Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0023241 (Legionella)
 6,990 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The efficacy and safety of grepafloxacin in treating patients with community-acquired pneumonia (CAP) was assessed in an open-label, noncomparative study. Patients (N = 273) received grepafloxacin 600 mg QD for 10 days. A total of 237 patients (87%) completed the study. In assessable patients, the clinical success rate at follow-up (4 to 6 weeks after the last dose) was 89% (211/238 patients). In microbiologically assessable patients, the eradication rate at follow-up was 95% (86/91 isolates). Grepafloxacin was highly effective in the treatment of bacterial CAP caused by Streptococcus pneumoniae (irrespective of penicillin susceptibility), Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, and Staphylococcus aureus and in the therapy of atypical pneumonia caused by Mycoplasma pneumoniae and Legionella pneumophila. Grepafloxacin was well tolerated, with the most frequently reported drug-related adverse events being taste perversion and nausea. Grepafloxacin 600 mg QD for 10 days was highly effective and well tolerated in the treatment of patients with CAP.
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PMID:Efficacy and safety of grepafloxacin 600 mg daily for 10 days in patients with community-acquired pneumonia. 938 85

The activity of grepafloxacin, a new orally active fluoroquinolone, was compared with the activities of ofloxacin, clarithromycin and doxycycline against Chlamydia pneumoniae, Chlamydia trachomatis, Mycoplasma pneumoniae, Mycoplasma hominis and Ureaplasma urealyticum, and with the activities of ofloxacin, clarithromycin and rifampicin against Legionella spp. Grepafloxacin (MIC range 0.06-0.12 mg/L) was some 8-16 times more active than ofloxacin against the chlamydiae, showing activity similar to that of doxycycline, and equal or two- to four-fold less active than clarithromycin. Grepafloxacin was four-fold more active than ofloxacin against M. pneumoniae (MIC 0.06-0.5 mg/L) and U. urealyticum (MIC 0.12-1.0 mg/L), but 16 times more active against M. hominis (MIC 0.015-0.05 mg/L). Grepafloxacin was highly active against Legionella spp. (MIC 0.008-0.03 mg/L), showing equivalent activity to ofloxacin, clarithromycin and rifampicin.
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PMID:The in-vitro activity of grepafloxacin against Chlamydia spp., Mycoplasma spp., Ureaplasma urealyticum and Legionella spp. 948 71

OBJECTIVE: To determine the in vitro antimicrobial activity, postantibiotic effect (PAE) and human monocyte activity of grepafloxacin compared with sparfloxacin, ciprofloxacin, clarithromycin, erythromycin and rifampicin against 181 strains of Legionella pneumophila, nine strains of L. micdadei, 10 strains of L. dumoffii, seven strains of L. longbeachae and seven other Legionella strains. METHODS: MICs were determined by standard agar dilution using buffered yeast extract (BYE) agar. PAE and human monocyte activity were determined by standard culture techniques. RESULTS: Grepafloxacin, sparfloxacin and rifampicin were the most active agents against L. pneumophila (MIC90 </=0.016 mg/L for most strains tested). Grepafloxacin was more active than erythromycin against L. dumoffii and L. longbeachae and more active than both erythromycin and clarithromycin against L. micdadei and isolates of other Legionella spp. The PAE of grepafloxacin against erythromycin-susceptible L. pneumophila (2.62 h) was higher than that of sparfloxacin (0.88 h), erythromycin (0.93 hours) and clarithromycin (0.72 h). Against erythromycin-resistant L. pneumophila, the PAE of grepafloxacin (4.18 h) was higher than those of all the other antibiotics tested. Grepafloxacin, sparfloxacin, ciprofloxacin and clarithromycin inhibited the growth of all L. pneumophila strains and other erythromycin-resistant Legionella spp. in human monocytes. However, only grepafloxacin and ciprofloxacin prevented regrowth or killed L. pneumophila after removal of extracellular antibiotic. CONCLUSIONS: Grepafloxacin showed effective antibacterial activity against the Legionella spp. tested, and has a PAE and activity within human monocytes that suggest it may be useful in the treatment of lower respiratory tract infections caused by Legionella spp.
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PMID:In vitro activity, postantibiotic effect and human monocyte activity of grepafloxacin against Legionella species. 1185 51

Studies in community-acquired pneumonia (CAP) have compared grepafloxacin, 600 mg o.d. for 7--10 days, with amoxycillin, 500 mg t.d.s., cefaclor, 500 mg t.d.s., or clarithromycin, 250 mg b.d. Grepafloxacin appeared to be clinically as effective as the comparators. In CAP caused by Haemophilus influenzae, grepafloxacin was significantly superior to amoxycillin (p=0.005) and cefaclor (p=0.003) and equivalent to clarithromycin in eradicating the infecting organism. Bacterial eradication with grepafloxacin in CAP caused by Moraxella catarrhalis or Streptococcus pneumoniae was effective and equivalent to the comparator antibiotic. In an open study, grepafloxacin was also effective in treating atypical pneumonia caused by Mycoplasma pneumoniae and Legionella pneumophila. In acute bacterial exacerbations of chronic bronchitis (ABECB), studies have found once-daily treatment with grepafloxacin, 400 mg or 600 mg for 7--10 days, to be equivalent to amoxycillin, 500 mg t.d.s., or ciprofloxacin, 500 mg b.d. In patients with documented infections, bacteriologic eradication with grepafloxacin, 400 mg or 600 mg o.d., was superior to amoxycillin, 500 mg t.d.s. Results from clinical trials so far indicate that grepafloxacin has a broad spectrum of activity covering all important community-acquired respiratory pathogens, and may be suitable for the empirical treatment of respiratory infection.
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PMID:Clinical efficacy and tolerability of grepafloxacin in lower respiratory tract infection. 1186 47

