Radboud University Nijmegen Medical Centre, Department of Clinical Pharmacy, Nijmegen, The Netherlands.
J Antimicrob Chemother. 2010 Oct;65(10):2188-94. doi: 10.1093/jac/dkq280. Epub 2010 Jul 28.
To manage the interaction between fosamprenavir/ritonavir and posaconazole, we hypothesized that ritonavir can be replaced by posaconazole as an alternative booster of fosamprenavir with no significant influence on posaconazole pharmacokinetics.
This was an open-label, randomized, three period, cross-over, single-centre trial in 24 healthy volunteers. All subjects received the following three treatments for 10 days, separated by washout periods of 17 days: posaconazole 400 mg twice daily; fosamprenavir/ritonavir 700/100 mg twice daily; posaconazole 400 mg twice daily with fosamprenavir 700 mg twice daily.
Twenty subjects completed the trial. Geometric mean ratios (GMR; +90% confidence interval) of posaconazole AUC and C(max) when taken with fosamprenavir versus posaconazole alone were 0.77 (0.68-0.87) and 0.79 (0.71-0.89), respectively. The GMRs of amprenavir AUC and C(max) when taken as fosamprenavir and posaconazole versus fosamprenavir/ritonavir were 0.35 (0.32-0.39) and 0.64 (0.55-0.76), respectively. No serious adverse events were reported during the trial.
Unboosted fosamprenavir should not be used concomitantly with posaconazole.
为了管理福沙那韦/利托那韦与泊沙康唑的相互作用，我们假设利托那韦可以被泊沙康唑替代，作为福沙那韦的替代增效剂，而对泊沙康唑的药代动力学没有显著影响。
这是一项在 24 名健康志愿者中进行的开放标签、随机、三周期、交叉、单中心试验。所有受试者接受以下三种治疗方案，每种方案治疗 10 天，洗脱期为 17 天：每日两次口服泊沙康唑 400mg；每日两次口服福沙那韦/利托那韦 700/100mg；每日两次口服泊沙康唑 400mg 同时口服福沙那韦 700mg 两次。
20 名受试者完成了试验。与单独服用泊沙康唑相比，当与福沙那韦合用时，泊沙康唑 AUC 和 C(max)的几何均数比值（GMR；+90%置信区间）分别为 0.77（0.68-0.87）和 0.79（0.71-0.89）。当作为福沙那韦和泊沙康唑服用时，福沙那韦 AUC 和 C(max)的 GMR 分别为 0.35（0.32-0.39）和 0.64（0.55-0.76）。试验期间未报告严重不良事件。
未增效的福沙那韦不应与泊沙康唑同时使用。
