PHARMACOKINETICS/DYNAMICS OF COMBINED KETOCONAZOLE/TRIAZOLAM/ALPRAZOLAM

复方酮康唑/三唑仑/阿普唑仑的药代动力学/动力学

• 批准号: 6245518
• 负责人: DAVID J GREENBLATT
• 金额: $ 2.82万
• 依托单位: TUFTS MEDICAL CENTER
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-05-01 至 1997-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6245518
• 关键词: alprazolam; clinical research; drug interactions; human subject; ketoconazole; pharmacokinetics; triazolam

In vitro studies of human liver microsomal preparations done in our laboratory identify the antifungal agent ketoconazole as a potent inhibitor of cytochrome P450-3A4, the enzyme responsible for biotransformation of the benzodiazepines triazolam and alprazolam in humans. In vitro data predicts a clinically important pharmacokinetic interaction of ketoconazole with triazolam and alprazolam in humans, much as has been reported during concurrent treatment of ketoconazole with terfenadine (seldane). The present study is a controlled evaluation of the potential interaction of ketoconazole with triazolam and with alprazolam, including the clinical consequences of the interaction.

在我们的研究中进行的人肝微粒体制备物的体外研究 实验室确定抗真菌剂酮康唑作为一种有效的 细胞色素P450 - 3A4的抑制剂， 苯二氮卓类药物三唑仑和阿普唑仑在 人类 体外数据预测了具有临床意义的药代动力学 酮康唑与三唑仑和阿普唑仑在人体内的相互作用， 与酮康唑与 特非那定（硒）。 本研究是一项对照评价， 酮康唑与三唑仑以及与 阿普唑仑，包括相互作用的临床后果。