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Characterization of histamine release induced by fluoroquinolone antibacterial agents in-vivo and in-vitro

K Mori1, C Maru, K Takasuna

  • 1Drug Safety Research Laboratory, Daiichi Pharmaceutical Co. Ltd, Tokyo, Japan.

The Journal of Pharmacy and Pharmacology
|June 23, 2000
PubMed

Insights

Fluoroquinolone antibacterials, levofloxacin and ciprofloxacin, trigger histamine release in dogs but not rats. Canine mast cells show higher sensitivity to these drugs compared to rat mast cells.

Area of Science:

  • Pharmacology
  • Immunology
  • Toxicology

Background:

  • Fluoroquinolone antibacterial agents are widely used.
  • Histamine release is a potential adverse effect of certain drugs.
  • Species-specific differences in drug responses are common.

Purpose of the Study:

  • To investigate histamine release induced by levofloxacin and ciprofloxacin.
  • To compare the effects of these fluoroquinolones in vivo and in vitro.
  • To examine species-specific sensitivity of mast cells to fluoroquinolones.

Main Methods:

  • In vivo studies using anesthetized dogs and rats.
  • In vitro studies using mast cells from canine and rat skin and peritoneum.
  • Measurement of plasma histamine levels.
  • Assessment of non-cytotoxic histamine secretion.

Main Results:

  • Levofloxacin and ciprofloxacin induced dose-related histamine release in dogs.
  • Ciprofloxacin, but not levofloxacin, caused histamine release in rats.
  • Canine mast cells were significantly more sensitive to fluoroquinolones than rat mast cells.

Conclusions:

  • Fluoroquinolones can induce histamine release, with species-dependent variations.
  • Canine mast cells exhibit higher sensitivity to fluoroquinolones compared to rat mast cells.
  • Functional heterogeneity of mast cells contributes to differential drug responses.

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