This paper reports an open label study of the pharmacokinetics of ofloxacin conducted on 12 Vietnamese healthy volunteers (4 females, 8 males). Oflaxacin was adminitered as an oral tablet presentation. The mean peak concentration was 2.270.53 mg.liter-1, occuring at 1.300.31h after dosing. The AUCo-24was 16.532.02mg.h.liter-1, the half-time was 5.040.44h and the volume of distribution was 1.120.18 liter.kg-1. Results collected from this study were similar to those of previous studies.
Pharmacokinetics ; Ofloxacin ; tablets\

Turtle-borne Salmonella enterica owns significance as a leading cause in human salmonellosis. The current study aimed to determine the quinolone susceptibility and the genetic characteristics of 21 strains of S. enterica subsp. enterica isolated from pet turtles. Susceptibility of four antimicrobials including nalidixic acid, ciprofloxacin, ofloxacin, and levofloxacin was examined in disk diffusion and MIC tests where the majority of the isolates were susceptible to all tested quinolones. In genetic characterization, none of the isolates were positive for qnr or aac(6')-Ib genes and no any target site mutations could be detected in gyrA, gyrB, and parC quinolone resistance determining regions (QRDR). In addition, neighbor-joining phylogenetic tree derived using gyrA gene sequences exhibited two distinct clads comprising; first, current study isolates, and second, quinolone-resistant isolates of human and animal origin. All results suggest that studied strains of S. enterica subsp. enterica isolated from pet turtles are susceptible to quinolones and genetically more conserved with regards to gyrA gene region.
Animals ; Ciprofloxacin ; Diffusion ; Humans ; Levofloxacin ; Nalidixic Acid ; Ofloxacin ; Quinolones ; Salmonella enterica* ; Salmonella Infections ; Salmonella* ; Trees ; Turtles*

BACKGROUND: Fluoroquinolones (FQs) are important drugs for treating multidrug-resistant tuberculosis (MDR-TB). However, due to widespread use of FQs, the resistance rates to FQs have been increasing among Mycobacterium tuberculosis. Rapid and reliable FQ drug susceptibility testing (DST) is crucial for successful treatment of MDR-TB. In this study, the feasibility of molecular detection of FQ resistance was evaluated. METHODS: A total of 95 MDR-TB isolates were collected from Jan through Oct 2009 at the Korean Institute of Tuberculosis. DST for ofloxacin (OFL), levofloxacin, and moxifloxacin was performed using the Lowenstein-Jensen media absolute concentration method. Minimum inhibitory concentrations (MIC) of these were determined using the broth microdilution method. DNA was extracted from cultured isolates using bead beating method. The quinolone resistance-determining region (QRDR) of gyrA and gyrB were amplified and those sequences were analyzed. RESULTS: Of 95 isolates, 79 were resistant to at least one of FQs. Of these, 71 (89.9%) harbored mutation in the QRDR of gyrA or gyrB. None of FQ susceptible strains possessed any mutation in gyrA or gyrB. Mutations in codon 94 of gyrA were most common; only two isolates had mutation in only the gyrB gene. OFL MICs for isolates with gyrA mutation ranged from 1 to 32 microg/mL, but FQ susceptible isolates showed MICs ranging from < or =0.06 to 0.5 microg/mL. CONCLUSION: Mutation analysis of QRDR of gyrA and gyrB showed 89.9% sensitivity and 100% specificity for detecting FQ resistance in MDR-TB. Therefore, molecular DST can be useful for rapid detection of FQ resistance in MDR-TB.
Codon ; DNA ; Fluoroquinolones ; Levofloxacin ; Microbial Sensitivity Tests ; Mycobacterium tuberculosis* ; Ofloxacin ; Tuberculosis ; Tuberculosis, Multidrug-Resistant

Anaphylaxis have been documented as adverse effects of ciprofloxacin, ofloxacin, norfloxacin, levofloxacin, and moxifloxacin. However resistant and biphasic anaphlylactic reactions to gemifloxacin have not been reported to date. Management of severe anaphylaxis in the elderly can be complicated by concurrent medications such as beta (β) adrenergic, alpha (α) adrenergic blockers and angiotensin-converting enzyme (ACE) inhibitors. We report here in the case of a 60-year-old male who was taking on ACE inhibitor, α and β blockers and experienced a severe, resistant and biphasic anaphlylactic reaction to gemifloxacin mesylate.
Adrenergic Antagonists ; Aged ; Anaphylaxis ; Ciprofloxacin ; Humans ; Levofloxacin ; Male ; Mesylates ; Middle Aged ; Norfloxacin ; Ofloxacin

AIMTo learn the electrophysiological interference of levofloxacin (LVFX) to heart in guinea pig.

