The effect of renal impairment and haemodialysis on single dose pharmacokinetics of oral enoxacin.
The effect of renal impairment on the single dose pharmacokinetics of oral enoxacin was studied in 28 volunteers with creatinine clearances ranging from less than 15 to 120 ml/min, including patients undergoing chronic haemodialysis. Following an overnight fast, 400 mg of enoxacin was administered orally to each subject. Blood and urine samples were collected at predetermined times for 48 and 72 h, respectively. Plasma and urine samples were assayed for enoxacin and for oxo metabolite concentrations by a specific high performance liquid chromatographic method. Area under the concentration-time curve from time 0 to infinity (AUC0-infinity) was increased in subjects with renal impairment. Plasma half-life (10.6-11.6 h) in volunteers with severe renal impairment was approximately double the 5.2 h half-life found in subjects with normal renal function, and this should result in steady-state enoxacin concentrations approximately double those measured in normal subjects given equivalent doses. Haemodialysis did not remove significant amounts of enoxacin. A significant correlation between creatinine clearance and enoxacin renal clearance was observed (r = 0.97).
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D E
DE
Department of Pharmaceutics, State University of New York, Buffalo.
Schultz
R W
RW
Frost
R W
RW
Sedman
A J
AJ
Thomas
D J
DJ
Kinkel
A W
AW
Schentag
J J
JJ
D000284:Administration, Oral; D000328:Adult; D000368:Aged; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001783:Blood Flow Velocity; D002851:Chromatography, High Pressure Liquid; D015365:Enoxacin; D005260:Female; D006207:Half-Life; D006801:Humans; D007674:Kidney Diseases / Q000378:metabolism*; D008297:Male; D008433:Mathematics; D008875:Middle Aged; D009287:Naphthyridines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D012044:Regression Analysis; D006435:Renal Dialysis
D000890:Anti-Infective Agents; D009287:Naphthyridines; D015365:Enoxacin