationship with genotype, and prolactin-related side effects in children and adolescents treated with antipsychotics. METHOD: Data on prolactin levels were available for haloperidol, pimozide, risperidone, olanzapine, clozapine, ziprasidone, and quetiapine. Twenty-nine studies were selected after a literature search in the English Medline/Embase/Psychinfo/EBM databases (1965 to August, 2008). RESULTS: All antipsychotics...

  9. Danish register-based study on the association between specific antipsychotic drugs and fractures in elderly individuals

    DEFF Research Database (Denmark)

    Torstensson, Maia; Leth-Møller, Katja; Andersson, Charlotte

    2017-01-01

    %) experienced a fracture. Associations were for all APs highest in the initial treatment period (0-30 days) with IRRs for risperidone 1.97 (95% CI: 1.70-2.28), olanzapine 2.31 (95% CI: 1.96-2.73), quetiapine 2.09 (95% CI: 1.73-2.52), zuclopenthixol 2.19 (95% CI: 1.82-2.63), chlorprothixen 1.62 (95% CI: 1...

  10. Late Onset Anorexia Nervosa Treated With Olanzapine: A Case Report

    Directory of Open Access Journals (Sweden)

    Paolo Santonastaso

    2008-12-01

    Full Text Available A case of late onset anorexia nervosa (AN treated with olanzapine is reported. The patient suffered AN onset at the age of 53 and was brought to our attention four years later in a very poor state of health due to extreme starvation and laxative abuse. She presented severe obsessions about food, a very disturbed body image, and “ascetic” rituals of self-punishment. There was no improvement of her symptoms with cognitive behavioural therapy, antidepressant drugs and inpatient nutritional therapy. After the prescription of olanzapine, the patient was more cooperative and able to maintain a stable acceptable weight, although her psychiatric and anorexic symptoms only improved partially.

  11. A randomized, double-blind study of the efficacy and tolerability of extended-release quetiapine fumarate (quetiapine XR monotherapy in patients with major depressive disorder

    Directory of Open Access Journals (Sweden)

    Wang G

    2014-01-01

    Full Text Available Gang Wang,1 Alexander McIntyre,2 Willie R Earley,3 Shane R Raines,3 Hans Eriksson4 1Beijing Anding Hospital, Capital Medical University, Beijing, People's Republic of China; 2Department of Psychiatry, Penticton Regional Hospital, Penticton, BC, Canada; 3AstraZeneca Pharmaceuticals, Wilmington, DE, USA; 4AstraZeneca R&D, Södertälje, Sweden Objectives: To evaluate the efficacy and tolerability of once-daily extended release quetiapine fumarate (quetiapine XR monotherapy in patients with major depressive disorder (MDD. Patients and methods: This was a 10-week (8-week active treatment/2-week post-treatment randomized, double-blind, placebo- and active-controlled study (D1448C00004. Patients received quetiapine XR 150 mg/day, escitalopram 10 mg/day, or placebo; patients with an inadequate response (<20% improvement in Montgomery–Åsberg Depression Rating Scale [MADRS] total score at week two received double-dose treatment. The primary end point was week eight change from randomization in MADRS total score. Secondary end points included MADRS response (≥50% improvement and remission (score ≤8; Hamilton Rating Scale for Depression total and item 1; Hamilton Rating Scale for Anxiety total, psychic, and somatic; Clinical Global Impressions – Severity of Illness total; Pittsburgh Sleep Quality Index (PSQI global; and Quality of Life Enjoyment and Satisfaction Questionnaire – Short Form percentage maximum total scores. Tolerability was assessed throughout. Results: A total of 471 patients was randomized. No significant improvements in MADRS total score were observed at week eight (last observation carried forward with either active treatment (quetiapine XR, -17.21 [P=0.174]; escitalopram, -16.73 [P=0.346] versus placebo (-15.61. There were no significant differences in secondary end points versus placebo, with the exception of week-eight change in PSQI global score (quetiapine XR, -4.96 [P<0.01] versus placebo, -3.37. Mixed-model repeated

  12. A Case of Priapism with Risperidone

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    Almari Ginory

    2014-01-01

    Full Text Available Priapism is a urologic emergency defined as a prolonged, possibly painful, penile erection. There are several known causes of priapism including psychotropic medications. One of the mechanisms by which antipsychotics are believed to induce priapism is through alpha-1 antagonism. This is case of a 50-year-old male with a history of schizophrenia with previous priapism related to trazodone, who presents with new onset priapism associated with risperidone. In this case, the treatment of priapism includes discontinuation of the offending agent and drainage of the corpus cavernosum twice along with intracavernosal phenylephrine injections. It is important to educate patients on priapism as a possible side effect of medications. It is also important to consider previous episodes of medication-induced priapism when prescribing psychotropic medications as this may increase the patient’s future risk of priapism.

  13. Metabolic and behavioral effects of chronic olanzapine treatment and cafeteria diet in rats.

    Science.gov (United States)

    Muller, Alexandre P; Tort, Ana H; Gnoatto, Jussânia; Moreira, Julia D; Vinadé, Elsa R; Perry, Marcos L; Souza, Diogo O; Lara, Diogo R; Portela, Luis V

    2010-10-01

    Olanzapine and highly palatable diets can alter metabolism and brain function. We investigated the interaction of chronic treatment (4 months) with olanzapine and a cafeteria diet on metabolic parameters, memory tasks (spatial and aversive), the elevated plus maze and locomotor activity induced by d-amphetamine. Male Wistar rats were separated into the following groups: standard diet vehicle, standard diet and olanzapine, cafeteria diet vehicle and cafeteria diet and olanzapine. Olanzapine was administered in the drinking water (approximately 1.5 mg/kg/day), and after 3 days of treatment, the rats exhibited an expected anxiolytic effect and reduced amphetamine-induced hyperlocomotion. After 4 months of treatment, cafeteria diet vehicle and cafeteria diet olanzapine rats exhibited an increased body weight and heavier fat pads compared with the standard diet groups. Olanzapine increased only the epididymal and mesenteric fat pads. The cafeteria diet and olanzapine group showed greater glucose intolerance compared with all other groups. The cafeteria diet altered the effects of chronic olanzapine on the performance in the water maze and inhibitory avoidance tasks. Chronic olanzapine treatment failed to affect amphetamine-induced locomotion and to produce anxiolytic effects in the elevated plus maze task, regardless of the diet. Our results suggest that chronic olanzapine caused an increase in fat pads, which is putatively involved in the etiology of many metabolic diseases. Rats on the cafeteria diet were overweight and exhibited glucose intolerance. We did not observe these effects with olanzapine treatment with the standard diet. Moreover, the chronic treatment regimen caused tolerance to the antipsychotic and anxiolytic effects of olanzapine and seemed to potentiate some of the metabolic effects of the cafeteria diet. The cafeteria diet also modified the effects of chronic treatment with olanzapine on cognitive tasks, which may represent an undesirable effect of

  14. Preventing olanzapine-induced weight gain using betahistine: a study in a rat model with chronic olanzapine treatment.

    Directory of Open Access Journals (Sweden)

    Jiamei Lian

    Full Text Available Olanzapine is the one of first line antipsychotic drug for schizophrenia and other serious mental illness. However, it is associated with troublesome metabolic side-effects, particularly body weight gain and obesity. The antagonistic affinity to histamine H1 receptors (H1R of antipsychotic drugs has been identified as one of the main contributors to weight gain/obesity side-effects. Our previous study showed that a short term (2 weeks combination treatment of betahistine (an H1R agonist and H3R antagonist and olanzapine (O+B reduced (-45% body weight gain induced by olanzapine in drug-naïve rats. A key issue is that clinical patients suffering with schizophrenia, bipolar disease and other mental disorders often face chronic, even life-time, antipsychotic treatment, in which they have often had previous antipsychotic exposure. Therefore, we investigated the effects of chronic O+B co-treatment in controlling body weight in female rats with chronic and repeated exposure of olanzapine. The results showed that co-administration of olanzapine (3 mg/kg, t.i.d. and betahistine (9.6 mg/kg, t.i.d. significantly reduced (-51.4% weight gain induced by olanzapine. Co-treatment of O+B also led to a decrease in feeding efficiency, liver and fat mass. Consistently, the olanzapine-only treatment increased hypothalamic H1R protein levels, as well as hypothalamic pAMPKα, AMPKα and NPY protein levels, while reducing the hypothalamic POMC, and UCP1 and PGC-1α protein levels in brown adipose tissue (BAT. The olanzapine induced changes in hypothalamic H1R, pAMPKα, BAT UCP1 and PGC-1α could be reversed by co-treatment of O+B. These results supported further clinical trials to test the effectiveness of co-treatment of O+B for controlling weight gain/obesity side-effects in schizophrenia with chronic antipsychotic treatment.

  15. One-year risk of psychiatric hospitalization and associated treatment costs in bipolar disorder treated with atypical antipsychotics: a retrospective claims database analysis

    Directory of Open Access Journals (Sweden)

    Pikalov Andrei

    2011-01-01

    Full Text Available Abstract Background This study compared 1-year risk of psychiatric hospitalization and treatment costs in commercially insured patients with bipolar disorder, treated with aripiprazole, ziprasidone, olanzapine, quetiapine or risperidone. Methods This was a retrospective propensity score-matched cohort study using the Ingenix Lab/Rx integrated insurance claims dataset. Patients with bipolar disorder and 180 days of pre-index enrollment without antipsychotic exposure who received atypical antipsychotic agents were followed for up to 12 months following the initial antipsychotic prescription. The primary analysis used Cox proportional hazards regression to evaluate time-dependent risk of hospitalization, adjusting for age, sex and pre-index hospitalization. Generalized gamma regression compared post-index costs between treatment groups. Results Compared to aripiprazole, ziprasidone, olanzapine and quetiapine had higher risks for hospitalization (hazard ratio 1.96, 1.55 and 1.56, respectively; p Conclusions In commercially insured adults with bipolar disorder followed for 1 year after initiation of atypical antipsychotics, treatment with aripiprazole was associated with a lower risk of psychiatric hospitalization than ziprasidone, quetiapine, olanzapine and risperidone, although this did not reach significance with the latter. Aripiprazole was also associated with significantly lower total healthcare costs than quetiapine, but not the other comparators.

  16. Risperidone versus pimozide in Tourette's disorder : A comparative double-blind parallel-group study

    NARCIS (Netherlands)

    Bruggeman, R; van der Linden, C.; Buitelaar, JK; Gericke, GS; Hawkridge, SM; Temlett, JA

    2001-01-01

    Background: The treatment of Tourette's disorder with classical neuroleptics is limited by their side effects. Risperidone is a new efficacious antipsychotic with a low propensity for extrapyramidal side effects. To establish risperidone's therapeutic potential in Tourette's disorder, we studied the

  17. Continuation of Quetiapine Versus Switching to Placebo or Lithium for Maintenance Treatment of Bipolar I Disorder (Trial 144 : A Randomized Controlled Study)

    NARCIS (Netherlands)

    Weisler, Richard H.; Nolen, Willem A.; Neijber, Anders; Hellqvist, Asa; Paulsson, Bjorn

    2011-01-01

    Objective: Quetiapine, combined with lithium or divalproex, demonstrates efficacy in the maintenance treatment of bipolar I disorder. This study investigated the efficacy and safety of quetiapine monotherapy as maintenance treatment in bipolar I disorder compared with switching to placebo or

  18. Olanzapine-induced tender pitting pre-tibial edema

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    Kaliaperumal Mathan

    2015-01-01

    Full Text Available Antipsychotic-induced edema is uncommonly encountered in clinical practice. We report a case of tender pitting pre-tibial edema with olanzapine in a woman with no medical comorbidities. The peculiar distribution of edema resulted in diagnostic confusion necessitating specific investigations. Eventually, the edema resolved following complete stoppage of the drug, but caused distress to the patient and the caregiver.

  19. The Effect of Ranitidine on Olanzapine-Induced Weight Gain

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    Fatemeh Ranjbar

    2013-01-01

    Full Text Available Induced weight gain is a disturbing side effect of Olanzapine that affects the quality of life in psychotic patients. The aim of this study was to assess the efficacy of Ranitidine in attenuating or preventing Olanzapine-induced weight gain. A parallel 2-arm clinical trial was done on 52 patients with schizophrenia, schizoaffective and schizophreniform disorders who received Olanzapine for the first time. All these were first-episode admitted patients. They were randomly allocated to receive either Ranitidine or placebo. The trend of body mass index (BMI was compared between groups over 16-week course of treatment. Mean weight was 62.3 (SD: 9.6 kg at baseline. Thirty-three subjects (63.5% had positive family history of obesity. The average BMI increment was 1.1 for Ranitidine group and 2.4 for the placebo group. The multivariate analysis showed this effect to be independent of sex, family history of obesity, and baseline BMI value. The longitudinal modeling after controlling for baseline values failed to show the whole trend slope to be different. Although the slight change in trend’s slope puts forward a hypothesis that combined use of Ranitidine and Olanzapine may attenuate the weight gain long run, this needs to be retested in future larger scale long-term studies. This trial is registered with IRCT.ir 201009112181N5.

  20. Quetiapine, QTc interval prolongation, and torsade de pointes: a review of case reports.

    Science.gov (United States)

    Hasnain, Mehrul; Vieweg, W Victor R; Howland, Robert H; Kogut, Christopher; Breden Crouse, Ericka L; Koneru, Jayanthi N; Hancox, Jules C; Digby, Geneviève C; Baranchuk, Adrian; Deshmukh, Anand; Pandurangi, Ananda K

    2014-06-01

    Recently, both the manufacturer of quetiapine and the US Food and Drug Administration warned healthcare providers and patients about quetiapine-induced QTc interval prolongation and torsade de pointes (TdP) when using this drug within the approved labeling.  We reviewed the case-report literature and found 12 case reports of QTc interval prolongation in the setting of quetiapine administration. There were no cases of quetiapine-induced TdP or sudden cardiac death (SCD) among patients using quetiapine appropriately and free of additional risk factors for QTc interval prolongation and TdP. Among the 12 case reports risk factors included female sex (nine cases), coadministration of a drug associated with QTc interval prolongation (eight cases), hypokalemia or hypomagnesemia (six cases) quetiapine overdose (five cases), cardiac problems (four cases), and coadministration of cytochrome P450 3A4 inhibitors (two cases). There were four cases of TdP. As drug-induced TdP is a rare event, prospective studies to evaluate the risk factors associated with QTc prolongation and TdP are difficult to design, would be very costly, and would require very large samples to capture TdP rather than its surrogate markers. Furthermore, conventional statistical methods may not apply to studies of TdP, which is rare and an 'outlier' manifestation of QTc prolongation. We urge drug manufacturers and regulatory agencies to periodically publish full case reports of psychotropic drug-induced QTc interval prolongation, TdP, and SCD so that clinicians and investigators may better understand the clinical implications of prescribing such drugs as quetiapine.

  1. Quetiapine-induced sleep-related eating disorder-like behavior: a case series

    Science.gov (United States)

    2012-01-01

    Introduction Somnambulism or sleepwalking is a disorder of arousal from non-rapid eye movement sleep. The prevalence of sleep-related eating disorder has been found to be approximately between 1% and 5% among adults. Many cases of medication-related somnambulism and sleep-related eating disorder-like behavior have been reported in the literature. Quetiapine, an atypical antipsychotic medication, has been associated with somnambulism but has not yet been reported to be associated with sleep-related eating disorder. Case presentation Case 1 is a 51-year-old obese African American male veteran with a body mass index of 34.11kg/m2 and severe sleep apnea who has taken 150mg of quetiapine at bedtime for more than one year for depression. He developed sleepwalking three to four nights per week which resolved after stopping quetiapine while being compliant with bi-level positive pressure ventilation therapy. At one year follow-up, his body mass index was 32.57kg/m2. Case 2 is a 50-year-old African American female veteran with a body mass index of 30.5kg/m2 and mild sleep apnea who has taken 200mg of quetiapine daily for more than one year for depression. She was witnessed to sleepwalk three nights per week which resolved after discontinuing quetiapine while being treated with continuous positive airway pressure. At three months follow-up, her body mass index was 29.1kg/m2. Conclusion These cases illustrate that quetiapine may precipitate complex motor behavior including sleep-related eating disorder and somnambulism in susceptible patients. Atypical antipsychotics are commonly used in psychiatric and primary care practice, which means the population at risk of developing parasomnia may often go unrecognized. It is important to recognize this potential adverse effect of quetiapine and, to prevent injury and worsening obesity, discuss this with the patients who are prescribed these medications. PMID:23130910

  2. Valutazione dei costi di trattamento dei disturbi psicotici con olanzapina, risperidone e neurolettici tipici di un DSM italiano

    Directory of Open Access Journals (Sweden)

    I. Rossi

    2001-12-01

    Full Text Available Objective of the present retrospective analysis was to evaluate resources consumption for psychotic patients treatment with olanzapine (OLZ, risperidone (RIS or typical neuroleptics (NL during year 2000 in the Dipartimento di Salute Mentale (DSM of Ravenna. The screening of total number of psychotic patients followed in the Ravenna DSM during year 2000 generated 26 cases treated with OLZ, 22 treated with RIS and 17 treated with NL that were respecting criteria of equivalence for age and illness severity. For these patients we analyzed pharmacological, non pharmacological (medical visits, nurse visits, social assistance, rehabilitative sessions and hospital interventions during the year of observation, choosing the point of view of the DSM for costs attribution. The analysis of pharmacological interventions evidentiated a major usage of associated neuroleptics in the RIS and NL groups in respect to OLZ (pNL>RIS, p<0,05 for all comparisons. Hospital days during the year of observation in the three groups were 4,42 for OLZ patients, 7,71 for NL patients and 10,95 for RIS patients (p<0,05 for all comparisons: OLZ vs RIS, OLZ vs NL and RIS vs NL. The sum of pharmacological, non pharmacological and hospital costs (from 8.856.000 to 10.818.000 LIT didn’t generated statistically significant differences even if the OLZ group followed more intense rehabilitative activities (+71,65% vs RIS and +24,41% vs NL.

  3. Quetiapine for acute bipolar depression: a systematic review and meta-analysis

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    Suttajit S

    2014-06-01

    Full Text Available Sirijit Suttajit, Manit Srisurapanont, Narong Maneeton, Benchalak Maneeton Department of Psychiatry, Faculty of Medicine, Chiang Mai University, Chiang Mai, Thailand Background: Precise estimated risks and benefits of quetiapine for acute bipolar depression are needed for clinical practice. Objective: To systematically review the efficacy and the tolerability of quetiapine, either as monotherapy or combination therapy, for acute bipolar depression. Methods: We included all randomized, controlled trials (RCTs comparing quetiapine with other treatments, including placebo, in patients with acute bipolar depression (bipolar I or II disorder, major depressive episode. Published and unpublished RCTs were identified using the Cochrane Central Register of Controlled Trials, MEDLINE®, Web of Knowledge™, CINAHL®, PsycINFO®, the EU Clinical Trials Register database, and ClinicalTrials.gov. The primary outcome was the change scores of depression rating scales. Results: Eleven RCTs (n=3,488 were included. Two of them were conducted in children and adolescents. The change in depression scores was significantly greater in the quetiapine group compared with the placebo group (mean difference, [MD] =-4.66, 95% confidence interval [CI] -5.59 to -3.73. The significant difference was observed from week 1. Compared with placebo, quetiapine had higher incidence rates of extrapyramidal side effects, sedation, somnolence, dizziness, fatigue, constipation, dry mouth, increased appetite, and weight gain but lower risks of treatment-emergent mania and headache. Quetiapine treatment was associated with significant improvement of clinical global impression, quality of life, sleep quality, anxiety, and functioning. Conclusion: Quetiapine monotherapy is effective for acute bipolar depression and the prevention of mania/hypomania switching. Its common adverse effects are extrapyramidal side effects, sedation, somnolence, dizziness, fatigue, constipation, dry mouth

  4. 喹硫平与利培酮对女性精神分裂症患者血清催乳素及体重指数的影响分析%Effect of quetiapine and risperdal on serum prolactin levels and body mass index of female patients with schizophrenic

    Institute of Scientific and Technical Information of China (English)

    徐炳聪; 涂健铭; 张明辉

    2014-01-01

    目的 探讨喹硫平与利培酮对女性精神分裂症患者血清催乳素和体重指数BMI的影响.方法 选取未用药或停药1月的100例女性精神分裂症患者,随机分为喹硫平组和利培酮组治疗,分别给予喹硫平与利培酮单独治疗12周.在治疗前后分别测定血清催乳素水平和体重,计算体重指数BMI.结果 治疗12周后喹硫平组血清催乳素和体重指数BMI无明显增加,利培酮组则显著增加,体重指数BMI和催乳素水平变化呈正相关.结论 喹硫平对女性患者催乳素和体重BMI指数无明显影响,利培酮对女性患者催乳素和体重指数BMI影响明显.%Objective To investigate the influence of quetiapine and risperdal on the serum prolactin levels and body mass index (BMI) of female patients with schizophrenic.Methods 100 female schizophrenic patients,who had never used medication or had discontinued medication for a month,were randomly divided into two groups,the quetiapine group and the risperdal group.Each group was provided with quetiapine or risperdal,respectively,for 12 weeks.The serum prolactin level and body weight were recorded and BMI was calculated for each patient,before and after the treatment.Results After 12 weeks of treatment,the serum prolactin level and BMI in the quetiapine group had no significant increase,while they increased significantly in the risperidone group.It also showed that BMI and serum prolactin level changes had positive correlation.Conclusion Risperdal has significant effect on the serum prolactin and BMI of female schizophrenic patients,but quetiapine has not.

  5. A Case of Diabetic Ketoacidosis Associated with Risperidone Treatment

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    Zeynel Beyhan

    2008-12-01

    Full Text Available The association between schizophrenia and diabetes has been previously documented. Case reports have also demonstrated that initiation of atypical antipsychotic agents may induce or exacerbate diabetes mellitus. A 26-year-old man without a family history of diabetes mellitus presented with deep coma after 5 months of treatment with risperidone. He was diagnosed with diabetic ketoacidosis, was given insulin and saline infusion, and his antipsychotic agent was changed from risperidone to ziprasidone.Insulin therapy and oral agent was discontinued within two months of follow-up. The rapid onset of diabetes, and the disappearance of hyperglycemia after discontinuation of the drug suggested that risperidone had been a factor in his diabetic ketoacidosis. During three years of subsequent follow-up, testing revealed no evidence of elevated serum glucose levels or impaired glucose tolerance. In our opinion psychiatrists should routinely ask patients treated with antipsychotic agents such as risperidone for diabetic symptoms, weight loss, lethargy, polydipsia and/or polyuria, and monitor serum glucose levels. Although there is no consensus on the best way to switch from one antipsychotic drug to another, for those patients who develop diabetes during therapy with risperidone a change to ziprasidone treatment may maintain normal glucose levels.

  6. RP-HPLC estimation of risperidone in tablet dosage forms

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    Bladania S

    2008-01-01

    Full Text Available A simple, specific, accurate, and precise reverse phase liquid chromatographic method was developed and validated for the estimation of risperidone in tablet dosage forms. A Phenomenex Gemini C-18, 5 µm column having 250x4.6 mm i.d. in isocratic mode, with mobile phase containing methanol: acetonitrile: 50 mM potassium dihydrogen orthophosphate (80:10:10 v/v was used. The flow rate was 1.3 ml/min and effluents were monitored at 234 nm. Clozapine was used as an internal standard. The retention time of risperidone and clozapine were 2.5 min and 3.3 min, respectively. The method was validated for linearity, accuracy, precision, specificity, limit of quantification, limit of detection, robustness and stability. The limit of detection and limit of quantification for estimation of risperidone was found to be 500 ng/ml and 990 ng/ml, respectively. Recovery of risperidone was found to be in the range of 99.02-101.68%. Proposed method was successfully applied for the quantitative determination of risperidone in tablet formulations.

  7. Role of extended release quetiapine in the management of bipolar disorders

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    Rayan K Al Jurdi

    2010-02-01

    Full Text Available Rayan K Al Jurdi1,2, Lena A Dixit1, Martha Sajatovic3 1Baylor College of Medicine, Department of Psychiatry, Houston, Texas, USA; 2South Central Mental Illness Research and Clinical Core, Department of Veterans Affairs, Houston, Texas; 3Department of Psychiatry, Case Western Reserve University School of Medicine, Cleveland, Ohio, USAAbstract: Atypical antipsychotics have become a widely utilized component of the bipolar disorder treatment armamentarium, with approximately 45% of bipolar patients prescribed atypicals. Over the last decade all atypical drugs except for clozapine have received a Food and Drug Administration (FDA bipolar indication. In October 2008, the FDA approved quetiapine XR monotherapy for the treatment of acute depressive episodes of bipolar disorder and acute manic or mixed episodes in bipolar I disorder based on two placebo-control trials. Quetiapine was also approved as adjunct therapy with lithium and divalproex for the treatment of acute manic or mixed episodes as well as maintenance of bipolar I disorder. In contrast to immediate release quetiapine which may require a twice-daily regimen, the XR formulation is intended for once-daily administration. This drug profile of quetiapine XR will address chemistry, pharmacodynamics, pharmacokinetics, metabolism, safety and tolerability and clinical trials in bipolar disorder.Keywords: quetiapine XR, bipolar disorder

  8. Early Nonresponse Determined by the Clinical Global Impressions Scale Predicts Poorer Outcomes in Youth with Schizophrenia Spectrum Disorders Naturalistically Treated with Second-Generation Antipsychotics

    DEFF Research Database (Denmark)

    Stentebjerg-Olesen, Marie; Jeppesen, Pia; Pagsberg, Anne K

    2013-01-01

    , treated naturalistically with aripiprazole, olanzapine, quetiapine, risperidone, or ziprasidone and evaluated monthly, were divided into ER/ENR groups at week 4, using at least "minimally improved" on the CGI-I scale. Prediction using week 4 ER/ENR status for UR (CGI-I=at least "much improved......"), effectiveness and adverse effect outcomes at 8-12 weeks were assessed. Results: At 4 weeks, 45.6% of subjects were ER and 54.4% were ENR without differences regarding baseline demographic, illness, and treatment variables, except for higher age (p=0.034) and maximum risperidone dose (p=0.0043) in ENR. ER...

  9. H3 histamine receptor antagonist pitolisant reverses some subchronic disturbances induced by olanzapine in mice

    OpenAIRE

    Dudek, Magdalena; Kuder, Kamil; Kołaczkowski, Marcin; Olczyk, Adrian; Żmudzka, Elżbieta; Rak, Aleksandra; Bednarski, Marek; Pytka, Karolina; Sapa, Jacek; Kieć-Kononowicz, Katarzyna

    2016-01-01

    The use of atypical antipsychotic drugs like olanzapine is associated with side effects such as sedation and depression-like symptoms, especially during the initial period of the use. It is believed that the occurrence of these undesirable effectsis mainly the result of the histamine H1receptors blockade by olanzapine. In addition, use of olanzapine increases the level of triglycerides in the blood, which correlates with growing obesity. The aim of this study was to investigate the influence ...

  10. Spotlight on quetiapine in acute mania and depression associated with bipolar disorder.

    Science.gov (United States)

    Dando, Toni M; Keating, Gillian M

    2006-01-01

    Quetiapine (Seroquel), an atypical antipsychotic with established efficacy in the treatment of schizophrenia, shows efficacy in the treatment of acute mania and depression associated with bipolar disorder.Quetiapine, either as monotherapy or in combination with lithium or divalproex sodium (valproate semisodium), is generally well tolerated and effective in reducing manic symptoms in adult and adolescent patients with acute bipolar mania, and is approved for use in adults for this indication. As monotherapy, the drug is also effective in reducing depressive symptoms in patients with bipolar depression. It is associated with a low incidence of extrapyramidal symptom (EPS)-related adverse events and low EPS ratings in bipolar disorder. Quetiapine thus shows potential in the treatment of bipolar depression, and represents a useful agent for the treatment of acute bipolar mania.

  11. Glucagon receptor knockout mice are protected against acute olanzapine-induced hyperglycemia.

    Science.gov (United States)

    Castellani, Laura N; Peppler, Willem T; Sutton, Charles D; Whitfield, Jamie; Charron, Maureen J; Wright, David C

    2017-08-01

    To determine if glucagon is involved in mediating the increase in blood glucose levels caused by the second-generation antipsychotic drug olanzapine. Whole body glucagon receptor deficient mice (Gcgr(-/-)) or WT littermate controls were injected with olanzapine (5mg/kg BW IP) and changes in blood glucose measured over the following 120min. Separate cohorts of mice were treated with olanzapine and changes in pyruvate tolerance, insulin tolerance and whole body substrate oxidation were determined. Olanzapine treatment increased serum glucagon and lead to rapid increases in blood glucose concentrations in WT mice. Gcgr(-/-) mice were protected against olanzapine-induced increases in blood glucose but this was not explained by differences in terminal serum insulin concentrations, enhanced AKT phosphorylation in skeletal muscle, adipose tissue or liver or differences in RER. In both genotypes olanzapine induced an equivalent degree of insulin resistance as measured using an insulin tolerance test. Olanzapine treatment led to an exaggerated glucose response to a pyruvate challenge in WT but not Gcgr(-/-) mice and this was paralleled by reductions in the protein content of PEPCK and G6Pase in livers from Gcgr(-/-) mice. Gcgr(-/-) mice are protected against olanzapine-induced increases in blood glucose. This is likely a result of reductions in liver glucose output, perhaps secondary to decreases in PEPCK and G6Pase protein content. Our findings highlight the central role of the liver in mediating olanzapine-induced disturbances in glucose homeostasis. Copyright © 2017 Elsevier Ltd. All rights reserved.

  12. Maintenance treatment of adolescent bipolar disorder: open study of the effectiveness and tolerability of quetiapine

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    Milin Robert

    2009-02-01

    Full Text Available Abstract Background The purpose of the study was to determine the effectiveness and tolerability of quetiapine as a maintenance treatment preventing against relapse or recurrence of acute mood episodes in adolescent patients diagnosed with bipolar disorder. Methods Consenting patients meeting DSM-IV lifetime criteria for a bipolar disorder and clinically appropriate for maintenance treatment were enrolled in a 48-week open prospective study. After being acutely stabilized (CGI-S ≤ 3 for 4 consecutive weeks, patients were started or continued on quetiapine and other medications were weaned off over an 8-week period. Quetiapine monotherapy was continued for 40-weeks and other mood stabilizers or antidepressants were added if clinically indicated. A neurocognitive test battery assessing the most reliable findings in adult patients was administered at fixed time points throughout the study to patients and matched controls. Results Of the 21 enrolled patients, 18 completed the 48-week study. Thirteen patients were able to be maintained without relapse or recurrence in good quality remission on quetiapine monotherapy, while 5 patients required additional medication to treat impairing residual depressive and/or anxiety symptoms. According to symptom ratings and global functioning scores, the quality of remission for all patients was very good. Neurocognitive test performance over treatment was equivalent to that of a matched control group of never ill adolescents. Quetiapine was generally well tolerated with no serious adverse effects. Conclusion This study suggests that a proportion of adolescent patients diagnosed with bipolar disorder can be successfully maintained on quetiapine monotherapy. The good quality of clinical remission and preserved neurocognitive functioning underscores the importance of early diagnosis and effective stabilization. Clinical Trials Registry D1441L00024

  13. A randomized controlled trial of quetiapine for psychosis in Parkinson’s disease

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    Paul Shotbolt

    2009-05-01

    Full Text Available Paul Shotbolt1, Michael Samuel2,3, Chris Fox3,4, Anthony S David11Section of Cognitive Neuropsychiatry, Institute of Psychiatry, King’s College, London, UK; 2Department of Neurology, King’s College hospital, London, UK; 3East Kent hospitals NHS Trust, William Harvey Hospital, Ashford, Kent, UK; 4Kent and Medway NHS and Social Care and Partnership Trust, Kent, UKIntroduction: Psychosis (delusions and/or hallucinations is a well-recognized complication of treatment of Parkinson’s disease (PD. Quetiapine is a currently favored treatment, but data on its efficacy are equivocal. This trial aimed to provide further evidence on the efficacy of quetiapine in PD psychosis.Methods: We conducted a 12 week double blind randomized placebo-controlled trial. Time to dropout due to lack of improvement of psychosis was the primary outcome measure. Other important secondary outcomes were evaluated using standard rating scales for PD and psychiatric symptoms.Results: Twenty-four eligible subjects gave consent. The primary outcome, time to dropout, was examined using survival analysis. It was shown that patients in the quetiapine group dropped out earlier than those in the placebo group, but this difference was not significant (p = 0.68. No significant changes were found for any of the secondary outcome measures in either group. Conclusions: In this study, quetiapine at doses of up to 150 mg/day failed to significantly improve psychosis compared to placebo, however the small sample size does not allow any conclusive interpretation of the results. Quetiapine did not appear to worsen PD motor functioning, but its use was limited by a faster drop out compared with placebo. Significant impediments were difficulty with recruitment and natural fluctuation in symptoms during the trial. Keywords: Parkinson’s disease, psychosis, antipsychotics, quetiapine

  14. Cost-effectiveness of lurasidone vs quetiapine extended-release (XR) in patients with bipolar depression.

    Science.gov (United States)

    Rajagopalan, Krithika; Meyer, Kellie; O'Day, Ken; Denno, Melissa; Loebel, Antony

    2015-01-01

    Bipolar disorder imposes a high economic burden on patients and society. Lurasidone and quetiapine extended-release (XR) are atypical antipsychotic agents indicated for monotherapy treatment of bipolar depression. Lurasidone is also indicated as adjunctive therapy with lithium or valproate for depressive episodes associated with bipolar disorder. The objective of this analysis was to estimate the cost-effectiveness of lurasidone and quetiapine XR in patients with bipolar depression. A cost-effectiveness model was developed to compare lurasidone to quetiapine XR. The model was based on a US third-party payer perspective over a 3-month time horizon. The effectiveness measure in the model was the percentage of patients achieving remission (Montgomery-Åsberg Depression Rating Scale [MADRS] total score ≤12 by weeks 6-8). The comparison of remission rates was made through an adjusted indirect treatment comparison of lurasidone and quetiapine XR pivotal trials using placebo as the common comparator. Resource utilization for remission vs no remission was estimated from published expert panel data, and resource costs were obtained from a retrospective database study of bipolar I depression patients. Drug costs were estimated using the mean dose from clinical trials and wholesale acquisition costs. Over the 3-month model time period, lurasidone and quetiapine XR patients, respectively, had similar mean numbers of emergency department visits (0.48 vs 0.50), inpatient days (2.1 vs 2.2), and office visits (9.3 vs 9.6). More lurasidone than quetiapine XR patients achieved remission (52.0% vs 43.2%) with slightly higher total costs ($4982 vs $4676), resulting in an incremental cost-effectiveness ratio of $3474 per remission. The probabilistic sensitivity analysis showed lurasidone had an 86% probability of being cost-effective compared to quetiapine XR at a willingness-to-pay threshold of $10,000 per remission. Lurasidone may be a cost-effective option when compared to

  15. Postinjection Delirium/Sedation Syndrome with Olanzapine Depot Injection

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    Sarangula, Sadhvi Mythili; Mythri, Starlin Vijay; Sanjay, Y.; Reddy, M. S.

    2016-01-01

    After 1 year of introduction of olanzapine long-acting injectable (LAI) in India, many psychiatrists believe that it is a very affordable, well-tolerated, and effective second generation long-acting antipsychotic depot compared to not well tolerated but cheap first generation antipsychotic depots and to other second generation depots which are costly. However, reports of its possible adverse events in clinical settings are not yet published. We report what probably might be the first case of postinjection delirium/sedation syndrome (PDSS) in India. Although the occurrence is uncommon, incorrect understanding of this event may hinder the future use of the potentially useful olanzapine LAI. We review the available literature on the proposed diagnostic guidelines, mechanism of this event, precautions, and management of PDSS. PMID:27570354

  16. Olanzapine versus Placebo in Adolescents with Schizophrenia; a 6-Week, Randomized Double-Blind, Placebo-Controlled Trial

    Science.gov (United States)

    Kryzhanovskaya, Ludmila; Schulz, Charles; McDougle, Christopher; Frazier, Jean; Dittman, Ralf; Robertson-Plouch, Carol; Bauer, Theresa; Xu, Wen; Wang, Wei; Carlson, Janice; Tohen, Mauricio

    2009-01-01

    The efficacy of olanzapine in treating schizophrenia was tested through a placebo-controlled trial involving one hundred seven inpatient and outpatients adolescents. Patients who took olanzapine experienced significant symptom improvement.

  17. DEVELOPMENT AND BIOEQUIVALENCE STUDY OF OLANZAPINE 10mg TABLETS

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    Ravindra Waykar et al

    2012-09-01

    Full Text Available Generic drugs are lower-cost versions of patent-expired original brand-name medications. According to guidelines of regulatory agencies of the Canada, US and European Union, a generic drug must be “identical, or bioequivalent to a brand name drug in dosage form, safety, strength, route of administration, quality, performance characteristics and intended use”. Bioequivalence is decreed when the ratio of the generic to the reference compound for the area-under-the-curve and maximum plasma concentration (Cmax fall within a 0.80–1.25 range. The present study was to develop Olanzapine Tablets and compare pharmacokinetic profile of Zyprexa 10 mg film-coated tablets, Zyprexa Velotabs 10 mg orodispersible tablets and Olanzapine 10mg tablets. Multi media dissolution studies in 0.1N HCl, pH 4.5 acetate buffer and pH 6.8 phosphate buffer were carried out for Reference (Zyprexa Velotab 10 mg and Zyprexa 10 mg and test product (i.e. Olanzapine 10 mg. A single centre, open-label, single-dose, randomised, 3-way crossover bioequivalence study, performed under fasting conditions. Based on the results obtained, it can be concluded that the test olanzapine (Treatment A is bioequivalent to both references Zyprexa Velotab (Treatment B and Zyprexa (Treatment C following a 10 mg dose under fasting conditions. All formulations were well tolerated, with no major side effects and no relevant differences in safety profiles were observed between the preparations, particularly with respect to the number and pattern of adverse event.

  18. Betahistine ameliorates olanzapine-induced weight gain through modulation of histaminergic, NPY and AMPK pathways.

    Science.gov (United States)

    Lian, Jiamei; Huang, Xu-Feng; Pai, Nagesh; Deng, Chao

    2014-10-01

    Olanzapine is widely used to treat schizophrenia and other disorders, but causes adverse obesity and other metabolic side-effects. Both animal and clinical studies have shown that co-treatment with betahistine (a histaminergic H1 receptor agonist and H3 receptor antagonist) is effective for ameliorating olanzapine-induced weight gain/obesity. To reveal the mechanisms underlying these effects, this study investigated the effects of co-treatment of olanzapine and betahistine (O+B) on expressions of histaminergic H1 receptor (H1R), AMP-activated protein kinase (AMPK), neuropeptide Y (NPY), and proopiomelanocortin (POMC) in the hypothalamus associated with reducing olanzapine-induced weight gain. Olanzapine significantly upregulated the mRNA and protein expressions of H1R, while O+B co-treatment significantly downregulated the H1R levels, compared to the olanzapine-only treatment group. The NPY mRNA expression was significantly enhanced by olanzapine, but it was significantly reversed by O+B co-treatment. The hypothalamic H1R expression was positively correlated with total food intake, and NPY expression. Olanzapine also increased AMPKα activation measured by the AMPKα phosphorylation (pAMPKα)/AMPKα ratio compared with controls, whereas O+B co-treatment decreased the pAMPKα/AMPKα ratio, compared with olanzapine only treatment. The pAMPKα/AMPKα ratio was positively correlated with total food intake and H1R expression. Although olanzapine administration decreased the POMC mRNA level, this level was not affected by O+B co-treatment. Therefore, these results suggested that co-treatment with betahistine may reverse olanzapine-induced body weight gain via the H1R-NPY and H1R-pAMPKα pathways.

  19. Role of quetiapine beyond its clinical efficacy in bipolar disorder: From neuroprotection to the treatment of psychiatric disorders (Review).

    Science.gov (United States)

    Soeiro-DE-Souza, Márcio G; Dias, Vasco Videira; Missio, Giovanni; Balanzá-Martinez, Vicent; Valiengo, Leandro; Carvalho, André F; Moreno, Ricardo Alberto

    2015-03-01

    The aim of the present review was to discuss the following aspects of treatment with quetiapine in psychiatric disorders: i) Neurocognition and functional recovery in bipolar disorder (BD); ii) neuroprotective profile in different models; and iii) potential off-label indications. A PubMed search was conducted of articles published in English between 2000 and 2012 on quetiapine, cross-referenced with the terms 'anxiety', 'attention deficit disorder', 'borderline personality disorder', 'dementia', 'insomnia', 'major depressive disorder' (MDD), 'obsessive-compulsive disorder', 'post-traumatic stress disorder', 'remission', 'cognition', 'neurobiology', 'neuroprotection', 'efficacy' and 'effectiveness'. Articles were selected from meta-analyses, randomized clinical trials and open trials, and the results were summarized. Quetiapine, when studied in off-label conditions, has shown efficacy as a monotherapy in MDD and general anxiety disorder. Quetiapine also appears to exhibit a small beneficial effect in dementia. The review of other conditions was affected by methodological limitations that precluded any definitive conclusions on the efficacy or safety of quetiapine. Overall, the present review shows evidence supporting a potential role for quetiapine in improving cognition, functional recovery and negative symptoms in a cost-effective manner in BD. These benefits of quetiapine are potentially associated with its well-described neuroprotective effects; however, further studies are clearly warranted.

  20. Risperidone and Adaptive Behavior in Children with Autism

    Science.gov (United States)

    Williams, Susan K.; Scahill, Lawrence; Vitiello, Benedetto; Aman, Michael G.; Arnold, L. Eugene; McDougle, Christopher J.; McCracken, James T.; Tierney, Elaine; Ritz, Louise; Posey, David J.; Swiezy, Naomi B.; Hollway, Jill; Cronin, Pegeen; Ghuman, Jaswinder; Wheeler, Courtney; Cicchetti, Domenic; Sparrow, Sara

    2006-01-01

    Objective: To evaluate the impact of risperidone on adaptive behavior in children with autistic disorder who have serious behavior problems and to examine different methods of scoring the Vineland Adaptive Behavior Scales to measure change. Method: Forty-eight children (5 years to 16 years, 5 months) who showed behavioral improvement during acute…

  1. Determination of olanzapine by spectrophotometry using permanganate

    Directory of Open Access Journals (Sweden)

    Nagaraju Rajendraprasad

    2009-09-01

    Full Text Available Two new spectrophotometric methods using permanganate as the oxidimetric reagent for the determination of olanzapine (OLP were developed and validated as per the current ICH guidelines. The methods involved the addition of known excess of permanganate to OLP in either acid or alkaline medium followed by the determination of unreacted permanganate at 550 nm (method A or bluish-green color of manganate at 610 nm (method B. The decrease in absorbance in method A or increase in absorbance in method B as a function of concentration of OLP was measured and related to OLP concentration. Under optimized conditions, Beer's law was obeyed over the ranges 2.0 to 20 and 1.0 to 10 μg mL-1 in method A and method B, respectively. The calculated molar absorptivity values were 1.34 x 10(4 and 2.54 x 10(4 l mol-1cm-1 for method A and method B respectively, and the respective Sandell sensitivities were 0.0233 and 0.0123 μg cm-2. The LOD and LOQ for method A were calculated to be 0.37 and 1.13 μg mL-1and the corresponding values for method B were 0.16 and 0.48 μg mL-1. Intermediate precision, expressed as RSD was in the range 0.51 to 2.66 %, and accuracy, expressed as relative error ranged from 0.79 to 2.24 %. The proposed methods were successfully applied to the assay of OLP in commercial tablets with mean percentage recoveries of 102 ±1.59 % (method A and 101 ±1.53 % (method B. The accuracy and reliability of the methods were further confirmed by performing recovery tests via standard addition procedure.Dois métodos espectrofotométricos novos, usando o permanganato como o reagente oxidimétrico para a determinação da olanzapina (OLP foram utilizados e validados de acordo com as diretrizes atuais do ICH. Os métodos envolveram a adição de excesso conhecido de permanganato à OLP em meio ácido ou alcalino, determinando-se o permanganato que não reagiu em 550 nm (método A, ou pela cor verde-azulada do manganato a 610 nm (método B. A diminuição da

  2. Risperidone long-acting injectable monotherapy in the maintenance treatment of bipolar I disorder.

    Science.gov (United States)

    Quiroz, Jorge A; Yatham, Lakshmi N; Palumbo, Joseph M; Karcher, Keith; Kushner, Stuart; Kusumakar, Vivek

    2010-07-15

    Treatment adherence is a significant problem in patients with bipolar disorder. This study was designed to determine the efficacy of risperidone long-acting injectable (LAI) in the maintenance treatment of bipolar I disorder. Eligible patients with current or recent manic or mixed episodes (n = 559, aged 18-65 years) were treated with open-label oral risperidone for 3 weeks (period II) and open-label risperidone LAI for 26 weeks (n = 501; period III). Patients who maintained response (n = 303) were randomly allocated 1:1 to placebo injections (n = 149) or to continue risperidone LAI (n = 154) for up to 24 months (period IV). Most (77%) patients on risperidone LAI received a dose of 25 mg every 2 weeks during period IV. Time to recurrence for any mood episode (primary outcome variable) was significantly longer in the risperidone LAI group versus placebo (p or = 7% (compared with the period's baseline) occurred in 15% of patients in period III; in 12% of patients on risperidone LAI and 3% of patients on placebo in period IV. Risperidone LAI monotherapy significantly delayed the time to recurrence of mood episodes, versus placebo, in this controlled, randomized study in patients with bipolar I disorder. Risperidone LAI was tolerable and no new safety concerns emerged compared with previous studies of risperidone LAI. Copyright 2010 Society of Biological Psychiatry. Published by Elsevier Inc. All rights reserved.

  3. Night locomotor activity and quality of sleep in quetiapine-treated patients with depression.

    Science.gov (United States)

    Todder, Doron; Caliskan, Serdal; Baune, Bernhard T

    2006-12-01

    This research assesses the development of the night-activity rhythm and quality of sleep during course of treatment among patients with unipolar or bipolar depression and receiving antidepressant treatment plus quetiapine. Twenty-seven patients with major depressive episode were included into a 4-week follow-up study and compared with 27 healthy controls. Motor activity was continuously measured with an electronic wrist device (actigraphy), sleep was assessed with the Pittsburgh Sleep Quality Index, and patients were clinically assessed with the Hamilton depression score. All patients received a standard antidepressant treatment plus quetiapine. Whereas we found a rapid and maintaining improvement of subjective sleep parameters during the 4-week study, we observed a rapid improvement of some objective sleep parameters (actigraph) within the first week, but no further significant change of objective sleep parameters during the rest of the study. Another main finding of this study is that changes of subjectively and objectively assessed sleep parameters do not necessarily reflect clinical improvement of depression during the same timeline. Despite partial clinical remission, objective sleep parameters still showed significantly different patterns compared with controls. This study is the first to examine the effect of quetiapine on locomotor activity alongside with sleep in depression. As the studied patients with depression showed improvement in subjective and objective sleep parameters, quetiapine may be a promising drug for patients with depression and insomnia. Further studies need to investigate in detail the timeline of clinical remission and alterations of objective and subjective sleep parameters.

