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Endothelial cell compatibility of fluoroquinolone solutions for intravenous use

H Vorbach1, G Weigel, B Robibaro

  • 1Department of Infectious Diseases, University Hospital of Vienna, Austria.

International Journal of Clinical Pharmacology and Therapeutics
|June 1, 1997
PubMed

Insights

Parenteral fluoroquinolones like ciprofloxacin and fleroxacin severely damage endothelial cells, increasing phlebitis risk. Ofloxacin showed no adverse effects on these cells, suggesting it may be a safer alternative.

Area of Science:

  • Vascular Biology
  • Pharmacology
  • Cell Biology

Background:

  • Phlebitis is a common side effect of parenteral fluoroquinolones.
  • Endothelial cell damage and inflammation are believed to cause phlebitis.

Purpose of the Study:

  • To assess the impact of ciprofloxacin, fleroxacin, and ofloxacin on human umbilical venous endothelial cell (HUVEC) viability.
  • To evaluate the potential of HUVECs as an in vitro model for assessing intravenous antibiotic tolerability.

Main Methods:

  • Intracellular ATP levels in HUVECs were measured using a luciferin-luciferase assay to determine cell viability.
  • Prostacyclin (PGI2) and thromboxane A2 (TXA2) levels were quantified via direct radioimmunoassay.
  • HUVECs were incubated with varying concentrations of ciprofloxacin, fleroxacin, and ofloxacin.

Main Results:

  • Ciprofloxacin (2 mg/ml) and fleroxacin (4 mg/ml) significantly reduced intracellular ATP levels by over 75% within 20 minutes, indicating severe endothelial cell damage.
  • Ofloxacin (2 mg/ml) did not cause significant detrimental effects on HUVEC viability.
  • At concentrations up to 20 µg/ml, all tested fluoroquinolones were well-tolerated. Higher concentrations (100-200 µg/ml) led to functional alterations, including increased PGI2 release.

Conclusions:

  • Ciprofloxacin and fleroxacin exhibit significant cytotoxicity to HUVECs, potentially explaining their association with phlebitis.
  • Ofloxacin demonstrates better tolerability in HUVECs compared to ciprofloxacin and fleroxacin.
  • Human venous endothelial cells provide a valuable in vitro model for evaluating the tolerability of intravenously administered antibiotics.

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