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At least 19 recordsLinked to original sources
PubMed1998

Reversed-phase high-performance liquid chromatographic determination of enoxacin and 4-oxo-enoxacin in human plasma and prostatic tissue. Application to a pharmacokinetic study.

A simple high-performance liquid chromatographic method has been developed for the simultaneous determination of enoxacin and 4-oxo-enoxacin in plasma and prostatic tissue. The work-up procedure involves a liquid-liquid extraction step followed by isocratic chromatography on a reversed-phase analytical column, with ultraviolet absorbance detection (lambda = 340 nm). Using a mobile phase of 20.9% (v/v) acetonitrile buffer (pH 2.1), adequate retention time and separation among the analytes has been obtained using tetrabutylammonium hydroxide included in the eluent. Retention times are 5.2 min for enoxacin, 6.8 min for pefloxacin and 12 min for 4-oxo-enoxacin. For plasma and prostatic tissue, the precision of the assay was below 9%. The percent recovery from the nominal values for accuracy ranged from 94 to 108%. The limits of quantitation were 20 ng/ml for plasma and 50 ng/g for tissue (precision < 18%). The detection limits were 10 ng/ml and 25 ng/g, respectively. The calibration curves were linear from 20 to 1000 ng/ml for plasma and from 50 to 2500 ng/g for tissue. In plasma, the extraction recoveries averaged 52% for enoxacin and 63% for 4-oxo-enoxacin. In prostatic tissue, they were 57 and 76% for the two analytes, respectively. This method has been employed for the determination of enoxacin and 4-oxo-enoxacin in plasma and prostatic tissue samples from patients following repeated oral administration of enoxacin (400 mg twice a day for four days).

Adenoma↗
PubMed1989

[Susceptibility of clinically important Bacteroides species against enoxacin-metronidazole and enoxacin-clindamycin combinations].

To assess the activity of enoxacin, clindamycin and metronidazole, MICs of clinical isolates of saccharolytic intestinal Bacteroides spp. were determined, using the agar dilution method according to NCCLS guidelines. Checkerboard titrations of enoxacin-metronidazole and enoxacin-clindamycin were done on Wilkins-Chalgren agar; inoculation, incubation and reading of plates were as for determination of MICs. Metronidazole MIC 90s for Bacteroides fragilis (23 strains) and Bacteroides thetaiotaomicron (23 strains) were 0.5 mg/l, clindamycin MIC 90 for B. fragilis was 1 mg/l, and for B. thetaiotaomicron 8 mg/l, whereas enoxacin MIC 90 values were 16 mg/l and 64 mg/l, respectively. The evaluation of the inhibitory effects of the combination enoxacin-metronidazole for B. fragilis showed additional effects in eleven strains, indifference in seven strains and antagonism in one. The figures for B. thetaiotaomicron showed addition in five strains, indifference in 17 strains, antagonism in one. For B. fragilis the combination enoxacin-clindamycin showed addition in ten strains, indifference in six, and antagonism in one; for B. thetaiotaomicron synergism in one strain, addition in four strains, indifference in 17 strains. In conclusion, the absence of antagonism and the overall preponderance of additional and indifferent effects warrant the use of enoxacin in combination with metronidazole or clindamycin in clinical trials of treatment of anaerobic-aerobic mixed infections.

Bacteroides↗
PubMed1989

The theophylline-enoxacin interaction: II. Changes in the disposition of theophylline and its metabolites during intermittent administration of enoxacin.

The pharmacokinetics of theophylline and its three major metabolites, 3-methylxanthine, 1-methylurate, and 1,3-dimethylurate, were studied during intermittent administration of enoxacin. The addition of enoxacin (400 mg, twice daily) to a theophylline dosing regimen (150 mg, twice daily) resulted in an immediate fall in plasma theophylline metabolite concentrations. Mean steady-state theophylline concentration in plasma during the dosing interval increased from 3.17 to 8.23 micrograms/ml. The mean 12-hour recovery of total theophylline metabolite decrease from 76.3 to 38.6 mg. After the discontinuation of enoxacin, but not theophylline, the plasma theophylline metabolite levels immediately increased to near or above the concentrations observed before enoxacin coadministration. Concurrently, theophylline concentrations decreased to levels equivalent to those observed before enoxacin coadministration. In general, the changes in plasma theophylline concentrations observed after the addition of discontinuation of enoxacin were complete within 3 days.

Adult↗
PubMed1993

Oral enoxacin for infection prevention in adults with acute nonlymphocytic leukemia. The Enoxacin Prophylaxis Study Group.