  4. Pharmacoeconomics of quetiapine for the management of acute mania in bipolar I disorder

    NARCIS (Netherlands)

    Klok, Rogier M; Al Hadithy, Asmar Fy; van Schayk, Nathalie Pjt; Antonisse, Ad Jj; Caro, Jaime J; Brouwers, Jacobus Rbj; Postma, Maarten J

    2007-01-01

    Bipolar disorder (or manic depression) is a lifelong, severe and complex psychiatric illness characterized by recurrent episodes of depression and mania. The aim of this study is to explore the cost-effectiveness of quetiapine compared with other alternatives for the treatment of acute manic episode

  5. Issues around the Prescription of Half Tablets in Northern Switzerland: The Irrational Case of Quetiapine

    Directory of Open Access Journals (Sweden)

    Samuel S. Allemann

    2015-01-01

    Full Text Available Background. Prescription of fragmented tablets is useful for individualisation of dose but includes several drawbacks. Although without score lines, the antipsychotic drug quetiapine was in 2011 the most often prescribed 1/2 tablet in discharge prescriptions at the University Hospital in Basel (USB, 671 beds. We aimed at analysing the prescription patterns of split tablets in general and of quetiapine in particular in Switzerland. Methods. All orders of community pharmacies for unit-of-use soft pouch blisters placed at Medifilm AG, the leader company in Switzerland for repackaging into pouch blisters, were analysed. Results. Out of 4,784,999 tablets that were repacked in 2012 in unit-of-use pouch blisters, 8.5% were fragmented, mostly in half (87.6%, and were predominantly psycholeptics (pipamperone 15.8%. Prescription of half quetiapine appears to be a Basel specificity (highest rates of fragments and half quetiapine. Conclusions. Prescription of fragmented tablet is frequent. It represents a safety issue for the patient, and a pharmaceutical care issue for the pharmacist. In ambulatory care, the patient’s cognitive and physical capacities must be clarified, suitability of the splitting of the tablet must be checked, appropriate aids must be offered, like a pill-splitting device in order to improve accuracy, and safe use of the drug must be ensured.

  6. Pharmacoeconomics of quetiapine for the management of acute mania in bipolar I disorder

    NARCIS (Netherlands)

    Klok, Rogier M; Al Hadithy, Asmar Fy; van Schayk, Nathalie Pjt; Antonisse, Ad Jj; Caro, Jaime J; Brouwers, Jacobus Rbj; Postma, Maarten J

    2007-01-01

    Bipolar disorder (or manic depression) is a lifelong, severe and complex psychiatric illness characterized by recurrent episodes of depression and mania. The aim of this study is to explore the cost-effectiveness of quetiapine compared with other alternatives for the treatment of acute manic

  7. [Olanzapine efficacy in the treatment of cocaine abuse in methadone maintenance patients. Interaction with plasma levels].

    Science.gov (United States)

    Baño, M D; Micó, J A; Agujetas, M; López, M L; Guillén, J L

    2001-01-01

    The aim of this study was to evaluate the efficacy of the treatment with antipsychotic olanzapine in cocaine abuse methadone patients. The decrease or interruption of cocaine consume as well as the possible pharmacokinetic interaction between olanzapine and methadone were studied. Patients (n= 21) include in a methadone maintenance program (14 months), with DSM-IV criteria for opioid and cocaine dependence and without schizophrenic diagnostic, were treated with olanzapine 5 to 10 mg/day. The therapeutic outcomes were assessed by personal interviews, cocaine consumption, changes of consumption patrons (via of administration) and secondary effects to olanzapine. Withdrawal symptoms were measured by means of the abbreviate version of the scale of Gossop. Cocaine used was measured by urine analysis (enzymoimmnuoassay). The possible pharmacokinetic interaction between olanzapine and methadone was measured in plasma before and during the treatment in 15 patients. Olanzapine combined with methadone in cocaine abusers was well tolerated in an important proportion of patients. Moreover the consumption of cocaine was decreased or stopped in 53,2% of the patients. In addition, no withdrawal syndrome was observed in any patients. Furthermore the ratios of methadone plasma levels did not change in relation to the dose before and during the treatment, suggesting a lack of pharmacokinetic interaction between methadone and olanzapine. In conclusion the results of this preliminary study, led us to advance that olanzapine could be a useful treatment for cocaine abuse at least in patients in a Methadone Maintenance Program, with the advantage of not to induce any pharmacokinetic interaction with methadone.

  8. Long-term outcomes in patients with schizophrenia treated with risperidone long-acting injection or oral antipsychotics in Spain: results from the electronic Schizophrenia Treatment Adherence Registry (e-STAR).

    Science.gov (United States)

    Olivares, J M; Rodriguez-Morales, A; Diels, J; Povey, M; Jacobs, A; Zhao, Z; Lam, A; Villalobos Vega, J C; Cuéllar, J Alonso; de Castro, F J Alberca; Quintero, C Morillo-Velarde; Martíin, J F Román; Domínguez, P Tabares; Ojeda, J L Prados; Cortés, S Sanz; Cala, F I Mata; Marín, C Gutiérrez; Castro, L Moyano; Duaso, M A Haza; Albarracín, J Requena; Vergara, G Narbona; Benítez, A Fernández; Cleries, F Mayoral; Pérez-Brian, J M García-Herrera; Aragón, A Bordallo; Navarro, J C Rodríguez; Biedma, J A Algarra; de Pedro, R Bravo; González, J F Delgado; López, M E Jaén; Moreno, H Díaz; López, J A Soto; Rodríguez, E Ojeda; de Hoyos, C Martínez; Sacristán, M Pardilla; Martín, M D Molina; Ballesteros, E Martín; Rodríguez, P A Sopelana; Menéndez, L Fernández; Rivas, R Santos; del Pino Cuadrado, P; Lauffer, J Correas; Solano, J J Rodríguez; Martínez, J M Fernández; Solano, F García; Rodríguez, P García-Lamberde; Rodríguez, J A Romero; Cano, T Rodríguez; Fortacin, M Ducaju; Lobeiras, J M Blanco; Sampedro, J M Piñeiro; Bravo, A Pérez; Pellicer, A Fernández; López, M D Alonso; Liste, J Fraga; Fernández, M Riobo; Losada, A Casas; Mendez, R Vazquez-Noguerol; Romero, S Agra; Blanco, J J Blanco; Bonaselt, I Tortajada; Mahia, M C García; del Valle, E Ferrer Gómez; Yañez, P Quiroga; Camarasa, M Gelabert; Alonso, J A Barbado; Mendez, G Florez; Feliz, F Doce; Lamela, M A López; Piñero, M Vega; Alvarado, P Fuentes; Gómez, I López; Martín, P Fadon; Gómez, J L Santos; López, A García; Jiménez, A Rodríguez; Nafs, A Escudero; Barquero, N Casas; Ortiz, R Fernández-Villamor; Noguera, J L Velez; Carrasco, P Ruiz; Muñoz, J Martín; Palma, M Masegoza; Hortelano, C Marín; Bonome, L Sánchez; Sevilla, J Sánchez; Juan, J M Mongil San; Ramos, J M García; Muñoz, J L Vallejo; Guisasola, J Elorza; Vazquez, L Santamaria; Guerras, F Campo; Nebot, F J Arrufat; Fernández, F J Baron; Nicolau, A L Palomo; Subirats, R Catala; Kidias, M Messays; Navarro, V Fabregat; García, B Frades; del Rosal, F Mejias; de Vicente Muñoz, T; Ballester, J Año; Lieb, P Malabia; Martel, A Delgado; Bea, E Roca; Joaquim, I Grau; Enjuanes, F Boatas; Piñol, M Bañuelos; Carbonell, E Fontova I; Muñoz, R Martín; Giribets, C Argila; Sans, L Albages; Blanco, A Serrano; Felipe, M Arcega; Muñoz, P González; Villanueva, A Pons; Arroyo, M Bernardo; Borri, R Coronas; Fallada, S Miret; Merola, M Celma; Rodon, E Parellada; Palmes, J R Pigem; Martínez, E Pérez; Catala, J Matarredona; Coca, A Sandoval; Ferrandiz, F Pascual; Paya, E Ferrandiz; Caballero, G Iturri; Bonet, A Franco; Figueras, J Fluvia; Pagador, P Moreno; Garibo, M Medina; Camo, V Pérez; Carrillo, C Sanz; Valero, C Pelegrin; Rebollo, F J Caro; García Campayo, J; Sala Ayma, J M Sala; Roig, M Martínez; de Uña Mateos, M A; Bertolin, R García; García, A Martín; Mazo, F Jiménez; Velasco, J L Galvez; Pérez, L Santa Maria; Casado, C Jiménez; Barba, J J Mancheño; Diaz, M Conde; Rubio, J P Alcon; Mandoli, A Soler; Herrero, A Uson; Martínez, A Rodríguez; Serrano, P Salgado; Rodríguez, E Nieto; Montesinos, J Segui; Macia, J Ferragud; Mateos Marcos, A Mateos; Soto, J V Pérez-Fuster; Dumont, M Verdaguer; Pagan, J Parra; Martínez, V Balanza; Santiuste de Pablos, M; Delgado, C Espinosa; Quiles, M D Martínez; López, F J Manzanera; Navarro, P Pozo; Torres, A Micol; Ingles, F J Martínez; Arias-Camison, J M Salmeron; Manzano, J C López; Peña, R Villanueva; Guitarte, G Petersen; Fontecilla, H Blasco; Romero, J Barjau; Gil, R Sanz; Lozano, J Marín; Adanez, L Donaire; Zarranz Herrera-Oria, I; Jiménez, J Pérez; Vaz, F Carrato; García, O Sanz; Anton, C Contreras; Casula, R Reixach; Hernandez, M C Natividad; Escabias, F Teba; Torresano, J Rodríguez; Pérez-Villamil, A Huidobro; Estevez, L; Figuero, M Aragües; Muñoz de Morales, A; Calvin, J L Rodríguez; Criado, M Delgado; Rodríguez, V Molina; Ambrosolio, E Balbo; Madera, P M Holgado; Alfaro, G Ponce; Vidal, M M Rojas; Valtuille, A García; Ruiz, O; Cabornero, G Lucas; Echevarria Martínez de Bujo, M; Mallen, M J Maicas; Puigros, J Santandreu; Martorell, A Liñana; Forteza, A Clar; Arrebola, E Rodríguez; Rodríguez de la Torre, M; Saiz, C G Anton; Bardolet I Casas, C; Linde, E Rodríguez; De Arce Cordon, R; Molina, E M Padial; Carazo, F J Ruiz; Romero, J J Muro; Cano, D Vico; Dorado, M Soria; Velazquez, S Campos; Sánchez, A J Rodríguez; Leon, S Ocio; Sánchez, K Pachas; Benitez, M Henry; Zugarramurai, A Intxausti; Contreras, M A; De la Varga González, M; Marín, P Barreiro; Robina, F Gómez; García, M Sánchez; Pérez, F J Otero; Bros, P Cubero; Gómez, A Carrillo; de Dios Molina Martín, J; Perera, J L Carrasco; Averbach, M C; Perera, J L Carrasco; Palancares, E Goenaga; Gallego de Dios, M T; Rojo, C Fernández; Iglesias, S Sánchez; Merino, M I Rubio; Mestre, N Prieto; Urdaniz, A Pérez; Sánchez, J M Martínez; Seco, R Gordo; Muñoz, J Franco; Agut, M Mateos; Lozano, M L Blanco; Herguedas, F Martín; Pena, A Torcal; García, J Vicente; Martínez, A Varona; Sanz Granado, O Sanz; Fernández, M A Medina; Canseco, J M Moran; López, P A Megia; Martín, M A Franco; Barrio, J A Espina; Ubago, J Giner; Bennassar, M Roca; Díez, J M Olivares; Fleta, J L Hernandez; Fortes, F Porras; López, C Arango; Medina, O; Alvarez, D Figuera; Roca, J M Peña; Valladolid, G Rubio; Tavera, J A Furquet; García-Castrillon Sales, J A; Llordes, I Batalla; Melgarejo, C Anchuistegui; Cañas de la Paz, F; Callol, V Vallés; García, M Bousoño; García, J Bobes; Leal, F J Vaz; Corrales, E Cáceres; Iglesias, E Sánchez; Gómez, M A Carreiras; Serrano, G García; Chillarón, E G Román; Aguado, F J Samino; Castillo, J J Molina; González, A González; Vázquez, J Gallardo; Peralvarez, M Bolivar; Diaz, M Rios; Mesa, M Ybarzabal; Artiles, F J Acosta; Chao, M Ajoy; Mesa, M Ybarzabal; del Rosario Santana, P; Escudero, M A García; Berenguer, M Molla; Llacer, J M Bonete; Berna, J A Juan; Ortiz, J Barragán; Pardell, L Tost; Hernández-Alvarez de Sotomayor, C; Méndez, M R Cejas; Garate, R Cabrera; Múgica, B Díaz; González, M Caballero; Domingo, J Pujol; Navarro, C Sáez; Vera, G Selva; Cuquerella, M A; Monzo, J Lonjedo; Boada, P Cervera; Pérez, M F Martín; Parrado, E Carrasco; Sánchez, J J Yañez; Fernández, J Calvo

    2009-06-01

    The electronic Schizophrenia Treatment Adherence Registry (e-STAR) is a prospective, observational study of patients with schizophrenia designed to evaluate long-term treatment outcomes in routine clinical practice. Parameters were assessed at baseline and at 3 month intervals for 2 years in patients initiated on risperidone long-acting injection (RLAI) (n=1345) or a new oral antipsychotic (AP) (n=277; 35.7% and 36.5% on risperidone and olanzapine, respectively) in Spain. Hospitalization prior to therapy was assessed by a retrospective chart review. At 24 months, treatment retention (81.8% for RLAI versus 63.4% for oral APs, p<0.0001) and reduction in Clinical Global Impression Severity scores (-1.14 for RLAI versus -0.94 for APs, p=0.0165) were significantly higher with RLAI. Compared to the pre-switch period, RLAI patients had greater reductions in the number (reduction of 0.37 stays per patient versus 0.2, p<0.05) and days (18.74 versus 13.02, p<0.01) of hospitalizations at 24 months than oral AP patients. This 2 year, prospective, observational study showed that, compared to oral antipsychotics, RLAI was associated with better treatment retention, greater improvement in clinical symptoms and functioning, and greater reduction in hospital stays and days in hospital in patients with schizophrenia. Improved treatment adherence, increased efficacy and reduced hospitalization with RLAI offer the opportunity of substantial therapeutic improvement in schizophrenia.

  9. Quetiapine-induced sleep-related eating disorder-like behavior: a case series

    Directory of Open Access Journals (Sweden)

    Tamanna Sadeka

    2012-11-01

    Full Text Available Abstract Introduction Somnambulism or sleepwalking is a disorder of arousal from non-rapid eye movement sleep. The prevalence of sleep-related eating disorder has been found to be approximately between 1% and 5% among adults. Many cases of medication-related somnambulism and sleep-related eating disorder-like behavior have been reported in the literature. Quetiapine, an atypical antipsychotic medication, has been associated with somnambulism but has not yet been reported to be associated with sleep-related eating disorder. Case presentation Case 1 is a 51-year-old obese African American male veteran with a body mass index of 34.11kg/m2 and severe sleep apnea who has taken 150mg of quetiapine at bedtime for more than one year for depression. He developed sleepwalking three to four nights per week which resolved after stopping quetiapine while being compliant with bi-level positive pressure ventilation therapy. At one year follow-up, his body mass index was 32.57kg/m2. Case 2 is a 50-year-old African American female veteran with a body mass index of 30.5kg/m2 and mild sleep apnea who has taken 200mg of quetiapine daily for more than one year for depression. She was witnessed to sleepwalk three nights per week which resolved after discontinuing quetiapine while being treated with continuous positive airway pressure. At three months follow-up, her body mass index was 29.1kg/m2. Conclusion These cases illustrate that quetiapine may precipitate complex motor behavior including sleep-related eating disorder and somnambulism in susceptible patients. Atypical antipsychotics are commonly used in psychiatric and primary care practice, which means the population at risk of developing parasomnia may often go unrecognized. It is important to recognize this potential adverse effect of quetiapine and, to prevent injury and worsening obesity, discuss this with the patients who are prescribed these medications.

  10. The antipsychotic olanzapine interacts with the gut microbiome to cause weight gain in mouse.

    Directory of Open Access Journals (Sweden)

    Andrew P Morgan

    Full Text Available The second-generation antipsychotic olanzapine is effective in reducing psychotic symptoms but can cause extreme weight gain in human patients. We investigated the role of the gut microbiota in this adverse drug effect using a mouse model. First, we used germ-free C57BL/6J mice to demonstrate that gut bacteria are necessary and sufficient for weight gain caused by oral delivery of olanzapine. Second, we surveyed fecal microbiota before, during, and after treatment and found that olanzapine potentiated a shift towards an "obesogenic" bacterial profile. Finally, we demonstrated that olanzapine has antimicrobial activity in vitro against resident enteric bacterial strains. These results collectively provide strong evidence for a mechanism underlying olanzapine-induced weight gain in mouse and a hypothesis for clinical translation in human patients.

  11. Effect of olanzapine treatment on INR of a patient receiving warfarin therapy

    Directory of Open Access Journals (Sweden)

    Derya Arslan

    2016-06-01

    Full Text Available Olanzapine is an atypical antipsychotic drug, commonly used in the management of psychotic symptoms in patients with schizoprenia and bipolar affective disorder. Deep venous thrombosis is a manifestation of venous thromboembolism. It is very well known that use of antipsychotic drugs increase the risk of thrombosis in a patient with schizophrenia. It has been reported in many studies the effects of olanzapine on thrombosis but there isn't any report about the effect of olanzapine on international normalized ratio (INR. in the medical literature. In this paper, a patient with schizophrenia and also family history of deep venous thrombosis who emerged deep venous thrombosis after being started on olanzapine treatment and effect of olanzapine treatment on INR has been reported. [Cukurova Med J 2016; 41(2.000: 370-373

  12. Effects of olanzapine on regional C-Fos expression in rat forebrain.

    Science.gov (United States)

    Robertson, G S; Fibiger, H C

    1996-02-01

    Compared to typical antipsychotic drugs, clozapine produces a unique pattern of Fos-like immunoreactive neurons in the rat forebrain. It has been proposed, therefore, that this approach may be useful in identifying other agents with clozapine's therapeutic profile. In the present study, we examined the ability of olanzapine to increase the number of Fos-like immunoreactive neurons in the striatum, nucleus accumbens, lateral septal nucleus, and prefrontal cortex. Olanzapine (5, 10 mg/kg) produced dose-dependent increases in the number of Fos-positive neurons in the nucleus accumbens and lateral septal nucleus, important components of the limbic system that may mediate some of the therapeutic actions of neuroleptics. Olanzapine also produced dose-dependent increases in the number of Fos-positive neurons in the dorsolateral striatum, an effect that correlates with the ability of neuroleptics to produce extrapyramidal side-effects. The effects of olanzapine on regional c-fos expression are not therefore identical to clozapine, which is without effect in the dorsolateral striatum. However, olanzapine-induced increases in the dorsolateral striatum were considerably smaller than those generated in the nucleus accumbens suggesting that at low, potentially therapeutic doses olanzapine may not generate significant extrapyramidal side effects. Olanzapine also increased the number of Fos-positive neurons in medical prefrontal cortex, an action unique to clozapine and a few other atypical antipsychotics. These findings are consistent with the hypothesis that olanzapine is an atypical antipsychotic in the sense that it does not produce significant extrapyramidal side-effects at low therapeutic doses. However, extrapyramidal side-effects at higher doses can be predicted by these results. Finally, olanzapine's actions in the medial prefrontal cortex may be predictive of a clozapine-like profile with respect to actions on negative symptoms in schizophrenia. Additional clinical

  13. Risperidone-induced enuresis in a 12-year-old child

    Directory of Open Access Journals (Sweden)

    Reetika Dikshit

    2017-01-01

    Full Text Available Risperidone has been documented to be effective in the management of behavior problems, aggression, and conduct disorder in children. While metabolic side effects like weight gain and obesity have been attributed to Risperidone use in children, side effects of the drug related to the urinary bladder are rare. We present a case of Risperidone-induced enuresis in a 12-year-old boy with conduct disorder that resolved completely after stopping the medication.

  14. Risperidone-induced Enuresis in a 12-year-old Child

    Science.gov (United States)

    Dikshit, Reetika; Karia, Sagar; De Sousa, Avinash

    2017-01-01

    Risperidone has been documented to be effective in the management of behavior problems, aggression, and conduct disorder in children. While metabolic side effects like weight gain and obesity have been attributed to Risperidone use in children, side effects of the drug related to the urinary bladder are rare. We present a case of Risperidone-induced enuresis in a 12-year-old boy with conduct disorder that resolved completely after stopping the medication. PMID:28149096

  15. Using Glycopyrrolate as an alternative option in case of Risperidone induced sialorrhoea

    Directory of Open Access Journals (Sweden)

    Dr. Hemanta Dutta

    2015-03-01

    Full Text Available Drug induced hypersalivation has been playing an unique factor in terms of noncompliance of antipsychotics. Hypersalivation has been described commonly with clozapine. Although Risperidone is also seen to be notorious to be causing hypersalivation. Use of Glycopyrrolate in Risperidone induced hypersalivation has not been covered though reported studies till yet. Here we are depicting the use of Glycopyrrolate as an alternative treatment option for hypersalivation induced by Risperidone.

  16. A case of drug-induced interstitial pneumonia potentially related to quetiapine (seroquel) therapy for behavioral and psychological symptoms.

    Science.gov (United States)

    Kim, Se-Jin; Han, Sang-Don; Lee, Jung Yeon; Chon, Gyu Rak

    2014-10-01

    Quetiapine is regarded as an effective and safe treatment for delirium. An 82-year-old man presented with a 1-week history of violent behavior and dizziness accompanied by weakness on the left side of his body. He was diagnosed with acute cerebral cortical infarction and delirium associated with alcohol abuse. After quetiapine treatment, he complained of fever and coughed up sputum, whereas his aggressive behavior improved. His symptoms persisted despite empirical antibiotic treatment. All diagnostic tests for infectious causes were negative. High-resolution computed tomography revealed bilateral consolidations and ground-glass opacities with predominantly peribronchial and subpleural distributions. The primary differential diagnosis was drug-associated interstitial lung disease, and therefore, we discontinued quetiapine and began methylprednisolone treatment. His symptoms and radiologic findings significantly improved after receiving steroid therapy. We propose that clinicians need to be aware of the possibility that quetiapine is associated with lung injury.

  17. Quetiapine monotherapy in acute treatment of generalized anxiety disorder: a systematic review and meta-analysis of randomized controlled trials

    Directory of Open Access Journals (Sweden)

    Maneeton N

    2016-01-01

    Full Text Available Narong Maneeton,1 Benchalak Maneeton,1 Pakapan Woottiluk,2 Surinporn Likhitsathian,1 Sirijit Suttajit,1 Vudhichai Boonyanaruthee,1 Manit Srisurapanont1 1Department of Psychiatry, Faculty of Medicine, Chiang Mai University, Chiang Mai, Thailand; 2Psychiatric Nursing Division, Faculty of Nursing, Chiang Mai University, Chiang Mai, Thailand Background: Some studies have indicated the efficacy of quetiapine in the treatment of generalized anxiety disorder (GAD.Objective: The purpose of this study was to systematically review the efficacy, acceptability, and tolerability of quetiapine in adult patients with GAD.Methods: The SCOPUS, MEDLINE, CINAHL, Cochrane Central Register of Controlled Trials, and ClinicalTrials.gov databases were searched in April 2015. All randomized controlled trials (RCTs of GAD were considered to be included in this meta-analysis. All RCTs of quetiapine in GAD patients providing endpoint outcomes relevant to severity of anxiety, response rate, remission rate, overall discontinuation rate, or discontinuation rate due to adverse events were included. The version reports from suitable clinical studies were explored, and the important data were extracted. Measurement for efficacy outcomes consisted of the mean-changed scores of the rating scales for anxiety, and response rate.Results: A total of 2,248 randomized participants in three RCTs were included. The pooled mean-changed score of the quetiapine-treated group was greater than that of the placebo-treated group and comparable to selective serotonin reuptake inhibitors (SSRIs. Unfortunately, the response and the remission rates in only 50 and 150 mg/day of quetiapine-XR (extended-release were better than those of the placebo. Their response and remission rates were comparable to SSRIs. The rates of pooled overall discontinuation and discontinuation due to adverse events of quetiapine-XR were greater than placebo. Only the overall discontinuation rate of quetiapine-XR at 50 and

  18. Multiple dose pharmacokinetics of risperidone and 9-hydroxyrisperidone in Chinese female patients with schizophrenia

    Institute of Scientific and Technical Information of China (English)

    Zhi-ling ZHOU; Qiu-xiong LIN; Chuan-yue WANG; Wen-biao LI; Shu-guang LIN; Huan-de LI; Xin LI; Huai-yan PENG; Xi-yong YU; Ming YANG; Feng-li SU; Feng WANG; Rong-hua ZHU; Chun-yu DENG

    2006-01-01

    Aim: To study the multiple dose clinical pharmacokinetics of risperidone and its main active metabolite, 9-hydroxyrisperidone, in Chinese female patients with schizophrenia. Methods: The subjects were 23 Chinese female inpatients aged 18-65 years who met the CCMD-Ⅲ (third revision of the Chinese Criteria of Mental Disorders) criteria for schizophrenia. Subjects were tested after 17 d of treatment with 2 mg risperidone twice daily. Plasma concentrations of risperidone and 9-hydroxy-risperidone were assayed by using validated high performance liquid chromatography-mass spectrometry (HPLC-MS) methods. Results: Risperidone was rapidly absorbed (Tmax was 1.6 h) and its Tin in plasma was short (3.2 h).9-hydroxy-risperidone was quickly metabolized from the parent drug with a mean Tmax of 2.5 h. It had a long half-life of 24.7 h. The Cssav of risperidone and 9-hydroxyrisperidone were 36.9±33.1 and 110.6±30.5 μg·h·L-1, respectively, and the AUCss0-12 were 443.2±397.4 and 1327.2±402.3 μg·h·L-1, respectively. CL/F and V/F of risperidone were 8.7±6.2 L/h and 34.1±24.3 L, respectively. Interindividual variations for pharmacokinetic parameters were quite large for risperidone. All 23 subjects experienced high prolactin levels when treated with risperidone. However there was no correlation between prolactin level and the concentration of risperidone, 9-hydroxy-risperidone, or the active moiety. Conclusion: Risperidone showed large interindividual variations in pharmacokinetics. Administration of risperidone resulted in high serum prolactin levels. The results indicate that systemic exposure to risperidone and 9-hydroxy-risperidone in female Chinese schizophrenic patients is higher relative to published data for white Caucasian patients. Larger studies regarding the PK/PD relationship may be required to develop a reasonable clinical dosage regimen for Chinese female patients.

  19. [Antipsychotic Treatment of the Adult Patient in the Acute Phase of Schizophrenia].

    Science.gov (United States)

    Bohórquez Peñaranda, Adriana; Gómez Restrepo, Carlos; García Valencia, Jenny; Jaramillo González, Luis Eduardo; de la Hoz, Ana María; Arenas, Álvaro; Tamayo Martínez, Nathalie

    2014-01-01

    To determine the efficacy and safety of different antipsychotic drugs in the management of patients diagnosed with schizophrenia in the acute phase. To formulate evidence-based recommendations on the antipsychotic (AP) drug management strategies for the treatment of the adult diagnosed with schizophrenia in the acute phase. Clinical practice guidelines were prepared, using the guidelines of the Methodology Guide of the Ministry of Health and Social Protection, in order to identify, synthesise, and evaluate the evidence and formulate recommendations as regards the management and follow-up of adult patients diagnosed with schizophrenia. The evidence of the NICE 82 guideline was adopted and updated, which answered the question on the management of the acute phase of adults with a diagnosis of schizophrenia. The evidence and its level were presented to the Guideline Development Group (GDG) in order to formulate recommendations following the methodology proposed by the GRADE approach. Clozapine, olanzapine, risperidone, ziprasidone, amisulpride, paliperidone, haloperidol, quetiapine, and aripiprazole were more effective than placebo for the majority of psychotic symptoms and the abandonment of treatment, but asenapine was not. Paliperidone, risperidone, quetiapine, clozapine, and olanzapine showed significant increases in weight compared to placebo. Haloperidol, risperidone, ziprasidone, and paliperidone had a higher risk of extrapyramidal symptoms than placebo. There was a significant risk of sedation or drowsiness with, risperidone, haloperidol, ziprasidone, quetiapine, olanzapine, and clozapine in the comparisons with placebo. Of the results of the comparisons between AP, it was shown that clozapine and paliperidone had a clinically significant effect compared to haloperidol and quetiapine, respectively. Olanzapine and risperidone had a lower risk of abandoning the treatment in general, and due to adverse reactions in two comparisons of each one, haloperidol was the

  20. INFLUENCE OF GLYCEROL, PROPYLENE GLYCOL, POLYSORBATE-80 AND SODIUM LAURYL SULFATE ON THE PARTITION COEFFICIENT OF QUETIAPINE FUMARATE

    OpenAIRE

    Mbah, C. J.; C. E. Chigozie

    2012-01-01

    The objective of the present study was to investigate the effects of glycerol, propylene glycol, polysorbate-80 and sodium lauryl sulfate on the lipophilic character of quetiapine fumarate by studying their effects on the partition coefficient of the drug. The partition coefficient was evaluated in n-hexane-water system at room temperature. Of the vehicles investigated, it was found that glycerol, propylene glycol, polysorbate-80 decreased the partition coefficient of quetiapine fumarate, whi...

  1. Effects of once-daily extended release quetiapine fumarate on patient-reported outcomes in patients with generalized anxiety disorder

    Directory of Open Access Journals (Sweden)

    Endicott J

    2012-07-01

    Full Text Available Jean Endicott,1 Henrik Svedsäter,2 Julie C Locklear21Department of Psychiatry, Columbia University, New York, NY; 2AstraZeneca Pharmaceuticals, Wilmington, DE, USABackground: We evaluated the effects of once-daily extended-release quetiapine fumarate (quetiapine XR on patient-reported outcomes in generalized anxiety disorder (GAD.Methods: This is a report of a pooled analysis from three acute 8-week, randomized, placebo-controlled, fixed-dose (50, 150, 300 mg/day studies and a 52-week maintenance flexible dose (50–300 mg/day study of quetiapine XR monotherapy in patients with GAD. Quality of Life Enjoyment and Satisfaction Questionnaire Short Form (Q-LES-Q-SF percent maximum total scores (items 1–14, item 15 ("satisfaction with medication", item 16 ("overall life satisfaction", and Pittsburgh Sleep Quality Index (PSQI global scores are reported. Sheehan Disability Scale (SDS total scores were also assessed (maintenance study only.Results: The acute studies showed significant improvements at week 8 in Q-LES-Q-SF percent maximum total score with quetiapine XR 150 mg/day (P < 0.001 and item 16 with quetiapine XR 50 (P < 0.05 and 150 mg/day (P < 0.001 versus placebo; PSQI global scores significantly improved with quetiapine XR 50, 150, and 300 mg/day versus placebo (P < 0.001. The maintenance study showed significant benefits versus placebo with quetiapine XR 50–300 mg/day in Q-LES-Q-SF percent total score, item 15 and item 16 scores, PSQI global score, and SDS total score.Conclusion: Quetiapine XR 150 mg/day (acute studies and 50–300 mg/day (maintenance study improved quality of life, overall functioning, and sleep quality in patients with GAD.Keywords: atypical antipsychotic, anxiety disorders, quality of life, sleep quality, functioning, randomized studies

  2. Neuroleptic malignant syndrome due to risperidone misdiagnosed as status epilepticus

    Directory of Open Access Journals (Sweden)

    Ali Ertug Arslankoylu

    2011-06-01

    Full Text Available Neuroleptic malignant syndrome (NMS is a rare but potentially fatal disease characterized by fever, muscle rigidity, delirium and autonomic instability. Here we report a child, with NMS due to the risperidone misdiagnosed as status epilepticus. Nine year old boy, who had been under high dose risperidone treatment for 8 weeks, admitted to the emergency room because of the contractions (evaluated as status epilepticus persisting for 7 hours. Since there was neuroleptic treatment in the past medical history and, unconsciousness, muscular rigidity, diaphoresis, hypertermi and, hypotension in physical examination, leucocytosis and elevated creatininphosphokinase levels in laboratory tests, the patient was evaluated as NMS and discharged without any complications. We reported this case to point out that; NMS may be misdiagnosed as status epilepticus in children when EEG monitoring is unavailable. When a child admitted to the emergency room because of suspicious convulsion neuroleptic drug use must surely be asked.

  3. Olanzapine for the treatment of bipolar disorder in children and adolescents.

    Science.gov (United States)

    Strawn, Jeffrey R; Delbello, Melissa P

    2008-02-01

    The second-generation antipsychotic olanzapine has been shown to be efficacious as a treatment for adults with bipolar disorder and is approved by the United States Food and Drug Administration for the treatment of acute manic or mixed episodes as well as for maintenance treatment in bipolar adults. This review examines the use of olanzapine for the treatment of children and adolescents with bipolar disorder and presents a discussion of the mechanism of action, pharmacokinetic and pharmacodynamic properties of olanzapine in children and adolescents. In addition, efficacy and safety data are reviewed and the risks and benefits of using olanzapine in bipolar youth are summarized. Articles published in English were identified using a search of the National Library of Medicine from 1990 to 2007 with manual review of references of each article as well as review of the US Clinical Trials database. Articles describing the use of olanzapine in children or adolescents were included. Olanzapine appears to have a rapid onset of action for mixed and manic episodes, but is associated with metabolic side effects including hyperprolactinemia, diabetes and weight gain. Therefore, olanzapine may best be used in the acute treatment of children and adolescents experiencing a manic or mixed episode as its side-effect profile may limit its use as a maintenance agent in this population.

  4. Effects of intracerebroventricular (ICV) olanzapine on insulin sensitivity and secretion in vivo: an animal model.

    Science.gov (United States)

    Hahn, Margaret K; Chintoh, Araba; Remington, Gary; Teo, Celine; Mann, Steve; Arenovich, Tamara; Fletcher, Paul; Lam, Loretta; Nobrega, Jose; Guenette, Melanie; Cohn, Tony; Giacca, Adria

    2014-03-01

    The atypical antipsychotics (AAPs) have been associated with an increased risk of type 2 diabetes. While weight gain associated with AAPs is a risk factor for diabetes, preclinical work suggests that among these medications, olanzapine, when given peripherally in a single dose, causes pronounced effects on insulin sensitivity and secretion. Given a critical role of the hypothalamus in control of glucose metabolism, we examined the effect of central administration of olanzapine. Sprague-Dawley rats were treated with a single 75 μg intracerebroventricular (ICV) dose of olanzapine and tested using separate hyperinsulinemic-euglycemic and hyperglycemic clamps. Dosing of olanzapine was established based on inhibition of amphetamine-induced locomotion. In contrast to the single dosing peripheral paradigm, there was no effect of central olanzapine on insulin sensitivity, either with respect to hepatic glucose production or peripheral glucose uptake. Analogous to the peripheral model, a single ICV dose of olanzapine followed by the hyperglycemic clamp decreased insulin (p=0.0041) and C-peptide response (p=0.0039) to glucose challenge as compared to vehicle, mirrored also by a decrease in the steady state glucose infusion rate required to maintain hyperglycemia (p=0.002). In conclusion, we demonstrate novel findings that at least part of the effect of olanzapine on beta-cell function in vivo is central.

  5. Risk of extrapyramidal syndrome in schizophrenic patients treated with antipsychotics: a population-based study.

    Science.gov (United States)

    Yang, S-Y; Kao Yang, Y-H; Chong, M-Y; Yang, Y-H; Chang, W-H; Lai, C-S

    2007-04-01

    To compare the prevalence of extrapyramidal syndrome (EPS) between the first-generation antipsychotics (FGAs) and second-generation antipsychotics (SGAs), the co-prescribing rate of anti-Parkinson drugs (APDs) of each antipsychotic drug was analyzed using population database. Fourteen antipsychotics had been prescribed during the 5-year study period. Among the SGAs, quetiapine had the lowest crude co-prescribing rate of APDs (27.09%), whereas risperidone had the highest rate (66.50%). Among the FGAs, thioridazine and loxapine had the lowest (60.99%) and highest rates (96.35%), respectively. The rankings of the co-prescribing rate of APDs among antipsychotics, in increasing order, were quetiapine, clozapine, olanzapine, thioridazine, zotepine, chlorpromazine, risperidone, sulpiride, clotiapine, flupentixol, haloperidol, zuclopentixol, trifluoperazine, and loxapine. The results indicate that the risk of EPS appears to be lower in SGAs than in FGAs; however, the considerably high rate of EPS in some of the newer generation of antipsychotics warrants clinical attention.

  6. Amantadine for weight gain associated with olanzapine treatment.

    Science.gov (United States)

    Deberdt, Walter; Winokur, Andrew; Cavazzoni, Patrizia A; Trzaskoma, Quynh N; Carlson, Christopher D; Bymaster, Frank P; Wiener, Karen; Floris, Michel; Breier, Alan

    2005-01-01

    Patients with schizophrenia (Sch), schizoaffective, schizophreniform, or bipolar (BP) I disorders [Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition (DSM-IV)]; not manic or acutely psychotic [Brief Psychiatric Rating Scale (BPRS) total score or =5% of their initial body weight were examined to determine whether amantadine could attenuate weight gain or promote weight loss. Olanzapine (Olz; 5-20 mg/day) was co-administered with double-blind treatment of 100-300 mg/day amantadine (Olz+Amt, n=60) or placebo (Olz+Plc, n=65). Visit-wise analysis of weight showed that weight change from baseline [last-observation-carried-forward (LOCF)] in the Olz+Amt group was significantly different from the Olz+Plc group at weeks 8 (P=0.042), 12 (P=0.029), and 16 (primary endpoint, mean+/-S.D.: -0.19+/-4.58 versus 1.28+/-4.26 kg, P=0.045). Mean BPRS total score, positive subscale, and anxiety-depression scores improved comparably in both groups, and Montgomery-Asberg Depression Rating Scale (MADRS) total score improved in the Olz+Amt group. Overall, amantadine was safe, was well tolerated, and attenuated weight gain or promoted weight loss in some patients who had gained weight during olanzapine therapy.

  7. How can lipid nanocarriers improve transdermal delivery of olanzapine?

    Science.gov (United States)

    Iqbal, Nimra; Vitorino, Carla; Taylor, Kevin M G

    2017-06-01

    The development of a transdermal nanocarrier drug delivery system with potential for the treatment of psychiatric disorders, such as schizophrenia and bipolar disorder, is described. Lipid nanocarriers (LN), encompassing various solid:liquid lipid compositions were formulated and assessed as potential nanosystems for transdermal delivery of olanzapine. A previously optimized method of hot high pressure homogenization (HPH) was adopted for the production of the LN, which comprised solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and nanoemulsions (NE). Precirol( ®) was selected as the solid lipid for progression of studies. SLN exhibited the best performance for transdermal delivery of olanzapine, based on in vitro release and permeation studies, coupled with results from physicochemical characterization of several solid:liquid lipid formulations. Stability tests, performed to give an indication of long-term storage behavior of the formulations, were in good agreement with previous studies for the best choice of solid:liquid lipid ratio. Overall, these findings highlight the SLN-based formulation as promising for the further inclusion in and production of transdermal patches, representing an innovative therapeutic approach.

  8. Long-term functional improvements in the 2-year treatment of schizophrenia outpatients with olanzapine long-acting injection

    Directory of Open Access Journals (Sweden)

    Ascher-Svanum H

    2014-06-01

    Full Text Available Haya Ascher-Svanum,1 Diego Novick,2,3 Josep Maria Haro,4 Jordan Bertsch,4 David McDonnell,1 Holland Detke11Eli Lilly and Company, Indianapolis, IN, USA; 2Eli Lilly and Company, Windlesham, Surrey, UK; 3Departament de Psiquiatria, Universitat Autonoma de Barcelona, Spain; 4Parc Sanitari Sant Joan de Déu, Centro de Investigación Biomédica en Red en el Área de Salud Mental, Universitat de Barcelona, Barcelona, SpainBackground: Little is known about the long-term changes in the functioning of schizophrenia patients receiving maintenance therapy with olanzapine long-acting injection (LAI, and whether observed changes differ from those seen with oral olanzapine.Methods: This study describes changes in the levels of functioning among outpatients with schizophrenia treated with olanzapine-LAI compared with oral olanzapine over 2 years. This was a secondary analysis of data from a multicenter, randomized, open-label, 2-year study comparing the long-term treatment effectiveness of monthly olanzapine-LAI (405 mg/4 weeks; n=264 with daily oral olanzapine (10 mg/day; n=260. Levels of functioning were assessed with the Heinrichs–Carpenter Quality of Life Scale. Functional status was also classified as “good”, “moderate”, or “poor”, using a previous data-driven approach. Changes in functional levels were assessed with McNemar’s test and comparisons between olanzapine-LAI and oral olanzapine employed the Student’s t-test. Results: Over the 2-year study, the patients treated with olanzapine-LAI improved their level of functioning (per Quality of Life total score from 64.0–70.8 (P<0.001. Patients on oral ­olanzapine also increased their level of functioning from 62.1–70.1 (P<0.001. At baseline, 19.2% of the olanzapine-LAI-treated patients had a “good” level of functioning, which increased to 27.5% (P<0.05. The figures for oral olanzapine were 14.2% and 24.5%, respectively (P<0.001. Results did not significantly differ between

  9. Rhabdomyolysis following Acute Extended-Release Quetiapine Poisoning: A Case Report

    Directory of Open Access Journals (Sweden)

    Antonios Liolios

    2012-01-01

    Full Text Available Background. During the past few years, there have been a number of case reports concerning rhabdomyolysis following quetiapine poisoning; however, there has been none concerning the medication in its extended-release form. Methods. We present the case report of a 48-year-old man presenting a major depressive disorder and borderline personality disorder, who after voluntary intoxication with 12000 mg of quetiapine extended-release developed signs of acute rhabdomyolysis. Results. The rhabdomyolysis was confirmed by the laboratory and the clinical findings, with elevated levels of creatinine, creatine phosphokinase, and CRP. Discussion. We would like to pinpoint the importance of this complication and our concern of prescribing it for psychiatric patients with chronic somatic comorbidities.

  10. Formulation Design and Optimization of Orodispersible Tablets of Quetiapine Fumarate by Sublimation Method

    OpenAIRE

    P Kalyankar; P Panzade; Lahoti, S.

    2015-01-01

    The objective of present study was to formulate directly compressible orodispersible tablets of quetiapine fumarate by sublimation method with a view to enhance patient compliance. A full 3 2 factorial design was used to investigate the effect of two variables viz., concentration of Indion 414 and camphor. Indion 414 (3-5 % w/w) was used as superdisintegrant and camphor (5-15 % w/w) as subliming agent. The tablets were evaluated for thickness, weight variation, hardness, friability, content u...

  11. An open-label study of quetiapine in the treatment of fibromyalgia.

    Science.gov (United States)

    Hidalgo, Javier; Rico-Villademoros, Fernando; Calandre, Elena Pita

    2007-01-30

    The aim of this exploratory study was to systematically assess the potential effectiveness and tolerability of quetiapine, an atypical antipsychotic, for the treatment of patients with fibromyalgia. This was a unicentre, open-label study conducted in thirty-five outpatients, 18 years or older, who met the ACR criteria for fibromyalgia and who had not satisfactorily responded to their previous fibromyalgia treatment. Quetiapine, flexibly dosed (25-100 mg/day), was added to their original treatment regimen for 12 weeks. The primary outcome measure was the mean change from baseline to endpoint in the Fibromyalgia Impact Questionnaire (FIQ) total score. Secondary efficacy measures included mean changes from baseline to endpoint in the scores of the Clinical Global Impression (CGI) of Severity scale, Pittsburgh Sleep Quality Index (PSQI), Beck Depression Inventory (BDI), State-Trait Anxiety Inventory (STAI), 12-Item Short Form Health Survey (SF-12), and individual items of the FIQ. Thirty (85.7%) patients (mean age 47+/-7.9, 93.3% females) had a postbaseline evaluation and constituted the intent-to-treat efficacy sample. Mean FIQ total score decreased significantly by 10.2 points from a baseline of 63.2 to 53.0 at study endpoint (pfatigue subscores but not in FIQ pain subscore. Large effect sizes were observed for the FIQ total (1.04), CGI-severity (1.00) and PSQI (1.07), while moderate effect sizes (i.e.> or =0.50) were encountered in the FIQ fatigue, FIQ stiffness and SF-12 mental component summary. Quetiapine was safely administered and well tolerated. Despite the lack of effect on pain, the significant and relevant improvement in overall efficacy measures and quality of life suggests that quetiapine may be a valuable drug for treatment of patients with fibromyalgia that should be further tested in double-blind, placebo-controlled trials.

  12. False-positive methadone urine drug screen in a patient treated with quetiapine.

    Science.gov (United States)

    Lasić, Davor; Uglesić, Boran; Zuljan-Cvitanović, Marija; Supe-Domić, Daniela; Uglesić, Lovro

    2012-06-01

    We present a case of T.M. admitted to University Department of Psychiatry, Split University Hospital Center, in Croatia, because of the acute psychotic reaction (F23.9). The patient's urine tested positive for methadone without a history of methadone ingestion. Urine drug screen was performed with the COBAS Integra Methadone II test kit (kinetic interaction of microparticles in solution /KIMS/ methodology) by Roche. Drugs that have been shown to cross-react with methadone feature a tricyclic structure with a sulfur and nitrogen atom in the middle ring, which is common for both quetiapine and methadone. Therefore, it is plausible that this structural similarity between quetiapine and methadone could underlie the cross-reactivity on methadone drug screen. Besides quetiapine, a number of routinely prescribed medications have been associated with triggering false-positive urine drug screen results. Verification of the test results with a different screening test or additional analytical tests should be performed to avoid adverse consequences for the patients.

