ABSTRACT

Biotransformation may be defined as the enzyme-catalyzed alteration of drugs by the living organism. Although few drugs are eliminated unchanged, urinary excretion is an ineffective means of terminating the action of most drugs or poisons in the body. In fact, the urinary excretion of a highly lipid-soluble substance such as

pentobarbital

would be so slow that it would take the body a century to rid itself of the effect of a single dose of the agent. Therefore, mammalian and other terrestrial animals have developed systems that allow the conversion of most lipid-soluble substances to water-soluble ones, so that they may be easily excreted by the kidney. In general, biotransformation may be divided into two forms of metabolism: hepatic and nonhepatic.