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Eur J Drug Metab Pharmacokinet. 1997 Jul-Sep;22(3):237-43.
Assessment of antibiotic levels in lung tissue with erosion-controlled dosage forms.

Saidna M, Ouriemchi EM, Vergnaud JM.

Laboratory of Materials and Chemical Engineering, Faculty of Sciences, University of St-Etienne, France.

The concentration-time curve of ciprofloxacin has been assessed in the blood compartment and in the lung tissue following oral administration of the drug. Immediate release and erosion-controlled dosage forms have been examined. A numerical model based on finite differences and taking into account all relevant data has been built: the kinetics of drug release in the gastrointestinal tract, drug absorption in the blood compartment and elimination, and the transient diffusion of the drug through the lung tissue. A partition coefficient for the drug at the tissue-blood interface has been considered to express the drug concentration at the tissue surface. The effect of dose frequency and erosion rate on the antibiotic versus time curves in the plasma and the lung tissue has been studied in detail.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9358205&dopt=Abstract

PRIUS.JNJ.com

Levofloxacin, the active L-isomer of ofloxacin, has demonstrated strong activity against Staphylococcus aureus both in vitro and in vivo. In a murine model of hematogenous pyelonephritis, the in vivo efficacies of levofloxacin and ciprofloxacin were evaluated against two methicillin-susceptible and two methicillin-resistant S. aureus strains. All four isolates had virtually identical susceptibilities to levofloxacin and ciprofloxacin. Pyelonephritis was induced in carrageenan-primed mice by an intravenous injection of 0.5 ml of 10(7) CFU of methicillin-susceptible S. aureus isolates per ml or 10(8) CFU of methicillin-resistant S. aureus isolates per ml. At 1 h postinfection, the mice were treated orally with levofloxacin or ciprofloxacin once a day or twice a day (total daily dose of 20 to 160 mg/kg of body weight) for 4 days. Mice were euthanized 24 h after the final treatment, and the kidneys were excised and weighed. The kidneys were prepared for histological examination or were homogenized to determine the numbers of CFU per gram of tissue quantitatively. The reduction in the mean log10 number of CFU per gram as a function of total daily dose was recorded. A dose-response analysis showed that levofloxacin was superior to ciprofloxacin for all four isolates at any dose or regimen tested, independent of the methicillin susceptibility of the isolates. By using an inverse prediction technique, the equivalent effective doses of levofloxacin (once a day) were less than those of ciprofloxacin (twice a day) by 5.2 and 3.2 times, respectively, for methicillin-susceptible S. aureus 9039 and 3087. For methicillin-resistant S. aureus 667 and 2878, the equivalent effective doses of levofloxacin (once a day) were less than those of ciprofloxacin (twice a day) by 4.1 and 6.4 times, respectively. In a separate study, histological examination of all infected, untreated mice showed moderate to marked hematogenous pyelonephritis. Levofloxacin-treated mice (40 mg/kg once a day) showed no evidence of pyelonephritis in the kidneys, whereas the kidneys of mice treated with the same dose of ciprofloxacin showed only a reduction in the severity of the lesions. Treatment with ciprofloxacin (80 mg/kg twice a day) demonstrated a histology comparable to that of treatment with levofloxacin (40 mg/kg once a day). Levofloxacin (40 mg/kg once a day) reduced the log10 numbers of CFU per gram by 5 log10; however, ciprofloxacin (80 mg/kg twice a day) reduced the numbers of CFU per gram by only 3 log10. In the present murine model of pyelonephritis, levofloxacin was superior to ciprofloxacin in preventing pyelonephritis and eradicating S. aureus.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8913458&dopt=Abstract




J Clin Microbiol. 1995 Jan;33(1):215-6.
Susceptibility to levofloxacin predicted from in vitro susceptibility testing results obtained with ciprofloxacin and with ofloxacin.

Cormican MG, Jones RN.

Department of Pathology, University of Iowa College of Medicine, Iowa City 52242.

A test battery of bacterial strains with a high incidence of resistance to fluoroquinolones was studied to determine the extent to which susceptibility to levofloxacin could be predicted from susceptibility tests performed with ciprofloxacin or ofloxacin as reagents. Isolates susceptible or intermediately susceptible to ofloxacin (MICs < or = 4 micrograms/ml) may be regarded as susceptible to levofloxacin, with the exception of Enterococcus faecium. Ciprofloxacin-susceptible isolates (MICs < or = 1 micrograms/ml) were also completely susceptible to levofloxacin. Clinical laboratories could use either of the currently used fluoroquinolones (ciprofloxacin or ofloxacin) to predict levofloxacin activity and spectrum with little risk of false-susceptible errors (0.0 to 1.3%). Results obtained with ofloxacin are superior in maximizing recognition of levofloxacin-susceptible clinical isolates.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7699045&dopt=Abstract













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