Department of Pharmacology, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla, Thailand.
Biopharm Drug Dispos. 2011 Apr;32(3):168-74. doi: 10.1002/bdd.748. Epub 2011 Mar 1.
To investigate the pharmacokinetic interaction between ciprofloxacin and itraconazole in healthy male volunteers.
Ten healthy male volunteers were assigned into a 2-sequence, 3-period pharmacokinetic interaction study. In phase 1, all subjects were randomly assigned to receive 500 mg of ciprofloxacin alone and 200 mg of itraconazole alone twice daily for 7 days with a 14 day wash-out period in a crossover design. Phase 2 was performed 14 days after finishing phase 1, all subjects received 500 mg of ciprofloxacin in combination with 200 mg of itraconazole twice daily for 7 days. Ciprofloxacin and itraconazole pharmacokinetics were studied and adverse effects noted.
Ciprofloxacin significantly increased the C(max) and AUC(0 - ∞) of itraconazole by 53.13% and 82.46%, respectively. The half-life and CL of itraconazole were not changed significantly. The combination of itraconazole and ciprofloxacin could therefore result in an increase in adverse drug reactions. Conversely, itraconazole had no significant effect on the pharmacokinetics of ciprofloxacin.
Ciprofloxacin decreases the metabolism of itraconazole, most likely through inhibition of CYP3A4. The dosage of itraconazole should be reduced and its therapeutic outcome should be monitored closely when these two agents are concomitantly administered.
研究环丙沙星与伊曲康唑在健康男性志愿者体内的药代动力学相互作用。
将 10 名健康男性志愿者随机分为 2 组，采用 3 周期交叉设计。第 1 阶段，所有受试者分别单独接受 500 mg 环丙沙星和 200 mg 伊曲康唑，每日 2 次，连续 7 天，洗脱期 14 天；第 2 阶段在第 1 阶段结束后 14 天进行，所有受试者接受 500 mg 环丙沙星与 200 mg 伊曲康唑，每日 2 次，连续 7 天。观察药物的药代动力学和不良反应。
环丙沙星使伊曲康唑的 Cmax 和 AUC（0-∞）分别增加了 53.13%和 82.46%。伊曲康唑的半衰期和清除率无明显变化。因此，伊曲康唑与环丙沙星合用可能会增加不良反应的发生。相反，伊曲康唑对环丙沙星的药代动力学无显著影响。
环丙沙星可抑制 CYP3A4，减少伊曲康唑的代谢。当这两种药物同时使用时，应减少伊曲康唑的剂量并密切监测其治疗效果。
