Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0032285 (pneumonia)
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Gatifloxacin is a novel extended-spectrum fluoroquinolone with improved gram-positive and anaerobe coverage compared with older agents such as ciprofloxacin. It has good activity (but is slightly less active than ciprofloxacin) against Enterobacteriaceae. Gatifloxacin is generally 2- to 4-fold more active than ciprofloxacin against staphylococci, streptococci and enterococci and 4- to 16-fold more active than ciprofloxacin against anaerobes, including Clostridium and Bacteroides spp. In comparative clinical trials that included patients with lower respiratory tract, urinary tract, skin and soft tissue or gonococcal infections, clinical cure rates of > or = 89% were achieved with oral gatifloxacin 400 mg/day for 7 to 14 days. Data from a subset of North American patients included in a multinational trial showed that oral gatifloxacin 400 mg/day produced a significantly higher clinical cure rate than cefuroxime axetil 250 mg twice daily (89 vs 77%; p = 0.01) in patients with acute exacerbations of chronic bronchitis. The clinical efficacy of gatifloxacin was similar to that of clarithromycin or levofloxacin or ceftriaxone (with or without erythromycin) in the treatment of patients with community-acquired pneumonia. Oral gatifloxacin 400 mg/day showed clinical and bacteriological efficacy similar to that of levofloxacin in patients with skin and soft tissue infections. In patients with urinary tract infections, clinical cure and bacterial eradication rates achieved with a single 400 g oral dose of gatifloxacin were similar to those produced with ciprofloxacin. In a pooled analysis of tolerability data from trials that included 3021 patients treated with oral gatifloxacin 400 mg/day, the most commonly reported adverse events were nausea (8%), diarrhoea (4%), headache (4%) and dizziness (3%). The drug was reported to be well tolerated. Gatifloxacin does not appear to cause phototoxic effects.
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PMID:Gatifloxacin. 1055 38

Gatifloxacin is a new 8-methoxy-fluoroquinolone antibiotic approved for use in the United States in December 1999. It has a broad spectrum of activity with potent activity against gram-positive bacteria, including penicillin-resistant Streptococcus pneumoniae, as well as excellent activity against gram-negative and atypical organisms. Gatifloxacin is available in both oral and injectable forms and is administered once/day. Bioavailability is 96%, with a plasma half-life of approximately 8 hours in individuals with normal renal function. Elimination is primarily renal excretion of unchanged drug with no cytochrome P450-mediated metabolism. The drug is distributed extensively into tissues and fluids and has a favorable pharmacodynamic profile against important pathogens. It had excellent efficacy in clinical studies of acute sinusitis, acute bacterial exacerbations of chronic bronchitis, community-acquired pneumonia, complicated and uncomplicated urinary tract infections and pyelonephritis, skin and skin structure infections, and uncomplicated gonococcal infections. The agent is well tolerated, with no evidence of hepatic, cardiac, or phototoxicity noted thus far. Drug interactions are uncommon; however, like other fluoroquinolones, coadministration with multivalent cations should be avoided due to significantly decreased absorption. Gatifloxacin should prove to be a safe and effective agent for a wide variety of infections.
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PMID:Gatifloxacin, an advanced 8-methoxy fluoroquinolone. 1119 37

Gatifloxacin is a novel fluoroquinolone with a 3-methylpiperazine group at position 7 of the quinolone ring and a methoxy group at position 8 [287520,379131]; the 8-methoxy substituent seems to decrease the rate of development of resistance in Gram-positive bacteria [378631]. Gatifloxacin appears safe and effective [286426,342518,378432] and has been approved in the US and several other countries for the treatment of community-acquired pneumonia (CAP), acute bacterial exacerbation of chronic bronchitis, acute sinusitis, uncomplicated skin and skin structure infections, uncomplicated urinary tract infections, complicated urinary tract infections and pyelonephritis, uncomplicated urethral, endocervical, pharyngeal and rectal gonorrhea [352761,359434].
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PMID:Gatifloxacin Kyorin Pharmaceutical Co. 1124 93

Respiratory tract infections (RTIs), the most common indication for outpatient antimicrobial therapy, impose a heavy medical and societal burden and present a difficult therapeutic challenge in the face of increasing pathogen resistance worldwide. Gatifloxacin is a new broad-spectrum fluoroquinolone with excellent activity against prevalent respiratory bacteria, including penicillin-resistant Streptococcus pneumoniae and atypical pathogens. A multicenter, open-label, noncomparative surveillance study carried out in Mexico evaluated the safety and efficacy of oral gatifloxacin 400 mg once daily in 17,923 adult outpatients with community-acquired pneumonia (CAP) (n = 3322), acute exacerbations of chronic bronchitis (AECB) (n = 5885), and acute bacterial sinusitis (n = 8716). Voluntary, unpaid physician participation contributed to an unbiased study design. Physician-assessed global rate of cure or improvement was 96.3%; efficacy was 95.8% in CAP, 96.1% in AECB, and 96.4% in sinusitis. The incidences of relapse (1.5%) and therapeutic failure (0.7%) were low. The most commonly reported adverse events, nausea (2.76%), headache (2.20%), and dizziness (1.33%), were generally mild and self-limited. Oral gatifloxacin 400 mg once daily is effective and safe for patients with CAP, AECB, and acute sinusitis.
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PMID:Multicenter evaluation of the efficacy and safety of gatifloxacin in Mexican adult outpatients with respiratory tract infections. 1131 29

