Pharmacokinetics and ocular penetration of grepafloxacin in albino and pigmented rabbits

Pérez, Salud; Solans, C.; Bregante, M. A.; Pinilla, Isabel; García, María Ángeles; Fm, Honrubia

doi:10.1093/jac/dkf178

Cited by 9 publications

(8 citation statements)

References 28 publications

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“…The difference in the strain (respectively, Dutch belted versus New Zealand) and weight (respectively, 2.2 to 2.5 kg versus 3.0 to 4.0 kg) of the rabbits used could partially explain the difference observed, because the vitreous volume of the tested rabbits could vary significantly. Ocular pigmentation could also play a role, since the affinity of daptomycin to melatonin could affect the intraocular pharmacokinetics of this antibiotic, as it has already been implicated in some studies comparing intraocular penetration of systemic antibiotics in albino and pigmented rabbits (15,19). The difference in the tested bacterial species (S. aureus versus S. epidermidis) could modify the bacterial toxin profiling and could explain the differences in strain virulence and histopathologic analysis.…”

Section: Discussionmentioning

confidence: 99%

Daptomycin versus Vancomycin in a Methicillin-Resistant Staphylococcus aureus Endophthalmitis Rabbit Model: Bactericidal Effect, Safety, and Ocular Pharmacokinetics

Lefèvre

Saleh

Marcellin

et al. 2012

Antimicrob Agents Chemother

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Staphylococcus aureus is a frequent cause of acute endophthalmitis, and infection with this virulent bacterium is often associated with a poor visual outcome. In this study, we investigated the bactericidal efficacy and the safety of intravitreal daptomycin (DAP), a lipopeptide antibiotic with broad-spectrum activity against Gram-positive bacteria, compared with those of intravitreal vancomycin (VAN) in a methicillin-resistant S. aureus endophthalmitis rabbit model. The pharmacokinetics and pharmacodynamics of daptomycin in the infected eyes were also studied. Rabbits were randomly divided into three treatment groups (n ‫؍‬ 8) and one untreated group (n ‫؍‬ 4), to compare the effect of single intravitreal injections of 0.2 mg and 1 mg of daptomycin (DAP 0.2 and DAP 1 groups, respectively) with that of 1 mg of intravitreal vancomycin (VAN 1 group). Vitreal aspirates were regularly collected and grading of ocular inflammation was regularly performed until euthanasia on day 7. In the DAP 0.2 group, 62.5% of the eyes were sterilized and the mean bacterial count presented a reduction of 1 log unit. In the DAP 1 and VAN 1 groups, the infection was eradicated (100% and 87.5% of eyes sterilized, respectively), with a 4-log-unit reduction of the mean bacterial count. The bactericidal efficacy in the DAP 1 group was not inferior to that in the VAN 1 group and was superior to that of the other regimens in limiting the ocular inflammation and preserving the architecture of the ocular structures (P < 0.05). The elimination half-life (t 1/2␤ ) of daptomycin was independent of the administered dose (38.8 ؎ 16.5 h and 40.9 ؎ 6.7 h, respectively, for the DAP 0.2 and DAP 1 groups) and was significantly longer than the t 1/2␤ of vancomycin (20.5 ؎ 2.0 h for the VAN 1 group) (P < 0.05). This antibiotic could therefore be considered for the treatment of intraocular infections caused by Gram-positive bacteria.

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Section: Discussionmentioning

confidence: 99%

Daptomycin versus Vancomycin in a Methicillin-Resistant Staphylococcus aureus Endophthalmitis Rabbit Model: Bactericidal Effect, Safety, and Ocular Pharmacokinetics

Lefèvre

Saleh

Marcellin

et al. 2012

Antimicrob Agents Chemother

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“…Fluoroquinolones are a group of synthetic antibiotics chemically related to nalidixic acid. These compounds have been developed for the treatment of a variety of microbial infections in both animal and human medicine (Abadia et al, 1995;Garcia et al, 1999a;McKellar et al, 1999;Bregante et al, 1999;Perez et al, 2002). These agents work by inhibiting the action of DNA gyrase, interfering with the supercoiling of antibacterial chromosomal material (Cornett and Wentland, 1985).…”

Section: Introductionmentioning

confidence: 99%

Determination of enro?oxacin and its primary metabolite, cipro?oxacin, in pig tissues. Application to residue studies

García

Solans

Calvo

et al. 2005

Biomed. Chromatogr.

