Hanna GJ, D'Aquila RT
Infectious Disease Unit and AIDS Research Center, Massachusetts General Hospital, 149 13th Street, Charlestown, MA 02129, USA.
Curr Infect Dis Rep. 1999 Aug;1(3):289-297. doi: 10.1007/s11908-999-0032-4.
Progress in understanding antiretroviral resistance has evolved rapidly in recent years. Specific resistance mutations have been associated with virologic failure of different nucleoside reverse transcriptase inhibitors (NRTIs). These mutations vary in the extent of cross resistance they confer to other drugs in the same class. In addition, two novel mutational patterns conferring resistance to multiple NRTIs have been recognized. Considerable class-specific cross resistance also exists among viruses with reduced susceptibility to nonnucleoside reverse transcriptase inhibitors (NNRTIs). Among protease inhibitors, low level resistance that arises early during virologic failure may be drug specific in some situations, but high level resistance seen later during suboptimal therapy is likely to confer cross resistance to the entire class. Prevalence of drug resistance in infected patients appears to be considerable, and transmission of multidrug-resistant virus has been documented. Current methods of testing for resistance are promising, but they have significant limitations and require further clinical validation. The best approach to prevent resistance is to start treatment early during infection with a regimen that engenders good compliance and is potent enough to decrease viral load to below detection limits of the most sensitive assay available. Once resistance arises, salvage regimens in general have compromised efficacy and should be planned with attention to the patient's prior drug treatment history and the viruses' suspected or demonstrated resistance patterns.
近年来,在理解抗逆转录病毒耐药性方面取得了迅速进展。特定的耐药突变与不同核苷类逆转录酶抑制剂(NRTIs)的病毒学失败有关。这些突变赋予同一类中其他药物的交叉耐药程度各不相同。此外,还识别出了两种赋予对多种NRTIs耐药性的新型突变模式。对非核苷类逆转录酶抑制剂(NNRTIs)敏感性降低的病毒之间也存在相当程度的类别特异性交叉耐药。在蛋白酶抑制剂中,病毒学失败早期出现的低水平耐药在某些情况下可能是药物特异性的,但在次优治疗后期出现的高水平耐药可能会赋予对整个类别的交叉耐药。感染患者中耐药性的流行情况似乎相当严重,并且已经记录了多重耐药病毒的传播。目前的耐药性检测方法很有前景,但它们有显著局限性,需要进一步的临床验证。预防耐药性的最佳方法是在感染早期开始治疗,采用一种能产生良好依从性且足够强效以将病毒载量降低到现有最敏感检测方法检测限以下的方案。一旦出现耐药性,挽救方案通常疗效会受损,制定时应注意患者既往的药物治疗史以及病毒疑似或已证实的耐药模式。