To evaluate the prevalence of typical pathogens, level of resistance, and risk factors associated with community-acquired pneumonia (CAP) in the outpatient primary care setting and define current antibiotic treatment for office-based CAP, the Respiratory Surveillance Program (RESP) recruited 1,200 primary care clinics during the 1999-2000 respiratory infection season. Participating community-based physicians submitted sputum samples from patients presenting with a community-acquired respiratory infection including community-acquired pneumonia (CAP). All patients were aged > or =18 years. Patient demographics and risk factors were collected. Physicians express-mailed the specimens to a central laboratory for identification and susceptibility testing. All isolates were tested against a select panel of antimicrobial agents that are used to treat CAP. Patients with CAP were diagnosed by the treating physicians. Chest radiographs were not required as part of the study. A total of 610 specimens were submitted from patients with CAP. A smoking history or reported history of chronic obstructive pulmonary disease were present in >50% of those diagnosed with CAP. The most common pathogens were, in order of prevalence, Haemophilus influenzae, Streptococcus pneumoniae, and Moraxella catarrhalis. During the study period, a variety of antibiotics were prescribed for the treatment of outpatient CAP. The top 3 prescribed antibiotics include levofloxacin (23%), clarithromycin (19%), and azithromycin (10%). Gatifloxacin, which was approved in December 1999 and therefore available for only part of the study, accounted for 4% of the prescriptions. Of S pneumoniae isolates, 8% demonstrated high-level resistance to penicillin (> or =2 microg/mL) and 33% were found resistant to macrolides and trimethoprim/sulfamethoxazole. All S pneumoniae isolates were sensitive to gatifloxacin, vancomycin, and levofloxacin. Other less common organisms isolated were staphylococci, streptococci, Enterobacteriaceae, Pseudomonas spp, and Acinetobacter spp. The choice of antibiotic to treat outpatient CAP varies from practice to practice and does not appear to be influenced by the patient's age, the patient's history of smoking, or comorbidity.
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PMID:Epidemiology of clinically diagnosed community-acquired pneumonia in the primary care setting: results from the 1999-2000 respiratory surveillance program. 1175 40

The in vitro antimicrobial activity of gatifloxacin against clinical isolates of pathogenic bacteria was evaluated. Minimum inhibitory concentrations of gatifloxacin, ofloxacin, ciprofloxacin, tosufloxacin, sparfloxacin, and rifampicin against 20 strains each of methicillin-susceptible Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, and Pseudomonas aeruginosa, 18 strains of Enterobacter cloacae, 15 strains each of Streptococcus Pneumoniae and Moraxella catarrhalis, 12 strains of Haemophilus influenzae, 18 strains of Mycobacterium intracellulare, and 22 strains each of Mycobacterium tuberculosis and Mycobacterium avium were determined. The minimum inhibitory concentrations90's of gatifloxacin against the above species were 0.12, 8, <==0.06, 0.5, 2, 2, <==0.06, 0.39, 0.05, 0.013, 2, 0.5, and 4 &mgr;g/ml, respectively. Gatifloxacin was four times as active as ofloxacin against methicillin-susceptible and -resistant Staphylococcus aureus, and as active as ofloxacin against Enterobacteriaceae and Pseudomonas aeruginosa. Gatifloxacin was as active as tosufloxacin and sparfloxacin against Streptococcus pneumoniae, Moraxella catarrhalis, and Haemophilus influenzae. The antimycobacterial activity of gatifloxacin was similar to that of sparfloxacin. Five patients with chronic respiratory infections and one patient with acute pneumonia received 100-400 mg/day of gatifloxacin orally for 5-12 days (mean, 8.17 days). The clinical effects were excellent in one patient and good in five. One strain of Haemophilus influenzae was eradicated and one strain of Pseudomonas aeruginosa persisted after therapy. Adverse reactions were mild and improved after completion of therapy. In one patient with chronic bronchitis, the maximum sputum concentrations 2-4 h after oral administration of 150 mg of gatifloxacin on days 1 and 6 were 0.88 and 1.45 &mgr;g/ml, respectively, and in serum the values were 0.84 and 1.24 &mgr;g/ml, respectively. Thus it was found that gatifloxacin possesses potent activity against respiratory pathogens (including Mycobacteriaceae), and shows good penetration rate into sputum, and that it can be used as the drug of first choice in the treatment of respiratory tract infections.
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PMID:In vitro antimicrobial activity and penetration rate into sputum of gatifloxacin, a novel 6-fluoro-8-methoxy quinolone, and its therapeutic efficacy in respiratory infections. 1181 May 7

