延长释放的药物动力学和耐受性。喹硫平延胡索酸酯在汉族精神分裂症患者。

文章的细节

引用

复制到剪贴板

李问,苏雅,刘Y,陈JX,谭YL,杨FD, Si TM

延长释放的药物动力学和耐受性。喹硫平延胡索酸酯在汉族精神分裂症患者。

Pharmacokinet。2014年5月,53 (5):455 - 65。doi: 10.1007 / s40262 - 013 - 0127 - 9。

PubMed ID

24385309 (在PubMed

]

文摘

延长释放形成的背景和目的:喹硫平(喹硫平XR),每日一次开发提供更方便管理,已被广泛研究,描述其药物动力学在高加索人群,但在亚洲人口很少被研究。这项研究进行了评估的药物动力学和耐受性喹硫平XR管理作为单个剂量(300毫克)和多个剂量(300、600和800毫克)汉族精神分裂症患者。方法:这是一个单中心,非盲、单剂和multiple-dose随机研究。在55随机主题,共有40名女性或男性患者在300毫克(n = 13), 600毫克(n = 13),或800毫克(n = 14)组完成喹硫平延胡索酸酯XR的研究。治疗阶段由连续5天,之前是1 -为期两天的滴定时期为600年和800毫克组。药代动力学参数为奎硫平和N-desalkyl喹硫平(norquetiapine)测定。耐受性评价包括不良事件(AEs)指出通过监测,身体检查,生命体征,临床实验室检测。结果:N-desalkyl喹硫平从喹硫平成立一个近似代谢物父母比0.5的三个剂量组。几何平均消除半衰期(t(1/2))的奎硫平和N-desalkyl喹硫平一致的三个剂量组(大约7 h奎硫平和大约18 h N-desalkyl喹硫平)。几何平均最大血浆浓度(C max)在稳定状态(C马克斯,ss)喹硫平的三组是467年,740年和1126 ng / mL,分别和N-desalkyl喹硫平138,262,和426 ng / mL,分别。 The values for the geometric mean area under the plasma concentration-time curve over a dosing interval at the steady-state (AUCss) of quetiapine were 5,094, 7,685, and 13,237 ng.h/mL, respectively, and for N-desalkyl quetiapine were 2,284, 4,341, and 7,216 ng.h/mL, respectively. The apparent oral clearance (CL/F) of quetiapine at steady state appeared to be comparable across the three dose groups. The pharmacokinetics of quetiapine XR were dose-proportional across the dosage range employed. The most common AE was somnolence, but all of the reported AEs were mild. There were no serious AEs or other significant AEs. CONCLUSION: Quetiapine fumarate XR has a dose-proportional pharmacokinetic profile at doses ranging from 300 to 800 mg once daily, and a slower time to reach C max and steady state after 3 days of sequential dosing. Therefore, it offers a simple and rapid dose-escalation option and more convenient once-daily administration. The three dosages of quetiapine fumarate XR were generally well-tolerated in this pharmacokinetic study of Han Chinese patients with schizophrenia.

DrugBank数据引用了这篇文章

药物

喹硫平