BIOCHEMICAL STUDIES ON CHLORAMPHENICOL (CHLOROMYCETIN)

II. Tissue Distribution and Excretion Studies

¹ Research Laboratories of Parke, Davis and Company, Detroit, Michigan

Chloramphenicol is rapidly absorbed, metabolized and excreted. In man the major route of excretion is by way of the kidneys, with approximately 90 per cent of the administered dose accounted for in 24 hours. Lesser amounts are excreted in the urine of lower animals. The bulk of the excreted drug is in the form of an inactive nitro compound, and less than 10 per cent of the administered dose is excreted unchanged. Renal plasma clearance figures indicate that chioramphenicol is largely excreted by glomerular filtration, while the inactive metabolic products appear to be excreted mainly by tubular secretion.

In the rat, parenteral administration of chioramphenicol results in excretion into the intestine by way of the bile, principally as inactive nitro compounds. These may be partly reabsorbed, or reduced in the intestine to form aryl amines which are excreted in the feces. Inactivation of chioramphenicol occurs in vitro with minced liver preparations, with the production of inactive nitro compounds and small amounts of aryl amines. The distribution of chloramphenicol in the tissues is not uniform, with high concentrations being found in the liver and kidneys and low concentrations in the brain and spinal fluid.

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