Gatifloxacin is an 8-methoxy fluoroquinolone with broad activity against respiratory tract pathogens, including those commonly associated with community-acquired pneumonia (CAP). To evaluate the efficacy and safety of oral gatifloxacin 400 mg once daily for seven to 14 days, community-based physicians enrolled adult outpatients with confirmed or suspected CAP in a prospective, single-arm, open-label, noncomparative study. Of 1488 clinically evaluable patients with radiographically confirmed or clinically suspected CAP, 1417 (95.2%) were cured. All strains of Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis, the most commonly isolated pathogens, were susceptible to gatifloxacin. Penicillin nonsusceptibility was seen in 32.6% of S. pneumoniae isolates, and beta-lactamase production was detected in H. influenzae (26.9%) and M. catarrhalis (88%) isolates. Clinical cure rates of 91%, 94%, and 92% were achieved in patients with S. pneumoniae, H. influenzae, and M. catarrhalis, respectively. All seven patients with fully penicillin-resistant S. pneumoniae (MIC > or =2 micro g/ml) were cured. Gatifloxacin was well tolerated, with the most common drug-related adverse events being nausea (2.8%) and diarrhea (1.7%). Gatifloxacin is effective and well tolerated as empiric therapy for CAP in the outpatient community setting.
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PMID:Oral gatifloxacin in outpatient community-acquired pneumonia: results from TeqCES, a community-based, open-label, multicenter study. 1237 37

Gatifloxacin is an advanced-generation fluoroquinolone with demonstrated efficacy and safety as therapy for community-acquired pneumonia (CAP). As part of a phase IV postmarketing surveillance program (TeqCES), 136 outpatients with CAP whose sputum was culture-positive for Streptococcus pneumoniae were enrolled in an open-label trial of oral gatifloxacin 400 mg daily for 7 to 14 days. An antibiogram of isolates showed 100% susceptibility to gatifloxacin (MIC(90) 0.5 micro g/mL) and respective susceptibilities of 67%, 70%, and 80% to penicillin, erythromycin, and tetracycline. Clinical cure was achieved in 95.3% of evaluable patients, including seven patients infected with penicillin-resistant S. pneumoniae (MIC > or =2 micro g/mL). The bacteriologic eradication rate for S. pneumoniae was 94.5%. Diarrhea, nausea, and dizziness, the most common adverse events in CAP patients (<3%), were generally mild to moderate; no serious adverse events were recorded. These results support recommendations to treat CAP, particularly due to S. pneumoniae including multidrug-resistant strains, with the newer 8-methoxy-fluoroquinolone, gatifloxacin.
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PMID:Gatifloxacin used for therapy of outpatient community-acquired pneumonia caused by Streptococcus pneumoniae. 1237 38

The elderly are at increased risk for respiratory tract infections. To evaluate the safety and efficacy of gatifloxacin in adults of any age with community-acquired respiratory tract infections, this open-label, multicenter, noncomparative study in community-based practices enrolled male and female outpatients at least 18 years old with a clinical diagnosis of community-acquired pneumonia (CAP), acute-bacterial exacerbation of chronic bronchitis (AECB), or acute uncomplicated maxillary sinusitis. Gatifloxacin 400 mg was administered once daily for seven to 14 days. Of 14781 clinically evaluable patients, 2505 were at least 65 years old, 499, at lest 80. Cure rates for CAP, AECB, and sinusitis ranged from 91.6% to 95.5% for patients less than 65 years old, 91.1% to 96.2% for those 65 to 79 years of age, and 89.5% to 94.8% for those at least 80 years old. Each age group, including patients with concomitant cardiovascular or diabetic conditions, tolerated treatment well. Gatifloxacin is efficacious and well tolerated in adult outpatients of any age with respiratory tract infections and is an important therapeutic option, particularly in communities with a high prevalence of resistant pathogens.
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PMID:Gatifloxacin in community-based treatment of acute respiratory tract infections in the elderly. 1237 40

To evaluate the safety and efficacy of gatifloxacin in adults <65, 65 to 79, or > or =80 years old with community-acquired pneumonia, adult male and female outpatients from general community-based practices were enrolled in an open-label, multicenter, noncomparative study. Gatifloxacin 400 mg once daily was administered for seven to 14 days. Medical history, physical examination, signs and symptoms of infection, Gram stain and culture if specimen available, clinical response, and safety were determined. Of 1655 treated patients, 1103 were at least 65 years old, 405 were 65 to 79, and 147 were at least 80. Patients > or =80 years old presented with chills, chest pain, fever, or headache less often than younger patients. Cure rates were 95.5% for patients <65 years old, 96.2% for those 65 to 79, and 90.2% for those at least 80 years old. Neither the frequency nor susceptibility of isolated pathogens appeared to differ with age. Between 93.7% and 100% of subsets of the two younger groups with verified Streptococcus pneumoniae or Hemophilus influenzae were cured. All oldest-group patients in the subset with verified S. pneumoniae and 71.4% (7) of patients with H. influenzae were cured. Each age group, including current or past smokers and patients receiving medications for concomitant conditions, tolerated treatment well. Gatifloxacin is safe and efficacious in adults of any age with community-acquired pneumonia, including the elderly up to 100 years old and patients with S. pneumoniae including penicillin-resistant strains.
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PMID:Efficacy and safety of gatifloxacin in elderly outpatients with community-acquired pneumonia. 1237 41


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