Penetration of ofloxacin into human lung tissue following a single oral dose of 200 milligrams

Serour, Francis; Dan, Michael; Gorea, Alfred; Yellin, Alon; Lieberman, Y; Berger, Stephen A.

doi:10.1128/aac.35.2.380

Antimicrob Agents Chemother

1991

DOI: 10.1128/aac.35.2.380

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Penetration of ofloxacin into human lung tissue following a single oral dose of 200 milligrams

Francis Serour

Michael Dan

Alfred Gorea

et al.

Abstract: The penetration of ofloxacin into lung tissue was studied in 10 patients subjected to pulmonary surgery. Samples of blood and lung tissue were obtained 3 to 8 h (mean, 5 h) after oral administration of 200 mg. The mean level in tissue was 2.17 +/- 0.5 micrograms/g, while the mean level in serum was 0.85 +/- 0.23 micrograms/ml. The mean lung tissue/serum concentration ratio was 2.55 +/- 0.30. The achievable levels of ofloxacin in lung tissue are above the MICs for most pulmonary pathogens.

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Cited by 6 publications

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“…Metabolite concentrations in all tissues assayed (lung, bronchial mucosa, and pleural tissue) are low compared to ciprofloxacin concentrations (20). The fluoroquinolone ofloxacin also penetrates well into human lung tissue (22), as do enoxacin (25) and lomefloxacin (2). This means that, unlike aminoglycosides and ␤-lactams, which are excluded from intracellular infection sites, fluoroquinolones are efficient in the treatment of respiratory infections (17), which can be caused by both intracellular and extracellular pathogens (18).…”

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confidence: 99%

Transepithelial transport of the fluoroquinolone ciprofloxacin by human airway epithelial Calu-3 cells

Cavet

West

Simmons

1997

Antimicrob Agents Chemother

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Although fluoroquinolone antibiotics such as ciprofloxacin are able to gain access to lung tissue and both pleural and bronchial secretions, the characteristics of transport and cellular uptake of ciprofloxacin in human epithelial lung tissue remain obscure. We have chosen human airway epithelial (Calu-3) cells, reconstituted as functional epithelial layers grown on permeable filter supports, as a model with which to assess both transepithelial transport and cellular uptake of ciprofloxacin. Transepithelial ciprofloxacin fluxes in absorptive (apical-to-basal) and secretory (basal-to-apical) directions were similar throughout the concentration range studied (1.0 microM to 3.0 mM). Transepithelial mannitol fluxes measured concurrently were substantially smaller than ciprofloxacin fluxes in Calu-3 epithelia, suggesting the existence of a mediated transcellular route in addition to a paracellular route for transepithelial permeation. Apical-to-basal ciprofloxacin flux (at 10 microM) was inhibited by a 100-fold excess of unlabelled norfloxacin, enoxacin, and ofloxacin, while secretory flux was unaffected. Cellular uptake of ciprofloxacin, determined as a cell/medium ratio, was greater from the basal compartment (2.7-fold) than apical uptake (1.39-fold) measured at 100 microM ciprofloxacin and showed no saturation up to 3 mM ciprofloxacin. Comparison of the permeation of ciprofloxacin was made with that of lipophilic substrates such as vinblastine and digoxin. There was a linear correlation between transepithelial permeability (Pa-b) and their oil/water partition coefficients with mannitol < ciprofloxacin < digoxin < vinblastine. Comparison of transport of ciprofloxacin across human airway Calu-3 epithelia with that across intestinal Caco-2 epithelia emphasizes the absence of a specific secretory pathway; ciprofloxacin permeation in Calu-3 epithelia appears to be mediated primarily by a transcellular route, with mediated transfer at apical and basal membranes occurring via transporters with low affinity to ciprofloxacin.

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mentioning

confidence: 99%

Transepithelial transport of the fluoroquinolone ciprofloxacin by human airway epithelial Calu-3 cells

Cavet

West

Simmons

1997

Antimicrob Agents Chemother

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The penetration of ciprofloxacin into bronchial mucosa, lung parenchyma, and pleural tissue after intravenous administration

Dan

Torossian

Weissberg

et al. 1993

Eur J Clin Pharmacol

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We have studied the concentrations of ciprofloxacin in serum, bronchial mucosa, lung parenchyma, and pleural tissue after a single intravenous dose of 200 mg in 20 patients subjected to lung surgery. The concentrations of ciprofloxacin in the tissues exceeded that in the serum by 3-fold to 7-fold: serum 0.6 micrograms.ml-1, bronchial mucosa 1.9 micrograms.g-1, lung parenchyma 3.4 micrograms.g-, and pleural tissue 1.7 micrograms.g-1. The achievable concentrations of ciprofloxacin in the tissues of the lower respiratory tract are above the MICs for most lung pathogens.

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Quinolones in the treatment of lower respiratory tract infections caused by intracellular pathogens

Chidiac

Mouton

1991

Infection

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Intracellular pathogens are inhibited to varying degrees, depending upon the strain of the organism and the quinolone tested. Quinolones achieve levels in the lower respiratory tract that equal or exceed serum concentrations, and they also achieve good intracellular concentrations. Experimental models of intracellular infection have demonstrated the efficacy of ciprofloxacin, difloxacin, fleroxacin, ofloxacin and pefloxacin. Animal models of experimental legionellosis have confirmed in vivo their efficacy in this field. Thus, quinolones appear to be a safe and efficacious alternative treatment in lower respiratory tract infection (LRTI) due to intracellular pathogens. Considering the in vitro and experimental studies, quinolones should play an important role in the treatment of LRTI caused by intracellular pathogens, and prospective controlled studies are strongly recommended.

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Penetration of ofloxacin into human lung tissue following a single oral dose of 200 milligrams

Cited by 6 publications

References 6 publications

Transepithelial transport of the fluoroquinolone ciprofloxacin by human airway epithelial Calu-3 cells

Transepithelial transport of the fluoroquinolone ciprofloxacin by human airway epithelial Calu-3 cells

The penetration of ciprofloxacin into bronchial mucosa, lung parenchyma, and pleural tissue after intravenous administration

Quinolones in the treatment of lower respiratory tract infections caused by intracellular pathogens

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