Human aqueous humor levels of oral ciprofloxacin, levofloxacin, and moxifloxacin

J Cataract Refract Surg. 2001 Dec;27(12):1969-74. doi: 10.1016/s0886-3350(01)00997-x.


Purpose: To evaluate the penetration of ciprofloxacin, levofloxacin, and moxifloxacin into the aqueous humor after oral administration.

Setting: Alcorcon Hospital, Madrid, Spain.

Methods: Forty-two patients having cataract surgery were randomly divided into 3 groups the day before surgery. The first group received 2 oral 500 mg doses of ciprofloxacin at 12-hour intervals. The second group received a single oral 500 mg dose of levofloxacin. The third group received a single oral 400 mg dose of moxifloxacin. At the time of surgery, 0.1 mL aqueous fluid was aspirated from the anterior chamber just before the operation and immediately stored at -80 degrees C. Drug concentrations were measured using a biological assay.

Results: The mean aqueous level of ciprofloxacin was 0.50 microg/mL +/- 0.25 (SD); of levofloxacin, 1.50 +/- 0.50 microg/mL; and of moxifloxacin, 2.33 +/- 0.85 microg/mL. The mean aqueous levels of levofloxacin and moxifloxacin were above the 90% minimum inhibitory concentration for most of the common microorganisms that cause endophthalmitis.

Conclusions: Therapeutic concentrations of fluoroquinolones, mainly levofloxacin and moxifloxacin, were reached with oral administration. These antibiotics may be effective for prophylaxis and adjuvant therapy of bacterial endophthalmitis.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Aged
  • Aged, 80 and over
  • Anti-Infective Agents / pharmacokinetics*
  • Aqueous Humor / metabolism*
  • Aza Compounds*
  • Biological Availability
  • Cataract Extraction
  • Ciprofloxacin / pharmacokinetics
  • Female
  • Fluoroquinolones*
  • Humans
  • Levofloxacin
  • Male
  • Microbial Sensitivity Tests
  • Middle Aged
  • Moxifloxacin
  • Ofloxacin / pharmacokinetics
  • Prospective Studies
  • Quinolines*
  • Tissue Distribution


  • Anti-Infective Agents
  • Aza Compounds
  • Fluoroquinolones
  • Quinolines
  • Ciprofloxacin
  • Levofloxacin
  • Ofloxacin
  • Moxifloxacin