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At least 685 records · Page 38Linked to original sources
PubMed1986

[Results of treatment of bacterial inflammation of the skin with enoxacin].

In a microbiologically controlled, open study the 4-quinolone derivative enoxacin was tested in 51 patients suffering from infectious dermatoses. Clinical cure or improvement was observed in 91% of the patients, microbiological cure occurred in 65%. According to the results of our trial enoxacin is recommended as a therapeutic alternative, especially for the treatment of dermatitis caused by gram-negative bacilli.

Adolescent↗
PubMed1996

Activity of trovafloxacin against blood isolates of Streptococcus pneumoniae in Sweden.

The in vitro activity of the fluoroquinolone trovafloxacin (CP-99,219) against 257 blood isolates of Streptococcus pneumoniae obtained from Swedish hospitals was compared with those of commonly prescribed oral antibiotics and also with those of ciprofloxacin and ofloxacin against a collection of strains resistant (n = 6) or intermediately resistant (n = 22) to penicillin (Pc-R). The MICs of trovafloxacin for Pc-R strains of pneumococci ranged from 0.032 to 0.25 mg/l. No difference was seen between the clinical isolates and the Pc-R strains (MIC50 = 0.064 mg/l and MIC90 = 0.125 mg/l for both collections). For the Pc-R strains, the MIC50 and MIC90 values of ciprofloxacin were 0.5 and 1 mg/l, and those of ofloxacin 2 and 4 mg/l. The incidence of resistance in the two collections (clinical isolates/Pc-R strains) was 3%/39% for tetracycline, 1%/18% for macrolides, and 3%/57% for trimethoprim/sulfamethoxazole. The results of the current study suggest that the clinical efficacy of trovafloxacin in the treatment of pneumococcal infections should be investigated.

Anti-Infective Agents↗
PubMed1996

Methods of measuring susceptibility of anaerobic bacteria to trovafloxacin, including quality control parameters.

Three methods approved by the National Committee for Clinical Laboratory Standards for testing the susceptibility of anaerobic bacteria were used to evaluate the fluoroquinolone, trovafloxacin. The methods gave essentially comparable results with 126 anaerobes and with three quality control strains. A collaborative study defined the quality control range for trovafloxacin MICs. Trovafloxacin had good in vitro activity against the more common anaerobes (MIC 90 < = or 2.0 micrograms/ml).

Anti-Infective Agents↗
PubMed1996

In vitro activity and selection of disk content for disk diffusion susceptibility tests with trovafloxacin.

The activity of the new fluoroquinolone trovafloxacin (CP-99,219) was compared with that of ciprofloxacin and ofloxacin against 517 bacterial isolates representing 50 different species. Against members of the family Enterobacteriaceae, all three drugs showed good in vitro activity. Against most anaerobic bacteria, Staphylococcus, Streptococcus, and Enterococcus species, trovafloxacin was four- to sixteenfold more active than ciprofloxacin. For disk diffusion testing, 10 micrograms trovafloxacin disks gave satisfactory results. Tentative criteria are proposed for use during clinical studies.

Anti-Infective Agents↗
PubMed1996

In vitro activity of trovafloxacin versus ciprofloxacin against clinical isolates.

The comparative in vitro activity of trovafloxacin (CP 99,219), a new fluoroquinolone, was evaluated against 511 clinical isolates. MICs of trovafloxacin were fourfold higher than those of ciprofloxacin for 184 Enterobacteriaceae and 110 non-fermentative gram-negative bacilli. However, trovafloxacin was 16-fold more active than ciprofloxacin against 162 gram-positive staphylococci, pneumococci, streptococci, and enterococci, and two- to fourfold more active against Haemophilus influenzae and Moraxella catarrhalis. MICs of trovafloxacin were correspondingly higher for strains with acquired resistance to ciprofloxacin.

Anti-Infective Agents↗
PubMed1996

In vitro susceptibility of pneumococci to trovafloxacin, penicillin G, and other antimicrobial agents in the Czech Republic and Slovakia.

The in vitro activity of the new naphthyridone trovafloxacin (CP 99,219) was compared with those of penicillin G and six other agents (cefpodoxime, erythromycin, azithromycin, clindamycin, ciprofloxacin, and sparfloxacin) against 316 penicillin-susceptible and -resistant pneumococci isolated in the former Czechoslovakia. Trovafloxacin was very active against strains of Streptococcus pneumoniae (MIC50 and MIC90 0.25 microgram/ml). Ciprofloxacin was less active (MIC50 1.0 microgram/ml, MIC90 2.0 micrograms/ml), and MICs of sparfloxacin were between those of trovafloxacin and ciprofloxacin (MIC50 and MIC90 both 0.5 microgram/ml). MICs of cefpodoxime, erythromycin, azithromycin, and clindamycin were higher for strains intermediately resistant or resistant to penicillin than for penicillin-susceptible strains.