  13. New-Onset Diabetes Mellitus Among Parkinsonian Patients Treated with Long-term Quetiapine

    Directory of Open Access Journals (Sweden)

    Hubert H. Fernandez

    2008-01-01

    Full Text Available Atypical antipsychotics (AA are commonly used to manage drug-induced psychosis (DIP in parkinsonian patients. In the treatment of schizophrenia, AA’s have been associated with increasing reports of new-onset diabetes mellitus (DM. This study examined the risk of developing new-onset DM among parkinsonian patients on long-term, low dose quetiapine. Fifty-three parkinsonian subjects (mean age: 71.3 years taking an average quetiapine dose of 70.5 mg/day (range: 12.5–350 mg/day for a mean duration of 21.3 months (range 3–61 months were reviewed. Eight out of 53 subjects carried a diagnosis of DM prior to quetiapine treatment. Four out of 45 patients (8.9% met criteria for new diagnosis of DM, giving a total prevalence rate of 22.6% (12 out of 53. This prevalence rate of 22.6% was slightly higher than that reported in the aged-matched general population (year 2003 DM prevalence = 17.3% for 65–74 years but methodological differences could explain the difference. Larger epidemiologic studies will be needed to confirm these results as they could potentially impact a significant number of patients.

  14. Quetiapine monotherapy in adolescents with bipolar disorder comorbid with conduct disorder.

    Science.gov (United States)

    Masi, Gabriele; Pisano, Simone; Pfanner, Chiara; Milone, Annarita; Manfredi, Azzurra

    2013-10-01

    Bipolar Disorders (BD) are often comorbid with disruptive behaviour disorders (DBDs) (oppositional-defiant disorder or conduct disorder), with negative implications on treatment strategy and outcome. The aim of this study was to assess the efficacy of quetiapine monotherapy in adolescents with BD comorbid with conduct disorder (CD). A consecutive series of 40 adolescents (24 males and 16 females, age range 12-18 years, mean age 14.9 ± 2.0 years), diagnosed with a clinical interview (Kiddie Schedule for Affective Disorders and Schizophrenia for School-Aged Children-Present and Lifetime Version [K-SADS-PL]) according to American Psychiatric Association, Diagnostic and Statistical Manual of Mental Disorders, 4th ed., Text Revision (DSM-IV-TR) criteria were included. All the patients were treated with quetiapine monotherapy (mean final dose 258 ± 124 mg/day, range 100-600 mg/day). At the end-point (3 months), 22 patients (55.0%) were responders (Clinical Global Impressions-Improvement [CGI-I] score of 1 or 2 and CGI-Severity [CGI-S] ≤ 3 and improvement of at least 30% Children's Global Assessment Scale [C-GAS] during 3 consecutive months). Both CGI-S and C-GAS significantly improved (pdisorder (ADHD) comorbidity. Eight patients (20.0%) experienced moderate to severe sedation and eight (20.0%) experienced increased appetite and weight gain. In these severely impaired adolescents, quetiapine monotherapy was well tolerated and effective in>50% of the patients.

  15. Low-dose intravenous lipid emulsion for the treatment of severe quetiapine and citalopram poisoning.

    Science.gov (United States)

    Purg, Darinka; Markota, Andrej; Grenc, Damjan; Sinkovič, Andreja

    2016-06-01

    The treatment of quetiapine and/or citalopram poisoning is mainly supportive and involves gastric lavage, activated charcoal, intubation, and mechanical ventilation. Recently, however, there were reports of successful treatment with intravenous lipid emulsion. Here we report a case of a 19-year-old Caucasian girl who ingested approximately 6000 mg of quetiapine, 400 mg of citalopram, and 45 mg of bromazepam in a suicide attempt. The patient developed ventricular tachycardia and epileptic seizures 12 h after admission to the hospital. As the patient's condition deteriorated, we combined standard therapy (intubation, mechanical ventilation, and vasopressors) with low-dose intravenous lipid emulsion (ILE) (a total of 300 mL of 20 % lipid emulsion) and normalised her heart rhythm and stopped the seizures. She was discharged to the psychiatric ward after 48 h and home after a prolonged (2-month) psychiatric rehabilitation. Intravenous lipid emulsion turned out to be effective even in the lower dose range than previously reported for quetiapine poisoning in patients presenting with seizure and ventricular arrhythmia. To our knowledge, there are no case reports describing the use of ILE in treating citalopram poisoning.

  16. RP-HPLC METHOD FOR ESTIMATION OF QUETIAPINE HEMI FUMARATE IN TABLET DOSAGE FORM

    Directory of Open Access Journals (Sweden)

    Mohite Mukesh. T

    2013-08-01

    Full Text Available A simple, sensitive, rapid, robust and reproducible method for the determination of Quetiapine Hemi Fumarate (QHF in bulk and Pharmaceutical Formulation (Tablets was developed using Reverse Phase High Performance Liquid Chromatographic method (RP-HPLC. The RP-HPLC analysis was performed isocratically on XTERRA C18 (4.6 X 150 mm, analytical column using a mobile phase consisting of Acetonitrile and methanol in the ratio of 60 : 40 v / v, with a flow rate of 1 ml / min. The analyte was monitored with UV detector at 290 nm. The developed method Quetiapine hemi fumarate elutes at a run time of 10 minutes. The proposed method is having linearity in the concentration range from 20 to 100 μg / mL of Quetiapine hemi fumarate. The present method was validated with respect to system suitability, linearity, precision, limit of detection (LOD and limit of quantification (LOQ, accuracy (recovery, and robustness as per ICH Guidelines. The proposed method can be readily utilized for bulk drug and pharmaceutical formulations.

  17. Prolactin release in children treated with risperidone - Impact and role of CYP2D6 metabolism

    NARCIS (Netherlands)

    Troost, Pieter W.; Lahuis, Bertine E.; Hermans, Mirjam H.; Buitelaar, Jan K.; van Engeland, Herman; Scahill, Lawrence; Minderaa, Ruud B.; Hoekstra, Pieter J.

    2007-01-01

    Objective: Little is known about the role of CYP2136 polymorphism in risperidone-induced prolactin release in children. Method: Twenty-five children (aged 5-15 years) with pervasive developmental disorders were genotyped for CYP2D6 polymorphisms. Serum prolactin, risperidone, and 9-hydroxyrisperidon

  18. Formulation, in vitro and in vivo evaluation of transdermal patches containing risperidone.

    Science.gov (United States)

    Aggarwal, Geeta; Dhawan, Sanju; Hari Kumar, S L

    2013-01-01

    The efficacy of oral risperidone treatment in prevention of schizophrenia is well known. However, oral side effects and patient compliance is always a problem for schizophrenics. In this study, risperidone was formulated into matrix transdermal patches to overcome these problems. The formulation factors for such patches, including eudragit RL 100 and eudragit RS 100 as matrix forming polymers, olive oil, groundnut oil and jojoba oil in different concentrations as enhancers and amount of drug loaded were investigated. The transdermal patches containing risperidone were prepared by solvent casting method and characterized for physicochemical and in vitro permeation studies through excised rat skin. Among the tested preparations, formulations with 20% risperidone, 3:2 ERL 100 and ERS 100 as polymers, mixture of olive oil and jojoba oil as enhancer, exhibited greatest cumulative amount of drug permeated (1.87 ± 0.09 mg/cm(2)) in 72 h, so batch ROJ was concluded as optimized formulation and assessed for pharmacokinetic, pharmacodynamic and skin irritation potential. The pharmacokinetic characteristics of the optimized risperidone patch were determined using rabbits, while orally administered risperidone in solution was used for comparison. The calculated relative bioavailability of risperidone transdermal patch was 115.20% with prolonged release of drug. Neuroleptic efficacy of transdermal formulation was assessed by rota-rod and grip test in comparison with control and marketed oral formulations with no skin irritation. This suggests the transdermal application of risperidone holds promise for improved bioavailability and better management of schizophrenia in long-term basis.

  19. Clinical utility of the risperidone formulations in the management of schizophrenia

    Directory of Open Access Journals (Sweden)

    Madaan V

    2011-10-01

    Full Text Available Vishal Madaan1, Durga P Bestha2, Venkata Kolli2, Saurabh Jauhari2, Roger C Burket1 1University of Virginia Health System, Charlottesville, VA, USA; 2Creighton University Medical Center, Omaha, NE, USA Abstract: Risperidone is one of the early second-generation antipsychotics that came into the limelight in the early 1990s. Both the oral and long-acting injectable formulations have been subject to numerous studies to assess their safety, efficacy, and tolerability. Risperidone is currently one of the most widely prescribed antipsychotic medications, used for both acute and long-term maintenance in schizophrenia. Risperidone has better efficacy in the treatment of psychotic symptoms than placebo and possibly many first-generation antipsychotics. Risperidone fares better than placebo and first-generation antipsychotics in the treatment of negative symptoms. Risperidone's long acting injectable preparation has been well tolerated and is often useful in patients with medication nonadherence. Risperidone has a higher risk of hyperprolactinemia comparable to first-generation antipsychotics (FGAs but fares better than many second-generation antipsychotics with regards to metabolic side effects. In this article, we briefly review the recent literature exploring the role of risperidone formulations in schizophrenia, discuss clinical usage, and highlight the controversies and challenges associated with its use. Keywords: risperidone, schizophrenia, formulation, antipsychotic, side effects

  20. Risperidone in the management of agitation and aggression associated with psychiatric disorders.

    NARCIS (Netherlands)

    Deyn, P.P. de; Buitelaar, J.K.

    2006-01-01

    OBJECTIVE: This review provides an overview of the prevalence and treatment of agitation and aggression, and focuses on the use of risperidone to treat these symptoms in patients from different age groups. METHODS: MEDLINE and EMBASE databases were used to identify controlled studies of risperidone

  1. Clozapine versus other atypical antipsychotics for schizophrenia

    Science.gov (United States)

    Asenjo Lobos, Claudia; Komossa, Katja; Rummel-Kluge, Christine; Hunger, Heike; Schmid, Franziska; Schwarz, Sandra; Leucht, Stefan

    2014-01-01

    Background Clozapine is an atypical antipsychotic demonstrated to be superior in the treatment of refractory schizophrenia which causes fewer movement disorders. Clozapine, however, entails a significant risk of serious blood disorders such as agranulocytosis which could be potentially fatal. Currently there are a number of newer antipsychotics which have been developed with the purpose to find both a better tolerability profile and a superior effectiveness. Objectives To compare the clinical effects of clozapine with other atypical antipsychotics (such as amisulpride, aripiprazole, olanzapine, quetiapine, risperidone, sertindole, ziprasidone and zotepine) in the treatment of schizophrenia and schizophrenia-like psychoses. Search methods We searched the Cochrane Schizophrenia Groups Register (June 2007) and reference lists of all included randomised controlled trials. We also manually searched appropriate journals and conference proceedings relating to clozapine combination strategies and contacted relevant pharmaceutical companies. Selection criteria All relevant randomised, at least single-blind trials, comparing clozapine with other atypical antipsychotics, any dose and oral formulations, for people with schizophrenia or related disorders. Data collection and analysis We selected trials and extracted data independently. For dichotomous data we calculated relative risks (RR) and their 95% confidence intervals (CI) based on a random-effects model. We calculated numbers needed to treat/harm (NNT/NNH) where appropriate. For continuous data, we calculated mean differences (MD) again based on a random-effects model. Main results The review currently includes 27 blinded randomised controlled trials, which involved 3099 participants. Twelve randomised control trials compared clozapine with olanzapine, five with quetiapine, nine with risperidone, one with ziprasidone and two with zotepine. Attrition from these studies was high (overall 30.1%), leaving the interpretation

  2. Olanzapine Versus Placebo in the Treatment of Adolescents With Bipolar Mania

    National Research Council Canada - National Science Library

    Robertson-Plouch, Carol; DelBello, Melissa; Lin, Daniel; Kryzhanovskaya, Ludmila; Xu, Wen; Biederman, Joseph; Tohen, Mauricio; Wagner, Karen; Carlson, Gabrielle; Dittmann, Ralf W; Wozniak, Janet; Kowatch, Robert; Findling, Robert

    2007-01-01

    Objective: The purpose of this study was to evaluate the efficacy and safety of olanzapine for the treatment of acute manic or mixed episodes associated with bipolar disorder in adolescents. Method...

  3. Olanzapine for the Prevention of Chemotherapy-Induced Nausea and Vomiting

    Science.gov (United States)

    Navari, Rudolph M.; Qin, Rui; Ruddy, Kathryn J.; Liu, Heshan; Powell, Steven F.; Bajaj, Madhuri; Dietrich, Leah; Biggs, David; Lafky, Jacqueline M.; Loprinzi, Charles L.

    2016-01-01

    BACKGROUND We examined the efficacy of olanzapine for the prevention of nausea and vomiting in patients receiving highly emetogenic chemotherapy. METHODS In a randomized, double-blind, phase 3 trial, we compared olanzapine with placebo, in combination with dexamethasone, aprepitant or fosaprepitant, and a 5-hydroxytryptamine type 3–receptor antagonist, in patients with no previous chemotherapy who were receiving cisplatin (≥70 mg per square meter of body-surface area) or cyclophosphamide–doxorubicin. The doses of the three concomitant drugs administered before and after chemotherapy were similar in the two groups. The two groups received either 10 mg of olanzapine orally or matching placebo daily on days 1 through 4. Nausea prevention was the primary end point; a complete response (no emesis and no use of rescue medication) was a secondary end point. RESULTS In the analysis, we included 380 patients who could be evaluated (192 assigned to olanzapine, and 188 to placebo). The proportion of patients with no chemotherapy-induced nausea was significantly greater with olanzapine than with placebo in the first 24 hours after chemotherapy (74% vs. 45%, P = 0.002), the period from 25 to 120 hours after chemotherapy (42% vs. 25%, P = 0.002), and the overall 120-hour period (37% vs. 22%, P = 0.002). The complete-response rate was also significantly increased with olanzapine during the three periods: 86% versus 65% (P<0.001), 67% versus 52% (P = 0.007), and 64% versus 41% (P<0.001), respectively. Although there were no grade 5 toxic effects, some patients receiving olanzapine had increased sedation (severe in 5%) on day 2. CONCLUSIONS Olanzapine, as compared with placebo, significantly improved nausea prevention, as well as the complete-response rate, among previously untreated patients who were receiving highly emetogenic chemotherapy. (Funded by the National Cancer Institute; ClinicalTrials.gov number, NCT02116530.) PMID:27410922

  4. Olanzapine-induced Priapism in a Child with Asperger’s Syndrome

    Science.gov (United States)

    Bozkurt, Hasan; Şahin, Serkan

    2017-01-01

    Background: Priapism is a potentially painful and prolonged erection that occurs in the absence of any stimulation. Olanzapine has been reported to induce priapism in several adult cases with schizophrenia and/or mood disorders but very rarely reported in children. Case Report: 9-year-old male with Asperger’s Syndrome (AS) referred to our clinic with the complaints of inattention, hyperactivity and impulsivity. He was diagnosed with attention deficit hyperactivity disorder (ADHD) and given methylphenidate treatment which ameliorated his ADHD symptoms. He started to have severe loss of appetite after methylphenidate treatment so olanzapine 2.5 mg/day was added to cope with severe inappetence. However he experienced priapism after olanzapine and priapism resolved after ceasing the drug. His mother restarted olanzapine because he benefited from olanzapine. But the same episodes occurred soon after olanzapine again and his mother had to stop the medication. Conclusion: Because atypical antipsychotics are now widely used in children, unusual side effects such as priapism should be taken into consideration for the differential diagnosis. PMID:28251031

  5. The promotion of olanzapine in primary care: an examination of internal industry documents.

    Science.gov (United States)

    Spielmans, Glen I

    2009-07-01

    Media reports have discussed how olanzapine was marketed off-label for dementia and subsyndromal bipolar disorder. Much of this marketing occurred in primary care settings. However, these reports have provided few details. In legal proceedings, Lilly disclosed internal documents that detail the strategies utilized to market olanzapine. The current paper addresses the marketing of olanzapine in detail based upon a review of these documents. All 358 documents released by Lilly are publicly available online. Documents were utilized for this review if they were relevant to the marketing of olanzapine in primary care settings in the United States. It was found that olanzapine was marketed off-label in primary care settings for relatively mild symptoms that were framed as bipolar disorder and schizophrenia. A key strategy in this campaign was the use of hypothetical patient profiles in detailing visits, most of which clearly failed to meet diagnostic criteria for any recognized mental disorder. Evidence emerged that olanzapine was also marketed off-label as a treatment for dementia.

  6. An unusual case of hypothermia associated with therapeutic doses of olanzapine: a case report

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    Ratnayake Shiroma L

    2011-05-01

    Full Text Available Abstract Introduction We report a case of a 42-year-old man who had symptomatic hypothermia as a result of taking olanzapine for paranoid schizophrenia. According to published data, only a few cases of hypothermia associated with olanzapine have been reported since its introduction into clinical use. Case presentation A 42-year-old Sri Lankan man with schizophrenia who was being treated with a therapeutic dose of olanzapine presented with reduced level of consciousness. He had a core temperature of 32°C and was bradycardic. At the time of admission, the electrocardiogram showed sinus bradycardia with J waves. He did not have any risk factors for developing hypothermia except the use of olanzapine. There was improvement in his clinical condition with reversal of electrocardiogram changes following gradual rewarming and the omission of olanzapine. Conclusion Hypothermia induced by antipsychotic medications is not uncommon, but olanzapine-induced hypothermia is rare and occurrence has been reported during initiation or increasing the dose. But here the patient developed hypothermia without dose adjustment.

  7. Betahistine decreases olanzapine-induced weight gain and somnolence in humans.

    Science.gov (United States)

    Barak, Nir; Beck, Yaffa; Albeck, Joseph H

    2016-03-01

    Olanzapine's efficacy in schizophrenia is attributed to antagonism of dopamine and serotonin receptors. Olanzapine is also a potent histamine-H1 antagonist that results in weight gain and somnolence. Betahistine is a centrally acting histamine-H1 agonist, and therefore may reduce olanzapine's effect on histamine receptors in the brain. Olanzapine's high affinity for the histamine-H1 receptor warrants the use of high doses of betahistine. Forty-eight healthy women were recruited and randomized to receive either betahistine 144 mg/day or matching placebo for 4 weeks. Due to the high dose of betahistine, olanzapine was started only on the second week and titrated up to 10 mg/day, and co-administration continued for an additional 2 weeks. Only nominal differences in adverse events were noted between the treatment groups. Betahistine caused a 37% reduction in mean weight gain (1.24 kg in the betahistine arm vs. 1.93 kg in the placebo arm; p=.049) and 60% reduction in the mean increase in daytime Epworth sleepiness scores (1.82 units in the betahistine group vs. 3.57 units in the placebo group; p=.042). The present study suggests that betahistine-olanzapine co-administration, in healthy female subjects, yields an acceptable safety profile with mitigation of weight gain and somnolence. This should be further tested in a patient cohort.

  8. Thrombocytopenia associated with olanzapine: A case report and review of literature

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    Swapnajeet Sahoo

    2016-01-01

    Full Text Available There is limited literature on olanzapine-associated thrombocytopenia. In this report, we present a case of a 32-year-old female, suffering from persistent delusional disorder who had thrombocytopenia (46,000/mm3 with the use of olanzapine 25 mg/day, 6 weeks after starting medication. Blood film did not reveal any evidence of any dysplastic cells, disturbance in the count of other cell lines, and autoimmune workup including antinuclear antibodies and anti-neutrophil cytoplasmic antibodies were found to be negative. Given no other etiology, olanzapine was gradually tapered, and platelet counts were monitored. Reduction in the dose of olanzapine led to an improvement in platelet counts which reached the normal range after complete stoppage of olanzapine. In view of continued psychotic symptoms, she was started on clozapine and which was gradually increased to 200 mg/day with biweekly monitoring of total platelet counts before each increment in the dose of clozapine. Thrombocytopenia did not recur with use of clozapine. With clozapine, her psychosis improved by nearly 60%. A review of literature revealed only eight case reports supporting the association of olanzapine and thrombocytopenia.

  9. Quetiapine monotherapy in acute phase for major depressive disorder: a meta-analysis of randomized, placebo-controlled trials

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    Maneeton Narong

    2012-09-01

    Full Text Available Abstract Background Schizophrenia and bipolar depression trials suggest that quetiapine may have an antidepressant effect. Objectives This meta-analysis aimed to determine the efficacy, acceptability and tolerability of quetiapine treatment for major depressive disorder (MDD. Only the randomized controlled trials (RCTs comparison between quetiapine and placebo were included. The authors searched such clinical trials carried out between 1991 and February 2012. Data sources MEDLINE, EMBASE, CINHL, PsycINFO and Cochrane Controlled Trials Register were searched in February 2012. Study populations comprised adults with MDD or major depression. Study eligible criteria, participants and interventions Eligible studies were randomized, placebo-controlled trials of quetiapine monotherapy carried out in adults with MDD and presenting endpoint outcomes relevant to: i depression severity, ii response rate, iii overall discontinuation rate, or iv discontinuation rate due to adverse events. No language restriction was applied. Study appraisal and synthesis methods All abstracts identified by the electronic searches were examined. The full reports of relevant studies were assessed, and the data of interest were extracted. Based on the Cochrane methods of bias assessment, risks of bias were determined. The studies with two risks or less were included. The efficacy outcomes were the mean change scores of depression rating scales, the overall response rate, and the overall remission rates. The overall discontinuation rate was considered as a measure of acceptability. The discontinuation rate due to adverse events was a measure of tolerability. Relative risks (RRs and weighted mean differences (WMDs with 95% confidence intervals (CIs were computed by using a random effect model. Results A total of 1,497 participants in three RCTs were included. All trials examined the quetiapine extended-release (XR. The pooled mean change scores of the Montgomery-Asberg Depression

  10. Analysis of potentially predictive factors of efficacy of adjunct extended-release quetiapine fumarate in patients with major depressive disorder.

    Science.gov (United States)

    Bauer, Michael; Thase, Michael E; Liu, Sherry; Earley, Willie; Eriksson, Hans

    2015-05-01

    Identification of predictors of treatment response in patients with major depressive disorder (MDD) may facilitate improved disease management. Data were pooled from two 6-week, double-blind, placebo-controlled studies of extended-release quetiapine (quetiapine XR; 150 or 300 mg/day) as adjunct to ongoing antidepressant therapy. Effects of psychiatric history and baseline demographic and disease characteristics on efficacy outcomes (Week 6 Montgomery Åsberg Depression Rating Scale [MADRS] total score reduction) were evaluated in population subgroups (quetiapine XR both doses pooled, n = 616; placebo, n = 303). Baseline Clinical Global Impressions-Severity (CGI-S) score and previous depressive episodes on Week 6 MADRS total score change, and baseline MADRS individual item scores on Week 6 change in CGI-Improvement score, were also evaluated. No major differences between responders and non-responders to quetiapine XR were observed for patient characteristics or demographic and disease characteristics. No suggestion of a predictive association was found between baseline CGI-S score, number of depressive episodes, and baseline MADRS item scores and efficacy outcomes. These analyses showed no major differences between responders and non-responders, and no predictive association between the parameters assessed and efficacy outcomes for adjunct quetiapine XR in patients with MDD and an inadequate response to prior antidepressant therapy.

  11. Determination of olanzapine and N-desmethyl-olanzapine in plasma using a reversed-phase HPLC coupled with coulochemical detection: correlation of olanzapine or N-desmethyl-olanzapine concentration with metabolic parameters.

    Directory of Open Access Journals (Sweden)

    Mong-Liang Lu

    Full Text Available BACKGROUND: Olanzapine (OLZ is one of the most prescribed atypical antipsychotic drugs but its use is associated with unfavorable metabolic abnormalities. N-desmethyl-olanzapine (DMO, one of the OLZ metabolites by CYP1A2, has been reported to have a normalizing action on metabolic abnormalities, but this remains unclear. Our aim was to explore the correlation between the concentrations of OLZ or DMO with various metabolic parameters in schizophrenic patients. METHODS: The chromatographic analysis was carried out with a solvent delivery system coupled to a Coulochem III coulometric detector to determine OLZ and DMO simultaneously in OLZ-treated patients. The correlation between the concentration of OLZ or DMO and the metabolic parameters was analyzed by the Spearman rank order correlation method (r s. PRINCIPAL FINDINGS: The established analytical method met proper standards for accuracy and reliability and the lower limitation of quantification for each injection of DMO or OLZ was 0.02 ng. The method was successfully used for the analysis of samples from nonsmoking patients (n = 48 treated with OLZ in the dosage range of 5-20 mg per day. There was no correlation between OLZ concentrations and tested metabolic parameters. DMO concentrations were negatively correlated with glucose (r s = -0.45 and DMO concentrations normalized by doses were also negatively correlated with insulin levels (r s = -0.39; however, there was a marginally positive correlation between DMO and homocysteine levels (r s = +0.38. CONCLUSIONS: The observed negative correlations between levels of DMO and glucose or insulin suggest a metabolic normalization role for DMO regardless of its positive correlation with a known cardiovascular risk factor, homocysteine. Additional studies of the mechanisms underlying DMO's metabolic effects are warranted.

  12. Investigation of a possible interaction between quetiapine and armodafinil in patients with schizophrenia: an open-label, multiple-dose study.

    Science.gov (United States)

    Darwish, Mona; Bond, Mary; Hellriegel, Edward T; Youakim, James M; Yang, Ronghua; Robertson, Philmore

    2012-09-01

    The wakefulness-promoting medication armodafinil (R-modafinil) is being studied as an adjunctive treatment for patients with schizophrenia receiving antipsychotic therapy. This open-label study in 37 adults with schizophrenia evaluated whether a drug-drug interaction occurs between armodafinil (a moderate CYP3A4 inducer) and the atypical antipsychotic quetiapine (primarily metabolized by CYP3A4). Patients were required to be on a stable dose of quetiapine ≥300 mg once daily in the evening before enrollment. Steady-state quetiapine pharmacokinetics were determined following daily administration of quetiapine alone in the evening (day 5) and then following concomitant armodafinil administration (titrated to 250 mg) daily in the morning (day 38). In 25 evaluable patients, concomitant armodafinil resulted in a statistically significant decrease in mean AUC(0-24) and C(max) values of quetiapine by 42% and 45%, respectively, versus quetiapine alone. Adverse events occurred more frequently with combination therapy and were consistent with the known profiles of the 2 drugs. No significant changes in mean PANSS negative, positive, and total scores or SANS scores were observed. Although the data do not suggest that the observed decrease in systemic exposure to quetiapine was associated with a change in disease state, patients with schizophrenia should be monitored during combination therapy with quetiapine and armodafinil.

  13. The effects of second generation antipsychotic drugs on sleep variables in healthy subjects and patients with schizophrenia.

    Science.gov (United States)

    Monti, Jaime M; Torterolo, Pablo; Pandi Perumal, Seithikurippu R

    2017-06-01

    Insomnia is a common feature in schizophrenia, and is characterized by an increase of sleep latency (SL), as well as reductions in total sleep time (TST) and sleep efficiency (SE). Regarding sleep architecture, non-rapid-eye-movement (NREM) sleep, slow wave sleep (SWS) and rapid-eye-movement (REM) sleep latency are decreased, whereas REM sleep tends to remain unchanged. According to polysomnographic studies, clozapine, olanzapine, quetiapine and ziprasidone administration increased TST and/or SE in healthy subjects. Additionally, olanzapine and ziprasidone augmented SWS, while changes corresponding to REM sleep were inconsistent. Furthermore, administration of clozapine, olanzapine and paliperidone to patients with schizophrenia was followed in most instances by a significant reduction of SL and an increase of TST and SE. In addition, olanzapine and paliperidone augmented SWS and REM sleep. By contrast, quetiapine administration further disrupted sleep as judged by the increase of SL, wake time after sleep onset (WASO) and REM sleep latency, and the reduction of SWS and REM sleep. No consistent effects on sleep variables were obtained during treatment with risperidone. To date, no polysomnographic studies have been published on the effects of aripiprazole, asenapine, iloperidone and lurasidone on sleep in either healthy subjects or patients with schizophrenia. Taken together, this evidence supports the conclusion that second generation antipsychotics (SGAs) including clozapine, olanzapine and paliperidone may ameliorate insomnia in patients with schizophrenia.

  14. Combination treatment of tamoxifen with risperidone in breast cancer.

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    Wei-Lan Yeh

    Full Text Available Tamoxifen has long been used and still is the most commonly used endocrine therapy for treatment of both early and advanced estrogen receptor-positive breast cancer in pre- and post-menopause women. Tamoxifen exerts its cytotoxic effect primarily through cytostasis which is associated with the accumulation of cells in the G0/G1 phase of the cell cycle. Apoptotic activity can also be exerted by tamoxifen which involves cleavage of caspase 9, caspase 7, caspase 3, and poly-ADP-ribose polymerase (PARP. Down-regulation of anti-apoptotic proteins Bcl-2 and Bcl-xL and up-regulation of pro-apoptotic proteins Bax and Bak have also been observed. In addition, stress response protein of GRP 94 and GRP 78 have also been induced by tamoxifen in our study. However, side effects occur during tamoxifen treatment in breast cancer patients. Researching into combination regimen of tamoxifen and drug(s that relieves tamoxifen-induced hot flushes is important, because drug interactions may decrease tamoxifen efficacy. Risperidone has been shown to be effective in reducing or eliminating hot flushes on women with hormonal variations. In this present study, we demonstrated that combination of tamoxifen with risperidone did not interfered tamoxifen-induced cytotoxic effects in both in vitro and in vivo models, while fluoxetine abrogated the effects of tamoxifen. This is the first paper suggesting the possibility of combination treatment of tamoxifen with risperidone in breast cancer patients, providing a conceivable resolution of tamoxifen-induced side effects without interfering the efficacy of tamoxifen against breast cancer.

  15. Evidence based administration of risperidone and paliperidone for the treating conduct disorder

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    Ahmad Ghanizadeh

    2013-01-01

    Full Text Available Background: This study evaluates the evidence-based administration of risperidone and paliperidone for the treating children and adolescents with conduct disorder (CD. Materials and Methods: A review of the current literature from clinical trials that investigated the efficacy of risperidone and paliperidone on CD considering the inclusion criteria and search strategies was performed by a search of PubMed and Google Scholar databases. Results: Out of 53 titles, 31 were irrelevant. The abstract of 22 potentially related articles were studied. Only six articles reported the results of clinical trial. However, one of them reported the effect of risperidone on conduct behaviors in autistic disorders. One study was a re-analysis of two previous studies, one study reported the effects of maintenance versus withdrawal of risperidone treatment and two studies included children with sub-average intelligence. Headache, somnolence and increased appetite are among the most common reported adverse effects. No study examined the effect of paliperidone on CD was found. Conclusion: Current literature suggests that risperidone could be effective for treating some conduct behaviors in children and adolescents. The effect of risperidone on CD is not a well-researched area. There is no well-controlled evidence based reports about the safety and efficacy of risperidone for the treatment of CD. Further trials should examine the efficacy of these medications on CD rather than conduct behaviors or disruptive behavior disorders.

  16. Cognitive effects of six months of treatment with quetiapine in antipsychotic-naïve first-episode schizophrenia

    DEFF Research Database (Denmark)

    Andersen, Rune; Fagerlund, Birgitte; Rasmussen, Hans

    2011-01-01

    Effects of quetiapine on cognition were assessed in a group of first-episode antipsychotic-naïve patients with schizophrenia (N=24). A comprehensive battery of neuropsychological tests was administered at baseline and after 6months of treatment with quetiapine. In order to examine retest effects,...... on sustained attention and working memory that were found in healthy controls. The main result of the study is that there was very little evidence of efficacy of quetiapine on cognition. The study also indicated a lack of normal retest effects in patients compared to controls........ Patients also improved on speed of processing; however, this was parallel to the retest effects found in healthy controls. When covaried for differences at baseline, patients showed smaller improvements in speed of processing than the retest effects found in controls, as well as a lack of retest effects...

  17. Acute and chronic treatment with quetiapine induces antidepressant-like behavior and exerts antioxidant effects in the rat brain.

    Science.gov (United States)

    Ignácio, Zuleide M; Réus, Gislaine Z; Abelaira, Helena M; de Moura, Airam B; de Souza, Thays G; Matos, Danyela; Goldim, Mariana P; Mathias, Khiany; Garbossa, Leandro; Petronilho, Fabricia; Quevedo, João

    2017-08-01

    Many studies note that changes in oxidative balance are involved in the pathogenesis of major depressive disorder (MDD) and in the success of some antidepressants. Quetiapine exerts a therapeutic response and induces changes in physiological mechanisms that appear to underlie MDD. The objective of this study was to evaluate the antidepressant and antioxidant effects of quetiapine (20 mg /kg) in adult animals. Sixty minutes after an acute treatment or the last administration of chronic treatment (14 days) with quetiapine, animals were subjected to the forced swimming test (FST) to evaluate mobility parameters. Then, the hippocampus, prefrontal cortex (CPF), amygdala and nucleus accumbens (NAc) were removed for the assessment of oxidative stress parameters. Both acute and chronic treatments exerted antidepressant-like effects. Myeloperoxidase (MPO) activity was reduced in the amygdala after acute treatment and in the hippocampus, PFC and amygdala after chronic treatment. In addition, after chronic treatment, the levels of thiobarbituric reactive species (TBARS) were reduced in the amygdala and NAc, and the protein carbonyl content was reduced in the CPF. Superoxide dismutase (SOD) activity increased in the NAc after acute and chronic treatments. Catalase (CAT) activity increased in the PFC after acute treatment and in the NAc after acute and chronic treatments. The concentration of nitrite/nitrate was lower in the CPF after chronic treatment. These results corroborate the antidepressant effect of quetiapine and indicate that quetiapine exhibits an antioxidant profile, a physiological mechanism that appears be involved in the therapeutic function of quetiapine in individuals resistant to classical antidepressant treatments.

  18. Alterations to melanocortinergic, GABAergic and cannabinoid neurotransmission associated with olanzapine-induced weight gain.

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    Katrina Weston-Green

    Full Text Available BACKGROUND/AIM: Second generation antipsychotics (SGAs are used to treat schizophrenia but can cause serious metabolic side-effects, such as obesity and diabetes. This study examined the effects of low to high doses of olanzapine on appetite/metabolic regulatory signals in the hypothalamus and brainstem to elucidate the mechanisms underlying olanzapine-induced obesity. METHODOLOGY/RESULTS: Levels of pro-opiomelanocortin (POMC, neuropeptide Y (NPY and glutamic acid decarboxylase (GAD(65, enzyme for GABA synthesis mRNA expression, and cannabinoid CB1 receptor (CB1R binding density (using [(3H]SR-141716A were examined in the arcuate nucleus (Arc and dorsal vagal complex (DVC of female Sprague Dawley rats following 0.25, 0.5, 1.0 or 2.0 mg/kg olanzapine or vehicle (3×/day, 14-days. Consistent with its weight gain liability, olanzapine significantly decreased anorexigenic POMC and increased orexigenic NPY mRNA expression in a dose-sensitive manner in the Arc. GAD(65 mRNA expression increased and CB1R binding density decreased in the Arc and DVC. Alterations to neurotransmission signals in the brain significantly correlated with body weight and adiposity. The minimum dosage threshold required to induce weight gain in the rat was 0.5 mg/kg olanzapine. CONCLUSIONS: Olanzapine-induced weight gain is associated with reduced appetite-inhibiting POMC and increased NPY. This study also supports a role for the CB1R and GABA in the mechanisms underlying weight gain side-effects, possibly by altering POMC transmission. Metabolic dysfunction can be modelled in the female rat using low, clinically-comparable olanzapine doses when administered in-line with the half-life of the drug.

  19. H3 histamine receptor antagonist pitolisant reverses some subchronic disturbances induced by olanzapine in mice.

    Science.gov (United States)

    Dudek, Magdalena; Kuder, Kamil; Kołaczkowski, Marcin; Olczyk, Adrian; Żmudzka, Elżbieta; Rak, Aleksandra; Bednarski, Marek; Pytka, Karolina; Sapa, Jacek; Kieć-Kononowicz, Katarzyna

    2016-10-01

    The use of atypical antipsychotic drugs like olanzapine is associated with side effects such as sedation and depression-like symptoms, especially during the initial period of the use. It is believed that the occurrence of these undesirable effectsis mainly the result of the histamine H1receptors blockade by olanzapine. In addition, use of olanzapine increases the level of triglycerides in the blood, which correlates with growing obesity. The aim of this study was to investigate the influence of pitolisant - H3 histamine antagonist - on subchronic olanzapine-induced depresion-like symptoms, sedation and hypertriglicerydemia. Forced swim test was conducted to determinate depressive-like effect of olanzapine and antidepressive-like activity during the co-administered pitolisant. The test was performed after the first and fifteenth day of the treatment of the mice. The spontaneous activity of the mice was measured on the fourteenth day of the treatment with a special, innovative RFID-system (Radio-frequency identification system) - TraffiCage (TSE-Systems, Germany). Triglyceride levels were determined on the sixteenth day of the experiment after 15 cycles of drug administration. Daily olanzapine treatment (4 mg/kg b.w., i.p., d.p.d) for 15 days significantly induces sedation (p < 0.05) and prolongs immobility time in forced swim tests (FST) in mice (p < 0.05); and also elevates the level of triglycerides (p < 0.05). Administration of pitolisant (10 mg/kg b.w., i.p.) subsequentto olanzapine normalizes these adverse effects. This study presents a promising alternative for counteracting some behavioral changes and metabolic disturbances which occur in the early period of treatment with antipsychotic drugs.

  20. Paliperidone ER and oral risperidone in patients with schizophrenia: a comparative database analysis

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    Schooler Nina

    2011-02-01

    Full Text Available Abstract Background To compare the efficacy and tolerability of paliperidone extended-release (ER with risperidone immediate-release using propensity score methodology. Methods Six double-blind, randomized, placebo-controlled, short-term clinical trials for acute schizophrenia with availability of individual patient-level data were identified (3 per compound. Propensity score pairwise matching was used to balance observed covariates between the paliperidone ER and risperidone patient populations. Scores were generated using logistic regression models, with age, body mass index, race, sex, baseline Positive and Negative Syndrome Scale (PANSS total score and baseline Clinical Global Impressions–Severity (CGI-S score as factors. The dosage range of paliperidone ER (6-12 mg/day was compared with 2 risperidone dosage ranges: 2-4 and 4-6 mg/day. The primary efficacy measure was change in PANSS total score at week 6 end point. Tolerability end points included adverse event (AE reports and weight. AEs with rates ≥5% and with a ≥2% difference between paliperidone ER and risperidone were identified. Results Completion rates for placebo-treated subjects in paliperidone ER trials (n = 95 and risperidone trials (n = 122 groups were 36.8% and 51.6%, respectively; end point changes on PANSS total scores were similar (p = 0.768. Completion rates for subjects receiving paliperidone ER 6-12 mg/day (n = 179, risperidone 2-4 mg/day (n = 113 or risperidone 4-6 mg/day (n = 129 were 64.8%, 54.0% and 66.7%, respectively (placebo-adjusted rates: paliperidone ER vs risperidone 2-4 mg/day, p = 0.005; paliperidone ER vs risperidone 4-6 mg/day, p = 0.159. PANSS total score improvement with paliperidone ER was greater than with risperidone 2-4 mg/day (difference in mean change score, -6.7; p Conclusions This indirect database analysis suggested that paliperidone ER 6-12 mg/day may be more efficacious than risperidone 2-4 mg/day and as efficacious as risperidone 4-6 mg

  1. Fatal hypertriglyceridaemia, acute pancreatitis and diabetic ketoacidosis possibly induced by quetiapine

    DEFF Research Database (Denmark)

    Madsen, Kristian Roerbaek

    2014-01-01

    within 36 h from initial presentation. While second-generation antipsychotics are well known to be causally linked to diabetes and hyperlipidaemia, this is to my knowledge the first-described case of a fatal triad of extreme hypertriglyceridaemia, acute pancreatitis and diabetic ketoacidosis possibly......A 27-year-old man treated with quetiapine for anxiety disorder developed hypertriglyceridaemia-induced acute pancreatitis and diabetic ketoacidosis. He was otherwise physically healthy with no family history of hyperlipidaemia. Despite aggressive intensive therapy he died of multiorgan failure...

  2. [Generic quetiapine in the treatment of acute schizophrenia and schizoaffective disorder].

    Science.gov (United States)

    György, Bartkó; Robert, Kárpáti; László, Csekey; Andrea, Juhász

    2008-12-01

    The aim of the study was to assess the efficacy, tolerability and safety of the own developed generic quetiapine, Ketilept (EGIS Pharmaceutical Ltd, Budapest) in patients with an acute episode of schizophrenia and schizoaffective disorder. These was a multicenter, non comparative, open label, 12-week trial on oral generic quetiapine conducted in 110 patients with DSM-IV acute schizophrenia or schizoaffective disorder. Patients received Ketilept 50 mg on day 1, 100 mg on day 2, 200 mg on day 3, 300 mg on day 4. The flexible dosing (150-750 mg/day) started on day 5. Patients were evaluated at baseline, at day 7, 14, 28 and 84. Baseline and outcome assessment included Positive and Negative Syndrome Scale (PANSS), Clinical Global Impression Severity of Illness Subscale (CGI-S) and Global Improvement Subscale (CGI-I), Subjective Well-being on Neuroleptics Scale (SWN), Simpson-Angus Extrapyramidal Rating Scale (SAS), Barnes Akathisia Rating Scale (BARS) and UKU Side Effects Rating Scale (UKU). Changes in overall body weight, body mass index (BMI) and abdominal circumference were also evaluated. After 12 weeks on Ketilept therapy, significant improvements were observed on all major symptoms measures and subscales. 44 (44%) of patients were rated much or very much improved on CGI-I at week 12. The mean SAS and BARS score significantly reduced during the generic quetiapine treatment period (p = 0.0001, p = 0.001). No change was found in the body weight, BMI and abdominal circumference during treatment with Ketilept for 12 weeks. The most common side effects were sedation, and dizziness. 14 adverse events occurred in 6 subjects (5%), of whom 3 patients (2.7%) encountered 3 serious adverse events. The adverse events were mainly mild and moderate. 103 patients (93.6)% completed the study, 2 patients (1.8%) were discontinued from the study due to serious adverse events (insufficient clinical response, sedation). Despite the limitations of the design, our results suggest that

  3. Efficacy and Safety of Extended-Release Quetiapine Fumarate in Youth with Bipolar Depression: An 8 Week, Double-Blind, Placebo-Controlled Trial

    Science.gov (United States)

    Pathak, Sanjeev; Earley, Willie R; Liu, Sherry; DelBello, Melissa P

    2014-01-01

    Abstract Objective: Quetiapine is an atypical antipsychotic with demonstrated efficacy in the treatment of adolescent schizophrenia and pediatric bipolar mania. Large, placebo-controlled studies of interventions in pediatric bipolar depression are lacking. The current study investigated the efficacy and safety of quetiapine extended-release (XR) in patients 10–17 years of age, with acute bipolar depression. Methods: This multicenter, double-blind, randomized, placebo-controlled study investigated quetiapine XR (dose range, 150–300 mg/day) in pediatric outpatients with an American Psychiatric Association, Diagnostic and Statistical Manual of Mental Disorders, 4th ed., Text Revision (DSM-IV-TR) diagnosis of bipolar I or bipolar II disorder (current or most recent episode depressed) treated for up to 8 weeks (ClinicalTrials.gov identifier: NCT00811473). The primary study outcome was mean change in Children's Depression Rating Scale–Revised (CDRS-R) total score. Secondary efficacy outcomes included CDRS-R-based response and remission rates. Results: Of 193 patients randomized to treatment, 144 patients completed the study (75.3% of quetiapine XR group [n=70]; 74.0% of placebo group [n=74]). Least squares mean changes in CDRS-R total score at week 8 were: −29.6 (SE, 1.65) with quetiapine XR and −27.3 (SE, 1.60) with placebo, a between-treatment group difference of −2.29 (SE, 1.99; 95% CI, −6.22, 1.65; p=0.25; mixed-model for repeated measures analysis). Rates of response and remission did not differ significantly between treatment groups. The safety profile of quetiapine XR was broadly consistent with the profile reported previously in adult studies of quetiapine XR and pediatric studies of quetiapine immediate-release (IR). Potentially clinically significant elevations in clinical chemistry values included triglycerides (9.3%, quetiapine XR; 1.4%, placebo group) and thyroid stimulating hormone (4.7%, quetiapine XR; 0%, placebo group). An adverse event

  4. Atypical Antipsychotics and the Risk of Hyperlipidemia: A Sequence Symmetry Analysis.

    Science.gov (United States)

    Takeuchi, Yoshinori; Kajiyama, Kazuhiro; Ishiguro, Chieko; Uyama, Yoshiaki

    2015-07-01

    Although hyperlipidemia is a well known adverse event of atypical antipsychotic (AAP) medication, there are few studies that have quantitatively compared the risks of various AAPs. Our aim was to comparatively evaluate the risk of hyperlipidemia associated with the use of AAPs approved in Japan through a consecutive epidemiological study. We conducted a sequence symmetry analysis (SSA) using health insurance claims data to analyze the following nine AAPs approved for use in Japan: risperidone, paliperidone, perospirone hydrochloride hydrate, blonanserin, clozapine, olanzapine, quetiapine fumarate, aripiprazole, and zotepine. Exposed cases were identified from drug dispensing records as those who had been administered both AAPs and antihyperlipidemic drugs. The adjusted sequence ratio (ASR) and 95 % confidence interval (CI) for each individual AAP and for all AAPs were calculated while controlling for time trends in dispensing patterns. Olanzapine was significantly associated with increased hyperlipidemia occurrence (ASR 1.56; 95 % CI 1.25-1.95). The ASRs obtained for risperidone (1.01; 95 % CI 0.80-1.27), perospirone hydrochloride hydrate (0.93; 95 % CI 0.63-1.39), blonanserin (0.83; 95 % CI 0.52-1.33), quetiapine fumarate (0.93; 95 % CI 0.73-1.18), and aripiprazole (1.02; 95 % CI 0.82-1.26) were approximately 1.0. Unstable estimates (wide CIs) were obtained for paliperidone and zotepine due to the small sample sizes. Among the AAPs used in Japan, only olanzapine was found to have an elevated risk of hyperlipidemia. In contrast, risperidone, perospirone hydrochloride hydrate, blonanserin, quetiapine fumarate, and aripiprazole had relatively low risks.

  5. Olanzapine for the prevention and treatment of chronic nausea and chemotherapy-induced nausea and vomiting.

    Science.gov (United States)

    Navari, Rudolph M

    2014-01-05

    Olanzapine is an atypical antipsychotic agent of the thiobenzodiazepine class. It blocks multiple neurotransmitter receptors including dopaminergic at D1, D2, D3, D4 brain receptors, serotonergic at 5-HT2a, 5-HT2c, 5-HT3, 5-HT6 receptors, catecholamines at alpha1 adrenergic receptors, acetylcholine at muscarinic receptors, and histamine at H1 receptors. Olanzapine has five times the affinity for 5-HT2 receptors than D2 receptors and has been used to treat schizophrenia and delirium. Olanzapine's activity at multiple receptors, particularly at the D2, 5-HT2c, and 5-HT3 receptors which appear to be involved in nausea and emesis, has prompted its use in the treatment of nausea and vomiting refractory to standard antiemetics. Case reports and formal clinical trials have demonstrated its efficacy in the treatment of chronic nausea, the prevention of chemotherapy-induced nausea and emesis, and the treatment of breakthrough chemotherapy-induced nausea and emesis. Phase II and phase III clinical trials have demonstrated that there is a significant improvement in nausea when olanzapine is added to guideline directed prophylactic antiemetic agents 5-HT3 receptor antagonists and tachykinin NK1 receptor antagonists in patients receiving moderately or highly emetogenic chemotherapy Common side effects of olanzapine when used over a period of months include weight gain as well as an association with the onset of diabetes mellitus, but these effects have not been seen with short term use of daily doses of less than one week.

