Single-dose pharmacokinetics of lomefloxacin in patients with normal and impaired renal function.
The quinolone antibiotic lomefloxacin was administered as a 400 mg single oral dose to 12 subjects with renal impairment (creatinine clearance 5-65 mL/min/1.73 m2) and to 13 healthy subjects (creatinine clearance 80-135 mL/min/1.73 m2). The concentrations of lomefloxacin in plasma and urine were determined by high-pressure liquid chromatography up to 48 hours post-administration. Linear correlations were found between lomefloxacin plasma and renal clearances and creatinine clearance. The mean nonrenal clearance of lomefloxacin (approximately 32 mL/min/1.72 m2) was not influenced by renal function. The mean plasma clearances of lomefloxacin in healthy subjects and in a subgroup of patients with severe renal impairment (creatinine clearance 5-15 mL/min/1.73 m2) were 209 and 43 mL/min/1.73 m2, respectively. The decrease in plasma clearance of lomefloxacin was explained fully by the decrease in renal clearance. The elimination half-life of lomefloxacin increased significantly with the degree of renal impairment, from 7.5 hours in normal subjects to 26.9 hours in subjects with severe renal impairment. The maximum serum concentration and the time to maximum serum concentration were not significantly affected by renal function. The pharmacokinetics of lomefloxacin are dependent on renal function, and appropriate dosage adjustment is necessary when creatinine clearance is less than 30 mL/min/1.73 m2.
Nilsen
O G
OG
SINTEF UNIMED, Department of Pharmacology and Toxicology, University of Trondheim, Norway.
Saltvedt
E
E
Walstad
R A
RA
Marstein
S
S
D000328:Adult; D000368:Aged; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D003404:Creatinine / Q000652:urine; D004334:Drug Administration Schedule; D005260:Female; D024841:Fluoroquinolones; D006801:Humans; D007668:Kidney / Q000378:metabolism*; D007674:Kidney Diseases / Q000378:metabolism*; D016014:Linear Models; D008297:Male; D008875:Middle Aged; D015363:Quinolones / Q000493:pharmacokinetics*
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; D003404:Creatinine; C053091:lomefloxacin