Abstract
The synthetic progestins used for contraception so far are structurally related either
to testosterone (estranes and gonanes) or to progesterone (pregnanes and 19-norpregnanes).
Several new progestins have been designed to minimize side-effects related to androgenic,
estrogenic or glucocorticoid receptor (GR) interactions. Dienogest (DNG) and drospirenone
(DRSP) exhibit a partial antiandrogenic action, and DRSP has predominant anti-mineralocorticoid
properties. The 19-norpregnanes include Nestorone (NES), nomegestrol acetate (NOMAc)
and trimegestone (TMG), and possess a high specificity for binding to the progesterone
receptor (PR) with no or little interaction with other steroid receptors. DRSP has
been developed as combination oral pills with ethinyl estradiol (EE); DNG has been
combined both with EE and, more recently, with estradiol valerate (E2V). NOMAc has
been used as a progestin-only method and more recently combined with estradiol (E2).
Nestorone is not active orally but proved to be the most active antiovulatory progestin
when used parenterally. It has been developed in various formulations such as implants,
vaginal rings or transdermal gel or spray. Risks and benefits of the new progestins
depend upon the type of molecular structure, the type of estrogen associated in a
combination and the route of administration.
Keywords
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Article info
Publication history
Published online: May 12, 2010
Accepted:
April 5,
2010
Received:
April 5,
2010
Identification
Copyright
© 2010 Elsevier Inc. Published by Elsevier Inc. All rights reserved.
