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5-氮胞嘧啶核苷对动物和人的好几种肿瘤治疗有效,有人用该药每天静注(15～30分钟内)5天一个疗程,剂量逐渐增加至400毫克/米~2,治疗急性白血病18例,3例完全缓解,4例部分缓解,有人用减半剂量,治疗18例,结果5例完全缓解,但由于静脉推注给药,造成严重的副作用:有粒细胞抑制、恶心、呕吐、腹泻、发热,偶而还可发生高血压。经薄层分析、核磁共振研究指出:在25℃缓冲溶液中,该药的半衰期为60～100小时。Karon等发现假如在维持抗肿瘤的有效浓度下,给药时间延长超过10～15分钟,或分散剂量给药,则可明显减少胄肠道的毒性反应。
5-Azacytidine is effective in the treatment of several tumors in animals and humans. Some people use the drug once a day for 5 days for a course of treatment (15 to 30 minutes) and the dosage gradually increases to 400 mg / m 2. Acute leukemia in 18 cases, 3 cases of complete remission, 4 cases of partial remission, some with half dose reduction, treatment of 18 cases, the results of 5 cases of complete remission, but due to intravenous injection, causing serious side effects: with granulocyte inhibition, nausea , Vomiting, diarrhea, fever, and occasionally high blood pressure can occur. After thin layer analysis, NMR studies indicate that the half-life of the drug in the buffer solution at 25 ° C is 60 to 100 hours. Karon et al. Found that if prolonged administration over 10 to 15 minutes at an effective concentration to maintain antitumor activity, or in a discrete dosage regimen, can significantly reduce the intestinal toxicity.