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炎症会影响RISPERIDONE的药理动力学:急性相反应期间是否需要调整剂量?

Gaoyu Wang¹, Xinghua Liu¹, Qiurui Huo¹

¹School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China.

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|December 21, 2023

概括

由于药理动力学变化,炎症显著增加了瑞斯佩里的血水平6倍,但大脑度保持稳定. 这表明,在精神病治疗中急性相反应 (APR) 期间,risperidone可能不需要调整剂量.

科学领域:

药理学药理学是指药理学的学科.
神经科学是一个神经科学.
免疫学免疫学免疫学

背景情况:

在炎症或感染的急性相反应 (APR) 期间,RISPERIDONE的血度增加了3-5倍.
随着在APR期间的剂量减少,精神病症状的恶化发生,需要检查炎症的药理动力学影响.

研究的目的:

调查APR对Risperidone的药理动力学,分布和处置 in vivo和 in vitro的影响.
阐明炎症期间改变RISPERIDONE暴露背后的机制.

主要方法:

建立了一个由脂聚糖 (LPS) 诱导的APR子模型.
通过肌肉内和口服途径服用RISPERIDONE,分析血和大脑度.
评估了血蛋白结合 (PPB) 和输送物相互作用 (OATP1B3,OCT2,OAT3,MATE-1,MATE-2K). 测试了多种蛋白质结合和输送物相互作用 (OATP1B3,OCT2,OAT3,MATE-1,MATE-2K).
测量了孕激素X受体和P-糖蛋白的表达.

主要成果:

在APR期间,Risperidone和9-hydroxyrisperidone的血暴露增加了大约6倍.
在炎症和对照组中,RISPERIDONE和代谢物的脑组织度在炎症和对照组之间仍然相似.
在APR期间,血蛋白结合 (PPB) 增加到>99%.
LPS抑制了P-糖蛋白的表达.

结论:

在APR期间减少P-糖蛋白表达和增加PPB有助于更高的血里斯比里暴露.
稳定的脑度表明在APR期间不需要调整RISPERIDONE剂量以适应心理药理学结果.

关键词:

急性相反应反应的急性阶段反应炎症炎症是一种炎症.这是一种P-glycoprotein蛋白.药理动力学药理动力学它与等离子体蛋白质结合.里斯比里胺是一种素.

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