Overview
| Generic Names: | Desogestrelum [INN-Latin] |
|---|---|
| Trade Names: | Cerazette; Cyclessa; Desogen; Kariva; Mircette |
| Brand Mixtures: | Marvelon 21 Tab (Desogestrel + Ethinyl Estradiol); Marvelon 28 Tab (Desogestrel + Ethinyl Estradiol); Ortho-Cept 21 Day (Desogestrel + Ethinyl Estradiol); Ortho-Cept 28 Day (Desogestrel + Ethinyl Estradiol) |
| PharmGKB Accession Id: | PA449238 |
Description
A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents. PubChem (source: Drug Bank)
Indication
For the prevention of pregnancy in women who elect to use this product as a method of contraception. (source: Drug Bank)
ATC Therapeutic Category
- G03AC:Progestogens
Pharmacology, Interactions, and Contraindications
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 (luteinizing hormone) surge. (source: Drug Bank)
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 lining of the womb for a possible pregnancy. If pregnancy occurs, progesterone levels in the body remain high, maintaining the womb lining. If pregnancy does not occur, progesterone levels in the body fall, resulting in a menstrual period. Desogestrel tricks the body processes into thinking that ovulation has already occurred, by maintaining high levels of the synthetic progesterone. This prevents the release of eggs from the ovaries. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Desogestrel is rapidly and completely metabolized by hydroxylation in the intestinal mucosa and on first pass through the liver to etonogestrel. Other metabolites (i.e., 3a-OH-desogestrel, 3b-OH-desogestrel, and 3a-OH-5a-H-desogestrel) with no pharmacologic actions also have been identified and these metabolites may undergo glucuronide and sulfate conjugation. (source: Drug Bank)
Protein Binding
98.3% (source: Drug Bank)
Absorption
Following oral administration, the relative bioavailability of desogestrel compared to a solution, as measured by serum levels of etonogestrel, is approximately 100%. (source: Drug Bank)
Toxicity
Symptoms of overdose include nausea and vaginal bleeding. (source: Drug Bank)
Isomeric SMILES Code:
CC[C@]12CC(=C)[C@H]3[C@H]([C@@H]1CC[C@]2(C#C)O)CCC4=CCCC[C@H]34 (source: Drug Bank)
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ESR1 |
|
(source: Drug Bank) |
| PGR |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