METHODSHigh, moderate and low doses of LVFX were given to the anesthetic guinea pig via i.p., and QT interval span and corrected QT-interval span in the II leading lines of ECG were recorded and analyzed from 5 min to 360 min after the drug administration. Single ventricular myocytes were obtained and impacted by LVFX solution of different concentrations. Then delayed rectifier potassium currents (I(K)) on single cells were recorded with whole-cell patch clamp technique, and compared with control group(without impact of LVFX).

RESULTS(1) After the administration of LVFX, at the dose of 200 mg/kg. QT-interval span was significantly elongated, and the increasing rate is 19.38% +/- 3.15% (P < 0.05). While at the relatively lower doses of 50 mg/kg and 100 mg/kg, the elongation is of low/no significance (P > 0.05). (2) LVFX inhibited I(K) dose-dependently and time-dependently.

CONCLUSIONLVFX might prolong the QT-interval span by the mechanism of inhibiting I(K), which implies a potential risk in clinical application.

Animals ; Guinea Pigs ; Levofloxacin ; Membrane Potentials ; Myocytes, Cardiac ; drug effects ; physiology ; Ofloxacin ; pharmacology ; Patch-Clamp Techniques

OBJECTIVETo study the therapeutic efficacy of Longqingpian combined with Levofloxacin on Type IIIA prostatitis.

METHODSEighty patients with Type IIIA prostatitis were equally randomized into a Longqingpian group and a Puleanpian group, both treated for 12 weeks. The former were given Longqingpian (once 6 tablets, twice a day) combined with Levofloxacin (once 0.2 g, twice a day) during the first 4 weeks, followed by Longqingpian alone (once 6 tablets, twice a day) for 8 weeks. The latter received Puleanpian (once 4 tablets, 3 times a day) combined with Levofloxacin (once 0.2 g, twice a day) in the initial 4 weeks, followed by Puleanpian alone (once 4 tablets, 3 times a day) for 8 weeks. Before and 4, 8, and 12 weeks after the treatment, all the patients were evaluated by The National Institutes of Health Chronic Prostatitis Symptom Index (NIH-CPSI) and EPS examination.

RESULTSAfter 4-week, 8-week and 12-week treatment, total score of NIH-CPSI, and the score of pain, voiding symptoms and the quality of life dropped significantly in both groups compared with pre-treatment (P < 0.05 or 0.01), so did the leukocyte count in EPS (P < 0.05). Compared with the 4-week treatment, total score of NIH-CPSI, and the score of pain, voiding symptoms and the quality of life were shown to be significantly different (P < 0.05) in the Longqingpian group from the 8-week and 12-week treatment, except the leukocyte count in EPS. However, there was no significant difference between the 8-week and 12-week treatment in any of the indexes (P > 0.05). Longqingpian effected significant differences in the above indexes (P < 0.05), while Puleanpian did not after the treatment (P > 0.05). And the lecithin Amato body analysis revealed no significant changes in EPS after the treatment in either group (P > 0.05).

CONCLUSIONLongqingpian combined with Levofloxacin is highly effective for Type IIIA prostatitis, by relieving pain and voiding symptoms, decreasing the leukocyte count in EPS and improving the life quality of the patients.

Adult ; Chronic Disease ; Humans ; Levofloxacin ; Male ; Middle Aged ; Ofloxacin ; therapeutic use ; Phytotherapy ; Prostatitis ; drug therapy

The study aims to identify the degradation products of levofloxacin by HPLC-MS. The degradation products of levofloxacin were chromatographed on Agilent Zorbax Extend-C18 column (250 mm x 4.6 mm, 5 microm). The mobile phase was 0.1% ammonium acetate solution (using methanoic acid to adjust to pH 3.5)-acetonitrile at the flow rate of 0.5 mL x min(-1) (gradient elution), the column temperature was 40 degrees C. Descarboxyl levofloxacin, desmethyl levofloxacin and levofloxacin N-oxide were identified through comparing with the standard spectrum and the results of mass spectrometry, i.e. m/z 318.2 was descarboxyl levofloxacin, m/z 348.2 was desmethyl levofloxacin, m/z 378.1 was levofloxacin-N-oxide. This method is simple, fast, accurate and suitable for the identification of degradation products of levofloxacin.
Chromatography, High Pressure Liquid ; methods ; Drug Stability ; Levofloxacin ; Mass Spectrometry ; methods ; Ofloxacin ; analysis ; chemistry ; Photolysis

