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At least 19 recordsLinked to original sources
PubMed1988

The pharmacokinetics of ofloxacin, desmethyl ofloxacin and ofloxacin N-oxide in haemodialysis patients with end-stage renal failure.

Six patients with end-stage chronic renal failure undergoing haemodialysis were given ofloxacin (600 mg) orally and blood samples were taken at intervals up to 32 h. In four patients samples were also taken before and after haemodialysis. Serum concentrations of ofloxacin, desmethyl ofloxacin and ofloxacin N-oxide were measured by HPLC. The drug was well tolerated. Mean pharmacokinetic parameters for ofloxacin were Cmax 5.5 h (S.D. 1.97 h), Tmax 3.9 h (S.D. 3.25 h), T1/2 28 h (S.D. 17.37 h), AUC0-24 83.1 mg/1 h (S.D. 32.69 mg/l h). The desmethyl metabolite was produced in all patients but only half produced N-oxide. Cmax values were 0.21 mg/l (desmethyl) and 0.37 mg/l (N-oxide). Ofloxacin and desmethyl ofloxacin were variably and only slightly removed by haemodialysis whilst ofloxacin N-oxide was not removed at all. These results confirm that dosage reduction of ofloxacin is required in haemodialysis patients. Therapeutic drug monitoring by HPLC is recommended because of the observed variability in absorption and plasma half life.

Adolescent↗
PubMed1987

A preliminary report on the pharmacokinetics of ofloxacin, desmethyl ofloxacin and ofloxacin N-oxide in patients with chronic renal failure.

The in vitro activities of ofloxacin, desmethyl ofloxacin and ofloxacin N-oxide were determined and a specific high performance liquid chromatography (HPLC) assay for these 3 compounds was devised as part of a study of the pharmacokinetics of ofloxacin and its metabolites in patients with impaired renal function. Desmethyl ofloxacin had significant antimicrobial activity but less than that of the parent drug. In 2 patients with chronic renal failure, specific HPLC assay indicated an extended half-life for ofloxacin (approximately 13 hours) and the appearance in serum of low concentrations of both metabolites after 10 hours, persisting until the last blood sample was taken (32 hours). Further studies using specific assays are needed, particularly in patients undergoing haemodialysis and after administration of multiple doses.

Anti-Infective Agents↗
PubMed1994

Kinetics of ofloxacin and its metabolites in cerebrospinal fluid after a single intravenous infusion of 400 milligrams of ofloxacin.

Ofloxacin has been reported to diffuse readily into the cerebrospinal fluid (CSF) in subjects with both inflamed and uninflamed meninges. However, with moderately susceptible bacteria, ofloxacin concentrations in CSF may be subtherapeutic after administration of an intravenous (i.v.) dose of 200 mg. For this reason, the kinetics of a higher dose of ofloxacin in CSF was studied with humans. Six patients with occlusive hydrocephalus caused by cerebrovascular diseases who had undergone external ventriculostomy received 400 mg of ofloxacin i.v. over 30 min. Serum and CSF samples were drawn repeatedly. Serum from 12 healthy volunteers was sampled repeatedly after they had received 400 mg of ofloxacin i.v. over 60 min. Ofloxacin, ofloxacin-N-oxide, and N-desmethyl-ofloxacin concentrations were determined by high-pressure liquid chromatography with fluorescence detection. The maximum ofloxacin concentrations in the serum of the patients ranged from 7.36 to 11.6 mg/liter (mean, 9.55 mg/liter), the apparent volume of distribution/body weight was 0.96 to 1.19 liters/kg (mean, 1.11 liters/kg), and the total body clearance was 115 to 280 ml/min (mean, 192 ml/min). In healthy volunteers, the volume of distribution/body weight and the total body clearance were higher and amounted to 1.27 +/- 0.18 liters/kg and 217 +/- 43 ml/min (means +/- standard deviations), respectively. These differences were attributed to the older ages of the patients than the volunteers. In the CSF of patients, maximum concentrations of 1.00 to 2.85 mg/liter (mean, 2.04 mg/liter) were observed 0.5 to 4 h following the completion of the ofloxacin infusion. Ofloxacin elimination from CSF was slightly slower than that from serum (half-lives, 4.33 to 10.02 versus 4.27 to 9.14 h). The overall penetration of ofloxacin into CSF, as expressed by the ratios of the areas under the concentration-curves, amounted to 0.59 to 0.81 (mean, 0.65). The more hydrophilic metabolites ofloxacin-N-oxide and N-desmethyl-ofloxacin passed less readily than ofloxacin into the CSF. In conclusion, the concentrations in CSF attained after a single i.v. infusion of 400 mg of ofloxacin in the absence of meningeal inflammation appear to be high enough to inhibit the growth of most staphylococci and members of the family Enterobacteriaceae, which are often involved in CSF shunt infection. Yet, in view of pharmacodynamic studies suggesting a peak concentration in CSF of at least 10-fold the MIC, the use of ofloxacin for central nervous systems infections is optimal only with highly susceptible pathogens (MIC, less than or equal to 0.12 mg/liter).

