"Grepafloxacin"

Biopharmaceutical Characterization of Nebulized Antimicrobial Agents in Rats. 1. Ciprofloxacin, Moxifloxacin and Grepafloxacin. The aim of this study was to evaluate the biopharmaceutical characteristics of three fluoroquinolones (FQs), ciprofloxacin (CIP), moxifloxacin (MXF), and grepafloxacin (GRX), after delivery via a nebulized aerosol to rats. Bronchoalveolar lavages (BAL) were conducted 0.5

2. Penicillin Sensitive 1. Ampicillin IV or Amoxicillin PO 2. Erythromycin 3. Azithromycin 4. Clarithromycin 5. Penicillin G IV 6. Doxycycline 7. Oral second generation Cephalosporin 8. Parenteral third generation Cephalosporin 3. High-Level Penicillin Resistance 1. Broad spectrum Fluoroquinolone 1. Levofloxacin 2. Gatifloxacin 3. Grepafloxacin

(Factive) 320 mg orally daily for 5 days 5. Grepafloxacin 6. Sparfloxacin 3. Combination Macrolide and Beta-Lactam (in lobar Pneumonia, reasonable to start beta-lactam alone) 1. Drug 1: Macrolide (Azithromycin, Clarithromycin) or Doxycyline (choose one) 1. Azithromycin 500 mg day 1, then 250 mg orally on days 2-5 2. Clarithromycin 500 mg orally twice daily : Single agent using broad spectrum Fluoroquinolone (see adverse effects) 1. Levofloxacin 2. Gatifloxacin 3. Grepafloxacin 4. Moxifloxacin 5. Sparfloxacin 6. Modification for ICU patients 1. Choose one of the 2 base options 2. If a Fluoroquinolone is used, add Aztreonam 7. Modification if risk of MRSA 1. See Healthcare Associated Multidrug Resistance Risk in Pneumonia

(RR 46) 4. Athletes 5. Transplant recipients 6. References 1. Delaney in Herbert (2015) EM:Rap 15(9):11-2 2. (2005) Clin Infect Dis 41: 144 [PubMed] 3. (2002) BMJ 324:1306 [PubMed] 12. QTc Prolongation (risk of Torsades de Pointes) 1. Grepafloxacin pulled from U.S. market in 1999 2. Also may occur

(RR 46) 4. Athletes 5. Transplant recipients 6. References 1. Delaney in Herbert (2015) EM:Rap 15(9):11-2 2. (2005) Clin Infect Dis 41: 144 [PubMed] 3. (2002) BMJ 324:1306 [PubMed] 12. QTc Prolongation (risk of Torsades de Pointes) 1. Grepafloxacin pulled from U.S. market in 1999 2. Also may occur

2. Penicillin Sensitive 1. Ampicillin IV or Amoxicillin PO 2. Erythromycin 3. Azithromycin 4. Clarithromycin 5. Penicillin G IV 6. Doxycycline 7. Oral second generation Cephalosporin 8. Parenteral third generation Cephalosporin 3. High-Level Penicillin Resistance 1. Broad spectrum Fluoroquinolone 1. Levofloxacin 2. Gatifloxacin 3. Grepafloxacin

(Factive) 320 mg orally daily for 5 days 5. Grepafloxacin 6. Sparfloxacin 3. Combination Macrolide and Beta-Lactam (in lobar Pneumonia, reasonable to start beta-lactam alone) 1. Drug 1: Macrolide (Azithromycin, Clarithromycin) or Doxycyline (choose one) 1. Azithromycin 500 mg day 1, then 250 mg orally on days 2-5 2. Clarithromycin 500 mg orally twice daily : Single agent using broad spectrum Fluoroquinolone (see adverse effects) 1. Levofloxacin 2. Gatifloxacin 3. Grepafloxacin 4. Moxifloxacin 5. Sparfloxacin 6. Modification for ICU patients 1. Choose one of the 2 base options 2. If a Fluoroquinolone is used, add Aztreonam 7. Modification if risk of MRSA 1. See Healthcare Associated Multidrug Resistance Risk in Pneumonia

withdrawn from the US market because of toxicity when given systemically; they include trovafloxacin (because of severe hepatic toxicity), gatifloxacin (because of hypoglycemia and hyperglycemia; it is still available in the US as an ophthalmic preparation), grepafloxacin (because of cardiac toxicity), temafloxacin (because of acute renal failure, hepatotoxicity, hemolytic anemia, coagulopathy

A multicenter study of grepafloxacin and clarithromycin in the treatment of patients with community-acquired pneumonia. To compare the efficacies of 10-day regimens of grepafloxacin (GFX) (Raxar or Vaxar; Glaxo Wellcome; Greenford, UK), 600 qd, and clarithromycin (CLA) (Klacid, Biaxin, or Klaracid; Abbott Laboratories; Chicago, IL), 500 mg bid, in patients with community-acquired pneumonia (CAP

Comparison of the abilities of grepafloxacin and clarithromycin to eradicate potential bacterial pathogens from the sputa of patients with chronic bronchitis: influence of pharmacokinetic and pharmacodynamic variables. A randomized open-label study was conducted to compare the pharmacokinetics and pharmacodynamics of grepafloxacin with those of clarithromycin in patients with chronic bronchitis whose sputa were colonized with potential bacterial pathogens. Patients received oral grepafloxacin 400 mg od for 10 days (n = 15) or oral clarithromycin 500 mg bd for 10 days (n = 10). Sputum samples were collected before the first dose, 1, 4 and 8 h after a dose on day 1 and then before a dose on days 2, 3, 5, 7 and 10 to determine the time to eradication (T(erad)) of the potential bacterial

