Pharmacokinetics of cefotiam in normal humans

Doses of 0.5, 1.0, and 2.0 g of cefotiam were infused intravenously over a 15-min period in a crossover fashion to eight volunteers. Doses of 1.0 and 2.0 g were infused intravenously over periods of 30 and 60 min in a double crossover fashion to another eight volunteers. Serum concentrations fell rapidly from peak levels between 30 and 170 micrograms/ml at the end of the infusion to less than 1.0 micrograms/ml within 6 h after all regimens. The terminal half-life in plasma varied between 0.6 and 1.1 h. The slopes of the time-concentration curves with the different regimens showed different half-life data. The urinary excretion of cefotiam was mostly completed within 4 h of the beginning of drug administration. The pharmacokinetics of cefotiam were dose dependent. With the 2-g dose, the peak plasma concentrations and the values for the area under the curve were more than twice the values observed with 1 g; decreasing values of plasma clearance were observed with higher doses. Injection of cefotiam caused no immediate discomfort or reaction at the infusion site.