Pharmacokinetics and tolerance of single intravenous doses of cefotetan disodium in male Caucasian volunteers.

Cefotetan, a third generation cephalosporin, in doses of 0.25, 0.5, 1.0 and 2.0 g was administered intravenously as the disodium salt to ten healthy male Caucasian volunteers and its pharmacokinetics and tolerance determined. The elimination half-life was 3.3 h. The drug was 88% plasma protein bound and 67% was recovered unchanged in the urine. HPLC and bioassay techniques for cefotetan plasma-concentration determinations gave virtually identical results. Cefotetan was well tolerated although half of the volunteers experienced transient mild to moderate diarrhoea. It is concluded that the pharmacokinetic disposition of cefotetan is similar in Caucasian and Japanese subjects and that the long elimination half-life, lack of detectable metabolism and high urinary excretion will result in plasma and urine concentrations in excess of the MIC of sensitive bacteria on a twice daily dosing regime.