Năstase Mihai-Gabriel, Vasile Antonia Ioana, Pietreanu Arina Cipriana, Trifu Simona
Doctoral School, "Carol Davila" University of Medicine and Pharmacy, 020021 Bucharest, Romania.
Department of Neurosciences, "Carol Davila" University of Medicine and Pharmacy, 020021 Bucharest, Romania.
Life (Basel). 2025 May 22;15(6):830. doi: 10.3390/life15060830.
We tried to synthesize the possibilities of predicting the response to clozapine treatment, which can significantly improve the efficacy of the active substance and reduce adverse reactions, and how the active substance acts at the D1 dopaminergic receptors D2, D3, D4, and D5, muscarinic M1, M2, M3, and M5, and the histamine and alpha 1 adrenergic receptor, as well as how it contributes to increased cerebral blood flow, the effect on ribosomal protein S6 function, or the effect on kynurenine 3-monooxygenase function. Clozapine is one of the most effective antipsychotics, and there is potential to improve performance by combining it with different compounds to limit adverse effects or by augmenting it with other antipsychotics (amisulpride, paliperidone), other active substances with different properties (minocycline, N-acetylcysteine, memantine), or alternative therapies (electroconvulsive therapy, repetitive transcranial magnetic stimulation). There are also significant steps in optimizing clozapine efficacy by predicting treatment response, which could be determined by testing the following: plasma levels of clozapine N-oxide and N-desmethylclozapine, serum levels of neurotrophins and glutamate, genetic testing, the polygenic risk score, morphometry, or even the identification and accurate determination of persistent negative symptoms.
我们试图综合预测氯氮平治疗反应的可能性,这可以显著提高活性物质的疗效并减少不良反应,以及该活性物质如何作用于多巴胺能D1、D2、D3、D4和D5受体、毒蕈碱M1、M2、M3和M5受体、组胺和α1肾上腺素能受体,以及它如何促进脑血流量增加、对核糖体蛋白S6功能的影响或对犬尿氨酸3-单加氧酶功能的影响。氯氮平是最有效的抗精神病药物之一,通过将其与不同化合物联合以限制不良反应,或与其他抗精神病药物(氨磺必利、帕利哌酮)、具有不同特性的其他活性物质(米诺环素、N-乙酰半胱氨酸、美金刚)或替代疗法(电惊厥治疗、重复经颅磁刺激)联合使用,有提高疗效的潜力。通过预测治疗反应来优化氯氮平疗效也有重要进展,这可以通过检测以下指标来确定:氯氮平N-氧化物和N-去甲基氯氮平的血浆水平、神经营养因子和谷氨酸的血清水平、基因检测、多基因风险评分、形态测量,甚至持续阴性症状的识别和准确测定。