Дезогестрел: свойства, применение и побочные эффекты

Medication

Desogestrel is a hormone blocker, progesterone receptors agonist, and antiandrogen. It is used in conjunction with estrogens and testosterones. Medications containing desogestrel and estrogen are used to treat endometriosis and as a component of menopausal hormone therapy. While commonly used as a female contraceptive, desogestrel suppresses spermogenesis and has been shown to have potential as a male contraceptive. Desogestrel and norethisterone are the only progestins that are widely used as a progestogen only "mini pill". These formulations are all indicated specifically for contraceptive purposes.

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. Hence, etonogestrel is exclusively responsible for the effects of desogestrel. Etonogestrel has about 150% of the affinity of promegestone and 300% of the affinity of progesterone for the PR. Desogestrel and etonogestrel are among the most potent progestogens available, along with gestodene and levonorgestrel (which have effective ovulation inhibiting dosages 40 μg/day and 60 μg/day, respectively). Oral desogestrel is clinically on the order of 5,000 times more potent than oral micronized progesterone (which has an effective ovulation inhibiting dosage of more than 300 mg/day) in humans. LH levels were suppressed maximally by desogestrel within 3 days, whereas 14 days were necessary for maximal suppression of FSH and testosterone levels. Conversely, its selectivity for the PR over the AR is similar to other newer 19 nortestosterone progestins like gestodene and norgestimate. In accordance with its very weak androgenic activity, desogestrel has minimal effects on lipid metabolism and the blood lipid profile, although there may still be some significant changes. Hence, desogestrel and etonogestrel have weak glucocorticoid activity. Certain other progestins act similarly in this assay, whereas progesterone acts neutrally.

The bioavailability of desogestrel has been found to range from 40 to 100%, with an average of 76%. Desogestrel and etonogestrel are eliminated exclusively as metabolites 50% in urine and 35% in feces. Desogestrel is the C3 deketo analogue of etonogestrel and the C3 deketo and C11 methylene analogue of levonorgestrel.

A chemical synthesis of desogestrel has been published.

Desogestrel was synthesized in 1972 by Organon International in the Netherlands and was first described in the literature in 1975. It was developed following the discovery that C11 substitutions enhance the biological activity of norethisterone.

Desogestrel is the generic name of the drug and its , , , , , and While under development, it was known as ORG 2969. Isibloom, Juleber, Kalliga, Kariva, Laurina, Lovima, Marvelon,

Desogestrel is available widely throughout the world, including in the United States, Canada, the United Kingdom, Ireland, many other European countries, Australia, New Zealand, South Africa, Latin America, Asia, and elsewhere. In the United States, it is available only in combination with ethinylestradiol as a combined oral contraceptive; it is not available alone and is not approved for any other indications. without requiring a prescription from a doctor beforehand. Pharmacists use a suitability questionnaire to determine if the medication is going to be suitable for the person, and if it is then they can purchase it from a pharmacy or online (all online purchases require the suitability questionnaire completed before the medication is sent to the customer).

In February 2007, the consumer advocacy group Public Citizen released a petition requesting that the Food and Drug Administration ban oral contraceptives containing desogestrel in the United States, citing studies going as far back as 1995 that suggest the risk of dangerous blood clots is doubled for women on such pills in comparison to other oral contraceptives. In 2009, Public Citizen released a list of recommendations that included numerous alternative, second generation birth control pills that women could take in place of oral contraceptives containing desogestrel. Most of those second generation medications have been on the market longer and have been shown to be as effective in preventing unwanted pregnancy, but with a lower risk of blood clots.

Desogestrel has been studied extensively as an antigonadotropin for use in combination with testosterone as a hormonal contraceptive in men. Such combinations have been found to be effective in producing reversible azoospermia in most men and reversible azoospermia or severe oligozoospermia in almost all men.