Tracking Susceptibility and Reducing Resistance - Fluoroquinolones at the Forefront in the Fight Against Bacterial Pathogens

29 March, 2018

Question 4

Do you have any data comparing PK/PD properties of levofloxacin with other fluoroquinolones and the influence on bacterial killing?

The PK concentrations obtained by levofloxacin are among the highest of the fluoroquinolones, with the 500 mg once daily dose associated with high free AUC and grater free C_max values than moxifloxacin and ciprofloxacin (Table 1) (5).

A recent study investigating rates and extent of bacterial killing of S. pneumoniae strains with moxifloxacin and levofloxacin demonstrated that moxifloxacin and levofloxacin achieved similar rates and extent of bacterial kill for the wild type, efflux pump type and parC mutant S. pneumoniae (6).

Table 1. Clinical dose and PK parameters of oral quinolones

Drug

Daily dose^a
(mg)

AUC^b
(μg h/ml)

Cmax^b,c
(μ/ml)

Protein binding^b
(%)

Free AUC^d
(μg h/ml)

Free Cmax^d
(μg/ml)

Moxifloxacin

400 x 1

51.5

4.08 (7 days)

25.8

2.04

Ciprofloxacin

200 x 3

13.8

9.7

Levofloxacin

500 x 1

47.5

5.72 (7 days)

32.8

3.95

^a	Maximum dose in accordance with the health insurance in Japan.
^b	AUC, C_max, and protein binding values were taken from interview forms for each drug, available from the manufacturer. For LVFX(500 mg x 1), AUC was taken from Wright et al (2000).
^c	The values were C_max under steady state during repetitive administration. Number in parenthesis is time required for reaching steady state.
^d	Free AUC = AUC x protein binding ratio. Free C_max = C_max x protein binding ratio.

Abbreviations: AUC = area under the plasma concentration-time curve, C_max = maximum serum drug concentration, NA = not available.
Adapted from reference (5).

Tracking Susceptibility and Reducing Resistance - Fluoroquinolones at the Forefront in the Fight Against Bacterial Pathogens

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