Aged↗
PubMed1994

North American (United States and Canada) comparative susceptibility of two fluoroquinolones: ofloxacin and ciprofloxacin. A 53-medical-center sample of spectra of activity. North American Ofloxacin Study Group.

Ofloxacin, a newer broad-spectrum fluoroquinolone, was evaluated against > 12,000 clinical isolates in a multicenter surveillance trial in the United States and Canada using the standardized disk diffusion method. A total of 53 geographically diverse clinical microbiology laboratories contributed zone diameter results for ofloxacin, ciprofloxacin, and norfloxacin for urinary tract infection (UTI) isolates; and ofloxacin and ciprofloxacin for respiratory tract infection (RTI) isolates, skin and soft tissue infection (SSTI) isolates, and genital tract pathogen isolates. In both the USA and Canada, ofloxacin was shown to have the wide spectrum of activity as follows: RTI isolates, ofloxacin (92.2%-93.8% susceptible) > ciprofloxacin (89.5%-90.4%); SSTI isolates, ofloxacin (87.1%-93.6%) > ciprofloxacin (78.8%-90.4%); UTI isolates, ofloxacin (91.6%-92.5%) > norfloxacin (87.3%-91.7%) > ciprofloxacin (86.4%-89.7%); and genital tract isolates, ofloxacin (94.0%) > ciprofloxacin (85.4%) (Canada only). US strains resistant to ofloxacin were confirmed by reference laboratory tests. Confirmed ofloxacin resistance, other than among staphylococci or nonenteric bacilli, was rare. The species most often found to be resistant to both ofloxacin and ciprofloxacin were methicillin-resistant staphylococci, Acinetobacter spp., and Enterococcus spp. From these contributing US and Canadian laboratory studies, ofloxacin appears to have a balanced spectrum of potential clinical use (91.8% susceptible aerobic isolates), particularly against Gram-positive pathogens and some species resistant to ciprofloxacin. The combined overall isolate (12,241 isolates) rates of susceptibility for ciprofloxacin (four infection sites) and norfloxacin (UTI only) were 87.3% and 88.8%, respectively. Monitoring for increasing fluoroquinolone resistance should be considered, however, as greater use of drugs in this class develops.

Bacteria↗
PubMed1992

Multiple dose kinetics of ofloxacin and ofloxacin metabolites in haemodialysis patients.

7 patients with end-stage renal disease on regular haemodialysis were treated orally with a loading dose of 200 mg ofloxacin and multiple maintenance doses of 100 mg per 24 h for 10 days. The pharmacokinetics of ofloxacin and its metabolites were studied at the end of the treatment period. Plasma and dialysate concentrations of ofloxacin and ofloxacin metabolites were measured by HPLC. Peak (3.1 mg.l-1) and trough levels (1.6 mg.l-1) and the AUC of ofloxacin were comparable to the values in healthy volunteers given 300 to 400 mg ofloxacin p.o. The mean half-life, determined in the dialysis-free interval (t1/2 beta) and during the haemodialysis session (t1/2 HD), was 38.5 h and 9.9 h, respectively. Extrarenal clearance (32.7 ml.min-1) was unchanged as compared to that reported in healthy volunteers after a single dose of ofloxacin. The fractional removal by haemodialysis amounted to 21.5%. Two metabolites, ofloxacin-N-oxide and demethyl-ofloxacin, were detected in plasma. Despite prolonged t1/2 beta of both metabolites (66.1 and 50.9 h) and multiple doses of ofloxacin the peak concentrations of the metabolites reached only 14% and 5% of that of the parent drug, respectively. It is concluded that in patients on regular haemodialysis treatment the dosage adjustment employed resulted in safe and therapeutically favourable plasma concentrations. The observed accumulation of ofloxacin metabolites does not appear to have any toxic or therapeutic significance.

