Pharmacokinetics, protein binding, and extravascular distribution of ceftizoxime in normal subjects

Thirteen normal subjects were given 2, 3, or 4 g of ceftizoxime intravenously in a prospective single-blinded study. Serum and urine concentrations were measured for 48 h. The β-phase serum half-life ranged from 1.4 to 1.7 h. Approximately 100% of the agent was recovered unchanged in the urine over 48 h. Six of 13 subjects reported subjective complaints consisting of mild dizziness and moderate headache, all of which were transient. One subject also had a minimally elevated serum glutamic oxalacetic transaminase level 1 day after drug administration. Based on serum pharmacokinetics and serum protein binding determined in this investigation, unbound ceftizoxime appeared to distribute with the total body water.