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Concept
Dimethisterone
Summary
Dimethisterone, formerly sold under the brand names Lutagan and Secrosteron among others, is a progestin medication which was used in birth control pills and in the treatment of gynecological disorders but is now no longer available. It was used both alone and in combination with an estrogen. It is taken by mouth.
Side effects of dimethisterone are similar to those of other progestins. When used in combination with high doses of an estrogen, an increased risk of endometrial cancer can occur. Dimethisterone is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has some antimineralocorticoid activity and no other important hormonal activity.
Dimethisterone was first described and was introduced for medical use in 1959. It started being used in birth control pills in 1965. However, due to its low potency and consequent inability to prevent the increased risk of endometrial cancer with estrogens, dimethisterone was soon discontinued for such purposes.
Dimethisterone was used alone in the treatment of gynecological disorders and in combination with ethinylestradiol in birth control pills.
Progestin#Side effects
Side effects of dimethisterone are similar to those of other progestins.
Dimethisterone was derived from modification of ethisterone via introduction of methyl groups at the C6α and C21 positions. Relative to ethisterone, it is 12 times as potent orally as a progestogen in animals (Clauberg test), and, unlike ethisterone, is a pure progestogen with no androgenic (or estrogenic) activity in animals even at very high doses (although some weak antimineralocorticoid activity was observed at high doses in animals). However, in spite of its improved potency over ethisterone, it is a weak progestogen relative to most other progestins, in fact one of the weakest known.
Official source
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