Adult↗
PubMed2000

Epithelial healing rates with topical ciprofloxacin, ofloxacin, and ofloxacin with artificial tears after photorefractive keratectomy.

PURPOSE: To determine whether corneal epithelial healing differs after the use of topical ciprofloxacin alone, topical ofloxacin alone, or topical ofloxacin with artificial tears in patients having photorefractive keratectomy (PRK). SETTING: Department of Ophthalmology and Visual Science, The University of Texas Health Science Center at Houston, Houston, Texas, USA. METHODS: Eighteen patients (6 women, 12 men) with moderate myopia (-1.50 to -6.00 diopters [D]) had standardized PRK. Patient age ranged from 25 to 62 years. The 28 eyes (16 right, 12 left) were randomized into 3 treatment groups: ofloxacin alone, n = 9 eyes; ciprofloxacin, n = 9 eyes; and ofloxacin with Refresh Plus, n = 10 eyes. The drugs were administered immediately after surgery and then every 6 hours. Video recordings of the corneal wounds stained with fluorescein were performed at 8:00 AM and 4:00 PM using a video slitlamp camera with a cobalt-blue light until the wound completely healed. The videotaped images were recorded and analyzed by a computer planimetry program. Wound areas were recorded and compared among the 3 drugs. The square-root transformation was applied to the wound area to obtain a constant healing rate. Statistical comparisons were analyzed using an analysis of variance test. RESULTS: Mean recovery time was 82.67 hours +/- 14.42 (SD) in the ofloxacin eyes, 120.89 +/- 34.05 hours in the ciprofloxacin eyes, and 76.80 +/- 19.30 hours in the ofloxacin with Refresh Plus eyes. Mean healing rate was 0.66 +/- 0.17 hours, 0.54 +/- 0.16 hours, and 0.67 +/- 0.15 hours, respectively. The healing rate was significantly higher in the ofloxacin with Refresh Plus eyes than in the ciprofloxacin eyes (P < .0001). There was no significant difference between the ofloxacin eyes and the ofloxacin with Refresh Plus eyes (P = .42). CONCLUSION: Ofloxacin with Refresh Plus and ofloxacin alone had a more positive effect on epithelial healing than ciprofloxacin. The ciprofloxacin eyes were significantly more prone to impaired or delayed wound healing and to the development of corneal haze.

Administration, Topical↗
PubMed1997

Single Dose Ofloxacin plus Loperamide Compared with Single Dose or Three Days of Ofloxacin in the Treatment of Traveler's Diarrhea.

Background: Although the use of the antimicrobial, trimethoprim-sulfamethoxazole, in combination with the antisecretory and antimotility agent, loperamide, has been shown to be efficacious in the treatment of traveler's diarrhea, the use of fluoroquinolone antimicrobials in combination with loperamide has less support in the literature. The present study was designed to compare the efficacy of ofloxacin versus ofloxacin plus loperamide in the treatment of acute traveler's diarrhea. Method: This prospective, randomized, evaluator-blinded treatment trial was conducted in Guadalajara, Mexico, during the summers of 1992-1994. Adults newly arrived in Mexico from the United States who developed acute diarrhea of less than 2 weeks' duration were randomized to receive orally either: A) ofloxacin, 400 mg once; B) ofloxacin, 200 mg twice a day for six doses; or C) ofloxacin, 400 mg once, plus loperamide, 4 mg once followed by 2 mg after each loose stool, not to exceed 16 mg per day, for 3 days. The duration of illness was the number of hours elapsed from the beginning of therapy to the passage of the last unformed stool. Results: Ofloxacin and loperamide were well tolerated. Combination therapy with single dose ofloxacin plus loperamide was significantly more efficacious in reducing the duration of diarrhea than single dose ofloxacin or ofloxacin given for 3 days (p <.00001). Furthermore, combination therapy was more efficacious when enterotoxigenic Escherichia coli (ETEC) was the pathogen (p <.01) or when no pathogen was isolated (p <.001). Sixty-three percent of subjects passed no further unformed stools after the initial doses of combination therapy, and 91% were well by the end of the first 24 hours. Conclusions: The combined use of a single dose of ofloxacin with loperamide is safe and more efficacious in the treatment of traveler's diarrhea than use of ofloxacin alone.

