Abstract
Publisher Summary This chapter reviews the metabolism and excretion of amphetamines in man. The influence of certain ring substituents on the excretion and metabolism of amphetamine and N-ethylamphetamine is indicated. It is found that while exact comparison is not possible due to lack of pH control, certain trends emerge and thus the introduction of a lipophilic group tends to lower the urinary recovery of the unchanged drug, results which parallel the characteristics of these compounds in the buccal absorption test. It is found that when the compound is capable of undergoing N-dealkylation as in the case of N-ethylamphetamine, then the effect of the ring substitution is to increase the importance of this route of metabolism. In the case of 4-hydroxyamphetamine metabolism prior to conjugation is unnecessary and high levels of unchanged drug are excreted as conjugates. Using 14C-4-hydroxyamphetamine, it is shown that up to 90% of the drug is excreted as a sulfate conjugate in man.
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