Cefotaxime: Pharmacokinetics and in vitro Antibacterial Activity of Serum and Urine in Normal Human VolunteersPlouffe J.F.a · Perkins R.L.a · Fass R.J.a · Prior R.B.a · Bernstein B.a · Ho I.b
aDivision of Infectious Diseases, Department of Medicine, The Ohio State University College of Medicine Columbus, Ohio, USA; bHoechst Roussell Pharmaceuticals, Somerville, N.J., USA
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The pharmacokinetic and antibacterial properties of cefotaxime were determined in normal adult volunteers. Single doses of 250, 500, 1,000 and 2,000 mg were evaluated following 5- and 20-min intravenous (i.v.) infusions and intramuscular (i.m.) administration. Cefotaxime was well tolerated and mean peak serum levels exceeded the minimum inhibition concentration (MIC) values for a wide spectrum of potential bacterial pathogens. Approximately 48% of the i.v. doses was excreted renally; average volume of distribution was 30% of body weight and the t½ was about 1 h. Cefotaxime was rapidly absorbed following i.m. injection with maximum serum concentrations occurring at approximately 0.6 h. Serum and urine antibacterial activity reflected the concentration of cefotaxime and MIC of the bacterial pathogens tested.
© 1983 S. Karger AG, Basel
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