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In vivo metabolism of N-oxides

  • Chapter
N-Oxidation of Drugs

Abstract

The in vivo metabolism of compounds which contain N-oxide groups, either aliphatic or heteroaromatic tertiary amines, has not been extensively studied. Just as there are differences in the enzymes involved in the oxidation of the two different types of tertiary amines to their N-oxides, it might be expected that there will be differences in the effect such a group has on the overall metabolism of substrates. Therefore, in order to simplify discussion, the focus in this chapter will be on only one type, namely the N-oxides of aliphatic tertiary amines. However, it should be realized that compounds containing a heteroaromatic tertiary amine group are important as is illustrated by two drugs which possess such a functionality, namely chlordiazepoxide and minoxidil. In both these cases some of the major metabolites in man either retain the N-oxide group as such or form conjugates thereof (Thomas and Harpootlian, 1975; Johnson et al., 1983; Boxenbaum et al., 1977; also see Chapter 4).

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Hawes, E.M., Jaworski, T.J., Midha, K.K., McKay, G., Hubbard, J.W., Korchinski, E.D. (1991). In vivo metabolism of N-oxides. In: Hlavica, P., Damani, L.A. (eds) N-Oxidation of Drugs. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-3112-4_15

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  • DOI: https://doi.org/10.1007/978-94-011-3112-4_15

  • Publisher Name: Springer, Dordrecht

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