Back to Search
Start Over
Mezlocillin pharmacokinetics after single intravenous doses to patients with varying degrees of renal function.
- Source :
-
Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 1980 Apr; Vol. 17 (4), pp. 599-607. - Publication Year :
- 1980
-
Abstract
- The pharmacokinetics of mezlocillin were examined after single 2- and 4-g intravenous injections to three groups of male patients with creatinine clearances of I >/= 60, II = 21 to 59, and III </= 20 ml min(-1) 1.73 m(-2). The decline in serum antibiotic levels was biphasic in all groups, and serum data were interpreted in terms of the pharmacokinetic two-compartment model. The mean elimination half-life of mezlocillin after the 2-g dose was 1.3, 1.5, and 2.3 h in groups I, II, and III, respectively. Equivalent values after the 4-g dose were 1.2, 1.6, and 4.4 h. In three functionally anephric patients the mean serum half-life of mezlocillin was 1.5 h during hemodialysis. Mean antibiotic levels in serum were greater than 10 mug ml(-1) for 4 h after the 2- and 4-g doses in group I and 8 h in group II. In group III, levels greater than 10 mug ml(-1) were maintained for 6 h after the 2-g dose and over 12 h after the 4-g dose. Mezlocillin distribution characteristics were largely independent of renal function and dose size. The only observable change occurred in the value of V(dss), which was significantly increased to 0.32 with 0.38 liter kg(-1) in severe renal impairment, compared to ca. 0.2 liter kg(-1) in subjects with normal or slightly impaired renal function. Cumulative 24-h urinary excretion accounted for 50, 40, and 3.2% of the dose in groups I, II, and III, respectively. Urine levels of mezlocillin were uniformly greater than the minimum inhibitory concentration for susceptible organisms for 12 h after dosing in all patients who produced urine. Because of the relatively small increase in the mezlocillin elimination half-life with declining renal function, dose reduction is necessary only in cases of severe renal impairment.
- Subjects :
- Anti-Bacterial Agents administration & dosage
Blood Proteins metabolism
Dose-Response Relationship, Drug
Half-Life
Humans
Injections, Intravenous
Kidney metabolism
Kidney physiopathology
Kinetics
Male
Metabolic Clearance Rate
Mezlocillin
Penicillins administration & dosage
Penicillins blood
Protein Binding
Regression Analysis
Renal Dialysis
Anti-Bacterial Agents metabolism
Kidney Diseases metabolism
Penicillins metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0066-4804
- Volume :
- 17
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Antimicrobial agents and chemotherapy
- Publication Type :
- Academic Journal
- Accession number :
- 6446877
- Full Text :
- https://doi.org/10.1128/AAC.17.4.599