A randomized, double-blind, placebo-controlled trial was conducted in eight hematologic units to determine the efficacy and safety of oral enoxacin for infection prevention in adult patients with acute nonlymphocytic leukemia. One hundred nineteen patients undergoing remission induction or consolidation chemotherapy were enrolled; 62 of them received enoxacin (400 mg orally every 12 h). Patients received antifungal prophylaxis with oral mycostatin (1,000,000 U four times daily) or clotrimazole (1 troche five times daily). Analysis was performed on an intent-to-treat basis. There was no significant difference between groups in race, age, or type and stage of leukemia, but there were more males in the placebo group (P = 0.073 [Fisher's exact test]). Fewer enoxacin patients had gram-negative bacteremia (1 versus 14 [P < 0.001]), gram-negative infection at any site (2 versus 19 [P < 0.001]), or bacterial and/or fungal infection (17 versus 26 [P = 0.056]). There was no significant difference in the number of patients with gram-positive infection at any site (12 versus 16), gram-positive bacteremia (9 versus 10), deep fungal infection (6 versus 2), death (2 versus 3), other antimicrobial therapy required (48 versus 48), therapy with amphotericin B (15 versus 7 [P = 0.105]), any adverse event (45 versus 36), or any study drug-associated adverse events (13 versus 6). Logistic regression confirmed (odds ratios and 95% confidence intervals are given in parentheses) that enoxacin reduced the risk of gram-negative infection (0.07; 0.01 to 0.30), especially gram-negative bacillary bacteremia (0.05; 0.01 to 0.37), without altering the risk of gram-positive bacterial (0.63; 0.26 to 1.5), deep fungal (2.57; 0.47 to 13.9), or Clostridium difficile (1.16; 0.3 to 4.56) infection. The median time to the onset of fever of more than or equal 102.8 F (39.3 degree C) was 32 days for the enoxacin group versus 15 days for patients receiving placebo (P=0.0007 [Wilcoxon test]). In patients with acute nonlymphocytic leukemia, oral enoxacin prevents gram-negative infections, delays the onset of fever, does not alter the incidence of gram-positive or proven deep fungal infections, and is well tolerated.

Administration, Oral↗
PubMedDate not supplied

In vitro susceptibility of aerobic gram-negative blood culture isolates to oxolinic acid, norfloxacin, ciprofloxacin, enoxacin, pefloxacin, ofloxacin and oxo-enoxacin.

100 gram-negative strains isolated from blood cultures were selected for the evaluation of the in vitro activity of oxolinic acid, norfloxacin, ciprofloxacin, enoxacin, pefloxacin, ofloxacin and oxo-enoxacin. Ciprofloxacin showed the highest intrinsic activity. Oxo-enoxacin, the major metabolite of enoxacin, was 10-15-fold less active than enoxacin. Against Enterobacteriaceae and Vibrionaceae, all fluorinated quinolones except norfloxacin were equally effective, while against non-fermenters, ciprofloxacin and ofloxacin demonstrated greater activity than the others. Resistance to oxolinic acid had a detrimental effect on susceptibility to the new fluorinated quinolones.

Anti-Bacterial Agents↗
PubMed1995

The intestinal transport mechanism of fluoroquinolones: inhibitory effect of ciprofloxacin, an enoxacin derivative, on the membrane potential-dependent uptake of enoxacin.

PURPOSE: To clarify the absorption-structure relationship for the fluoroquinolones from the point of view of inhibitory behavior. METHODS: The inhibitory effects of ciprofloxacin on the transport process of enoxacin across the rat intestinal brush-border membrane was examined. RESULTS: Ciprofloxacin, which has a similar structure to enoxacin, exhibited a pH-dependent interference with enoxacin absorption from rat jejunal loops. The uptake experiments using BBM vesicles showed that ciprofloxacin significantly reduced not only the initial binding of enoxacin to the membrane surface, but also the K(+)- or H(+)-diffusion potential-dependent transport across the membrane. Furthermore, an H(+)-diffusion potential (interior negative) also exhibited a stimulative uptake of ciprofloxacin. CONCLUSIONS: These results suggest that the inhibition behavior of ciprofloxacin from the jejunal loop was closely related to the ionic diffusion potential-dependent uptake of enoxacin across the brush-border membrane.

Animals↗
PubMed1988

The theophylline-enoxacin interaction: I. Effect of enoxacin dose size on theophylline disposition.

