...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Antimicrobial agents and chemotherapy. >Pharmacokinetics of saquinavir, atazanavir, and ritonavir in a twice-daily boosted double-protease inhibitor regimen.
【24h】

Pharmacokinetics of saquinavir, atazanavir, and ritonavir in a twice-daily boosted double-protease inhibitor regimen.

机译：沙奎那韦，阿扎那韦和利托那韦在每天两次加强双蛋白酶抑制剂治疗方案中的药代动力学。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

The objective of this study was to evaluate the pharmacokinetics of atazanavir (ATV), saquinavir (SQV), and ritonavir (RTV) in a boosted double-protease inhibitor (PI) therapy regimen without reverse transcriptase inhibitors (RTIs). The study design was as follows. Patients with limited RTI options received a PI combination of 300/100 mg ATV/RTV once daily and 1,000 mg SQV twice daily (group 1; n=49) without RTI comedication. The results were compared to the plasma concentrations of PIs of patients taking either 300 mg ATV/100 mg RTV once daily plus RTIs (group 2; n=72) or patients taking 1,000 mg SQV/100 mg RTV plus RTIs (group 3; n=90). The study methods were as follows. Patients were given a 12/24-h pharmacokinetic assessment at steady state. Drug concentrations were measured by liquid chromatography-tandem mass spectrometry. The minimum and maximum concentrations (Cmin and Cmax), area under the concentration-time curve under steady-state conditions (AUCss), elimination half-life, time of maximum concentration and lag time were subject to statistical analysis. The results show that patients treated with ATV/SQV/RTV exhibited significantly high SQV concentrations and moderate enhancement of the AUCss of ATV in comparison to those of patients of the control groups: for SQV in groups 1 and 3, the geometric mean (GM) of the AUCss was 22,794 versus 15,759 ng.h/ml (GM ratio [GMR]=1.45; P<0.05), the GM of the Cmax was 3,257 versus 2,331 ng/ml (GMR=1.40; P<0.05), and the GM of the Cmin was 438 versus 437 ng/ml (GMR=1.00); for ATV in groups 1 and 2, the GM of the AUCss was 39,154 versus 33,626 ng.h/ml (GMR=1.16), the GM of the Cmax was 3,488 versus 2,924 ng/ml (GMR=1.20), and the GM of the Cmin was 515 versus 428 ng/ml (GMR=1.21). RTV levels were comparable for all groups. A subgroup analysis detected only marginal differences in ATV plasma exposure if combined with tenofovir-disoproxilfumarate and without it. We conclude that our pharmacokinetic results support the use of a boosted double-PI regimen of ATV/SQV/RTV as a treatment option for patients who need antiretroviral therapy without RTIs.
机译：这项研究的目的是评估在没有逆转录酶抑制剂（RTIs）的加强型双蛋白酶抑制剂（PI）治疗方案中阿扎那韦（ATV），沙奎那韦（SQV）和利托那韦（RTV）的药代动力学。研究设计如下。 RTI选择受限的患者每天接受一次300/100 mg ATV / RTV和每天两次1,000 mg SQV的PI组合（第1组; n = 49），无需RTI喜剧。将结果与每天服用300 mg ATV / 100 mg RTV加上RTIs的患者血浆PI浓度进行比较（第2组; n = 72）或服用1,000 mg SQV / 100 mg RTV加上RTIs的患者PI 3血浆浓度（第3组; n = 90）。研究方法如下。患者在稳态下接受12/24小时药代动力学评估。通过液相色谱-串联质谱法测量药物浓度。对最小和最大浓度（Cmin和Cmax），稳态条件下浓度时间曲线下的面积（AUCss），消除半衰期，最大浓度时间和滞后时间进行统计分析。结果显示，与对照组患者相比，接受ATV / SQV / RTV治疗的患者表现出明显高的SQV浓度和ATV的AUCs适度增强：对于第1组和第3组的SQV，几何平均值（GM） AUCss的平均值为22,794对15,759 ng.h / ml（GM比[GMR] = 1.45; P <0.05），Cmax的GM为3,257对2,331 ng / ml（GMR = 1.40; P <0.05）， Cmin的GM为438对437 ng / ml（GMR = 1.00）;对于第1组和第2组中的ATV，AUCss的GM为39,154对33,626 ng.h / ml（GMR = 1.16），Cmax的GM为3,488对2,924 ng / ml（GMR = 1.20），GM为Cmin为515对428 ng / ml（GMR = 1.21）。所有组的RTV水平相当。亚组分析仅在与替诺福韦-二异丙基富马酸酯联合使用时和没有联合使用时，仅检测到亚视血浆暴露的边缘差异。我们得出的结论是，我们的药代动力学结果支持ATV / SQV / RTV的双PI强化方案作为需要抗逆转录病毒治疗而无需RTI的患者的治疗选择。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号