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Query: UMLS:C0519030 (Klebsiella)
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Nalidixic acid and three fluoroquinolones were tested on 389 strains belonging to 13 bacterial species, all isolated in Algeria. Ofloxacin, norfloxacin and pefloxacin have the same activities on E. coli, Acinetobacter and S. aureus. Norfloxacin has the best activity on Proteus, Enterobacter, Shigella and Klebsiella. Norfloxacin and ofloxacin have the same activities on S. typhi, Salmonella and choleric Vibrio. Norfloxacin has the same activity than pefloxacin on P. aeruginosa. It is necessary to prescribe a quinolone in the right way and to consider the pharmacokinetic properties.
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PMID:[Comparative activities in vitro of 4 quinolones (nalidixic acid, pefloxacin, norfloxacin, ofloxacin) on 13 bacterial species]. 130 46

The attainable inhibitory ratios (AR) for oral antibiotics were calculated by using literature reports of concentrations attained in respiratory secretions for amoxicillin-clavulanic acid (AMX/CA), ofloxacin (OFL), L-ofloxacin (L-OFL), cefuroxime (CEFU), ciprofloxacin (CIP), and enoxacin (ENO), and using microdilution minimum inhibitory concentration data of these antimicrobials against the common bacterial respiratory pathogens. AR of each antibiotic against the pathogens was expressed as multiples of the MICs achieved at the respiratory site. Bacteria tested included Staphylococcus aureus, group-A and group-B streptococci, Viridans streptococci, Streptococcus pneumoniae, Brahamella catarrhalis, Klebsiella pneumoniae, Eikenella corrodens, Haemophilus influenzae, H. parainfluenzae, Pseudomonas aeruginosa, and Legionella pneumophila. The antimicrobials with the narrowest spectrum of activity were amoxicillin-clavulanic acid and cefuroxime which had high attainable inhibitory ratios only against Gram-positive cocci. Ofloxacin and L-oflaxacin were among the quinolones with the highest overall ARs against respiratory pathogen, including, L. pneumophila, H. influenzae, and B. catarrhalis. All agents showed no, or inadequately low ARs for P. aeruginosa.
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PMID:A comparison of antimicrobial activity of ofloxacin, L-ofloxacin, and other oral agents for respiratory pathogens. 157 39

The efficacy and safety of parenteral ofloxacin were evaluated in an open, multicenter study of hospitalized patients with pyelonephritis. The patients received ofloxacin 400 mg IV as an initial dose followed by ofloxacin 200 mg IV b.i.d. for a minimum of three days. The patients could then continue ofloxacin orally 200 mg b.i.d. for a total of seven to fourteen days. The most common pathogens isolated were Escherichia coli, Enterobacter cloacae, and Klebsiella pneumoniae. Microbiologic eradication was achieved in 65 of 66 evaluable patients (98%), and clinical cure or clinical improvement was noted in all patients. Of 82 patients evaluable for safety, 12 (15%) reported drug-related adverse events, the most frequent of which was pruritus or rash. None of the patients experienced drug-related central nervous system symptoms. Ofloxacin is well tolerated and highly effective in the treatment of pyelonephritis.
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PMID:Multicenter open-label study of parenteral ofloxacin in treatment of pyelonephritis in adults. 158 38

A multicenter randomized study was conducted to compare the efficacy and safety of ofloxacin with that of trimethoprim/sulfamethoxazole (TMP/SMX) in the treatment of uncomplicated urinary tract infection in adults. Patients were randomized to receive either oral ofloxacin 200 mg daily for three days (102 patients), or oral TMP/SMX 160 mg/800 mg twice daily for seven days (100 patients). The pathogen was eradicated in 73 (97.3%) of the 75 evaluable patients receiving ofloxacin and in 66 (97.1%) of the 68 evaluable patients receiving TMP/SMX. The most frequently isolated pathogens were Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis. More urinary pathogens were susceptible to ofloxacin than to TMP/SMX, although this difference was not statistically significant. The clinical cure rate for patients receiving ofloxacin was 93.3%, with 4% improved and 2.7% failed. For patients receiving TMP/SMX, the clinical cure rate was 86.4%, with 12.1% improved and 1.5% failed. Side effects were reported by 29.7% of the patients receiving ofloxacin and by 40.4% of the patients receiving TMP/SMX. Drug-related adverse experiences, as determined by the investigators, occurred in 5% of the ofloxacin patients and in 15.2% of the TMP/SMX patients, a statistically significant difference. No patients receiving ofloxacin, compared with three patients receiving TMP/SMX, discontinued therapy because of an adverse reaction. These results indicate that short-course ofloxacin is as effective as TMP/SMX in the treatment of uncomplicated urinary tract infection. Ofloxacin therapy is also better tolerated than TMP/SMX.
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PMID:Ofloxacin versus trimethoprim/sulfamethoxazole in the treatment of uncomplicated urinary tract infection. 163 86