Journal Article↗
PubMed1994

The determination of ofloxacin in human skin tissue by high-performance liquid chromatography and correlation between skin tissue concentration and serum level of ofloxacin.

A simple high-performance liquid chromatographic (HPLC) assay was developed for the measurement of ofloxacin in skin tissue, and the correlation between serum levels and skin tissue levels of ofloxacin was determined. The homogenized skin samples were directly introduced into an HPLC system after filtering through a Molcut II membrane filter to remove proteins. The filtrate was concentration on a pre-column using a phenyl-stationary phase and was then introduced to an analytical column using an ODS-stationary phase by column-switching techniques. Ofloxacin and lomefloxacin as an internal standard were detected by UV absorbance at 300 nm. Determination was possible for ofloxacin over the concentrated range 250-3000 ng (g skin tissue)-1; the limit of detection was 100 ng g-1. The absolute recovery of ofloxacin added to skin tissue homogenate was over 72% with a coefficient of variation of less than 4.1%. This method is applied to determination of skin tissue level of ofloxacin in patients after treatment with ofloxacin. The correlation between serum levels and skin tissue levels of ofloxacin was determined for 30 patients after oral administration of ofloxacin. Good correlation was obtained and the coefficient of correlation was 0.84.

Administration, Oral↗
PubMed2000

Concentration of ofloxacin in canine prostate tissue and prostate fluid after intraprostatic injection of biodegradable sustained-releasing microspheres containing ofloxacin.

PURPOSE: Excellent treatment results in chronic prostatitis by direct intra-prostatic injection of antibiotic were reported several decades ago with only minimal scientific background. We examined the distribution, in prostatic tissue and fluid, of the antibiotic in canines after intra-prostatic injection of biodegradable sustained-releasing microspheres containing 12 mg. of ofloxacin. MATERIALS AND METHODS: A total of 36 male dogs, 12 controls and 24 experimental, older than 2 years, were used. Experimental dogs were given biodegradable sustained releasing microspheres containing ofloxacin 12 mg. and poly(D,L-lactic) acid 28 mg., designed to release over more than a 4 week period. The 12 control animals were divided into 2 groups, and oral ofloxacin 100 mg. was given twice a day for 2 and 4 weeks. The 24 experimental animals were divided into 4 subgroups of 6 dogs each, 4 for prostatic tissue and 2 for prostatic fluid level of ofloxacin determination. Anesthesia was initiated with ketamine HCl and xylazine, and maintained with intermittent ketamine HCl. In the experimental groups, 1 ml. of resolved formula was injected into one lobe of surgically exposed prostates. The concentration of ofloxacin was measured by high performance liquid chromatography (HPLC) of blood, prostatic tissue and prostatic fluid. Pilocarpine 0.5 mg./kg. was used for the collection of the prostatic fluid. RESULTS: The total ofloxacin of controls were 2,800 (2 weeks) and 5,600 (4 weeks) mg. In control groups, tissue concentrations of ofloxacin were relatively even at all segments of prostate, 7.4 +/- 0.8 (2 weeks) and 9.2 +/- 1.1 microg./ml. (4 weeks). The blood level ranged between 3.6 to 5.1 microg./ml. The prostatic fluid level ranged from 3.1 to 5.7 microg. /ml. In the experimental groups, the tissue levels of ofloxacin were 10.5 +/- 3.0 (1 week), 13.8 +/- 4.5 (2 weeks), 7.1 +/- 0.9 (3 weeks) and 7.7 +/- 3.0 microg./ml. (4 weeks) in the injected lobe. The opposite lobes were 8.0 +/- 1.1 (1 week), 10.2 +/- 4.2 (2 weeks), 5. 1 +/- 1.4 (3 weeks) and 7.6 +/- 0.8 (4 weeks) microg./ml. The blood level in the experimental groups ranged between 0.16 to 0.59 microg./ml. The prostate fluid level ranged from 2.9 to 6.1 microg./ml. in 8 dogs. Upon pathologic examination, the microspheres were interposed between prostate stroma and their size was reduced over time. CONCLUSIONS: Our study indicates that there is communication between the right and left prostate lobes. Direct injection of biodegradable sustained releasing ofloxacin formula into the prostate may be a substitute for long term antibiotic medication in humans for chronic prostatitis in the future without hurting the minimal inhibitory concentration(MIC)90.

