Bioavailability and clearance of chloramphenicol after intravenous chloramphenicol succinate

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Abstract
Bioavailability of chloramphenicol and kinetics of chloramphenicol succinate and chloramphenicol were studied in 12 patients. Chloramphenicol succinate, 25 mg/kg, was injected i.v. every 6 h over 0.5-1 h. Both the drug and the prodrug were analyzed by high-pressure liquid chromatography. Bioavailability of chloramphenicol ranged from 0.55-0.92 and total, renal and nonrenal clearance from 6.81-98.22, 2.54-26.90 and 3.73-87.38 ml/m2 per min, while clearances of chloramphenicol succinate ranged from 84.75-916.00, 28.40-312.00 and 27.06-760.93 ml/m2 per min. Urinary recovery of chloramphenicol was 3-25% and that of chloramphenicol succinate was 7-45%. Mean apparent volumes of distribution were 0.71 l/kg for chloramphenicol and 2.10 l/kg for chloramphenicol succinate and elimination half-lifes were 4.03 and 2.65 h, respectively. There were relationships between patient age and clearance of both drugs. Incomplete bioavailability of chloramphenicol and the more than 10-fold variability in clearance of both chloramphenicol and chloramphenicol succinate explain the need for individualizing doses to achieve therapeutic effect and minimize the risk of toxicity.

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