Ofloxacin, a newer broad-spectrum fluoroquinolone, was evaluated against 6967 clinical isolates in a multicenter surveillance trial using a standardized disk diffusion method. Thirty-five geographically diverse laboratories contributed zone diameter results for two (ofloxacin and ciprofloxacin) to five (ofloxacin, ciprofloxacin, ampicillin, cefaclor, and cefixime) antimicrobial agents, depending on the site of infection. Ofloxacin was determined to have the widest spectrum of activity and potential empiric use (90.6%, range 87.1%-92.2%) for respiratory tract, urinary tract, and cutaneous infections. The spectrum was superior to ciprofloxacin (average 85.3% versus three sites), ampicillin (35.5%, respiratory tract), cefaclor (60.5%, respiratory tract), cefixime (60.9%, respiratory tract), and norfloxacin (87.3%, urinary tract). Strains resistant to ofloxacin (35 isolates, 0.5%) were confirmed by reference laboratory tests and cross resistance was observed among several current and investigational fluoroquinolone agents. The species most often found to be fluoroquinolone resistant among the Enterobacteriaceae were Klebsiella pneumoniae, Serratia marcescens, and Providencia spp. Monitoring for increasing fluoroquinolone resistance should be considered as greater use of drugs in this class develops. By these cited statistics, ofloxacin appears to have a broad and balanced spectrum of potential use, particularly against Gram-positive pathogens.
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PMID:Ofloxacin, a new broad-spectrum fluoroquinolone. Results from a Multicenter, National Comparative Activity Surveillance Study. The Ofloxacin Surveillance Group. 164 19

We report a multicentric, open trial of intravenous followed by oral ofloxacin, 400 mg every 12 h, as therapy for 100 cases of nosocomial pneumonia and community-acquired pneumonia requiring hospitalization. The typical subject was 57 yr old, and underlying diseases, such as chronic obstructive pulmonary diseases (COPD), diabetes mellitus, and congestive heart failure, were common. For 10 subjects previous therapy had failed. There were 118 pathogens isolated in blood or sputum; S. pneumoniae was the most common (42), followed by H. influenzae (13), Klebsiella spp. (11), and S. aureus (10). Ofloxacin was administered for an average of 5.7 days intravenously followed by 6.9 days orally. Response to therapy was judged to be cure in 71 subjects, improvement in 24, and failure in 5. Among the more seriously ill subjects, ofloxacin therapy was successful for four of five immunocompromised subjects, for 12 of 12 subjects with nosocomial pneumonia, three of whom were on the ventilator, and for nine of 10 subjects with community-acquired pneumonia and bacteremia, including seven of eight cases due to S. pneumoniae. Univariate risk factor analysis revealed underlying COPD and/or tachypnea upon admission to be associated with failure of ofloxacin therapy, with bacteremia suggestive of failure. Conversely, ofloxacin was equally effective in cases in whom previous therapy failed and in cases of nosocomial pneumonia, multilobar pneumonia, and/or pneumonia due to S. pneumoniae. Results for P. aeruginosa were inconclusive. Intravenous followed by oral ofloxacin was highly effective in many difficult cases of pneumonia.
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PMID:Parenteral followed by oral ofloxacin for nosocomial pneumonia and community-acquired pneumonia requiring hospitalization. 173 95

We made an open, noncomparative evaluation of ofloxacin, 400 mg orally bid for 10 days, in 98 subjects with community-acquired pneumonia or pathogen-confirmed bronchitis. Thirty-nine (40%) of the subjects were treated in the hospital and 59 (60%) were treated as outpatients. The mean age of those treated was 56.2 years; 73 (74%) of the subjects either were more than 60 years old or had a history of chronic obstructive pulmonary disease, or both. There were 95 organisms initially isolated in sputum, aspirate, or lavage fluid; all were susceptible to ofloxacin, and none acquired resistance during therapy. Haemophilus influenzae was the most common pathogen (19 isolates), followed by Streptococcus pneumoniae (18) and Staphylococcus aureus (10). Clinical responses included cure in 70 patients (71%), improvement in 26 (27%), and failure in two (2%). After 10 days of therapy, pathogens persisted in two cases; in one case, Streptococcus salivarius was isolated, though it remained susceptible to ofloxacin, and in the other, Klebsiella pneumoniae was accompanied by superinfection due to a resistant strain of Serratia marcescens. We included in this study three confirmed cases of atypical pneumonia successfully treated with ofloxacin, two of them due to Mycoplasma pneumonia and one to Legionella pneumophila. Ofloxacin was well tolerated. Our data indicate that ofloxacin is effective and safe as specific and empiric treatment for many lower respiratory tract infections.
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PMID:Oral ofloxacin therapy for lower respiratory tract infection. 173 27

