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Abstract
There is limited information on the metabolism of levonorgestrel, norethindrone and
structurally related contraceptive steroids. Both levonorgestrel and norethindrone
undergo extensive reduction of the α,β-unsaturated ketone in ring A. Levonorgestrel
also undergoes hydroxylation at carbons 2 and 16. The metabolites of both compounds
circulate predominantly as sulfates. In urine, levonorgestrel metabolites are found
primarily in the glucuronide form, whereas norethindrone metabolites are present in
approximately equal amounts as sulfates and glucuronides. Of the progestogens structurally
related to norethindrone, norethindrone acetate, ethynodiol diacetate, norethindrone
enanthate, and perhaps lynestrenol, undergo rapid hydrolysis and are converted to
the parent compound and its metabolites. There is no convincing evidence that norethynodrel
is converted to norethindrone. Of the progestogens structurally related to levonorgestrel,
it appears that neither desogestrel nor gestodene are transformed to the parent compound.
However, there is evidence that norgestimate can be, at least partly, converted to
levonorgestrel. Further studies on the metabolism of these progestogens are required
before we can understand their mechanism of action.
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Article info
Publication history
Accepted:
April 6,
1990
Received:
January 3,
1990
Identification
Copyright
© 1990 Published by Elsevier Inc.
