COMPARISON OF CARDIOVASCULAR ACTIONS OF DAUNOMYCIN, ADRIAMYCIN AND N-ACETYLDAUNOMYCIN IN HAMSTERS AND MONKEYS
COMPARISON OF CARDIOVASCULAR ACTIONS OF DAUNOMYCIN, ADRIAMYCIN AND N-ACETYLDAUNOMYCIN IN HAMSTERS AND MONKEYS
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DOI：
10.1159/000136248
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发表时间：
1971-01-01
期刊：
影响因子：
3.1
通讯作者：
WARAVDEKAR, VS
中科院分区：
文献类型：
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作者：
HERMAN, E;MHATRE, R;WARAVDEKAR, VS
阿霉素（12.5-50.0 mg/kg）对仓鼠和恒河猴最一致的初始效应是心动过缓、低血压、室性心律失常和呼吸抑制。道诺霉素（50mg /kg）产生室性心律失常，剂量是阿霉素的两倍。在这两个物种中，大剂量的n -乙酰道诺霉素（200 mg/kg）只引起所有参数的微小变化。在注射后不久，在仓鼠的心脏和肺组织中检测到所有3种母体化合物的显著量。发现道霉素和阿霉素转化为苷元的速度都相对较快，但阿霉素苷元在这两种组织中的浓度明显较高。相比之下，n -乙酰道诺霉素的转化相对较少。因此，观察到的药理作用可能与3种化合物的代谢差异有关。
The most consistent initial effects of adriamycin (12.5–50.0 mg/kg) in hamsters and rhesus monkeys were bradycardia, hypotension, ventricular arrhythmias and respiratory depression. Daunomycin (50 mg/kg) produced ventricular arrhythmias at twice the dose of adriamycin. In both species large doses of N-acetyldaunomycin (200 mg/kg) caused only minimal changes in all parameters. Significant amounts of all 3 parent compounds were detected in hamster heart and lung tissues soon after injection. A relatively rapid conversion of both daunomycin and adriamycin to the aglycone was found, but a significantly higher percentage of the adriamycin aglycone was concentrated in these 2 tissues. In contrast, relatively little conversion of N-acetyldaunomycin was detected. Thus, the observed pharmacological actions may be related to differences in metabolism of the 3 compounds.