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核苷的可逆性转录酶抑制剂中,第一个为齐多夫丁(Zidovudine,AZT),用于艾滋病或艾滋病相关综合征(ARC)患者,能明显延长寿命,但有血液学毒性,还可能有抗AZT株。本文讨论其中第二个,即双脱氧胞苷(Dideoxycytidine,ddC)。单-ddC对人免疫缺陷病毒(HIV)感染的疗效ddC口服生物利用度约87%,血浆半减期1小时左右。本品能全部穿过血脑屏障,但AZT仅1/3。临床证明,ddC降低循环HIVP 24抗原水平,增加CD_4~+淋巴细胞数,说明它具有抗HIV活性。
Among the reversible nucleoside reverse transcriptase inhibitors, the first is Zidovudine (AZT) for patients with AIDS or AIDS-related complex (ARC), which significantly prolongs lifespan but has hematologic toxicity There may be anti-AZT strains. This article discusses the second of these, dideoxycytidine (ddC). Therapeutic effect of mono-ddC on human immunodeficiency virus (HIV) infection The oral bioavailability of ddC is about 87% and the half-life of plasma is about 1 hour. This product can all cross the blood-brain barrier, but only 1/3 AZT. Clinically proven, ddC reduce circulating HIVP 24 antigen levels, increased CD_4 ~ + lymphocyte count, indicating that it has anti-HIV activity.