Spoelstra S K, Visser L, Knegtering H
Tijdschr Psychiatr. 2019;61(10):702-709.
Since 2018, cariprazine has been available for the treatment of schizophrenia on the Dutch and Belgian markets.
AIM: To give an overview of the indications, effectiveness and side effects of cariprazine. To make an inventory of the advantages and disadvantages of this new antipsychotic drug.
METHOD: A clinically oriented literature review of published clinical studies and pharmacodynamic and -kinetic publications.
RESULTS: Cariprazine is unique because of its preferential D3 receptor partial agonist affinity and has, in theory, a beneficial effect on negative symptoms. The antipsychotic has two active metabolites: desmethylcariprazine and didesmethylcariprazine. The long half-life of cariprazine indicates that, in theory, the drug should not be given daily. Cariprazine is metabolized by cyp3a4 and to a lesser extent by cyp2d6 enzymes. Extrapyramidal symptoms and akathisia are relatively frequent side effects. In contrast, metabolic side effects and weight gain have been reported rarely.
CONCLUSION: Cariprazine can be an effective treatment option for schizophrenia. The final positioning of this antipsychotic drug will have to be based on future research.
自2018年以来，卡立普嗪已在荷兰和比利时市场上用于治疗精神分裂症。
概述卡立普嗪的适应症、有效性和副作用。盘点这种新型抗精神病药物的优缺点。
对已发表的临床研究以及药效学和药代动力学出版物进行以临床为导向的文献综述。
卡立普嗪因其对D3受体的优先部分激动剂亲和力而独具特色，理论上对阴性症状有有益作用。该抗精神病药物有两种活性代谢物：去甲基卡立普嗪和双去甲基卡立普嗪。卡立普嗪的半衰期较长，这表明理论上该药不应每日给药。卡立普嗪通过cyp3a4代谢，在较小程度上通过cyp2d6酶代谢。锥体外系症状和静坐不能是相对常见的副作用。相比之下，代谢副作用和体重增加的报告很少。
卡立普嗪可以是治疗精神分裂症的一种有效选择。这种抗精神病药物的最终定位将必须基于未来的研究。
