ABSORPTION, EXCRETION AND FATE OF PRODILIDINE

¹ Department of Pharmacology and Chemotherapy, Mead Johnson Research Center, Evansville, Indiana

The physiological disposition of prodilidine was studied in rats. It was well absorbed from the gastreintestinal tract, but exhibited low blood levels following oral administration. The drug was rapidly removed from the tissues and very little unchanged drug was excreted in the urine. After subcutaneous administration the blood levels of prodilidine-like material were somewhat higher and a greater amount of unchanged prodilidine was excreted in the urine. None of the expected metabolites of prodilidine were found in the urine after oral or subcutaneous dosage. However, the drug was found to undergo N-demethylation by liver microsomes of several species in vitro, and the l isomer was demethylated by rat liver microsomes to a greater extent than the d isomer.