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A simple and sensitive HPLC method has been developed for the simultaneous determination of enrofloxacin (ENR) and ciprofloxacin (CIP) in pig tissue using difloxacin (DIF) as internal standard. Tissue sample preparations were carried out by adding phosphate buffer (pH 7.4, 0.1 m), followed by extraction with trichloromethane. Fluoroquinolones were separated on a reversed-phase column and eluted with aqueous buffer solution-acetonitrile (80:20, v/v). The concentrations of CIP, ENR and DIF eluted from the column, with retention times of 2.20, 2.73 and 4.38 min, respectively, were monitored by fluorescence detection at lambda(ex) 276 and lambda(em) 442 nm. The detection and quantitation limit were 8 and 25 ng/g, respectively, for both compounds. Standard curves were linearly related to concentration in the range 25-400 ng/g. The consequences of the introduction of minor reasonable variations (ruggedness studies) have also been analysed. Finally, the measurement of the tissue levels of ENR and CIP in the pig tissues after oral administration confirmed the utility of the proposed method.

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“…In common with systemic grepafl oxacin administration, we have found that intravitreal grepafl oxacin administration is associated with the highest concentrations being found in the chorioretina and iris of pigmented rabbits [8,35] . However, our results on the grepafl oxacin concentrations in the sclera have to be viewed with some caution, because this tissue is very diffi cult to separate from the chorioretina.…”

Section: Discussionmentioning

confidence: 84%

“…This antimicrobial agent can be considered a member of the third-generation fl uoroquinolone family and can be studied as a model of penetration and activity for this group of antimicrobial agents [8] . In an earlier paper [8] , we studied the pharmacokinetics and ocular penetration of grepafl oxacin in albino and pigmented rabbits following intravenous administration of grepafl oxacin, with good penetration into several ocular tissues.…”

mentioning

confidence: 99%

Ocular Penetration of Grepafloxacin after Intravitreal Administration in Albino and Pigmented Rabbits

Solans¹,

Bregante²,

García

et al. 2004

Chemotherapy

Self Cite

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Ocular penetration of grepafloxacin into several ocular tissues was determined in albino and pigmented rabbits following a single intravitreal administration. After administration, grepafloxacin was detected in all ocular tissues studied in both breeds of rabbits. The superior mean penetration ratios were found in the chorioretina and lens of albino rabbits, and in the chorioretina, iris and lens of pigmented rabbits. A significantly greater penetration of grepafloxacin was found in the chorioretina and iris of the pigmented rabbits than in those of the albino rabbits. As a final conclusion, grepafloxacin detected in different ocular structures could attain therapeutic concentrations against a variety of ocular conditions.

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Pharmacokinetics and ocular penetration of grepafloxacin in albino and pigmented rabbits

Cited by 9 publications

References 28 publications

Daptomycin versus Vancomycin in a Methicillin-Resistant Staphylococcus aureus Endophthalmitis Rabbit Model: Bactericidal Effect, Safety, and Ocular Pharmacokinetics

Daptomycin versus Vancomycin in a Methicillin-Resistant Staphylococcus aureus Endophthalmitis Rabbit Model: Bactericidal Effect, Safety, and Ocular Pharmacokinetics

Determination of enro?oxacin and its primary metabolite, cipro?oxacin, in pig tissues. Application to residue studies

Ocular Penetration of Grepafloxacin after Intravitreal Administration in Albino and Pigmented Rabbits

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