Anti-Infective Agents↗
PubMed1996

In vitro activity of trovafloxacin in combination with ceftazidime, meropenem, and amikacin.

The in vitro activity of trovafloxacin alone and in combination with ceftazidime, meropenem, and amikacin was studied by determining the minimal inhibitory concentrations (MICs) for 111 gram-negative and 71 gram-positive bacteria. In addition, the synergy of these combinations against 46 strains of gram-negative and gram-positive organisms was studied by checkerboard titration and time-kill kinetics. Trovafloxacin exhibited excellent in vitro activity against all strains tested. Synergism was observed in 17% of the gram-negative strains and in 32% of the gram-positive strains. No antagonism was observed with any of the combinations tested.

Amikacin↗
PubMed1998

Bacteriological activity of trovafloxacin, a new quinolone, against respiratory tract pathogens.

The use of established fluoroquinolones, such as ciprofloxacin and ofloxacin, as empirical therapy for the treatment of moderate-to-severe respiratory tract infections is limited by their poor activity against gram-positive and atypical pathogens. Data from in vitro susceptibility studies and in vivo animal protection models suggest that the new fluoroquinolone, trovafloxacin, compared with ciprofloxacin and ofloxacin offers equivalent activity against gram-negative pathogens and improved activity against gram-positive pathogens. In particular, susceptibility data indicate that trovafloxacin is at least 16-fold more potent than either ciprofloxacin or ofloxacin against penicillin-susceptible and penicillin-resistant strains of Streptococcus pneumoniae. Other susceptible pathogens include Streptococcus pyogenes, vancomycin-susceptible Enterococcus faecalis and the atypical respiratory pathogens Legionella pneumophila, Mycoplasma pneumoniae and Chlamydia pneumoniae. In vivo studies involving models of protection against acute systemic infection and pneumococcal pneumonia in mice, and Legionnaires' disease in guinea pigs, indicate that the antibacterial spectrum observed for trovafloxacin in vitro extends to the in vivo setting. Together, these findings suggest that trovafloxacin may offer clinical efficacy against respiratory pathogens superior to that of ciprofloxacin and of ofloxacin, and may find a useful role as empiric therapy in both the community and hospital setting.

Animals↗
PubMed1998

Susceptibility of European respiratory tract isolates to trovafloxacin, ciprofloxacin, clarithromycin, azithromycin and ampicillin.

As part of the Artemis project, 11500 isolates (3000 from patients with respiratory tract infections) were collected throughout six European countries between 1994 and 1996. Twenty-seven hospitals or laboratories participated in this first phase of the study. The activities of three classes of antimicrobial agents (fluoroquinolones, beta-lactam agents, macrolides) are presented for the six most frequently isolated pathogens (Streptococcus pneumoniae, Staphylococcus aureus, Haemophilus influenzae, Moraxella catarrhalis, Pseudomonas aeruginosa, Klebsiella pneumoniae). Overall, trovafloxacin and ciprofloxacin activities were similar for Haemophilus influenzae, Moraxella catarrhalis and Klebsiella pneumoniae isolates. Of the Streptococcus pneumoniae isolates, 6% were resistant to penicillin. Trovafloxacin had the highest activity against the Streptococcus pneumoniae isolates, with a minimum inhibitory concentration of 0.25 mg/l for 90% of isolates (MIC90); all strains tested were susceptible to trovafloxacin. The MIC90 of ciprofloxacin for Streptococcus pneumoniae was 3 mg/l, and overall 52% of the strains were susceptible; 9% were resistant. Azithromycin and clarithromycin exhibited similar activity against all collected pathogens, except Haemophilus influenzae. All strains of Haemophilus influenzae were susceptible to azithromycin compared with 79% for clarithromycin, with respective MIC90s of 2 and 16 mg/l. The data presented demonstrate differences in the susceptibility patterns of six major respiratory tract pathogens in Europe.

Ampicillin↗
PubMed1998

Hepatobiliary elimination of trovafloxacin and metabolites following single oral doses in healthy volunteers.

