Cisplatin

Cisplatin is a white powder or yellow crystalline solid with the melting point 268-272°C (decomposition). It is slightly soluble in water and easily soluble in dimethylformamide. In aqueous solution, it can be gradually transformed into trans-and hydrolysis.

Cisplatin is a cytostatic agent and it is used to treat various cancer types, including cancer of ovary, testis, lung, head, neck, bladder, neuroblastoma, and nephroblastoma, and Hodgkin’s disease and non-Hodgkin lymphoma.

administrationin the treatment of a wide variety of cancers includingnon-Hodgkin’s lymphoma, bladder cancer, ovarian cancer,testicular cancer, and cancers of the head and neck. A liposomalform is also available as well as an injectable collagenmatrix gel containing cisplatin. Compared with other platins,cisplatin is the most reactive and therefore the most effectivein platinating DNA. After IV administration, the agent iswidely distributed, highly protein bound (90%), and concentratesin the liver and kidney. After infusion, covalent attachmentto plasma proteins occurs such that after 4 hours, 90%of drug is protein bound. The elimination of platinum fromthe blood is a slow process with a terminal elimination halflifeof 5 to 10 days. Metabolism involves aquation, which occursto a greater extent once distribution out of the plasmahas occurred. Additional metabolites have been seen resultingfrom reaction with glutathione and cysteine. The greaterreactivity of cisplatin gives rise to significant toxicitiescompared with other platins. These include dose-limitingnephrotoxicity, which normally presents as elevated bloodurea nitrogen (BUN) and creatinine. This effect is cumulativeupon repeated dosing and may progress further to necrosis,altered epithelial cells, cast formation, and thickening ofthe tubular basement membranes but is generally reversibleupon discontinuation of drug treatment. Sodium thiosulfatemay be given to reduce the nephrotoxicity. Neurotoxicitymay also be dose limiting, normally presenting initially asnumbness but may progress to seizure. Other adverse effectsinclude myelosuppression, nausea, vomiting, alopecia,ototoxicity, ocular toxicity, azoospermia, impotence, myocardialinfarction, thrombotic events, and inappropriatesecretion of antidiuretic hormone.