• Tuberculosis and Respiratory Diseases
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• v.38 no.4
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• pp.372-378
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• 1991

Some kinds of newer fluoroquinolone antibiotics are known to interact with theophylline, which is widely used as a potent bronchodilator in asthma or chronic obstructive lung disease. To evaluate the effect of enoxacin and ciprofloxacin on the metabolism of theophylline, aminophylline was administered intravenously in bolus (6 mg/kg) over 30 minutes to 6 healthy volunteers (age: $23.3{\pm}4.2$ year, body weight: $63.2{\pm}9.0\;kg$, height: $169.0{\pm}6.5\;cm$, female 3, male 3) before and after per oral 5-day medication of enoxacin and ciprofloxacin, respectively and we measured the level of theophylline in serum. The results were as follows: 1) Enoxacin and ciprofloxacin did not influence the volume of distribution significantly. 2) Enoxacin decreased the clearance of theophylline significantly (from $42.9{\pm}14.6\;ml/min$ to $30.1{\pm}6.3\;ml/min$: p<0.05), but ciprofloxacin did not cause significant decrease (to $32.8{\pm}6.2\;ml/min$: p>0.005). 3) Enoxacin increased the elimination half life of theophylline significantly (from $496{\pm}83\;min$ to $693{\pm}32\;min$: p<0.001), but ciprofloxacin did not cause significant increase (to $687{\pm}222\;min$: p>0.05). These results suggested that enoxacin influenced clearance and elimination half life significantly and thorough monitoring of the level of theophylline in patients with coadminstration of enoxacin and theophylline was necessary. In case of ciprofloxacin, the influence on the metabolism of theophylline was not statistically significant, but one exceptionally large decrease of the clearance and increase of the elimination halflife of theophylline suggested the necessity of monitoring of theophylline level during coadministration of ciprofloxacin and theophylline.

• YAKHAK HOEJI
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• v.43 no.4
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• pp.437-441
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• 1999

Enoxacin[1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-\piperazinyl)-1,8-naphthyridine-3-carboxylic acid, ENX] is a new quinolone antibacterial agent. The method is based on the highly colored charge-transfer complex formation of this drug as a $\pi$-electron donor with 7,7,8,8-tetracyanoquinodimethane(TCNQ) or chloranil(CL) as $\pi$-acceptors. The colored products were measured spectrophotometrically at 842 nm and 552 nm for TCNQ and CL, respectively. The different experimental conditions are optimized. The linearities for TCNQ and CL were $1.6{\;}\mu\textrm{g}/mL~32{\;}\mu\textrm{g}/mL$ and $6.4{\;}\mu\textrm{g}/mL~160{\;}\mu\textrm{g}/mL$, respectively and colors were produced in non-aqueous media. This report describes a simple and ra\pid method for the analysis of enoxacin.

• YAKHAK HOEJI
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• v.35 no.5
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• pp.353-359
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• 1991

Treatment of 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(l-piperazinyl)-I, 8- naphthyridine-3-ca rboxylic acid (Enoxacin) with alkyl(or aryl) isothiocyanates which obtained from alkyl(or aryl) amines afforded six 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-alkylthiocarbamylpiperazinyl)-1, 8- naphthyridine-3-carboxylic acids and five 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(l-arylthiocarbamyl piperazinyl)-1, 8-naphthyridine-3-carboxylic acids. The compounds synthesized were evaluated for their antimicrobial activities, in vitro, against Escherichia coli 6-PE-4, Bacillus subtilis 74-51, Proteus vulgaris 78645, Klebsiella pneumoniae JYA-78314, Staphylococcus aureus 79110 and Pseudomonas aeruginosa 8765-1 P$_{2}$.

