Acta pharmacol. et toxicol. 1968, 26, 332-342 From the Department of Pharmacology, University of Bergen, Norway (Professor dr, med, Tollak B. Sirnes) The Metabolism of Drugs and Other Organic Compounds by the Intestinal Microflora By Ronald R. Scheline (Received February 14, 1968) Studies on the metabolic fate of drugs and foreign organic compounds up to the present have dealt almost exclusively with the changes occurring in the tissues. These reactions include oxidation, reduction, hydrolysis and conjugation and have been the subject of a review by Giterre (1963), However, drug metabolism need not be confined to the tissues, as oral administration of the drug or the excretion of the drug or its metabolites in the bile will bring it into contact with the gastrointestinal micro- flora, where metabolic alterations may take place. Studies dealing with the metabolism of drugs by the gastrointestinal microflora have been carried out in only a few instances and much of our present knowledge of the subject comes from incidental observations made in the course of other studies. Increasing numbers of such reports have appeared in the past few years with the result that the possibilities of drug metabolism by the gut flora are becoming more widely recognized. Investigations carried out in this laboratory (SCHELINE & LONGBERG 1965; SCHELINE 1966a & b; 1967 & 1968) demonstrated the importance of the intestinal microflora in the metabolism of a sulphonated azo dye and a number of phenolic acids, These results prompted a fuller study of the metabolic capabilities of the microflora. The present report deals with the metabolism, by the rat caecal microflora, of a number of com- pounds belonging to some common classes of foreign compounds, drugs or their metabolites, Methods ‘Compounds The following compounds were prepared: 4-methylumbelliferone glucuronide (MEAD, Sur & Wittias 1955) and 8-hydroxyquinaldic acid (Invinc & PINNINGTON 1957), The