Hirschel B
Division des maladies infectieuses, Hôpital cantonal universitaire, Genève.
Ther Umsch. 1994 Aug;51(8):545-50.
Three drugs are currently available to treat HIV infection: zidovudine, didanosine, and zalcitabine. They resemble the natural nucleosides and inhibit retrotranscriptase, an enzyme which transforms HIV's genomic RNA into DNA. Indications for treatment are symptomatic HIV infection and, in asymptomatic patients, moderate immunodeficiency with a CD4-lymphocyte count below 350/mm3. In patients who have not yet received antiviral treatment, zidovudine remains the drug of choice, in spite of its toxicity for the bone marrow, which is particularly problematic in those with advanced immunodeficiency. Unfortunately, HIV develops resistance to zidovudine, and its efficacy wanes after a few months. When that happens, zidovudine may be replaced by didanosine, which is mainly toxic for the pancreas, or by zalcitabine, which causes peripheral neuropathy. A number of drugs are being developed. Among these, nonnucleoside retrotranscriptase inhibitors are well tolerated, but rapid development of resistance is problematic. Resistance seems less of a problem for inhibitors of the viral protease, but biodispensibility of these drugs is poor.
目前有三种药物可用于治疗HIV感染：齐多夫定、去羟肌苷和扎西他滨。它们类似于天然核苷，可抑制逆转录酶，该酶能将HIV的基因组RNA转化为DNA。治疗指征为有症状的HIV感染，对于无症状患者，CD4淋巴细胞计数低于350/mm³的中度免疫缺陷也适用。在尚未接受抗病毒治疗的患者中，尽管齐多夫定对骨髓有毒性，这在晚期免疫缺陷患者中尤其成问题，但它仍是首选药物。不幸的是，HIV会对齐多夫定产生耐药性，几个月后其疗效就会减弱。出现这种情况时，齐多夫定可被主要对胰腺有毒性的去羟肌苷或导致周围神经病变的扎西他滨替代。许多药物正在研发中。其中，非核苷类逆转录酶抑制剂耐受性良好，但耐药性快速产生是个问题。对于病毒蛋白酶抑制剂，耐药性似乎不是什么大问题，但这些药物的生物利用度较差。
