Absence of age and gender effects on the pharmacokinetics of a single 500-milligram oral dose of levofloxacin in healthy subjects

Abstract

The influence of age and gender on the pharmacokinetics of levofloxacin in healthy subjects receiving a single oral 500-mg dose of levofloxacin was investigated in this parallel design study. Six young males (aged 18 to 40 years), six elderly males (aged > or = 65 years), six young females (aged 18 to 40 years), and six elderly females (aged > or = 65 years) were enrolled and completed the study. The study reveals that the bioavailability (rate and extent) of levofloxacin was not affected by either age or gender. In both age (young and elderly) and gender (male and female) groups of subjects, peak concentrations in plasma were reached at approximately 1.5 h after dosing; renal clearance of levofloxacin accounted for approximately 77% of total body clearance, and approximately 76% of the administered dose was recovered unchanged in urine over the 36 h of collection. The apparent differences in the calculated pharmacokinetic parameters for levofloxacin between the age groups (young versus elderly) and between the gender groups (males versus females) could be explained by differences in renal function among the subjects. A single dose of 500 mg of levofloxacin administered orally to both young and old, male and female healthy subjects was found to be safe and well tolerated. As the differences in levofloxacin kinetics between the young and the elderly or the males and the females are limited and are mainly related to the renal function of the subjects, dose adjustment based on age or gender alone is not necessary.

Levofloxacin can be used effectively as a positive control in thorough QT/QTc studies in healthy volunteers

“…Mean exposure (AUC 24 ) was approximately 150 µg h −1 ml −1 (Table 2). Levofloxacin parameters observed in this study were in the same range as those presented in the literature [9, 19, 20].…”

Influence of Morbid Obesity on the Clinical Pharmacokinetics of Various Anti-Infective Drugs: Reappraisal Using Recent Case Studies—Issues, Dosing Implications, and Considerations

“…Similarities in the pharmacokinetics were observed for parameters such as peak concentration and V D for levofloxacin between morbidly obese and ambulatory patients; such data were comparable with other patient pool including healthy volunteers [33][34][35] However, morbidly obese patients seemed to have a slower CL of levofloxacin leading to a considerably higher exposure of the drug and shorter half-life values when compared with the ambulatory patients (2.6 vs. 6.9 hours in morbidly obese and ambulatory, respectively). As suggested by Figures 1, 2, 32,33,35 the V SS and CL for levofloxacin seemed to be at the lower end of the values observed for nonobese subjects suggesting that BW consideration may need to be factored in dosing decisions for morbidly obese patients.…”

Pharmacokinetics of levofloxacin after single and multiple oral doses in patients undergoing intermittent haemodialysis

“…Levofloxacin has 99% oral availability, with adequate penetration into tissues and body fluids; the maximum concentration ranges between 5 mg/L and 7 mg/L in healthy subjects after a single 500 mg oral or intravenous dose and between 6 mg/L and 9 mg/L following multiple doses [4,5]. The maximum concentration is observed 1-2 h after oral administration; however, factors such as age, gender and concomitant food intake appear to influence the extent of absorption [6,7].…”