Pharmacokinetics of @entity4258 in XXXX .

@entity1 @entity4258 @entity177 @entity1011 @entity293
@entity4258 is an antibacterial drug chiefly eliminated by the kidney and therefore useful in the treatment of @entity293 . To study its pharmacokinetics in @entity177 , we administered a single oral dose of 400 mg to 14 @entity1 and 6 controls with normal renal function. @entity1 were divided into three groups according to the severity of @entity177 . @entity4258 was measured in serum and urine by bioassay. Serum half-life in controls was 3.87 hours and prolonged to 5.85 hours in group I ( @entity1011 clearance 80-45 ml/min), 7.25 hours (p less than 0.05) in group II ( @entity1011 clearance 44-20 ml/min) and 8.34 hours (p less than 0.01) in group III @entity1 ( @entity1011 clearance less than 20 ml/min). A good linear correlation between the elimination rate constant and @entity1011 clearance (r = 0.79, p less than 0.01) has been found. Total urinary excretion in the 72 hour period after administration achieves 40.4% in controls, falls to 23.5% (p less than 0.05), 15.6% (p less than 0.01) and 8.2% (p less than 0.01) of administered dose in groups I, II and III, respectively. Similarly, urinary concentrations decrease in all @entity1 groups with respect to controls. Our data show that effective urinary antibacterial concentrations of @entity4258 after 400 mg single oral dose were obtained even in @entity1 with severe @entity177 . In these @entity1 systemic accumulation after repeated dose administration is a probable event. Therefore, dosage adjustment is advisable in @entity1 with @entity1011 clearance less than 20 ml/min, although it will inevitably cause lower urinary concentrations.
