Ekwall B
Toxicol Lett. 1981 Feb;7(4-5):359-66. doi: 10.1016/0378-4274(81)90061-8.
As a measure of the relevance to human drug effects of drug cytotoxicity in vitro, calculated and actual therapeutic blood concentrations of 50 drugs were divided by their 50% inhibitory concentrations for HeLa cells in vitro to make up three types of cytotoxic quotients (CQTv, CQTd, and CQTr). When the various quotients were compared with known cytotoxic effects of the drugs the parameters correlated well. While most drugs at single dosage reached concentrations with low quotients (CQTv and CQTd) corresponding to few reported cytotoxic effects and side effects, a substantial number of drugs at repeated dosage reached concentrations with high quotients (CQTr) corresponding to known or suspected cytotoxic action in man.
作为体外药物细胞毒性与人体药物效应相关性的一种衡量方法,计算了50种药物的实际治疗血药浓度,并将其除以它们对体外HeLa细胞的50%抑制浓度,以构成三种类型的细胞毒性商数(CQTv、CQTd和CQTr)。当将各种商数与药物已知的细胞毒性作用进行比较时,这些参数具有良好的相关性。虽然大多数单次给药的药物达到的浓度对应的商数较低(CQTv和CQTd),报告的细胞毒性作用和副作用较少,但相当数量的重复给药药物达到的浓度对应的商数较高(CQTr),与人已知的或疑似的细胞毒性作用相对应。