Products
Grepafloxacin is no longer commercially available because of potential adverse effects. Raxar or Vaxar film-coated tablets were withdrawn from the market in 1999.
Structure and properties
Grepafloxacin (C19H22FN3O3, Mr = 359.4 g/mol) is present in drugs as grepafloxacin hydrochloride.
Effects
Grepafloxacin (ATC J01MA11) has bactericidal properties against Gram-positive and Gram-negative pathogens. The effects are due to inhibition of bacterial topoisomerase II (gyrase) and topoisomerase IV, which play a central role in bacterial proliferation.
Indications
For the treatment of bacterial infectious diseases.
Adverse effects
Grepafloxacin may prolong the QT interval and cause life-threatening cardiac arrhythmias. It has potential for drug-drug interactions because it is metabolized by CYP1A2 and CYP3A4. Therefore, it has been withdrawn from the market.