No abstract available.
Gram-Positive Cocci* ; Imipenem* ; Ofloxacin*

PURPOSE: Reports evaluating diagnosis and cross reactivity of quinolone hypersensitivity have revealed contradictory results. Furthermore, there are no reports investigating the cross-reactivity between gemifloxacin (GFX) and the others. We aimed to detect the usefulness of diagnostic tests of hypersensitivity reactions to quinolones and to evaluate the cross reactivity between different quinolones including the latest quinolone GFX. METHODS: We studied 54 patients (mean age 42.31±10.39 years; 47 female) with 57 hypersensitivity reactions due to different quinolones and 10 nonatopic quinolone tolerable control subjects. A detailed clinical history, skin test (ST), and single-blind placebo-controlled drug provocation test (SBPCDPT), as well as basophil activation test (BAT) and lymphocyte transformation test (LTT) were performed with the culprit and alternative quinolones including ciprofloxacin (CFX), moxifloxacin (MFX), levofloxacin (LFX), ofloxacin (OFX), and GFX. RESULTS: The majority (75.9%) of the patients reported immediate type reactions to various quinolones. The most common culprit drug was CFX (52.6%) and the most common reaction type was urticaria (26.3%). A quarter of the patients (24.1%) reacted to SBPCDPTs, although their STs were negative; while false ST positivity was 3.5% and ST/SBPCDPTs concordance was only 1.8%. Both BAT and LTT were not found useful in quinolone hypersensitivity. Cross-reactivity was primarily observed between LFX and OFX (50.0%), whereas it was the least between MFX and the others, and in GFX hypersensitive patients the degree of cross-reactivity to the other quinolones was 16.7%. CONCLUSIONS: These results suggest that STs, BAT, and LTT are not supportive in the diagnosis of a hypersensitivity reaction to quinolone as well as in the prediction of cross-reactivity. Drug provocation tests (DPTs) are necessary to identify both culprit and alternative quinolones.
Basophils ; Ciprofloxacin ; Diagnosis* ; Diagnostic Tests, Routine* ; Humans ; Hypersensitivity* ; In Vitro Techniques* ; Levofloxacin ; Lymphocyte Activation ; Ofloxacin ; Quinolones* ; Skin Tests ; Urticaria

BACKGROUND: Fluoroquinolone drugs are an important anti-tuberculous agent for the treatment of multi-drug resistant tuberculosis. However, many drugs belonging to the fluoroquinolones have different cross resistance to each other. METHODS: Sixty-three ofloxacin (OFX) resistant and 10 pan-susceptible M. tuberculosis isolates were selected, and compared for their cross resistance using a proportion method on Lowenstein-Jensen media, containing ofloxacin (OFX), ciprofloxacin (CIP), levofloxacin (LVX), moxifloxacin (MXF), gatifloxacin (GAT) and sparfloxacin (SPX), at concentrations ranging from 0.5 to 3microgram/ml. DNA extracted from the isolates was directly sequenced after amplifying from the gyrA and gyrB genes. RESULTS: The 63 OFX resistant M. tuberculosis isolates showed complete cross resistance to CIP, but only 90.5, 44.4, 36.5 and 46.0% to LVX, MXF, GAT, and to SPX, respectively. Fifty-one of the isolates (81.0%) had point mutations in codons 88, 90, 91 and 94 in gyrA, which are known to be correlated with OFX resistance. The Gly88Ala, Ala90Valand Asp94Ala mutations in gyrA showed a tendency to be susceptible to MXF, GAT and SPX. Only 4 isolates had mutations in the gyrB gene, which did not affect the OFX resistance. CONCLUSION: About 60% of the OFX resistant M. tuberculosis isolates were susceptible to GAT, SPX and MXF. These fluoroquinolones may be useful in the treatment of TB patients showing OFX resistance.
Ciprofloxacin ; Codon ; DNA ; Fluoroquinolones ; Genotype ; Humans ; Levofloxacin ; Mycobacterium tuberculosis* ; Mycobacterium* ; Ofloxacin ; Point Mutation ; Tuberculosis ; Tuberculosis, Multidrug-Resistant