Disease relevance of A 56619

• Evaluation of difloxacin in the treatment of uncomplicated urethral gonorrhea in men [1].
• A-56619 had the lowest MICs against Chlamydia trachomatis (MIC range, 0.125 to 0.25 micrograms/ml) and Haemophilus ducreyi (MIC for 90% of isolates tested, 0.1 micrograms/ml) [2].
• Comparative evaluation of A-56619, A-56620, and nafcillin in the treatment of experimental Staphylococcus aureus osteomyelitis [3].
• This study compared difloxacin administered orally, enoxacin administered orally, and cefazolin administered intramuscularly for the treatment of experimental Staphylococcus aureus endocarditis [4].
• The MICs required to inhibit at least 90% of the strains tested ranged from 0.25 to 4 micrograms/ml for A-56619 and from 0.06 to 0.5 microgram/ml for A-56620 for members of the Enterobacteriaceae [5].

High impact information on A 56619

• In this study, clarithromycin, erythromycin, difloxacin, temafloxacin, ciprofloxacin, rifampin, amikacin, and ethambutol were tested in vitro and in vivo against the M. avium complex [6].
• We compared the efficacies of rifampin, doxycycline, and five 4-quinolone compounds (ciprofloxacin, difloxacin, ofloxacin, norfloxacin, and pefloxacin) in reducing persistent C. burnetii infection of L929 fibroblasts [7].
• The in vitro activity of S-25930 and S-25932, two new 4-quinolones, against 450 aerobic gram-negative organisms isolated from cancer patients was evaluated and compared with the activity of ciprofloxacin, enoxacin, difloxacin (A-56619), and A-56620 [8].
• The in vitro and in vivo properties of a new 1-difluorophenyl-6-fluoroquinolone, temafloxacin hydrochloride (A-62254), were compared with those of difloxacin and ciprofloxacin [9].
• Factors influencing the in vitro activity of two new aryl-fluoroquinolone antimicrobial agents, difloxacin (A-56619) and A-56620 [10].

Chemical compound and disease context of A 56619

• Lomefloxacin, temafloxacin, and difloxacin were the most active drugs tested against Campylobacter spp [11].
• The 4-quinolones ciprofloxacin, difloxacin, enoxacin, norfloxacin, ofloxacin, and nalidixic acid were found to induce the SOS response in qualitative and quantitative tests on Escherichia coli K12 containing the sfiA::lacZ gene fusion [12].
• Ciprofloxacin (MICs 0.06-1 mg/l) was the most active compound against Pseudomonas aeruginosa; A-56619 and CI-934 (MICs 1-16 mg/l) were the least active against this species [13].
• Calves in each group were treated with 10% difloxacin (2.5 or 5 mg/kg of body weight), 5% difloxacin (2.5 or 5 mg/kg), enrofloxacin (5 mg/kg), or saline (0.9% NaCl) solution (control group), once daily for 5 days, and clinical signs were scored daily [14].
• Determination of the inhibitory concentration 50% (IC50) of four selected drugs (chlortetracycline, doxycycline, enrofloxacin and difloxacin) that reduce in vitro the multiplication of Chlamydophila psittaci [15].

Biological context of A 56619

• Difloxacin metabolism and pharmacokinetics in humans after single oral doses [16].
• Pharmacokinetic properties and oral bioavailabilities of difloxacin in pig and chicken [17].
• CONCLUSIONS: The data demonstrate that difloxacin can reverse drug resistance in unselected human neuroblastoma cells and is therefore a potential candidate for future clinical trials [18].
• The single-dose disposition kinetics of difloxacin were determined in clinically normal lactating goats (n = 6) after intravenous (i.v.), subcutaneous (s.c.) and intramuscular (i.m.) administration of 5 mg/kg [19].
• The extent of serum protein binding of difloxacin in goats was 13.79 +/- 1.02% and the systemic availability was 95.4 +/- 1.17% [20].

Anatomical context of A 56619

• Morphologic and biochemical changes in articular cartilages of immature beagle dogs dosed with difloxacin [21].
• Integrin staining on chondrocytes was not significantly affected by difloxacin under the given conditions with the exception of a slight reduction of the alpha v integrin chain in 1 of 5 dogs of the 48-hr group [22].
• Collagen, however, was depleted from the cartilages of the dogs that were euthanized 36 or 48 hr after the first dose of difloxacin [21].
• In this study, we have examined the in vitro chemosensitizing activity of difloxacin, a quinolone antimicrobial agent, in the multidrug-resistant human myeloid leukemia HL-60/AR cell line [23].
• Pharmacokinetics of difloxacin and its concentration in body fluids and endometrial tissues of mares after repeated intragastric administration [24].

Associations of A 56619 with other chemical compounds

• The MICs of temafloxacin hydrochloride and difloxacin were increased by 2 to 5 twofold dilutions in urine at pH 6.5 compared with 4 to 5 twofold-dilution increases in the MICs of ciprofloxacin [9].
• A rapid, specific reversed-phase HPLC method is described, with solid-phase extraction, for assaying five quinolones (ciprofloxacin, difloxacin, enrofloxacin, norfloxacin and marbofloxacin) with confirmative diode-array detection in samples of bovine kidney, muscle and eggs [25].
• Ciprofloxacin and the internal standard, difloxacin, were separated on a Keystone ODS column (100 x 2.1 mm I.D., 5 microns Hypersil) using a mobile phase of 30 mM phosphate buffer (pH 3), 20 mM triethylamine, 20 mM sodium dodecyl sulphate-acetonitrile (60:40, v/v) [26].
• The most active agents were imipenem, SCH 34343, ciprofloxacin, difloxacin (A-56619), and A-56620 [27].
• An in vitro investigation of the intraphagocytic bioactivity of difloxacin, ciprofloxacin, pefloxacin and fleroxacin [28].

Gene context of A 56619

• We conclude that difloxacin is an effective chemosensitizer of MRP-associated multidrug-resistant tumor cells and is a potential candidate for clinical use to reverse multidrug resistance [23].
• Difloxacin reverses multidrug resistance in HL-60/AR cells that overexpress the multidrug resistance-related protein (MRP) gene [23].
• Ciprofloxacin and the internal standard difloxacin were separated on a mu-Bondapak C18 column (30 cm x 3.9 mm inside diameter, 10 microns particle size), using a mobile phase of 0.1 M phosphate buffer (pH 2.5):acetonitrile (75:25, vol/vol) [29].
• Overall, the most important results is the finding that fibronectin was a sensitive immunohistochemical marker for change in cartilage samples due to difloxacin treatment in dogs [22].

Analytical, diagnostic and therapeutic context of A 56619

• By using high-performance liquid chromatography, the metabolism and pharmacokinetics of difloxacin were characterized in humans after single oral doses of 200, 400, and 600 mg [16].
• The peak serum concentration and serum half-life of temafloxacin hydrochloride in mice were approximately one-half and one-sixth, respectively, that of difloxacin after oral administration [9].
• Immunohistochemistry of articular cartilage from immature beagle dogs dosed with difloxacin [22].
• An injectable formulation of difloxacin (5%) was administered IV and IM in single doses (5 mg/kg); for IG administration, an oral solution was prepared and administered via nasogastric tube [30].
• Comparison of fluoroquinolone pharmacokinetic parameters after treatment with marbofloxacin, enrofloxacin, and difloxacin in dogs [31].

References