The medical agent and drug idarubicin is a common cytostatic drug used to treat acute leukemias. The substance is classified in the anthracycline class because of its chemical properties and is usually administered as a solution for injection.
What is idarubicin?
Idarubicin, often called demethoxidaunorubicin, is a medical agent administered as part of a comprehensive chemotherapy regimen to combat acute leukemias. Idarubicin is taken parenterally through a solution for injection, although the drug is marketed as a capsule, solvent or powder. Idarubicin is thus administered directly into the bloodstream under medical supervision by infusion. This achieves rapid efficacy. In chemistry, idarubicin is described by the molecular formula C 26 – H 27 – N – O 9, which corresponds to a moral mass of about 533.95 g/mol. Thus, idarubicin is similar to its closely related drug daunorubicin (molecular formula: C 27 – H 29 – N – O 10, morale mass: 527.52 g/mol). Compared to the latter, however, idarubicin is more readily fat-soluble due to its lack of a methoxy group, which greatly facilitates its uptake into the cell. Idarubicin achieves its effects by inducing an interaction with topoisomerase II within the targeted cancer cell. Because of its effects, idarubicin is considered a cytostatic. These are cell-toxic substances that are deliberately used in human medicine to kill cancer cells. Unlike some other cytostatic drugs, idarubicin is not used for palliative therapy in some patients (e.g., AML patients) but only for curative treatment.
Pharmacologic Action
Idarubicin represents a cytostatic agent. The active ingredient is toxic on its face. However, in the context of medically supervised chemotherapy, it is administered to patients in a deliberate and controlled manner to kill cancer cells. Idarubicin is able to do this by entering the cell and inhibiting the enzyme topoisomerase II by intercalating into the cell DNA. In medicine, an intercalation is a reversible insertion of molecules in chemical compounds. Because of the activities of idarubicin, the cancer cell is no longer able to produce nucleic acid and protein synthesis. The growth of the cell is inhibited and spread is prevented. The percentage of the active ingredient that is available for metabolism (bioavailability) is between 18 and 39 percent. This is a comparatively good value. Bound idarubicin can be detected on up to 97% of plasma proteins after ingestion. Metabolism occurs via the liver and thus hepar. Elimination, on the other hand, occurs largely via the bile. Only small amounts of the substance are processed renally (via the kidney). In the literature, the plasma half-life of idarubicin ranges from a minimum of 10 to a maximum of 39 hours.
Medical application and use
An indication of idarubicin is primarily for leukemia. This is treated with comprehensive combination chemotherapy. Within this, idarubicin plays a critical role. In older people with AML (amulter myeloid leukemia), no pretreatment is given. In them, however, palliative therapy with idarubicin must not be given. Only curative treatment is indicated here. The drug is usually marketed as a powder, solvent or capsule. A solution for injection is prepared from these, prior to administration to the patient, by healthcare professionals. In certain cases, infusion may also be indicated. In contrast, independent ingestion by the patient is not permitted.
Risks and side effects
Because idarubicin is a very potent drug, undesirable side effects may occur in the course of treatment. These are often reflected in various disturbances of the blood count, which is a typical side effect of cytostatic drugs. In particular, a pathologically reduced level of neutrophil granulocytes (a neutropenia), a greatly reduced number of white blood cells (a leukopenia), and a reduction in hemoglobin (an anemia) can be triggered by treatment with idarubicin. Increased bilirubin levels are also among the known side effects of idarubicin.In addition, patients also report a general feeling of weakness, fever, gastrointestinal complaints and cardiac arrhythmias. Allergic reactions are also possible. These are usually manifested by severe skin reactions such as itching, rash or redness. In this case, treatment should not be continued because there is a contraindication. This is also the case with insufficiencies of the liver or kidneys. There is also a contraindication from a medical point of view during pregnancy and lactation. In addition, treatment with idarubicin must also be refrained from in severe diseases of the heart (e.g., fourth-straight heart failure or after a myocardial infarction).