Clinical efficacy and tolerance of fleroxacin in patients with urethritis caused by Chlamydia trachomatis

Pust, R; Aekenheil-Köppe, H.R.; Weidner, W.; Meier-Ewert, Herbert

doi:10.1093/jac/22.supplement_d.227

Cited by 17 publications

(4 citation statements)

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“…Interestingly, despite the observation that Chlamydia trachomatis is more susceptible than U. urealyticum to fluoroquinolones in vitro, a higher fraction of patients with nongonococcal urethritis caused by U. urealyticum was cured by norfloxacin (75) and ciprofloxacin (235) than those with Chlamydia trachomatis, and ciprofloxacin appeared to be more effective (P = 0.12) than doxycycline (235). In contrast, ofloxacin (200 mg twice daily) (50, 243,530,622) or fleroxacin (400 to 800 mg per day) (603) given for 5 to 15 days eradicated Chlamydia trachomatis from the urethra or cervix in >90% of patients, a result comparable to that with doxycycline in one study (243). Urethritis that was culture negative for chlamydia responded to ofloxacin less well in men (530).…”

Section: Sexually Transmitted Diseasesmentioning

confidence: 94%

Fluoroquinolone antimicrobial agents

1989

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The fluoroquinolones, a new class of potent orally absorbed antimicrobial agents, are reviewed, considering structure, mechanisms of action and resistance, spectrum, variables affecting activity in vitro, pharmacokinetic properties, clinical efficacy, emergence of resistance, and tolerability. The primary bacterial target is the enzyme deoxyribonucleic acid gyrase. Bacterial resistance occurs by chromosomal mutations altering deoxyribonucleic acid gyrase and decreasing drug permeation. The drugs are bactericidal and potent in vitro against members of the family Enterobacteriaceae, Haemophilus spp., and Neisseria spp., have good activity against Pseudomonas aeruginosa and staphylococci, and (with several exceptions) are less potent against streptococci and have fair to poor activity against anaerobic species. Potency in vitro decreases in the presence of low pH, magnesium ions, or urine but is little affected by different media, increased inoculum, or serum. The effects of the drugs in combination with a beta-lactam or aminoglycoside are often additive, occasionally synergistic, and rarely antagonistic. The agents are orally absorbed, require at most twice-daily dosing, and achieve high concentrations in urine, feces, and kidney and good concentrations in lung, bone, prostate, and other tissues. The drugs are efficacious in treatment of a variety of bacterial infections, including uncomplicated and complicated urinary tract infections, bacterial gastroenteritis, and gonorrhea, and show promise for therapy of prostatitis, respiratory tract infections, osteomyelitis, and cutaneous infections, particularly when caused by aerobic gram-negative bacilli. Fluoroquinolones have also proved to be efficacious for prophylaxis against travelers' diarrhea and infection with gram-negative bacilli in neutropenic patients. The drugs are effective in eliminating carriage of Neisseria meningitidis. Patient tolerability appears acceptable, with gastrointestinal or central nervous system toxicities occurring most commonly, but only rarely necessitating discontinuance of therapy. In 17 of 18 prospective, randomized, double-blind comparisons with another agent or placebo, fluoroquinolones were tolerated as well as or better than the comparison regimen. Bacterial resistance has been uncommonly documented but occurs, most notably with P. aeruginosa and Staphylococcus aureus and occasionally other species for which the therapeutic ratio is less favorable. Fluoroquinolones offer an efficacious, well-tolerated, and cost-effective alternative to parenteral therapies of selected infections.

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Section: Sexually Transmitted Diseasesmentioning

confidence: 94%

Fluoroquinolone antimicrobial agents

1989

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“…Animal studies have suggested that there is excellent penetration of drug into most tissues (5, 18, 30-34, 41, 49, 53), but only limited information on tissue penetration of fleroxacin in humans is available (22,26,41,44,53). Initial clinical experience in the treatment of sexually transmitted diseases, urinary tract infection, skin and soft tissue infections, gastrointestinal infection, and even acute exacerbations of chronic bronchitis has been quite promising, with 74 to 100% bacteriological cure rates and a tolerability comparable to those for other drugs of this class (3,12,27,35,38,42,43,45,47). However, to optimize the clinical use of * Corresponding author.…”

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confidence: 99%

Pharmacokinetics of [18F]fleroxacin in healthy human subjects studied by using positron emission tomography

