灰黄霉素和氟伏沙明交互与茶碱的新陈代谢。

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拉斯穆森BB Jeppesen U, Gaist D, Brosen K

灰黄霉素和氟伏沙明交互与茶碱的新陈代谢。

其他药物Monit。1997年2月,19 (1):56 - 62。

PubMed ID

9029748 (在PubMed

]

文摘

茶碱主要是由细胞色素代谢P4501A2 (CYP1A2)。灰黄霉素之间可能的相互作用和茶碱据报道,我们的实验室,导致我们形成了灰黄霉素诱发的假设茶碱的新陈代谢。本研究的目的是调查这一假设。这项研究进行了随机交叉研究的12个健康志愿者。时期的研究,每个志愿者接受单剂量300毫克茶碱乙二胺口服。这些受试者时期B,氟伏沙明、50毫克1天,100毫克6天,第四天,受试者摄入300毫克茶碱乙二胺。氟伏沙明是CYP1A2的强有力的抑制剂和B是包括作为一个积极的控制。这些受试者时期C, 500毫克灰黄霉素为9天;8天再次受试者摄入300毫克茶碱乙二胺。茶碱及其代谢物(1-methyluric酸(IMU) 3-methylxanthine [3 mx),和1,3-dimethyluric酸[13 dmu])的高效液相色谱在血浆和尿液化验。 During fluvoxamine intake, the median of the total clearance of theophylline decreased from 80 ml/min to 24 ml/min, and the half-life increased from 6.6 to 22 h. The partial formation clearances of the metabolites decreased from 17 to 1.7 ml/min, from 8.9 to 0.9 ml/min, and from 21 to 6.8 ml/min for 1MU, 3MX, and 13DMU, respectively. The results confirm that assessment of theophylline metabolism indeed serves as a biomarker for CYP1A2. During griseofulvin ingestion, the median of the total and partial clearances of theophylline were 84 ml/min, 22 ml/min (1MU), 9.4 ml/min (3MX), and 25 ml/min (13DMU). The half-life decreased significantly from 6.6 to 5.7 h. The increase in partial formation clearances of 1MU and 13DMU, but not of 3MX, were statistically significant. The increase in the total clearance reached only borderline significance. In four subjects a marked induction was seen for all pharmacokinetic parameters, suggesting that the susceptibility to induction is more pronounced in some subjects. This susceptibility could theoretically be explained by a polymorphism in the inducibility of the gene coding for the CYP1A2 enzyme.

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药物酶

药物	酶	类	生物	药理作用	行动
灰黄霉素	细胞色素P450 1 a2	蛋白质	人类	未知的	诱导物	细节