沙奎那韦软胶囊与利福布汀在HIV感染患者中的相互作用。
Interaction between saquinavir soft-gel and rifabutin in patients infected with HIV.
作者信息
Moyle G J, Buss N E, Goggin T, Snell P, Higgs C, Hawkins D A
机构信息
Kobler Clinic, Chelsea and Westminster Hospital, 369 Fulham Rd, London SW10 9NH, UK.
出版信息
Br J Clin Pharmacol. 2002 Aug;54(2):178-82. doi: 10.1046/j.1365-2125.2002.01631.x.
AIMS
To evaluate the potential pharmacokinetic interaction between the HIV protease inhibitor saquinavir and rifabutin.
METHODS
Fourteen HIV-infected patients provided full steady-state pharmacokinetic profiles following administration of rifabutin alone (300 mg once daily) or saquinavir soft-gel formulation (1200 mg three times daily) plus rifabutin (300 mg once daily) in this open label, partially randomized study.
RESULTS
Coadministration of saquinavir and rifabutin resulted in a reduction in saquinavir AUC(0,8 h) and C(max)(0,8 h) of 47% (95% CI 30, 60%) and 39% (95% CI 11, 59%), respectively. Rifabutin AUC(0,24 h) and C(max)(0,24 h) was increased by an average of 44% (95% CI 17, 78%) and 45% (95% CI 14, 85%), respectively. Saquinavir in combination with rifabutin was well tolerated. Gastrointestinal intolerance and asymptomatic increases in liver enzymes were the only adverse events of note.
CONCLUSIONS
Administration of rifabutin with saquinavir may decrease the efficacy of this HIV protease inhibitor.
目的
评估HIV蛋白酶抑制剂沙奎那韦与利福布汀之间潜在的药代动力学相互作用。
方法
在这项开放标签、部分随机的研究中，14名HIV感染患者在单独服用利福布汀（每日一次，300毫克）或沙奎那韦软胶囊制剂（每日三次，1200毫克）加利福布汀（每日一次，300毫克）后提供了完整的稳态药代动力学资料。
结果
沙奎那韦与利福布汀合用时，沙奎那韦的AUC(0,8 h)和C(max)(0,8 h)分别降低了47%（95%可信区间30, 60%）和39%（95%可信区间11, 59%）。利福布汀的AUC(0,24 h)和C(max)(0,24 h)分别平均增加了44%（95%可信区间17, 78%）和45%（95%可信区间14, 85%）。沙奎那韦与利福布汀联合使用耐受性良好。胃肠道不耐受和无症状的肝酶升高是唯一值得注意的不良事件。
结论
利福布汀与沙奎那韦联用时可能会降低这种HIV蛋白酶抑制剂的疗效。
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