Theophylline interacts pharmacokinetically with a variety of other drugs. Recently enoxacin was found to change theophylline's disposition. In a four-subject, four-way crossover study enoxacin was administered every 12 hours at four levels (0, 25, 100, and 400 mg) for 14 doses. With the ninth dose of enoxacin, 200 mg theophylline was coadministered. Blood and urine samples were assayed by sensitive and specific assays for the parent drugs and their metabolites. Significant reduction in the formation of theophylline's three major metabolites occurred on coadministration of enoxacin. At the 400 mg dose level, enoxacin caused a threefold decrease in theophylline's plasma clearance, a fourfold decrease in the urinary recovery of 3-methylxanthine and 1,3-dimethylurate, and a threefold decrease in the recovery of 1-methylurate.

Adult↗
PubMed1990

[Photosensitivity following enoxacin and xipamide: combined phototoxic and photo-allergic reaction to enoxacin, photo-allergic reaction to xipamide with subsequent transient light reaction].

In a 51-year-old female patient, we observed a combined phototoxic and photoallergic reaction to Enoxacin, a photoallergic reaction to Xipamide, as well as increased sensitivity to light after withdrawal of the drugs. This unusual diagnosis was based on the clinical picture, graded radiation with UV-A and UV-B, the irradiated intradermal assay, and histological findings. To the best of our knowledge, this is the first report on a photoallergic reaction to Xipamide associated with a combined phototoxic and photoallergic reaction to Enoxacin.

Biopsy↗
PubMed1988

Pharmacokinetics of intravenous and oral enoxacin in healthy volunteers.

In a randomized, crossover study single 200 and 800 mg doses of enoxacin were administered intravenously and orally to eight healthy normal volunteers. Plasma and urinary enoxacin concentrations and urinary concentrations of its oxo-metabolite were determined by high-performance liquid chromatography. At the end of a 1 h intravenous infusion period, mean enoxacin plasma concentrations were 1.8 and 6.6 mg/l for the 200 and 800 mg doses, respectively. Disappearance of enoxacin from the systemic circulation appeared to follow first order kinetics with harmonic mean elimination half lives of 3.3 and 4.7 h for the 200 and 800 mg dose groups, respectively. However, enoxacin kinetics were dose-dependent over the dose range tested. Total body clearance decreased and elimination half-life increased with increasing dose. The volume of distribution was large (2.8 l/kg) and independent of dose. Absorption of orally administered enoxacin was rapid, with mean peak plasma concentrations (1.0 and 3.8 mg/l) appearing one to two hours postdose. Absolute oral bioavailability averaged 89%, and was independent of the dose administered. Cumulative enoxacin urinary recovery accounted for 51-53% of the dose irrespective of dose or route of administration. Enoxacin renal clearance exceeded creatinine clearance indicating that urinary excretion of enoxacin involved both glomerular filtration and tubular secretion. Urinary excretion of the oxo-metabolite averaged 16% and 11% following the 200 and 800 mg dose, respectively. Evidence of dose dependent decrease in enoxacin renal clearance and formation of its oxo-metabolite was observed. Enoxacin was well tolerated during the course of the trial. The present study shows that enoxacin pharmacokinetics can be characterized by apparent first order elimination, large volume of distribution, and dose-dependent increase of half life. Oral absorption of enoxacin is complete over a wide dose range.

Administration, Oral↗
PubMed1998

Urinary bactericidal activity and pharmacokinetics of enoxacin versus norfloxacin and ciprofloxacin in healthy volunteers after a single oral dose.