• Bulletin of the Korean Chemical Society
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• v.33 no.9
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• pp.3055-3060
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• 2012

A simple, rapid and sensitive spectrofluorometric method was developed for the determination of folic acid (FA), based on its quenching effect on the fluorescence intensity of enoxacin (ENX)-europium ($Eu^{3+}$) complex as a fluorescent probe. Fluorometric interaction between ENX-$Eu^{3+}$ complex and FA was studied using UV-visible and fluorescence spectroscopy. The quenched fluorescence intensity at an emission wavelength of 614 nm was proportional to the concentration of FA. Optimum conditions for the determination of FA were investigated. Under optimal conditions, the reduced fluorescence intensity at 614 nm was responded linearly with the concentration of FA. The linearity was maintained in the range of $1.25{\times}10^{-9}$ to $1.50{\times}10^{-7}$ M (R = 0.9986) with the limit of detection ($3S_b/m$) (where $S_b$ is the standard deviation of blank and m is the slop of linear calibration curve) of $6.94{\times}10^{-10}$ M. The relative standard deviation (RSD) for 9 repeated measurements of $1.0{\times}10^{-9}$ M FA was 1.42%. This method was simple, cost effective, and relatively free of interference from coexisting substances. Successful determinations of FA in pharmaceutical formulation and biological samples with the developed method were demonstrated.

• Biomolecules & Therapeutics
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• v.6 no.1
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• pp.63-72
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• 1998

-4-Quinolone antibiotics (pefloxacin, ciprofloxacin, norfoxacin, ofloxacin and enoxacin) were tested for mutagenicity in Salmonella typhimurium TA98, TA100, TA1535, TA1537, TA1538 and TA102, for chromosomal aberrations in cultured Chinese hamster lung (CHL) cells, and for wing somatic mutations and recombinations (wing spot) in Drosophila. Five 4-quinolones did not show any mutagenicity in Salmonella typhimurium TA98, TA100, TA1535, TA1537 and TA1538. However, they were mutagenic inSalmonella typhimurium TA102 with and without metabolic activation in both plate incorporation method and preincubation method. Ciprofloxacin induced structural chromosome aberrations in CHL cells both with and without metabolic activation, and the frequencies were 6% and up to 28%, respectively. Pefloxacin showed equivocal evidence, however, norfloxacin, ofloxacin and enoxacin did not induce the structural chromosome aberrations both in the presence and absence of metabolic activation. In the wing spot assay in Drosophila, ofloxacin increased the frequency of small single spots significantly in a dose-dependent manner but there was no dose-dependent increase of single or twin spots in the others.

• Toxicological Research
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• v.8 no.1
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• pp.63-70
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• 1992

The present study was performed to evaluate whether the application of Fenbufen is reasonable for predicting the convulsive liability of the quinolone derivatives and to examine whether pentylenetetrazole (PTZ) can be used as a screening tool for their Central Nervous System (CNS) toxic pontential. The convulsive activity of the quinolones was markedly potentiated by the pretreatment of Fenbufen. In combination with Fenbufen, enoxacin (ENX), norfloxacin (XFLX), and ciprofloxacin (CPFX) provoked convlusions and subsequent death at the intravenous doses of 0.5mg/kg, 10mg/kg, and 40mg/kg, respectively, whereas ofloxacin (OFLX) and pefloxacin (PFLX) did not induce convulsions and death even at a relatively high dose of 100mg/kg iv.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1997.04a
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• pp.57-63
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• 1997

Animal and clinical investigations have shown that fluoroquinolones, new quinolone antibacterial agents (NQs), are well absorbed across the intestinal tract, with a bioavailability of 60-90% after oral administration. Although some types of carrier-mediated intestinal transport mechanisms have been reported for enoxacin (ENX), ofloxacin (OFLX) and sparfloxacin (SPFX), recent results using a human intestinal epithelial cell line, Caco-2, indicated a passive or nonsaturable transport of SPFX, one of the most hydrophobic NQs. The mechanism underlying the intestinal absorption of NQs is still largely unknown. The distribution of NQs into peripheral tissues including erythrocytes is very rapid and their tissue-to-plasma concentration ratios (Kp) are considerably larger than those of inulin (an extracellular fluid space marker), in spite of almost complete ionization of NQs at the physiological pH. Our findings suggest that OFLX and lomefloxacin (LFLX) are taken up by rat erythrocytes via a transport system common to that of a water-soluble vitamin, nicotinic acid.