Animals↗
PubMed1998

Effect of subinhibitory concentrations of vancomycin, cefazolin, ofloxacin, L-ofloxacin and D-ofloxacin on adherence to intravascular catheters and biofilm formation by Staphylococcus epidermidis.

Staphylococcus epidermidis is the preeminent cause of nosocomial bacteraemia and infection of prosthetic medical devices. Bacterial adherence to biomaterial is a crucial early event in the pathogenesis of these infections. Antibiotics affect bacterial adherence to eukaryotic cells, capsule formation and biofilm production. However, results from studies involving coagulase-negative staphylococci are equivocal. In this study, the in-vitro adherence of radiolabelled bacteria was assayed to determine the effect of sublethal concentrations of a number of antibiotics on the attachment of four strains of S. epidermidis, with well-characterized adherence profiles, to intravascular catheters. The effect of antibiotics on biofilm production by S. epidermidis was assayed using a quantitative spectrophotometric assay. Although there was some strain-to-strain variability, none of the tested antibiotics affected bacterial attachment. However, treatment with cefazolin or vancomycin resulted in a significant decrease in biofilm elaboration. These data suggest that bacterial attachment by S. epidermidis, the initiating event associated with prosthetic device infection, cannot be prevented by subtherapeutic levels of fluoroquinolone, glycopeptide or beta-lactam antibiotics. However, later aggregative stages of adherence, associated with biofilm production, may be influenced by cell wall-active agents such as cefazolin and vancomycin.

Bacterial Adhesion↗
PubMed2006

In vivo selection during ofloxacin therapy of Escherichia coli with combined topoisomerase mutations that confer high resistance to ofloxacin but susceptibility to nalidixic acid.

OBJECTIVES: To investigate quinolone resistance mechanisms in an Escherichia coli clinical isolate (Ar2) resistant to ofloxacin but susceptible to nalidixic acid selected after 10 days of ofloxacin therapy in a patient with prostatitis. METHODS: Molecular typing (ERIC-PCR and RAPD), antibiotic susceptibility and gyrA, gyrB, parC and parE QRDR sequences were compared for E. coli Ar2 and a wild-type E. coli (Ar1) isolated 2 months earlier in the same patient. Ofloxacin-resistant mutants were selected in vitro in order to reproduce the mutations observed and the original phenotype. RESULTS: The two strains were similar with regard to antibiotic susceptibility except quinolones and for ERIC-PCR and RAPD patterns, suggesting a clonal relationship and acquisition of quinolone resistance by chromosomal mutation. Quinolone MICs were 3, 0.12, 0.05 and 0.02 mg/L of nalidixic acid, ofloxacin, levofloxacin and ciprofloxacin, respectively, for E. coli Ar1 and 6, 32, 8 and 1 mg/L, respectively, for E. coli Ar2. The strain Ar2 harboured two substitutions, Gly-81-->Asp in GyrA and Ser-80-->Arg in ParC. Introduction into E. coli Ar2 of the wild-type gyrA fully complemented fluoroquinolone resistance. Although the strain was not a hypermutator, ofloxacin first-step resistant mutants with gyrA mutations were easily obtained from E. coli Ar1 and 25% of them were at codon 81. In vitro stepwise combination of Gly-81-->Asp in GyrA and Ser-80-->Arg in ParC reproduced the original phenotype in E. coli KL16. CONCLUSIONS: A double topoisomerase mutant was selected in vivo by 10 days ofloxacin. The mutations were originally combined for a result of ofloxacin resistance but nalidixic acid susceptibility.

