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Sample records for chlorprothixene

  1. Thioxanthenes, chlorprothixene and flupentixol inhibit proton currents in BV2 microglial cells.

    Science.gov (United States)

    Kim, Jiwon; Song, Jin-Ho

    2016-05-15

    The thioxanthene antipsychotic drugs chlorprothixene and flupentixol have anti-inflammatory and antioxidant properties. The reactive oxygen species produced by NADPH oxidase during microglia-mediated inflammatory responses cause neuronal damage, thereby contributing to various neurodegenerative diseases. Voltage-gated proton channels sustain the NADPH oxidase activity, and inhibition of the channels' activity reduces the production of reactive oxygen species. Herein, the effects of chlorprothixene and flupentixol on proton currents were investigated in BV2 microglial cells using the whole-cell patch-clamp method. Both drugs inhibited the proton currents in a concentration-dependent manner (IC50=1.7μM and 6.6μM, respectively). Chlorprothixene at 3μM slightly shifted the activation voltage toward depolarization. Both the activation and the deactivation kinetics of the proton currents were slowed by chlorprothixene 1.2- and 3.5-fold, respectively. Thus, the inhibition of proton currents may be partly responsible for the antioxidant effects of thioxanthene antipsychotic drugs. PMID:26945819

  2. COMPARATIVE EFFECTIVENESS PIPOFEZINE, TIANEPTINE AND CHLORPROTHIXENE IN PATIENTS WITH ATTENTION DEFICIT DISORDER , AND HYPERTENSION: AN OPEN NON-RANDOMIZED STUDY

    OpenAIRE

    V. V. Glushchenko

    2015-01-01

    Aim. To evaluate the influence of pipofezine, tianeptine and chlorprothixene on blood pressure (BP) level and neuropsychological performance in patients with attention deficit hyperactivity disorder (ADHD) and arterial hypertension (HT). Material and methods. Young males with ADHD and HT (n=58) were included into the study. Patients were split into three treatment groups: group 1 (n=19) received pipofezine 50 mg/day, group 2 (n=20) — tianeptine 25 mg/day , group 3 (n=19) — chlorprothixene 50 ...

  3. Determination of chlorprothixene and amitryptyline hydrochlorides by UV-derivative spectrophotometry and UV-solid-phase spectrophotometry

    Science.gov (United States)

    Karpińska, Joanna; Szostak, Jolanta

    2005-03-01

    Two methods for spectrophotometric determination of chlorprothixene and amitryptyline hydrochlorides were proposed. One of them is based on spectral analysis of their derivative spectra. The measurement of the value at 316.0 nm of first derivative was used for construction of calibration graph for chlorprothixene. The Beer law was obeyed in the concentration range 0.5-50.0 μg ml -1. The amplitude of the second derivative at 261.4 nm was used for determination of amitryptyline in the range 0.5-75.0 μg ml -1. The second proposed method is utilized the use of solid sorbent for simultaneous preconcentration and assay of studied compounds. For this purpose the filtration gel Sephadex G100 was applied. The elaborated solid-phase spectrophotometric method was used for determination of chlorprothixene at 268.0 nm in the range 2.5-75.0 μg ml -1 and amitryptyline at 238.0 nm in the concentration range 10.0-75.0 μg ml -1.

  4. COMPARATIVE EFFECTIVENESS PIPOFEZINE, TIANEPTINE AND CHLORPROTHIXENE IN PATIENTS WITH ATTENTION DEFICIT DISORDER , AND HYPERTENSION: AN OPEN NON-RANDOMIZED STUDY

    Directory of Open Access Journals (Sweden)

    V. V. Glushchenko

    2015-12-01

    Full Text Available Aim. To evaluate the influence of pipofezine, tianeptine and chlorprothixene on blood pressure (BP level and neuropsychological performance in patients with attention deficit hyperactivity disorder (ADHD and arterial hypertension (HT. Material and methods. Young males with ADHD and HT (n=58 were included into the study. Patients were split into three treatment groups: group 1 (n=19 received pipofezine 50 mg/day, group 2 (n=20 — tianeptine 25 mg/day , group 3 (n=19 — chlorprothixene 50 mg/day. Clinicopsychopathologic and neurophysiological findings were evaluated at baseline and after 4 weeks of treatment. BP self-monitoring, analysis of psychiatric disorders severity with Brief Psychiatric Rating Scale, electroencephalography (EEG were performed. Results. The positive dynamics of disregulatory-motor hyperactivity , subjective-cognitive and emotional-vegetative components of ADHD was observed. The positive dynamics of neurophysiological parameters (increase in EEG frequencies index in groups 1 and 2 (from 0.37±0.05 to 0.54±0.07 and 0.38±0.06 to 0.50±0.05, respectively , p<0.05 for both was also found. There were no significant effects of the study drugs on BP levels in patients of all groups (p>0.05. Conclusion. Four-week usage of the study drugs in adolescents with ADHD and HT had no significant effect on BP levels. Pipofezine and tianeptine showed more pronounced improvement of clinicopsychiatric and neuropsychological performance in comparison with chlorprothixene in patients with ADHD.

  5. 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; Køber, Lars; Torp-Pedersen, Christian; Andersson, Charlotte

    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...... treatment, compared with risperidone, incidence rate ratios of major adverse cardiovascular events were higher with use of levomepromazine (3.80, 95% CI 3.43 to 4.21) and haloperidol (1.85, 95% CI 1.67 to 2.05) and lower for treatment with flupentixol (0.54, 95% CI 0.45 to 0.66), ziprasidone (0.31, 95% CI 0...

