Kouzan S, Nebout T
Therapie. 1989 Nov-Dec;44(6):393-9.
3'-azido-3'-deoxythymidine is a thymidine analogue with an in vitro as well as in vivo efficacy towards HIV-mediated infection. Zidovudine exerts its action, following an intracellular three-step phosphorylation, through viral reverse transcriptase inhibition. Its half-life is approximately one hour. Oral biodisponibility is 65%, and passage through blood-brain barrier results in therapeutic levels is CSF. Clinical evaluation has enabled demonstration of a beneficial effect on survival of stage IV AIDS patients, when treated after a PCP episode. In this setting, aggregate survival ratios reach 73% after one year of follow-up, and 41% after 2 years. In addition, zidovudine activity has been demonstrated in treatment of HIV-induced thrombopenias as well as HIV-related central nervous system disorders. Presently, zidovudine therapeutic evaluation proceeds through the following main axes: dosage tuning (either by lowering of standard dose, and/or dose interval modification); combination with other antiviral therapies; lastly, patient treatment et an early stage of disease.
3'-叠氮-3'-脱氧胸苷是一种胸苷类似物,对HIV介导的感染具有体外和体内疗效。齐多夫定通过细胞内三步磷酸化作用,抑制病毒逆转录酶发挥作用。其半衰期约为1小时。口服生物利用度为65%,通过血脑屏障后可在脑脊液中达到治疗水平。临床评估表明,IV期艾滋病患者在PCP发作后接受治疗时,对其生存有有益影响。在此情况下,随访一年后的总生存率达到73%,两年后为41%。此外,齐多夫定在治疗HIV引起的血小板减少症以及HIV相关的中枢神经系统疾病方面也有活性。目前,齐多夫定的治疗评估主要通过以下几个方面进行:调整剂量(通过降低标准剂量和/或改变给药间隔);与其他抗病毒疗法联合使用;最后,在疾病早期对患者进行治疗。