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Endothelial cell compatibility of trovafloxacin and levofloxacin for intravenous use

C Armbruster1, B Robibaro, A Griesmacher

  • 1Second Medical Department/Pulmologisches Zentrum Vienna, Austria.

The Journal of Antimicrobial Chemotherapy
|April 5, 2000
PubMed

Insights

High doses of parenteral fluoroquinolones like trovafloxacin and levofloxacin can harm endothelial cells by depleting cellular energy. Dilution and administration into large veins are recommended to mitigate these risks.

Area of Science:

  • Pharmacology
  • Cell Biology
  • Microbiology

Background:

  • Fluoroquinolones, including levofloxacin and trovafloxacin, are effective against resistant bacteria.
  • Parenteral administration of fluoroquinolones can cause local side effects like phlebitis.
  • Endothelial cell viability is crucial for vascular health during intravenous drug administration.

Purpose of the Study:

  • To investigate the impact of trovafloxacin and levofloxacin on endothelial cell viability.
  • To quantify the effects of these fluoroquinolones on intracellular energy metabolites (ATP, ADP, GTP, GDP).

Main Methods:

  • High-performance liquid chromatography (HPLC) was used to measure intracellular levels of adenosine triphosphate (ATP), adenosine diphosphate (ADP), guanosine triphosphate (GTP), and guanosine diphosphate (GDP).
  • Endothelial cells were exposed to varying concentrations of trovafloxacin and levofloxacin.
  • Measurements were taken after 60 minutes of exposure.

Main Results:

  • Trovafloxacin (1-2 mg/mL) significantly reduced intracellular ATP levels within 60 minutes.
  • Levofloxacin (2.5-5 mg/mL) also caused a significant decline in ATP levels.
  • Both drugs led to substantial depletion of ADP, GTP, and GDP in endothelial cells.

Conclusions:

  • High-dose infusions of trovafloxacin and levofloxacin compromise endothelial cell function.
  • These findings suggest that parenteral fluoroquinolones are not compatible with direct, undiluted administration.
  • Recommendations include diluting commercial preparations and administering them into larger veins to minimize local toxicity.

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