Aged↗
PubMed1996

Column-switching high-performance liquid chromatography of ofloxacin in human saliva and correlation of ofloxacin level in saliva and serum.

A column-switching high-performance liquid chromatography (HPLC) assay was developed for the determination of ofloxacin in saliva. The saliva samples were directly introduced into a C8 HPLC column using a C18 precolumn. Ofloxacin and lomefloxacin as internal standards were detected spectrophotometrically at 300 nm. Determination of ofloxacin was possible in the concentration range 50-3,000 ng/ml, and the limit of detection was 20 ng/ ml. The recovery of ofloxacin added to saliva was 96.9-101.2% with a coefficient of variation of < 2.9%. These pharmacokinetic studies were made of healthy volunteers after treatment with ofloxacin. The maximum concentration of saliva and serum ofloxacin was 513.3-2,053.0 ng/ml and 768.2-3,089.0 ng/ml for dose of 100 mg or 200 mg, respectively. The AUC0-6 was 1,736.8-6,519.9 ng/h/ml in saliva and 2,875.5-10,086.0 ng/h/ml in serum, respectively. The saliva versus serum concentration ratio was 0.4-0.7 for doses of 100 and 200 mg. A good correlation between saliva and serum level of ofloxacin was obtained by this HPLC method (r = 0.949).

Anti-Infective Agents↗
PubMed2006

Randomized controlled comparison of ofloxacin, azithromycin, and an ofloxacin-azithromycin combination for treatment of multidrug-resistant and nalidixic acid-resistant typhoid fever.

Isolates of Salmonella enterica serovar Typhi that are multidrug resistant (MDR, resistant to chloramphenicol, ampicillin, and trimethoprim-sulfamethoxazole) and have reduced susceptibility to fluoroquinolones (nalidixic acid resistant, Na(r)) are common in Asia. The optimum treatment for infections caused by such isolates is not established. This study compared different antimicrobial regimens for the treatment of MDR/Na(r) typhoid fever. Vietnamese children and adults with uncomplicated typhoid fever were entered into an open randomized controlled trial. Ofloxacin (20 mg/kg of body weight/day for 7 days), azithromycin (10 mg/kg/day for 7 days), and ofloxacin (15 mg/kg/day for 7 days) combined with azithromycin (10 mg/kg/day for the first 3 days) were compared. Of the 241 enrolled patients, 187 were eligible for analysis (186 S. enterica serovar Typhi, 1 Salmonella enterica serovar Paratyphi A). Eighty-seven percent (163/187) of the patients were children; of the S. enterica serovar Typhi isolates, 88% (165/187) were MDR and 93% (173/187) were Na(r). The clinical cure rate was 64% (40/63) with ofloxacin, 76% (47/62) with ofloxacin-azithromycin, and 82% (51/62) with azithromycin (P = 0.053). The mean (95% confidence interval [CI]) fever clearance time for patients treated with azithromycin (5.8 days [5.1 to 6.5 days]) was shorter than that for patients treated with ofloxacin-azithromycin (7.1 days [6.2 to 8.1 days]) and ofloxacin (8.2 days [7.2 to 9.2 days]) (P < 0.001). Positive fecal carriage immediately posttreatment was detected in 19.4% (12/62) of patients treated with ofloxacin, 6.5% (4/62) of those treated with the combination, and 1.6% (1/62) of those treated with azithromycin (P = 0.006). Both antibiotics were well tolerated. Uncomplicated typhoid fever due to isolates of MDR S. enterica serovar Typhi with reduced susceptibility to fluoroquinolones (Na(r)) can be successfully treated with a 7-day course of azithromycin.

Adolescent↗
PubMed1991

[Therapeutic effect of ofloxacin on intractable pulmonary tuberculosis and ofloxacin resistance of tubercle bacilli isolated from the patients. Chest DIsease Cooperative Study Unit of National Sanatoriums in Kinki District].