  6. Spectrum of binge eating symptomatology in patients treated with clozapine and olanzapine.

    Science.gov (United States)

    Theisen, F M; Linden, A; König, I R; Martin, M; Remschmidt, H; Hebebrand, J

    2003-01-01

    The authors explored the binge eating symptomatology in 74 patients receiving clozapine (N = 57) or olanzapine (N = 17), and compared body mass index (BMI, kg/m(2)) and weight gain in patients with and without binge eating symptomatology. Subjects who screened positively for binge eating were interviewed using a modified version of the Questionnaire on Eating and Weight Patterns (QEWP). Current BMIs were assessed cross-sectionally, BMIs at initiation of clozapine/olanzapine treatment retrospectively. Thirty-seven subjects (50%) screened positively. Taking clozapine and olanzapine together, 6/27 (22.2%) females and 3/47 (6.4%) males fulfilled criteria for binge eating disorder, 3/27 (11.1%) females and 2/47 (4.3%) males for bulimia nervosa. Patients who screened positively showed higher current BMIs (26.8 +/- 3.9 vs. 24.7 +/- 3.7 kg/m(2)) and higher BMI increments during clozapine/olanzapine treatment (3.9 +/- 3.1 vs. 2.6 +/- 3.4 kg/m(2)) than patients who screened negatively. We conclude that clozapine/olanzapine may induce binge eating and full blown eating disorders which may have predictive value for weight gain. For future research in this field we suggest a novel DSM-IV research classification "Medication-induced eating disorders".

  7. A comparative study of olanzapine versus asenapine in acute treatment of manic episode: A 3-week prospective study

    Directory of Open Access Journals (Sweden)

    Ajeet Sidana

    2014-01-01

    Full Text Available Introduction: Treatment of bipolar disorders has evolved over the years from conventional mood stabilizers to second-generation antipsychotics. Among the atypical antipsychotics, few have been approved by Food and Drug Administration as treatment of bipolar disorders. Aim: To study the efficacy and tolerability of olanzapine and asenapine in the acute treatment of bipolar disorder-manic episode in a 3-week randomized prospective study. Materials and Methods: A 3-week randomized, prospective, comparative, flexible doses of olanzapine (5-30 mg/day and asenapine (10-20 mg/day for acute treatment of bipolar disorder-current manic episode with or without psychotic symptoms in hospitalized patients. Results: The end-point reduction in mean score of Young Mania rating scale in the olanzapine group was 15.82 in comparison to 6.88 in the asenapine group. Mean score on clinical global impression for bipolar disorder and positive and negative syndrome scale was significantly less in the olanzapine group at the end of the study. 81.81% patients in olanzapine group and 17.60% patients in asenapine group had clinical response. There was significant average weight gain in the olanzapine group - 1.9 kg in comparison to 0.87 kg in asenapine group. Conclusion: The clinical response with olanzapine is significantly higher than the asenapine in the treatment of bipolar disorder-manic episode with or without psychotic symptoms. However, there is significant weight gain in olanzapine-treated patients.

  8. Reducing olanzapine-induced weight gain side effect by using betahistine: a study in the rat model.

    Science.gov (United States)

    Deng, Chao; Lian, Jiamei; Pai, Nagesh; Huang, Xu-Feng

    2012-09-01

    Olanzapine is effective at treating multiple domains of schizophrenia symptoms. However, it induces serious metabolic side effects. Antipsychotic drug's antagonistic affinity to histamine H₁ receptors has been identified as a main contributor for weight gain/obesity side effects. This study therefore investigated whether a combined treatment of betahistine (a H₁ receptor agonist and H₃ receptor antagonist) could reduce the body weight/obesity induced by olanzapine. Female Sprague Dawley rats were treated orally with olanzapine (1 mg/kg, t.i.d.) and/or betahistine (2.67 mg/kg, t.i.d.), or vehicle for two weeks. Rats treated with olanzapine exhibited significant body weight gain and increased food intake. Co-treatment of olanzapine with betahistine significantly prevented (-45%) weight gain and reduced feeding efficiency compared to sole olanzapine treatment. Betahistine treatment alone had no effect on weight gain and food intake. Olanzapine reduced locomotor activity, but not betahistine. These findings demonstrate that olanzapine-induced body weight gain can partially be reduced by co-treatment with betahistine. Betahistine has H₃ receptor antagonistic effects to increase histamine release, which may augment its direct agonistic effects on H₁ receptors. These findings have important implications for clinical trials using betahistine to control antipsychotic-induced obesity side effects.

  9. Sensitive liquid chromatography/tandem mass spectrometry method for the simultaneous determination of olanzapine, risperidone, 9-hydroxyrisperidone, clozapine, haloperidol and ziprasidone in rat brain tissue.

    Science.gov (United States)

    Zhang, Guodong; Terry, Alvin V; Bartlett, Michael G

    2007-10-15

    One prerequisite for therapeutic effects of psychiatric drugs is the ability to pass the blood brain barrier. Hence, it is important to know the concentration of antipsychotic drugs in brain tissue. In general, determinations of lipophilic compounds from lipophilic matricies such as the brain are a challenge. Here we have adapted a plasma assay for antipsychotics for the target organ the brain. Using modified sample preparation and chromatographic strategies, the analytes were extracted from rat brain homogenate and analyzed by LC-MS/MS. The method used a Waters Atlantis dC-18 (30 mm x 2.1 mm i.d., 3 microm) column with a mobile phase of acetonitrile/5 mM ammonium formate (pH 6.1 adjusted with formic acid) and gradient elution. All analytes were detected in positive ion mode using multiple-reaction monitoring. The method was validated and the linearity, lower limit of quantitation, precision, accuracy, recoveries, specificity and stability were determined. This method was then successfully used to quantify the rat brain tissue concentration of the analytes after chronic treatment with these antipsychotic drugs.

  10. A case study: neuroleptic malignant syndrome with risperidone and CYP2D6 gene variation.

    Science.gov (United States)

    Ochi, Shinichiro; Kawasoe, Koichiro; Abe, Masao; Fukuhara, Ryuji; Sonobe, Kantaro; Kawabe, Kentaro; Ueno, Shu-ichi

    2011-01-01

    We present a schizophrenic patient who experienced neuroleptic malignant syndrome with risperidone treatment due to variants of the CYP2D6 gene with reduced function. Clinicians need to be aware of this potential complication.

  11. Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice

    Directory of Open Access Journals (Sweden)

    David Holthoewer

    2010-06-01

    Full Text Available Pharmacokinetic interactions, e.g. modulation of drug transporters like P-glycoprotein at the blood-brain barrier, can be a reason for treatment non-response. This study focuses on the influence of induction of drug transporters on the disposition of the antipsychotic drugs risperidone and 9-hydroxyrisperidone. Brain and serum concentrations of risperidone and its active metabolite 9-hydroxyrisperidone, which are known P-glycoprotein substrates, were measured after drug transporter induction with rifampicin, dexamethasone or 5-pregnene-3beta-ol-20-on-16alpha-carbonitrile using high performance liquid chromatography. Disposition of risperidone and 9-hydroxyrisperidone was dramatically decreased in mouse brain and serum after drug transporter induction. The metabolism of risperidone was also affected.

  12. 78 FR 52777 - Draft Guidance for Industry on Bioequivalence Recommendations for Risperidone Injection...

    Science.gov (United States)

    2013-08-26

    ... on Bioequivalence Recommendations for Risperidone Injection; Availability AGENCY: Food and Drug... provides specific recommendations on the design of bioequivalence (BE) studies to support abbreviated new... availability of a draft guidance for industry entitled ``Bioequivalence Recommendations for Specific...

  13. Serum prolactin levels and sexual dysfunctions in antipsychotic medication, such as risperidone : a review

    NARCIS (Netherlands)

    Knegtering, H; Lambers, PA; Prakken, G; ten Brink, C

    2000-01-01

    Classical antipsychotic drugs increase the level of serum prolactin. The atypical antipsychotic clozapine barely increases prolactin levels. An open naturalistic study in the University Hospital of Groningen suggests that treatment with risperidone in comparison to classical antipsychotics seems to

  14. In Vitro-In Vivo Correlation of Parenteral Risperidone Polymeric Microspheres

    OpenAIRE

    2015-01-01

    The objective of the present study was to determine whether an in vitro-in vivo correlation (IVIVC) can be established for polymeric microspheres that are equivalent in formulation composition but prepared with different manufacturing processes. Risperidone was chosen as a model therapeutic and poly(lactic-co-glycolic acid) (PLGA) with similar molecular weight as that used in the commercial product Risperdal® Consta® was used to prepare risperidone microspheres. Various manufacturing processe...

  15. Development of novel risperidone implants using blends of polycaprolactones and in vitro in vivo correlation studies

    OpenAIRE

    2014-01-01

    The objective of this study was to develop a novel implant containing risperidone intended for long-term treatment in Schizophrenia utilizing in vitro in vivo correlation (IVIVC) studies. Different implants (F1-F8) containing an antipsychotic drug, risperidone, were prepared using a hot melt extrusion technique by taking polycaprolactones of different molecular weights (Mwt. 15000, 45000, 80000) either alone or as their blends, and PLGA (75:25). The implants contained 40% of the drug. After f...

  16. Combination treatment with risperidone long-acting injection and psychoeducational approaches for preventing relapse in schizophrenia

    Science.gov (United States)

    Zhao, Yueren; Kishi, Taro; Iwata, Nakao; Ikeda, Manabu

    2013-01-01

    A recent meta-analysis showed that long-acting injectable (LAI) antipsychotics were not superior to oral antipsychotics for preventing relapse in patients with schizophrenia. We therefore designed a treatment strategy combining risperidone LAI and COMPASS (COMprehensive Psycho-educational Approach and Scheme Set), an original psychoeducational program supporting treatment with risperidone LAI and evaluating subjective treatment satisfaction, transition of symptoms, and effectiveness in preventing symptomatic relapse. The aim of this study was to examine whether addition of COMPASS to risperidone LAI was more effective in preventing relapse in schizophrenia patients than risperidone LAI alone, with the latter group consisting of patients enrolled in a Phase III trial of risperidone LAI in Japan. Patients were followed up for 6 months, with COMPASS continuously implemented from the transition to the observation phase. The primary efficacy measurements were relapse rate (rates of rehospitalization and discontinuation due to inefficacy). Secondary efficacy measurements were the Brief Psychiatric Rating Scale (BPRS) and Global Assessment of Functioning (GAF) scores. Of the 96 patients originally enrolled, 19 (19.8%) were discontinued from all causes. During the 6-month study period, ten of the 96 patients (10.4%) relapsed, compared with a 12.2% relapse rate in patients enrolled in a Phase III trial of risperidone LAI in Japan. Patients showed significant improvements in BPRS total scores (P = 0.0031), BPRS positive (P = 0.0451), BRPS negative (P < 0.0001), and general subscale scores (P = 0.0031), and GAF (P < 0.0001) from baseline to 6 months. In conclusion, the lower relapse rate observed in patients treated with COMPASS plus risperidone LAI than in patients treated with risperidone LAI alone suggests that COMPASS may have benefits in the treatment of schizophrenia, indicating a need for randomized, controlled trials in larger numbers of patients. PMID:24194642

  17. Evaluation of potential pharmacokinetic drug-drug interaction between armodafinil and risperidone in healthy adults.

    Science.gov (United States)

    Darwish, Mona; Bond, Mary; Yang, Ronghua; Hellriegel, Edward T; Robertson, Philmore

    2015-11-01

    Patients with bipolar I disorder and schizophrenia have an increased risk of obstructive sleep apnea. The effects of armodafinil, a weak cytochrome P450 (CYP) 3A4 inducer, on pharmacokinetics and safety of risperidone, an atypical antipsychotic used to treat major psychiatric illness, were investigated. Healthy subjects received 2 mg risperidone alone and after armodafinil pretreatment (titrated to 250 mg/day). Pharmacokinetic parameters were derived from plasma concentrations of risperidone and its active metabolite, 9-hydroxyrisperidone (formed via CYP2D6 and CYP3A4), collected before and over 4 days after risperidone administration, and from steady-state plasma concentrations of armodafinil and its circulating metabolites, R-modafinil acid and modafinil sulfone. Safety and tolerability were assessed. Thirty-six subjects receiving study drug were evaluable for safety; 34 were evaluable for pharmacokinetics. Risperidone maximum plasma concentration (C max) decreased from mean 16.5 ng/mL when given alone to 9.2 ng/mL after armodafinil pretreatment (geometric mean ratio [90 % CI] 0.55 [0.50-0.61]); area under the plasma concentration-time curve from time 0 to infinity (AUC0-∞) decreased from 92.3 to 44.5 ng·h/mL (geometric mean ratio [90 % CI] 0.51 [0.46-0.55]). C max and AUC0-∞ for 9-hydroxyrisperidone were also reduced (geometric mean ratios [90 % CI] 0.81 [0.77-0.85] and 0.73 [0.69-0.77], respectively). Adverse events were consistent with known safety profiles. Consistent with CYP3A4 induction, risperidone and 9-hydroxyrisperidone systemic exposure was reduced in the presence of armodafinil. Concomitant armodafinil and risperidone use may necessitate risperidone dosage adjustment, particularly when starting or stopping coadministration of the two drugs. However, any such decision should be based on patient disease state and clinical status.

  18. A Comparison of Risperidone and Buspirone for Treatment of Behavior Disorders in Children with Phenylketonuria

    OpenAIRE

    FAYYAZi, Afshin; Salari, Elham; Ali KHAJEH; GAJARPOUR, Abdi

    2014-01-01

    How to Cite This Article: Fayyazi A, Salari E, Khajeh A, Ghajarpour A. A Comparison of Risperidone and Buspirone for Treatment ofBehavior Disorders in Children with Phenylketonuria. Iran J Child Neurol. 2014 Autumn; 8(4):33-38.AbstractObjectiveMany patients with late-diagnosed phenylketonuria (PKU) suffer from severe behavior problems. This study compares the effects of buspirone and risperidone on reducing behavior disorders in these patients.Materials & MethodsIn this crossover clinical...

  19. DEVELOPMENT AND VALIDATION OF A BIOANALYTICAL METHOD FOR DETERMINATION OF QUETIAPINE FROM HUMAN PLASMA

    Directory of Open Access Journals (Sweden)

    Khanvilkar Vineeta V.

    2013-02-01

    Full Text Available A simple high-performance liquid chromatographic (HPLC method for the analysis of the antipsychotic drug quetiapine fumarate in human plasma has been developed. Zolpidem tartrate was employed as the internal standard (IS. Biological samples were pretreated by liquid-liquid extraction (LLE technique using tert-butyl methyl ether (TBME. Separation was performed on a HiQSil C18HS (250x4.6 mm, 5µm column. The mobile phase used was Acetonitrile-ammonium acetate buffer (pH 3.5, 10 mM (40:60 v/v pumped at a flow rate of 1 mL/min. Samples were injected by means of an autosampler via a variable loop and detected using UV detector at a wavelength of 254 nm. A good linearity was found in the concentration range of 100-2000 ng/mL. Within and between batch precision and accuracy of the proposed method were evaluated by percent relative standard deviation (% R.S.D. and percent relative error (% RE respectively; both being within the acceptable limits. The method was also validated for recovery, carry-over and stability. Freeze and thaw stability, short term stability and long term stability were evaluated for the developed bioanalytical method. The described method can be applied for quantitation of quetiapine in real clinical samples.

  20. Formulation design and optimization of orodispersible tablets of quetiapine fumarate by sublimation method

    Directory of Open Access Journals (Sweden)

    P Kalyankar

    2015-01-01

    Full Text Available The objective of present study was to formulate directly compressible orodispersible tablets of quetiapine fumarate by sublimation method with a view to enhance patient compliance. A full 3 2 factorial design was used to investigate the effect of two variables viz., concentration of Indion 414 and camphor. Indion 414 (3-5 % w/w was used as superdisintegrant and camphor (5-15 % w/w as subliming agent. The tablets were evaluated for thickness, weight variation, hardness, friability, content uniformity, wetting time, porosity, in vitro disintegration time and in vitro drug release. The formulation containing 5% w/w of Indion 414 and 5% w/w camphor was emerged as promising based on evaluation parameters. The disintegration time for optimized formulation was 18.66 s. The tablet surface was evaluated for presence of pores by scanning electron microscopy before and after sublimation. Differential scanning colorimetric study did not indicate any drug excipient incompatibility, either during mixing or after compression. The effect of independent variables on disintegration time, % drug release and friability is presented graphically by surface response plots. Short-term stability studies on the optimized formulation indicated no significant changes in drug content and in vitro disintegration time. The directly compressible orodispersible tablets of quetiapine fumarate with lower friability, greater drug release and shorter disintegration times were obtained using Indion 414 and camphor at optimum concentrations.

  1. Formulation Design and Optimization of Orodispersible Tablets of Quetiapine Fumarate by Sublimation Method.

    Science.gov (United States)

    Kalyankar, P; Panzade, P; Lahoti, S

    2015-01-01

    The objective of present study was to formulate directly compressible orodispersible tablets of quetiapine fumarate by sublimation method with a view to enhance patient compliance. A full 3(2) factorial design was used to investigate the effect of two variables viz., concentration of Indion 414 and camphor. Indion 414 (3-5 % w/w) was used as superdisintegrant and camphor (5-15 % w/w) as subliming agent. The tablets were evaluated for thickness, weight variation, hardness, friability, content uniformity, wetting time, porosity, in vitro disintegration time and in vitro drug release. The formulation containing 5% w/w of Indion 414 and 5% w/w camphor was emerged as promising based on evaluation parameters. The disintegration time for optimized formulation was 18.66 s. The tablet surface was evaluated for presence of pores by scanning electron microscopy before and after sublimation. Differential scanning colorimetric study did not indicate any drug excipient incompatibility, either during mixing or after compression. The effect of independent variables on disintegration time, % drug release and friability is presented graphically by surface response plots. Short-term stability studies on the optimized formulation indicated no significant changes in drug content and in vitro disintegration time. The directly compressible orodispersible tablets of quetiapine fumarate with lower friability, greater drug release and shorter disintegration times were obtained using Indion 414 and camphor at optimum concentrations.

  2. Use of Antipsychotics in Children Is Criticized%阻止精神病药"标签外"用途

    Institute of Scientific and Technical Information of China (English)

    Gardiner Harris; 雪梅

    2008-01-01

    @@ Risperdal (risperidone) 和 Zyprexa (olanzapine)是两种近年来十分常用的精神障碍治疗药.随着近年美国被诊断出患有双相情感障碍的儿童数量突然增加,包括上述两种抗精神病药物在内的一系列药物如Seroquel (quetiapine)、Abilify (aripiprazole)和Geodon(ziprasidone)用于儿童的处方量也迅速上升.

  3. Use of psychotropic drugs during pregnancy and breast-feeding

    DEFF Research Database (Denmark)

    Larsen, E R; Damkier, P; Pedersen, L H

    2015-01-01

    : Sertraline and citalopram are first-line treatment among selective serotonin reuptake inhibitor for depression. It is recommended to use lithium for bipolar disorders if an overall assessment finds an indication for mood-stabilizing treatment during pregnancy. Lamotrigine can be used. Valproate...... and carbamazepin are contraindicated. Olanzapine, risperidone, quetiapine and clozapine can be used for bipolar disorders and schizophrenia. CONCLUSION: It is important that health professionals treating fertile women with a psychiatric disease discuss whether psychotropic drugs are needed during pregnancy and how...

  4. Comparing Efficacy and Side Effects of Memantine vs. Risperidone in the Treatment of Autistic Disorder.

    Science.gov (United States)

    Nikvarz, Nikvarz; Alaghband-Rad, Javad; Tehrani-Doost, Mehdi; Alimadadi, Abbas; Ghaeli, Padideh

    2017-01-01

    Introduction: This study was aimed to compare the efficacy and side effects of memantine, an antagonist of the NMDA receptor of glutamate, with risperidone given the fact that glutamate has been noted for its possible effects in the pathogenesis of autism. Risperidone, an atypical antipsychotic, has been approved by FDA for the management of irritability associated with autism. Methods: 30 children, aged 4-17 years, entered an 8-week, randomized trial. Patients were randomly assigned to receive either risperidone or memantine. Autism Behavior Checklist (ABC), Childhood Autism Rating Scale (CARS), Clinical Global Impressions - Improvement (CGI-I) and Clinical Global Impression-Severity (CGI-S) scales were used to assess behavioral symptoms of the patients. Results: Both risperidone and memantine reduced the scores of 4 subscales of ABC as well as the 10-item and the total score of CARS significantly. However, differences between the 2 drugs in the scores of each evaluating scale were not found to be significant. Relatively, larger number of patients on risperidone showed "very much improvement" when assessed by CGI-I scale when compared with those on memantine. Discussion and conclusion: The present study suggests that memantine may have beneficial effects in the treatment of many core symptoms of autism. Therefore, memantine may be considered as a potential medication in the treatment of those autistic children who do not respond or cannot tolerate side effects of risperidone.

  5. In vitro-in vivo correlation of parenteral risperidone polymeric microspheres.

    Science.gov (United States)

    Shen, Jie; Choi, Stephanie; Qu, Wen; Wang, Yan; Burgess, Diane J

    2015-11-28

    The objective of the present study was to determine whether an in vitro-in vivo correlation (IVIVC) can be established for polymeric microspheres that are equivalent in formulation composition but prepared with different manufacturing processes. Risperidone was chosen as a model therapeutic and poly(lactic-co-glycolic acid) (PLGA) with similar molecular weight as that used in the commercial product Risperdal® Consta® was used to prepare risperidone microspheres. Various manufacturing processes were investigated to produce the risperidone microspheres with similar drug loading (approx. 37%) but distinctly different physicochemical properties (e.g. porosity, particle size and particle size distribution). In vitro release of the risperidone microspheres was investigated using different release testing methods (such as sample-and-separate and USP apparatus 4). In vivo pharmacokinetic profiles of the risperidone microsphere formulations following intramuscular administration were determined using a rabbit model. Furthermore, the obtained pharmacokinetic profiles were deconvoluted using the Loo-Riegelman method and the calculated in vivo release was compared with the in vitro release of these microspheres. Level A IVIVCs were established and validated for the compositionally equivalent risperidone microspheres based on the in vitro release data obtained using USP apparatus 4. The developed IVIVCs demonstrated good predictability and were robust. These results showed that the developed USP apparatus 4 method was capable of discriminating PLGA microspheres that are equivalent in formulation composition but with manufacturing differences and predicting their in vivo performance in the investigated animal model.

  6. Treatment with the antipsychotic agent, risperidone, reduces disease severity in experimental autoimmune encephalomyelitis.

    Science.gov (United States)

    O'Sullivan, David; Green, Laura; Stone, Sarrabeth; Zareie, Pirooz; Kharkrang, Marie; Fong, Dahna; Connor, Bronwen; La Flamme, Anne Camille

    2014-01-01

    Recent studies have demonstrated that atypical antipsychotic agents, which are known to antagonize dopamine D2 and serotonin 5-HT2a receptors, have immunomodulatory properties. Given the potential of these drugs to modulate the immune system both peripherally and within the central nervous system, we investigated the ability of the atypical anti-psychotic agent, risperidone, to modify disease in the animal model of multiple sclerosis (MS)4, experimental autoimune encephalomyelitis (EAE). We found that chronic oral administration of risperidone dose-dependently reduced the severity of disease and decreased both the size and number of spinal cord lesions. Furthermore, risperidone treatment substantially reduced antigen-specific interleukin (IL)-17a, IL-2, and IL-4 but not interferon (IFN)-γ production by splenocytes at peak disease and using an in vitro model, we show that treatment of macrophages with risperidone alters their ability to bias naïve T cells. Another atypical antipsychotic agent, clozapine, showed a similar ability to modify macrophages in vitro and to reduce disease in the EAE model but this effect was not due to antagonism of the type 1 or type 2 dopamine receptors alone. Finally, we found that while risperidone treatment had little effect on the in vivo activation of splenic macrophages during EAE, it significantly reduced the activation of microglia and macrophages in the central nervous system. Together these studies indicate that atypical antipsychotic agents like risperidone are effective immunomodulatory agents with the potential to treat immune-mediated diseases such as MS.

  7. Treatment of aggression with risperidone in children and adolescents with bipolar disorder: a case series.

    Science.gov (United States)

    Saxena, Kirti; Chang, Kiki; Steiner, Hans

    2006-08-01

    To evaluate the effectiveness and safety of risperidone in children and adolescents with bipolar disorder characterized by aggression and mania, despite treatment with mood stabilizers. A retrospective chart review of patients seen in an outpatient pediatric mood disorders clinic over an 18-month period was performed. Data were extracted from charts of patients who had a diagnosis of bipolar disorder with aggression that was uncontrolled on a mood stabilizer; as a result, these patients had risperidone added to their regimen. Four boys (aged 7-15 years) and two girls (aged 8 and 14 years) were treated with risperidone (mean dosage, 0.85 mg/day) for 3-16 months. Aggressive behavior improved in all patients after risperidone was started and remained improved for the duration of follow-up. Other symptoms of mania also improved. Risperidone was generally well tolerated. Sedation and akathisia were reported in one patient. The addition of risperidone to a mood stabilizer may improve aggression and other symptoms of mania in pediatric patients with bipolar disorder who do not respond adequately to a mood stabilizer alone. The long-term efficacy and safety of this regimen should be evaluated in a controlled clinical trial.

  8. Galactorrhea - side effect of risperidone in combination with depakine chrono in a patient with bipolar disorder.

    Science.gov (United States)

    Peitl, Marija Vucić; Peitl, Vjekoslav; Grahovac, Tanja; Pavlović, Eudard

    2010-03-01

    Risperidone, as all atypical antipsychotics, can cause hyperprolactinemia which can in turn lead to galactorrhea. Mood stabilizers, one of which is valproic acid and its derivate "Depakine Chrono", are rarely linked with symptomatic hyperprolactinemia and do not alter prolactin concentrations. This case is based around a patient suffering from a bipolar disorder that has been psychiatrically treated in an outpatient clinic during four years. Bipolar disorder treatment was started with carbamazepine, but later it was discontinued due to adverse events and extreme increase of liver transaminases. Treatment was continued with introduction of lithium, but the patient stated that she could not tolerate it. Subsequently, her endocrinologist advised for lithium discontinuation due to very severe osteoporosis. At the beginning of 2009, lithium was discontinued and Depakine Chrono was introduced. Due to patient's psychotic decompensation it was necessary to introduce risperidone into treatment and soon afterwards her psychotic symptoms settled. After several months of treatment her mood lowered, she began to feel sedated, psychomotorically retarded and that lead to dose lowering of Depakine Chrono and risperidone, at which point galactorrhea as a serious adverse event occurred. Occurrence of galactorrhea at lower risperidone doses in this case might be partially explained by recent studies that showed that lower doses of risperidone can also improve psychic state, but could also cause adverse events. Although galactorrhea, as a direct consequence of hyperprolactinemia caused by risperidone has mainly been researched with higher doses of this atypical antipsychotic, we have to keep in mind that lower doses could also cause serious adverse events.

  9. Early onset of treatment effects with oral risperidone

    Directory of Open Access Journals (Sweden)

    Naber Dieter

    2007-01-01

    Full Text Available Abstract Background The dogma of a delayed onset of antipsychotic treatment effects has been maintained over the past decades. However, recent studies have challenged this concept. We therefore performed an analysis of the onset of antipsychotic treatment effects in a sample of acutely decompensated patients with schizophrenia. Methods In this observational study, 48 inpatients with acutely decompensated schizophrenia were offered antipsychotic treatment with oral risperidone. PANSS-ratings were obtained on day 0, day 1, day 3, day 7 and day 14. Results Significant effects of treatment were already present on day 1 and continued throughout the study. The PANSS positive subscore and the PANSS total score improved significantly more than the PANSS negative subscore. Conclusion Our results are consistent with the growing number of studies suggesting an early onset of antipsychotic treatment effects. However, non-pharmacological effects of treatment also need to be taken into consideration.

  10. Is quetiapine suitable for treatment of acute schizophrenia with catatonic stupor? A case series of 39 patients

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    Yoshimura B

    2013-10-01

    Full Text Available Bunta Yoshimura,1,2 Tomoya Hirota,3 Manabu Takaki,2 Yoshiki Kishi,11Department of Psychiatry, Okayama Psychiatric Medical Center, 2Department of Neuropsychiatry, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, Japan; 3Department of Psychiatry, Vanderbilt University Medical Center, Nashville, TN, USAPurpose: We aimed to determine which antipsychotic is most effective for the treatment of acute schizophrenia with catatonic stupor.Patients and methods: Data were obtained from the medical records of 450 patients with the diagnosis of schizophrenia, who had received acute psychiatric inpatient treatment between January 2008 and December 2010 at our hospital. Among them, 39 patients (8.7% met the definition of catatonic stupor during hospitalization. The diagnoses of schizophrenia in all 39 patients were reconfirmed during the maintenance phase. We retrospectively reviewed the medical records of these 39 patients to investigate which antipsychotics were chosen for treatment during the period from admission to recovery from catatonia, at the time of discharge, and 12 and 30 months after discharge.Results: As compared to other antipsychotics, it was found out that use of quetiapine had better outcomes and hence was used more often. A total of 61.5% of patients were on quetiapine at the time of recovery from catatonia and 51.3% of patients were on quetiapine at the time of discharge as compared to only 17.9% of patients on quetiapine on admission. However, at 12 and 30 months after discharge, the rates had decreased to 38.4% and 25.6%. Similarly, of 29 patients who were not administered electroconvulsive therapy, quetiapine was used at significantly higher rates at the time of recovery from catatonia (48.3% than at the time of admission (17.2%. All 39 patients had received an antipsychotic as the first-line treatment and some antipsychotics might have contributed to the development of catatonia

  11. Quetiapine fumarate augmentation for patients with a primary anxiety disorder or a mood disorder: a pilot study

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    Chen Yi-Chih

    2012-09-01

    Full Text Available Abstract Background Comorbid anxiety symptoms,in patients with a primary anxiety disorder or a mood disorder, leads to poor patient outcomes and burdens the healthcare system. This pilot study evaluated the feasibility of extended-release quetiapine fumarate (quetiapine XR for the treatment of patients with either a primary anxiety disorder or a mood disorder with comorbid anxiety symptoms compared to a placebo, as an adjunct to antidepressant therapy. Methods Thirty-nine patients with a diagnosis of a primary anxiety disorder or a mood disorder with comorbid anxiety symptoms were enrolled in this study. Patients with a stable dose of antidepressant therapy were randomized according to a 2:1 probability of receiving either quetiapine XR or a placebo adjunctive treatment for 8 weeks. The efficacy was assessed by the Hamilton Anxiety Rating Scale (HAM-A and the Clinical Global Impression of severity (CGI-S score at baseline, week 1, 4, and 8. Results A total of 35 patients were included in this intention-to treat (ITT population for the efficacy analysis (quetiapine XR: 22 patients; placebo: 13 patients. At week 4, statistically significant differences were observed on both the HAM-A score (p = 0.003 and the CGI-S score (p = 0.025, favouring the quetiapine XR (−13.00 ± 4.14 compared to placebo (−6.63 ± 5.42. However, no statistically significant difference was observed between the two groups with regard to changes from the baseline to week 8 on the HAM-A score (p = 0.332 or the CGI-S score (p = 0.833. Conclusions Augmentation of antidepressant treatment with quetiapine XR did not result in clinical improvement according to the outcome measure of anxiety using the HAM-A and CGI-S scores at week 8, among the patients with either a primary anxiety disorder or a mood disorder with comorbid anxiety symptoms. However, treatment with quetiapine XR as an adjunct to antidepressant therapy appeared to provide a short

  12. Olanzapine induced biochemical and histopathological changes after its chronic administration in rats

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    Rehmat Shah

    2016-11-01

    Full Text Available Objective: Olanzapine is a second generation antipsychotic acting mainly as a dopamine D2 and serotonine 5-HT2 receptors antagonist prescribed in the treatment of schizophrenia and various other psychiatric illnesses. Even though olanzapine is widely used in psychiatry, its effects on the architecture of pancreas, liver and kidneys are little known. The histology of pancreas especially has never been studied. For these reasons, the current study was designed to elucidate the toxic effects of chronic administration of olanzapine on pancreas, liver and kidneys and the enzymes released by these tissues in an escalating dose manner. Methods: Fourteen male rats were divided into two groups equally, the olanzapine group and the controls. Olanzapine was administered in a dose of 5 mg/kg/d for the first eight weeks, 10 mg/kg/d for next four weeks and 15 mg/kg/d through the last two week period of 14 weeks experiment. The controls received acidified saline only. Both the groups received restricted diet (20 g/12 h. The body weight and level of random blood sugar (RBS were measured on a weekly basis. The levels of lipase, amylase, alanine transaminase (ALT and aspartate transaminase (AST were determined terminally. At the end of the experiment, the tissues were dissected out for histopathological evaluation. Results: Significant loss in body weight, change in the level of random blood sugar (∗∗P  0.05. The pancreas has shown derangement of beta cells and fibrotic growth. A mild to moderate focal increase in glomerular cellularity, cellular proliferation and glomerular capsules with negligible basement membranes were observed in the kidneys. No changes were observed in the architecture of the liver. Conclusion: The findings of this study indicated that the incidence of adverse effects associated with olanzapine could be prevented/alleviated/delayed by allowing restricted diet.

  13. RNA sequencing reveals a slow to fast muscle fiber type transition after olanzapine infusion in rats.

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    Christopher J Lynch

    Full Text Available Second generation antipsychotics (SGAs, like olanzapine, exhibit acute metabolic side effects leading to metabolic inflexibility, hyperglycemia, adiposity and diabetes. Understanding how SGAs affect the skeletal muscle transcriptome could elucidate approaches for mitigating these side effects. Male Sprague-Dawley rats were infused intravenously with vehicle or olanzapine for 24h using a dose leading to a mild hyperglycemia. RNA-Seq was performed on gastrocnemius muscle, followed by alignment of the data with the Rat Genome Assembly 5.0. Olanzapine altered expression of 1347 out of 26407 genes. Genes encoding skeletal muscle fiber-type specific sarcomeric, ion channel, glycolytic, O2- and Ca2+-handling, TCA cycle, vascularization and lipid oxidation proteins and pathways, along with NADH shuttles and LDH isoforms were affected. Bioinformatics analyses indicate that olanzapine decreased the expression of slower and more oxidative fiber type genes (e.g., type 1, while up regulating those for the most glycolytic and least metabolically flexible, fast twitch fiber type, IIb. Protein turnover genes, necessary to bring about transition, were also up regulated. Potential upstream regulators were also identified. Olanzapine appears to be rapidly affecting the muscle transcriptome to bring about a change to a fast-glycolytic fiber type. Such fiber types are more susceptible than slow muscle to atrophy, and such transitions are observed in chronic metabolic diseases. Thus these effects could contribute to the altered body composition and metabolic disease olanzapine causes. A potential interventional strategy is implicated because aerobic exercise, in contrast to resistance exercise, can oppose such slow to fast fiber transitions.

  14. Efficacy, tolerability and cost effectiveness of zotepine versus olanzapine in patients of acute schizophrenia

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    Saroj Kothari

    2013-10-01

    Full Text Available Background: Schizophrenia is a functional psychosis with severe personality changes and thought disorders without cerebral damage. No reports are available in literature regarding efficacy and tolerability of atypical antipsychotic drug zotepine over olanzapine a preferred drug worldwide for the treatment of schizophrenia. Therefore, present study is undertaken to evaluate efficacy, tolerability and cost effectiveness of zotepine over olanzapine in patients suffering from schizophrenia. Methods: A prospective, randomized, single blind, parallel, 6 weeks clinical study was conducted on a total of 112 patients, of schizophrenia attending psychiatry outpatient department at G. R. Medical College, Gwalior, India randomized into two groups (56 in each. Patients received either olanzapine (10-20mg or zotepine (75-150mg per day for a period of 6 week. Efficacy was measured by Positive and Negative Syndrome Scale (PANSS and Clinical Global Impression (CGI scale whereas tolerability was measured by dropout rate and frequency of adverse effects. Cost effectiveness was calculated in terms of cost incurred for improvement at the end of treatment period. Results: Both the drugs showed significant (P.0.05. Olanzapine showed significantly better (P0.05 between the two groups. Incidence of akathisia and drop out (16% and 23% with zotepine were significant (P<0.05 as compared to olanzapine (2% and 11% respectively. Conclusions: Though the efficacy of both the drugs is comparable, olanzapine appears to have better tolerability and cost effectiveness than zotepine in patients of schizophrenia. [Int J Basic Clin Pharmacol 2013; 2(5.000: 577-582

  15. Olanzapine as an antiemetic in refractory nausea and vomiting in advanced cancer.

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    Srivastava, Manish; Brito-Dellan, Norman; Davis, Mellar P; Leach, Marie; Lagman, Ruth

    2003-06-01

    Nausea and vomiting are difficult symptoms to manage in patients with advanced cancer. Several classes of antiemetics are available, including phenothiazines, butyrophenones, substituted benzamides and selective serotonin antagonists, as well as corticosteroids. Most patients will respond to either single agents or combinations that frequently include corticosteroids. A minority of patients will have nausea that fails to respond. The atypical antipsychotic, olanzapine, relieves nausea in some patients failing to respond to the usual antiemetics. Two case reports are presented and the rationale for olanzapine's benefit is discussed.

  16. [3-D ultrasound-assisted gait analysis of schizophrenic patients. Comparison between conventional neuroleptics and olanzapine].

    Science.gov (United States)

    Putzhammer, Albert; Heindl, Bernhard; Müller, Jürgen; Broll, Karin; Pfeiff, Liane; Perfahl, Maria; Hess, Linda; Koch, Horst

    2003-05-01

    Schizophrenic disorders as well as neuroleptic treatment can affect locomotion. The study assessed the influence of neuroleptic treatment on human gait via ultrasonic topometric gait analysis. In a control sample the test system proved high test-retest-reliability. Spatial and temporal gait parameters were assessed in schizophrenic patients without neuroleptic treatment (n = 12) and under treatment with conventional neuroleptics (n = 14) and re-assessed after treatment change to the atypical neuroleptic olanzapine in a repeated measures design. After switch from conventional neuroleptics to olanzapine patients showed an increase of gait velocity (p step length (p gait analysis.

  17. Adverse events in children and adolescents treated with quetiapine: an analysis of adverse drug reaction reports from the Danish Medicines Agency database.

    Science.gov (United States)

    Jakobsen, Klaus D; Wallach-Kildemoes, Helle; Bruhn, Christina H; Hashemi, Nasseh; Pagsberg, Anne K; Fink-Jensen, Anders; Nielsen, Jimmi

    2017-03-01

    Quetiapine is a low-affinity dopamine D2 receptor antagonist, approved for the treatment of bipolar disorder and schizophrenia in children and adolescents by the Food and Drug Administration, but not by European Medicine Agency. Although knowledge of adverse drug reactions in children and adolescents is scarce, quetiapine is increasingly being used for youth in Denmark. The aim of this case study is to discuss adverse drug events (ADEs) spontaneously reported to the Danish Medicines Agency on quetiapine used in the pediatric population in relation to adversive drug reactions (ADRs) reported in the European Summary of Product Characteristics (SPCs). The ADE report database at Danish Medicines Agency was searched for all quetiapine ADRs involving individuals (children and adolescents gives rise to safety concerns.

  18. A Randomized Open Label Comparison of the Effects ofRisperidone and Haloperidol on Sexual Function

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    S. Jaber Mousavi

    2009-12-01

    Full Text Available "n Objective: "nSexual dysfunction in patients who take antipsychotics causes adecline in their quality of life and medication acceptance. Considering the restrictions in cross sectional design of many earlier researches, we used a clinical trial aimed at assessing sexual dysfunction by substituting Risperidone, an atypical antipsychotic drug, with Haloperidol, a typical one . "n "n "nMethod: This clinical trial was conducted on 51 patients who had been using Risperidone with a minimum dose of 2 mg/daily for at least 2 months. The patients were randomly divided into 2 groups. The first group continued taking Risperidone, whereas the second group was given Haloperidol. Sexual function prior to and after the drug substitution was assessed using a sexual questionnaire designed to assess four stages of sexual function . "nResults: Compared to those who changed their medication to Haloperidol, the patients who remained on Risperidone therapy suffered from more sexual dysfunction, especially in their tendency towards having sexual activities (P= 0.01, post menstrual sexual activity (P= 0.002, and reaching orgasm in their sexual activities (P= 0.04; however in the Haloperidol group, no significant difference was observed before and after the change in medication . "nConclusion: Although Risperidone and Haloperidol can both disturb patients'sexual function, the side effects of Risperidone are stronger. Hence toprevent the decline of medication acceptance or irregular consumption by patients which may lead to possible relapse, substitution of Risperidone withanother drug with fewer side effects on sexual activities is definitely to the advantage of the patients .

  19. CYP2D6 polymorphisms and their influence on risperidone treatment

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    Puangpetch A

    2016-12-01

    Full Text Available Apichaya Puangpetch,1 Natchaya Vanwong,1 Nopphadol Nuntamool,2 Yaowaluck Hongkaew,1 Monpat Chamnanphon,1 Chonlaphat Sukasem1 1Division of Pharmacogenomics and Personalized Medicine, Department of Pathology, Faculty of Medicine Ramathibodi Hospital, 2Molecular Medicine, Faculty of Science, Mahidol University, Bangkok, Thailand Abstract: Cytochrome P450 enzyme especially CYP2D6 plays a major role in biotransformation. The interindividual variations of treatment response and toxicity are influenced by the polymorphisms of this enzyme. This review emphasizes the effect of CYP2D6 polymorphisms in risperidone treatment in terms of basic knowledge, pharmacogenetics, effectiveness, adverse events, and clinical practice. Although the previous studies showed different results, the effective responses in risperidone treatment depend on the CYP2D6 polymorphisms. Several studies suggested that CYP2D6 polymorphisms were associated with plasma concentration of risperidone, 9-hydroxyrisperidone, and active moiety but did not impact on clinical outcomes. In addition, CYP2D6 poor metabolizer showed more serious adverse events such as weight gain and prolactin than other predicted phenotype groups. The knowledge of pharmacogenomics of CYP2D6 in risperidone treatment is increasing, and it can be used for the development of personalized medication in term of genetic-based dose recommendation. Moreover, the effects of many factors in risperidone treatment are still being investigated. Both the CYP2D6 genotyping and therapeutic drug monitoring are the important steps to complement the genetic-based risperidone treatment. Keywords: CYP2D6, risperidone, polymorphisms, adverse drug reaction, pharmacogenetics, pharmacokinetics, pharmacodynamics

  20. 多次利培酮治疗致抗精神病药恶性综合征%Neuroleptic malignant syndrome after repeated treatment with risperidone

    Institute of Scientific and Technical Information of China (English)

    丁跃庆; 李华; 谢振强; 张伟娟; 代俊; 孔君; 吴洪军

    2012-01-01

    1例31岁女性患者因精神分裂症给予利培酮1 mg,2次/d口服,1周后剂量增至2 mg,2次/d.此前患者曾3次间断应用利培酮治疗.本次治疗规律服药49 d,患者精神症状缓解.第50~52天未遵医嘱规律服药.第54天患者出现大汗淋漓,体温达38.5 ℃.第55天出现意识障碍、心动过速、双上肢肌强直、肌张力增高.心电图示窦性心动过速.实验室检查示:白细胞计数12.3×109/L,胆碱酯酶 13 268 U /L,肌酸激酶 1447 U/L,利培酮血液浓度70.5 μg/L.诊断为抗精神病药恶性综合征(NMS).立即停用利培酮,进行物理降温、补液、抗心律失常、抗感染、纠正酸碱平衡、护肝等治疗.6 d后患者体温恢复正常,NMS症状消失.换用奥氮平治疗后,未再出现类似症状.%A 31-year-old woman with schizophrenia received risperidone 1 mg twice daily. One week later, the dose was increased to 2 mg twice daily. The patient had previously received risperidone intermittent treatment for three times. After a 49-day regular treatment, the psychiatric symptoms relieved. On days 50 to 52, she did not adhere to the instructions of the physician for regular use of the drug. On day 54, the patient experienced profuse sweating with a temperature of 38. 5 ℃. On day 55, she developed disturbance of consciousness, tachycardia, muscle rigidity of the upper limbs, and hypermyotonia. Her electrocardiograph showed sinus tachycardia. Laboratory tests showed the following findings: white blood cell count 12. 3 × 109/L, cholinesterase 13 268 U/L, creatine kinase 1447 U/L. The blood concentrations of risperidone was 70. 5 μg/L. Neuroleptic malignant syndrome ( NMS ) was diagnosed. The medication was stopped immediately. Physical methods for lowering body temperature, fluid supplement, antiarrhythmics, anti-infective therapy, correction of the acid-base imbalance, and liver-protective treatment were given. Six days later, the temperature returned to normal, the NMS symptoms

  1. Quetiapine-induced Priapism Requiring Frequent Emergency Admissions: A Case Report

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    Jon C. Jackson

    2015-01-01

    Full Text Available Priapism, a rare but well-known adverse reaction of first and second generation anti-psychotics, has been hypothesized to be associated with blockade of alpha 1 receptors. However, genetic abnormalities or heritability of affected cytochrome P450 alleles has not been ruled out as a causal mechanism. A case is presented with three episodes of priapism within 17 days while taking standard FDA (Food and Drug Administration approved doses of quetiapine. Cytochrome P450 3A4 genotype testing was performed and resulted with normal enzymatic activity. This case further eliminates enzymatic metabolism as a possible cause of priapism, thus strengthening the alpha one receptor blockade hypothesis.

  2. The metabolic effects of olanzapine and topiramate in rats and humans

    NARCIS (Netherlands)

    Evers, S.S.; van Dijk, G.; van Vliet, A.; Scheurink, A.J.W.

