The role of combinations of HIV protease inhibitors in the management of persons with HIV infection.
The role of combinations of HIV protease inhibitors in the management of persons with HIV infection.
复制标题
HIV 蛋白酶抑制剂组合在 HIV 感染者管理中的作用。
DOI：
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发表时间：
1998
影响因子：
6.1
通讯作者：
Graeme Moyle
中科院分区：
文献类型：
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作者：
Graeme Moyle
目前抗逆转录病毒治疗的标准包括两种核苷类似物逆转录酶抑制剂(NRTI)和一种有效的第三种药物，通常是艾滋病毒蛋白酶抑制剂(PI)。然而，在临床研究中，约有20%-30%的患者开始治疗，在临床实践中，可能更多的患者使用这些方案未能达到最佳的治疗反应，即持续的无法检测的病毒载量。此外，许多三联疗法目前需要每天三次剂量，这使得治疗坚持很难持续。有或没有NRTI的两种PI的组合在病毒载量方面提供了令人印象深刻的减少，新出现的数据表明，与三种药物方案相比，使用四种药物方案的患者实现低于检测反应的比例更高。此外，PI之间的药代动力学相互作用提供了减少剂量和使用PI组合每日两次给药的可能性。然而，来自双重PI失败的有限的抵抗数据，以及对脂肪代谢紊乱、脂肪营养不良和葡萄糖耐量减低的担忧仍然是这些方案作为初始治疗广泛使用的障碍。
The current standard of care in antiretroviral therapy includes two nucleoside analogue reverse transcriptase inhibitors (NRTIs) plus a potent third agent, usually an HIV protease inhibitor (PI). However, around 20 - 30% of patients initiating therapy in clinical studies, and probably more in clinical practice, fail to achieve an optimal therapeutic response, a sustained undectectable viral load, using these regimens. Additionally, many triple therapy regimens currently require three times per day dosing, making treatment adherence difficult to sustain. Combinations of two PIs with or without NRTIs provide impressive reductions in viral load, with emerging data suggesting a higher proportion of patients on four drug regimens achieving below detection responses than those on three drug regimens. Additionally, pharmacokinetic interactions between PIs provide the potential for both dose reductions and twice daily dosing with PI combinations. However, limited resistance data are available from dual PI failures, and concerns regarding disturbances in fat metabolism, lipodystrophy and glucose intolerance remain obstacles to the widespread use of these regimens as initial therapy.
HIV-1 的临床分离株几乎不含有预先存在的蛋白酶抑制剂耐药性突变。
DOI：
10.1016/0167-4838(95)00167-1
发表时间：
1995
期刊：
Biochimica et biophysica acta
影响因子：
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作者：
Yamaguchi,K;Byrn,RA
通讯作者：
Byrn,RA