Fludarabine

Products

Fludarabine is commercially available as an injection/infusion preparation (generic, original: Fludara). It was approved in the United States in 1991 and in many countries in 1995.

Structure and properties

Fludarabine (C10H12FN5O4, Mr = 285.2 g/mol) or 9-β-D-arabinosyl-2-fluoroadenine is present in drugs as fludarabine phosphate, a white, crystalline, hygroscopic powder that is sparingly soluble in water. It is a [nucleotide analog>nucleic acid] and a fluorinated derivative of the antiviral drug vidarabine.

Effects

Fludarabine (ATC L01BB05) has cytotoxic properties. It is present in the drug as fludarabine phosphate and is rapidly dephosphorylated in the body. In cells, it is rephosphorylated to the active fludarabine triphosphate. As a false substrate, the active metabolite inhibits DNA and RNA synthesis, among other things, causing cell death. Fludarabine has a half-life of approximately 20 hours.

Indications

Dosage

According to the SmPC. The drug is administered as an intravenous bolus injection or intravenous infusion.

Contraindications

  • Hypersensitivity
  • Renal insufficiency
  • Decompensated hemolytic anemia
  • Pregnancy and lactation

Full precautions can be found in the drug label.

Interactions

Drug-drug interactions have been described with pentostatin (contraindicated), dipyridamole, vaccines, and other inhibitors of adenosine uptake.

Adverse effects

The most common potential adverse effects include:

Overdose can cause severe neurological side effects and is life-threatening.