INTERACTION OF DILTIAZEM & VERAPAMIL WITH SIMVASTATIN

地尔硫卓的相互作用

• 批准号: 6265102
• 负责人: D CRAIG BRATER
• 金额: $ 0.04万
• 依托单位: INDIANA UNIV-PURDUE UNIV AT INDIANAPOLIS
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-12-01 至 1999-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6265102
• 关键词: antihypercholesterolemic agent; clinical research; clinical trial phase I; cytochrome P450; diltiazem; drug interactions; human subject; human therapy evaluation; pharmacokinetics; verapamil

Simvastatin, like lovastatin is converted to active metabolites by cytochrome P450 3A4 (CYP3A4). We have shown that lovastatin is susceptible to interactions with a commonly used calcium antagonist, diltiazem, that is known to have the capacity to block CYP3A4. Verapamil can similarly block this enzyme. The current study is to quantify the interaction of diltiazem and of verapamil with simvastatin since combinations of either of these calcium antagonists with simvastatin are likely to occur frequently.

辛伐他汀与洛伐他汀一样，通过细胞色素P450 3A4（CYP3A4）转化为活性代谢物。 我们已经证明，洛伐他汀易与常用的钙拮抗剂地尔硫卓发生相互作用，已知地尔硫卓具有阻断CYP3A4的能力。 维拉帕米同样可以阻断这种酶。 目前的研究是定量地尔硫卓和维拉帕米与辛伐他汀的相互作用，因为这些钙拮抗剂与辛伐他汀的组合可能经常发生。