Trovafloxacin, a fluoronaphthyridone derivative related to fluoroquinolones, has significant activity against gram-negative and gram-positive pathogens, including penicillin-resistant Streptococcus pneumoniae, anaerobes and atypical organisms, good tissue penetration and a long elimination half-life. Following oral administration, less than 10% of the dose is renally eliminated as unchanged drug. Hepatobiliary elimination of trovafloxacin was examined by comparing the time course and bile and serum concentrations of trovafloxacin and its metabolites following oral administration to three patients with in-dwelling nasobiliary catheters or T-tubes. Following a single 200 mg oral dose, the mean maximum plasma trovafloxacin concentration was 2.0+/-0.4 mg/l, the area under the concentration-time curve 22.0+/-5.5 mg x h/l and the elimination half-life 8.5 h. Values in bile for the same subjects were 27.8+/-9.6 mg/l, 327.7+/-142.9 mg x h/l and 10.7 h. Corresponding values for the N-acetyl metabolite in bile were 3.8+/-3.4 mg/l, 35.3+/-29.8 mg x h/l and 8.3 h. The mean bile : serum ratio of trovafloxacin was 14:9 and consistent with biliary elimination. Serum concentrations of trovafloxacin in this study were similar to those reported in healthy volunteers. Bile concentrations of trovafloxacin substantially exceeded those of the N-acetyl metabolite, suggesting efficient clearance of the metabolite or that hepatic metabolism of trovafloxacin is not extensive.

Administration, Oral↗
PubMed1998

Single- and multiple-dose administration, dosing regimens, and pharmacokinetics of trovafloxacin and alatrofloxacin in humans.

A simplified dosing algorithm for trovafloxacin was evaluated following a single-dose infusion of alatrofloxacin at trovafloxacin equivalent doses of 30, 100, 200, 300 and 400 mg (57 subjects), and multiple doses of 200, 300 and 400 mg (30 subjects). Maximum serum concentration and area under the concentration-time curve for trovafloxacin increased with dose. Trovafloxacin clearance (82-85 ml x h/kg) and volume of distribution (1.3-1.6 l/kg) were independent of dose. Infusion of alatrofloxacin at a trovafloxacin equivalent dose of 300 mg at 1, 2 or 3 mg/ml over 1 h did not alter the pharmacokinetics of trovafloxacin. A plot of the weight-adjusted dose of trovafloxacin in individual subjects against the maximum serum concentration following single and multiple dosing, indicated that the maximum serum concentration increased 1 microg/ml for each 1 mg/kg of trovafloxacin administered. Thus, a prior knowledge of the desired serum concentration will permit appropriate dosing without the use of complex nomograms in patients with normal hepatic function.

Administration, Oral↗
PubMed1998

An open, controlled, crossover study on the effects of cimetidine on the steady-state pharmacokinetics of trovafloxacin.

Twelve healthy male volunteers participated in this open, randomized, placebo-controlled, two-way crossover study to investigate the effects of cimetidine on the steady-state pharmacokinetics of oral trovafloxacin. Volunteers were randomized to receive either 400 mg cimetidine twice daily or placebo for 5 days. From day 3-5, volunteers received 200 mg trovafloxacin once daily in addition to either cimetidine or placebo. After a minimum 7-day washout period, the study was repeated: those volunteers who received placebo during the first study period were administered cimetidine, and vice versa. The maximum observed serum trovafloxacin concentration, the area under the concentration-time curve of trovafloxacin within the dosing interval of 24 h and the earliest time to the maximum serum concentration for trovafloxacin in volunteers receiving concomitant cimetidine were 2.4 microg/ml. 27.8 microg x h/ml and 1.4 h, respectively, compared with 2.5 microg/ml, 27.1 microg x h/ml and 1.5 h, respectively, in volunteers receiving concomitant placebo. Thus. multiple dosing with cimetidine had no significant effect on the absorption or disposition of trovafloxacin at steady state. Co-administration of cimetidine and trovafloxacin was also well tolerated and without serious adverse effects.

Administration, Oral↗
PubMed1998

Trovafloxacin versus amoxicillin/clavulanic acid in the treatment of acute exacerbations of chronic obstructive bronchitis.

Treatments with once-daily trovafloxacin (200 or 100 mg) and amoxicillin/clavulanic acid (500/125 mg three times daily) were compared in adults with acute exacerbations of chronic obstructive bronchitis. At end of treatment, 95% (113/119) of clinically evaluable patients receiving trovafloxacin 200 mg, 98% (113/115) of patients treated with trovafloxacin 100 mg and 97% (113/117) of patients receiving amoxicillin/clavulanic acid were cured or improved. At study end, 91%, 87% and 88%, respectively, were cured or improved. At end of treatment, trovafloxacin 200 mg eradicated Haemophilus influenzae in 97% of patients, Streptococcus pneumoniae in 90% and Chlamydia pneumoniae in 100%. The respective eradication rates for trovafloxacin 100 mg were 84%, 100% and 100%; those for amoxicillin/clavulanic acid were 92%, 100% and 100%. At study end, trovafloxacin 200 mg totally eradicated all three pathogens. Trovafloxacin 100 mg eradicated Haemophilus influenzae in 91% of patients, Streptococcus pneumoniae in 100% and Chlamydia pneumoniae in 80%. Respective eradication rates for amoxicillin/clavulanic acid were 78%, 100% and 80%. Only 7% (10/144) of patients receiving trovafloxacin 200 mg reported treatment-related adverse events, as did 7% (10/135) of patients given trovafloxacin 100 mg and 12% (17/140) of patients given amoxicillin/clavulanic acid.

