Hirschel B, Vanhems P
Division des maladies infectieuses, Hôpital cantonal universitaire, Genève.
Schweiz Med Wochenschr. 1991 Aug 24;121(34):1187-93.
Zidovudine (azidothymidine, Retrovir) and ddI (di-deoxy-inosine, Videx) interfere with the multiplication of HIV by incorporation into nascent DNA chains and interruption of the further linking of nucleotides. Zidovudine lowers early mortality in patients with Aids and pneumocystis carinii pneumonia. However, much of the effectiveness of zidovudine is lost later on; the average prolongation of life in treated patients is estimated to be about 1 year. About two thirds of patients with Aids can be treated with zidovudine; in the others, the drug is ineffective or contraindicated. Frequent blood counts are necessary to monitor myelotoxicity, even at relatively low doses of 500 mg/day. In contrast, zidovudine is well tolerated by asymptomatic patients with 200 to 500 CD4 lymphocytes/mm3, in whom it diminishes the incidence of Aids from about 7 to 3% during the first year of treatment, with less than 2% severe anemia or leukopenia. For patients who do not tolerate zidovudine, ddI is an alternative. It is not myelotoxic but can cause neuritis and pancreatitis, especially at doses in excess of 10 mg/kg/day. Although its antiviral effect is excellent both in vitro and in vivo, there is still a lack of firm data on its clinical value, such as the decrease in opportunistic infections and increase in survival.
齐多夫定（叠氮胸苷，Retrovir）和去羟肌苷（双脱氧肌苷，Videx）通过掺入新生DNA链并中断核苷酸的进一步连接来干扰HIV的增殖。齐多夫定可降低艾滋病合并卡氏肺孢子虫肺炎患者的早期死亡率。然而，齐多夫定的大部分疗效在后期会丧失；接受治疗的患者平均预期寿命延长约1年。约三分之二的艾滋病患者可用齐多夫定治疗；对其他患者而言，该药无效或禁忌使用。即使在相对低剂量（500毫克/天）时，也需要频繁进行血细胞计数以监测骨髓毒性。相比之下，齐多夫定在无症状且CD4淋巴细胞计数为200至500个/立方毫米的患者中耐受性良好，在这些患者中，治疗第一年艾滋病发病率从约7%降至3%，严重贫血或白细胞减少症发生率低于2%。对于不能耐受齐多夫定的患者，去羟肌苷是一种替代药物。它没有骨髓毒性，但可引起神经炎和胰腺炎，尤其是剂量超过10毫克/千克/天时。尽管其在体外和体内的抗病毒效果都很好，但关于其临床价值，如机会性感染减少和生存率提高等，仍缺乏确凿数据。
