Desogestrel

Desogestrel, sold under the brand names Cerazette and Mircette among many others, 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. Desogestrel, sold under the brand names Cerazette and Mircette among many others, 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 2016 the version with ethinylestradiol was the 133rd most prescribed medication in the United States with more than 5 million prescriptions. 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. Along with norethisterone, it is one of the only progestins that is widely used as a progestogen-only 'mini pill'. It is also the only newer-generation progestin with reduced androgenic activity that is used in such formulations. In addition to hormonal contraception, desogestrel has been used in combination with estrogens such as estradiol as a component of menopausal hormone therapy. The medication has also been used in the treatment of endometriosis. Desogestrel is available alone in the form of 75 µg oral tablets and at a dose of 150 µg in combination with 20 or 30 µg ethinylestradiol in oral tablets. These formulations are all indicated specifically for contraceptive purposes. Contraindications of desogestrel include: Desogestrel is not indicated for use in pregnancy. It is not contraindicated during lactation and breastfeeding. Common side effects of desogestrel may include menstrual irregularities, amenorrhea, headaches, nausea, breast tenderness, and mood changes (e.g., depression), as well as weight gain, acne, and hirsutism. However, it has also been reported to not adversely affect weight. In addition, acne and hirsutism are negligible when combined with ethinylestradiol, and this combination can actually be used to treat such symptoms. Desogestrel can also cause changes in total, LDL, and HDL cholesterol. Uncommon side effects of desogestrel may include vaginal infection, contact lens intolerance, vomiting, hair loss, dysmenorrhea, ovarian cysts, and fatigue, while rare side effects include rash, urticaria, and erythema nodosum. Breast discharge, ectopic pregnancies, and aggravation of angioedema may also occur with desogestrel. Serious side effects of combined oral contraceptives containing desogestrel may include venous thromboembolism, arterial thromboembolism, hormone-dependent tumors (e.g., liver tumors, breast cancer), and melasma. No serious harmful effects have been reported with overdose of desogestrel. Symptoms may include nausea, vomiting, and, in young girls, slight vaginal bleeding. In safety studies, dosages of up to 750 µg/day desogestrel in women showed no adverse effects on laboratory and various other parameters and produced no reported subjective side effects. There is no antidote to desogestrel overdose and treatment should be based on symptoms.