Penetration of moxifloxacin into the human aqueous humour after oral administration

Abstract

Aims: To determine the pharmacokinetics of moxifloxacin, a new generation fluoroquinolone, in the anterior chamber of the human uninflamed eye. Methods: 35 patients undergoing cataract surgery received two doses of 400 mg of oral moxifloxacin with a 12 hour interval and were divided into six groups. Moxifloxacin levels in aqueous humour and serum were determined by a microbiological agar well diffusion technique at 2, 4, 6, 8, 10, and 12 hours after the second dose in each group respectively. Results: Mean moxifloxacin levels in the anterior chamber were 1.20 (SD 0.35) mg/ml at the 2 hours group, 1.22 (0.48) mg/ml at the 4 hours group, 1.20 (0.45) mg/ml at the 6 hours group, 1.58 (0.38) mg/ ml at the 8 hours group, 1.37 (0.44) mg/ml at the 10 hours group, and 1.23 (0.55) mg/ml at the 12 hours group. The mean ratio of aqueous to serum moxifloxacin level was 38%. Conclusion: Moxifloxacin penetrates well into the anterior chamber of the human uninflamed eye after oral administration, reaching early significant levels, which are maintained for at least 12 hours and are much higher than the MIC 90 values of Gram positive and Gram negative pathogens commonly implicated in intraocular infections with the exceptions of fluoroquinolone resistant staphylococci, MRSA, and Pseudomonas aeruginosa. Bacterial endophthalmitis is one of the most serious complications following intraocular operations and penetrating ocular trauma. In the first setting the commonest micro-organisms involved are either Gram positive (Staphylococcus epidermidis, Staphylococcus aureus, streptococci, Propionibacterium acnes) or Gram negative (Pseudomonas aeruginosa, Haemophilus influenza, and Serratia marcescens) while in post-traumatic endophthalmitis there is significant involvement of Bacillus cereus and Staphylococcus aureus.

Pharmacokinetics of intravenously administered moxifloxacin in eye compartments: an experimental study

“…The achieved concentrations after topical application in eye compartments were considerably lower than those reported in the present study in rabbits [21,22]. In another study [1], patients undergoing cataract surgery received two oral doses of 400 mg moxifloxacin with a 12-h interval between them. Mean concentrations in aqueous humour 2-6 h after the last dose were 1.2 g/mL, i.e.…”

“…The fluoroquinolones have commonly been used for prophylaxis during the perioperative period, typically through the topical route of administration. Among them, moxifloxacin applied as a topical solution can safely penetrate the cornea and achieve concentrations in the aqueous humour that are greater than those of other fluoroquinolones [1][2][3]. Based on these properties, several animal studies have been performed in rabbits showing a favourable efficacy of moxifloxacin applied as a topical solution for the prevention and treatment of staphylococcal keratitis and endophthalmitis [4,5].…”

“…The leading causative organisms are Gram-positive pathogens, mainly Staphylococcus epidermidis and Staphylococcus aureus [1]. The fluoroquinolones have commonly been used for prophylaxis during the perioperative period, typically through the topical route of administration.…”

Stenotrophomonas maltophilia Induced Post-Cataract-Surgery Endophthalmitis: Outbreak Investigation and Clinical Courses of 26 Patients

“…A role for oral, topical or intracameral moxifloxacin and oral levofloxacin has also been proposed [30][31][32]. Given the potentially devastating implications of single or serial cases of post-surgery endophthalmitis [33], the role of perioperative antibiotic prophylaxis might gain in importance.…”

Ocular Penetration of Intravenously Administered Colistin in Rabbit Uveitis Model

“…The leading causative organisms are Gram-positive pathogens. 1 Gram-negative bacteria are a less common cause of acute-onset endophthalmitis following cataract surgery 2 and have been isolated in 26% to 42% of patients with cataract surgery related to endophthalmitis in developing countries 2-4 as compared with 5.9% to 12.2% in developed countries. [5][6][7][8][9] The common Gram-negative organisms causing endophthalmitis include species of Pseudomonas, Haemophilus, Klebsiella, and Proteus.…”