The effect of repeated administration of berenil, a trypanocide, on urinary excretion of some enzyme activities in rat and their corresponding levels in the kidney and serum was investigated. Daily administration of this drug to rats resulted in increased urinary volume, excretion of protein, alkaline phosphatase and lactate dehydrogenase activities. However, the level of acid phosphatase activity was not significantly increased while muramidase activity disappeared completely during the period of drug administration. In the kidney tissue, there was a significant loss of lactate dehydrogenase activity immediately after the first dose and this trend continued until the end of drug administration. In the same tissue, there was an increase in alkaline phosphatase activity while the lysosomal enzymes were not significantly affected. In the serum, except for the increase in alkaline phosphatase activity, all other enzymes were not significantly affected. All these results indicate that there is cellular damage to rat kidney as a result of repeated berenil administration, and that the plasma membrane and the soluble portion of the cytoplasm are the primary site of injury to the cells. They also suggest that urinary enzyme excretion could be useful in determining the site of cellular damage by chemical agents in kidneys.