Randomized, double-blind study of short-course (5 day) grepafloxacin versus 10 day clarithromycin in patients with acute bacterial exacerbations of chronic bronchitis. The efficacy and safety of grepafloxacin were compared with clarithromycin in a randomized, double-blind, multicentre clinical trial of 805 patients with acute bacterial exacerbations of chronic bronchitis (ABECB). Patients were randomized to receive grepafloxacin 400 mg od for either 5 (n = 273) or 10 days (n = 268) or clarithromycin 250 mg bd for 10 days (n = 261). Patients were assessed pre-treatment, 3-5 days during treatment, 1-3 days post-treatment and at follow-up (21-28 days post-treatment). The clinical success rates for the evaluable patients were 91% in the 5 day grepafloxacin group, 95% in the 10 day grepafloxacin

Comparative pharmacokinetics of ciprofloxacin, gatifloxacin, grepafloxacin, levofloxacin, trovafloxacin, and moxifloxacin after single oral administration in healthy volunteers. In an open, randomized, six-period crossover study, the pharmacokinetics of ciprofloxacin, gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin, and trovafloxacin were compared after a single oral dose in 12 healthy volunteers (6 men and 6 women). The volunteers received 250 mg of ciprofloxacin, 400 mg of gatifloxacin, 600 mg of grepafloxacin, 500 mg of levofloxacin, 400 mg of moxifloxacin, and 200 mg of trovafloxacin. The concentrations of the six fluoroquinolones in serum and urine were measured by a validated high-performance liquid chromatography method. Blood and urine samples were collected before

clinical phototoxicity studies on systemically administered pharmaceuticals. The in vitro phototoxicity of eight fluoroquinolone (FQ) antibiotics (ciprofloxacin, grepafloxacin, lomefloxacin, norfloxacin, ofloxacin, trovafloxacin, BAYy3118, moxifloxacin) was determined by exposing Chinese hamster fibroblasts to UVA radiation. Cell damage was quantified with standard MTT or neutral red assays

Effectiveness of short-course therapy (5 days) with grepafloxacin in the treatment of acute bacterial exacerbations of chronic bronchitis. Three hundred eighty-nine patients were enrolled in a double-masked, multicenter, randomized clinical trial comparing the clinical and bacteriologic efficacies and safety of a 5-day course (n = 195) versus a 10-day course (n = 194) of grepafloxacin 400 mg once susceptibility (intermediate or high-level resistance) to penicillin. A satisfactory clinical outcome (cure or improvement) was achieved in 83% (128 of 155) and 81% (122 of 150) of clinically evaluable patients treated with grepafloxacin for 5 or 10 days, respectively. Pathogens were eradicated or presumed eradicated in 77% (106 of 138) and 80% (98 of 123) of bacteriologically evaluable patients treated

Crossover assessment of serum bactericidal activity of grepafloxacin, ofloxacin and clarithromycin against respiratory pathogens after oral administration to healthy volunteers. Serum bactericidal activity was studied in a crossover manner in 10 volunteers, after 2-day administration of grepafloxacin 600 mg qd, ofloxacin 400 mg bid and clarithromycin 500 mg bid. Bactericidal activity against clinical isolates of Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis and Klebsiella pneumoniae, was estimated using a standardized microdilution method. Grepafloxacin was highly active against Gram-negative organisms and adequate against pneumococci (mean, 1:13.3). Clarithromycin was very active against both penicillin-susceptible and penicillin-partially-resistant S. pneumoniae

Comparison of single-dose oral grepafloxacin with cefixime for treatment of uncomplicated gonorrhea in men. The STD Study Group. In a randomized open study, 351 male patients with uncomplicated gonorrhea were given single oral doses of grepafloxacin (400 mg) or cefixime (400 mg). In the 299 microbiologically evaluable patients, urethral infections were cured in 99% (147 of 149) of those receiving grepafloxacin and 97% (145 of 150) of those given cefixime. Eradication rates for both regimens were 100% in the 16% (47 of 299) of participants who were infected with penicillin-resistant Neisseria gonorrhoeae and 97% in the 21% (62 of 299) of participants infected with tetracycline-resistant strains. Grepafloxacin is a well-tolerated alternative to cefixime for treatment of uncomplicated gonorrhea in males.

Daily oral grepafloxacin vs. twice daily oral doxycycline in the treatment of Chlamydia trachomatis endocervical infection. To compare the efficacy and safety of a 7-day course of treatment with oral grepafloxacin, 400 mg once daily, and oral doxycycline, 100 mg twice daily, in patients with chlamydial cervicitis. Women aged 18 years or older attending 17 sexually transmitted disease clinics randomized to receive a 7-day course of treatment with either oral grepafloxacin, 400 mg once daily, or oral doxycycline, 100 mg twice daily. Response to therapy was assessed 3-8 days and 21-28 days after completion of treatment. The primary measure of efficacy was eradication of C. trachomatis at the 21-28 day follow-up visit. Clinical success, defined as improvement or complete resolution of the signs