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QuickView for Desogestrel (compound)
PubChem
| Name: | Desogestrel |
|---|---|
| PubChem Compound ID: | 40973 |
| Description: | A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents. |
| Molecular formula: | C22H30O |
| Molecular weight: | 310.473 g/mol |
| Synonyms: |
C07629; Desogestrel; Desogestrel (USAN); Desogestrel [USAN:BAN:INN]; Desogestrelum [INN-Latin]; Org-2969; D02367; 13-Ethyl-11-methylene-18,19-dinor-17alpha-pregn-4-en-20-yn-17-ol; EINECS 258-929-4; HSDB 3593.
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DrugBank
Identification
| Name: | Desogestrel |
|---|---|
| Name (isomeric): | DB00304 |
| Drug Type: | small molecule |
| Description: | A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents. |
| Synonyms: |
Desogestrelum [INN-Latin]
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| Brand: | Cerazette |
| Brand name mixture: | Kariva(Desogestrel + Ethinyl Estradiol), Mircette(Desogestrel + Ethinyl Estradiol), Cyclessa(Desogestrel + Ethinyl Estradiol), Marvelon 28 Tab(Desogestrel + Ethinyl Estradiol), Marvelon 21 Tab(Desogestrel + Ethinyl Estradiol), Desogen(Desogestrel + Ethinyl Estradiol), Ortho-Cept 28 Day(Desogestrel + Ethinyl Estradiol), Ortho-Cept 21 Day(Desogest... show more » |
| Category: | Progestins, Contraceptives, Oral, Synthetic |
| CAS number: | 54024-22-5 |
Pharmacology
| Indication: | For the prevention of pregnancy in women who elect to use this product as a method of contraception. |
|---|---|
| Pharmacology: |
Desogestrel is used as a female contraceptive. Desogestrel is a progestin or a synthetic form of the naturally occurring female sex hormone, progesterone. In a woman's normal menstrual cycle, an egg matures and is released from the ovaries (ovulation). The ovary then produces progesterone, preventing the release of further eggs and priming the lini...
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| Mechanism of Action: |
Binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like desogestrel will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (lutein...
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| Absorption: | Following oral administration, the relative bioavailability of desogestrel, as measured by serum levels of etonogestrel, is approximately 84%. The absolute oral bioavailability is about 76%. |
| Protein binding: | 98.3% |
| Biotransformation: | Desogestrel is rapidly and completely metabolized by hydroxylation in the intestinal mucosa and on first pass through the liver. It is primarily metabolized to 3α-hydroxydesogestrel with small amounts of 3β-hydroxydesogestrel being formed. Both of these metabolites are then rapidly oxidized to its active metabolite, etonogestrel (3-ketodesogestrel). Other metabolites (e.g. 2-hydroxydesogestrel) with no pharmacologic action have also been identified. Desogestrel and some of its metabolites (e.g. 3β-hydroxydesogestrel, 15β-hydroxydesogestrel) may also undergo glucuronide and sulfate conjugation. Early in vitro studies demonstrated that CYP2C9 and possibly CYP2C19 were involved in the conversion of desogestrel to 3α-hydroxydesogestrel and 3β-hydroxydesogestrel (PMID 9864282); however, later clinical studies conducted in humans refuted this result (PMID 15963096). The latter study indicates that CYP3A4 plays an important role in metabolizing etonogestrel. Thus, strong CYP3A4 inhibitors or inducers could result in increased side effects or therapeutic failure, respectively. |
| Half Life: | 27.8±7.2 hours |
| Toxicity: | Symptoms of overdose include nausea and vaginal bleeding. |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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Targets
