A Preliminary Report on the Pharmacokinetics of Ofloxacin, Desmethyl Ofloxacin and Ofloxacin N-Oxide in Patients with Chronic Renal Failure

White, L. O.; MacGowan, A. P.; Lovering, A. M.; Reeves, D. S.; Mackay, I. G.

doi:10.2165/00003495-198700341-00013

Cited by 26 publications

(11 citation statements)

References 4 publications

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“…However, the results of this study indicate that the higher concentrations of quinolones in the circulation might be due to an inhibition of the hepatic microsomal drug metabolism enzyme activity. Norfloxacin, ofloxacin and pefloxacin are metabolized in this way, so the decrease in the rate of metabolism, under stress, may enhance the levels in plasma (34)(35)(36).…”

Section: Discussionmentioning

confidence: 99%

Changes in serum levels of quinolones in rats under the influence of experimental trauma

Trichilis¹,

Tesserommatis²,

Varonos³

2000

Eur. J. Drug Metab. Pharmacokinet.

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Administration of antibiotics is considered an important factor during, or after, operational procedures in the maxillofacial area, in order to avoid post-surgical complications. In the present study, the levels of quinolones in serum and tissues such as the parotid gland, the tongue and the bone of the jaws were estimated during traumatic injury in the oral cavity. For this purpose, two groups (A and B) of Wistar rats, consisting of 35 animals each were used. Group A (control) and group B (experimental) were divided in five subgroups (A1, A2, A3, A4, A5, and B1, B2, B3, B4, B5). In the experimental group, model traumatic injury was performed through the whole lenght of the cheek. Subjects received orally ciprofloxacin, pefloxacin, norfloxacin, ofloxacin and cinoxacin. The concentration of quinolones in serum and in most of the tissues was significantly higher in the experimental groups than in controls. In addition, the FFA levels and the weight of adrenals (as indicators of stress) were higher in the trauma groups. Stress seemed to affect many pathophysiological mechanisms which are responsible for the alterations observed.

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Section: Discussionmentioning

confidence: 99%

Changes in serum levels of quinolones in rats under the influence of experimental trauma

Trichilis¹,

Tesserommatis²,

Varonos³

2000

Eur. J. Drug Metab. Pharmacokinet.

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“…Serum samples were prepared by centrifuging the blood samples at 2,500 x g for 10 min and were stored at -20°C until analysis. Urine samples were collected in plastic bags before dosing and at 2,4,6,8,12,24, and 48 h after it. The volumes of the samples were measured immediately after collection, and the urine samples were stored at -20°C until analysis.…”

Section: Methodsmentioning

confidence: 99%

“…However, there exist species differences in OFLX glucuronidation, as the small amount of glucuronide excreted in urine by dogs and monkeys indicates (19). In humans, (±)-OFLX has been shown to undergo only limited metabolism with urinary excretion of small amounts of metabolites (desmethyl OFLX and OFLX N-oxide) and most of the administered drug is excreted unchanged in the urine (11,24,25).…”

mentioning

confidence: 99%

Enantioselective disposition of ofloxacin in humans

Okazaki

Kojima

Hakusui

et al. 1991

Antimicrob Agents Chemother

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The enantioselective disposition of ofloxacin (OFLX) was studied in healthy subjects after oral administration of (+/-)-OFLX at a dose of 200 mg. S-(-)-OFLX and R-(+)-OFLX concentrations in serum and urine were measured separately by high-performance liquid chromatography, and various pharmacokinetic parameters were calculated from the data. The ratio of S-(-) to R-(+) enantiomer concentrations in serum showed a increase with time, with S/R ratios of 1.01 at 2 h and 1.31 at 24 h. The terminal elimination half-life of S-(-)-OFLX was 6.9 h, which was significantly greater (P less than 0.05) than that of the R-(+) enantiomer (6.3 h). S-(-)-OFLX also revealed a significantly greater area under the concentration-time curve in serum, mean residence time, and total body clearance than the R-(+) enantiomer did. The renal clearance of S-(-)-OFLX (7.14 liters/h/1.73 m2) was significantly lower than that of the R-(+) enantiomer (7.53 liters/h/1.73 m2). Although the difference in the pharmacokinetic parameters of the enantiomers was small, their disposition in humans was found to be stereoselective. The difference between the enantiomers may be explained by the difference in their renal excretion.

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“…For instance, ofloxacin N-oxide possesses a weaker antibacterial activity against various bacterial strains such as Bacillus pumilus (minimum inhibitory concentration (MIC) > 20 mg L −1 ). 33 Compared to the parent compound (MIC = 0.675 mg L −1 ), the MIC for ofloxacin N-oxide is > 29-fold higher, and thus the metabolite is quite inactive. 33 Similar results have been reported for amifloxacin and its N-oxide.…”

Section: Journal Of Agricultural and Food Chemistrymentioning

confidence: 99%

Biotransformation of the Antibiotic Danofloxacin by Xylaria longipes Leads to an Efficient Reduction of Its Antibacterial Activity

Rusch

Kauschat

Spielmeyer

et al. 2015

J. Agric. Food Chem.

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Fluoroquinolones are considered as critically important antibiotics. However, they are used in appreciable quantities in veterinary medicine. Liquid manure and feces can contain substantial amounts of unmetabolized antibiotics and, thus, antibiotics can enter the environment if manure is used for soil fertilization. In this study, the microbial biotransformation of the synthetic veterinary fluoroquinolone danofloxacin by the ascomycete Xylaria longipes was investigated. Fungal submerged cultures led to a regioselective and almost quantitative formation of a single metabolite within 3 days. The metabolite was unequivocally identified as danofloxacin N-oxide by high-resolution mass spectrometry and one- and two-dimensional nuclear magnetic resonance spectroscopic techniques. An oxidation of the terminal nitrogen of the substituted piperazine moiety of the substance led to a remarkable reduction of 80% of the initial antibacterial activity. Thus, fungal enzymes involved in the biotransformation process might possess the potential to reduce the entrance of antibiotics via biotransformation of these compounds.

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A Preliminary Report on the Pharmacokinetics of Ofloxacin, Desmethyl Ofloxacin and Ofloxacin N-Oxide in Patients with Chronic Renal Failure

Cited by 26 publications

References 4 publications

Changes in serum levels of quinolones in rats under the influence of experimental trauma

Changes in serum levels of quinolones in rats under the influence of experimental trauma

Enantioselective disposition of ofloxacin in humans

Biotransformation of the Antibiotic Danofloxacin by Xylaria longipes Leads to an Efficient Reduction of Its Antibacterial Activity

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