Desogestrel is a progestin medication which is used in birth control pills for women. It is also used in the treatment of menopausal symptoms in women. The medication is available and used alone or in combination with an estrogen. It is taken by mouth.Side effects of desogestrel include menstrual irregularities, headaches, nausea, breast tenderness, mood changes, acne, increased hair growth, and others. Desogestrel 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 very weak androgenic and glucocorticoid activity and no other important hormonal activity. The medication is a prodrug of etonogestrel (3-ketodesogestrel) in the body.Desogestrel was discovered in 1972 and was introduced for medical use in Europe in 1981. It became available in the United States in 1992. Desogestrel is sometimes referred to as a "third-generation" progestin. Along with norethisterone, it is one of the only progestins that is widely available as a progestogen-only "mini pill" for birth control. Desogestrel is marketed widely throughout the world. It is available as a generic medication. In 2019, the version with ethinylestradiol was the 128th most commonly prescribed medication in the United States, with more than 5 million prescriptions. Medical uses
Desogestrel is used in hormonal contraception in women, specifically in birth control pills. It is used alone in progestogen-only pills ("mini pills") and in combination with the estrogen ethinylestradiol in combined oral contraceptive pills. Desogestrel and norethisterone are the only progestins that are widely used as a progestogen-only "mini pill".
The contraceptive effects of desogestrel in women are mediated not only by prevention of ovulation via its antigonadotropic effects but also by its marked progestogenic and antiestrogenic effects on cervical mucus and the endometrium.Aside from its progestogenic activity, desogestrel also has some off-target hormonal activity at other steroid hormone receptors (see below). However, these activities are relatively weak, and desogestrel is said to be one of the most selective and pure progestogens used in oral contraceptives. Antigonadotropic effects
Desogestrel has antigonadotropic effects via its progestogenic activity, similarly to other progestogens. It has been found to reduce testosterone levels by 15% in women at a dosage of 125 μg/day. In addition, desogestrel has been extensively investigated as an antigonadotropin at dosages of 150 to 300 μg/day in combination with testosterone in male contraceptive regimens. One study found that 150 μg/day and 300 μg/day desogestrel alone in healthy young men suppressed luteinizing hormone (LH) levels by about 35% and 42%, respectively; follicle-stimulating hormone (FSH) levels by about 47% and 55%, respectively; and testosterone levels by about 59% and 68%, respectively. LH levels were suppressed maximally by desogestrel within 3 days, whereas 14 days were necessary for maximal suppression of FSH and testosterone levels. A previous study by the same authors found that increasing the dosage of desogestrel from 300 μg/day to 450 μg/day resulted in no further suppression of gonadotropin concentrations.