1,4 - 二羟基 - 5,8 - 双[（2 - [（2 - 羟乙基）氨基]乙基]氨基] - 9,10 - 蒽二酮的临床动力学
Clinical kinetics of 1, 4-dihydroxy-5,8-bis [(2-[(2-hydroxyethyl) amino] ethyl] amino ]-9, 10-anthracenedione.
作者信息
Savaraj N, Lu K, Valdivieso M, Burgess M, Umsawasdi T, Benjamin R S, Loo T L
出版信息
Clin Pharmacol Ther. 1982 Mar;31(3):312-6. doi: 10.1038/clpt.1982.39.
The clinical kinetics of 1, 4-dihydroxy-5,8-bis[[ 2-[(2-hydroxyethyl) amino] ethyl] amino]-9,10-anthracenedione dihydrochloride (DHAQ) are reported. DHAQ, 1 to 3 mg/m2, was administered as an intravenous bolus to six patients with metastatic cancer. Plasma clearance of the drug followed a biphasic pattern with a harmonic mean initial half-life (t 1/2) of 13.7 min and a terminal t 1/2 of 37.4 hr. Recovery of unchanged drug in the urine was 6.8% at 24 hr and 7.3% at 72 hr, while the corresponding recovery of total radioactivity was 9.4% and 11.3%. Apparent volume of distribution of DHAQ was about 13.8 +/- 2.9 l/kg. Total clearance was 238.7 ml/kg/hr, twice the creatinine clearance.
报告了1,4 - 二羟基 - 5,8 - 双[[2 - [(2 - 羟乙基)氨基]乙基]氨基] - 9,10 - 蒽二酮二盐酸盐（DHAQ）的临床动力学。以1至3mg/m²的剂量将DHAQ静脉推注给予6例转移性癌症患者。该药物的血浆清除呈双相模式，谐波平均初始半衰期（t1/2）为13.7分钟，终末t1/2为37.4小时。24小时尿液中未变化药物的回收率为6.8%，72小时时为7.3%，而相应的总放射性回收率分别为9.4%和11.3%。DHAQ的表观分布容积约为13.8±2.9l/kg。总清除率为238.7ml/kg/hr，是肌酐清除率的两倍。
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