Abstract
The metabolism of orthofomocaine (I) after i.p. or oral administration to rats has been qualitatively investigated. In urine unchanged drug (I) and following metabolites were found: orthofomocaine-N-oxide (II), p-hydroxyorthofomocaine (III), p-hydroxyorthofomocaine-N-oxide (IV), metabolite A (V) and phenol (VI). Metabolites III, IV and V occured also in conjugated forms, partly as glucuronides. The rat excretes into the bile metabolites III, IV and V, both free and conjugated; unchanged drug or N-oxide were not found in the bile. In rat liver microsomes the metabolites II, III, V and VI were formed. The drug is metabolized in the rat by aromatic hydroxylation, N-oxidation and oxidative dearalkylation; the resulting N-oxide was found to be reduced in vivo and in vitro to the original drug. Using rabbit liver microsomes the kinetic parameters for individual biotransformation reactions were determined.
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