We determined the efficacy and safety of orally administered ofloxacin, 400 mg twice daily, in the treatment of infections due to multiply-resistant bacteria. Patients (n = 99) were treated for 84 infections in 82 patients evaluable for efficacy with a bacteriologic response of 71%. Organisms treated included Pseudomonas aeruginosa (39), Staphylococcus aureus (11), Serratia marcescens (9), Enterobacter species (7), five each of Escherichia coli, Citrobacter, Salmonella, Klebsiella, and other organisms. The overall clinical responses was 89%: 28 (90%) of 16 osteomyelitis, 10 (83%) of 12 urinary tract infections, and three of three bacteremias. Insomnia occurred in 27% and responded to dose reduction. Resistance of P. aeruginosa to ofloxacin developed in 15% of isolates. No hepatic, renal, or hematologic toxicity developed in spite of long therapy, 283 days. Ofloxacin was an effective therapy for lower respiratory, urinary, bone, and soft tissue infections due to multiply-resistant Gram-negative bacteria and is effective for selected Staphylococcus aureus infections.
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PMID:Oral ofloxacin therapy of infections due to multiply-resistant bacteria. 179 58

We evaluated the combination of ofloxacin with piperacillin, gentamicin, vancomycin, rifampin, clindamycin, and metronidazole by the checkerboard agar dilution method against 165 isolates which included Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens, Pseudomonas aeruginosa, Providencia stuartii, Acinetobacter, Staphylococcus aureus, Bacteroides fragilis, and Citrobacter perfringens. Synergy of piperacillin-ofloxacin was demonstrated for 50% and 40% respectively of E. cloacae and P. aeruginosa. Some ofloxacin and piperacillin-resistant isolates were susceptible with the combination. Ofloxacin-gentamicin was indifferent for aerobic gram-negative species. Ofloxacin and vancomycin or gentamicin was indifferent for S. aureus and E. faecalis, but rifampin-ofloxacin showed addition. Combination of ofloxacin and metronidazole or clindamycin or erythromycin was indifferent for aerobic and anaerobic species. Ofloxacin could be combined with piperacillin with benefit against P. aeruginosa, but combination with aminoglycosides is not of benefit.
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PMID:Combination of ofloxacin and other antimicrobial agents. 209 3

Ofloxacin is highly active against common respiratory pathogens including Haemophilus influenzae and Branhamella catarrhalis and has clinically applicable activity against Streptococcus pneumoniae, Staphylococcus aureus and Pseudomonas aeruginosa. Sputum, lung tissue and bronchial mucosal concentrations of ofloxacin equal or, in most cases significantly exceed the MICs of such pathogens. These in vitro attributes are reflected in the results of the worldwide ofloxacin clinical trial program which achieved overall response rates of 98% in lower respiratory tract infections, 83% in pneumonias and 87% to 95%, in open and comparative studies respectively, in patients with acute exacerbations of chronic bronchitis (CB). Overall bacterial eradication rates ranged from 70% for pneumococci and 84.5% for B. catarrhalis to 88.5% for H. influenzae. In lower respiratory infection ofloxacin gave equal or superior clinical results to amoxycillin or erythromycin therapy together with an overall bacterial eradication rate of 100%. Clinical results comparable with standard agents were also obtained in pneumonia, cure rates ranging from 77-89% at various dosages. Eradication rates proved greatest for H. influenzae (92%) and were satisfactory for Klebsiella spp. (80%), although less so for pneumococci (73%). Bacteriological eradication rates in acute exacerbations of chronic bronchitis ranged from 68% for pneumococcal infections, to 85% in B. catarrhalis and 94% in H. influenzae infections. Ofloxacin compared favourably with pivampicillin, co-trimoxazole and doxycycline clinically. A daily oral ofloxacin dose of 400 mg produced a good clinical response in 92% of patients or more. The available clinical data therefore substantially confirm the claim of ofloxacin to offer an effective alternative in many forms of acute bacterial respiratory infection, especially where H. influenzae and B. catarrhalis are involved.
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PMID:Overview of experience with ofloxacin in respiratory tract infection. 221 24


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