Dexrazoxane

Dexrazoxane is a drug that is 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 effects of dexrazoxane. Due to its pharmacological properties as well as the specific area of ​​application, dexrazoxane belongs to the class of cytostatics.

What is dexrazoxane?

Dexrazoxane is an active ingredient that is used in human medicine. There is an indication for chemotherapy, which is why dexrazoxane is an important cytostatic agent. The fabric is also called Eucardion and sold under the trade name Cardioxane®. In chemistry and pharmacology, dexrazoxane is described by the empirical formula C 11 - H 16 - N 4 - O 4, which corresponds to a moral mass of approx. 268.27 g / mol.

Dexrazoxane was discovered in 1964 together with several other substances and has been used in human medicine as a cytostatic agent since the 1990s. Before that, dexrazoxane was used as a colorant in the textile industry. Today there are approvals in several countries. Dexrazoxane is subject to comprehensive pharmacy and prescription requirements in every country for which it is approved for human therapy.

Pharmacological effect on the body and organs

Dexrazoxane is a white to off-white powder at room temperature and has a very high bioavailability of almost 100% after ingestion. In human blood, less than two percent of the drug is bound to the plasma proteins. The metabolism (metabolism) of dexrazoxane takes place via the liver and thus hepatically. In the literature, the plasma half-life of the cytostatic is set at around two to two and a half hours, depending on the individual case. 42% of the elimination takes place via the kidneys and thus renally.

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 and thereby enables the replication of genetic information. In addition, topoisomerase II α also enables cell division. Since dexrazoxane renders topoisomerase IIα inoperative, it becomes impossible for cells to divide.

In addition, dexrazoxane also has cytoprotective effects. These are based on the ability of the cytostatic to trap iron ions in the cells of the heart. This makes it impossible for the heart cells to integrate into the anthracycline-induced formation of toxic radicals. Dexrazoxane thus also has a cardioprotective effect.

Medical application & use for treatment & prevention

The active ingredient is sold as a white to off-white powder, from which an infusion solution is made shortly before application. The usual form of application is accordingly intravenous, which is typical for a cytostatic.

Usually, dexrazoxane is given together with anthracyclines. The lowest cumulative dose that is administered in medical practice is 300 mg per square meter of doxorubicin or 540 mg per square meter of epirubicin.

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Risks & side effects

Since dexrazoxane is a highly effective cytostatic agent, serious side effects are possible. It may only be taken under the supervision of a healthcare professional. For this reason, the substance is not freely available. In addition, you should also watch out for interactions with other drugs.

Do not take it at all if you have an allergy or intolerance or if there is a contraindication. Such is the case if concrete facts make the application appear unreasonable from a medical point of view, i.e. a counter-notification 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 a greatly increased risk of neoplasia, infections and bone marrow depression.

The most important undesirable side effects that may occur during or shortly after treatment with dexrazoxane include fever, severe tiredness, a general feeling of weakness and Disorders of the gastrointestinal tract (gastrointestinal tract). 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, coughs, headaches, pharyngitis, and skin reactions can also occur. The latter often manifest as itching, red spots, rashes or a burning sensation.