Intravenous Pharmacokinetics and in Vitro Bactericidal Activity of Trimethoprim-Sulfamethoxazole

Abstract
Trimethoprim-sulfamethoxazole (240 mg of trimethoprim plus 1,200 mg of sulfamethoxazole) was administeredintravenouslyin a volumeof 200 ml to 7 volunteers every 12 hr for 4 days. The mean peak levels of TMP and SMZ in plasma were 3.22 and 100 I-lg/ml, respectively, on day 1 and 5.91 and 178 μg/ml, respectively, on day 4, when a steady state wasachieved. Tests of in vitro susceptibility indicated that these concentrations are bactericidal for a large proportion of enteric gram-negative bacilli.

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