    2011-01-01

    In humans the anti-psychotic Olanzapine (OLZ) has negative side effects on metabolism: it causes weight gain and increases the risk of developing type 2 Diabetes. The anti-convulsant Topiramate (TPM) has the opposite effects: it reduces body weight and improves insulin sensitivity. Because of this,

  3. Open-label study of olanzapine in children with pervasive developmental disorder.

    NARCIS (Netherlands)

    Kemner, C.; Swinkels, S.H.N.; Jonge, M.J.A. de; Tuynman-Qua, H.G.; Engeland, H.M. van

    2002-01-01

    The effects of olanzapine on the symptomatology of children with pervasive developmental disorder with emphasis on problems of communication and the safety of the drug were investigated in a 3-month open-label, open-dosage study. Participating in the study were 25 children age 6 to 16 years with a d

  4. Microtitrimetric determination of a drug content of pharmaceuticals containing olanzapine in non-aqueous medium

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    KANAKAPURA BASAVAIAH

    2009-05-01

    Full Text Available Two simple, rapid, reliable and cost-effective methods based on titrimetry in non-aqueous medium are described for the determination of olanzapine in pharmaceuticals. In these methods, the drug dissolved in the glacial acetic acid was titrated with the acetous perchloric acid with visual and potentiometric end point detection, crystal violet being used as the indicator for visual titration. The methods are applicable over 1-15 mg range of olanzapine. The procedures were applied to determine olanzapine in pharmaceutical products and the results were found to be in a good agreement with those obtained by the reference method. Associated pharmaceutical materials did not interfere. The precision results, expressed by inter-day and intra-day relative standard deviation values, were satisfactory, higher than 2%. The accuracy was satisfactory as well. The methods proved to be suitable for the analysis of olanzapine in bulk drug and in tablets. The accuracy and reliability of the methods were further ascertained by recovery studies via a standard addition technique with percent recoveries in the range 97.51-103.7% with a standard deviation of less than 2%.

  5. The stress stability of olanzapine: studies of interactions with excipients in solid state pharmaceutical formulations.

    Science.gov (United States)

    Djordjević Filijović, Nataša; Antonijević, Milan D; Pavlović, Aleksandar; Vučković, Ivan; Nikolić, Katarina; Agbaba, Danica

    2015-03-01

    Stress stability testing represents an important part of the drug development process. It is used as an important tool for the identification of degradation products and degradation pathways, as well as for the assessment of changes in physical form of drug molecules. The impact of excipients on the stability of olanzapine confirms that levels of impurities and degradants are limiting parameters and are therefore used for stability evaluation. The major degradation product of olanzapine was identified as 2-methyl-5,10-dihydro-4H-thieno[2,3-b][1,5]benzodiazepine-4-one (III). The structure of III was determined by using LC-MS, IR and NMR. Compatibility and stress stability results demonstrated that tablet formulations of olanzapine are sensitive to temperature and moisture. In samples protected from moisture, the increase in concentration of III was shown to be highly temperature dependent and the degradation followed zero-order kinetics. In addition, studies of olanzapine with excipients and in formulated tablets revealed polymorphic phase changes in some samples, influenced by a combination of stress temperature and humidity conditions. Polymorphic transitions were monitored using x-ray powder diffraction (XRPD) analysis and exhibited no correlation between the phase change (appearance of a new polymorph) and the degradation process.

  6. Olanzapine-induced Fos expression in the rat forebrain; cross-tolerance with haloperidol and clozapine

    NARCIS (Netherlands)

    Sebens, JB; Koch, T; Ter Horst, GJ; Korf, J

    1998-01-01

    Acute administration of the atypical antipsychotic drug olanzapine (5 mg kg(-1) i.p.) increased the number of Fos-positive cells moderately in the prefrontal cortex and the striatum; more pronounced were the effects in the nucleus accumbens, the lateral septum, the hypothalamic paraventricular nucle

  7. Olanzapine-Induced Mania in Bipolar Spectrum Disorder:A Case Report

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    Mehrdad Eftekhar

    2006-07-01

    Full Text Available Objective: To report the case of a 46-year old male with major depressive disorder, who represented manic symptoms, when olanzapine was added to his treatment. Method: A 46-year old female, with a diagnosis of treatment resistant depression was referred to the authors. He had past history of depression for more than 20 years. The symptoms were present nearly every day since 1981, without any distinct period of remission, nor any noticeable fluctuation. His irritability had been disruptive to his family all these years. His doctor had prescribed maprotiline 25 mg/day, and lorazepam, 2mg/day, in addition to fluoxetine for the last 5 months. He is also a father of two children with methylphenidateresistant and sodium valproate-responsive attention-deficit hyperactivity disorder. Considering the antidepressant effects of olanzapine and its positive effects on irritability, the authors added olanzapine, to the patient’s previous medications. Results: After one week, he showed new problems such as talkativeness and beginning to smoke for the first time in his life, elevated mood, grandiosity about his intelligence and abilities, talkativeness, and shopping sprees. The score on the mania rating scale was 14. Fluoxetine was discontinued and sodium valproate, were prescribed. It took around 2 months to completely control the manic symptoms. Conclusions: In the patients with depression who show bipolar spectrum disorder features, adding mood stabilizers may be preferred to the drugs as olanzapine which could induce mania.

  8. Olanzapine-induced weight gain: lessons learned from developing rat models

    NARCIS (Netherlands)

    van der Zwaal, E.M.

    2011-01-01

    Olanzapine is an effective and commonly prescribed antipsychotic drug, used for the treatment of schizophrenia and bipolar disorder. Unfortunately significant weight gain is a common side effect. In order to effectively address this side effect, it is crucial to gain insight into the underlying mech

  9. Olanzapine orally-disintegrating tablet in severe psychotic agitation: a naturalistic study.

    Science.gov (United States)

    Pascual, J C; Pérez, V; Martín, J L R; Safont, G; Puigdemont, D; Alvarez, E

    2007-01-01

    This study was conducted to determine effectiveness and safety of olanzapine in patients with severe agitation. A naturalistic, open-label study in 80 acutely agitated psychotic patients visited in our psychiatric emergency department. Patients received either a 20-mg olanzapine orally-disintegrating tablet or conventional treatment depending on attending psychiatrist's preference. Efficacy was assessed by the Excitement Component of the Positive and Negative Syndrome Scale (PANSS-EC), the Agitation-Calmness Evaluation Scale (ACES) and pragmatic variables (second pharmacological intervention and need for physical restraints). 60 % patients completed a 6 hour trial. Both groups showed a significant reduction in mean PANSS-EC score. The olanzapine-treated group showed statistically significant improvements: PANSS-EC (F=122.9; df=2.4; p=0.000), ACES (F=68.2; df=2.8; p=0.000). Treatment was well-tolerated and no serious side-effects were observed. In this naturalistic study in patients with severe agitation, 20-mg oral olanzapine was effective, rapid and safe.

  10. Influence of olanzapine on QT variability and complexity measures of heart rate in patients with schizophrenia.

    Science.gov (United States)

    Bär, Karl-Jürgen; Koschke, Mandy; Berger, Sandy; Schulz, Steffen; Tancer, Manuel; Voss, Andreas; Yeragani, Vikram K

    2008-12-01

    Previous studies have shown that untreated patients with acute schizophrenia present with reduced heart rate variability and complexity as well as increased QT variability. This autonomic dysregulation might contribute to increased cardiac morbidity and mortality in these patients. However, the additional effects of newer antipsychotics on autonomic dysfunction have not been investigated, applying these new cardiac parameters to gain information about the regulation at sinus node level as well as the susceptibility to arrhythmias. We have investigated 15 patients with acute schizophrenia before and after established olanzapine treatment and compared them with matched controls. New nonlinear parameters (approximate entropy, compression entropy, fractal dimension) of heart rate variability and also the QT-variability index were calculated. In accordance with previous results, we have observed reduced complexity of heart rate regulation in untreated patients. Furthermore, the QT-variability index was significantly increased in unmedicated patients, indicating increased repolarization lability. Reduction of the heart rate regulation complexity after olanzapine treatment was seen, as measured by compression entropy of heart rate. No change in QT variability was observed after treatment. This study shows that unmedicated patients with acute schizophrenia experience autonomic dysfunction. Olanzapine treatment seems to have very little additional impact in regard to the QT variability. However, the decrease in heart rate complexity after olanzapine treatment suggests decreased cardiac vagal function, which may increase the risk for cardiac mortality. Further studies are warranted to gain more insight into cardiac regulation in schizophrenia and the effect of novel antipsychotics.

  11. Role of Polymeric Excipients in the Stabilization of Olanzapine when Exposed to Aqueous Environments

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    Maria Paisana

    2015-12-01

    Full Text Available Hydrate formation is a phase transition which can occur during manufacturing processes involving water. This work considers the prevention of hydration of anhydrous olanzapine and hydrate conversions in the presence of water and polymers (polyethyleneglycol; hydroxypropylcellulose; polyvinylpyrrolidone in forming pellets by wet extrusion and spheronisation. Anhydrous olanzapine was added to water with or without those polymers prior to extrusion with microcrystalline cellulose. Assessment of olanzapine conversion was made by XRP-Diffraction; FTIR spectroscopy; calorimetry (DSC and microscopy (SEM for crystal size and shape. The addition of water converted the anhydrous form into dihydrate B and higher hydrate; whereas polyethyleneglycol promoted a selective hydrate conversion into the higher hydrate olanzapine form. Both polyvinylpyrrolidone and hydroxypropylcellulose prevented the hydrate transformations of the anhydrous drug; the latter even in the presence of hydrate seeds. This may be explained by the higher H-bond ability; higher network association and higher hydrophobicity of hydroxypropylcellulose by comparison with polyethyleneglycol and polyvinylpyrrolidone; which could contribute to its higher affinity to the crystal surfaces of the hydrate nuclei/initial crystals and promoting steric hindrance to the incorporation of other drug molecules into the crystal lattice; thus, preventing the crystal growth. The addition of microcrystalline cellulose needed for the pellets production (final product did not eliminate the protector effect of both hydroxypropylcellulose and polyvinylpyrrolidone during pellets’ processing and dissolution evaluation.

  12. Open-label study of olanzapine in children with pervasive developmental disorder.

    NARCIS (Netherlands)

    Kemner, C.; Swinkels, S.H.N.; Jonge, M.J.A. de; Tuynman-Qua, H.G.; Engeland, H.M. van

    2002-01-01

    The effects of olanzapine on the symptomatology of children with pervasive developmental disorder with emphasis on problems of communication and the safety of the drug were investigated in a 3-month open-label, open-dosage study. Participating in the study were 25 children age 6 to 16 years with a

  13. Olanzapine-induced weight gain: lessons learned from developing rat models

    NARCIS (Netherlands)

    van der Zwaal, E.M.

    2011-01-01

    Olanzapine is an effective and commonly prescribed antipsychotic drug, used for the treatment of schizophrenia and bipolar disorder. Unfortunately significant weight gain is a common side effect. In order to effectively address this side effect, it is crucial to gain insight into the underlying

  14. The role of hypothalamic pathways in the metabolic side effects of Olanzapine

    NARCIS (Netherlands)

    Girault, E.M.

    2013-01-01

    Atypical antipsychotic drugs such as Olanzapine (Ola) induce weight gain and metabolic changes associated with the development of type 2 diabetes. The mechanisms underlying these undesired side effects are currently unknown. In this thesis, we showed that both acute and chronic administration of Ola

  15. Quetiapine attenuates cognitive impairment and decreases seizure susceptibility possibly through promoting myelin development in a rat model of malformations of cortical development.

    Science.gov (United States)

    Ma, Lei; Yang, Feng; Zhao, Rui; Li, Li; Kang, Xiaogang; Xiao, Lan; Jiang, Wen

    2015-10-05

    Developmental delay, cognitive impairment, and refractory epilepsy are the most frequent consequences found in patients suffering from malformations of cortical development (MCD). However, therapeutic options for these psychiatric and neurological comorbidities are currently limited. The development of white matter undergoes dramatic changes during postnatal brain maturation, thus myelination deficits resulting from MCD contribute to its comorbid diseases. Consequently, drugs specifically targeting white matter are a promising therapeutic option for the treatment of MCD. We have used an in utero irradiation rat model of MCD to investigate the effects of postnatal quetiapine treatment on brain myelination as well as neuropsychological and cognitive performances and seizure susceptibility. Fatally irradiated rats were treated with quetiapine (10mg/kg, i.p.) or saline once daily from postnatal day 0 (P0) to P30. We found that postnatal administration of quetiapine attenuated object recognition memory impairment and improved long-term spatial memory in the irradiated rats. Quetiapine treatment also reduced the susceptibility and severity of pentylenetetrazol-induced seizures. Importantly, quetiapine treatment resulted in an inhibition of irradiation-induced myelin breakdown in the cerebral cortex and corpus callosum. These findings suggest that quetiapine may have beneficial, postnatal effects in the irradiated rats, strongly suggesting that improving MCD-derived white matter pathology is a possible underlying mechanism. Collectively, these results indicate that brain myelination represents an encouraging pharmacological target to improve the prognosis of patients with MCD. Copyright © 2015 Elsevier B.V. All rights reserved.

  16. An open-label pilot study of quetiapine plus mirtazapine for heavy drinkers with alcohol use disorder.

    Science.gov (United States)

    Brunette, Mary F; Akerman, Sarah C; Dawson, Ree; O'Keefe, Christopher D; Green, Alan I

    2016-06-01

    Animal research suggests that medications that produce a weak dopamine D2 receptor blockade and potentiate noradrenergic activity may decrease alcohol drinking. In an open-label pilot study of subjects with alcohol dependence, we tested whether the combination of quetiapine, a weak dopamine D2 receptor antagonist, whose primary metabolite, desalkylquetiapine, is a norepinephrine reuptake inhibitor, and mirtazapine, a potent α2 norepinephrine receptor antagonist, would decrease alcohol drinking and craving. Twenty very heavy drinkers with alcohol dependence entered a trial of 8 weeks of treatment with quetiapine followed by 8 weeks of treatment with a combination of quetiapine plus mirtazapine. Alcohol use was assessed weekly with a Timeline Follow-Back interview and craving with the Penn Alcohol Craving Scale. Among the 11 completers, subjects reported improved outcomes in the quetiapine plus mirtazapine period compared to the quetiapine alone period: fewer very heavy drinking days per week (1.3 [SD = 2.4] vs. 2.1 [SD = 2.8]; t = 2.3, df = 10, p = 0.04); fewer total number of drinks per week (39.7 [SD = 61.6] vs. 53.4 [SD = 65.0]; t = 2.8, df = 10, p = 0.02); and lower craving scores (2.5 [SD = 1.4] vs. 3.2 [SD = 1.2]; t = 2.4, df = 10, p = 0.04). All subjects reported at least one adverse event; 72.7% reported somnolence. In this open-label pilot study, treatment with quetiapine plus mirtazapine was associated with a decrease in alcohol drinking and craving. These findings are consistent with our previous work in animal models of alcohol use disorders and suggest that further study of medications or combinations of medications with this pharmacologic profile is warranted.

  17. Combination treatment with risperidone long-acting injection and psychoeducational approaches for preventing relapse in schizophrenia

    Directory of Open Access Journals (Sweden)

    Zhao Y

    2013-10-01

    Full Text Available Yueren Zhao,1–3 Taro Kishi,1 Nakao Iwata,1 Manabu Ikeda3,4 1Department of Psychiatry, Fujita Health University School of Medicine, Toyoake, Aichi, Japan; 2Department of Psychiatry, Okehazama Hospital Fujita Kokoro Care Center, Toyoake, Aichi, Japan; 3Department of Neuropsychiatry, Graduate School of Medical Sciences, Kumamoto University, Kumamoto, Kumamoto, Japan; 4Department of Neuropsychiatry, Faculty of Life Sciences, Kumamoto University, Kumamoto, Kumamoto, Japan Abstract: A recent meta-analysis showed that long-acting injectable (LAI antipsychotics were not superior to oral antipsychotics for preventing relapse in patients with schizophrenia. We therefore designed a treatment strategy combining risperidone LAI and COMPASS (COMprehensive Psycho-educational Approach and Scheme Set, an original psychoeducational program supporting treatment with risperidone LAI and evaluating subjective treatment satisfaction, transition of symptoms, and effectiveness in preventing symptomatic relapse. The aim of this study was to examine whether addition of COMPASS to risperidone LAI was more effective in preventing relapse in schizophrenia patients than risperidone LAI alone, with the latter group consisting of patients enrolled in a Phase III trial of risperidone LAI in Japan. Patients were followed up for 6 months, with COMPASS continuously implemented from the transition to the observation phase. The primary efficacy measurements were relapse rate (rates of rehospitalization and discontinuation due to inefficacy. Secondary efficacy measurements were the Brief Psychiatric Rating Scale (BPRS and Global Assessment of Functioning (GAF scores. Of the 96 patients originally enrolled, 19 (19.8% were discontinued from all causes. During the 6-month study period, ten of the 96 patients (10.4% relapsed, compared with a 12.2% relapse rate in patients enrolled in a Phase III trial of risperidone LAI in Japan. Patients showed significant improvements in BPRS total

  18. Risperidone Improves Behavioral Symptoms in Children with Autism in a Randomized, Double-Blind, Placebo-Controlled Trial

    Science.gov (United States)

    Pandina, Gahan J.; Bossie, Cynthia A.; Youssef, Eriene; Zhu, Young; Dunbar, Fiona

    2007-01-01

    Subgroup analysis of children (5-12 years) with autism enrolled in an 8-week, double-blind, placebo-controlled trial of risperidone for pervasive developmental disorders. The primary efficacy measure was the Aberrant Behavior Checklist-Irritability (ABC-I) subscale. Data were available for 55 children given risperidone (n = 27) or placebo (n =…

  19. Risperidone Dosing in Children and Adolescents with Autistic Disorder: A Double-Blind, Placebo-Controlled Study

    Science.gov (United States)

    Kent, Justine M.; Kushner, Stuart; Ning, Xiaoping; Karcher, Keith; Ness, Seth; Aman, Michael; Singh, Jaskaran; Hough, David

    2013-01-01

    Efficacy and safety of 2 risperidone doses were evaluated in children and adolescents with autism. Patients (N = 96; 5-17 years), received risperidone (low-dose: 0.125 mg/day [20 to 45 kg] or high-dose: 1.25 mg/day [20 to 45 kg]) or placebo. Mean baseline (range 27-29) to endpoint change…

  20. Risperidone – Solid-state characterization and pharmaceutical compatibility using thermal and non-thermal techniques

    Energy Technology Data Exchange (ETDEWEB)

    Daniel, Josiane Souza Pereira; Veronez, Isabela Pianna; Rodrigues, Larissa Lopes [Laboratório de Análise e Caracterização de Fármacos – LACFar, Instituto de Química, Universidade Federal de Alfenas, Alfenas, Minas Gerais (Brazil); Trevisan, Marcello G. [Laboratório de Análise e Caracterização de Fármacos – LACFar, Instituto de Química, Universidade Federal de Alfenas, Alfenas, Minas Gerais (Brazil); National Institute of Bioanalytics Science and Technology – INCTBio, Institute of Chemistry – UNICAMP, 13084-653, Campinas, São Paulo (Brazil); Garcia, Jerusa Simone, E-mail: jerusa.garcia@unifal-mg.edu.br [Laboratório de Análise e Caracterização de Fármacos – LACFar, Instituto de Química, Universidade Federal de Alfenas, Alfenas, Minas Gerais (Brazil)

    2013-09-20

    Highlights: • DSC was used to characterize Risperidone and study its compatibility with excipients. • FT-IR associated with PCA was used to complement DSC data. • LC analyzes confirmed the DSC and FT-IR/PCA results. • Risperidone was incompatible with three among five excipients evaluated. - Abstract: A full solid-state characterization of risperidone was conducted using differential scanning calorimetry (DSC), thermogravimetry (TG), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM) to examine its physicochemical properties and polymorphism. The primary aim of this work was to study the compatibility of risperidone with pharmaceutical excipients using DSC to obtain and compare the curves of the active pharmaceutical ingredient (API) and the excipients with their 1:1 (w/w) binary mixtures. These same binary mixtures were turned to room temperature and analyzed by FT-IR combined with principal component analysis (PCA) to evaluate solid-state incompatibilities. The chemical incompatibilities of these samples were verified using a stability-indicating liquid chromatography (LC) method to assay for the API and evaluate the formation of degradation products. All of these methods showed incompatibilities between risperidone and the excipients magnesium stearate, lactose and cellulose microcrystalline.

  1. Optimization and in vivo toxicity evaluation of G4.5 PAMAM dendrimer-risperidone complexes.

    Directory of Open Access Journals (Sweden)

    Maria Jimena Prieto

    Full Text Available Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%. Since new strategies to improve efficient treatments are needed, we studied the efficiency of anionic G4.5 PAMAM dendrimers as nanocarriers for this therapeutic drug. To this end, we explored dendrimer-risperidone complexation dependence on solvent concentration, pH and molar relationship. The best dendrimer-risperidone incorporation (46 risperidone molecules per dendrimer was achieved with a mixture of chloroform:methanol 50∶50 v/v solution pH 3. In addition, to explore the possible effects of this complex, in vivo studies were carried out in the zebrafish model. Changes in the development of dopaminergic neurons and motoneurons were studied using tyrosine hydroxylase and calretinin, respectively. Physiological changes were studied through histological sections stained with hematoxylin-eosin to observe possible morphological brain changes. The most significant changes were observed when larvae were treated with free risperidone, and no changes were observed when larvae were treated with the complex.

  2. Optimization and in vivo toxicity evaluation of G4.5 PAMAM dendrimer-risperidone complexes.

    Science.gov (United States)

    Prieto, Maria Jimena; del Rio Zabala, Nahuel Eduardo; Marotta, Cristian Hernán; Carreño Gutierrez, Hector; Arévalo Arévalo, Rosario; Chiaramoni, Nadia Silvia; del Valle Alonso, Silvia

    2014-01-01

    Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%). Since new strategies to improve efficient treatments are needed, we studied the efficiency of anionic G4.5 PAMAM dendrimers as nanocarriers for this therapeutic drug. To this end, we explored dendrimer-risperidone complexation dependence on solvent concentration, pH and molar relationship. The best dendrimer-risperidone incorporation (46 risperidone molecules per dendrimer) was achieved with a mixture of chloroform:methanol 50∶50 v/v solution pH 3. In addition, to explore the possible effects of this complex, in vivo studies were carried out in the zebrafish model. Changes in the development of dopaminergic neurons and motoneurons were studied using tyrosine hydroxylase and calretinin, respectively. Physiological changes were studied through histological sections stained with hematoxylin-eosin to observe possible morphological brain changes. The most significant changes were observed when larvae were treated with free risperidone, and no changes were observed when larvae were treated with the complex.

  3. Review of risperidone for the treatment of pediatric and adolescent bipolar disorder and schizophrenia

    Directory of Open Access Journals (Sweden)

    Jeffrey R Bishop

    2008-03-01

    Full Text Available Jeffrey R Bishop1,2, Mani N Pavuluri21Department of Pharmacy Practice, University of Illinois at Chicago College of Pharmacy, Chicago, IL, USA; 2Department of Psychiatry, Pediatric Mood Disorders Program and Center for Cognitive Medicine, University of Illinois at Chicago College of Medicine, Chicago, IL, USAAbstract: Risperidone is a commonly used medication for the treatment of bipolar disorder and schizophrenia in children and adolescents. It has been studied as a monotherapy treatment in early onset schizophrenia and as both monotherapy and combination therapy for pediatric bipolar disorder. Studies to date indicate that risperidone is an effective treatment for positive and negative symptoms of schizophrenia and mania symptoms of bipolar disorder. In young patient populations, side effects such as weight gain, extrapyramidal side effects, and prolactin elevation require consideration when evaluating the risk benefit ratio for individual patients. Here we review published studies of risperidone for the treatment of bipolar disorder and schizophrenia in children and adolescents to provide practitioners with an overview of published data on the efficacy and safety of risperidone in these patient populations.Keywords: risperidone, bipolar disorder, schizophrenia, children, adolescents

  4. High-Dose Risperidone Induced Latent Syndrome of Inappropriate Antidiuretic Hormone Secretion With Seizure Presentation.

    Science.gov (United States)

    Lee, Yen-Feng; Tsai, Chia-Kuang; Liang, Chih-Sung

    2015-01-01

    We report a case of a patient with schizophrenia treated with high-dose risperidone, who developed syndrome of inappropriate antidiuretic hormone secretion (SIADH) with the only early symptom of tonic-clonic seizures. A 40-year-old woman with schizophrenia was treated with risperidone 2 mg/d. After the dosage was titrated to 6 mg/d, she experienced generalized seizure attacks. Laboratory screening revealed that the serum sodium level was 106 mmol/L, the urine sodium concentration was 41.2 mmol/L, and the urine osmolality was 371 mOsm/kg H2O. A diagnosis of SIADH was made, and risperidone was stopped. After infusion of hypertonic saline, the serum sodium returned to normal levels, and seizures did not recur. In this patient, SIADH advanced in a latent manner because the first and only symptom of SIADH was seizure attack. High-dose risperidone treatment is the most probable cause, and the mechanisms may be related to risperidone's high affinity for the 5-hydroxytryptamine 2A and dopamine 2 receptors. Patients with schizophrenia can display atypical features of medical illnesses. Routine physical and laboratory examinations may prevent silent disease progression.

  5. Risperidone and NAP protect cognition and normalize gene expression in a schizophrenia mouse model.

    Science.gov (United States)

    Vaisburd, Sinaya; Shemer, Zeev; Yeheskel, Adva; Giladi, Eliezer; Gozes, Illana

    2015-11-10

    Mutated disrupted in schizophrenia 1 (DISC1), a microtubule regulating protein, leads to schizophrenia and other psychiatric illnesses. It is hypothesized that microtubule stabilization may provide neuroprotection in schizophrenia. The NAP (NAPVSIPQ) sequence of activity-dependent neuroprotective protein (ADNP) contains the SxIP motif, microtubule end binding (EB) protein target, which is critical for microtubule dynamics leading to synaptic plasticity and neuroprotection. Bioinformatics prediction for FDA approved drugs mimicking SxIP-like motif which displace NAP-EB binding identified Risperidone. Risperidone or NAP effectively ameliorated object recognition deficits in the mutated DISC1 mouse model. NAP but not Risperidone, reduced anxiety in the mutated mice. Doxycycline, which blocked the expression of the mutated DISC1, did not reverse the phenotype. Transcripts of Forkhead-BOX P2 (Foxp2), a gene regulating DISC1 and associated with human ability to acquire a spoken language, were increased in the hippocampus of the DISC1 mutated mice and were significantly lowered after treatment with NAP, Risperidone, or the combination of both. Thus, the combination of NAP and standard of care Risperidone in humans may protect against language disturbances associated with negative and cognitive impairments in schizophrenia.

  6. Impact of risperidone on leptin and insulin in children and adolescents with autistic spectrum disorders.

    Science.gov (United States)

    Srisawasdi, Pornpen; Vanwong, Natchaya; Hongkaew, Yaowaluck; Puangpetch, Apichaya; Vanavanan, Somlak; Intachak, Boontarika; Ngamsamut, Nattawat; Limsila, Penkhae; Sukasem, Chonlaphat; Kroll, Martin H

    2017-08-01

    To evaluate the influence of dose and duration of risperidone treatment on cardiovascular and diabetes risk biomarkers in children and adolescents with autistic spectrum disorders (ASDs). In this cross-sectional analysis, a total of 168 ASDs patients (89% male) treated with a risperidone-based regimen for ≥12months were included. Blood samples were analyzed for glucose and lipid metabolic markers, adiponectin, leptin, prolactin, cortisol and high sensitive C-reactive protein. The mean concentrations of glucose, insulin, prolactin and leptin and HOMA-IR significantly rose with risperidone dosage (all Pleptin, prolactin and glucose concentrations and HOMA-IR show significant association with dosage. None of the markers except adiponectin showed dependence on duration of treatment. However, insulin and leptin concentrations and HOMA-IR clearly increased with increasing both dosage and duration. Dosage and duration of treatment had minimal effect on standard lipid profile and lipoprotein subclasses. Risperidone treatment disturbed glucose homeostasis and endocrine regulation (particularly leptin) in children and adolescents with ASDs, in a dose- and duration-dependent manner, being suggestive of leptin and insulin resistance mechanisms. Metabolic adverse effects, especially development of type 2 diabetes mellitus should be closely monitored, particularly in individuals receiving high doses and/or long-term risperidone treatment. Copyright © 2017 The Canadian Society of Clinical Chemists. Published by Elsevier Inc. All rights reserved.

  7. Desipramine enhances the ability of risperidone to decrease alcohol intake in the Syrian golden hamster.

    Science.gov (United States)

    Gulick, Danielle; Chau, David T; Khokhar, Jibran Y; Dawson, Ree; Green, Alan I

    2014-08-30

    The atypical antipsychotic clozapine reduces alcohol drinking in patients with schizophrenia. We have proposed that clozapine׳s ability to decrease alcohol drinking relates to its weak blockade of the dopamine D2 receptor and potent blockade of the norepinephrine α-2 receptor, as well as its ability to elevate plasma and brain norepinephrine. Another atypical antipsychotic, risperidone, which is a potent blocker of both the dopamine D2 receptor and norepinephrine α-2 receptor, does not decrease alcohol drinking. In this study, we used the Syrian golden hamster to test whether the ability of risperidone to reduce alcohol drinking would be enhanced if it was used in combination with the norepinephrine reuptake inhibitor desipramine. Hamsters were given free access to water and alcohol (15% v/v) until they reached a steady drinking baseline. They were then treated daily with each drug or drug combination for 20 days. Risperidone (0.2mg/kg) only transiently decreased alcohol drinking. However, 5.0mg/kg, and possibly 1.0mg/kg, desipramine added to 0.2mg/kg risperidone appeared to produce a more substantial and relatively sustained effect than risperidone alone. Data from this study provide leads toward the development of new treatments for patients with schizophrenia and alcoholism, and also for those with alcoholism alone.

  8. Cost effectiveness of olanzapine in prevention of affective episodes in bipolar disorder in the United Kingdom.

    Science.gov (United States)

    McKendrick, J; Cerri, K H; Lloyd, A; D'Ausilio, A; Dando, S; Chinn, C

    2007-08-01

    This study evaluated the cost effectiveness of olanzapine compared with lithium as maintenance therapy for patients with bipolar I disorder (BP1) in the UK. A Markov model was developed to assess costs and outcomes from the perspective of the UK National Health Service over a 1-year period. Patients enter the model after stabilization of a manic episode and are then treated with olanzapine or lithium. Using the findings of a recent randomized clinical trial, the model considers the monthly risk of manic or depressive episodes and of dropping out from allocated therapy. health care resources associated with acute episodes were derived primarily from a recent UK chart review. Costs of maintenance therapy and monitoring were also considered. Key factors influencing cost effectiveness were identified and included in a stochastic sensitivity analysis. The model estimated that, compared to lithium, olanzapine significantly reduced the annual number of acute mood episodes per patient from 0.81 to 0.58 (difference -0.23; 95% CI: -0.34, -0.12). Per patient average annual care costs fell by 799 UK pounds (95% CI: - 1,824 UK pounds, 59 UK pounds) driven by reduced inpatient days--but the cost difference was not statistically significant. Sensitivity analysis found the results to be robust to plausible variation in the model's parameters. The model estimated that using olanzapine instead of lithium as maintenance therapy for BP1 would significantly reduce the rate of acute mood events resulting in reduced hospital costs. Based on available evidence, there is a high likelihood that olanzapine would reduce costs of care compared to lithium.

  9. Midazolam-Droperidol, Droperidol, or Olanzapine for Acute Agitation: A Randomized Clinical Trial.

    Science.gov (United States)

    Taylor, David McD; Yap, Celene Y L; Knott, Jonathan C; Taylor, Simone E; Phillips, Georgina A; Karro, Jonathan; Chan, Esther W; Kong, David C M; Castle, David J

    2017-03-01

    We aim to determine the most efficacious of 3 common medication regimens for the sedation of acutely agitated emergency department (ED) patients. We undertook a randomized, controlled, double-blind, triple-dummy, clinical trial in 2 metropolitan EDs between October 2014 and August 2015. Patients aged 18 to 65 years and requiring intravenous medication sedation for acute agitation were enrolled and randomized to an intravenous bolus of midazolam 5 mg-droperidol 5 mg, droperidol 10 mg, or olanzapine 10 mg. Two additional doses were administered, if required: midazolam 5 mg, droperidol 5 mg, or olanzapine 5 mg. The primary outcome was the proportion of patients adequately sedated at 10 minutes. Three hundred forty-nine patients were randomized to the 3 groups. Baseline characteristics were similar across the groups. Ten minutes after the first dose, significantly more patients in the midazolam-droperidol group were adequately sedated compared with the droperidol and olanzapine groups: differences in proportions 25.0% (95% confidence interval [CI] 12.0% to 38.1%) and 25.4% (95% CI 12.7% to 38.3%), respectively. For times to sedation, the differences in medians between the midazolam-droperidol group and the droperidol and olanzapine groups were 6 (95% CI 3 to 8) and 6 (95% CI 3 to 7) minutes, respectively. Patients in the midazolam-droperidol group required fewer additional doses or alternative drugs to achieve adequate sedation. The 3 groups' adverse event rates and lengths of stay did not differ. Midazolam-droperidol combination therapy is superior, in the doses studied, to either droperidol or olanzapine monotherapy for intravenous sedation of the acutely agitated ED patient. Copyright © 2016 American College of Emergency Physicians. Published by Elsevier Inc. All rights reserved.

  10. Neuroanatomical substrates of the disruptive effect of olanzapine on rat maternal behavior as revealed by c-Fos immunoreactivity

    OpenAIRE

    Zhao, Changjiu; Li, Ming

    2012-01-01

    Olanzapine is one of the most widely prescribed atypical antipsychotic drugs in the treatment of schizophrenia. Besides its well-known side effect on weight gain, it may also impair human parental behavior. In this study, we took a preclinical approach to examine the behavioral effects of olanzapine on rat maternal behavior and investigated the associated neural basis using the c-Fos immunohistochemistry. On postpartum Days 6–8, Sprague-Dawley mother rats were given a single injection of ster...

  11. Association of Selected Antipsychotic Agents With Major Adverse Cardiovascular Events and Noncardiovascular Mortality in Elderly Persons

    DEFF Research Database (Denmark)

    Sahlberg, Marie; Holm, Ellen; Gislason, Gunnar H

    2015-01-01

    events and noncardiovascular mortality associated with individual APs (ziprasidone, olanzapine, risperidone, quetiapine, levomepromazine, chlorprothixen, flupentixol, and haloperidol) in Danish treatment-naïve patients aged ≥70 years. METHODS AND RESULTS: We followed all treatment-naïve Danish citizens...... aged ≥70 years that initiated treatment with APs for the first time between 1997 and 2011 (n=91 774, mean age 82±7 years, 35 474 [39%] were men). Incidence rate ratios associated with use of different APs were assessed by multivariable time-dependent Poisson regression models. For the first 30 days.......10 to 0.97), chlorprothixen (0.76, 95% CI 0.61 to 0.95), and quetiapine (0.68, 95% CI 0.58 to 0.80). Relationships were generally similar for long-term treatment. The majority of agents were associated with higher risks among patients with cardiovascular disease compared with patients without...

  12. Iron Deficiency in Pediatric Patients in Long-Term Risperidone Treatment

    Science.gov (United States)

    Ziegler, Ekhard E.

    2013-01-01

    Abstract Objective Atypical antipsychotics, increasingly used in children and adolescents, modulate brain dopamine. Iron plays a critical role in dopaminergic signaling. Therefore, we explored whether body iron status is related to psychiatric symptom severity, treatment response, and tolerability following extended antipsychotic therapy. Methods Between November 2005 and August 2009, medically healthy 7–17-year-old risperidone-treated participants enrolled in a cross-sectional study examining the long-term safety of this antipsychotic. Anthropometric measurements were obtained. Psychiatric symptom severity and dietary intake were assessed. Serum ferritin, transferrin receptor, and prolactin concentrations were measured. Linear multivariable regression analysis tested the association among body iron, symptom severity, the dose of risperidone and psychostimulants, and serum prolactin concentration. Results The sample consisted of 115 patients (87% males) with a mean (±SD) age of 11.6 (±2.8) years. The majority had externalizing disorders, and they had taken risperidone for 2.4 (±1.7) years. Body iron was low, with 45% having iron depletion and 14% having iron deficiency. Iron status was inversely associated with weight gain during risperidone treatment and with interleukin-6. Body iron was neither associated with psychiatric symptom severity nor with the daily dose of risperidone and psychostimulants. It was, however, inversely associated with prolactin concentration, which was nearly 50% higher in the iron-deficient group. Conclusions Iron depletion and deficiency are prevalent in children and adolescents chronically treated with risperidone. Iron deficiency accentuates the antipsychotic-induced elevation in prolactin. Future studies should confirm this finding and investigate the potential benefit of iron supplementation in antipsychotic-treated patients. PMID:23480322

  13. Enhancing the aqueous solubility and dissolution of olanzapine using freeze-drying

    Directory of Open Access Journals (Sweden)

    Mudit Dixit

    2011-12-01

    Full Text Available The aim of the present study was to develop an olanzapine freeze-dried tablet (FDT. The solubility and dissolution rate of poorly water-soluble olanzapine was improved by preparing a freeze-dried tablet of olanzapine using the freeze-drying technique . The FDT was prepared by dispersing the drug in an aqueous solution of highly water-soluble carrier materials consisting of gelatin, glycine, and sorbitol. The mixture was poured in to the pockets of blister packs and then was subjected to freezing and lyophilisation. The FDT was characterised by DSC, XRD and SEM and was evaluated for saturation solubility and dissolution. The samples were stored in a stability chamber to investigate their physical stability. Results obtained by DSC and X-ray were analysed and showed the crystalline state of olanzapine in FDT transformation to the amorphous state during the formation of FDT. Scanning electron microscope (SEM results suggest reduction in olanzapine particle size. The solubility of olanzapine from the FDT was observed to be nearly four and a half times greater than the pure drug. Results obtained from dissolution studies showed that olanzapine FDT significantly improved the dissolution rate of the drug compared with the physical mixture (PM and the pure drug. More than 90% of olanzapine in FDT dissolved within 5 minutes, compared to only 19.78% of olanzapine pure drug dissolved over the course of 60 minutes. In a stability test, the release profile of the FDT was unchanged, as compared to the freshly prepared FDT after 90 days of storing.O objetivo do presente estudo foi desenvolver comprimidos liofilizados de olanzapina (FDT. A solubilidade e a taxa de dissolução da olanzapina, fracamente solúvel em água, foram melhoradas com a preparação de comprimidos liofilizados de olanzapina usando a técnica de liofilização. O FDT foi preparado por dispersão do fármaco em solução aquosa de materiais altamente solúveis em água, como gelatina

  14. Freeze Dried Quetiapine-Nicotinamide Binary Solid Dispersions: A New Strategy for Improving Physicochemical Properties and Ex Vivo Diffusion

    Science.gov (United States)

    Al-Remawi, Mayyas Mohammad Ahmad

    2016-01-01

    Improving the physicochemical properties and oral bioavailability of quetiapine fumarate (QF) enabling enhanced antipsychotic attributes are the main aims of this research. The freeze dried solid dispersion strategy was adopted using nicotinamide (NIC) as highly soluble coformer. The prepared dispersions were characterized using scanning electron microscopy (SEM) differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Static disc intrinsic dissolution rate and ex vivo diffusion through intestinal tissues were conducted and compared to pure quetiapine fumarate. The results demonstrated a highly soluble coamorphous system formed between quetiapine fumarate and nicotinamide at 1 : 3 molar ratio through H-bonding interactions. The results showed >14-fold increase in solubility of QF from the prepared dispersions. Increased intrinsic dissolution rate (from 0.28 to 0.603 mg cm−2 min−1) and faster flux rate through duodenum (from 0.027 to 0.041 mg cm−2 h−1) and jejunum (0.027 to 0.036 mg cm−2 h−1) were obtained. The prepared coamorphous dispersion proved to be effective in improving the drug solubility and dissolution rate and ex vivo diffusion. Therefore, binary coamorphous dispersions could be a promising solution to modify the physicochemical properties, raise oral bioavailability, and change the biopharmaceutics classification (BCS) of some active pharmaceutical ingredients. PMID:28042494

  15. Olanzapine Prevents the PCP-induced Reduction in the Neurite Outgrowth of Prefrontal Cortical Neurons via NRG1.

    Science.gov (United States)

    Zhang, Qingsheng; Yu, Yinghua; Huang, Xu-Feng

    2016-01-19

    Accumulating evidence suggests that reducing neurite outgrowth and synaptic plasticity plays a critical role in the pathology of cognitive deficits in schizophrenia. The N-methyl-D-aspartate receptor antagonist phencyclidine (PCP) can induce symptoms of schizophrenia as well as reduce dendritic spine density and neurite growth. The antipsychotic drug olanzapine may improve these deficits. This study aimed to investigate: (1) if olanzapine prevents PCP-induced suppression of neurite outgrowth and synaptic protein expression; (2) if olanzapine affects the Akt-GSK3 signaling pathway; and (3) the role of neuregulin 1 (NRG1) in this process. Immunofluorescence revealed that PCP treatment for 24 hours reduces both neurite length (28.5%) and the number of neurite branches (35.6%) in primary prefrontal cortical neuron cultures. PCP reduced protein and mRNA expressions of synaptophysin (24.9% and 23.2%, respectively) and PSD95 (31.5% and 21.4%, respectively), and the protein expression of p-Akt (26.7%) and p-GSK3β (35.2%). Olanzapine co-treatment prevented these PCP-induced effects in normal neurons but not in neurons from NRG1-knockout mice. These results indicate that NRG1 mediates the preventive effects of olanzapine on the PCP-induced impairment of neurite outgrowth and synaptic protein expression. This study provides potential targets for interventions on improving the efficacy of olanzapine on preventing cognitive deficits in schizophrenia.

  16. Sulpiride augmentation of olanzapine in the management of treatment-resistant chronic schizophrenia: evidence for improvement of mood symptomatology.

    Science.gov (United States)

    Kotler, Moshe; Strous, Rael D; Reznik, Ilya; Shwartz, Sima; Weizman, Abraham; Spivak, Baruch

    2004-01-01

    Several recent studies, albeit limited in sample number, design and generalizability, have suggested that augmentation of atypical antipsychotic medication (such as clozapine and olanzapine) with sulpiride, a substituted benzamide antipsychotic medication, may play a role in the management of treatment-resistant psychotic conditions. The objective of this study was to investigate any change in clinical symptomatology or side-effect profile in treatment-resistant schizophrenia patients receiving sulpiride in addition to olanzapine. Seventeen patients with treatment-resistant chronic schizophrenia, who were receiving olanzapine monotherapy for at least 6 months before study commencement, were randomized in a 1:1 fashion to receive either adjunctive treatment with sulpiride (study group) or to continue their pre-study treatment with olanzapine with no medication augmentation (control group), each for a period of 8 weeks. Changes in measures of positive and negative symptoms, anxiety, depression and extrapyramidal symptoms were assessed at baseline and at 8 weeks. Study observations indicated no significant differences in the changes in positive or negative symptomatology between patients receiving a combined regimen of olanzapine with sulpiride (600 mg/ day) augmentation and controls. However, a significantly greater improvement of depressive symptomatology (P Depression) was noted in the sulpiride augmentation group. These data indicate improvement in depressive symptomatology with sulpiride augmentation of olanzapine in treatment-resistant chronic schizophrenia patients.

  17. Comparison the effectiveness of aripiprazole and risperidone for the treatment of acute bipolar mania

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    Amir Akhavan Rezayat

    2014-01-01

    Full Text Available Background: Second-generation antipsychotics, approved for the treatment of mania, are associated with adverse effects such as weight gain and metabolic disorders. Aripiprazole, a recently introduced second-generation antipsychotic, are thought to account for its low propensity for weight gain, metabolic disturbances and sedation. The purpose of this study was to investigate the effect of risperidone versus aripiprazole in the treatment of acute mania. Materials and Methods: Fifty patients with acute episodes of mania were enrolled in this study, and they were randomly assigned into a risperidone group of 24 cases and an aripiprazole group of 26 cases. In group A, aripiprazole with a dose of 5-30 mg/day and in group B, risperidone with a dose of 2-8 mg/day was given to patients. The average dose of aripiprazole was 27 mg/day, and the average dose of risperidone was 6 mg/day. The effects of each drug for the treatment of acute mania were assessed on the 1 st day of admission and on days 2, 4, 6, 8 and at weeks 2, 4 and 6 after therapy using the young mania rating scale (YMRS and at the baseline and on weeks 3 and 6 after admission using the clinical global impression (CGI scale. Results: The mean age of the group of risperidone was 34 ± 8.6 years and in a group of aripiprazole it was 34 ± 9.1 years (P = 0.83. Comparison of YMRS scores over the period of 6 weeks revealed a statistically significant difference in both groups (P < 0.0001.There was also a statistically significant difference in YMRS scores between risperidone and aripiprazole at day 8 (P = 0.026 and weeks 2 (P = 0.035 and 4 (P = 0.042. There was also a statistically significant difference in CGI-Severity scale score at weeks 3 (P = 0.003 and 6 (P = 0.000 and in CGI-Improvement scale score at weeks 3 (P = 0.005 and 6 (P = 0.002. The most common side-effect observed in both groups was headache (0%15/4 in aripiprazole vs. %16/7 in risperidone Conclusion: Aripiprazole that is readily

  18. Maintenance treatment with quetiapine when combined with either lithium or divalproex in bipolar I disorder: analysis of two large randomized, placebo-controlled trials.

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    Suppes, Trisha; Vieta, Eduard; Gustafsson, Urban; Ekholm, Birgit

    2013-11-01

    To determine the efficacy and safety of quetiapine combined with lithium or divalproex for preventing mood events in patients with bipolar I disorder. In this pooled analysis of two similar long-term studies (D1447C00126 [NCT00107731] and D1447C00127 [NCT00081380]), lithium and divalproex treatment groups were analyzed separately. Patients received open-label quetiapine (400-800 mg/d) plus lithium or divalproex to achieve ≥12 weeks of clinical stability before being randomized to double-blind combination treatment with quetiapine (400-800 mg/d) or placebo plus lithium or divalproex for up to 104 weeks. The primary endpoint was time to first mood event postrandomization following open stabilization. Of 3,414 patients in the stabilization phase, 1,326 were randomized. There were no differences in the risk of recurrence of mood, mania, or depression between quetiapine plus lithium or quetiapine plus divalproex. Among patients co-treated with placebo and lithium, the risk of recurrence of a mania event was significantly higher than among patients co-treated with placebo and divalproex. In patients with an index episode of mania, placebo plus lithium was associated with a significantly higher risk of recurrence of a mania event than placebo plus divalproex. Safety data were generally consistent with recognized safety profiles. In patients with bipolar I disorder previously stabilized on quetiapine and lithium or divalproex, maintenance therapy with quetiapine significantly increased the time to recurrence of a mood event (mania or depression) versus placebo, regardless of whether it was combined with lithium or divalproex. © 2013 Wiley Periodicals, Inc.

  19. Continuation of quetiapine versus switching to placebo or lithium for maintenance treatment of bipolar I disorder (Trial 144: a randomized controlled study).

