1967 Volume 16 Issue 6 Pages 256-262
To know the biological fate of a new local anesthetic 2-methyl-2-n-propylaminopropion-o-toluide hydrochloride (LA-012), the absorption, the excretion, the distribution and the metabolism of the drug were studied in guinea pig by using tritium labeled LA-012. 3H-LA-012 was found to be well absorbed when injected intramuscularly in the guinea pig. Ten minutes after 3H-LA-012 was given to a guinea pig, the highest concentration was found in the kidney. Lung and spleen had appreciable levels whereas very low levels were present in the liver and blood. Most of the administered radioactivity were excreted in the urine within 24 hours. Only a few percent of the excreted radioactivity was present as unchanged 3H-LA-012, and more than 90 percent were metabolites including conjugates. Liver was found to be the chief organ for the metabolism of LA-012. The drug was metabolized mainly by oxidative reactions, hydroxylation and N dealkylation.
