Gestodene

Gestodene, sold under the brand names Femodene and Minulet among others, is a progestin medication which is used in birth control pills for women.

[6][9] Side effects of the combination of an estrogen and gestodene include menstrual irregularities, headaches, nausea, breast tenderness, mood changes, and others.

[13] It is marketed in birth control pills widely throughout the world, whereas it is available for use in menopausal hormone therapy only a few countries.

[9] Gestodene has very high affinity for the mineralocorticoid receptor (MR), but has only a relatively weak antimineralocorticoid effect that is comparable to that of progesterone.

[11][25] Gestodene shows some inhibition of cytochrome P450 enzymes in vitro, and has greater potency in this action compared to other progestins (IC50Tooltip half-maximal inhibitory concentration = 5.0 μM).

[4] Gestodene is metabolized in the liver via reduction of the δ4-3-keto group to form 3,5-tetrahydrogenated metabolites (major pathway) and via hydroxylation at the C1, C6, and C11 positions (substantial).

[4][1] In spite of differing from it only by the presence of an additional double bond between the C15 and C16 positions, gestodene is not metabolized into levonorgestrel in the body.

[30] Gestodene is almost identical to levonorgestrel in terms of chemical structure, differing only in having an additional double bond between the C15 and C16 positions, and for this reason is also known as δ15-norgestrel or as 15-dehydronorgestrel.

[12] The medication was introduced for use in menopausal hormone therapy in combination with estradiol in some countries such as in Europe and Latin America years later.

[7][8] Gestodene is marketed in the United Kingdom, Ireland, elsewhere throughout Europe, South Africa, Australia, Latin America, Asia, and elsewhere in the world.

[8] It is not listed as being marketed in the United States, Canada, New Zealand, Japan, South Korea, India, or certain other countries.

[8] Gestodene is marketed for use specifically in menopausal hormone therapy only in a few countries, including Colombia, Ecuador, Mexico, Peru, and Portugal.