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Pharmacokinetics and tolerance of single intramuscular doses of cefotetan in normal Caucasian volunteers.

Cefotetan, a third-generation cephalosporin, is extremely well tolerated by healthy Caucasian volunteers when given by intramuscular injection. It gives rise to prolonged high plasma antibiotic concentrations. Lignocaine (0.5%), when used as a diluent, had no effect on the pharmacokinetic parameters of cefotetan. Two grams of cefotetan given as the disodium salt 12 hourly by the intramuscular route gives plasma levels that are likely to be clinically effective in the treatment of infections due to a very wide range of Gram-positive and Gram-negative aerobes and anaerobes. The validity of this prediction however can only be established by subsequent clinical trials.