Clinical Pharmacokinetics of Atypical Antipsychotics: An Update

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Abstract

Therapeutic drug monitoring studies have generally concentrated on controlling compliance and avoiding side effects by maintaining long-term exposure to minimally effective blood concentrations. The rationale for using therapeutic drug monitoring in relation to second-generation antipsychotics is still being discussed at least with regard to the real clinical utility, but there is evidence that it can improve efficacy, especially when patients do not respond or develop side effects using therapeutic doses. Furthermore, drug plasma concentration determinations can be of some utility in medico-legal problems. This review concentrates on the clinical pharmacokinetic data related to clozapine, risperidone, paliperidone, olanzapine, quetiapine, amisulpride, ziprasidone, aripiprazole, sertindole, asenapine, iloperidone, lurasidone, brexpiprazole and cariprazine and briefly considers the main aspects of their pharmacodynamics. Optimal plasma concentration ranges are proposed for clozapine, risperidone, paliperidone and olanzapine because the studies of quetiapine, amisulpride, asenapine, iloperidone and lurasidone provide only limited information and there is no direct evidence concerning ziprasidone, aripiprazole, sertindole, brexpiprazole and cariprazine: the few reported investigations need to be confirmed and extended.

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Change history

  • 19 June 2019

    The pharmacokinetics of CRP was tested in small short-term studies in both healthy volunteers and in subjects with schizophrenia, with similar results [242].

  • 19 June 2019

    The pharmacokinetics of CRP was tested in small short-term studies in both healthy volunteers and in subjects with schizophrenia, with similar results [242].

  • 19 June 2019

    The pharmacokinetics of CRP was tested in small short-term studies in both healthy volunteers and in subjects with schizophrenia, with similar results [242].

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Massimo Carlo Mauri, Silvia Paletta, Chiara Di Pace, Alessandra Reggiori, Giovanna Cirnigliaro, Isabel Valli and Alfredo Carlo Altamura have no conflicts of interest that are directly relevant to the contents of this article.

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Mauri, M.C., Paletta, S., Di Pace, C. et al. Clinical Pharmacokinetics of Atypical Antipsychotics: An Update. Clin Pharmacokinet 57, 1493–1528 (2018). https://doi.org/10.1007/s40262-018-0664-3

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