• Journal of fish pathology
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• v.9 no.2
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• pp.185-193
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• 1996

Extensive acquirement of drug resistance to traditional antibacterial agents poses a serious problem to eel aquaculturists. To collect the basic information for new drug development in the future, we assessed the in vitro antibacterial efficacy of 14 new quinolones with 75 isolates of Edwardsiella tarda from local aquaculture tanks of Anguilla japonica. Of all tested quinolones under development or marketed for human use, DU-6859 was most potent with its $MIC_{50}$ value of $0.05{\mu}g$/ml in broth microdilution assay. The drugs whose $MIC_{50}$ values ranged from 0.2 to $0.78{\mu}g$/ml were T-3762, Bay-y3118, ciprofloxacin, norfloxacin, ofloxcin and tosufloxacin. The weakest group of drugs, with their $MIC_{50}$ being 1.56-$3.13{\mu}g$/ml, were difloxacin, sparfloxacin, fleroxacin, Q-35, amifloxacin, lomefloxacin and enoxacin. The number of resistant strains, when arbitrarily defined with their MICs of $\geq6.25{\mu}g$/ml, was : 3 to T-3762, 3 to Bay-y3118, 44 to difloxacin, 16 to sparfloxacin, 13 to ciprofloxacin, 19 to fleroxacin, 36 to Q-35). 31 to amifloxacin, 5 to norfloxacin, 13 to ofloxacin, 31 to lomefloxacin, 41 to enoxacin, 12 to tosufloxacin and 0% to DU-6859, respectively. This information can be taken into consideration for the future development of fisheries antibacterial quinolones.

• Journal of Yeungnam Medical Science
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• v.10 no.1
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• pp.135-143
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• 1993

The susceptibilities of 45 clinical isolates of bacteroides frogilis to cefaclor, ciproflxacin and imipenem were determined by new method, E-test (AB Bidisk, Solna, Sweden) and were compared with those from conventional agar dilution method by using brain heart infusion, Mueller-Hinton and Wilkins Chalgren agar plates. And the susceptibility of 60 clinical isolates of Bacteroides fragilis group (B. fragilis 45 strains, B. distasonis 6 strains, B. ovatus 5 strains, B. thetaiotaomicron 4 strains) to 5 quinolones (ciprofloxacin, enoxacin, norfloxacin, ofloxacin, pefloxacin) were determined by in vitro agar dilution method. Compared with agar dilution MICs for B. fragilis 45 strains, 90.3% of E-test MICs were within ${\pm}$1 dilution of the agar dilutions, and 98.4% were within 2 dilutions. And there were little effect of different medium bases to determine MICs except Mueller-Hinton agar. On Mueller-Hinton agar, B. fragilis showed have or no growth activity. In vitro susceptibility of B. fragjlis group to quinolones, most of the test strains showed resistant patterns to quinolones except ofloxacin and there was little difference of susceptibility patterns between species of B. fragilis group.

• Korean Journal of Veterinary Pathology
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• v.1 no.1
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• pp.40-45
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• 1997

The phototoxic potentials of LB20304a a new quinolone compound being developed by LG Chemical Ltd, and reference compounds (Ciprofloxacin; CPFX, Enoxacin; ENX and Lomefloxacin; LFLX) were compared in a murine model. in addition photostability of these compunds was studied after irradiation with long-wave UV light(UVA, 0, 0.3 1 or 3 Joule/$Cm^2$) When hairless mice(9 to 11 weeks old 19-26g) were orally administered with different dose levels of test compunds and exposed to UVA(40J/$cm^2$) inflammatory reactions were observed in a dose dependent manner. Among the compounds tested, LB20304a demonstrated the least phototoxic effects and showed no inflammatroy lesions at a dose level of 100mg.kg (Low dose). ENX and LFLX demonstrated much greater phototoxic reactions while CPFX showed similar or slightly greater phototoxic reactions compared to LB20304a. Similar to the in-vivo results the solutions of LB20304a and CPFX irradiated with UVA demonstrated reduced spectral changes compared to those of ENX and LFLX. In conclusion these data suggest that phototoxic potencies of the quinolones tested were; LFLX > ENX > CPFX $\geq$ LB20304a. No phototoxic dose of LB20304a in mice was 100 mg/kg.