Penetration of ciprofloxacin into human pleural fluid

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...

Section: Discussionmentioning

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

Kimura

Matsushima

Nakamura

et al. 1992

“…Although there are several studies (5)(6)(7)(8)(9) about ciprofloxacin (CIP) penetration in human pleural fluid (PF), data on MXF are scarce and are based on experimental pleural empyema in rabbits (10,11). On the basis of these data, MXF penetrates well into infected rabbit pleural fluid.…”

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Moxifloxacin Pharmacokinetics and Pleural Fluid Penetration in Patients with Pleural Effusion

Chatzika

Manika

Kontou

et al. 2014

The aim of this study was to evaluate the pharmacokinetics and penetration of moxifloxacin (MXF) in patients with various types of pleural effusion. Twelve patients with empyema/parapneumonic effusion (PPE) and 12 patients with malignant pleural effusion were enrolled in the study. A single-dose pharmacokinetic study was performed after intravenous administration of 400 mg MXF. Serial plasma (PL) and pleural fluid (PF) samples were collected during a 24-h time interval after drug administration. The MXF concentration in PL and PF was determined by high-performance liquid chromatography, and main pharmacokinetic parameters were estimated. Penetration of MXF in PF was determined by the ratio of the area under the concentration-time curve from time zero to 24 h (AUC 24 ) in PF (AUC 24PF ) to the AUC 24 in PL. No statistically significant differences in the pharmacokinetics in PL were observed between the two groups, despite the large interindividual variability in the volume of distribution, clearance, and elimination half-life. The maximum concentration in PF (Cmax PF ) in patients with empyema/PPE was 2.23 ؎ 1.31 mg/liter, and it was detected 7.50 ؎ 2.39 h after the initiation of the infusion. In patients with malignant effusion, Cmax PF was 2.96 ؎ 1.45 mg/liter, but it was observed significantly earlier, at 3.58 ؎ 1.38 h (P < 0.001). Both groups revealed similar values of AUC 24PF (31.83 ؎ 23.52 versus 32.81 ؎ 12.66 mg · h/liter). Penetration of MXF into PF was similarly good in both patient groups (1.11 ؎ 0.74 versus 1.17 ؎ 0.39). Despite similar plasma pharmacokinetics, patients with empyema/parapneumonic effusion showed a significant delay in achievement of PF maximum MXF levels compared to those with malignant effusion. However, in both groups, the degree of MXF PF penetration and the on-site drug exposure, expressed by AUC 24PF , did not differ according to the type of pleural effusion.

“…These studies, however, focused only on normal or noninfected material (4,5,11). Studies that examined the levels of these drugs in infected material seem more pertinent to clinical settings and have greater potential therapeutic implications (6,12).…”

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Ofloxacin penetration into tuberculous pleural effusion

Yew

Lee

Chan

et al. 1991

After 3 days of treatment with ofloxacin (300 mg given orally once daily), the drug levels in serum and pleural fluid 2 and 4 h after drug administration in patients with tuberculous pleural effusion were assessed by a rapid high-performance liquid chromatography assay. The levels in serum (mean standard error of the mean[SEM]) were 4.70 0.14 and 4.63 + 0.09 mg/liter 2 and 4 h after administration, respectively, and the levels in pleural fluid (mean SEM) were 3.82 + 0.09 and 4.21 0.08 mg/liter, respectively. The pleural fluid-to-serum ofloxacin ratio at 2 h was 0.82 0.02 (mean ± SEM), and the ratio at 4 h was 0.92 ± 0.02 (mean SEM). This study demonstrated very good penetration of ofloxacin into pleural fluid in tuberculous pleuritis.