In an open, randomised monocentric crossover study in six male and six female healthy volunteers, the urinary antibacterial activity and pharmacokinetics of enoxacin, norfloxacin and ciprofloxacin were assessed. Urine was collected up to 6 days, and venous blood samples up to 12 h, after a single oral dose of 400 mg enoxacin, 400 mg norfloxacin and 500 mg ciprofloxacin. Enoxacin (250 mg/l) demonstrated the highest peak concentration (median) in the urine (0-6 h), followed by ciprofloxacin (237 mg/l) and norfloxacin (157 mg/l) as determined by the HPLC assay. The total amount (mean) excreted by the kidneys as parent drugs were as follows: enoxacin 54% of dose, ciprofloxacin 33% of dose, and norfloxacin 22% of dose. The mean plasma concentrations decreased from 1 to 4 h after administration for enoxacin from 1.9 to 1.4 mg/l, for ciprofloxacin from 2.0 to 0.8 mg/l and for norfloxacin from 1.3 to 0.5 mg/l. The antibacterial activity in urine was determined as urinary bactericidal titers (UBT), i.e. the highest 2-fold dilution of urine still bactericidal for the reference organism (E. coli ATCC 25,922) and for five uropathogens with minimal inhibitory (MIC) and bactericidal (MBC) concentrations ranging from highly susceptible to resistant cultured from the urine of patients with complicated urinary tract infections (UTI). For the E. coli ATCC 25,922, the organism with the lowest MIC, median UBTs of ciprofloxacin were present for 4 days, decreasing from 1:512 to 1:2, that of enoxacin for 2 days, decreasing from 1:256 to 1:4, and that of norfloxacin for 2 days, decreasing from 1:128 to 1:2. For the five uropathogens (with increasing MICs: K. pneumoniae, P. mirabilis, E. coli (resistant to nalidixic acid), P. aeruginosa and E. faecalis), the UBTs decreased in general, according to MICs, demonstrating the same relations of UBTs for ciprofloxacin (highest) versus enoxacin (medium) versus norfloxacin (lowest) with one exception (P. mirabilis) for which norfloxacin showed higher UBTs than enoxacin. The minimal urinary bactericidal concentrations (MUBC), as derived from urinary concentrations, and UBTs showed a fairly wide inter- and intraindividual range and were generally higher than the corresponding MBCs as determined in Mueller Hinton broth. In conclusion, according to antibacterial activity in urine determined as UBTs, a single oral dose of ciprofloxacin (500 mg) generally resulted in the highest and longest-lasting UBTs followed by that of enoxacin (400 mg) and norfloxacin (400 mg). A dose of 400 mg enoxacin can be expected to be at least equivalent if not superior to that of 400 mg norfloxacin. Only enoxacin and ciprofloxacin exhibited urinary bactericidal activity against all test organisms up to 12 h in all individuals. Therefore, clinical comparison of enoxacin versus ciprofloxacin in the treatment of complicated UTI could be worth testing.

Administration, Oral↗
PubMed1987

Accumulation of enoxacin by Escherichia coli and Bacillus subtilis.

Several methods were used to determine enoxacin uptake in Escherichia coli strains because washing of cells removed all or most cell-associated enoxacin whereas no washing was associated with large amounts of cell-bound enoxacin. Washing after up to 40 to 45 min of exposure to enoxacin followed by suspension in drug-free medium prevented a significant effect of enoxacin on cell growth. Cell uptakes obtained with different methods showed no difference in the shape of the timed uptake curves but did show significant quantitative differences. These results are consistent with cell-associated enoxacin comprising a freely exchangeable pool of drug. Lineweaver-Burk plots of uptake were consistent with uptake of enoxacin by simple diffusion. No saturability and no competition with ciprofloxacin were observed. Low temperature (4 degrees C) was associated with decreased uptake. Arsenate, carbonyl cyanide m-chlorophenylhydrazone, sodium fluoride, sodium azide, and 2,4-dinitrophenol had no effect on uptake. We conclude that the mechanism of transport of enoxacin into cells is by simple diffusion. Mutants of E. coli with deficiency of outer membrane proteins F and C and an enoxacin-resistant mutant selected by serial passage with increasing enoxacin concentrations demonstrated that F porins play a significant role in enoxacin uptake and influence susceptibility to enoxacin. Uptake was shown to be similar in a strain of Bacillus subtilis.

Bacillus subtilis↗
PubMed1989

Inhibition of enoxacin absorption by antacids or ranitidine.

Ten normal volunteers participated in a randomized, five-way crossover study to determine the effect of concurrent enoxacin and antacid or ranitidine administration on enoxacin absorption. The bioavailability of a single oral 400-mg enoxacin dose was significantly decreased, by 73 and 49%, when Maalox TC was administered 0.5 and 2 h before enoxacin, respectively. Enoxacin bioavailability was not significantly altered when the antacid was given 8 h before or 2 h after enoxacin administration. Ranitidine, administered intravenously 2 h before enoxacin, also significantly decreased enoxacin bioavailability, by 40%. The correlation between the proximity of antacid administration and the magnitude of the decrease in enoxacin bioavailability supports complexation as the mechanism of the antacid-enoxacin interaction. However, reduction of enoxacin bioavailability by ranitidine suggests that elevated gastric pH may also play a role in the antacid-enoxacin drug-drug interaction.

Adolescent↗
PubMed1988

The absorption and disposition of enoxacin in healthy subjects.