Acute Disease↗
PubMed1998

Treatment of acute exacerbations of chronic bronchitis: comparison of trovafloxacin and amoxicillin in a multicentre, double-blind, double-dummy study. Trovafloxacin Bronchitis Study Group.

The efficacy and safety of trovafloxacin and amoxicillin were compared in a double-blind, double-dummy multicentre trial involving 412 patients (> or = 40 years of age) with acute exacerbations of chronic bronchitis (AECBs). Patients were randomized to 5 days' oral treatment with 200 or 100 mg trovafloxacin administered once daily, or 500 mg amoxicillin given three times daily. Overall clinical efficacy at the end of therapy was similar in each treatment group, with clinical success (cure+improvement) achieved in 88% and 91% of clinically evaluable patients receiving trovafloxacin 200 mg and 100 mg, respectively, and in 89% of amoxicillin-treated patients. Corresponding rates at follow-up were 77%, 85% and 79%, respectively. Similar responses were noted at the end of treatment and end of study in the intent-to-treat patients. Although all three treatments produced similar bacteriological efficacy, there was a trend towards higher eradication rates for Haemophilus influenzae among patients (both clinically evaluable and intent-to-treat populations) treated with trovafloxacin 200 mg compared with those treated with amoxicillin. Both drugs were well tolerated, with treatment-related adverse events, of which headache and gastrointestinal disturbances were the most common, occurring in 12% and 6% of patients in the trovafloxacin 200 mg and 100 mg groups, respectively, and in 9% of amoxicillin-treated patients.

Acute Disease↗
PubMed1998

Trovafloxacin versus high-dose amoxicillin (1 g three times daily) in the treatment of community-acquired bacterial pneumonia.

Once-daily trovafloxacin 200 mg was compared with high-dose amoxicillin, 1 g three times daily, given for 7 to 10 days. At end of treatment (day 10), the response was clinically successful (cure + improvement) in 93% of 152 clinically evaluable trovafloxacin patients and in 89% of 160 amoxicillin patients. At study end (day 35), respective rates were 91% and 81% (95% confidence interval: 1.6, 17.6; P=0.01). In evaluable patients with positive baseline radiographs, 93% of trovafloxacin and 88% of amoxicillin patients demonstrated radiological resolution at end of treatment. Streptococcus pneumoniae and Haemophilus influenzae eradication rates were comparable at end of treatment in both treatment groups, but at study end Streptococcus pneumoniae eradication rates were higher in trovafloxacin patients (100% vs 81%). At study end, all four trovafloxacin patients with baseline penicillin-resistant Streptococcus pneumoniae were clinically cured with pathogen eradication, whereas two of five amoxicillin patients with baseline penicillin-resistant Streptococcus pneumoniae were clinical failures with pathogen persistence. For patients in whom no pathogen was identified, trovafloxacin was significantly more effective at end of treatment (P=0.096) and study end (P=0.013). Treatment-related adverse events were comparable; the most common were headache, vomiting and dizziness in trovafloxacin patients, and diarrhoea. headache and abdominal pain in amoxicillin patients.

Adolescent↗
PubMed1998

Safety of trovafloxacin in treatment of lower respiratory tract infections.

Safety and toleration of oral trovafloxacin has been assessed in Phase III trials in patients with acute lower respiratory tract infections. Patients were treated orally with either trovafloxacin 100 or 200 mg (n=881) or a comparator (500 or 1000 mg amoxicillin, or 625 mg amoxicillin/clavulanic acid; n = 593). Adverse events were recorded in 112 (12.7%) trovafloxacin- and 74 (12.5%) comparator-treated patients. Frequency of effects on the autonomic nervous, musculoskeletal, respiratory, special senses, urinary and reproductive systems was <1%. Photosensitivity reactions were not reported in trovafloxacin-treated patients. Central or peripheral nervous system adverse effects (headache and dizziness) were slightly more common in trovafloxacin-treated patients (4.4% vs 1.9%). Patients treated with comparators experienced gastrointestinal events more frequently (6.1% vs 8.3%). Comparable incidences of adverse events were reported in patients > or = 65-years-old. Most events were mild to moderate in severity. Treatment was discontinued because of an adverse event in 18 (2%) trovafloxacin- and four (0.7%) comparator-treated patients. Despite the high prevalence of risk factors, serious adverse events were rare and the mortality rate over the 35-day study period was low: trovafloxacin 0.8%, comparator agents 1.5%. Laboratory test abnormalities were recorded in less than 1% of patients in either treatment group.

Acute Disease↗