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PubMed1998

In vitro activity of quinupristin/dalfopristin and newer quinolones combined with gentamicin against resistant isolates of Enterococcus faecalis and Enterococcus faecium.

In a study designed to obtain data on compounds active against enterococci, the minimum inhibitory concentrations (MICs) of quinupristin/dalfopristin (RP 59500) and the novel quinolones DU-6859a, trovafloxacin, levofloxacin, and sparfloxacin were determined for 122 Enterococcus faecalis and seven Enterococcus faecium isolates. In addition, 15 Enterococcus faecalis isolates resistant to gentamicin, DU-6859a, and trovafloxacin were exposed over time to combinations of DU-6859a plus gentamicin and trovafloxacin plus gentamicin. DU-6859a and trovafloxacin were found to be the most active compounds against Enterococcus faecalis and DU-6859a and RP 59500 against Enterococcus faecium. Synergy between either DU-6859a or trovafloxacin and gentamicin was observed with 27 to 35% of the isolates. It is concluded that DU-6859a and trovafloxacin are very potent against enterococci, especially when combined with gentamicin.

Anti-Bacterial Agents↗
PubMed1991

Antistaphylococcal activity of the fluoroquinolones CI-960, PD 131628, sparfloxacin, ofloxacin and ciprofloxacin.

Five fluoroquinolones were tested against 300 staphylococci from a wide variety of US medical centers including 150 strains resistant to penicillinase-resistant penicillins (PRP-resistant). Ten ciprofloxacin-resistant strains of PRP-resistant Staphylococcus aureus were relatively resistant to the other fluoroquinolones, but the remaining 290 isolates were susceptible to all five drugs at established or anticipated breakpoint concentrations. The relative potency of the study drugs could be ranked as follows: CI-960 greater than PD 131628 greater than sparfloxacin greater than ciprofloxacin greater than ofloxacin. All five drugs were bactericidal against PRP-resistant and PRP-susceptible staphylococci.

Anti-Infective Agents↗
PubMed1990

Comparative in vitro activity of the new fluoroquinolone BMY-40062.

The results are presented of comparative in vitro susceptibility testing of BMY-40062, a new fluorinated quinolone which contains a tetrabutyl moiety at N-1 and a piperazinyl group at C-7. BMY-40062 inhibited 90% of Enterobacteriaceae strains at less than 0.5 microgram/ml, being either equal in activity to ciprofloxacin or two- to four-fold less active, depending upon the species. BMY-40062 was as active as ciprofloxacin against Pseudomonas aeruginosa (MIC90 0.5 micrograms/ml) and inhibited most other strains of Pseudomonas species at less than 1 microgram/ml. It was more active than ciprofloxacin or ofloxacin against hemolytic streptococci and Streptococcus pneumoniae, 90% of strains being inhibited at less than 0.5 micrograms/ml. MICs increased in the presence of 9 mM Mg2+ and at pH 5.5. The frequency of spontaneous mutation was low for Enterobacteriaceae, Pseudomonas aeruginosa and Staphylococcus aureus (10(-10), but repeated exposure to BMY-40062 caused selection of resistant isolates. Clinical isolates of Pseudomonas aeruginosa resistant to ciprofloxacin and ofloxacin were resistant to BMY-40062.

Anti-Infective Agents↗
PubMed1992

Susceptibility of anaerobic bacteria to PD 131628.

The in vitro activity of PD 131628 against anaerobic cocci, Propionibacterium acnes, Clostridium perfringens, Clostridium difficile, Bacteroides fragilis, Bacteroides spp. and fusobacteria was determined by the agar dilution method. This activity was compared with that of ciprofloxacin, piperacillin, cefoxitin, imipenem, clindamycin, metronidazole and chloramphenicol. PD 131628, imipenem, clindamycin, metronidazole and chloramphenicol were the most active agents tested.

Anti-Infective Agents↗
PubMed1990

In vitro activity of tosufloxacin (A-60969) and clarithromycin (A-56268, TE-031) against resistant Haemophilus influenzae, Streptococcus pneumoniae and Branhamella catarrhalis isolates.

The activity of tosufloxacin (A-60969), a new oral quinolone, and clarithromycin (A-56268, TE-031), a new oral macrolide, was compared in vitro to that of other oral quinolones and beta-lactam antimicrobial agents against clinical isolates of ampicillin and/or chloramphenicol resistant Haemophilus influenzae, penicillin resistant Streptococcus pneumoniae and beta-lactamase producing Branhamella catarrhalis. Results were compared to those for sensitive isolates. Tosufloxacin was the most active compound against Haemophilus influenzae and was more active than ciprofloxacin or ofloxacin against all strains of Streptococcus pneumoniae. Tosufloxacin was also more active than any of the beta-lactam drugs tested against penicillin resistant or relatively penicillin resistant isolates. Clarithromycin was the most active compound tested against both penicillin sensitive and penicillin resistant Streptococcus pneumoniae, and was as active as ciprofloxacin against Branhamella catarrhalis. In view of the favourable in vitro activity against common bacterial respiratory pathogens, tosufloxacin should be considered for clinical trials in adults with respiratory tract infections, while clarithromycin might be useful in treatment of infection with these organisms in all age groups.

