In vitro and in vivo activity of NY-198, a new difluorinated quinolone

Hirose, Tohru; Okezaki, Eiichi; Kato, Hideo; Ito, Yoshihisa; Inoue, Matsuhisa; Mitsuhashi, Susumu

doi:10.1128/aac.31.6.854

Cited by 119 publications

(27 citation statements)

References 7 publications

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“…In vitro and in vivo experiments have demonstrated that lomefloxacin has a broad antibacterial spectrum, with particularly good activity against gram-negative aerobic bacteria and staphylococci (7,12). For example, the MICs for 90% of strains for the majority of the members of the family Enterobacteriaceae are .1 ,ug/ml.…”

Section: Discussionmentioning

confidence: 99%

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Pharmacokinetics and tissue penetration of orally administered lomefloxacin

Stone

Andrews

Ashby

et al. 1988

Antimicrob Agents Chemother

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The pharmacokinetics of the quinolone lomefloxacin were determined following a single 400-mg oral dose given to each of six male volunteers. Concentrations in serum, urine, and cantharidin-induced inflammatory fluid were determined by a microbiological assay. Samples from two volunteers were also assayed by high-performance liquid chromatography. The mean peak level in serum, 4.7 ,uglml, was attained within 1 h of administration. The mean elimination half-life from serum was 7 h. Inflammatory fluid was penetrated rapidly, with a mean peak level of 3.5 ,ug/ml occurring after 2.7 h. The mean recovery of lomefloxacin from urine over 48 h was 76% of the administered dose. There was a minor peak on the high-performance liquid chromatography trace, suggesting a small amount of unidentified metabolite. This was present only in urine; no detectable metabolites were found in serum. This study suggests that either once-daily or twice-daily dosage of lomefloxacin should be sufficient to treat urinary or systemic infections, respectively, caused by susceptible pathogens.

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Section: Discussionmentioning

confidence: 99%

“…It has been shown to have activity against both gram-negative and gram-positive bacteria including many strains that are multiply resistant to beta-lactam antibiotics and aminoglycosides (7,12). Its in vitro activity is similar to that of ofloxacin and norfloxacin.…”

mentioning

confidence: 85%

Pharmacokinetics and tissue penetration of orally administered lomefloxacin

Stone

Andrews

Ashby

et al. 1988

Antimicrob Agents Chemother

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“…Fluid for standards was prepared in 1/15 M phosphate buffer (pH 7.0). The half-lives of LFLX and CIRX were about 7.5 h. The protein-binding ratios of LFLX and CTRX are 20 and 95%, respectively (4,9). The molecular weights of LFLX and CrRX are 387.8 and 661.6, respectively.…”

Section: Methodsmentioning

confidence: 85%

“…In the present study, we investigated the pharmacokinetics of a new quinolone (LFLX) in exudative and transudative pleural fluids and the difference in pharmacokinetics between LFLX and a 1-lactam agent (CTRX). These drugs were chosen because they had almost the same half-lives in blood (4,9).…”

Section: Discussionmentioning

confidence: 99%

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Comparative study of penetration of lomefloxacin and ceftriaxone into transudative and exudative pleural effusion

