Cytostatically effective antibiotics

The cytostatically effective antibiotics are active ingredients produced either by Actinomyces species (Anthracyclines: Doxorubicin, Daunorubicin) or Streptomyces species(Bleomycin). Their antibiotic use was prohibited because of their considerable toxicity. They develop their cytostatic effect by intercalation into the DNA.

Anthracyclines (intercalants)

• Daunorubicin (ALL, AML, Kaposi's sarcoma)
• Doxorubicin (bronchial, ovarian, breast cancer, lymphomas, soft tissue sarcomas)
• Epirubicin (sarcoma, breast carcinoma, stomach carcinoma, non-Hodgkin's lymphoma)

Glycopeptic antibiotic

• Bleomycin (testicular tumors, Hodgkin's disease, NHL)

Doxorubicin is the hydroxy derivative of daunorubicin and belongs to the group of anthracyclines. Epirubicin is almost identical to doxorubicin, but is less cardiotoxic in comparison to the latter.

The anthracyclines have a tetracyclic basic structure and move between two DNA base pairs, preferably between guanine and cytosine(intercalation). This leads to an inhibition of DNA and RNA synthesis. In addition, the inhibition of topoisomerase II leads to strand breaks. The glycoside bleomycin also acts by intercalation and the formation of free radicals, which leads to an interruption of the cell cycle in the G2 phase.

With anthracyclines, myelosuppression (especially daunomycin) and cardiotoxicity (especially doxorubicin) are dose-limiting. In addition, effluvium and even alopecia, gastrointestinal adverse events such as nausea, vomiting and diarrhoea occur. Furthermore, allergic symptoms can be observed. In the case of bleomycin, acute and chronic lung toxicities with pneumonitis and pulmonary fibrosis are in the foreground, while on the skin toxicities with exanthema and hyperpigmentation(flagellant dermatitis).

1. Graefe KH et al. non-selective cytotoxic chemotherapeutics (cytostatics) In: Graefe KH et al (Eds) Pharmacology and Toxicology. Georg Thieme Publisher Stuttgart S 672