  6. Quantification of typical antipsychotics in human plasma by ultra-high performance liquid chromatography tandem mass spectrometry for therapeutic drug monitoring.

    Science.gov (United States)

    Gradinaru, Julieta; Vullioud, Astrid; Eap, Chin B; Ansermot, Nicolas

    2014-01-01

    A selective and sensitive method was developed for the simultaneous quantification of seven typical antipsychotic drugs (cis-chlorprothixene, flupentixol, haloperidol, levomepromazine, pipamperone, promazine and zuclopenthixol) in human plasma. Ultra-high performance liquid chromatography (UHPLC) was used for complete separation of the compounds in less than 4.5min on an Acquity UPLC BEH C18 column (2.1mm×50mm; 1.7μm), with a gradient elution of ammonium formate buffer pH 4.0 and acetonitrile at a flow rate of 400μl/min. Detection was performed on a tandem quadrupole mass spectrometer (MS/MS) equipped with an electrospray ionization interface. A simple protein precipitation procedure with acetonitrile was used for sample preparation. Thanks to the use of stable isotope-labeled internal standards for all analytes, internal standard-normalized matrix effects were in the range of 92-108%. The method was fully validated to cover large concentration ranges of 0.2-90ng/ml for haloperidol, 0.5-90ng/ml for flupentixol, 1-450ng/ml for levomepromazine, promazine and zuclopenthixol and 2-900ng/ml for cis-chlorprothixene and pipamperone. Trueness (89.1-114.8%), repeatability (1.8-9.9%), intermediate precision (1.9-16.3%) and accuracy profiles (international recommendations. The method was successfully used in our laboratory for routine quantification of more than 500 patient plasma samples for therapeutic drug monitoring. To the best of our knowledge, this is the first UHPLC-MS/MS method for the quantification of the studied drugs with a sample preparation based on protein precipitation. PMID:24036032

  7. 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; Køber, Lars; Torp-Pedersen, Christian; Andersson, Charlotte

    2015-01-01

    BACKGROUND: Data from observational studies have raised concerns about the safety of treatment with antipsychotic agents (APs) in elderly patients with dementia, but this area has been insufficiently investigated. We performed a head-to-head comparison of the risk of major adverse cardiovascular...... treatment, compared with risperidone, incidence rate ratios of major adverse cardiovascular events were higher with use of levomepromazine (3.80, 95% CI 3.43 to 4.21) and haloperidol (1.85, 95% CI 1.67 to 2.05) and lower for treatment with flupentixol (0.54, 95% CI 0.45 to 0.66), ziprasidone (0.31, 95% CI 0.......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...

  8. Detection of antidepressant and antipsychotic drugs in human hair.

    Science.gov (United States)

    Shen, Min; Xiang, Ping; Wu, Hejian; Shen, Baohua; Huang, Zhongjie

    2002-04-18

    The presence of therapeutic drugs and their metabolites in the hair of psychiatric patients was investigated using gas chromatography (GC)-mass spectroscopy (MS)-electron ionization (EI) and GC-MS-chemical ionization (CI). In hair samples tested from 35 subjects, carbamazepine, amitriptyline, doxepin, trihexyphenidyl, chlorpromazine, chlorprothixene, trifluoperazine, clozapine and haloperidol were detected, with maximal concentrations of 22.5, 57.7, 183.3, 15.6, 68.2, 30.0, 36.8, 59.2 and 20.1 ng/mg of hair sample, respectively. Chlorpromazine and clozapine concentrations in the hair were found to be dependent on the dosage used and their correlation coefficients were 0.8047 (P<0.001, n=16) and 0.7097 (P<0.001, n=16), respectively. Segmental analysis demonstrated that there was a correlation between the history of subject's drug exposure and the distribution of drug along the hair shaft. Our results also show that drug analysis in hair may provide useful information about drug treatment and the history of usage, and that drugs can be detected in normally kept hair for at least 16 months after intake. PMID:12084493

  9. Real-time 2D separation by LC × differential ion mobility hyphenated to mass spectrometry.

    Science.gov (United States)

    Varesio, Emmanuel; Le Blanc, J C Yves; Hopfgartner, Gérard

    2012-03-01

    The liquid chromatography-mass spectrometry (LC-MS) analysis of complex samples such as biological fluid extracts is widespread when searching for new biomarkers as in metabolomics. The success of this hyphenation resides in the orthogonality of both separation techniques. However, there are frequent cases where compounds are co-eluting and the resolving power of mass spectrometry (MS) is not sufficient (e.g., isobaric compounds and interfering isotopic clusters). Different strategies are discussed to solve these cases and a mixture of eight compounds (i.e., bromazepam, chlorprothixene, clonapzepam, fendiline, flusilazol, oxfendazole, oxycodone, and pamaquine) with identical nominal mass (i.e., m/z 316) is taken to illustrate them. Among the different approaches, high-resolution mass spectrometry or liquid chromatography (i.e., UHPLC) can easily separate these compounds. Another technique, mostly used with low resolving power MS analyzers, is differential ion mobility spectrometry (DMS), where analytes are gas-phase separated according to their size-to-charge ratio. Detailed investigations of the addition of different polar modifiers (i.e., methanol, ethanol, and isopropanol) into the transport gas (nitrogen) to enhance the peak capacity of the technique were carried out. Finally, a complex urine sample fortified with 36 compounds of various chemical properties was analyzed by real-time 2D separation LC×DMS-MS(/MS). The addition of this orthogonal gas-phase separation technique in the LC-MS(/MS) hyphenation greatly improved data quality by resolving composite MS/MS spectra, which is mandatory in metabolomics when performing database generation and search. PMID:22006241