Fredholm B, Gunnarsson K, Jensen G, Müntzing J
Acta Pharmacol Toxicol (Copenh). 1978 Mar;42(3):159-63. doi: 10.1111/j.1600-0773.1978.tb02185.x.
Prednimustine, a chlorambucil ester of pregnisolone, retarded growth of DMBA-induced mammary tumours in rats and reduced the number of tumours. A combination of chlorambucil and prednisolone (C + P) in the same proportion as in prednimustine, had similar effects, 8 and 26 mg per kg of the C + P combination being equipotnet to 16 and 64 mg per kg of prednimustine, respectively. The mortality figures suggested that prednimustine was considerably less toxic than equipotent doses of C + P. This toxicity difference was confirmed in a parallel investigation of the subacute toxicity in rats of prednimustine and C + P. This study showed that the mortality, reduction of lymphocytes and platelets, and bone marrow depression was much lower after pregnimustine than after equimolar amounts of the C + P combination. The results suggest that the low toxicity of prednimustine makes this drug a better cytostatic agent than the C + P combination treatment.
泼尼莫司汀是泼尼松龙的苯丁酸氮芥酯,可抑制二甲基苯并蒽诱导的大鼠乳腺肿瘤生长并减少肿瘤数量。与泼尼莫司汀中相同比例的苯丁酸氮芥和泼尼松龙组合(C + P)具有相似的效果,每千克体重8毫克和26毫克的C + P组合分别与每千克体重16毫克和64毫克的泼尼莫司汀等效。死亡率数据表明,泼尼莫司汀的毒性远低于等效剂量的C + P。在对泼尼莫司汀和C + P在大鼠中的亚急性毒性进行的平行研究中证实了这种毒性差异。该研究表明,泼尼莫司汀给药后,死亡率、淋巴细胞和血小板减少以及骨髓抑制程度均远低于等摩尔量的C + P组合给药后。结果表明,泼尼莫司汀的低毒性使其成为比C + P联合治疗更好的细胞抑制剂。