Kimura

Matsushima

Nakamura

et al. 1992

Antimicrob Agents Chemother

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We investigated the transpieural penetration of lomefloxacin (LFLX) and ceftriaxone (CTRX). LFLX (200 mg) was administered orally to three patients with transudative fluid and four with exudative fluid, and 2 g of CTRX was administered by drip infusion to four patients with transudative fluid and three with exudative fluid. For both groups that received LFLX and CTRX, blood samples were drawn at time zero and 1, 2, and 6 h after drug administration. Thoracocentesis of each group was performed at 6 h after drug administration. The mean ratios of concentrations in pleural fluid/maximum concentrations in serum (P/S max) of LFLX were 66% in patients with transudative fluid and 69%o in patients with exudative fluid. The mean ratios of P/S max of CTRX were 9.1% in patients with transudative fluid and 13.5% in patients with exudative fluid. The P/S max ratios for the penetration of LFLX were five to six times higher than those for CTRX. In addition, there was less differentiation in concentrations of LFLX in pleural fluid between the transudative and exudative effisions than there was in the concentrations of CTRX.Although there have been many studies on the penetration of ,B-lactam agents into pleural fluid (1, 2), little attention has been given to the penetration of new quinolones into pleural fluid (5,8). In the study described here, we investigated the transpleural penetration of lomefloxacin (LFLX) and ceftriaxone (CTRX) by comparing the concentrations of both drugs in pleural fluid (transudative and exudative fluid). LFLX is a new quinolone antibacterial agent developed by Hokuriku Seiyaku Co., Ltd. CIRX is a 1-lactam agent developed by Kyorin Yakuhin Co., Ltd. These drugs were chosen because they had almost the same half-lives in blood (4, 9). MATERIALS AND METHODSFourteen patients with pleural fluid (nine males and five females; age range, 47 to 84 years; mean age, 71.6 years) who were admitted to our hospital between January 1989 and September 1990 were used for the present study (Table 1). Patients 5 and 6 in the LFLX group and patient 6 in the CTRX group were diagnosed histologically by pleural biopsy. Patient 7 in the LFLX group and patient 7 in the CTRX group are the same patient; the patient was diagnosed clinically. The study was carried out after receiving informed consent from all patients.We administered 200 mg of LFLX orally to three patients with transudative effusions and to four patients with exudative effusions. Two grams of CTRX in 100 ml of saline was administered by drip infusion to four patients with transudative effusions and to three patients with exudative effusions. In the LFLX group, blood samples was drawn at 1, 2, and 6 h after administration. In the CTRX group, they were drawn just after administration of CTRX and at the times mentioned above. Thoracocentesis of each group was performed 6 h after drug administration. All samples were centrifuged, and serum and pleural fluid supernatants were stored at -20°C until they were assayed. The concentrations of LFLX were determined by the hi...

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Bioequivalence evaluation of lomefloxacin 400 mg tablets (Lomax® Versus Maxaquin®) in healthy human volunteers

Al‐Rashood

Al-Khamis

El–Sayed

et al. 1999

Biopharm. Drug Dispos.

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This study represents the results of a randomized, single dose, two-treatment, two-period crossover study in 18 healthy male volunteers to assess the bioequivalence of two tablets of 400 mg lomefloxacin. The two formulations were: Lomax(R) (Julphar, United Arab Emirates) as the test formulation and Maxaquin(R) (Searle, S.A., UK) as the reference formulation. The study was conducted at the College of Pharmacy, King Saud University, Riyadh, Saudi Arabia, jointly with King Khalid University Hospital, Riyadh, Saudi Arabia. After overnight fasting the two products were administered as a single dose on two treatment days separated by a 1 week washout period. Serial blood samples were collected thereafter, for a period of 48 h. Plasma harvested from blood was analysed for lomefloxacin by a sensitive, reproducible and accurate HPLC method. Various pharmacokinetic parameters including AUC(0-t), AUC(0-infinity), C(max,) T(max), T(1/2), K(elm) and C(max)/AUC(0-infinity) were determined from plasma concentrations for both formulations and found to be in good agreement with reported values. Statistical modules applied to AUC(0-t), AUC(0-infinity) and C(max) revealed no significant difference in the two tested products. Based on these statistical inferences it was concluded that Lomax(R) is bioequivalent to Maxaquin(R).

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In vitro and in vivo activity of NY-198, a new difluorinated quinolone

Cited by 119 publications

References 7 publications

Pharmacokinetics and tissue penetration of orally administered lomefloxacin

Pharmacokinetics and tissue penetration of orally administered lomefloxacin

Comparative study of penetration of lomefloxacin and ceftriaxone into transudative and exudative pleural effusion

Bioequivalence evaluation of lomefloxacin 400 mg tablets (Lomax® Versus Maxaquin®) in healthy human volunteers

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