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Risperidone RSP is usually defined as an atypical antipsychotic drug which belongs to the chemical class of benzisoxazoles, approved in the treatment of many disorders due to its lower extra-pyramidal side effects when compared to conventional drugs used for psychotic disorders. David Germann CYP3A4 also appears to be involved, to a lesser extent, in metabolism of risperidone and 9-hydroxy-risperidone. The minor metabolic routes for risperidone include oxidative N-dealkylation and hydroxylation to 7-hydroxy-risperidone Fig. These metabolites do not exhibit pharmacologic effects.
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CNS-active drugs produce specific electroencephalographic changes and the concentration-effect relationship of antipsychotics may be elucidated by adopting electroencephalography EEG as an effect measurement tool. The purpose of the present study was to determine the concentration-effect relationship of risperidone by assessing the EEG effect after oral administrations of single dose risperidone in healthy young males. Nine healthy male volunteers received a 1 mg single oral dose of risperidone according to a placebo controlled crossover design. Plasma levels of risperidone and its active metabolite 9-hydroxyrisperidone were measured by radioimmunoassay. The difference in the absolute power in the delta frequency band for the F3 lead between risperidone and placebo was used as a drug effect parameter. The hysteresis loop was observed in the plot of plasma concentration of risperidone or sum of risperidone and 9-hydroxyrisperidone Cp versus EEG effect for each subject.
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