Fischman

Livni

Babich

et al. 1993

Antimicrob Agents Chemother

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Positron emission tomography (PET) with [18Fjfleroxacin was used to study the pharmacokinetics of fleroxacin, a new broad-spectrum fluoroquinolone, in 12 healthy volunteers (9 men and 3 women). The subjects were infused with a standard therapeutic dose of fleroxacin (400 mg) supplemented with -20 mCi of[18F]fleroxacin. Serial PET images were made and blood samples were collected for 8 h, starting at the initiation of the infusion. The subjects were then treated with unlabeled drug for 3 days (400 mg/day). On the fifth day, infusion of radiolabeled drug, PET imaging, and blood collection were repeated. In most organs, there was rapid accumulation of radiolabeled drug, with stable levels achieved within 1 h after completion of the infusion.Especially high peak concentrations (in micrograms per gram) were achieved in the kidney (>34), liver (>25), lung (>20), myocardium (>19), and spleen (>18). Peak concentrations of drug more than two times the MIC for 90% of Enterobacteriaceae strains tested (>10-fold for most organisms) were achieved in all tissues except the brain and remained above this level for more than 6 to 8 h. The plateau concentrations in tissues (2 to 8 h, in micrograms per gram ± standard error of the mean) of drug were as follows: brain, 0.

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“…The fact that PET measurements yield only total concentrations of drug per gram of tissue and cannot differentiate between intra-and extracel- VOL. 40,1996 PHARMACOKINETICS OF [ 18 F]FLEROXACIN lular drug somewhat limits the conclusions that can be drawn. However, rough relationships between total tissue concentrations and MICs are suggested.…”

Section: Discussionmentioning

confidence: 99%

“…Fleroxacin is a new fluoroquinolone that has been shown to possess a number of desirable characteristics: excellent bioavailability after oral administration, high concentrations in plasma relative to the susceptibilities of relevant pathogens, a long elimination half-life which is consistent with a once-a-day administration schedule, and good tissue penetration (2, 3, 5-9, 11, 19-23, 25-30, 32, 35-39, 43-50). In addition, the initial clinical experience with fleroxacin in the treatment of sexually transmitted diseases, urinary tract infection, skin and soft tissue infection, gastrointestinal infection, and acute bacterial exacerbations of chronic bronchitis has been encouraging (4,10,24,33,34,37,39,40,42).…”

mentioning

confidence: 99%

Pharmacokinetics of [18F]fleroxacin in patients with acute exacerbations of chronic bronchitis and complicated urinary tract infection studied by positron emission tomography

Fischman

Livni

Babich

et al. 1996

Antimicrob Agents Chemother

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The pharmacokinetics of fleroxacin, a new broad-spectrum fluoroquinolone, were measured by positron emission tomography (PET) with [18F]fleroxacin in five patients with acute bacterial exacerbations of chronic bronchitis and in five patients with symptomatic, complicated urinary tract infection. Two studies were performed with each patient, one within 24 h of the initiation and one within 24 h of the completion of a 7-day course of fleroxacin, 400 mg/day. For each study, the patient received an infusion of that day's therapeutic dose of fleroxacin (400 mg) supplemented with approximately 740 MBq of [18F]fleroxacin, and serial PET images and blood samples were collected for 6 to 8 h starting at the initiation of the infusion. Between studies, the drug was administered orally. In all infected tissues, there was rapid accumulation of radiolabeled drug, with stable levels achieved within 1 h after completion of the infusion. In kidneys, accumulation was greater in the presence of active infection (P < 0.01), while in lungs, accumulation was lower (P < 0.02). Infection of the lung or urinary tract had no effect on drug delivery to uninvolved tissues. Also, there was no difference between the results obtained at the beginning and the end of therapy. Overall, peak concentrations of drug many times the MIC at which 90% of the infecting organisms are inhibited (MIC90) were achieved in the kidneys (> 30 micrograms/g), prostate glands (> 11 micrograms/g), and lungs (> 14 micrograms/g). Plateau concentrations (2 to 8 h; given as mean micrograms per gram +/- standard error of the mean) of drug in kidneys (15.11 +/- 0.55), prostate glands (5.08 +/- 0.19), and lungs (5.75 +/- 0.22) were also well above the MIC90 for most relevant pathogens. All patients had a good therapeutic response to fleroxacin.

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Clinical efficacy and tolerance of fleroxacin in patients with urethritis caused by Chlamydia trachomatis

Cited by 17 publications

References 0 publications

Fluoroquinolone antimicrobial agents

Fluoroquinolone antimicrobial agents

Pharmacokinetics of [18F]fleroxacin in healthy human subjects studied by using positron emission tomography

Pharmacokinetics of [18F]fleroxacin in patients with acute exacerbations of chronic bronchitis and complicated urinary tract infection studied by positron emission tomography

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