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Bioavailability and clearance of chloramphenicol after intravenous chloramphenicol succinate
Author(s) -
Nahata Milap C,
Powell Dwight A
Publication year - 1981
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1981.174
Subject(s) - chloramphenicol , bioavailability , pharmacology , clearance , metabolic clearance rate , medicine , chemistry , pharmacokinetics , antibiotics , biochemistry , urology
Bioavailability of chloramphenicol and kinetics of chloramphenicol succinate and chloramphenicol were studied in 12 patients. Chloramphenicol succinate, 25 mg/kg, was injected intravenously every 6 hr over 0.5 to 1 hr. Both the drug and the prodrug were analyzed by high‐pressure liquid chromatography. Bioavailability of chloramphenicol ranged from 0.55 to 0.92 and total, renal, and nonrenal clearance from 6.81 to 98.22, 2.54 to 26.90, and 3.73 to 87.38 ml/m 2 /min, while clearances of chloramphenicol succinate ranged from 84.75 to 916.00, 28.40 to 312.00, and 27.06 to 760.93 ml/m 2 /min. Urinary recovery of chloramphenicol was 3% to 25% and that of chloramphenicol succinate was 7% to 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 hr, 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. Clinical Pharmacology and Therapeutics (1981) 30 , 368–372; doi: 10.1038/clpt.1981.174