Ofloxacin in human aqueous humour and lens

Fisch, A; Lafaix, C; Salvanet, A.; Cherifi, Mouna; Meulemans, A.

doi:10.1093/jac/20.3.453

Cited by 17 publications

(4 citation statements)

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“…In this study the mean concentrations of ofloxacin in the aqueous humour, which peaked 4 h postdose and ranged from 0.96 to 1.87 ~g/ml ( Figure 5), were higher than those observed by Bron (11,14,15,20). Differences in the dosage schedule and route of administration probably accounted for the observed discrepancies.…”

Section: Results Andcontrasting

confidence: 57%

Comparative pharmacokinetics of ciprofloxacin, ofloxacin and pefloxacin in human aqueous humour

Giamarellou

Kanellas

Kavouklis

et al. 1993

Eur. J. Clin. Microbiol. Infect. Dis.

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Eighty-five patients undergoing cataract surgery were given for prophylaxis of intraocular infection two intravenous doses each of 200 mg, 300 mg or 400 mg ciprofloxacin (35 patients), 400 mg or 800 mg pefloxacin (30 patients), or 400 mg ofloxacin (20 patients). Ciprofloxacin levels in aqueous humour ranged from 0.02 to 0.50 microgram/ml, pefloxacin levels from 1.04 to 7.80 micrograms/ml, and ofloxacin levels from 0.44 to 2.27 micrograms/ml with ratios of aqueous humour to serum levels ranging from 3.8% to 25%, 21% to 48.1% and 44% to 88.4%, respectively. It is concluded that the quinolones studied might be suitable for surgical prophylaxis or treatment of anterior chamber infections due to Enterobacteriaceae, while ciprofloxacin at high doses is preferable for Pseudomonas aeruginosa infections.

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Section: Results Andcontrasting

confidence: 57%

Comparative pharmacokinetics of ciprofloxacin, ofloxacin and pefloxacin in human aqueous humour

Giamarellou

Kanellas

Kavouklis

et al. 1993

Eur. J. Clin. Microbiol. Infect. Dis.

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“…The National Eye Institute Endophthalmitis Vitrectomy Study (EVS) is currently evaluating the relative impact of vitrectomy and systemic antibiotics on the outcome of patients receiving intraocular antibiotics. However, recent studies with humans and animals (3,7,12,14,15,18,23,25,29,33,36) suggest that quinolone antimicrobial agents penetrate into the vitreous humor better than the conventional antibiotics that are being used in the EVS study. Since the EVS will not evaluate the role of systemic quinolones, pharmacokinetic and outcome studies with animals may be useful in evaluating the role of systemic quinolones in the treatment of endophthalmitis.…”

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confidence: 99%

Pharmacokinetics of ofloxacin in serum and vitreous humor of albino and pigmented rabbits

