The pharmacokinetics of mezlocillin at two dosages were studied over the course of therapy in 12 patients receiving the drug for the treatment of infections. Patients received an initial dosing regimen of 4 g every 6 h or 5 g every 8 h, which was switched to the alternative regimen after 5 days of treatment. Both drug regimens demonstrated similar pharmacokinetic characteristics, which suggests that the reported dose-dependent elimination of mezlocillin is not an important factor in the clinical use of mezlocillin at the dosages currently used.