4-Quinolones↗
PubMed1986

The effect of the 4-quinolone enoxacin on plasma theophylline concentrations.

In patients treated concomitantly with theophylline and enoxacin, a broad spectrum antibacterial agent for oral administration, unexpectedly high plasma theophylline concentrations were observed. In six patients receiving intravenous aminophylline under controlled conditions, enoxacin was started in a daily dose of 800 or 1200 mg. Plasma theophylline concentrations increased from 8.4 +/- 2.4 mg/l to 15.0 +/- 5.1 mg/l at day 3 of co-administration. Total body clearance of theophylline decreased significantly, whereas renal clearance and protein binding did not change. When enoxacin, 800 mg daily, was administered to seven patients with a stable chronic obstructive pulmonary disease, who were on long-term theophylline treatment a significant increase in plasma theophylline concentrations occurred as well: elimination half-life was prolonged. It is concluded that the rise of plasma theophylline concentrations is caused by a reduced metabolic clearance of theophylline. If concomitant use of both drugs is necessary, monitoring of plasma theophylline concentration and adjustment of the theophylline dose is recommended, to avoid toxicity.

Adult↗
PubMed1984

A laboratory assessment of ciprofloxacin and comparable antimicrobial agents.

The in vitro activity of ciprofloxacin against a wide range of bacterial isolates was assessed in comparison with norfloxacin, enoxacin, co-trimoxazole and penicillin (or ampicillin) where appropriate. Minimal inhibitory concentrations (MICs) indicated that ciprofloxacin was highly active against gram-negative bacilli of the Enterobacteriaceae and Pseudomonas groups, notably against strains resistant to gentamicin. Similarly, Staphylococcus aureus (including methicillin-resistant strains) and Haemophilus influenzae were susceptible, regardless of penicillinase production. Norfloxacin and enoxacin were less active than ciprofloxacin against the majority of species tested, although enoxacin blood levels were generally higher. Most co-trimoxazole-resistant strains were susceptible to the quinoline group of drugs.

Anti-Bacterial Agents↗
PubMed1987

Effect of enoxacin on colonic microflora of healthy volunteers.

Ten healthy volunteers received 400 mg enoxacin orally twice daily for seven days. Fecal specimens were collected at 0, 2, 4, 7, 9, 11, 16 and 21 days to study the effect of enoxacin on the normal colonic microflora. On the seventh day the fecal mean concentration of enoxacin was 348 mg/kg feces. Whereas enterobacteria were strongly suppressed during the administration of enoxacin, the gram-positive and anaerobic microflora was not significantly altered. Two weeks after enoxacin was discontinued, the colonic microflora had returned to normal.

Adult↗
PubMed1987

Comparative in vitro activity of amifloxacin and five other fluoroquinolone antimicrobial agents and preliminary criteria for the disk susceptibility test.

Amifloxacin is a fluoroquinolone with a spectrum of activity similar to that of ofloxacin, pefloxacin, enoxacin, norfloxacin and ciprofloxacin. For disk susceptibility tests, 10 micrograms amifloxacin disks are recommended with zone size interpretive standards of less than or equal to 16 mm and greater than or equal to 20 mm for the resistant and susceptible categories respectively.

Anti-Bacterial Agents↗
PubMed1987

Quinolones in the treatment of gonorrhoea and Chlamydia trachomatis infections.

The results of two therapeutic trials in female patients with uncomplicated urogenital gonorrhoea (A) and in male patients with uncomplicated urethral gonorrhoea (B) treated with either 200 mg and 400 mg enoxacin orally, of one therapeutic trial in male patients with uncomplicated urogenital gonorrhoea treated with either 250 mg or 500 mg ciprofloxacin orally (C) and of one therapeutic trial in male patients with non-gonococcal urethritis (NGU) treated with ciprofloxacin 1 g daily during seven days (D) are presented and compared with the results of other investigators. The cure rate in study A was 100% (n = 40) in the 400 mg group and 95.7% (n = 46) in the 200 mg group. The cure rate in study B was 92% (n = 78) in the 400 mg group and 90% (n = 77) in the 200 mg group. In both studies no antichlamydial effect of enoxacin was observed. The cure rates in study C were 100% with 250 and 500 mg. An antichlamydial effect seemed to be present. In studies A, B and C side effects were minor and rare and were mainly nausea and headache. In study D (100 patients suffering from NGU) disappearance of Chlamydia trachomatis and Ureaplasma urealyticum one day after the end of treatment was observed in 29 of 32 (91%) and 28 of 32 (88%) cases, respectively. Pyuria disappeared in 44% and 74% of the patients showed clinical cure. However, two weeks after the end of treatment Chlamydia trachomatis and Ureaplasma urealyticum were observed in respectively six and eight cases. In 30% pyuria was still absent. Side effects were only minor.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1987

