Effect of levofloxacin and ciprofloxacin injection on permeability of the tail vein in mice and skin microvasculature in rats.
We examined the effects of levofloxacin (LVFX) and ciprofloxacin (CPFX) on the permeability of the tail vein in mice and skin microvasculature in rats after a single intravenous and intracutaneous injection, respectively, with 125I-human serum albumin. In addition, the effect of an H1 histamine antagonist, diphenhydramine, on the hyperpermeability induced by quinolone injections was examined, and the injections were also performed into the tail vein of WBB6F1 (mast cell-deficient) mice. LVFX and CPFX significantly increased the permeability of the mouse tail vein at injection concentrations of 0.2% and 0.05% of more, respectively, and both quinolones increased the permeability of rat skin microvasculature by 0.5% or more. Diphenhydramine concomitantly injected with quinolones completely blocked the hyperpermeability induced by LVFX and CPFX at 0.5% in the mouse tail vein and rat skin microvasculature. Neither quinolone increased the tail vein permeability in WBB6F1 mice. These results suggest that LVFX and CPFX increase vascular permeability through the induction of histamine release from mast cells in rodents.
Drug Safety Research Centre, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
M
M
Yoshida
S
S
Takayama
M
M
Kato
D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology*; D002199:Capillary Permeability / Q000187:drug effects*; D002939:Ciprofloxacin / Q000494:pharmacology*; D004155:Diphenhydramine / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D007275:Injections, Intravenous; D064704:Levofloxacin; D008297:Male; D008407:Mast Cells / Q000187:drug effects; D051379:Mice; D008807:Mice, Inbred BALB C; D008833:Microcirculation / Q000187:drug effects; D015242:Ofloxacin / Q000494:pharmacology*; D009994:Osmolar Concentration; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000098:blood supply; D013623:Tail / Q000098:blood supply; D014680:Veins / Q000187:drug effects*
D000890:Anti-Infective Agents; D002939:Ciprofloxacin; D064704:Levofloxacin; D004155:Diphenhydramine; D015242:Ofloxacin