奥氮平的药物动力学的影响缺乏单一剂量氨茶碱在健康男性。

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Macias西城,Bergstrom射频、Cerimele BJ Kassahun K,泰特姆·德·卡拉汉JT

奥氮平的药物动力学的影响缺乏单一剂量氨茶碱在健康男性。

药物治疗。1998;11 - 12月18 (6):1237 - 48。

PubMed ID
9855322 (在PubMed
]
文摘

研究目的:测试是否奥氮平,非典型抗精神病药物,是一种抑制剂细胞色素P450 (CYP) 1 a2的活动,我们进行了一项与茶碱药物相互作用的研究,一个已知的CYP1A2衬底。设计:双向随机交叉研究。背景:临床研究实验室。必威国际app主题:19岁的健康男性(16吸烟者,3不吸烟者)。干预措施:因为先天的期望没有奥氮平对茶碱药物动力学的影响,一个平行的研究使用甲氰咪胍作为一个积极的控制。在组1中,12名健康受试者收到后30分钟静脉输液氨茶碱350毫克连续9天的奥氮平或安慰剂。2组,7个健康受试者收到类似氨茶碱注入经过连续9天的西咪替丁或安慰剂。测量及主要结果:茶碱和其在血清和尿液代谢物的浓度测定24和72小时,分别。奥氮平及其代谢物的血浆浓度测定24小时后下一个最后剂量和168小时后最后奥氮平剂量。奥氮平并不影响茶碱药物动力学。 However, cimetidine significantly decreased theophylline clearance and the corresponding formation of its metabolites. Urinary excretion of theophylline and its metabolites was unaffected by olanzapine but was reduced significantly by cimetidine. Steady-state concentrations of olanzapine (15.3 ng/ml), 10-N-glucuronide (4.9 ng/ml), and 4'-N-desmethyl olanzapine (2.5 ng/ml) were observed after olanzapine 10 mg once/day and were unaffected by coadministration of theophylline. CONCLUSION: As predicted by in vitro studies, steady-state concentrations of olanzapine and its metabolites did not affect theophylline pharmacokinetics and should not affect the pharmacokinetics of other agents metabolized by the CYP1A2 isozyme.

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药物酶
药物 生物 药理作用 行动
氨茶碱 细胞色素P450 1 a2 蛋白质 人类
未知的
底物
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