The use of fluoroquinolones in chronic otitis suppurativa.

The present review covers fluoroquinolone usage in chronic otitis suppurativa (COS) in case of chronic otitis media, cholesteatoma, radical mastoid cavity infection and chronic or relapsing otitis externa. A total of six publications were included in the final evaluation. Enoxacin was effective in 35%; ciprofloxacin (five publications) was used in 82 patients with 67% effectivity in otitis externa and otitis media and 61% effectivity in radical mastoid cavity infection. No serious adverse reactions were reported. The promising efficacy of otitis media and otitis externa and safety profile needs further confirmation in double blind prospective clinical studies, that will provide a firm basis for changing the current treatment schedules of COS.

Cholesteatoma↗
PubMed1986

Treatment of uncomplicated urogenital gonorrhoea in women with a single dose of enoxacin.

One hundred and twenty-three female patients suffering from uncomplicated urogenital gonorrhoea were treated in a double blind randomised trial with either 200 mg enoxacin (one capsule of 200 mg, one of placebo) or 400 mg enoxacin (two capsules of 200 mg). The cure rate in the 46 evaluable patients in the 400 mg group was 100%, and in the 40 evaluable patients in the 200 mg group 98.7%. Minor side effects such as nausea, headache and skin rash occurred in three of 109 evaluable patients (2.8%). The minimum inhibitory concentration of enoxacin for the Neisseria gonorrhoeae strains isolated varied between 0.03 and 0.12 mcg/ml. Enoxacin would seem to be a very effective drug in the treatment of uncomplicated urogenital gonorrhoea in female patients.

Administration, Oral↗
PubMed1992

Susceptibility of anaerobic bacteria to tosufloxacin.

The in vitro activity of tosufloxacin against anaerobic cocci, Propionibacterium acnes, Clostridium perfringens, Clostridium difficile, Bacteroides fragilis, Bacteroides spp. and fusobacteria was determined by the agar dilution method. This activity was compared with that of ciprofloxacin, piperacillin, cefoxitin, imipenem, clindamycin, metronidazole and chloramphenicol. Tosufloxacin, imipenem, clindamycin, metronidazole and chloramphenicol were the most active agents tested. Tosufloxacin has an antibacterial activity that warrants investigation in clinical trials.

4-Quinolones↗
PubMed1985

In vitro activity of enoxacin compared with norfloxacin and amikacin.

The in vitro activity of enoxacin was tested against 1000 clinical isolates of gram-positive and gram-negative microorganisms and compared with that of norfloxacin and amikacin. The MIC90 of enoxacin was 1 mg/l for Enterobacteriaceae, 2.6 mg/l for Pseudomonas aeruginosa and 6.2 mg/l or Staphylococcus aureus. The inoculum effect was minimal. The MICs and MBCs for Pseudomonas aeruginosa strains were significantly affected by the addition of calcium and magnesium ions. Synergy was occasionally observed between enoxacin and the antibiotics tested; antagonism was rare.

Amikacin↗
PubMed1999

Can quinolones cause hemorrhagic colitis of late onset? Report of three cases.

PURPOSE: This study was undertaken to demonstrate that quinolones may cause acute colitis resembling penicillin-induced hemorrhagic colitis. METHODS: We reviewed the medical records of patients with acute colitis in our institutes. Twenty-eight patients with acute hemorrhagic colitis in which no pathogenic microorganisms were identified were the subjects of this study. Pseudomembranous colitis caused by Clostridium difficile was excluded. Ulcerative colitis, Crohn's disease, and radiation proctocolitis were also excluded. RESULTS: Among these patients, 25 had a history of recent administration of penicillin derivatives. The remaining three patients had never been given any penicillin derivatives, but had ingested quinolones approximately four weeks before the developing colitis had been identified. Klebsiella oxytoca was also isolated in these three patients. CONCLUSIONS: Quinolones may cause acute hemorrhagic colitis. The time interval from antibiotic ingestion to onset of the condition may be much longer in quinolones than in penicillin derivatives.

Acute Disease↗