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All steroid hormones are structurally similar, but relatively minor differences cause
profound alterations in biochemical activity. The 21-carbon series (pregnane nucleus)
includes the corticoids and the true progestins (e.g., medroxyprogesterone acetate).
The 19-carbon series (androstane nucleus) includes all the androgens, among them the
progestins used in most oral and parenteral contraceptives. The removal of carbon
19 from testosterone changes the major hormonal effect from androgenic to progestogenic,
but these “19-nor” steroids retain varying degrees of androgenic activity. (They can
also have limited estrogenic activity, but this is insignificant at the low doses
used for contraception.) Some of the 19-nortestosterone progestins are metabolized
to other compounds (e.g., norethynodrel, ethynodiol diacetate, and lynestrenol to
norethindrone), and some (levonorgestrel, desogestrel) are active unchanged. The lingering
androgenic effects of 19-nor progestins are dose-related, opposed by estrogen, and
are manifested metabolically (e.g., glucose tolerance, lipoprotein synthesis) and
symptomatically (e.g., acne, weight gain). The effect of 19-nortestosterones on lipoproteins
prompted the development of less androgenic compounds, but the obvious benefit of
the new progestins (desogestrel, gestodene, norgestimate)is a reduction in the symptoms
associated with the androgenicity of the older compounds. Mitigation of androgenic
effects on lipoprotein and carbohydrate metabolism could have long-term benefits,
especially for women who are at risk of arteriosclerotic vascular disease; however,
these effects remain to be epidemiologically demonstrated.
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© 1995 Published by Elsevier Inc.