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    Weisler, Richard H; Nolen, Willem A; Neijber, Anders; Hellqvist, Asa; Paulsson, Björn

    2011-11-01

    Quetiapine, combined with lithium or divalproex, demonstrates efficacy in the maintenance treatment of bipolar I disorder. This study investigated the efficacy and safety of quetiapine monotherapy as maintenance treatment in bipolar I disorder compared with switching to placebo or lithium. Patients aged ≥ 18 years with DSM-IV-diagnosed bipolar I disorder and a current or recent manic, depressive, or mixed episode received open-label quetiapine (300-800 mg/d) for 4-24 weeks. Patients achieving stabilization were randomized to continue quetiapine or to switch to placebo or lithium (0.6-1.2 mEq/L) for up to 104 weeks in a double-blind trial. Outcome measures included times to recurrence of any mood event (primary outcome measure), manic event, or depressive event. Safety assessments included adverse events and laboratory values. The study was terminated early after planned interim analysis provided positive results. The study was conducted between March 2005 and July 2007. Of 2,438 patients starting open-label quetiapine, 1,226 (50.3%) were randomized to double-blind treatment, including 1,172 (95.6%) in the intent-to-treat population. Time to recurrence of any mood event was significantly longer for quetiapine versus placebo (hazard ratio [HR] = 0.29; 95% CI, 0.23-0.38; P lithium versus placebo (HR = 0.46; 95% CI, 0.36-0.59; P lithium significantly increased time to recurrence of both manic events (quetiapine: HR = 0.29; 95% CI, 0.21-0.40; P lithium: HR = 0.37; 95% CI, 0.27-0.53; P lithium: HR = 0.59; 95% CI, 0.42-0.84; P lithium was also more effective than placebo for the prevention of manic and depressive events. clinicaltrials.gov Identifier: NCT00314184. © Copyright 2011 Physicians Postgraduate Press, Inc.

  20. Effect of cyamemazine on the steady-state plasma concentrations of risperidone and 9-hydroxyrisperidone: a preliminary retrospective study.

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    Lancelin, Frédérique; Bourcier, Elsa; Le Masson, Valérie; Lemeille, Yolande; Brovedani, Sophie; Paubel, Pascal; Piketty, Marie-Liesse

    2010-12-01

    Administration of cyamemazine, an antipsychotic drug with anxiolytic properties, together with other antipsychotic agents is common in patients with schizophrenia. This retrospective study investigated the effects of cyamemazine on the steady-state plasma concentrations of risperidone and 9-hydroxyrisperidone in 47 patients treated with 1 to 12 mg/day of risperidone. Of these 47 patients, 24 were receiving cyamemazine comedication ("cyamemazine" group) and 23 patients were treated with risperidone alone ("control" group). Plasma concentrations were measured using a high-performance liquid chromatographic method with photodiode-array ultraviolet detection. The median plasma concentration of risperidone was significantly higher in the cyamemazine group (31.5 ng/mL) than in the control group (5.0 ng/mL), whereas the 9-hydroxyrisperidone median concentration was significantly lower in the cyamemazine group (16.5 ng/mL versus 39.0 ng/mL in the control group). However, the sum of risperidone plus 9-hydroxyrisperidone (active moiety) plasma concentration was not significantly affected by cyamemazine comedication. A combination with cyamemazine resulted in an inverted metabolic ratio (risperidone/9-hydroxyrisperidone). These findings suggest that cyamemazine inhibits the 9-hydroxylation of risperidone and is probably an inhibitor of cytochrome P450 2D6 as are many other phenothiazine drugs.

  1. Risperidone: a review of its use in the treatment of irritability associated with autistic disorder in children and adolescents.

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    Scott, Lesley J; Dhillon, Sohita

    2007-01-01

    Risperidone (Risperdal), a psychotropic atypical antipsychotic agent, is thought to act via dopamine D(2) and serotonin (5-HT [5-hydroxytryptamine])(2A) receptor antagonism. The clinical efficacy of oral risperidone in the treatment of bipolar mania and schizophrenia in adult patients is well established. In the US, risperidone is also approved for the treatment of irritability associated with autistic disorder in children and adolescents aged 5-16 years, for the treatment of schizophrenia in adolescents aged 13-17 years and, as monotherapy, for the short-term treatment of acute manic and mixed episodes associated with bipolar I disorder in children and adolescents aged 10-17 years. Oral risperidone treatment was better than placebo treatment in reducing irritability and other behavioral symptoms associated with autistic disorder in children and adolescents in two well designed short-term trials, with these benefits maintained in those receiving risperidone for up to 6 months. The drug had a clinically manageable tolerability profile, with most adverse events being of mild to moderate intensity. There are some aspects of treatment, such as weight gain, somnolence, and hyperglycemia, that require monitoring, and the long-term safety of risperidone in children and adolescents with autistic disorder remains to be fully determined. With these issues in mind, risperidone offers a valuable emerging option for the treatment of irritability associated with autistic disorder in children and adolescents.

  2. Aripiprazole versus risperidone for treating children and adolescents with tic disorder: a randomized double blind clinical trial.

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    Ghanizadeh, Ahmad; Haghighi, Alireza

    2014-10-01

    There are some uncontrolled studies about the efficacy and safety of both aripiprazole and risperidone for treating tic disorder. Moreover, the efficacy of these medications has never been compared. This is the first double blind randomized clinical trial comparing the safety and efficacy of aripiprazole and risperidone for treating patients with tic disorder. Sixty children and adolescents with tic disorder were randomly allocated into one of the two groups to receive either aripiprazole or risperidone for 2 months. The primary outcome measure was the score of Yale Global Tic Severity Scale. In addition, health related quality of life and adverse events were assessed. Both aripiprazole and risperidone decreased the Yale Global Tic Severity Scale score during this trial. Moreover, both medications increased the health related quality of life score. Both aripiprazole and risperidone were tolerated well. Aripiprazole [3.22 (1.9) mg/day] decreased tic score as much as risperidone [0.6 (0.2) mg/day]. Their adverse effects and their effects on health related quality of life were comparable. However, risperidone increased the patients' social functioning more than aripiprazole in short term.

  3. Risperidone-induced weight gain is mediated through shifts in the gut microbiome and suppression of energy expenditure

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    Sarah M. Bahr

    2015-11-01

    Full Text Available Risperidone is a second-generation antipsychotic that causes weight gain. We hypothesized that risperidone-induced shifts in the gut microbiome are mechanistically involved in its metabolic consequences. Wild-type female C57BL/6J mice treated with risperidone (80 μg/day exhibited significant excess weight gain, due to reduced energy expenditure, which correlated with an altered gut microbiome. Fecal transplant from risperidone-treated mice caused a 16% reduction in total resting metabolic rate in naïve recipients, attributable to suppression of non-aerobic metabolism. Risperidone inhibited growth of cultured fecal bacteria grown anaerobically more than those grown aerobically. Finally, transplant of the fecal phage fraction from risperidone-treated mice was sufficient to cause excess weight gain in naïve recipients, again through reduced energy expenditure. Collectively, these data highlight a major role for the gut microbiome in weight gain following chronic use of risperidone, and specifically implicates the modulation of non-aerobic resting metabolism in this mechanism.

  4. Enhancement of the anti-immobility action of antidepressants by risperidone in the forced swimming test in mice.

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    Rogóż, Zofia; Kabziński, Marcin

    2011-01-01

    The aim of the present study was to examine the effect of antidepressants (ADs) belonging to different pharmacological groups and risperidone (an atypical antipsychotic drug), given separately or jointly, on immobility time in the forced swimming test in male C57BL/6J mice. The antidepressants: citalopram, fluvoxamine, sertraline, reboxetine, milnacipran (5 and 10 mg/kg), or risperidone in low doses (0.05 and 0.1 mg/kg) given alone did not change the immobility time of mice in the forced swimming test. Co-treatment with reboxetine or milnacipran (10 mg/kg) and risperidone in a lower dose of 0.05 mg/kg or with sertraline, reboxetine (5 and 10 mg/kg), citalopram, fluvoxamine, milnacipran (10 mg/kg) and risperidone in a higher dose of 0.1 mg/kg produced antidepressant-like effect in the forced swimming test. WAY100635 (a 5-HT(1A) receptor antagonist) inhibited the effects induced by co-administration of ADs and risperidone. Active behavior in the forced swimming test was not a consequence of an increased general activity, since the combined treatment with ADs and risperidone failed to enhance the locomotor activity of mice. The obtained results indicate that a low dose of risperidone enhances the activity of ADs in an animal model of depression, and that, among other mechanisms, 5-HT(1A) receptors may play a role in these effects.

  5. A Comparison of Risperidone and Buspirone for Treatment of Behavior Disorders in Children with Phenylketonuria

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    Afshin FAYYAZI

    2014-12-01

    Full Text Available How to Cite This Article: Fayyazi A, Salari E, Khajeh A, Ghajarpour A. A Comparison of Risperidone and Buspirone for Treatment ofBehavior Disorders in Children with Phenylketonuria. Iran J Child Neurol. 2014 Autumn; 8(4:33-38.AbstractObjectiveMany patients with late-diagnosed phenylketonuria (PKU suffer from severe behavior problems. This study compares the effects of buspirone and risperidone on reducing behavior disorders in these patients.Materials & MethodsIn this crossover clinical trial study, patients with severe behavior disorders after medical examination were randomly divided into two groups of two 8-week crossover treatments with risperidone or buspirone. Patient behavioral disorders before and after treatment by each drug was rated by parents on the Nisonger Child Behavior Rating Form (NCBRF, and after treatment by each drug, were assessed by a physician through clinical global impression (CGI.ResultsThirteen patients were able to complete the therapy period with these two medications.The most common psychiatric diagnoses were intellectual disability accompanied by pervasive developmental disorder NOS, and intellectual disability accompanied by autistic disorder. Risperidone was significantly effective in reducing the NCBRF subscales of hyperactivity disruptive/ stereotypic, and conduct problems. Treatment by buspirone only significantly decreased the severity of hyperactivity, but other behavior aspects showed no significant differences. Assessment of the severity of behavior disorder after treatment by risperidone and buspirone showed significant differences in reducing hyperactivity and masochistic/stereotype.ConclusionAlthough buspirone is effective in controlling hyperactivity in patients with PKU, it has no preference over risperidone. Therefore, it is recommended as an alternative to risperidone.ReferencesSmith I, Nowles JK. Behaviour in early treated phenylketonuria: a systematic review. Eur J Pediatr 2000;159:89-93.Targum SD

  6. 奥美拉唑对利培酮和9-羟利培酮血药浓度影响的研究%Influence study of omeprazole on blood drug concentration of risperidone and 9-hydroxy risperidone

    Institute of Scientific and Technical Information of China (English)

    巫艳芬; 王玉梅; 陈宝燕

    2014-01-01

    目的:观察奥美拉唑对利培酮和9-羟利培酮血药浓度的影响。方法20例精神分裂症合并胃溃疡患者,给予利培酮联合奥美拉唑治疗1周。检测奥美拉唑治疗后利培酮以及9-羟利培酮血药浓度。结果未使用奥美拉唑前,利培酮与9-羟利培酮血药浓度为(29.25±7.82)μg/L;使用奥美拉唑后,利培酮与9-羟利培酮血药浓度为(37.15±11.68)μg/L,差异有统计学意义(P<0.05)。结论奥美拉唑能够提高利培酮与9-羟利培酮血药浓度,因此,临床上治疗精神分裂症合并胃溃疡患者,给予奥美拉唑联合利培酮治疗时,应该监测患者利培酮与9-羟利培酮血药浓度,及时对药物剂量进行调整。%Objective To observe the influence of omeprazole on blood drug concentration of risperidone and 9-hydroxy risperidone. Methods A total of 20 schizophrenia with gastric ulcer cases were treated by risperidone combined with omeprazole for 1 week. Detections of blood drug concentration of risperidone and 9-hydroxy risperidone were made after the omeprazole treatment. Results Before application of omeprazole, blood drug concentration of risperidone and 9-hydroxy risperidone was (29.25±7.82)μg/L. After using omeprazole, blood drug concentration of risperidone and 9-hydroxy risperidone was (37.15±11.68) μg/L. The difference had statistical significance (P<0.05). Conclusion Omeprazole can increase the blood drug concentration of risperidone and 9-hydroxy risperidone, which should be monitored in the risperidone combined with omeprazole treatment of schizophrenia with gastric ulcer, and timely adjustment of drug dose is necessary.

  7. Efficacy of amisulpride and olanzapine for negative symptoms and cognitive impairments: An open-label clinical study

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    Subodh Kumar

    2014-01-01

    Full Text Available Background: Negative symptoms and diminished cognitive ability are also considered as core features of schizophrenia. There are many studies in which negative symptoms and cognitive impairments are individually treated with atypical antipsychotic in comparison with either a placebo or a typical antipsychotic. There is paucity of studies comparing the efficacy of olanzapine and amisulpride on improvement of negative symptoms and cognitive impairments. Aim: To examine the effectiveness of amisulpride and olanzapine in treatment of negative symptoms and cognitive impairments in schizophrenia. Materials and Methods: Total 40 adult inpatients diagnosed as schizophrenia fulfilling inclusion/exclusion criteria were included in the study with their informed consent. These patients were recruited consecutively to one of the two drug regimen group, i.e. tab Amisulpride (100-300 mg/day and tab Olanzapine (10-20 mg. Patients were evaluated on day 0 and day 60 with various rating scales like Scale for the Assessment of Negative Symptoms (SANS, Scale for the Assessment of Positive Symptoms (SAPS, Schizophrenia Cognition Rating Scale (SCoRS, Brief Psychiatric Rating Scale (BPRS, Calgary Depression Scale for Schizophrenia (CDSS, and three different scales to measure drug side effects. Results: The mean SANS score in amisulpride and olanzapine group at day 0 and day 60 were 83.89 (±12.67 and 21.00 (±11.82 and 84.40 (±13.22 and 26.75 (±12.41, respectively. The mean rank of SCoRS global in amisulpride and olanzapine group at day 0 and day 60 were 4.78 (±1.13 and 2.78 (±0.63 and 4.85 (±1.18 and 3.30 (±1.12, respectively. The percentage improvement in SANS, SAPS, SCoRS interviewer, and SCoRS global in amisulpride group are 74.96%, 13.36%, 54.14%, and 42.00%, respectively. Similarly in olanzapine group percentage improvement in SANS, SAPS, SCoRS interviewer, and SCoRS global are 68.30%, 30.28%, 35.22%, and 31.95%, respectively. There is significant

  8. Comparative study of treatment continuation using second-generation antipsychotics in patients with schizophrenia or schizoaffective disorder

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    Azekawa T

    2011-11-01

    Full Text Available Takaharu Azekawa, Shizuko Ohashi, Akira ItamiShioiri Mental Clinic, Yokosuka-shi, Kanagawa-ken, JapanBackground: Effectiveness of a drug is a key concept dependent on efficacy, safety, and tolerability. Time to discontinuation of treatment is also representative of effectiveness. We investigated differences in treatment discontinuation among newly started second-generation antipsychotics in the clinical setting.Methods: Using a retrospective cohort study design, we screened all outpatients (n = 7936 who visited the Shioiri Mental Clinic between July 1, 2008 and June 30, 2010. We identified a cohort of patients (n = 703 diagnosed with schizophrenia or schizoaffective disorder and calculated the time to discontinuation of each second-generation antipsychotic.Results: Of the 703 patients, 149 were newly treated with aripiprazole, 67 with blonanserin, 95 with olanzapine, 36 with quetiapine, 74 with perospirone, and 120 with risperidone. The time to discontinuation for all causes was significantly longer for aripiprazole than for blonanserin, olanzapine, and risperidone. In addition, aripiprazole tended to be continued for longer than quetiapine and perospirone, but these differences were not significant.Conclusion: Aripiprazole may be considered the best available option for long-term treatment of patients with schizophrenia or schizoaffective disorder.Keywords: retrospective study, second-generation antipsychotics, effectiveness, treatment continuation, schizophrenia, aripiprazole

  9. Comparative study of treatment continuation using second-generation antipsychotics in patients with schizophrenia or schizoaffective disorder.

    Science.gov (United States)

    Azekawa, Takaharu; Ohashi, Shizuko; Itami, Akira

    2011-01-01

    Effectiveness of a drug is a key concept dependent on efficacy, safety, and tolerability. Time to discontinuation of treatment is also representative of effectiveness. We investigated differences in treatment discontinuation among newly started second-generation antipsychotics in the clinical setting. Using a retrospective cohort study design, we screened all outpatients (n = 7936) who visited the Shioiri Mental Clinic between July 1, 2008 and June 30, 2010. We identified a cohort of patients (n = 703) diagnosed with schizophrenia or schizoaffective disorder and calculated the time to discontinuation of each second-generation antipsychotic. Of the 703 patients, 149 were newly treated with aripiprazole, 67 with blonanserin, 95 with olanzapine, 36 with quetiapine, 74 with perospirone, and 120 with risperidone. The time to discontinuation for all causes was significantly longer for aripiprazole than for blonanserin, olanzapine, and risperidone. In addition, aripiprazole tended to be continued for longer than quetiapine and perospirone, but these differences were not significant. Aripiprazole may be considered the best available option for long-term treatment of patients with schizophrenia or schizoaffective disorder.

  10. A patient with schizophrenia presenting with post-lobotomy catatonia treated with olanzapine: a case report.

    Science.gov (United States)

    Kumagai, Ryo; Kitazawa, Maiko; Ishibiki, Yoshiro; Narumi, Kenji; Ichimiya, Yosuke

    2017-05-01

    A 79-year-old Japanese woman with schizophrenia was hospitalized because of idiopathic duodenal stenosis. Three days after discontinuing ingestion, including the administration of psychotropic drugs, the patient demonstrated incoherent behaviour and strong general muscle tension, and was unable to engage in conversation. Computed tomography indicated bilateral regions of low density in the frontal lobes, subsequent to which she was diagnosed with post-lobotomy catatonia. Administration of olanzapine (10 mg/day) improved the patient's condition within a short period. Previous studies have demonstrated an association between the dysfunction of frontal circuits and catatonia; therefore, the observed catatonic episode might relate to the disconnection of nerve fibres in the prefrontal lobes induced by her lobotomy. Olanzapine was likely effective in treating catatonia because of its reported efficacy in improving frontal lobe function. © 2016 The Authors. Psychogeriatrics © 2016 Japanese Psychogeriatric Society.

  11. Fever development in neuroleptic malignant syndrome during treatment with olanzapine and clozapine.

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    Szota, Anna; Ogłodek, Ewa; Araszkiewicz, Aleksander

    2013-01-01

    Neuroleptic malignant syndrome (NMS) is the most dangerous life-threatening complication of antipsychotic medication. It's development is connected with the blockade of dopaminergic transmission (D2 receptors) in the nigrostriatal system of the brain. Fever is one of the main symptoms of this syndrome and it's elevation is due to the activation of the immune system. Numerous studies report that treatment with clozapine (doses 37.5-600 mg) or olanzapine (doses 10-25 mg) or the use of these drugs in polytherapy cause pyrexia between 37.8-40.6 °C. Additionally, levels of proinflammatory interleukins such as IL-6, IL-1,TNF-α were increased. The aim of this article is to describe how olanzapine and clozapine influence fever development in NMS, in relation to the dose of the drug taken by schizophrenic patients including changes in immunological system.

  12. Acute-Onset Type 1 Diabetes that Developed During the Administration of Olanzapine

    Science.gov (United States)

    Iwaku, Kenji; Otuka, Fumiko; Taniyama, Matsuo

    2017-01-01

    The patient was 32-year-old man, who received olanzapine for schizophrenia and developed polyuria and thirst without drinking soft-drinks after 4 months. Five months after the initiation of treatment, he developed diabetic ketoacidosis (blood glucose: 490 mg/dL, HbA1c: 15.5%). He was diagnosed with type 1 diabetes (glutamic acid decarboxylase (GAD)-Ab: 5.6 U/mL, IA-2 Ab: 5.9 U/mL, fasting C-peptide: 0.12 ng/mL) and was put on intensive insulin therapy. At four months after the onset of 1A diabetes, he experienced a honeymoon phase that was sustained until the 40th month of treatment. We hypothesize that the administration of olanzapine to a patient with pre-type 1A diabetes induced marked hyperglycemia and accelerated the onset of type 1A diabetes. PMID:28154279

  13. Efficacy and safety of quetiapine in children and adolescents with mania associated with bipolar I disorder: a 3-week, double-blind, placebo-controlled trial.

    Science.gov (United States)

    Pathak, Sanjeev; Findling, Robert L; Earley, Willie R; Acevedo, Larisa D; Stankowski, Jill; Delbello, Melissa P

    2013-01-01

    To evaluate the efficacy and safety of quetiapine monotherapy in children and adolescents with mania associated with bipolar I disorder. Patients aged 10 to 17 years, with a DSM-IV-TR diagnosis of a manic episode associated with bipolar I disorder and Young Mania Rating Scale (YMRS) total score ≥ 20 were randomized to 3 weeks of quetiapine (400 or 600 mg/d) or placebo. The primary efficacy measure was change in YMRS total score. The study was conducted at 34 centers in the United States between August 2004 and July 2006. The intent-to-treat population included 277 patients. Least squares mean change in YMRS score from baseline to end point by mixed-model, repeated-measures analysis was -14.25, -15.60, and -9.04 for quetiapine 400 mg/d, quetiapine 600 mg/d, and placebo, respectively (P bipolar disorder. Treatment was generally well tolerated and adverse events were broadly consistent with the known profile of quetiapine in adults with bipolar disorder. ClinicalTrials.gov identifier: NCT00090311. © Copyright 2013 Physicians Postgraduate Press, Inc.

  14. Schizophrenia relapse after stopping olanzapine treatment during pregnancy: a case report

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    Ifteni P

    2014-10-01

    Full Text Available Petru Ifteni,1,2 Marius A Moga,1 Victoria Burtea,1,2 Christoph U Correll3,4 1Faculty of Medicine, Transilvania University, Brasov, Romania; 2Psychiatry and Neurology Hospital, Brasov, Romania; 3Department of Psychiatry, The Zucker Hillside Hospital, North Shore-Long Island Jewish (LIJ Health System, New York, NY, USA; 4Hofstra North Shore-LIJ School of Medicine, New York, NY, USA Abstract: Women with schizophrenia have a high risk for symptom exacerbation or relapse during pregnancy and thereafter. Relapses are more frequent when antipsychotics are discontinued. This paper describes the case of a 28-year old woman with schizophrenia who continued treatment with olanzapine during the first trimester. Olanzapine, a second-generation antipsychotic, was administered at a therapeutic dose from week 1 of gestation until week 13 when she reported the pregnancy to her psychiatrist. Despite the psychiatrist’s recommendation to continue treatment, the patient stopped olanzapine at 20 weeks. She was hospitalized at week 36 for a schizophrenia relapse and was transferred to the obstetrics department where she gave birth by Cesarean section to a normal child. This case is important, illustrating the perils of unplanned pregnancy during antipsychotic treatment and abrupt discontinuation. Ultimately, clinical decisions should be made on a case-by-case basis, weighing the risks to the mother in terms of symptom exacerbation and relapse if antipsychotic treatment is discontinued, and the potential risk to the fetus regarding possible teratogenic effects of continued antipsychotic treatment. Keywords: relapse, pregnancy, schizophrenia, olanzapine

  15. A pharmaco-economic analysis of patients with schizophrenia switching to generic risperidone involving a possible compliance loss

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    Möller Hans-Jürgen

    2009-02-01

    Full Text Available Abstract Background As schizophrenia patients are typically suspicious of, or are hostile to changes they may be reluctant to accept generic substitution, possibly affecting compliance. This may counteract drug costs savings due to less symptom control and increased hospitalization risk. Although compliance losses following generic substitution have not been quantified so far, one can estimate the possible health-economic consequences. The current study aims to do so by considering the case of risperidone in Germany. Methods An existing DES model was adapted to compare staying on branded risperidone with generic substitution. Differences include the probability of non-compliance and medication costs. Incremental probability of non-compliance after generic substitution was varied between 2.5% and 10%, while generic medication costs were assumed to be 40% lower. Effect of medication price was assessed as well as the effect of applying compliance losses to all treatment settings. The probability of staying on branded risperidone being cost-effective was calculated for various outcomes of a hypothetical study that would investigate non-compliance following generic substitution of risperidone. Results If the incremental probability of non-compliance after generic substitution is 2.5%, 5.0%, 7.5% and 10% respectively, incremental effects of staying on branded risperidone are 0.004, 0.007, 0.011 and 0.015 Quality Adjusted Life Years (QALYs. Incremental costs are €757, €343, -€123 and -€554 respectively. Benefits of staying on branded risperidone include improved symptom control and fewer hospitalizations. If generic substitution results in a 5.2% higher probability of non-compliance, the model predicts staying on branded risperidone to be cost-effective (NICE threshold of ₤30,000 per QALY gained. Compliance losses of more than 6.9% makes branded risperidone the dominant alternative. Results are sensitive to the locations at which compliance

  16. Sustained release of risperidone from biodegradable microspheres prepared by in-situ suspension-evaporation process.

    Science.gov (United States)

    An, Taekun; Choi, Juhyuen; Kim, Aram; Lee, Jin Ho; Nam, Yoonjin; Park, Junsung; Sun, Bo kyung; Suh, Hearan; Kim, Cherng-ju; Hwang, Sung-Joo

    2016-04-30

    Risperidone-loaded poly (D,L-lactide-co-glycolide) (PLGA) microspheres were prepared with a suspension-evaporation process with an aqueous suspension containing an in situ-formed aluminum hydroxide inorganic gel (SEP-AL process) and evaluated for encapsulation efficiency, particle size, surface morphology, glass transition temperature, in vitro drug release profile, and in vivo behavior. The SEP-AL microspheres were compared with conventional oil-in-water (O/W) emulsion solvent evaporation method using polyvinylalcohol (PVA) as an emulsifier (CP-PVA process). The microspheres were spherical in shape. DSC measurements showed that risperidone crystallinity was greatly reduced due to the homogeneous distribution of risperidone in PLGA microspheres. In vitro drug release profile from the microspheres showed a sigmoidal pattern of negligible initial burst up to 24h and minimal release (time-lag) for 7 days. After the lag phase, slow release took a place up to 25 days and then rapid release occurred sharply for 1 week. In vivo rat pharmacokinetic profile from the microspheres showed very low blood concentration level at the initial phase (up to 24h) followed by the latent phase up to 21 days. At the 3rd week, main phase started and the blood concentration of the drug increased up to the 5th week, and then gradually decreased. The risperidone-loaded PLGA microspheres produced by SEP-AL process showed excellent controlled release characteristics for the effective treatment of schizophrenia patients.

  17. Dietary Status and Impact of Risperidone on Nutritional Balance in Children with Autism: A Pilot Study

    Science.gov (United States)

    Lindsay, Ronald L.; Arnold, L. Eugene; Aman, Michael G.; Vitiello, Benedetto; Posey, David J.; McDougle, Christopher J.; Scahill, Lawrence; Pachler, Maryellen; McCracken, James T.; Tierney, Elaine; Bozzolo, Dawn

    2006-01-01

    Background: Risperidone may be effective in improving tantrums, aggression, or self-injurious behaviour in children with autism, but often leads to weight gain. Method: Using a quantitative Food Frequency Questionnaire (FFQ), we prospectively examined the nutritional intake of 20 children with autism participating in a randomised…

  18. Risperidone treatment for ADHD in children and adolescents with bipolar disorder

    Directory of Open Access Journals (Sweden)

    Joseph Biederman

    2008-03-01

    Full Text Available Joseph Biederman, Paul Hammerness, Robert Doyle, Gagan Joshi, Megan Aleardi, Eric MickPediatric Psychopharmacology Research Department, Massachusetts General Hospital, Boston, MA, USAObjective: Children and adolescents with bipolar disorder are also at high risk of having comorbid attention-deficit hyperactivity disorder (ADHD. The objective of this study was to estimate improvement in ADHD symptoms in children with bipolar disorder.Methods: This was an open-label, study of risperidone monotherapy for the treatment of pediatric bipolar disorder. Thirty-one children and adolescents 4–15 years of age (7.2 ± 2.8 years of both sexes (71%, N = 22 male with pediatric bipolar disorder (YMRS score = 32.9 ± 8.8 and ADHD (ADHD-RS score = 37.9 ± 8.9 were included in these analyses.Results: Improvement in ADHD symptoms was contingent on improvement in manic symptoms. Although both hyperactive/impulsive (−7.5 ± 5.5.6, p < 0.05 and inattentive (−6.8 ± 5.0, p < 0.05 ADHD symptoms were significantly improved with risperidone, improvement was modest, and only 29% of subjects (N = 6 showed a 30% reduction in ADHD rating scale scores and had a CGI-I ≤ 2.Conclusions: These results suggest that that treatment with risperidone is associated with tangible but generally modest improvement of symptoms of ADHD in children with bipolar disorder.Keywords: ADHD, bipolar disorder, children, risperidone

  19. Neuropsychological effects of risperidone in children with pervasive developmental disorders : A blinded discontinuation study

    NARCIS (Netherlands)

    Troost, Pieter W.; Althaus, Monika; Lahuis, Bertine E.; Buitelaar, Jan K.; Minderaa, Ruud B.; Hoekstra, Pieter J.

    2006-01-01

    Objective: Little is known about the neuropsychological effects of risperidone in children with pervasive developmental disorders. Method: Twenty-four children (aged 5-17 years) with pervasive developmental disorders and co-morbid disruptive behavior who responded favorably to open-label treatment

  20. Tic Reduction with Risperidone Versus Pimozide in a Randomized, Double-Blind, Crossover Trial

    Science.gov (United States)

    Gilbert, Donald L.; Batterson, J. Robert; Sethuraman, Gopalan; Sallee, Floyd R.

    2004-01-01

    Objective: To compare the tic suppression, electrocardiogram (ECG) changes, weight gain, and side effect profiles of pimozide versus risperidone in children and adolescents with tic disorders. Method: This was a randomized, double-blind, crossover (evaluable patient analysis) study. Nineteen children aged 7 to 17 years with Tourette's or chronic…

  1. Paediatric European Risperidone Studies (PERS) : context, rationale, objectives, strategy, and challenges

    NARCIS (Netherlands)

    Glennon, Jeffrey; Purper-Ouakil, Diane; Bakker, Mireille; Zuddas, Alessandro; Hoekstra, Pieter; Schulze, Ulrike; Castro-Fornieles, Josefina; Santosh, Paramala J.; Arango, Celso; Koelch, Michael; Coghill, David; Flamarique, Itziar; Penzol, Maria J.; Wan, Mandy; Murray, Macey; Wong, Ian C. K.; Danckaerts, Marina; Bonnot, Olivier; Falissard, Bruno; Masi, Gabriele; Fegart, Joerg M.; Vicari, Stefano; Carucci, Sara; Dittmann, Ralf W.; Buitelaar, Jan K.

    2014-01-01

    In children and adolescents with conduct disorder (CD), pharmacotherapy is considered when non-pharmacological interventions do not improve symptoms and functional impairment. Risperidone, a second-generation antipsychotic is increasingly prescribed off-label in this indication, but its efficacy and

  2. Spontaneous seizures after ECT in a patient medicated with bupropion, sertraline and risperidone

    Directory of Open Access Journals (Sweden)

    Orlando von Doellinger

    Full Text Available Abstract Objective: To report a case of post-electroconvulsive therapy spontaneous seizures in a patient medicated with sertraline, bupropion and risperidone. Case description: A 53-year-old woman with recurrent major depression was admitted to our psychiatry department for a major depressive episode of 6 weeks' duration, with psychotic symptoms. She was already on 200 mg/day of sertraline and 2 mg/day of risperidone. After 8 weeks on 200 mg/day of sertraline, 4 mg/day of risperidone and slow release bupropion (titrated to 300 mg/day, with no objective improvements, the decision was taken to initiate a course of 8-10 electroconvulsive therapy (ECT sessions. Two days after the first treatment, three generalized tonic-clonic seizures occurred within 6 hours. Phenytoin and sodium valproate were added to the patient's daily medication and no further spontaneous seizures were observed. After neurologic assessment and discussion of the case, phenytoin and bupropion were withdrawn at once (two days after the spontaneous seizures and the decision was taken to resume the ECT treatment. No further spontaneous seizures occurred and, at discharge, the patient exhibited significant improvements and was free from major depressive symptoms. Comments: This report illustrates a case of post-ECT spontaneous seizures that might have been due to a specific pharmacological etiological pathway, namely, bupropion's proconvulsive properties, although both sertraline and risperidone also lower the convulsive threshold.

  3. Paediatric European Risperidone Studies (PERS): context, rationale, objectives, strategy, and challenges

    NARCIS (Netherlands)

    Glennon, J.C.; Purper-Ouakil, D.; Bakker, M; Zuddas, A.; Hoekstra, P.; Schulze, U.; Castro-Fornieles, J.; Santosh, P.J.; Arango, C.; Kolch, M.; Coghill, D.; Flamarique, I.; Penzol, M.J.; Wan, M.; Murray, M.; Wong, I.C.; Danckaerts, M.; Bonnot, O.; Falissard, B.; Masi, G.; Fegert, J.M.; Vicari, S.; Carucci, S.; Dittmann, R.W.; Buitelaar, J.

    2014-01-01

    In children and adolescents with conduct disorder (CD), pharmacotherapy is considered when non-pharmacological interventions do not improve symptoms and functional impairment. Risperidone, a second-generation antipsychotic is increasingly prescribed off-label in this indication, but its efficacy and

  4. Paediatric European Risperidone Studies (PERS) : context, rationale, objectives, strategy, and challenges

    NARCIS (Netherlands)

    Glennon, Jeffrey; Purper-Ouakil, Diane; Bakker, Mireille; Zuddas, Alessandro; Hoekstra, Pieter; Schulze, Ulrike; Castro-Fornieles, Josefina; Santosh, Paramala J.; Arango, Celso; Koelch, Michael; Coghill, David; Flamarique, Itziar; Penzol, Maria J.; Wan, Mandy; Murray, Macey; Wong, Ian C. K.; Danckaerts, Marina; Bonnot, Olivier; Falissard, Bruno; Masi, Gabriele; Fegart, Joerg M.; Vicari, Stefano; Carucci, Sara; Dittmann, Ralf W.; Buitelaar, Jan K.

    2014-01-01

    In children and adolescents with conduct disorder (CD), pharmacotherapy is considered when non-pharmacological interventions do not improve symptoms and functional impairment. Risperidone, a second-generation antipsychotic is increasingly prescribed off-label in this indication, but its efficacy and

  5. Stability Indicating HPLC Determination of Risperidone in Bulk Drug and Pharmaceutical Formulations

    Directory of Open Access Journals (Sweden)

    Zarna R. Dedania

    2011-01-01

    Full Text Available The objective of the current study was to develop a validated stability-indicating assay method (SIAM for risperidone after subjecting it to forced decomposition under hydrolysis, oxidation, photolysis, and thermal stress conditions. The liquid chromatographic separation was achieved isocratically on a symmetry C18 column (5 μm size, 250 mm × 4.6 mm i.d. using a mobile phase containing methanol: acetonitrile (80 : 20, v/v at a flow rate of 1 mL/min and UV detection at 280 nm. Retention time of risperidone was found to be 3.35±0.01. The method was linear over the concentration range of 10–60 μg/mL(2=0.998 with a limit of detection and quantitation of 1.79 and 5.44 μg/mL, respectively. The method has the requisite accuracy, specificity, sensitivity, and precision to assay risperidone in bulk form and pharmaceutical dosage forms. Degradation products resulting from the stress studies did not interfere with the detection of Risperidone, and the assay is thus stability indicating.

  6. Long-term effects of risperidone in children with autism spectrum disorders : A placebo discontinuation study

    NARCIS (Netherlands)

    Troost, PW; Lahuis, BE; Steenhuis, MP; Ketelaars, CEJ; Buitelaar, JK; Van Engeland, H; Scahill, L; Minderaa, RB; Hoekstra, PJ

    2005-01-01

    Objective: The short-term benefit of risperidone in ameliorating severe disruptive behavior in pediatric patients with autism spectrum disorders is well established; however, only one placebo-controlled, long-term study of efficacy is available. Method: Thirty-six children with an autism spectrum di

  7. Clinical and pharmacokinetic evaluation of risperidone for the management of autism spectrum disorder

    NARCIS (Netherlands)

    Dinnissen, Mariken; Dietrich, Andrea; van den Hoofdakker, Barbara J.; Hoekstra, Pieter J.

    2015-01-01

    Introduction: Autism spectrum disorder (ASD) is a neurodevelopmental disorder that is often accompanied by psychiatric comorbidity. Although there is no medication currently available to treat the core symptoms of ASD, risperidone was the first drug to be approved for use in ASD and is still the bes

  8. Antipsychotic-induced extrapyramidal syndromes - Risperidone compared with low- and high-potency conventional antipsychotic drugs

    NARCIS (Netherlands)

    Schillevoort, [No Value; de Boer, A; Herings, RMC; Roos, RAC; Jansen, PAF; Leufkens, HGM

    2001-01-01

    Aim: To compare the risk of extrapyramidal syndromes (EPS) between patients using risperidone and those using low-potency conventional antipsychotic drugs (APDs) in outpatient clinical practice, as measured by the use of anticholinergic medication. We tried to replicate results from previous clinica

  9. Neuropsychological effects of risperidone in children with pervasive developmental disorders: a blinded discontinuation study.

    NARCIS (Netherlands)

    Troost, P.W.; Althaus, M.; Lahuis, B.E.; Buitelaar, J.K.; Minderaa, R.B.; Hoekstra, P.J.

    2006-01-01

    OBJECTIVE: Little is known about the neuropsychological effects of risperidone in children with pervasive developmental disorders. METHOD: Twenty-four children (aged 5-17 years) with pervasive developmental disorders and co-morbid disruptive behavior who responded favorably to open-label treatment w

  10. Direct association between orbitofrontal atrophy and the response of psychotic symptoms to olanzapine in schizophrenia.

    Science.gov (United States)

    Molina, Vicente; Sanz, Javier; Benito, Carlos; Palomo, Tomás

    2004-07-01

    The study of cerebral variables associated with response to neuroleptics holds interest from both theoretical and clinical points of view. To date, no studies have aimed to identify predictors of response to olanzapine based on cerebral measurements. Here, we used magnetic resonance to assess the relationship between volumes of the prefrontal (dorsolateral and orbitofrontal) and temporal (temporal lobe and hippocampus) cortical regions and ventricles and, on the other hand, the response to olanzapine in 16 schizophrenic patients. Data from 42 healthy controls were used to calculate volume residuals in the patients, defined as deviations from the expected values, given individual age and intracranial volume. Residuals thus represent the effect of illness on regional measurements. The association between clinical change and those residuals was calculated separately for the positive, negative and total scores from the Positive and Negative Syndrome Scale (PANSS). There was a significant direct association between the degree of orbitofrontal atrophy and the improvement of positive symptoms with olanzapine. No predictors were found for change in the negative dimension. A trend was found for patients with larger ventricles to show a greater global decrease in total PANSS scores. Neither age nor duration of illness explained a significant proportion of the symptom improvement. This result, together with others from the literature, supports the idea that atypical antipsychotics may offer some benefit to patients with significant regional atrophy, and this may have implications for the choice of antipsychotic in clinical practice.

  11. Spectroscopic and molecular docking studies on the interaction of the drug olanzapine with calf thymus DNA

    Science.gov (United States)

    Shahabadi, Nahid; Bagheri, Somayeh

    2015-02-01

    The present study investigated the binding interaction between olanzapine and calf thymus DNA (ct-DNA) using emission, absorption, circular dichroism, viscosity measurements and molecular modeling. Thermodynamic parameters (ΔH < 0 and ΔS < 0) indicated that hydrogen bond and van der Waals play main roles in the binding of the drug to ct-DNA. Spectrophotometric studies of the interaction of olanzapine with DNA have shown that it could bind to ct-DNA (Kb = 2 × 103 M-1). The binding constant is comparable to standard groove binding drugs. Competitive fluorimetric studies with Hoechst 33258 have shown that olanzapine exhibits the ability to displace the DNA-bound Hoechst 33258 indicating that binds strongly in minor groove of DNA helix. Furthermore, the drug induces detectable changes in the CD spectrum of ct-DNA as well as changes in its viscosity. All of the experimental results prove that the groove binding must be predominant. The results obtained from experimental data were in good agreement with molecular modeling studies.

  12. Olanzapine-Induced Diabetic Ketoacidosis and Neuroleptic Malignant Syndrome with Rhabdomyolysis: A Case Report

    Directory of Open Access Journals (Sweden)

    Young Kyoung Sa

    2013-03-01

    Full Text Available Atypical antipsychotics have replaced conventional antipsychotics in the treatment of schizophrenia because they have less of a propensity to cause undesirable neurologic adverse events including extrapyramidal symptoms, tardive dyskinesia, and neuroleptic malignant syndrome (NMS. However, atypical antipsychotics have been known to result in various metabolic complications such as impaired glucose tolerance, diabetes and even diabetic ketoacidosis (DKA. In addition, a number of NMS cases have been reported in patients treated with atypical antipsychotics, although the absolute incidence of neurologic side effects is currently significantly low. Here, we report a patient who simultaneously developed DKA, acute renal failure and NMS with rhabdomyolysis after olanzapine treatment. Olanzapine-induced metabolic complications and NMS were dramatically improved with cessation of the olanzapine treatment and initiation of supportive management including fluid therapy, hemodialysis, and intensive glycemic control using insulin. At short-term follow-up, insulin secretion was markedly recovered as evidenced by a restoration of serum C-peptide level, and the patient no longer required any hypoglycemic medications. Despite the dramatic increase in the use of atypical antipsychotics treatment, individualized treatments along with careful monitoring may be prudent for high risk or vulnerable patients in order to avoid the development of metabolic side effects.

  13. Plasma metabonomics study of first-Episode schizophrenia treated with olanzapine in female patients.

    Science.gov (United States)

    Qiao, Ying; Zhang, Lei; He, Shen; Wen, Hui; Yu, Yi-Min; Cao, Chun-Hua; Li, Hua-Fang

    2016-03-23

    Schizophrenia is a persistent chronic mental illness with an unknown pathogenic mechanism; no empirical laboratory-based tests are available to support the diagnosis of schizophrenia or to identify biomarkers correlated with the therapeutic effect of olanzapine. For this study, 15 female first-episode, drug-naïve patients with schizophrenia and 15 healthy female volunteers were recruited. Tests for blood glucose and lipids were conducted at baseline and after 4 weeks of treatment with olanzapine. UPLC-MS based metabonomic analysis was performed on both case and control groups to identify biomarkers of schizophrenia at baseline and to explore which biomarkers correlated with the therapeutic effect of olanzapine after a 4-week treatment. Compared with the control group, the case group showed significant changes in plasma metabolites. Thirteen distinct metabolites were identified. Among all the therapeutically effective cases, levels of these metabolites appeared to shift towards the normal trend; 8 of the identified 13 metabolites changed dramatically. The metabolites that we found are potential biomarkers for the diagnosis and treatment of schizophrenia.

  14. A dual strategy to improve psychotic patients’ compliance using sustained release quetiapine oral disintegrating tablets

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    Refaat Ahmed

    2016-12-01

    Full Text Available Quetiapine (QT is a short acting atypical antipsychotic drug effective in schizophrenia and bipolar disorder. This study aims at designing a novel dosage form of sustained release taste-masked QT orally disintegrating tablets (ODTs based on solid lipid micro-pellets (SLMPs. QT SLMPs were prepared using the hot melt extrusion technique and utilizing three lipid carriers: Compritol, Precirol and white beeswax either alone or in mixtures. They showed sustained QT release and a taste masking effect. The selected QT SLMP was further blended with an aqueous solution containing polyvinylpyrollidone (2.5 %, croscarmellose sodium (2 % and mannitol (50 %; it was then lyophilized into ODT in a mass ratio of 1:2, respectively. ODTs containing QT SLMPs showed: average wetting time (40.92 s, average oral disintegration time (21.49 s, average hardness (16.85 N and also imparted suitable viscosity to suspend pellets during the lyophilization process. In conclusion, lyophilization is a promising technique for the formulation of multiparticulate systems into ODTs.

  15. A double-blind comparison of the effect of the antipsychotics haloperidol and olanzapine on sleep in mania

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    R.A. Moreno

    2007-03-01

    Full Text Available The effects of haloperidol and olanzapine on polysomnographic measures made in bipolar patients during manic episodes were compared. Twelve DSM-IV mania patients were randomly assigned to receive either haloperidol (mean ± SD final dosage: 5.8 ± 3.8 mg or olanzapine (mean ± SD final dosage: 13.6 ± 6.9 mg in a 6-week, double-blind, randomized, controlled clinical trial. One-night polysomnographic evaluation was performed before and after the haloperidol or olanzapine treatment. Psychopathology and illness severity were rated respectively with the Young Mania Rating Scale (YMRS and the Clinical Global Impressions - Bipolar version (CGI-BP. There was a significant improvement in the YMRS and CGI-BP scores at the end of the study for both groups. Mixed ANOVA used to compare the polysomnographic measures of both drugs demonstrated significant improvement in sleep measures with olanzapine. In the olanzapine group, statistically significant time-drug interaction effects on sleep continuity measures were observed: sleep efficiency (mean ± SEM pre-treatment value: 6.7 ± 20.3%; after-treatment: 85.7 ± 10.9%, total wake time (pre-treatment: 140.0 ± 92.5 min; after-treatment: 55.2 ± 44.2 min, and wake time after sleep onset (pre-treatment: 109.7 ± 70.8 min; after-treatment: 32.2 ± 20.7 min. Conversely, improvement of polysomnographic measures was not observed for the haloperidol group (P > 0.05. These results suggest that olanzapine is more effective than haloperidol in terms of sleep-promoting effects, although olanzapine is comparatively as effective as haloperidol in treating mania. Polysomnography records should provide useful information on how manic states can be affected by psychopharmacological agents.

  16. Celecoxib and omega-3 fatty acids alone and in combination with risperidone affect the behavior and brain biochemistry in amphetamine-induced model of schizophrenia.