Ofloxacin, a synthetic antibacterial pyridone-carboxylic acid derivative, was used in the treatment of intractable pulmonary tuberculosis. In this study, the therapeutic effect of Ofloxacin on pulmonary tuberculosis and Ofloxacin resistance were analyzed. All patients had been hospitalized in eight national sanatoria in Kinki district, and were excreting tubercle bacilli resistant to various anti-tuberculosis drugs agents. Ofloxacin was given to 118 patients orally at a daily dose of 300 mg to 600 mg for more than 3 months. A few anti-tuberculosis drugs, which had failed in the negative conversion of bacilli previously, were used in combination. By Ofloxacin, 23 patients (19.5%) showed negative conversion of tubercle bacilli in sputum culture within 5 months, and they remained culture-negative for at least 6 months after conversion. Side-effects were observed in 2 patients. One complained of arthralgia and the other felt abdominal fullness. But both were not serious. From these results, it was concluded that Ofloxacin was effective for intractable pulmonary tuberculosis. The resistance of tubercle bacilli to Ofloxacin increased significantly after it was used.

Adult↗
PubMed1992

Ofloxacin, a new broad-spectrum fluoroquinolone. Results from a Multicenter, National Comparative Activity Surveillance Study. The Ofloxacin Surveillance Group.

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.

Anti-Infective Agents↗
PubMed1991

Effect of antimicrobial agents on the uptake of ofloxacin and its optically active isomer (-)-ofloxacin by human polymorphonuclear leucocytes.

The effect of several antimicrobial agents, active against Gram-positive cocci, anaerobes or fungi on the intracellular penetration of ofloxacin and its optically active isomer (-)-ofloxacin into human polymorphonuclear leucocytes (PMNs) was studied. In the presence of therapeutic extracellular concentrations of these drugs, both ofloxacin and (-)-ofloxacin reached high intracellular concentrations (cellular to extracellular ratio (C/E greater than 3). Ofloxacin and (-)-ofloxacin uptake by PMNs was higher when cells were stimulated with opsonized zymosan (C/E greater than 5). It is concluded that none of the antimicrobial agents studied significantly affected the uptake of both quinolones by human PMNs.

Anti-Bacterial Agents↗
PubMed1999

In-vitro activity of levofloxacin, ofloxacin and D-ofloxacin against coryneform bacteria and Listeria monocytogenes.

The objective of this study was to evaluate the in-vitro activity of levofloxacin, ofloxacin and D-ofloxacin compared with ciprofloxacin, norfloxacin and sparfloxacin against coryneform bacteria and Listeria monocytogenes isolated from clinical samples. The following organisms (and number of strains) were studied: Corynebacterium jeikeium (20), Corynebacterium urealyticum (20), Corynebacterium minutissimum (20), Corynebacterium striatum (20), Corynebacterium amycolatum (30), Brevibacterium spp. (15) and Listeria monocytogenes (15). Antimicrobial activity was determined by microdilution using cation-adjusted Mueller-Hinton broth supplemented with 0.5% Tween 80 when testing C. jeikeium or C. urealyticum. Fluoroquinolones were used in the range 0.015-16 mg/L. Plates were incubated in air at 35 degrees C for 18-20 h (24 h when testing C. jeikeium or C. urealyticum). The following MIC50 values were obtained for all 140 organisms tested: levofloxacin, 1 mg/L; ofloxacin, 2 mg/L; D-ofloxacin, > 16 mg/L; ciprofloxacin, 1 mg/L; norfloxacin, 16 mg/L; sparfloxacin, 1 mg/L. MIC90 values were > 16 mg/L for all test antibiotics with the exception of levofloxacin, which had an MIC90 value of 16 mg/L. At a concentration of 2 mg/L, levofloxacin inhibited all L. monocytogenes strains and 35-93% of the remaining species. MIC90 values of ofloxacin were one dilution step higher than those of levofloxacin against C. minutissimum, C. striatum, Brevibacterium spp. and L. monocytogenes. Levofloxacin showed similar (C. jeikeium, C. urealyticum, C. amycolatum and Brevibacterium spp.) or greater (C. minutissimum and C. striatum) activity than ciprofloxacin and sparfloxacin, and higher than D-ofloxacin or norfloxacin against all species studied. In conclusion, levofloxacin was the most active of the six fluoroquinolones evaluated against coryneform bacteria isolated from clinical samples and could therefore be a promising treatment option in this setting.

Anti-Infective Agents↗