J Med Assoc Thai 1999; 82 (11):1127

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Pharmacokinetics of Levofloxacin in Healthy Thai Male Volunteers
Chulavatnatol S Mail, Chindavijak B , Vibhagool A , Wananukul W , Sriapha C , Sirisangtragul C

The pharmacokinetics of levofloxacin, a new tluoroquinolone, were investigated in 12
healthy Thai male volunteers with an average age (SD) of 22.92 (2.50) years. A single oral dose
of 300 mg or 500 mg levotloxacin was given to subjects following an 8- hour overnight fast.
The drug was given in a controlled, randomized, 2 x 2 crossover design with a I week washout
period. Venous blood samples were drawn prior to and from 0.25 up to 48 hours after dosing.
Plasma levotloxacin concentrations were determined by HPLC assay.
The pharmacokinetics of levotloxacin were well described by a linear, 2-compartment
open model with first-order absorption with lag time and first-order elimination. Mean ±
SEM of Cmax after 300 mg and 500 mg dose was 4.83 ± 0.33 and 7.75 ± 0.71 µg/mL, respectively.
Tmax ranged from 0.7 to 0.8 hours for both doses. Mean ± SEM of AUC0-∞ was 35.77 ±
2.06 µg x h/mL for 300 mg dose and 61.57 ± 2.84 µg x h/mL for 500 mg dose. High distribution
with V ss/F value of approximately 1.5 L/kg was demonstrated after both doses. Mean ± SEM
of CL/F value was 8.64 ± 0.41 L/h and 8.31 ± 0.37 L/h for a 300-mg and a 500-mg dose. respectively.
Long t1/2β of 7 to 8 hours with the mean residence time of 10.43 ± 0.43 hours and
10.49 ± 0.38 hours after 300 mg and 500 mg dose, respectively, was observed. The results suggested
that an oral 300 mg dose once daily provides sufficient Cmax to cover most Gramnegative
and atypical bacteria (median MIC90 0.032-0.5 µg/mL) common in mild to moderate
respiratory tract infections or complicated urinary tract infections and Gram-positive bacteria
(median MIC90 0.5 µg/mL) common in skin and soft tissue infections. For severe cases or
Streptococcus pneumoniae (MIC90 2 µg/mL) infection, a 500-mg dose should be recommended.
Key word : Levotloxacin, Pharmacokinetics, F1uoroquino1one

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