    Science.gov (United States)

    El-Sayed El-Sisi, Alaa; Sokkar, Samia Salem; El-Sayed El-Sayad, Magda; Sayed Ramadan, Ehab; Osman, Enass Yossef

    2016-08-01

    The implications of oxidative stress and neuro-inflammation in the pathogenesis of schizophrenia have been elucidated. Despite their effectiveness against positive symptoms of schizophrenia, antipsychotics have limited effectiveness against negative and cognitive symptoms and are associated with remarkable adverse effects. The use of celecoxib or omega-3 in schizophrenia may have beneficial effects. This study aimed to evaluate the possible efficacies of celecoxib, omega-3 or the combination of celecoxib+risperidone and omega-3+ risperidone compared to risperidone on the behavior and brain biochemistry in rats. In the present study, an amphetamine-induced model of schizophrenia in adult male rats was used to evaluate the effects of celecoxib, omega-3, celecoxib+risperidone and omega-3+ risperidone on the behavior of animals and on brain lipid peroxidation or tumor necrosis factor-alpha. In the water maze task, celecoxib, omega-3, celecoxib+risperidone, omega-3+ risperidone significantly decreased the latency time compared to amphetamine-treated group. Celecoxib, omega-3, celecoxib+risperidone, omega-3+risperidone also significantly reversed the decreased spontaneous alternation induced by amphetamine in the Y-maze task. In the social interaction task, groups treated with celecoxib, omega-3, celecoxib+risperidone, omega-3+ risperidone spent less time to recognize foreign animals than animals in the amphetamine-treated group. Increased brain MDA and TNF-α levels due to amphetamine were significantly reduced in groups treated with celecoxib+risperidone or omega-3+ risperidone. The present findings showed that celecoxib or omega-3 can attenuate amphetamine- induced behavioral impairment and these effects may be associated with their ability to decrease lipid peroxidation and cytokine release. Celecoxib or omega-3 may be promising candidates as adjuvant therapy for schizophrenia.

  17. Analisi farmacoeconomica del trattamento di pazienti psicotici cronici con olanzapina, antipsicotici atipici e neurolettici tipici: uno studio regionale

    Directory of Open Access Journals (Sweden)

    Felice Vadruccio

    2005-06-01

    Full Text Available BACKGROUND: Psychotic disorders are a ravaging and costly mental illness. Treatment of these disorders involves pharmacological and non pharmacological resources. Pharmacological therapy with antipsychotic drugs contribute strongly to relieve psychotic patients symptoms. By the end of 90’s the new atypical antipsychotic have been introduced. This kind of drugs is supposed to be more effective but also more expensive compared with the old typical neuroleptics. OBJECTIVE: To compare costs and outcomes associated with 12 months treatment of psychotic disorders using typical and atypical antipsychotics in addition to psychiatric services. Moreover to extend the same comparison among the atypical drugs currently used in the clinical practice (olanzapine, risperidone, quetiapine and clozapine. METHODS AND PATIENTS: A multicentre observational study was carried out in 131 patients affected by psychotic disorders (schizophrenia and bipolar. Data were collected with reference to patients followed by several Psychiatric Services of Regione Puglia (Italy. Patients were classified in five groups (typical neuroleptics, olanzapine, risperidone, quetiapine and clozapine according to their main antipsychotic therapy. Treatment outcomes had been assessed during 12 months of observation considering the patients improvement in their work and social functioning. For these patients we analyzed pharmacological, non pharmacological (medical/ nurse visits, social assistance, rehabilitative sessions and hospital interventions, choosing the perspective of the Italian Mental Health Centers for costs attribution. Moreover indirect costs (caregiver and private assistance to the patient had been evaluated for each group of treatment. The study is based on the observation of real clinical behaviours; therefore patients are not randomised to different treatments. RESULTS: The analysis of treatment outcomes didn’t generate significant differences among the groups despite a

  18. In-depth neuropharmacokinetic analysis of antipsychotics based on a novel approach to estimate unbound target-site concentration in CNS regions: link to spatial receptor occupancy.

    Science.gov (United States)

    Loryan, I; Melander, E; Svensson, M; Payan, M; König, F; Jansson, B; Hammarlund-Udenaes, M

    2016-11-01

    The current study provides a novel in-depth assessment of the extent of antipsychotic drugs transport across the blood-brain barrier (BBB) into various brain regions, as well as across the blood-spinal cord barrier (BSCB) and the blood-cerebrospinal fluid barrier (BCSFB). This is combined with an estimation of cellular barrier transport and a systematic evaluation of nonspecific brain tissue binding. The study is based on the new Combinatory Mapping Approach (CMA), here further developed for the assessment of unbound drug neuropharmacokinetics in regions of interest (ROI), referred as CMA-ROI. We show that differences exist between regions in both BBB transport and in brain tissue binding. The most dramatic spatial differences in BBB transport were found for the P-glycoprotein substrates risperidone (5.4-fold) and paliperidone (4-fold). A higher level of transporter-mediated protection was observed in the cerebellum compared with other brain regions with a more pronounced efflux for quetiapine, risperidone and paliperidone. The highest BBB penetration was documented in the frontal cortex, striatum and hippocampus (haloperidol, olanzapine), indicating potential influx mechanisms. BSCB transport was in general characterized by more efficient efflux compared with the brain regions. Regional tissue binding was significantly different for haloperidol, clozapine, risperidone and quetiapine (maximally 1.9-fold). Spatial differences in local unbound concentrations were found to significantly influence cortical 5-HT2A receptor occupancy for risperidone and olanzapine. In conclusion, the observed regional differences in BBB penetration may potentially be important factors contributing to variations in therapeutic effect and side effect profiles among antipsychotic drugs.

  19. Deltoid injections of risperidone long-acting injectable in patients with schizophrenia.

    Science.gov (United States)

    Quiroz, Jorge A; Rusch, Sarah; Thyssen, An; Palumbo, Joseph M; Kushner, Stuart

    2011-06-01

    Risperidone long-acting injectable was previously approved for treatment of schizophrenia as biweekly injections in the gluteal muscle only. We present data on local injection-site tolerability and safety of risperidone long-acting injectable and comparability of systemic exposure of deltoid versus gluteal injections. Risperidone long-acting injectable was administered in an open-label, single-dose, two-way crossover study, with patients randomized to receive either 25mg gluteal/37.5mg deltoid crossover in two treatment periods or 50mg gluteal/50mg deltoid injections crossover; each treatment period was separated by an 85-day observation period (Study 1) and an open-label, multiple-dose study (4 sequential 37.5mg or 50mg deltoid injections every 2 weeks) (Study 2). The pharmacokinetic results from both the studies have already been published. In Study 1 (n=170), the majority of patients had no local injection-site findings, based on investigator and patient-rated evaluations. In Study 2 (n=53), seven of the 51 patients who received at least two deltoid injections discontinued (primary endpoint). However, none of the discontinuations were due to injection-site related reasons. The 90-percent upper confidence limit of the true proportion of injection-site issue withdrawals was 5.7 percent. No moderate or severe injection-site reactions were reported. Intramuscular injections via the deltoid and gluteal sites are equivalent routes of administration of risperidone long-acting injectable with respect to local injection-site tolerability. The overall safety and tolerability profile of risperidone long-acting injectable was comparable when administered as an intramuscular injection in the deltoid (37.5mg and 50mg) and gluteal (25mg and 50mg) sites.

  20. Risperidone significantly inhibits interferon-gamma-induced microglial activation in vitro.

    Science.gov (United States)

    Kato, Takahiro; Monji, Akira; Hashioka, Sadayuki; Kanba, Shigenobu

    2007-05-01

    Microglia has recently been regarded to be a mediator of neuroinflammation via the release of proinflammatory cytokines, nitric oxide (NO) and reactive oxygen species (ROS) in the central nervous system (CNS). Microglia has thus been reported to play an important role in the pathology of neurodegenerative disease, such as Alzheimer's disease (AD) and Parkinson's disease (PD). The pathological mechanisms of schizophrenia remain unclear while some recent neuroimaging studies suggest even schizophrenia may be a kind of neurodegenerative disease. Risperidone has been reported to decrease the reduction of MRI volume during the clinical course of schizophrenia. Many recent studies have demonstrated that immunological mechanisms via such as interferon (IFN)-gamma and cytokines might be relevant to the pathophysiology of schizophrenia. In the present study, we thus investigated the effects of risperidone on the generation of nitric oxide, inducible NO synthase (iNOS) expression and inflammatory cytokines: interleukin (IL)-1beta, IL-6 and tumor necrosis factor (TNF)-alpha by IFN-gamma-activated microglia by using Griess assay, Western blotting and ELISA, respectively. In comparison with haloperidol, risperidone significantly inhibited the production of NO and proinflammatory cytokines by activated microglia. The iNOS levels of risperidone-treated cells were much lower than those of the haloperidol-treated cells. Antipsychotics, especially risperidone may have an anti-inflammatory effect via the inhibition of microglial activation, which is not only directly toxic to neurons but also has an inhibitory effect on neurogenesis and oligodendrogenesis, both of which have been reported to play a crucial role in the pathology of schizophrenia.

  1. Comparative study on clinically latent aggressiveness inoutpatients with schizophrenia treated with classical antipsychotics and with risperidone

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    Konstantinos Tsirigotis

    2014-03-01

    Full Text Available Objective: The use of neuroleptics causes not only regression of psychotic symptoms; neuroleptics affect also the patients’ mental state which is changing not only due to medications effects but also secondarily, as a result of regression of psychotic symptoms. The aim of this study was evaluation of subjectively felt “silent” (clinically latent hostility and aggressiveness in patients with paranoid schizophrenia treated with typical neuroleptics and risperidone. Material and methods: Sixty patients (30 patients treated with typical neuroleptics and the other 30 – with risperidone were examined with the Polish version of the following tools: Minnesota Multiphasic Personality Inventory (MMPI, Adjective Check List (ACL and Stern Activities Index (SAI. Results: The statistical analysis of the obtained results yielded many statistically significant differences within the intensity of hostility and aggressiveness in the examined groups. Conclusions: The results of this study showed a higher severity of psychological and personality problems in patients treated with typical neuroleptics, as compared to those treated with risperidone. In patients with paranoid schizophrenia treated with risperidone a lower severity of psychopathological, especially schizophrenic and paranoid, symptoms and lower hostility and aggressiveness were found. Considering that risperidone improves verbal functions, it can be assumed that this entails an improvement in the patients’ communicative competences, thereby improving also their interpersonal relationships. The results of this study indicate a higher susceptibility of people in this group to social influences and less hostility and negativity experienced by them.

  2. Combination of Risperidone and Paroxetine for inappropriate sexual behaviors in an adolescent with autism and mental retardation/Otizm ve zeka geriligi olan bir ergende uygunsuz cinsel davranislar icin Risperidone ve Paroxetine birlikte kullanimi

    National Research Council Canada - National Science Library

    Herguner, Sabri; Herguner, Arzu; Cicek, Erdinc

    2012-01-01

    .... In this paper, we describe an adolescent with autistic disorder and mental retardation who developed severe inappropriate sexual behaviors and has been treated successfully with risperidone-paroxetine combination...

  3. Detection of the antipsychotic drug quetiapine in the blood, urine and hair samples of the victim of a drug-facilitated sexual assault

    DEFF Research Database (Denmark)

    Johansen, Sys Stybe

    2017-01-01

    A drug rape facilitated with the sedative antipsychotic drug quetiapine is presented here. A teenage girl and her girlfriend went to the home of an adult couple they had met at a bar. Here, the teenage girl (victim) felt tired after consuming some alcoholic drinks and fell asleep. While she...... was asleep, the others left her at the house alone and returned to the bar. Later, the girl woke up to witness the adult male having intercourse with her, but she was not able to resist the attack. She fell asleep again and slept through the next day and a half, after which she left the house. Forty...... negative. The low level of quetiapine in the hair segment and its absence in the other segments indicate that the victim had only consumed one or a few doses of quetiapine within that period and was not a regular user. This study describes the first drug-facilitated assault involving a single dose...

  4. Quetiapine extended release versus aripiprazole in children and adolescents with first-episode psychosis: the multicentre, double-blind, randomised tolerability and efficacy of antipsychotics (TEA) trial

    DEFF Research Database (Denmark)

    Pagsberg, Anne Katrine; Jeppesen, Pia; Klauber, Dea Gowers

    2017-01-01

    of quetiapine-extended release (quetiapine-ER) versus aripiprazole in children and adolescents with first-episode psychosis, to determine whether differences between the two treatments were sufficient to guide clinicians in their choice of one drug over the other. Methods In this multicentre, double......-blind, randomised trial in seven Danish university clinics, we recruited children and adolescents aged 12–17 years with a diagnosis of ICD-10 schizophrenia-spectrum disorder, delusional disorder, or affective-spectrum psychotic disorder, and psychotic symptoms scoring at least 4 on at least one of the following......-generated concealed sequence with a block size of 8, and stratified by baseline PANSS positive score (≤20 points or >20 points) and age (12–14 years or 15–17 years). Study drugs were administered in identical capsules, and interventions, assessments, and data analysis were done masked. The primary outcome was PANSS...

  5. Clinical Analysis of Olanzapine in the Treatment of Behavioral and Psy-chological Symptoms of 50 Patients with Senile dementia%奥氮平治疗50例老年痴呆患者精神行为症状临床分析

    Institute of Scientific and Technical Information of China (English)

    乐守江

    2014-01-01

    Objective To investigate the efficacy of olanzapine in the treatment of senile dementia. Methods 98 cases of senile dementia patients were divided into two groups, 50 patients in research group were treated with olanzapine, 48 cases in control group were given risperidone. Results The to-tal effective rate of research group was 94.00%, the incidence rate of adverse reaction was 12.00%, to-tal effective rate of the control group was 68.75%, the incidence rate of adverse reaction was 33.33%. The research group has higher efficiency, lower incidence rate of adverse reaction. After treatment, PANSS score decreased more obviously, there was a significant difference between the two groups.(P<0.05). Conclusion Olanzapine in the treatment of behavioral and psychological symptoms of senile de-mentia, can achieve better curative effect, PANSS score decreased significantly.%目的:探讨奥氮平治疗老年痴呆患者的疗效。方法将98例老年痴呆症患者分为两组,研究组50例给予奥氮平治疗,对照组48例给予利培酮治疗。结果研究组总有效率为94.00%,不良反应发生率为12.00%,对照组总有效率为68.75%,不良反应发生率为33.33%,研究组研究组总有效率较高,不良反应发生率较低,治疗后PANSS量表评分下降更明显,两组差异有统计学意义(P<0.05)。结论奥氮平治疗老年痴呆患者精神行为症状,可取得较好的疗效,PANSS量表评分下降明显。

  6. Bipolar CHOICE (Clinical Health Outcomes Initiative in Comparative Effectiveness): a pragmatic 6-month trial of lithium versus quetiapine for bipolar disorder.

    Science.gov (United States)

    Nierenberg, Andrew A; McElroy, Susan L; Friedman, Edward S; Ketter, Terence A; Shelton, Richard C; Deckersbach, Thilo; McInnis, Melvin G; Bowden, Charles L; Tohen, Mauricio; Kocsis, James H; Calabrese, Joseph R; Kinrys, Gustavo; Bobo, William V; Singh, Vivek; Kamali, Masoud; Kemp, David; Brody, Benjamin; Reilly-Harrington, Noreen A; Sylvia, Louisa G; Shesler, Leah W; Bernstein, Emily E; Schoenfeld, David; Rabideau, Dustin J; Leon, Andrew C; Faraone, Stephen; Thase, Michael E

    2016-01-01

    Bipolar disorder is among the 10 most disabling medical conditions worldwide. While lithium has been used extensively for bipolar disorder since the 1970s, second-generation antipsychotics (SGAs) have supplanted lithium since 1998. To date, no randomized comparative-effectiveness study has compared lithium and any SGA. Within the duration of the study (September 2010-September 2013), participants with bipolar I or II disorder (DSM-IV-TR) were randomized for 6 months to receive lithium (n = 240) or quetiapine (n = 242). Lithium and quetiapine were combined with other medications for bipolar disorder consistent with typical clinical practice (adjunctive personalized treatment [APT], excluding any SGA for the lithium + APT group and excluding lithium or any other SGA for the quetiapine + APT group). Coprimary outcome measures included Clinical Global Impressions-Efficacy Index (CGI-EI) and necessary clinical adjustments, which measured number of changes in adjunctive personalized treatment. Secondary measures included a full range of symptoms, cardiovascular risk, functioning, quality of life, suicidal ideation and behavior, and adverse events. Participants improved across all measures, and over 20% had a sustained response. Primary (CGI-EI, P = .59; necessary clinical adjustments, P = .15) and secondary outcome changes were not statistically significantly different between the 2 groups. For participants with greater manic/hypomanic symptoms, CGI-EI changes were significantly more favorable with quetiapine + APT (P = .02). Among those with anxiety, the lithium + APT group had fewer necessary clinical adjustments per month (P = .02). Lithium was better tolerated than quetiapine in terms of the burden of side effects frequency (P = .05), intensity (P = .01), and impairment (P = .01). Despite adequate power to detect clinically meaningful differences, we found outcomes with lithium + APT and quetiapine + APT were not significantly different across 6 months of treatment

  7. Olanzapine-induced hepatopathy in albino rats: A newer model for screening putative hepatoprotective agents, namely silymarin

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    Sengupta Parama

    2010-01-01

    Full Text Available Backgrounds: This study was conducted to establish olanzapine-induced hepatopathy in Wistar albino rats as a newer model to screen putative hepatoprotective agents namely silymarin. Materials and Methods: Albino rats were divided into three groups, namely vehicle control group (CG, olanzapine-treated group (OZ, and olanzapine plus silymarin (OZS treated groups. Both the OZ and OZS groups were treated with the same dose of intraperitoneal olanzapine for 6 weeks and group OZS additionally received oral silymarin. Baseline and terminal hepatic enzymes (SGOT, SGPT, and ALP were measured in all three groups. Results: Histopathological examination of livers of both OZ and OZS groups showed degenerative changes, whereas those of control group showed normal architecture. Liver enzyme levels showed statistically significant rise in comparison to the control group as well as the respective base line values in both the test groups, but the differences in the rise of liver enzymes between the two test groups were not statistically significant. Conclusion: Olanzapine-induced hepatopathy in rats can be used as a model for screening putative hepatoprotective agents and in our setting silymarin has failed to provide any hepatoprotection.

  8. Intramuscular Olanzapine in the Management of Behavioral and Psychological Symptoms in Hospitalized Older Adults: A Retrospective Descriptive Study

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    Silvia Duong

    2015-01-01

    Full Text Available Background. While behavioral and psychological symptoms are frequent in hospitalized older adults with dementia or delirium, data supporting the off-label use of intramuscular atypical antipsychotics remain scarce. We examined the use of short-acting intramuscular (IM olanzapine in hospitalized older adults to manage behavioral and psychological symptoms. Methods. A retrospective observational study of inpatients 65 years or older with at least one order for olanzapine IM during admission in urban Ontario Canada was conducted. Patient demographics, prescriptions for olanzapine IM, reason for administration, perceived effectiveness, adverse events, concurrently prescribed psychotropics, comorbidities, and patient discharge destination were recorded. Results. Among 82 patients aged 65–96 years (mean ± SD 79.3 ± 7.7 85 cases were identified. Cognitive impairment or dementia affected 63.5% and 50.6% had comorbidities. Olanzapine IM was ordered 102 times and 34 patients (41% received at least one dose. The intended efficacy was achieved in 79.4% of 78 cases of 124 doses given (62.9%. Fourteen (41% patients who received doses experienced adverse events, with sedation and hypotension being the most common. Conclusions. Olanzapine IM appears effective in hospitalized older adults but is associated with potential adverse events. Structured monitoring and documentation are needed to ensure safe use in this high-risk population.

  9. Pharmaco-epidemiological description of the population of the Marche Region (central Italy treated with the antipsychotic drug olanzapine

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    Fiorenzo Mignini

    2013-03-01

    Full Text Available BACKGROUND. In Italy, even though olanzapine has been discouraged for treatment of behaviour disorders in older patients affected by dementia, some physicians chose to prescribe for them. In response to this situation, the Italian Drug Agency (Agenzia Italiana del Farmaco, AIFA promulgated a cautionary note. MATERIALS AND METHODS. This study examined epidemiological indices for olanzapine prescriptions between 2004 and 2007 in the Marche Region of central Italy and in its provinces, to assess physician compliance with the AIFA note, and to determine whether there were differences in drug prescription between populations of the same territory, or differences based on gender or age group. RESULTS. Our analyses revealed high olanzapine use among young men and mature women, suggesting that these groups are most prone to psychotic symptoms. Analysis revealed that olanzapine prescription in elderly patients was reduced in some provinces, in line with the AIFA note. CONCLUSIONS. Prudent use of olanzapine prescription, in compliance with the AIFA note, was noted throughout the Region. Furthermore, this work offers details that may be useful in future studies of adverse drug reactions.

  10. DESIGN, DEVELOPMENT AND IN VITRO EVALUATION OF CONTROLLED RELEASE GEL FOR TOPICAL DELIVERY OF QUETIAPINE USING BOX- BEHNKEN DESIGN

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    Hardik K Patel et al

    2012-09-01

    Full Text Available The purpose of this work was to develop and characterize a vesicular drug carrier for topical delivery of Quetiapine to overcome the problems related with oral route that is high first pass metabolism and fluctuating drug plasma concentration. The effects of key formulation variables on entrapment efficiency (EE %, vesicle size and in vitro drug permeation were studied using a Box- Behnken design. Liposomes bearing Quetiapine were prepared by using saturated lipids like 1, 2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC and 1, 2-Distearoyl-sn-glycero-3-phosphocholine (DSPC with relatively less stability problems through rotary evaporation method. The liposomal formulation was characterized for various parameters including EE %, vesicles shape, size distribution, lamellarity, in vitro release study, skin permeation and stability studies. Firstly liposomal suspension was prepared and then previously prepared suspension was incorporated in carbopol 940P gel with an objective of enhancing stability of liposome by avoiding aggregation of vesicles and for better skin permeation. The encapsulation efficiency of drug was found to be ranging from 60.59±4.54% to 83.56±2.97%. Nano liposomes were found to have mean particle size of 405.8±1.1 nm and zeta potential of −10.9±1.54 mV. The optimized liposomal gel showed the desired controlled release of drug uptil 12 h and J flux was also found to be higher than the plain gel of drug. The stability studies proved that both liposome suspension and gel were stable uptil 6 months. Finally, from the research work it could be concluded that the liposome accentuates the transdermal flux of Quetiapine and could be used as an effective carrier for transdermal delivery.

  11. Efficacy and tolerability of Blonanserin in the patients with schizophrenia: a randomized, double-blind, risperidone-compared trial.

    Science.gov (United States)

    Yang, Jaewon; Bahk, Won-Myong; Cho, Hyun-Sang; Jeon, Yang-Whan; Jon, Duk-In; Jung, Hee-Yeon; Kim, Chan-Hyung; Kim, Hee-Cheol; Kim, Yong-Ku; Kim, Young-Hoon; Kwon, Jun-Soo; Lee, Sang-Yeol; Lee, Seung-Hwan; Yi, Jung-Seo; Yoon, Bo-Hyun; Kim, Seung-Hyun

    2010-07-01

    The objective of this study was to evaluate the efficacy and tolerability of blonanserin for the treatment of Korean patients with schizophrenia using a double-blind risperidone-compared design. Patients aged 18 to 65 years with schizophrenia were randomly assigned to blonanserin or risperidone treatment for 8 weeks. The efficacy was assessed using the mean change in Positive and Negative Syndrome Scale score total scores from baseline to week 8. Safety assessments included monitoring of vital signs, a physical examination, laboratory tests, and adverse events. Of 206 randomly enrolled patients, 103 receiving blonanserin and 103 receiving risperidone were included in the analysis. In this study, noninferiority between blonanserin and risperidone was demonstrated. The mean change in the Positive and Negative Syndrome Scale total score at the final evaluation time point was -23.48 +/- 19.73 for the blonanserin group and -25.40 +/- 18.38 for the risperidone group. Adverse events, which occurred less frequently in the blonanserin than in the risperidone group, included dysarthria (P = 0.0288), dizziness (P = 0.0139), increased alanine aminotransferase and aspartate aminotransferase (P = 0.0095 and P = 0.0032, respectively), and increased level blood prolactin (P = 0.0012). On the other hand, the adverse events that occurred more frequently in the blonanserin than in the risperidone group was hand tremor (P = 0.0006). Blonanserin was effective in the treatment of Korean patients with schizophrenia compared with risperidone and was more tolerable with a better safety profile, particularly with respect to prolactin elevation. These findings suggest that blonanserin is useful in the treatment of schizophrenia.

  12. A case of resistant schizophrenia responding at a higher than recommended dose of risperidone without significant side effects

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    Anirban Ray

    2013-01-01

    Full Text Available A patient, diagnosed with schizophrenia, non-responsive to two atypical antipsychotics and partially responsive to the third (risperidone in therapeutic dose, ultimately showed complete response without any unacceptable side-effect in a dose (20mg that was untried previously. This case makes an important observation that high dose of risperidone can be tried in a patient with good results if his clinical condition permits.

  13. Chronic betahistine co-treatment reverses olanzapine's effects on dopamine D₂ but not 5-HT2A/2C bindings in rat brains.

    Science.gov (United States)

    Lian, Jiamei; Huang, Xu-Feng; Pai, Nagesh; Deng, Chao

    2015-01-02

    Olanzapine is widely prescribed for treating schizophrenia and other mental disorders, although it leads to severe body weight gain/obesity. Chronic co-treatment with betahistine has been found to significantly decrease olanzapine-induced weight gain; however, it is not clear whether this co-treatment affects the therapeutic effects of olanzapine. This study investigated the effects of chronic treatment of olanzapine and/or betahistine on the binding density of the serotonergic 5-HT2A (5-HT2AR) and 5-HT2C (5-HT2CR) receptors, 5-HT transporter (5-HTT), and dopaminergic D₂ receptors (D₂R) in the brain regions involved in antipsychotic efficacy, including the prefrontal cortex (PFC), cingulate cortex (Cg), nucleus accumbens (NAc), and caudate putamen (CPu). Rats were treated with olanzapine (1 mg/kg, t.i.d.) or vehicle for 3.5 weeks, and then olanzapine treatment was withdrawn for 19 days. From week 6, the two groups were divided into 4 groups (n=6) for 5 weeks' treatment: (1) olanzapine-only (1 mg/kg, t.i.d.), (2) betahistine-only (9.6 mg/kg, t.i.d.), (3) olanzapine and betahistine co-treatment (O+B), and (4) vehicle. Compared to the control, the olanzapine-only treatment significantly decreased the bindings of 5-HT2AR, 5-HT2CR, and 5-HTT in the PFC, Cg, and NAc. Similar changes were observed in the rats receiving the O+B co-treatment. The olanzapine-only treatment significantly increased the D₂R binding in the Cg, NAc, and CPu, while the betahistine-only treatment reduced D₂R binding. The co-treatment of betahistine reversed the D₂R bindings in the NAc and CPu that were increased by olanzapine. Therefore, chronic O+B co-treatment has similar effects on serotonin transmission as the olanzapine-only treatment, but reverses the D₂R that is up-regulated by chronic olanzapine treatment. The co-treatment maintains the therapeutic effects of olanzapine but decreases/prevents the excess weight gain.

  14. 老年性痴呆精神行为症状实施奥氮平治疗的有效性分析%Effectiveness of behavioral and psychological symptoms of senile dementia implementation of olanzapine treatment

    Institute of Scientific and Technical Information of China (English)

    何炳接

    2014-01-01

    目的:对奥氮平治疗老年性痴呆精神行为症状的有效性实施分析。方法随机选取我院2012年1月-2013年12月实施治疗的120例老年性痴呆精神行为症状患者,并将其平均分成对照组和观察组两组,每组60例患者,其中对照组患者采用利培酮实施治疗,观察组患者则采用奥氮平实施治疗。对比分析两组患者的临床治疗效果和不良反应发生率。结果其中观察组患者的治疗总有效率为90.0%,对照组患者仅为76.7%,两组之间差异显著,对比具有统计学意义(P<0.05);观察组患者的各项不良反应发生率也均明显的低于对照组,两组之间差异显著,对比具有统计学意义(P<0.05)。结论在老年性痴呆精神行为症状中,采用奥氮平进行治疗,其不但有助于对其临床治疗效果进行提高,同时还可以有效降低患者的不良反应发生率,因此可以说其值得推广应用。%Purpose: The effectiveness of the implementation of olanzapine treatment of senile dementia behavioral and psychological symptoms of analysis. Method: I randomly selected hospital in January 2012 -2013 in December implemented 120 cases of behavioral and psychological symptoms of senile dementia patients treated, and were divided into a control group and observation group two groups of 60 patients, including the control group were treated with risperidone implementation of treatment, the observation group were then implemented using olanzapine treatment. Comparative analysis of the two groups of patients with clinical outcomes and incidence of adverse reactions. Results: Observed among patients treated group total effective rate was 90.0% in the control group of patients was only 76.7%, a significant difference between the two groups, compared with statistical significance (P <0.05); the incidence of adverse reactions observed in patients also were significantly lower than the control group, a

  15. LC-MS/MS method applied to preclinical pharmacokinetic investigation of olanzapine-loaded lipid-core nanocapsules

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    Frantiescoli A. Dimer

    2014-01-01

    Full Text Available In spite of different methods reported in the literature to determine olanzapine in biological fluids, all of them used high volumes of plasma. Therefore, the purpose of this paper was to develop an LC-MS/MS method using small plasma volume (0.1 mL to apply in a preclinical pharmacokinetic investigation. The method was linear over the concentration ranges of 10 - 1000 ng mL-1. Extraction recoveries, stability, and validation parameters were evaluated. Results were within the acceptable limits of international guidelines. A significant decrease in clearance led to a significant 2.26-times increase in AUC0 - 6h of olanzapine-loaded lipid-core nanocapsules compared with free-olanzapine.

  16. Neuroanatomical substrates of the disruptive effect of olanzapine on rat maternal behavior as revealed by c-Fos immunoreactivity.

    Science.gov (United States)

    Zhao, Changjiu; Li, Ming

    2012-12-01

    Olanzapine is one of the most widely prescribed atypical antipsychotic drugs in the treatment of schizophrenia. Besides its well-known side effect on weight gain, it may also impair human parental behavior. In this study, we took a preclinical approach to examine the behavioral effects of olanzapine on rat maternal behavior and investigated the associated neural basis using the c-Fos immunohistochemistry. On postpartum days 6-8, Sprague-Dawley mother rats were given a single injection of sterile water or olanzapine (1.0, 3.0 or 5.0mg/kg, sc). Maternal behavior was tested 2h later, after which rats were sacrificed and brain tissues were collected. Ten brain regions that were either implicated in the action of antipsychotic drugs and/or in the regulation of maternal behavior were examined for c-Fos immunoreactivity. Acute olanzapine treatment dose-dependently disrupted various components of maternal behavior (e.g., pup retrieval, pup licking, nest building, crouching) and increased c-Fos immunoreactivity in the medial prefrontal cortex (mPFC), nucleus accumbens shell and core (NAs and NAc), dorsolateral striatum (DLSt), ventral lateral septum (LSv), central amygdala (CeA) and ventral tegmental area (VTA), important brain areas generally implicated in the incentive motivation and reward processing. In contrast, olanzapine treatment did not alter c-Fos in the medial preoptic nucleus (MPN), ventral bed nucleus of the stria terminalis (vBST) and medial amygdala (MeA), the core brain areas directly involved in the mediation of rat maternal behavior. These findings suggest that olanzapine disrupts rat maternal behavior primarily by suppressing incentive motivation and reward processing via its action on the mesocorticolimbic dopamine systems, other limbic and striatal areas, but not by disrupting the core processes involved in the mediation of maternal behavior in particular.

  17. Predictors of antipsychotic monotherapy with olanzapine during a 1-year naturalistic study of schizophrenia patients in Japan

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    Ye W

    2012-01-01

    Full Text Available Wenyu Ye1, Haya Ascher-Svanum2, Jennifer A Flynn3, Yuka Tanji3, Michihiro Takahashi3,41Lilly Suzhou Pharmaceutical Co, Shanghai, People's Republic of China; 2Eli Lilly and Company, Indianapolis, IN, USA; 3Lilly Research Laboratories Japan, Eli Lilly Japan K.K., Kobe, 4Terauchi-Takahashi Psychiatric Clinic, Ashiya, JapanPurpose: Although expert guidelines for the treatment of schizophrenia recommend antipsychotic monotherapy, the use of antipsychotic polypharmacy is common. This study identified characteristics that differentiate patients with schizophrenia who are treated with olanzapine monotherapy versus polypharmacy in usual care in Japan.Patients and methods: In a large (N = 1850 prospective, observational study, Japanese patients with schizophrenia who initiated treatment with olanzapine were followed for 1 year. Consistent with past research, antipsychotic polypharmacy was defined as the concurrent use of olanzapine and another antipsychotic for at least 60 days. Switching was defined as discontinuing a prior antipsychotic therapy rather than augmenting the medication regimen. Predictors of antipsychotic monotherapy were based on information available at the time of olanzapine initiation. Baseline characteristics were compared using t-tests and Χ2 tests. Stepwise logistic regression was used to identify independent predictors of monotherapy.Results: Patients treated with olanzapine monotherapy (43.2% differed from those treated with antipsychotic polypharmacy (56.8% on demographics, treatment history, baseline symptom levels, functional levels, and treatment-emergent adverse events. Stepwise logistic regression identified multiple variables that significantly predicted monotherapy: older age, shorter duration of schizophrenia, outpatient status, comorbid medical conditions, lower body mass index, no prior anticholinergic use, no prior mood stabilizer use, and switching from a previous antipsychotic (typical or atypical

  18. 非典型抗精神病药物对女性精神分裂症患者泌乳素水平的影响%Influence of atypical antipsychotics on the level of prolactin in female schizophrenia

    Institute of Scientific and Technical Information of China (English)

    徐开营; 张慧芳; 沈利; 赵洁

    2014-01-01

    Objective To investigate the influence of atypical antipsychotics on the level of prolactin in female schizophre-nia.Methods 18 to 45 years old female patients with schizophrenia in hospital were randomly allocated to four groups treated with olanzapine ,risperidone ,quetiapine and aripiprazole respectively ,30 cases in each group. Prolactin were measured at base-line and after 4 ,8 weeks of treatment respectively ,with menstruation and spilled milk recorded. Results The level of prolactin was increased in both olanzapine and risperidone groups (P< 0.01) ,especially in risperidone group as the treatment contin-ues. There was no significant difference between quetiapine and aripiprazole group. Conclusion Both olanzapine and risperi-done can increase the level of prolactin ,while either quetiapine or aripiprazole has no effect on the level of serum prolactin.%目的:探讨非典型抗精神病药物对女性精神分裂症泌乳素的影响。方法选择18~45岁女性精神分裂症住院患者,随机分为奥氮平组、利培酮组、喹硫平组、阿立哌唑组,每组30例。于治疗开始第0、4、8周检测血清泌乳素。并记录月经、溢乳等情况。结果与治疗前相比,奥氮平组及利培酮组患者的血清泌乳素水平升高(P<0.01),随着治疗时间的延长利培酮组患者的泌乳素水平明显升高,并有相应的临床症状;喹硫平组及阿立哌唑组患者的血清泌乳素水平无明显升高。结论奥氮平和利培酮均可引起血清泌乳素水平升高,并出现月经延迟、溢乳等症状。喹硫平及阿立哌唑对血清泌乳素无影响。

  19. Pharmacogenetics and olanzapine treatment: CYP1A2*1F and serotonergic polymorphisms influence therapeutic outcome.

    Science.gov (United States)

    Laika, B; Leucht, S; Heres, S; Schneider, H; Steimer, W

    2010-02-01

    Psychiatric pharmacotherapy with olanzapine is commonplace. We investigated the influence of CYP1A2*1F (-163A, rs762551) and serotonergic polymorphisms on olanzapine serum concentrations and clinical outcome in a naturalistic clinical setting. Included were 124 Caucasian psychiatric inpatients treated with olanzapine for at least 4 weeks with steady-state serum concentrations available for 73 patients. The CYP1A2*1F polymorphism was reported to affect the inducibility of CYP1A2. In our study population, CYP1A2*1F/*1F genotype alone resulted in a 22% reduction of dose-/body weight-normalized olanzapine serum concentrations compared to homo- and heterozygote carriers of CYP1A2*1A (both groups without inducers). This effect was independent of the well-known effect of inducing agents (here tobacco smoke and carbamazepine which led to on average 28% lower concentrations in CYP1A2*1A carriers and 26% lower concentrations in CYP1A2*1F/*1F carriers). Consistently, patients with the CYP1A2*1F/*1F genotype taking inducers had 22% lower concentrations compared to CYP1A2*1A carriers taking inducers. The influence of genotype alone remained significant after Bonferroni's post hoc test. Higher olanzapine concentrations were significantly correlated with better improvement of paranoid and depressive symptoms in patients with schizophrenic disorders (Spearman's r=0.5, P=0.026 and P=0.006, respectively). No relationship between serum concentrations and the side effects (DOTES) score was detected. However, patients with the 5-HTR2A intron 2 (rs7997012) AA genotype suffered from more pronounced side effects compared to carriers of the GA or GG genotype (P=0.018 and P=0.002). Short-term weight gain under olanzapine therapy was significantly lower for 5-HTR2C -759 T-allele carriers (P=0.011). Our data suggest that the CYP1A2*1F/*1F genotype exhibits a significant influence on olanzapine concentrations independent of other inducing factors. Thus, CYP1A2*1F genotyping may be useful for

  20. Double-blind comparison of ziprasidone and risperidone in the treatment of Chinese patients with acute exacerbation of schizophrenia

    Directory of Open Access Journals (Sweden)

    Hongyan Zhang

    2011-03-01

    Full Text Available Hongyan Zhang1, Huafang Li2, Liang Shu1, Niufan Gu2, Gang Wang3, Yongzhen Weng3, Shiping Xie4, Xinbao Zhang4, Ting Li5, Cui Ma5, Wei Yu6, Bruce Parsons7, Manjula Schou81Institute of Mental Health, Peking University, Beijing, China; 2Shanghai Mental Health Center, Shanghai, China; 3Capital Medical University, Beijing An Ding Hospital, Beijing, China; 4Nanjing Brain Hospital, Nanjing, China; 5Guangzhou Brain Hospital, Guangzhou, China; 6Pfizer China, Beijing, China; 7Pfizer Inc, New York, NY, USA; 8Pfizer Australia, Sydney, AustraliaBackground: The aim of the study was to evaluate the efficacy and safety of ziprasidone versus risperidone in Chinese subjects with acute exacerbation of schizophrenia.Methods: In patients meeting the Chinese Classification of Mental Disorders criteria for schizophrenia and with a Positive and Negative Syndrome Scale (PANSS total score ≥60 were randomly assigned to six weeks of double-blind treatment with ziprasidone 40–80 mg twice daily or risperidone 1–3 mg bid, flexibly dosed. Noninferiority was demonstrated if the upper limit of the two-sided 95% confidence interval (CI for the difference in PANSS total score improvement from baseline in the evaluable population was smaller than the prespecified noninferiority margin of 10 units.Results: The intent-to-treat population comprised 118 ziprasidone-treated and 121 risperidone-treated subjects. Improvement (reduction from baseline to week 6 in PANSS total score was (-35.6 [95% CI: -38.6, -32.6] for ziprasidone and (-37.1 [95% CI: -39.9, -34.4] for risperidone. Noninferiority was demonstrated in the evaluable population with a difference score of 1.5 [95% CI: -2.5, 5.5]. Mean prolactin levels decreased at week 6 compared with baseline for ziprasidone (-3.5 ng/mL, but significantly increased for risperidone (61.1 ng/mL; P < 0.001. More risperidone-treated subjects (14.9% than ziprasidone-treated subjects (4.2% reported weight gain ≥7%. Akathisia and somnolence in

  1. Efficacy of olanzapine in symptom relief and quality of life in gastric cancer patients receiving chemotherapy

    Directory of Open Access Journals (Sweden)

    Novin Nikbakhsh

    2016-01-01

    Full Text Available Background: Considering the incidence and prevalence rates of gastric cancer in Mazandaran Province of Iran, this research was performed to evaluate the efficacy and safety of olanzapine in symptom relief and quality of life (QOL improvement of gastric patients receiving chemotherapy. Materials and Methods: This clinical trial was conducted on thirty new cases of gastric cancer patients whose treatment protocol was planned on chemotherapy and were allocated into two groups by simple random sampling. Intervention group (15 patients received olanzapine tablets (2.5–10 mg/day a day before the beginning of chemotherapy; in the 1st day of chemotherapy to 8 weeks after chemotherapy, besides the routine treatment regimens. The control group received only the routine treatment regimens. The patients were followed for 8 weeks after intervention. All of the patients were assessed with Hospital Anxiety and Depression Scale (HADS and WHO-QOL-BREF questionnaires; further, Rhodes index was used to evaluate nausea and vomiting (N/V status. Results: All the recruited patients continued the allocated interventions (no lost to follow-up. N/V decreased in the case group, but the difference was not statistically significant (P = 0.438. The patients' appetite and body mass index increased (P = 0.006. Anxiety and depression subscales of HADS had significant differences between the two groups (P 0.05. No significant increase was observed in fasting and 2-h postprandial blood glucose and lipid profile (P > 0.05. Conclusion: Olanzapine can be considered as an effective drug to increase appetite and decrease anxiety and depression in patients with gastric cancer.

  2. Single dose bioequivalence study of two brands of olanzapine 10 mg tablets in Iranian healthy volunteers.

    Science.gov (United States)

    Zakeri-Milani, P; Islambulchilar, Z; Ghanbarzadeh, S; Valizadeh, H

    2013-07-01

    This single dose, randomized, open label, 2-period and crossover study in healthy Iranian adult volunteers was conducted to compare the bioavailability of 2 branded formulations of olanzapine 10 mg tablets. 24 volunteers received one tablet of each olanzapine 10 mg formulation. Drugs were administered after a 12 h overnight fast in each of 2 treatment days which separated by a 2-week washout period. Serial blood samples were collected over a period of 72 h. Plasma was analyzed using a validated high performance liquid chromatography method with ultraviolet detection in the range of 2-24 ng/mL with a lower limit of quantitation of 1.25 ng/mL. A non-compartmental method was employed to determine the pharmacokinetic properties (Cmax, Tmax, AUC0-t, AUC0-∞ and T1/2) to test to bioequivalence. Cmax, AUC0-t and AUC0-∞ were used to test the bioequivalence after log-transformation of plasma data. The mean (SD) Cmax, AUC0-t and AUC0-∞ for the test formulation were 15.82 (3.15) ng/mL, 447.19 (100.64) ng.h/L and 570.75 (130.55) ng.h/L respectively. Corresponding values for the test formulation were 15.72 (4.25) ng/mL, 440.37 (98.75) ng.h/mL and 558.66 (129.57) ng.h/mL. For test formulation vs. the reference formulation, the 90% CIs of the least squares mean test/reference ratios of Cmax, AUC0-t and AUC0-∞ were 97.6-110.0%, 96.4-109.4% and 97.3-109.2%. In these volunteers, based on the FDA regulatory definition, results from the pharmacokinetic analysis suggested that the test and reference formulations of olanzapine 10 mg tablets were bioequivalent.

  3. Long-term treatment with olanzapine in hospital conditions: Prevalence and predictors of the metabolic syndrome

    Directory of Open Access Journals (Sweden)

    Popović Irena

    2015-01-01

    Full Text Available Introduction. The risk of metabolic abnormalities is greatly increased in schizophrenic patients started on an atypical antipsychotic medication. Patients with psychiatric disorders exceed mortality ranges resulting from, among others, increased risk of cardiovascular events. Other factors contributing to the development of metabolic syndrome include prolonged duration of illness, increasing age, female sex and lifestyle factors. Objective. This cross-sectional study was taken up to assess the prevalence of the metabolic syndrome (MetS in schizophrenic patients receiving olanzapine monotherapy for at least six months and to determine the most important risk factors associated with metabolic syndrome presence in these patients. Methods. A total of 93 long term hospitalized schizophrenic patients (71 men, 22 women, had a screening of the following: case-history data, psychiatric scales, anthropometric measures, blood (fasting glucose, lipid status, C-reactive protein - CRP and urine samples (microalbuminuria. Results. Prevalence of MetS according to International Diabetes Federation criteria in our study was 34.4%. The multivariate analysis distinguished the following significant predictors of MetS presence (in order of appearance: data about diabetes mellitus in family history (p=0.002, body mass index >25 kg/m2 (p=0.002, hyperlipidemia in family history (p=0.008, and elevated CRP value (p=0.042. Conclusion. High rate of MetS in patients treated with olanzapine in this study exceeds MetS prevalence in general population. Among observed parameters, our study pointed to several “high risk” predictors associated with MetS presence. Regular monitoring of cardiometabolic risk factors is highly recommended. Positive heredity distress mentioned above may direct a psychiatrist to prescribe some other drug than olanzapine in the long term treatment of schizophrenia.

  4. 'Myxoedema madness' with Capgras syndrome and catatonic features responsive to combination olanzapine and levothyroxine.

    Science.gov (United States)

    Shlykov, Maksim A; Rath, Swapnil; Badger, Alison; Winder, Gerald Scott

    2016-09-09

    We present the case of an elderly woman with hypothyroidism and no psychiatric history who presented with new onset of psychosis, paranoia, catatonic features and Capgras syndrome (CS). This case illustrates the spectrum of neuropsychiatric symptoms that may accompany hypothyroidism and the importance of considering thyroid dysfunction as a primary contributor to severe psychiatric symptoms, especially in previously stable patients. We demonstrate the effectiveness of combination levothyroxine and olanzapine, with its favourable cardiac profile, in the treatment of myxoedema madness. Antipsychotics can be weaned once psychiatric symptoms resolve and hormone levels are stabilised. 2016 BMJ Publishing Group Ltd.

  5. Use of Orally Disintegrating Olanzapine During Electroconvulsive Therapy for Prevention of Postictal Agitation.

    Science.gov (United States)

    Hermida, Adriana P; Janjua, A Umair; Tang, Yilang; Syre, Sharyn R; Job, Gregory; McDonald, William M

    2016-11-01

    A major medical problem for patients undergoing electroconvulsive therapy (ECT) is the occurrence of postictal agitation (PIA). This phenomenon is associated with confusion and disorientation that can have severe clinical implications for the safety of the patient and health care professionals. Many different pharmacological strategies have been used to prevent PIA. We present data on 40 patients who suffered from PIA after a course of ECT and evaluate the prophylactic use of orally disintegrating olanzapine in the prevention of PIA in subsequent ECT treatments.

  6. Management of symptoms associated with advanced cancer: olanzapine and mirtazapine. A World Health Organization project.

    Science.gov (United States)

    Davis, Mellar P; Khawam, Elias; Pozuelo, Leo; Lagman, Ruth

    2002-08-01

    Advanced cancer patients are polysymptomatic and often receive multiple medications for symptom relief. Common symptoms include anorexia, weight loss, delirium and depression. Olanzapine and mirtazapine may have several advantages over older agents despite increased acquisition costs. Both medications can treat several symptoms with a low risk for drug-drug interactions and with only once- or twice-daily dosing. Drug side effects are low, compared with more conventionally used agents. The pharmacokinetics and pharmacodynamics of both agents are unique and explain many of the benefits. More research and clinical experience will be necessary to define their role in the palliation of advanced cancer.

