Pefloxacin in acute exacerbations of chronic bronchitis

Maesen, F. P. V.; Davies, B. I.; Teengs, J. P.

doi:10.1093/jac/16.3.379

Cited by 40 publications

(9 citation statements)

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“…In addition, the mean concentrations in sputum of 2.63 and 1.42 pug/ml at 8 and 16 h after administration, respectively, were sufficiently high to inhibit many respiratory pathogens (4,8,13,21) (14), and other investigators demonstrated its therapeutic success in patients with acutely exacerbated chronic bronchitis (9,12).…”

Section: Resultsmentioning

confidence: 93%

Effective monitoring of concentrations of ofloxacin in saliva of patients with chronic respiratory tract infections

Koizumi

Ohnishi

Takemura

et al. 1994

Antimicrob Agents Chemother

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To ascertain whether monitoring of the concentrations of ofloxacin in saliva during a course of treatment is more suitable and safer than that of its levels in blood, we simultaneously monitored its concentrations in three body fluids (blood, saliva, and expectorated sputum) after a 300-mg administration in 18 patients with chronic respiratory infection. The mean (± standard error of the mean) half-lives derived from the three drug level-time relationships were similar: 6.04 ± 0.58 h for serum, 6.34 ± 0.63 h for sputum, and 6.61 ± 0.65 h for saliva. The mean peak concentration (4.06 to 4.53 ,ug/ml) did not differ at the three sites, but the times taken to reach peak concentration in saliva and sputum (3.17 ± 0.46 h) were significantly longer than that in serum (2.22 ± 0.28 h). The ratios of the concentrations in saliva and sputum to the concentration in serum increased during the first 2 h and reached 1.0 between 2 and 8 h after administration. They rose above 1.0 16 h after administration: 1.14 ± 0.11 for saliva and 1.19 ± 0.10 for sputum. The concentration-time relationship for sputum corresponded closely with the concentration-time relationship for saliva, and an overall significant correlation between the concentrations in sputum and saliva was obtained (P < 0.01). These results suggest that monitoring concentrations in saliva may be more valid, as well as less invasive, than monitoring of the levels in blood for ensuring that the drug concentration reaches its therapeutic level in bronchial secretions.Ofloxacin (OFLX) is a fluoroquinolone antimicrobial agent having a broad spectrum of activity against gram-negative and -positive bacteria and some anaerobes in vitro (4, 13). Grassi reported the successful use of OFLX against respiratory tract infections in a multicenter study (6), and many other clinical investigations have proved its effectiveness in the treatment of various systemic bacterial infections (8,14,21).Ofloxacin is widely distributed in the body and penetrates thoroughly into extravascular fluids such as bronchial secretions (8, 10, 20, 21). We consider that its relatively high concentration in such secretions is especially important in chronic infections, since it maintains levels higher than the MICs for various respiratory pathogens. In chronic airway infections, it is necessary to maintain the concentration of an antibiotic in bronchial secretions at a level equal to or higher than the concentration in blood because the bacteria are usually present in and around the airways. On the other hand, since OFLX is mostly eliminated via the kidney and is excreted unchanged in the urine (3, 11), careful regulation of the dosage during chronic administration in patients with impaired renal function has been advised (3, 5).In the present study, we performed simultaneous monitoring of OFLX concentrations in three fluids, blood, expectorated sputum, and saliva, in patients with chronic respiratory infections and various degrees of renal impairment. Our purpose was to determine whether the measurement of ...

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Section: Resultsmentioning

confidence: 93%

Effective monitoring of concentrations of ofloxacin in saliva of patients with chronic respiratory tract infections

Koizumi

Ohnishi

Takemura

et al. 1994

Antimicrob Agents Chemother

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“…Concentrations in bronchial secretions were 20 to 100% of peak serum concentrations for ciprofloxacin (45, 49), ofloxacin (753), pefloxacin (476), and enoxacin (145,237,835), while concentrations in lung tissue were higher than those in serum, in the 1.6-to 3.5-fold range for ciprofloxacin (368,673), ofloxacin (834), enoxacin (835), and, for bronchial mucosa, fleroxacin (852).…”

Section: Pharmacokinetic Properties In Healthy Personsmentioning

confidence: 94%

“…Overall, where enumerated in nine studies (213, 233, 282, 349, 359, 608,610,644,716), pathogens developed ciprofloxacin resistance in 17 of 302 patients (5.6%). Pefloxacin resistance has also been reported during treatment of P. aeruginosa infections in the respiratory tract (476) and other sites (861). P. aeruginosa has been the predominant organism developing quinolone resistance in these studies, but resistant Streptococcus pneumoniae (359), P. maltophilia, H. parainfluenzae, and Serratia marcescens (610) have also been reported.…”

Section: Development Of Microbial Resistance In Clinical Studiesmentioning

confidence: 99%

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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“…Also it is cost-effective to control an occurrence of exacerbation because the number of times of admission and parenteral therapy can be decreased (Sato et al 1991). In recent years, new-quinolones have been reported to be effective in the treatment of acute exacerbations of chronic RTI's (Maesen et al 1985(Maesen et al ,1986; Hoogkamp-Korstanje and Klein 1986; Davies and Maesen 1987; Grassi et al 1987). Oral ofloxacin in this study was used not for the treatment, but for the control or prophylaxis of acute exacerbations of chronic RTI's.…”

Section: Discussionmentioning

confidence: 99%

Daily Single-Dose Regimen and Alternate-Two-Week Triple-Dose/Day Regimen of Oral Ofloxacin for the Prophylaxis and Control of Exacerbations of Chronic Respiratory Tract Infections.

Watanabe

Ōizumi

Motomiya

et al. 1995

Tohoku J. Exp. Med.

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, 1995, 176 (1), 25-33 Two different oral ofloxacin regimens, a daily single-dose regimen with 200 mg (Regimen I) and an every-two-week multidose regimen with 3 x 200 mg/day (Regimen II) was compared as to the efficacy in controlling repeated acute exacerbations of chronic respiratory tract infections. Fifty-eight patients consisting of 19 patients each of bronchiectasis and pulmonary emphysema, 10 patients of chronic bronchitis, 5 patients of old pulmonary tuberculosis, 4 patients of diffuse panbronchiolitis and 1 patient of multiple pulmonary bullae were evaluated: 32 patients in Regimen I and 26 patients in Regimen II. The corrected mean incidence of exacerbations per case decreased from pre-study 2.47 to intra-study 0.59 in Regimen I, and from pre-study 2.66 to intra-study 0.95 in Regimen II, respectively, with a statistically significant difference (p <0.05, respectively). Only one of 12 persistent isolates of Pseudomonas aeruginosa acquired a certain degree of resistance to ofloxacin. Adverse reactions were found in six of 66 patients. We conclude that long-term administration of an new-quinolone, especially a daily single-dose regimen with ofloxacin, is useful to control acute exacerbations of chronic repiratory tract infections.

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Pefloxacin in acute exacerbations of chronic bronchitis

Cited by 40 publications

References 0 publications

Effective monitoring of concentrations of ofloxacin in saliva of patients with chronic respiratory tract infections

Effective monitoring of concentrations of ofloxacin in saliva of patients with chronic respiratory tract infections

Fluoroquinolone antimicrobial agents

Daily Single-Dose Regimen and Alternate-Two-Week Triple-Dose/Day Regimen of Oral Ofloxacin for the Prophylaxis and Control of Exacerbations of Chronic Respiratory Tract Infections.

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