149003-01-0

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Questions And Answer

• Description

  Dexrazoxane hydrochloride is a cytoprotective agent which is hydrolysed to an active metabolite that chelates iron within cells.
  It is used (as Cardioxane) to reduce the cardiotoxicity of doxorubicin and other anthracyclines. It actively chelates iron within cells, thus preventing the formation of the anthracycline--iron complex that is thought to cause cardiotoxicity.
  It is also use (as Savene) in the management of anthracycline extravasation, where its action is to inhibit the enzyme topoisomerase II.;

• Biological Activity

  Dexrazoxane hydrochloride is a topoisomerase II inhibitor and intracellular ion chelator. Bridges and stabilizes an interface between two ATPase promoters to inhibit topoisomerase II activity. Cardioprotective when co-administered with doxorubicin; decreases formation of reactive oxygen species (ROS) and activates the PI3K/Akt survival pathway.;

• ZINECARD

  ZINECARD® (dexrazoxane for injection) is a sterile, pyrogen-free lyophilizate intended for intravenous administration. It is a cardioprotective agent for use in conjunction with doxorubicin.
  Dexrazoxane, a potent intracellular chelating agent is a derivative of EDTA. Dexrazoxane is a whitish crystalline powder that melts at 191° to 197°C. It is sparingly soluble in water and 0.1 N HCl, slightly soluble in ethanol and methanol, and practically insoluble in nonpolar organic solvents. The pKa is 2.1. Dexrazoxane has an octanol/water partition coefficient of 0.025 and degrades rapidly above a pH of 7.0.
  ZINECARD is available in 250 mg and 500 mg single use only vials. ZINECARD must be reconstituted with Sterile Water for Injection, USP.
  Each 250 mg vial contains dexrazoxane hydrochloride equivalent to 250 mg dexrazoxane. Hydrochloric Acid, NF is added for pH adjustment.. When reconstituted as directed with 25 mL of Sterile Water for Injection, USP, each mL contains: 10 mg dexrazoxane. The pH of the resultant solution is 1.0 to 3.0.;

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