RED WINE EFFECTS ON CYTOCHROME P450 3A4 ACTIVITY IN HEALTHY INDIVIDUALS

通常摄入的化合物，如葡萄柚汁和红酒，可能对细胞色素P450 3A4 （CYP3A4）酶代谢的药物的治疗效果有影响。我们之前的体外研究表明，红酒可能抑制CYP3A4的程度与葡萄柚汁相似。我们目前的研究目的是确定红酒对CYP3A4的抑制是否会导致药物水平的临床显著升高。本研究将对12名健康志愿者进行双向交叉研究。单次口服8mg /kg环孢素（CYP3A4活性的标记物）将在不同场合与水和红酒一起服用。全血水平将被提取并通过特定的荧光偏振免疫分析法分析，并将环孢素的药代动力学进行比较。

Commonly ingested compounds such as grapefruit juice and red wine may have effects on the therapeutic efficacy of drugs metabolized by the cytochrome P450 3A4 (CYP3A4) enzyme. Our previous in vitro work suggests that red wine may inhibit CYP3A4 to a similar degree as found with grapefruit juice. Our current investigation purposes to determine whether inhibition of CYP3A4 by red wine can result in clinically significant elevations in drug levels. This study will investigate twelve healthy volunteers in a two-way cross-over study. A single 8 mg/kg oral dose of cyclosporine (a marker for CYP3A4 activity) will be given with water and red wine on separate occasions. Whole blood levels will be drawn and analyzed by a specific fluorescence polarization immunoassay, and the pharmacokinetics of cyclosporine will be compared.