Cephalotin (Cephalotin) is a beta-lactam antibiotic, inhibits class C β-lactamase AmpC, with an Ki of 0.32 µM[1]. The maximum plasma cephalothin concentration after IM administration was 11.3 +/- 3.71 micrograms/ml. The terminal half-life was 47.0 minutes and was longer than the half-life after IV administration. The bioavailability of cephalothin given IM ranged from 38.3% to 93.1% and averaged 65.0 +/- 20.5%[2]. Two derivatives of cephalothin, compound I and II, were synthesized and demonstrated strong growth inhibition of ampicillin resistant Escherichia coli (E. coli). The MIC50 of I and II were determined to be 55 microg/mL and 30 microg/mL, respectively. Cephalothin showed less than 20% growth inhibition of E. coli at all concentrations based on assay of colony forming units. Compounds I and II showed greater than 50% growth inhibition of E. coli at all concentrations greater than 50 microg/mL (more than 65% at 400 microg/mL)[3]. Patients receiving intravenous sodium cephalothin or intravenous penicillin-G. Immunogenicity was indicated by a higher incidence of anti-cephalothin antibody in patients after having received the drug than in controls and by an increase in titre of anti-cephalothin antibody during administration of the drug. Further, patients receiving cephalothin had a high incidence of anti-penicillin antibodies and the anti-penicillin antibody titre increased during cephalothin administration[4].
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