Grepafloxacin potency and spectrum of activity were re-evaluated against contemporary pathogens collected from clinical infections in 2001-2002. A total of 995 isolates were tested for grepafloxacin by the reference agar dilution method and these results were compared to those of 25 other antimicrobial agents. Grepafloxacin activity remained comparable to that of ciprofloxacin, levofloxacin and gatifloxacin against Escherichia coli, Klebsiella pneumoniae and Enterobacter cloacae (MIC(90), 0.03-2 microg/ml; 0.0-7.7% resistance rates). For Pseudomonas aeruginosa, grepafloxacin was active against ciprofloxacin-susceptible (MIC(90), 2 microg/ml), but not against ciprofloxacin-resistant (MIC(90), >8 microg/ml) isolates. Against methicillin-susceptible Staphylococcus aureus, grepafloxacin susceptibility rate was 91.4%, equal to that of levofloxacin. None of the fluoroquinolones showed reasonable activity against methicillin-resistant staphylococci. Gatifloxacin and grepafloxacin had the same MIC(90) against beta-hemolytic streptococci (0.25 microg/ml) and penicillin-susceptible Streptococcus pneumoniae (0.25 microg/ml). Grepafloxacin and other fluoroquinolone activities were not influenced by penicillin resistance in S. pneumoniae. Grepafloxacin was very active against Haemophilus influenzae (MIC(90), 0.03 microg/ml), Moraxella catarrhalis (MIC(90), 0.03 microg/ml) and Legionella spp. (MIC(90), 0.5 microg/ml). These results on recently isolated organisms indicate that grepafloxacin has a sustained potency and spectrum against most clinically important and indicated pathogens.
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PMID:Contemporary re-evaluation of the activity and spectrum of grepafloxacin tested against isolates in the United States. 1296 54

The treatment of respiratory tract infection is the most common reason for antibiotic prescribing. However, therapeutic options are diminishing as antibiotic resistance to penicillins and macrolides in key respiratory pathogens is increasing. As resistance increases, there are parallel rises in the number of treatment failures and the total cost of infection management. New generation broad-spectrum fluoroquinolones, such as grepafloxacin, have recently been recommended as a first-line treatment option in guidelines for lower respiratory tract infection. Grepafloxacin is an oral fluoroquinolone, with a microbiological and clinical profile that is particularly suited to the treatment of community-acquired respiratory infections. In vitro, it is rapidly bactericidal, and compared with earlier quinolones, its broad spectrum activity encompasses all important respiratory pathogens; Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, Chlamydia pneumoniae and Legionella pneumophila, including strains which are resistant to penicillin, other beta-lactam antibiotics and macrolides. In addition, grepafloxacin achieves high lung concentrations, and its long half-life (up to 15 h) enables once daily dosing. Overall, grepafloxacin combines the positive properties of the beta-lactam antibiotics against conventional Gram-positive and Gram-negative respiratory pathogens, with the activity of the macrolides against atypical pathogens. In patients with bacteriologically documented infections, clinical studies in community-acquired pneumonia have shown that treatment for 7-10 days once daily (o.d.) with approximately 600 mg is equivalent to that with either twice daily (b.i.d.) clarithromycin 250 mg, or three times daily (t.i.d.) cefaclor 500 mg, and superior to that with t.i.d. amoxycillin 500 mg. In these studies, grepafloxacin proved effective in the treatment of both typical and atypical pneumonia. In acute bacterial exacerbations of chronic bronchitis (ABECB), 7-10 days treatment with o.d. grepafloxacin 400 mg or 600 mg has been shown to be equivalent to that with either t.i.d. amoxycillin 500 mg, or b.i.d. ciprofloxacin 500 mg. In patients with a documented bacterial pathogen, microbiological success with both grepafloxacin dosage regimens was superior to amoxycillin 500 mg t.i.d. In addition, short course treatment of ABECB with 400 mg of grepafloxacin given o.d. for five days has been shown to be as effective, clinically and microbiologically as a ten-day course of the same dose. The safety profile of grepafloxacin has been well-characterised from data from over 12,000 patients treated in Phase II/III and post-marketing studies, and over 400,000 patients treated worldwide in routine clinical practice. The most commonly reported adverse events are gastrointestinal, mainly nausea and unpleasant taste. The potential for photosensitivity and central nervous system effects is low, and there have been no reports of convulsions. No unique or unexpected.
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PMID:Grepafloxacin: an overview of antibacterial activity, pharmacokinetics, clinical efficacy and safety. 1599 94