PHARMACOKINETICS AND PROTEIN-BINDING OF CIS-DICHLORODIAMMINE PLATINUM (II) ADMINISTERED AS A ONE-HOUR OR AS A 20-HOUR INFUSION CANCER CHEMOTHERAPY AND PHARMACOLOGY GULLO, J. J., LITTERST, C. L., Maguire, P. J., Sikic, B. I., Hoth, D. F., Woolley, P. V. 1980; 5 (1): 21-26

Abstract

The pharmacokinetics of cis-dichlorodiam-minoplatinum (II) (cisplatin) have been studied in seven patients, of whom four received the drug as a one hour infusion and three received it as a 20 h infusion. The patients receiving the drug over one hour exhibited biphasic clearance of total platinum with a rapid initial phase (8.7-22.5 min) and a prolonged second phase (30.5-106 h). Free (ultrafilterable) cisplatin was readily detectable in this group and was rapidly cleared (half-life about 22 min). The volume of distribution of the drug was 50.3-65.6 liters and it was 26.6-50% excreted in the urine in 48 h. In the patients receiving the 20 h infusion, a more complex plasma elimination curve was seen, with the appearance of a secondary peak. Free drug was not detectable in these patients and they showed less urinary excretion (21.4-25.9% at 48 h) than the one hour group. Cisplatin was bound to several plasma proteins, including albumin, transferrin, and gamma-globulin. The data indicate that cisplatin is retained in the body more extensively after a 20 h infusion than after a one hour infusion.

View details for Web of Science ID A1980KV35500004

View details for PubMedID 6161715