Perkins

Liu

Drusano

et al. 1995

Antimicrob Agents Chemother

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The purpose of this study was to evaluate the pharmacokinetics of ofloxacin in serum and vitreous humor samples from albino and pigmented rabbits by using a recently described animal model which permits robust estimation of parameter values. The drug was administered to rabbits intravenously, multiple vitreous humor and serum samples were taken from each rabbit, and the vitreous humor and serum samples were assayed by high-pressure liquid chromatography. The pharmacokinetic parameters were determined with RSTRIP, an iterative, nonlinear, weighted, least-squares regression program. Eight New Zealand White rabbits and eight Dutch Belted rabbits (split into single-dose and multiple-dose groups) were investigated in this study. The value of penetration into the vitreous humor of albino rabbits (n ‫؍‬ 6) was 32.6% ؎ 2.12%, with terminalelimination half-life values of 3.21 and 2.39 h, respectively, for vitreous humor and serum. In pigmented rabbits after a single dose (n ‫؍‬ 3) and with a steady-state concentration of drug in serum (n ‫؍‬ 4), penetration values were similar, at 30.4% ؎ 2.98% and 30.0% ؎ 4.12%, respectively (P > 0.10). Following a single dose of ofloxacin, pigmented animals had elimination half-life values from serum and vitreous humor of 2.64 and 4.32 h, respectively. After steady state was achieved, half-life values for serum and vitreous humor were 3.12 and 6.05 h, respectively. By comparing pigmentation, dose mode, and elimination from vitreous humor, the vitreous humor half-life value for singly dosed albino rabbits (3.21 h) was not more rapid than that for singly dosed pigmented rabbits (4.32 h [P > 0.10]) but was more rapid than that for multiply dosed pigmented rabbits (6.05 h [P < 0.05]). The excellent penetration of ofloxacin into uninflamed rabbit eyes in conjunction with the higher levels in blood found in humans and greater activity against coagulase-negative staphylococci suggest that ofloxacin may be preferable to other quinolones for evaluation in the prophylaxis and treatment of bacterial endophthalmitis.We have recently developed and validated an ocular pharmacokinetic animal model which differs from conventional methods that obtain a single sample of vitreous humor from different animals (20,25,26,29). In our model, serial samples are obtained from the vitreous humor after intravenous drug administration. This model does not alter the pharmacokinetics of drugs in the eye (24,25,29). Serial sampling is preferable, since it permits more-rigorous pharmacokinetic analysis and decreases the number of animals which are needed for the same degree of certainty in the pharmacokinetics parameter estimates by more than 50-fold compared with the single-sample approach (20).Bacterial endophthalmitis is a severe, sight-threatening infection which most commonly occurs after cataract surgery (10, 32). The current therapy of bacterial endophthalmitis includes the intraocular and systemic administration of antibiotics combined with a pars plana vitrectomy (9,10,32,34,35). The National Eye Institute En...

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“…Ofloxacin concentrations in the conjunctiva and aqueous humor were analyzed by a sensitive and selective high performance liquid chromatography (HPLC) method with fluorescein detection (6,13). The assay quantitation limit was 0.2 ng.…”

Section: Methodsmentioning

confidence: 99%

“…Preliminary studies in our laboratory have evaluated the ocular concentrations after topical dosing of 0.3% ofloxacin ointment in rabbits, but not in humans. In addition, ofloxacin 400 mg administered orally demonstrated significant aqueous humor concentrations following one dose in humans (13). The objective of this investigation was to compare the ocular bioavailability of ofloxacin 0.3% ointment with ofloxacin 0.3% solution in human conjunctiva and aqueous humor in patients undergoing cataract surgery.…”

Section: Introductionmentioning

confidence: 99%

Availability of 0.3% Ofloxacin Ointment and Solution in Human Conjunctiva and Aqueous Humor

Tang-Liu

Lambert²,

Blancaflor³

et al. 1995

Journal of Ocular Pharmacology and Therapeutics

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Ofloxacin 0.3% ophthalmic solution or ointment was administered preoperatively to 13 patients undergoing cataract surgery. Mean drug concentrations in conjunctival biopsies were 2.62 and 6.55 micrograms/gm and in aqueous humor samples were 0.36 micrograms/mL and 0.43 micrograms/mL, for ointment and solution respectively. Mean conjunctival concentrations of ofloxacin achieved MIC90 values for 419 gram-positive and gram-negative organisms previously analyzed.

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Ofloxacin in human aqueous humour and lens

Cited by 17 publications

References 0 publications

Comparative pharmacokinetics of ciprofloxacin, ofloxacin and pefloxacin in human aqueous humour

Comparative pharmacokinetics of ciprofloxacin, ofloxacin and pefloxacin in human aqueous humour

Pharmacokinetics of ofloxacin in serum and vitreous humor of albino and pigmented rabbits

Availability of 0.3% Ofloxacin Ointment and Solution in Human Conjunctiva and Aqueous Humor

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