Mauri M C, Paletta S, Maffini M, Colasanti A, Dragogna F, Di Pace C, Altamura A C
Department of Neuroscience and Mental Health, Pychiatric Unit, Clinical Neuropsychopharmacology Unit, University of Milan, Fondazione IRCCS Ca' Granda, Ospedale Maggiore Policlinico, Via F. Sforza 35, 20122 Milano, Italy.
Center for Affective Disorders, Department of Psychological Medicine, Institute of Psychiatry, King's College Denmark Hill, London SE5 8AF, England.
EXCLI J. 2014 Oct 13;13:1163-91. eCollection 2014.
This review will concentrate on the clinical pharmacology, in particular pharmacodynamic data, related to atypical antipsychotics, clozapine, risperidone, paliperidone, olanzapine, que¬tiapine, amisulpride, ziprasidone, aripiprazole, asenapine, iloperidone, lurasidone and cariprazine. A summary of their acute pharmacokinetics properties are also reported. Four new second-generation antipsychotics are available: iloperidone, asenapine, lurasidone and in the next future cariprazine. Similar to ziprasidone and aripiprazole, these new agents are advisable for the lower propensity to give weight gain and metabolic abnormalities in comparison with older second-generation antipsychotics such as olanzapine or clozapine. Actually lurasidone seems to be best in terms of minimizing unwanted alterations in body weight and metabolic variables. Therapeutic drug monitoring is not strictly necessary for all of the new antipsychotic drugs because there are no unequivocal data supporting a relationship between plasma drug levels and clinical outcomes or side effects. The exception can be represented by clozapine for which plasma levels of 350-420 ng/ml are reported to be associated with an increased probability of a good clinical response. Also for olanzapine an established therapeutic range (20-50 ng/ml) is proposed to yield an optimal response and minimize side effects.
本综述将聚焦于与非典型抗精神病药物相关的临床药理学，尤其是药效学数据，这些药物包括氯氮平、利培酮、帕利哌酮、奥氮平、喹硫平、氨磺必利、齐拉西酮、阿立哌唑、阿塞那平、伊潘立酮、鲁拉西酮和卡利拉嗪。文中还报告了它们的急性药代动力学特性总结。有四种新型第二代抗精神病药物可供使用：伊潘立酮、阿塞那平、鲁拉西酮，以及在不久的将来会上市的卡利拉嗪。与齐拉西酮和阿立哌唑类似，相较于奥氮平或氯氮平这类较老的第二代抗精神病药物，这些新药导致体重增加和代谢异常的倾向较低。实际上，就将体重和代谢变量的不良改变降至最低而言，鲁拉西酮似乎是最佳的。并非所有新型抗精神病药物都严格需要进行治疗药物监测，因为没有明确的数据支持血浆药物水平与临床疗效或副作用之间存在关联。氯氮平可能是个例外，据报道，血浆水平在350 - 420 ng/ml时，临床良好反应的概率会增加。对于奥氮平，也提出了一个既定的治疗范围（20 - 50 ng/ml），以产生最佳反应并将副作用降至最低。
