喹硫平的临床药物动力学:非典型抗精神病药物。

文章的细节

引用

复制到剪贴板

迪瓦恩CL,内梅萝芙CB

喹硫平的临床药物动力学:非典型抗精神病药物。

Pharmacokinet。2001; 40(7): 509 - 22所示。doi: 10.2165 / 00003088-200140070-00003。

PubMed ID

11510628 (在PubMed

]

文摘

喹硫平是一种dibenzothiazepine导数已经评估管理患者的精神障碍的表现。在药代动力学研究在人类中,喹硫平口服后迅速吸收,中位数时间达到最大观察血浆浓度从1到2个小时。绝对生物利用度是未知的,但相对生物利用度从口头管理平板电脑解决方案相比几乎是完整的。食物对喹硫平吸收的影响最小。绑定血清蛋白质的药物是大约83%。单个和多个剂量线性药物动力学研究已经证明在临床剂量(375毫克每日两次)。药物消除半衰期平均终端约7个小时。消除的主要途径是通过肝脏代谢。体外研究表明,喹硫平主要是生物新陈代谢的细胞色素P450 (CYP) 3 a4。政府[14 c]喹硫平后,大约73%的放射性排出的尿液和粪便的21%。 Quetiapine accounted for less than 1% of the excreted radioactivity. 11 metabolites formed through hepatic oxidation have been identified. Two were found to be pharmacologically active, but they circulate in plasma at 2 to 12% of the concentration of quetiapine and are unlikely to contribute substantially to the pharmacological effects of the drug. The pharmacokinetics of quetiapine do not appear to be altered by cigarette smoking. Oral clearance declines with age, and was reduced in 2 of 8 patients with hepatic dysfunction but not in patients with renal impairment. Quetiapine has no effect on the in vitro activity of CYP1A2, 2C9, 2C19, 2D6 and 3A4 at clinically relevant concentrations. The lack of effect of quetiapine on hepatic oxidation was confirmed in vivo by the lack of effect of quetiapine on antipyrine disposition. Quetiapine had no effect on serum lithium concentration. Phenytoin and thioridazine increase the clearance of quetiapine, and ketoconazole decreases clearance. No clinically significant effects of cimetidine, haloperidol, risperidone or imipramine on the pharmacokinetics of quetiapine were noted. Quetiapine dosage adjustment, therefore, may be necessary when coadministered with phenytoin, thioridazine or other potent CYP3A4 inducers or inhibitors. The relationship between the therapeutic effects and the plasma concentrations of quetiapine has been investigated in a multicentre clinical trial. There was no statistically significant association between trough plasma quetiapine concentration and clinical response as measured by traditional assessments of psychotic symptom severity. Subsequent clinical studies of the plasma concentration versus effect relationships for quetiapine may help to further define guidelines for dosage regimen design.

beplay体育安全吗DrugBank数据引用了这篇文章

药物

喹硫平

药物酶

药物	酶	类	生物	药理作用	行动
喹硫平	细胞色素P450 3 a4	蛋白质	人类	未知的	底物	细节