Cytostatic Therapy: Alkylants

Active ingredients Dosage Special features
Cyclophosphamide 500 mg/m² i. v. Cyclophosphamide is a prodrug (inactive substance), which is cytotoxic only after activation in the liver. To reduce cytotoxicity, MESNA* is administered.
Ifosfamide 3-5 g/m² i. v. as a 4 h/24 h infusion.
Chlorambucil 0.4 mg/kg bw* * p. o., dose increase by 0.1 mg/kg bw to max 0.8 mg/kg or signs of toxicity Maximum 12 months of therapy
Busulfan Continuous therapy 2-4 to 8 mg p. o., per day 0.1 mg/kg bw. Onset of action is delayed after 2-4 weeks when the usual dose is taken
Carmustine 200 mg/m² i.v. every 6 weeks Used mainly in severely advanced tumors because of severe side effects
Procarbazine 100 mg/m² p. o. 10-14 days Procarbazine is a prodrug that is metabolized hepatically (liver) and in erythrocytes (red blood cells)

* MESNA – mercapto-ethanesulfonate sodium * * kg KG – kilogram of body weight.

  • Mode of action: Alkylants have the property of transferring alkyl groups to DNA. If the alkylants are provided with two functional groups, then they can cross-link two DNA strands and are then usually more cytotoxic.
  • Side effects: Leukopenia (lack of white blood cells), thrombopenias (lack of platelets), nausea (nausea), vomiting, sterility, sensitivity disorders, alopecia (hair loss), carcinogenicity (increased risk of secondary/secondary tumors), neurotoxic – depending on the drug.

The effects, indications, side effects and substances listed above represent an overview and do not claim to be complete.