  7. Development of novel risperidone implants using blends of polycaprolactones and in vitro in vivo correlation studies.

    Science.gov (United States)

    Navitha, Aerrolla; Jogala, Satheesh; Krishnamohan, Chinnala; Aukunuru, Jithan

    2014-04-01

    The objective of this study was to develop a novel implant containing risperidone intended for long-term treatment in Schizophrenia utilizing in vitro in vivo correlation (IVIVC) studies. Different implants (F1-F8) containing an antipsychotic drug, risperidone, were prepared using a hot melt extrusion technique by taking polycaprolactones of different molecular weights (Mwt. 15000, 45000, 80000) either alone or as their blends, and PLGA (75:25). The implants contained 40% of the drug. After fabrication, the implants were characterized for various in vitro properties such as drug release and physical strength. Prior to conducting drug release studies, optimum drug release method was developed based on IVIVC studies. An optimized formulation based on drug release and physical strength at the end of fabrication was selected from the various implants fabricated. The bioactivity, reversibility, and IVIVC of optimized formulation were determined using pharmacokinetic studies in rats. Short-term stability studies were conducted with optimized formulation. Drug release depended on polymer molecular weight. Implant fabricated using 50:50 polycaprolactone 45,000 and polycaprolactone 80,000 was considered optimized implant. Optimized formulation selected released the drug for 3-months in vitro and was physically rigid. The optimized implant was able to release the drug in vivo for a period of 3 months, the implants are reversible throughout the delivery interval and, a 100% IVIVC was achieved with optimized implant, suggesting the development of 3-month drug-releasing implant for risperidone. The optimized implant was stable for 6 months at room temperature (25°C) and 45°C. A novel implant for risperidone was successfully prepared and evaluated.

  8. Development of novel risperidone implants using blends of polycaprolactones and in vitro in vivo correlation studies

    Directory of Open Access Journals (Sweden)

    Aerrolla Navitha

    2014-01-01

    Full Text Available The objective of this study was to develop a novel implant containing risperidone intended for long-term treatment in Schizophrenia utilizing in vitro in vivo correlation (IVIVC studies. Different implants (F1-F8 containing an antipsychotic drug, risperidone, were prepared using a hot melt extrusion technique by taking polycaprolactones of different molecular weights (Mwt. 15000, 45000, 80000 either alone or as their blends, and PLGA (75:25. The implants contained 40% of the drug. After fabrication, the implants were characterized for various in vitro properties such as drug release and physical strength. Prior to conducting drug release studies, optimum drug release method was developed based on IVIVC studies. An optimized formulation based on drug release and physical strength at the end of fabrication was selected from the various implants fabricated. The bioactivity, reversibility, and IVIVC of optimized formulation were determined using pharmacokinetic studies in rats. Short-term stability studies were conducted with optimized formulation. Drug release depended on polymer molecular weight. Implant fabricated using 50:50 polycaprolactone 45,000 and polycaprolactone 80,000 was considered optimized implant. Optimized formulation selected released the drug for 3-months in vitro and was physically rigid. The optimized implant was able to release the drug in vivo for a period of 3 months, the implants are reversible throughout the delivery interval and, a 100% IVIVC was achieved with optimized implant, suggesting the development of 3-month drug-releasing implant for risperidone. The optimized implant was stable for 6 months at room temperature (25°C and 45°C. A novel implant for risperidone was successfully prepared and evaluated.

  9. Risperidone-induced priapism in an autistic child: a case report

    OpenAIRE

    Aabbassi, Bouchra; Benali, Abdeslam; Asri, Fatima

    2016-01-01

    Background Priapism is a prolonged stimulation with painful, persistent penile erection unaccompanied by sexual desire. It is a rare but serious urological emergency. Risperidone is an atypical antipsychotic widely prescribed for the treatment of behavior problems in children with autism spectrum disorder. It seems associated with priapism in children. Case presentation We present a case of a 12-year-old Moroccan boy diagnosed with autism spectrum disorder who developed priapism while on an e...

  10. Risperidone Long-Acting Injections: Successful Alternative Deltoid Muscle Injections for Refractory Schizophrenia

    OpenAIRE

    Saxena, Arjun; Grace, Jeffery; Olympia, Josie L.; Trigoboff, Eileen; Watson, Thomas; Cushman, Sharon; Newcomer, David

    2008-01-01

    Treatment-resistant paranoid schizophrenia is often addressed with long-term intramuscular preparations of conventional antipsychotics (haloperidol and fluphenazine), which can be associated with the development of painful, lumpy nodules at the injection site. In this article, we present a case example of a 58-year-old male patient with paranoid schizophrenia who was treated with risperidone long-acting injection given into the deltoid muscle instead of the US Food and Drug Administration (FD...

  11. A Rapid and Selective LC-MS/MS Method for Quantification of Quetiapine in Human Plasma and its Application to Pharmacokinetic Study on Indian Schizophrenia Patients

    Directory of Open Access Journals (Sweden)

    S. Ravinder

    2011-01-01

    Full Text Available A rapid, robust and selective high pressure liquid chromatography–positive electrospray ionization tandem mass spectrometry method has been developed and validated for the quantification of quetiapine (QUE in human plasma with K2EDTA using oxcarbazepine (IS as an internal standard. Analyte and internal standard were extracted from human plasma by solid-phase extraction using acetonitrile. The eluted samples were chromatographed on a C18 column by using a 10:75:15v/v mixture of ammonium formate buffer (5 mM, pH 4.50 and acetonitrile and methanol as an isocratic mobile phase at a flow rate of 0.4 mL/min and analyzed by mass spectrometry in the multiple reaction monitoring mode using the respective [M+H]+ ions, m/z 384.3/253.2 for Quetiapine and m/z 253.1/208.1 for the internal standard. The assay exhibited a linear dynamic range of 5.01 - 2501.04 ng/mL for quetiapine in human plasma. Acceptable precision and accuracy were obtained for concentrations over the standard curve range. A run time of 2.5 min for each sample made it possible to analyze 300 patient plasma samples per day. The validated method has been successfully used for the estimation of quetiapine in real time schizophrenia patient’s plasma samples for pharmacokinetic study.

  12. Acute anxiolytic effects of quetiapine during virtual reality exposure--a double-blind placebo-controlled trial in patients with specific phobia.

    Science.gov (United States)

    Diemer, Julia; Domschke, Katharina; Mühlberger, Andreas; Winter, Bernward; Zavorotnyy, Maxim; Notzon, Swantje; Silling, Karen; Arolt, Volker; Zwanzger, Peter

    2013-11-01

    Anxiety disorders are among the most frequent psychiatric disorders. With regard to pharmacological treatment, antidepressants, the calcium modulator pregabalin and benzodiazepines are recommended according to current treatment guidelines. With regard to acute states of anxiety, so far practically only benzodiazepines provide an immediate anxiolytic effect. However, the risk of tolerance and dependency limits the use of this class of medication. Therefore, there is still a need for alternative pharmacologic strategies. Increasing evidence points towards anxiety-reducing properties of atypical antipsychotics, particularly quetiapine. Therefore, we aimed to evaluate the putative acute anxiolytic effects of this compound, choosing the induction of acute anxiety in patients with specific phobia as a model for the evaluation of ad-hoc anxiolytic properties in a proof-of-concept approach. In a randomized, double-blind, placebo-controlled study, 58 patients with arachnophobia were treated with a single dose of quetiapine XR or placebo prior to a virtual reality spider challenge procedure. Treatment effects were monitored using rating scales for acute anxiety as well as measurements of heart rate and skin conductance. Overall, quetiapine showed significant anxiolytic effects compared to placebo. However, effects were not seen on the primary outcome measure (VAS Anxiety), but were limited to somatic anxiety symptoms. Additionally, a significant reduction of skin conductance was observed. Further exploratory analyses hint towards a mediating role of the (COMT) val158met genotype on treatment response. The present results thus suggest a possible suitability of quetiapine in the acute treatment of anxiety, particularly with regard to somatic symptoms.

  13. Quetiapine versus aripiprazole in children and adolescents with psychosis--protocol for the randomised, blinded clinical Tolerability and Efficacy of Antipsychotics (TEA) trial

    DEFF Research Database (Denmark)

    Pagsberg, Anne Katrine; Jeppesen, Pia; Klauber, Dea Gowers

    2014-01-01

    BACKGROUND: The evidence for choices between antipsychotics for children and adolescents with schizophrenia and other psychotic disorders is limited. The main objective of the Tolerability and Efficacy of Antipsychotics (TEA) trial is to compare the benefits and harms of quetiapine versus aripipr...

  14. Low doses of mirtazapine or quetiapine for transient insomnia : A randomised, double-blind, cross-over, placebo-controlled trial

    NARCIS (Netherlands)

    Karsten, Julie; Hagenauw, Loes A.; Kamphuis, Jeanine; Lancel, Marike

    Low doses of the antidepressant mirtazapine or the neuroleptic quetiapine are often prescribed off-label for insomnia. However, studies on the effects on sleep and hangover effects the following day are scarce. In this randomised, double-blind, cross-over, placebo-controlled trial, the influence of

  15. On-Line Organic Solvent Field Enhanced Sample Injection in Capillary Zone Electrophoresis for Analysis of Quetiapine in Beagle Dog Plasma.

    Science.gov (United States)

    Cao, Yuqing; Wen, Jun; Zhou, Tingting; Fan, Guorong

    2016-01-21

    A rapid and sensitive capillary zone electrophoresis (CZE) method with field enhanced sample injection (FESI) was developed and validated for the determination of quetiapine fumarate in beagle dog plasma, with a sample pretreatment by LLE in 96-well deep format plate. The optimum separation was carried out in an uncoated 31.2 cm × 75 μm fused-silica capillary with an applied voltage of 13 kV. The electrophoretic analysis was performed by 50 mM phosphate at pH 2.5. The detection wavelength was 210 nm. Under these optimized conditions, FESI with acetonitrile enhanced the sensitivity of quetiapine about 40-50 folds in total. The method was suitably validated with respect to stability, specificity, linearity, lower limit of quantitation, accuracy, precision and extraction recovery. Using mirtazapine as an internal standard (100 ng/mL), the response of quetiapine was linear over the range of 1-1000 ng/mL. The lower limit of quantification was 1 ng/mL. The intra- and inter-day precisions for the assay were within 4.8% and 12.7%, respectively. The method represents the first application of FESI-CZE to the analysis of quetiapine fumarate in beagle dog plasma after oral administration.

  16. On-Line Organic Solvent Field Enhanced Sample Injection in Capillary Zone Electrophoresis for Analysis of Quetiapine in Beagle Dog Plasma

    Directory of Open Access Journals (Sweden)

    Yuqing Cao

    2016-01-01

    Full Text Available A rapid and sensitive capillary zone electrophoresis (CZE method with field enhanced sample injection (FESI was developed and validated for the determination of quetiapine fumarate in beagle dog plasma, with a sample pretreatment by LLE in 96-well deep format plate. The optimum separation was carried out in an uncoated 31.2 cm × 75 μm fused-silica capillary with an applied voltage of 13 kV. The electrophoretic analysis was performed by 50 mM phosphate at pH 2.5. The detection wavelength was 210 nm. Under these optimized conditions, FESI with acetonitrile enhanced the sensitivity of quetiapine about 40–50 folds in total. The method was suitably validated with respect to stability, specificity, linearity, lower limit of quantitation, accuracy, precision and extraction recovery. Using mirtazapine as an internal standard (100 ng/mL, the response of quetiapine was linear over the range of 1–1000 ng/mL. The lower limit of quantification was 1 ng/mL. The intra- and inter-day precisions for the assay were within 4.8% and 12.7%, respectively. The method represents the first application of FESI-CZE to the analysis of quetiapine fumarate in beagle dog plasma after oral administration.

  17. Sensorimotor gating and habituation in antipsychotic-naive, first-episode schizophrenia patients before and after 6 months' treatment with quetiapine

    DEFF Research Database (Denmark)

    Aggernaes, Bodil; Glenthøj, Birte Yding; Ebdrup, Bjorn H

    2010-01-01

    . Treatment with quetiapine for 6 months increased male PPI to a level where it was no longer statistically different from the controls. The much smaller group of females did not show PPI deficits at baseline. In addition, compared to controls, patients appeared highly aroused and showed a strong yet non...

  18. Amenorrhoea - consequence of combined treatment with sulpiride and risperidone in a patient suffering from schizophrenia.

    Science.gov (United States)

    Peitl, Marija Vucić; Pavlović, Eudard; Peitl, Antun; Peitl, Vjekoslav

    2010-03-01

    It is well documented that sulpiride causes hormonal adverse events, like amenorrhoea and galactorrhea, due to its mechanism of action. Furthermore, risperidone can produce amenorrhoea and galactorrhea also, due to its mechanism of action, which differs from that of sulpiride. This case report is of a patient that was treated with large doses of sulpiride, but did not develop an adverse event like amenorrhoea. However, when risperidone was introduced into therapy it leads to the onset of amenorrhoea. Gynecologist saw it as the beginning of menopause. General practitioner questioned the existence of an intra-cerebral process that could produce amenorrhoea as well. Therefore, the patient was sent to perform an MRI of the brain, under work diagnosis of pituitary adenoma, which was later ruled out as a cause of the illness. Well experienced psychiatrist linked the loss of menstruation with the adverse event profile of sulpiride and therefore gradually discontinued sulpiride from therapy, while risperidone was left and subsequently menstrual cycle was restored. Good knowledge of adverse events profile of antipsychotic medication used, especially when used in a combination, allows us to correctly question appearance of adverse events, to adequately treat them and lowers the cost of unneeded medical procedures.

  19. Risperidone oral disintegrating mini-tablets: A robust-product for pediatrics

    Directory of Open Access Journals (Sweden)

    El-Say Khalid M.

    2015-12-01

    Full Text Available This study was aimed at developing risperidone oral disintegrating mini-tablets (OD-mini-tablets as age-appropriate formulations and to assess their suitability for infants and pediatric use. An experimental Box-Behnken design was applied to assure high quality of the OD-mini-tablets and reduce product variability. The design was employed to understand the influence of the critical excipient combinations on the production of OD-mini-tablets and thus guarantee the feasibility of obtaining products with dosage form uniformity. The variables selected were mannitol percent in Avicel (X1, swelling pressure of the superdisintegrant (X2, and the surface area of Aerosil as a glidant (X3. Risperidone-excipient compatibilities were investigated using FTIR and the spectra did not display any interaction. Fifteen formulations were prepared and evaluated for preand post-compression characteristics. The prepared ODmini- tablet batches were also assessed for disintegration in simulated salivary fluid (SSF, pH 6.2 and in reconstituted skimmed milk. The optimized formula fulfilled the requirements for crushing strength of 5 kN with minimal friability, disintegration times of 8.4 and 53.7 s in SSF and skimmed milk, respectively. This study therefore proposes the risperidone OD-mini-tablet formula having robust mechanical properties, uniform and precise dosing of medication with short disintegration time suitable for pediatric use.

  20. A placebo controlled study of quetiapine-XR in bipolar depression accompanied by generalized anxiety with and without a recent history of alcohol and cannabis use.

    Science.gov (United States)

    Gao, Keming; Ganocy, Stephen J; Conroy, Carla; Brownrigg, Brittany; Serrano, Mary Beth; Calabrese, Joseph R

    2017-08-01

    This study aims to compare treatment response in bipolar I or II depression and generalized anxiety disorder (GAD) with and without recent alcohol and/or cannabis use disorder (ALC/CAN) to quetiapine-XR (extended release) or placebo. A randomized, double-blind, 8-week study of quetiapine-XR versus placebo in patients with bipolar I or II depression and GAD with or without a recent ALC/CAN was used to compare changes in Hamilton Depression Rating Scale-17, Hamilton Anxiety Rating Scale, the 16-item Quick Inventory of Depressive Symptomatology-Self-Report (QIDS-SR-16), Clinical Global Impression for Bipolar Disorder-Severity (CGI-BP-S), and Timeline Follow Back within and between groups. In the quetiapine-XR group, patients with a recent ALC/CAN (n = 22) had significant decreases in QIDS-SR-16 (-9.6 ± 1.6 vs. -3.7 ± 1.7) and CGI-BP-S (-1.6 ± 0.4 vs. -0.8 ± 0.03) than those without a recent ALC/CAN (n = 24). In the placebo group, both patients with a recent ALC/CAN (n = 23) and those without (n = 21) had similar reductions in these measures. The reduction of QIDS-SR-16 scores in patients with a recent ALC/CAN was also significantly different from that of their counterparts in the placebo group. Patients who received quetiapine-XR had larger decreases in the number of drinking days/week (p = 0.17) and number of cannabis joints/week (p = 0.09) compared to those who received placebo. Quetiapine-XR was superior to placebo in reducing QIDS-SR-16 total score in patients with a recent ALC/CAN. Patients taking quetiapine-XR used less alcohol and cannabis than patients on placebo, suggesting that quetiapine-XR may be of use in patients with bipolar disorder accompanied by GAD and other comorbidities.

  1. A Naturalistic, Single-blind Comparison of Rapid Dose Administration of Divalproex ER Versus Quetiapine in Patients with Acute Bipolar Mania

    Science.gov (United States)

    Galangue, Barbara; MacDonald, Kai; Cobb, Patrice; Dinca, Ana; Becker, Olga; Cooper, J.; Hadley, Allison

    2011-01-01

    Objective: When treating acute bipolar mania, the speed of onset of anti-manic effects is crucial. Quetiapine and divalproex ER are widely used agents to treat acute mania. Rapid dose administration regimens for divalproex ER and for quetiapine have been described. We conducted a naturalistic, head-to-head, pilot study comparing the efficacy and safety of rapidly titrated divalproex ER and quetiapine in acutely manic inpatients, with the primary outcome being improvement within the first seven days. Method: Thirty consenting bipolar patients with acute mania (Young Mania Rating Scale >17 ) needing hospitalization due to acute mania were randomized to receive rapidly loaded divalproex ER (30mg/kg/day) or rapidly titrated quetiapine (200mg Day 1, raised by 200mg/day up to 800mg as tolerated). Assessments were made on Day 1 (baseline), Day 3, Day 7, Day 14, and Day 21 and included Young Mania Rating Scale, Clinical Global Impressions-Severity, Clinical Global Impressions-Improvement, and Montgomery-Asberg Depression Rating Scale. Raters but not patients or treating physicians were blinded (single-blinded study). Results: Subjects in both treatment groups exhibited significant and rapid improvement in their mania starting at Day 3 with few significant adverse effects; however, there were no significant differences in the degree or rate of improvement between the two treatment groups in any of the efficacy or adverse effects scales. Conclusion: Results of this small study indicate that rapid-dose administration of both quetiapine and divalproex ER produce rapid improvement in acute mania within the first seven days and both seem to be well tolerated. PMID:21311705

  2. The psychopharmacology algorithm project at the Harvard South Shore Program: an algorithm for acute mania.

    Science.gov (United States)

    Mohammad, Othman; Osser, David N

    2014-01-01

    This new algorithm for the pharmacotherapy of acute mania was developed by the Psychopharmacology Algorithm Project at the Harvard South Shore Program. The authors conducted a literature search in PubMed and reviewed key studies, other algorithms and guidelines, and their references. Treatments were prioritized considering three main considerations: (1) effectiveness in treating the current episode, (2) preventing potential relapses to depression, and (3) minimizing side effects over the short and long term. The algorithm presupposes that clinicians have made an accurate diagnosis, decided how to manage contributing medical causes (including substance misuse), discontinued antidepressants, and considered the patient's childbearing potential. We propose different algorithms for mixed and nonmixed mania. Patients with mixed mania may be treated first with a second-generation antipsychotic, of which the first choice is quetiapine because of its greater efficacy for depressive symptoms and episodes in bipolar disorder. Valproate and then either lithium or carbamazepine may be added. For nonmixed mania, lithium is the first-line recommendation. A second-generation antipsychotic can be added. Again, quetiapine is favored, but if quetiapine is unacceptable, risperidone is the next choice. Olanzapine is not considered a first-line treatment due to its long-term side effects, but it could be second-line. If the patient, whether mixed or nonmixed, is still refractory to the above medications, then depending on what has already been tried, consider carbamazepine, haloperidol, olanzapine, risperidone, and valproate first tier; aripiprazole, asenapine, and ziprasidone second tier; and clozapine third tier (because of its weaker evidence base and greater side effects). Electroconvulsive therapy may be considered at any point in the algorithm if the patient has a history of positive response or is intolerant of medications.

  3. The effects of neuroleptics on the GABA-induced Cl- current in rat dorsal root ganglion neurons: differences between some neuroleptics.

    Science.gov (United States)

    Yokota, Kenjiro; Tatebayashi, Hideharu; Matsuo, Tadashi; Shoge, Takashi; Motomura, Haruhiko; Matsuno, Toshiyuki; Fukuda, Akira; Tashiro, Nobutada

    2002-03-01

    1. Several neuroleptics inhibited the 3 microM gamma-aminobutyric acid induced-chloride current (GABA-current) on dissociated rat dorsal root ganglion neurons in whole-cell patch-clamp investigations. 2. The IC(50) for clozapine, zotepine, olanzapine, risperidone and chlorpromazine were 6.95, 18.26, 20.30, 106.01 and 114.56 microM, respectively. The values for the inhibitory effects of neuroleptics on the GABA (3 microM)-current, which were calculated by the fitting Hill's equations where the concentrations represent the mean therapeutic blood concentrations, were ranked clozapine>zotepine>chlorpromazine>olanzapine>risperidone. These inhibitory effects, weighted with the therapeutic concentrations of neuroleptics, were correlated with the clinical incidences of seizure during treatment with neuroleptics. 3. Clozapine reduced the picrotoxin-inhibiton, and may compete with a ligand of the t-butylbicyclophosphorothionate (TBPS) binding site. 4. Haloperidol and quetiapine did not affect the peak amplitude of the GABA (3 microM)-current. However, haloperidol reduced the clozapine-inhibition, and may antagonize ligand binding to TBPS binding site. 5. Neuroleptics including haloperidol and quetiapine enhanced the desensitization of the GABA (3 microM)-current. However, haloperidol and quetiapine at 100 microM inhibited the desensitization at the beginning of application. 6. Blonanserin (AD-5423) at 30 and 50 microM potentiated the GABA (3 microM)-current to 170.1+/-6.9 and 192.0+/-10.6% of the control current, respectively. Blonanserin shifted GABA concentration-response curve leftward. Blonanserin only partly negatively interacted with diazepam. The blonanserin-potentiation was not reversed by flumazenil. Blonanserin is not a benzodiazepine receptor agonist. 7. The various effects of neuroleptics on the GABA-current may be related to the clinical effects including modifying the seizure threshold.

  4. The effects of neuroleptics on the GABA-induced Cl− current in rat dorsal root ganglion neurons: differences between some neuroleptics

    Science.gov (United States)

    Yokota, Kenjiro; Tatebayashi, Hideharu; Matsuo, Tadashi; Shoge, Takashi; Motomura, Haruhiko; Matsuno, Toshiyuki; Fukuda, Akira; Tashiro, Nobutada

    2002-01-01

    Several neuroleptics inhibited the 3 μM γ-aminobutyric acid induced-chloride current (GABA-current) on dissociated rat dorsal root ganglion neurons in whole-cell patch-clamp investigations. The IC50 for clozapine, zotepine, olanzapine, risperidone and chlorpromazine were 6.95, 18.26, 20.30, 106.01 and 114.56 μM, respectively. The values for the inhibitory effects of neuroleptics on the GABA (3 μM)-current, which were calculated by the fitting Hill's equations where the concentrations represent the mean therapeutic blood concentrations, were ranked clozapine>zotepine>chlorpromazine>olanzapine>risperidone. These inhibitory effects, weighted with the therapeutic concentrations of neuroleptics, were correlated with the clinical incidences of seizure during treatment with neuroleptics. Clozapine reduced the picrotoxin-inhibiton, and may compete with a ligand of the t-butylbicyclophosphorothionate (TBPS) binding site. Haloperidol and quetiapine did not affect the peak amplitude of the GABA (3 μM)-current. However, haloperidol reduced the clozapine-inhibition, and may antagonize ligand binding to TBPS binding site. Neuroleptics including haloperidol and quetiapine enhanced the desensitization of the GABA (3 μM)-current. However, haloperidol and quetiapine at 100 μM inhibited the desensitization at the beginning of application. Blonanserin (AD-5423) at 30 and 50 μM potentiated the GABA (3 μM)-current to 170.1±6.9 and 192.0±10.6% of the control current, respectively. Blonanserin shifted GABA concentration-response curve leftward. Blonanserin only partly negatively interacted with diazepam. The blonanserin-potentiation was not reversed by flumazenil. Blonanserin is not a benzodiazepine receptor agonist. The various effects of neuroleptics on the GABA-current may be related to the clinical effects including modifying the seizure threshold. PMID:11906969

  5. Simultaneous determination of olanzapine and fluoxetine hydrochloride in capsules by spectrophotometry, TLC-spectrodensitometry and HPLC.

    Science.gov (United States)

    Tantawy, Mahmoud A; Hassan, Nagiba Y; Elragehy, Nariman A; Abdelkawy, Mohamed

    2013-03-01

    This paper describes sensitive, accurate and precise spectrophotometric, TLC-spectrodensitometric and high performance liquid chromatographic (HPLC) methods for simultaneous determination of olanzapine and fluoxetine HCl. Two spectrophotometric methods were developed, namely; first derivative (D (1)) and derivative ratio (DD (1)) methods. The TLC method employed aluminum TLC plates precoated with silica gel GF254 as the stationary phase and methanol:toluene:ammonia (7:3:0.1, by volume) as the mobile phase, where the chromatogram was scanned at 235 nm. The developed HPLC method used a reversed phase C18 column with isocratic elution. The mobile phase composed of phosphate buffer pH 4.0:acetonitrile:triethylamine (53:47:0.03, by volume) at flow rate of 1.0 mL min(-1). Quantitation was achieved with UV detection at 235 nm. The methods were validated according to the International Conference on Harmonization (ICH) guidelines. The selectivity of the proposed methods was tested using laboratory-prepared mixtures. The developed methods were successfully applied for the determination of olanzapine and fluoxetine HCl in bulk powder and combined capsule dosage form.

  6. The antidepressant- and anxiolytic-like effects following co-treatment with escitalopram and risperidone in rats.

    Science.gov (United States)

    Kaminska, K; Rogoz, Z

    2016-06-01

    Several clinical reports have documented a beneficial effect of the addition of a low dose of risperidone to the ongoing treatment with antidepressants, in particular selective serotonin reuptake inhibitors (SSRI), in the treatment of drug-resistant depression and treatment-resistant anxiety disorders. In the present study, we investigated the effect of treatment with the antidepressant escitalopram (SSRI) given separately or jointly with a low dose of risperidone (an atypical antipsychotic) in the forced swim test and in the elevated plus-maze test in rats. The obtained results showed that escitalopram at doses of 2.5 or 5 mg/kg evoked antidepressant-like effect in the forced swim test. Moreover, risperidone at low doses (0.05 or 0.1 mg/kg) enhanced the antidepressant-like activity of escitalopram (1 mg/kg) in this test by increasing the swimming time and decreasing the immobility time in those animals. WAY 100635 (a serotonin 5-HT1A receptor antagonist) at a dose of 0.1 mg/kg abolished the antidepressant-like effect induced by co-administration of escitalopram and risperidone. The active behavior in that test did not reflect an increase in general activity, since the combined treatment with escitalopram and risperidone failed to enhance the exploratory activity of rats. In the following experiment, we showed that escitalopram (5 mg/kg) and mirtazapine (5 or 10 mg/kg) or risperidone (0.1 mg/kg) induced an anxiolytic-like effect in the elevated plus-maze test, and the combined treatment with an ineffective dose of risperidone (0.05 mg/kg) enhanced the anxiolytic-like effects of escitalopram (2.5 mg/kg) or mirtazapine (1 and 2.5 mg/kg) in this test. The obtained results suggest that risperidone applied at a low dose enhances the antidepressant-like activity of escitalopram in the forced swim test, and that 5-HT1A receptors may play some role in these effects. Moreover, a low dose of risperidone may also enhance the anxiolytic-like action of the studied

  7. Olanzapine reduces physical activity in rats exposed to activity-based anorexia : possible implications for treatment of anorexia nervosa?

    NARCIS (Netherlands)

    Hillebrand, Jacquelien J G; van Elburg, Annemarie A; Kas, Martien J H; van Engeland, Herman; Adan, Roger A H

    2005-01-01

    BACKGROUND: Anorexia nervosa (AN) patients often show extreme hypophagia and excessive physical activity. Activity-based anorexia (ABA) is considered an animal model of AN and mimics food restriction and hyperactivity in rats. This study investigated whether treatment with olanzapine (Zyprexa) reduc

  8. Comparison of the effect of Olanzapine and Sertraline on patients suffering from personality disorder, receiving methadone maintenance therapy

    Directory of Open Access Journals (Sweden)

    mozhgan Jariani

    2009-03-01

    Full Text Available Background: Borderline Personality disorder is a disabling disease affecting 2% of general population. Various drugs have been suggested for treatment of borderline Personality disorder. If a drug could alleviate a wide range of symptoms, it would be more suitable. In these disorders drug addiction is very common. This fact makes the symptoms complicated and the treatment more difficult. This study is designed to evaluate the effect of Olanzapine and Sertraline in patients suffering from personality disorders who are on methadone maintenance therapy. Materials and Methods: This clinical trial study was carried out on 120 male and female cases chosen for methadone maintenance therapy through interview by a psychiatrist based on DSM-IV-TR diagnostic criteria for BPD. Afterwards they were randomly divided into two groups. These groups separately received Olanzapine (5-10 mg daily and Sertraline (50-100 mg daily therapy. The SCL-90 questionnaire was filled out by the participants before treatment and at the 4th, 8th and 12th weeks of the treatment. Results: According to this clinical trial, Olanzapine and Sertraline were effective in ameliorating symptoms of depression, anxiety and aggression, reducing sensitivity in interpersonal relationship and alleviating obsessive symptoms, pessimistic behaviors and somatization disorders in patients with personality disorders on methadone maintenance therapy. Conclusion: As results of this study stated that Olanzapine and Sertraline are definitely effective in alleviating symptoms of patients with personality disorder, prescribing theses drugs are highly recommended for these patients. .

  9. Mechanism-Based Pharmacokinetic-Pharmacodynamic Modeling of the Dopamine D-2 Receptor Occupancy of Olanzapine in Rats

    NARCIS (Netherlands)

    Johnson, Martin; Kozielska, Magdalena; Reddy, Venkatesh Pilla; Vermeulen, An; Li, Cheryl; Grimwood, Sarah; de Greef, Rik; Groothuis, Geny M. M.; Danhof, Meindert; Proost, Johannes H.

    2011-01-01

    A mechanism-based PK-PD model was developed to predict the time course of dopamine D-2 receptor occupancy (D2RO) in rat striatum following administration of olanzapine, an atypical antipsychotic drug. A population approach was utilized to quantify both the pharmacokinetics and pharmacodynamics of ol

  10. Translation of randomised controlled trial findings into clinical practice: comparison of olanzapine and valproate in the EMBLEM study

    DEFF Research Database (Denmark)

    Novick, D; Gonzalez-Pinto, A; Haro, J M

    2009-01-01

    OBJECTIVES: The aim of this study was to compare the outcomes of olanzapine- and valproate-treated patients in an observational study of acute mania with the results of a randomised controlled trial (RCT) assessing the same treatments. METHODS: EMBLEM (European Mania in Bipolar Evaluation...

  11. Determination of olanzapine in whole blood using simple protein precipitation and liquid chromatography-tandem mass spectrometry

    DEFF Research Database (Denmark)

    Nielsen, Marie Katrine Klose; Johansen, Sys Stybe

    2009-01-01

    A simple, sensitive, and reproducible liquid chromatography-tandem mass spectrometry method has been developed and validated for the quantification of the antipsychotic drug olanzapine in whole blood using dibenzepine as internal standard (IS). After acidic methanol-induced protein precipitation...

  12. Olanzapine reduces physical activity in rats exposed to activity-based anorexia : possible implications for treatment of anorexia nervosa?

    NARCIS (Netherlands)

    Hillebrand, Jacquelien J G; van Elburg, Annemarie A; Kas, Martien J H; van Engeland, Herman; Adan, Roger A H

    2005-01-01

    BACKGROUND: Anorexia nervosa (AN) patients often show extreme hypophagia and excessive physical activity. Activity-based anorexia (ABA) is considered an animal model of AN and mimics food restriction and hyperactivity in rats. This study investigated whether treatment with olanzapine (Zyprexa) reduc

  13. Mucoadhesive Amphiphilic Methacrylic Copolymer-Functionalized Poly(ε-caprolactone) Nanocapsules for Nose-to-Brain Delivery of Olanzapine.

    Science.gov (United States)

    Fonseca, Francisco N; Betti, Andresa H; Carvalho, Flávia C; Gremião, Maria P D; Dimer, Frantiescoli A; Guterres, Sílvia S; Tebaldi, Marli L; Rates, Stela M K; Pohlmann, Adriana R

    2015-08-01

    Nose-to-brain drug delivery has been proposed to overcome the low absorption of drugs in central nervous system due to the absence of brain-blood barrier in the olfactory nerve pathway. However, the presence of a mucus layer and quick clearance limit the use of this route. Herein, amphiphilic methacrylic copolymer-functionalized poly(ε-caprolactone) nanocapsules were proposed as a mucoadhesive system to deliver olanzapine after intranasal administration. In vitro evaluations showed that these nanocapsules were able to interact with mucin (up to 17% of increment in particle size and 30% of reduction of particle concentration) and nasal mucosa (2-fold higher force for detaching), as well as to increase the retention of olanzapine (about 40%) on the nasal mucosa after continuous wash. The olanzapine-loaded amphiphilic methacrylic copolymer-functionalized PCL nanocapsules enhanced the amount of drug in the brain of rats (1.5-fold higher compared to the drug solution). In accordance with this finding, this formulation improved the prepulse inhibition impairment induced by apomorphine, which is considered as an operational measure of pre-attentive sensorimotor gating impairment present in schizophrenia. Besides, nanoencapsulated olanzapine did not affect the nasal mucosa integrity after repeated doses. These data evidenced that the designed nanocapsules are a promising mucoadhesive system for nose-to-brain delivery of drugs.

  14. A case of catatonia status-post left middle cerebral artery cerebrovascular accident, treated successfully with olanzapine.

    Science.gov (United States)

    Spiegel, David R; Klaiber, Nicholas

    2013-01-01

    Catatonia is a psychomotor phenomenon associated with psychiatric/medical conditions. We present a patient who developed catatonia status-post left middle cerebral artery infarct. With a Bush Francis Catatonia Rating Scale score of 43 on admission, treatment with olanzapine reduced this score to 2, by discharge.

  15. Heart rate variability in schizophrenic patients switched from typical antipsychotic agents to amisulpride and olanzapine. 3-month follow-up.

    Science.gov (United States)

    Wang, Ying-Chieh; Yang, Cheryl C H; Bai, Ya-Mei; Kuo, Terry B J

    2008-01-01

    Schizophrenia is a severe mental disorder that requires lifelong treatment, and therefore information on the cardiovascular safety and tolerance of antipsychotics is of significant clinical importance. Atypical antipsychotics have been used to treat schizophrenia patients since the 1990s, and more and more patients have been switched to these from typical antipsychotics; however, there is still no accessible evaluation tool for assessing cardiovascular safety. In this study, we used a computer-assisted 5-min measurement of resting heart rate variability (HRV) in schizophrenia patients who were switched to atypical antipsychotic agents (amisulpride and olanzapine) due to severe side effects (tardive dyskinesia). In 15 patients who switched to amisulpride and 18 to olanzapine, HRV was evaluated before the medication was switched, and patients were followed up every month for 3 months after the switch. Frequency-domain analyses of short-term and stationary respiratory rate (RR) intervals were performed to evaluate low-frequency power (LF; 0.04-0.15 Hz), high-frequency power (HF; 0.15-0.40 Hz), the ratio of LF to HF (LF/HF), and LF in normalized units (LF%). Our results showed significant increases in the mean, variance and HF of RR intervals in the amisulpride group, but not in the olanzapine group. These results indicate that amisulpride has a more vagotonic effect, suggesting greater cardiovascular safety as compared with olanzapine when subjects are switched from typical antipsychotic agents.

  16. Sertindole, in contrast to clozapine and olanzapine, does not disrupt water maze performance after acute or chronic treatment

    DEFF Research Database (Denmark)

    Didriksen, Michael; Kreilgaard, Mads; Arnt, Jørn

    2006-01-01

    Cognitive deficits in schizophrenia are associated with poor functional outcome, and may be further aggravated by treatment with antipsychotics. In the present study the acute and chronic (3 weeks of treatment) effects of clozapine, olanzapine, and sertindole on performance in the Morris water ma...

  17. Risperidone and Divalproex Differentially Engage the Fronto-Striato-Temporal Circuitry in Pediatric Mania: A Pharmacological Functional Magnetic Resonance Imaging Study

    Science.gov (United States)

    Pavuluri, Mani N.; Passarotti, Alessandra M.; Fitzgerald, Jacklynn M.; Wegbreit, Ezra; Sweeney, John A.

    2012-01-01

    Objective: The current study examined the impact of risperidone and divalproex on affective and working memory circuitry in patients with pediatric bipolar disorder (PBD). Method: This was a six-week, double-blind, randomized trial of risperidone plus placebo versus divalproex plus placebo for patients with mania (n = 21; 13.6 [plus or minus] 2.5…

  18. Risperidone and Divalproex Differentially Engage the Fronto-Striato-Temporal Circuitry in Pediatric Mania: A Pharmacological Functional Magnetic Resonance Imaging Study

    Science.gov (United States)

    Pavuluri, Mani N.; Passarotti, Alessandra M.; Fitzgerald, Jacklynn M.; Wegbreit, Ezra; Sweeney, John A.

    2012-01-01

    Objective: The current study examined the impact of risperidone and divalproex on affective and working memory circuitry in patients with pediatric bipolar disorder (PBD). Method: This was a six-week, double-blind, randomized trial of risperidone plus placebo versus divalproex plus placebo for patients with mania (n = 21; 13.6 [plus or minus] 2.5…

  19. Adverse Effects of Risperidone in Children with Autism Spectrum Disorders in a Naturalistic Clinical Setting at Siriraj Hospital, Thailand

    Directory of Open Access Journals (Sweden)

    Vitharon Boon-yasidhi

    2014-01-01

    Full Text Available A cross-sectional study was conducted to evaluate adverse effects associated with risperidone in 45 children with autism spectrum disorders (ASD, aged 2–15 years, who were treated at Siriraj Hospital, Thailand, between the years 2006 and 2007. Adverse effects were assessed by parent interview, using a semistructure questionnaire, and medical records review. The mean ± SD age of the children at starting risperidone was 8.15±2.98 years. The mean ± SD of risperidone dose was 0.94±0.74 mg/day and the mean ± SD duration of treatment was 36.8±27.8 months. Adverse effects were reported in 39 children (86.7%. Common adverse effects included increased appetite, somnolence, and rhinorrhea and most of the adverse effects were tolerable. Tardive dyskinesia or other serious adverse events were not found in this study. The child’s mean ± SD weight gain was 4.18±2.82 kg/year, which exceeded developmentally expected norms. The results from this study suggest that risperidone treatment in children with ASD is associated with frequent mild and tolerable adverse effects. However, excessive weight gain could be found to be a concerning adverse effect and weight monitoring is warranted when risperidone is being prescribed.

  20. Parenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluation.

    Science.gov (United States)

    Đorđević, Sanela M; Cekić, Nebojša D; Savić, Miroslav M; Isailović, Tanja M; Ranđelović, Danijela V; Marković, Bojan D; Savić, Saša R; Timić Stamenić, Tamara; Daniels, Rolf; Savić, Snežana D

    2015-09-30

    This paper describes design and evaluation of parenteral lecithin-based nanoemulsions intended for brain delivery of risperidone, a poorly water-soluble psychopharmacological drug. The nanoemulsions were prepared through cold/hot high pressure homogenization and characterized regarding droplet size, polydispersity, surface charge, morphology, drug-vehicle interactions, and physical stability. To estimate the simultaneous influence of nanoemulsion formulation and preparation parameters--co-emulsifier type, aqueous phase type, homogenization temperature--on the critical quality attributes of developed nanoemulsions, a general factorial experimental design was applied. From the established design space and stability data, promising risperidone-loaded nanoemulsions (mean size about 160 nm, size distribution emulsifier, were produced by hot homogenization and their ability to improve risperidone delivery to the brain was assessed in rats. Pharmacokinetic study demonstrated erratic brain profiles of risperidone following intraperitoneal administration in selected nanoemulsions, most probably due to their different droplet surface properties (different composition of the stabilizing layer). Namely, polysorbate 80-costabilized nanoemulsion showed increased (1.4-7.4-fold higher) risperidone brain availability compared to other nanoemulsions and drug solution, suggesting this nanoemulsion as a promising carrier worth exploring further for brain targeting. Copyright © 2015 Elsevier B.V. All rights reserved.

  1. The role of antipsychotics in the management of fibromyalgia.

    Science.gov (United States)

    Calandre, Elena P; Rico-Villademoros, Fernando

    2012-02-01

    Fibromyalgia is a syndrome characterized by chronic generalized pain associated with different somatic symptoms, such as sleep disturbances, fatigue, stiffness, balance problems, hypersensitivity to physical and psychological environmental stimuli, depression and anxiety. It has been estimated to affect roughly the 2-4% of the general population in most countries studied, and it has been shown to be much more prevalent in women than in men. Although its pathophysiology is not yet fully understood, it is known that both genetic and environmental factors are involved in its development. Fibromyalgia shares a high degree of co-morbidity with other conditions, including chronic headache, temporomandibular disorder, irritable bowel syndrome, major depression, anxiety disorders and chronic fatigue syndrome. Therefore, this is a syndrome difficult to treat for which multimodal treatments including physical exercise, psychological therapies and pharmacological treatment are recommended. Although different kinds of drugs have been studied for the treatment of fibromyalgia, the most widely used drugs that have the higher degree of evidence for efficacy include the α(2)δ ligands pregabalin and gabapentin, and the tricyclic antidepressants (TCAs) and serotonin noradrenaline (norepinephrine) reuptake inhibitors (SNRIs). However, there is a need to look for newer additional therapeutic pharmacological options for the treatment of this complex and disabling disease. First- and second-generation antipsychotics have shown analgesic properties both in an experimental setting and in humans, although most of the available evidence for the treatment of human pain concerns older antipsychotics and involves clinical trials performed several decades ago. In addition, several second-generation antipsychotics, risperidone, olanzapine and quetiapine, have shown efficacy in the treatment of some anxiety disorders. Some second-generation antipsychotics, mainly quetiapine, aripiprazole and

  2. Assessing the synergy between cholinomimetics and memantine as augmentation therapy in cognitive impairment in schizophrenia. A virtual human patient trial using quantitative systems pharmacology.

    Science.gov (United States)

    Geerts, Hugo; Roberts, Patrick; Spiros, Athan

    2015-01-01

    While many drug discovery research programs aim to develop highly selective clinical candidates, their clinical success is limited because of the complex non-linear interactions of human brain neuronal circuits. Therefore, a rational approach for identifying appropriate synergistic multipharmacology and validating optimal target combinations is desperately needed. A mechanism-based Quantitative Systems Pharmacology (QSP) computer-based modeling platform that combines biophysically realistic preclinical neurophysiology and neuropharmacology with clinical information is a possible solution. This paper reports the application of such a model for Cognitive Impairment In Schizophrenia (CIAS), where the cholinomimetics galantamine and donepezil are combined with memantine and with different antipsychotics and smoking in a virtual human patient experiment. The results suggest that cholinomimetics added to antipsychotics have a modest effect on cognition in CIAS in non-smoking patients with haloperidol and risperidone and to a lesser extent with olanzapine and aripiprazole. Smoking reduces the effect of cholinomimetics with aripiprazole and olanzapine, but enhances the effect in haloperidol and risperidone. Adding memantine to antipsychotics improves cognition except with quetiapine, an effect enhanced with smoking. Combining cholinomimetics, antipsychotics and memantine in general shows an additive effect, except for a negative interaction with aripiprazole and quetiapine and a synergistic effect with olanzapine and haloperidol in non-smokers and haloperidol in smokers. The complex interaction of cholinomimetics with memantine, antipsychotics and smoking can be quantitatively studied using mechanism-based advanced computer modeling. QSP modeling of virtual human patients can possibly generate useful insights on the non-linear interactions of multipharmacology drugs and support complex CNS R&D projects in cognition in search of synergistic polypharmacy.

  3. GABA, Selank, and Olanzapine Affect the Expression of Genes Involved in GABAergic Neurotransmission in IMR-32 Cells

    Science.gov (United States)

    Filatova, Elena; Kasian, Anastasiya; Kolomin, Timur; Rybalkina, Ekaterina; Alieva, Anelya; Andreeva, Lyudmila; Limborska, Svetlana; Myasoedov, Nikolay; Pavlova, Galina; Slominsky, Petr; Shadrina, Maria

    2017-01-01

    Clinical studies have shown that Selank had an anxiolytic effect comparable to that of classical benzodiazepine drugs, which can enhance the inhibitory effect of GABA by allosteric modulation of GABAA receptors. These data suggest that the molecular mechanism of the effect of Selank may also be related to its ability to affect the performance of the GABAergic system. To test this hypothesis, we studied the changes in expression of 84 genes involved in the functioning of the GABAergic system and in the processes of neurotransmission in the culture of neuroblastoma IMR-32 cells using qPCR method. As test substances, in addition to Selank, we selected the major GABAA receptor ligand, GABA, the atypical antipsychotic, olanzapine, and combinations of these compounds (Selank and GABA; Selank and olanzapine). We found no changes in the mRNA levels of the genes studied under the effect of Selank. The combined effect of GABA and Selank led to nearly complete suppression of changes in expression of genes in which mRNA levels changed under the effect of GABA. When Selank was used in conjunction with olanzapine, the expression alterations of more genes were observed compared with olanzapine alone. The data obtained indicate that Selank has no direct effect on the mRNA levels of the GABAergic system genes in neuroblastoma IMR-32 cells. At the same time, our results partially confirm the hypothesis that the peptide may affect the interaction of GABA with GABAA receptors. Our data also suggest that Selank may enhance the effect of olanzapine on the expression of the genes studied. PMID:28293190

  4. Natural oils as skin permeation enhancers for transdermal delivery of olanzapine: in vitro and in vivo evaluation.

    Science.gov (United States)

    Aggarwal, Geeta; Dhawan, Sanju; HariKumar, S L

    2012-03-01

    The feasibility of development of transdermal delivery system of olanzapine utilizing natural oils as permeation enhancers was investigated. Penetration enhancing potential of corn (maize) oil, groundnut oil and jojoba oil on in vitro permeation of olanzapine across rat skin was studied. The magnitude of flux enhancement factor with corn oil, groundnut oil and jojoba oil was 7.06, 5.31 and 1.9 respectively at 5mg/ml concentration in solvent system. On the basis of in vitro permeation studies, eudragit based matrix type transdermal patches of olanzapine were fabricated using optimized concentrations of natural oils as permeation enhancers. All transdermal patches were found to be uniform with respect