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  • 1985-1989  (2)
  • Pharmacokinetics  (1)
  • Substituted benzamide  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 86 (1985), S. 241-243 
    ISSN: 1432-2072
    Keywords: Remoxipride ; Antipsychotic efficacy ; Schizophrenia ; Substituted benzamide ; Brief Psychiatric Rating Scale
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Remoxipride is a novel substituted benzamide derivative with specific dopamine-(D2)-receptor blocking properties and selective action on brain mesolimbic functions. Ten inpatients with a DSM-III diagnosis of schizophrenia were treated with the drug in a 6-week open-label study. After 1 week placebo washout, the patients were given stepwise increased doses from 20 to 100 mg t.i.d. Most patients showed a clinically significant improvement; the mean scores in the Brief Psychiatric Rating Scale decreased from 25.8 at baseline to 11.3 at endpoint. Few adverse events were recorded and the rated extrapyramidal symptoms were lower at endpoint than at baseline. No abnormalities in clinical chemistry, haematology, cardiovascular assessments or EEG recordings were seen.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-2072
    Keywords: Haloperidol ; Pharmacokinetics ; Psychotic patients ; Serum levels ; High performance liquid chromatography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Nine psychotic patients under continuous oral treatment with haloperidol were randomly given a test dose of 1.5–5 mg haloperidol orally and/or intravenously. Serum levels of haloperidol were determined by high performance liquid chromatography and serum concentration data obtained were submitted to pharmacokinetic analysis. The steady state concentration ratio between blood and plasma was determined and found to be 0.79±0.03. The blood clearance was then calculated to be 550±133 ml/min. The mean hepatic extraction ratio was intermediate (0.37). Consequently, for a drug mainly eliminated by hepatic metabolism like haloperidol, the total blood clearance and the extent of oral bioavailability can be affected by changes in hepatic blood flow, hepatic enzyme activities and drug binding. During continuous oral treatment with haloperidol, however, it can be shown that changes in the total metabolic capacity of the liver due to hepatic enzyme induction or inhibition should be important for the therapeutic effects of haloperidol. The volume of distribution at steady state (Vdss) was large (7.9±2.5 l/kg). The terminal half-life was 18.8 h after intravenous and 18.1 h after oral administration. The oral bioavailability (0.60±0.18) were in accordance with previous results in healthy subjects. A mean lag time after oral dose was 1.3±1.1 h and a longer absorption half-life (1.9±1.4 h) was found in the patients compared with healthy volunteers.
    Type of Medium: Electronic Resource
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