Enoxacin is a new orally active, synthetic broad-spectrum antibacterial drug of the fluorinated quinolone class. The pharmacokinetics and renal handling of this drug have not been thoroughly investigated, in particular, with specific analytical methodology. Sixteen healthy, young subjects received a single 400-mg oral dose of enoxacin after an overnight fast and multiple blood samples and all urine were collected for 33 hours. Enoxacin in plasma and urine and oxo-enoxacin in urine were determined by a high-performance liquid chromatographic method. Enoxacin was absorbed rapidly, with tmax values ranging from 0.5 to 2.5 hours. The variability in the AUC values of 35% was reduced to 23% when variations in body weight were taken into consideration. The terminal half-life ranged from 4.2 to 6.8 hours and the unbound fraction in plasma was 0.33 +/- 0.07. In urine, 44 +/- 9% of the dose was recovered as unchanged enoxacin and 5.4 +/- 3.9% as oxo-enoxacin; there was no evidence of conjugates of enoxacin in urine. Renal clearance of enoxacin was 230 +/- 92 mL/min, with 17 +/- 8% of this being due to glomerular filtration and 83 +/- 8% being due to tubular secretion. These data indicate that the major potential drug interactions affecting enoxacin disposition are likely with drugs competing for renal proximal tubular secretion and hepatic elimination. These conclusions regarding enoxacin are likely to be applicable to the fluorinated quinolones in general.

Administration, Oral↗
PubMed1986

In vitro activity, pharmacokinetics, clinical safety and therapeutic efficacy of enoxacin in the treatment of patients with complicated urinary tract infections.

Minimal inhibitory concentrations (MIC) of enoxacin, nalidixic acid, pipemidic acid, norfloxacin, ciprofloxacin, ofloxacin and pefloxacin against isolates from 400 urological in-patients with complicated urinary tract infections (UTI) were determined by means of an agar dilution technique (10(4) cfu, multipointer). 28 patients (21 male, seven female) aged 36 to 84 years with complicated UTI due to sensitive bacteria were treated orally with 200 mg enoxacin b.i.d. for six to 14 days. Plasma and urine samples were collected from 19 patients, at intervals prior to and following a 400 mg dose of enoxacin, and enoxacin concentrations were determined by a high pressure liquid chromatography (HPLC) method. The MICs of enoxacin against all but one of the gram-negative isolates cultured from 265 urological patients were between 0.03 and 4 mg/l. The MICs against 134 gram-positive isolates were between 0.25 and 16 mg/l except two strains of streptococci. At a concentration of 4 mg/l (8 mg/l), 90.3% (98%) of the total spectrum of isolates were inhibited by enoxacin. Of the quinolones tested, ciprofloxacin appeared to be the most active compound in vitro and cinoxacin the least active antimicrobial agent. The in vitro activity of enoxacin was comparable to that of norfloxacin, ofloxacin and pefloxacin. Oral administration of 400 mg enoxacin to elderly patients resulted in peak serum concentrations between 0.7 and 6.3 mg/l (mean 3.6 mg/l) attained between 1.0 and 6.0 h following drug ingestion. The mean urinary recovery of parent drug within 24 h was 31.2% of the administered dose. 25 of 28 patients treated orally with enoxacin could be followed-up for five to 14 days after the end of treatment. Enoxacin therapy in these patients resulted in 18 cures, one failure and six relapses (same species). The drug was well tolerated and there was no evidence of renal, hepatic or haematological toxicity. Enoxacin appears to be well suited for the treatment of complicated UTI.

Administration, Oral↗
PubMed1988

Pharmacokinetics of enoxacin and its penetration into bronchial secretions and lung tissue.

Pharmacokinetic data were obtained from four healthy volunteers after oral administration of a single 400 or 600 mg dose of enoxacin. Enoxacin was absorbed quickly and absorption was increased when enoxacin was ingested after a meal. Renal clearance of enoxacin and 4-oxo-enoxacin decreased after simultaneous administration of probenecid. In addition, pharmacokinetic parameters of enoxacin and its 4-oxo metabolite were determined for plasma and sputum from 19 patients treated with enoxacin, 400 or 600 mg bd, for a respiratory tract infection. The half-life of both enoxacin and 4-oxo-enoxacin was 5-6 h; during treatment with 400 and 600 mg bd, the plasma concentrations exceeded MIC values for most bacteria isolated in respiratory tract infections, including most Pseudomonas aeruginosa strains; Streptococcus pneumoniae was an exception. Diffusion from plasma to sputum was approximately 100%. Of an ingested dose, 60-65% was recovered in the urine in 24 h. In a third study, a single 600 mg dose of enoxacin was given to 15 patients undergoing thoracotomy. Subsequent lung tissue concentrations of enoxacin were significantly higher than plasma concentrations at the same time after ingestion.

Administration, Oral↗