Dexrazoxane is a drug used in human medicine. It is used as part of chemotherapy to treat various forms of cancer. For these purposes, dexrazoxane is usually administered with anthracyclines, which reduces the cytotoxic effect of dexrazoxane. Due to its pharmacological properties as well as its specific field of application, dexrazoxane belongs to the cytostatic drug class.
What is dexrazoxane?
Dexrazoxane is an active substance used in human medicine. There is an indication to perform chemotherapy, which is why dexrazoxane is a major cytostatic drug. The substance is also known as Eucardione and is sold under the trade name Cardioxane. In chemistry and pharmacology, dexrazoxane is described by the molecular formula C 11 – H 16 – N 4 – O 4 , which corresponds to a moral mass of about 268.27 g/mol. Dexrazoxane was discovered in 1964 along with several other compounds and has been used in human medicine as a cytostatic agent since the 1990s. Previously, dexrazoxane was used as a colorant in the textile industry. Today, approvals exist in several countries. In every country for which there is approval for human therapy, dexrazoxane is subject to comprehensive pharmacy and prescription requirements.
Pharmacological effects on the body and organs
Dexrazoxane exists as a white to grayish-white powder at room temperature and has a very high bioavailability of nearly 100% after ingestion. In human blood, less than two percent of the drug is present on plasma proteins in bound form. The metabolism (metabolization) of dexrazoxane occurs via the liver and thus hepatically. In the literature, the plasma half-life of the cytostatic drug – depending on the situation of the specific individual case – is set at about two to two and a half hours. Elimination is 42% via the kidneys and thus renal. The cytostatic effects of dexrazoxane, which make the drug attractive for human medicine, are based on an inhibition of topoisomerase II α. This is an enzyme that unwinds the double helix of human DNA, thereby enabling the replication of genetic information. In addition, topoisomerase II α also enables cell division. Since dexrazoxane causes topoisomerase II α to become non-functional, it becomes impossible for cells to divide. In addition, dexrazoxane also exerts cytoprotective effects. These are based on the cytostatic drug’s ability to scavenge iron ions in the cells of the heart. This makes it impossible for the heart cells to become involved in the anthracycline-induced formation of toxic radicals. Dexrazoxane thus also has a cardioprotective effect.
Medical application and use for treatment and prevention.
The active ingredient is marketed as a white to grayish-white powder, from which an infusion solution is prepared shortly before application. Accordingly, the common route of administration is intravenous, which is typical for a cytostatic drug. Usually, dexrazoxane is administered together with anthracyclines. In this context, the lowest cumulative dose administered in medical practice is 300 mg per square meter of doxorubicin or 540 mg per square meter of epirubicin.
Risks and side effects
Because dexrazoxane is a highly potent cytostatic drug, serious side effects are possible. It should be taken only under the supervision of healthcare professionals. For this reason, the substance is not freely available. In addition, attention must be paid to interactions with other drugs. The substance must not be taken at all if an allergy or intolerance is known or if there is a contraindication. Such a contraindication exists if concrete facts make the application appear unreasonable from a medical point of view, i.e. a contraindication is known. This is particularly the case during breastfeeding and pregnancy. Dexrazoxane is also contraindicated in children and adolescents under 18 years of age, as they are at greatly increased risk of neoplasia, infection, and bone marrow depression. Major adverse reactions that may occur during or shortly after treatment with dexrazoxane include fever, severe fatigue, a general feeling of weakness, and
Gastrointestinal tract (GI) disorders. These are mainly characterized by nausea, vomiting, diarrhea (diarrhea), constipation (constipation) and loss of appetite.Other side effects include anemia, neutropenia, leukopenia, cardiac arrhythmias, thrombocytopenia, asthenia, and dizziness. In addition, cough, headache, pharyngitis, and skin reactions may also occur. The latter are often manifested by itching, red patches, rash, or a burning sensation.
