Desogestrel

Desogestrel
ATC Code G03AC09
Formula C22H30O
Molar Mass (g·mol−1) 310,47
Physical State solid
Melting Point (°C) 109-110
PKS Value 13.04
CAS Number 54024-22-5
PUB Number 40973
Drugbank ID DB00304
Solubility moderate in water / poor in ethanol

Basics

Desogestrel is a progestin medication used in birth control pills for women. It is also used to treat menopausal symptoms in women. The drug is available and is used alone or in combination with an estrogen. It is taken by mouth.

Pharmacology

Pharmacodynamics

Oral contraceptives containing desogestrel suppress gonadotropins, thereby inhibiting ovulation. Specifically, desogestrel binds to progesterone and androgen receptors and slows the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus. This process results in suppression of the normal physiological rise in luteinizing hormone (LH) that precedes ovulation. It inhibits follicular rupture and the release of viable eggs from the ovaries. Desogestrel has been shown to be more effective when administered prior to ovulation.

Pharmacokinetics

Oral absorption is rapid and maximum plasma concentration is reached after about 2 hours. Bioavailability is approximately 60-80%. Plasma protein binding is approximately 96-98%. Metabolism occurs in the liver where desogestrel is converted to its active metabolite etonogestrel. Excretion takes place mainly in the urine.

Toxicity

Side effects

Common side effects of Desogestrel may include menstrual irregularities, amenorrhea, headache, nausea, breast tenderness, and mood changes (e.g., depression), as well as weight gain, acne, and hirsutism.

Desogestrel may also cause changes in total, LDL, and HDL cholesterol levels. Rare side effects of desogestrel include vaginal infections, contact lens intolerance, vomiting, hair loss, dysmenorrhea, ovarian cysts, and fatigue, while rare side effects include rash, urticaria, and erythema nodosum. Breast discharge, ectopic pregnancy, and worsening of angioedema may also occur with desogestrel.

Serious adverse reactions to combined oral contraceptives containing desogestrel may include venous thromboembolism, arterial thromboembolism, hormone-dependent tumors (e.g., liver tumors, breast cancer), and melasma.

Toxicological data

LD50 (rat, oral): >2000 mg/kg

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

Your personal medicine assistent

afgis-Qualitätslogo mit Ablauf Jahr/Monat: Mit einem Klick auf das Logo öffnet sich ein neues Bildschirmfenster mit Informationen über Medikamio GmbH & Co KG und sein/ihr Internet-Angebot: medikamio.com/ This website is certified by Health On the Net Foundation. Click to verify.
Drugs

Search our database for drugs, sorted from A-Z with their effects and ingredients.

Substances

All substances with their common uses, chemical components and medical products which contain them.

Diseases

Causes, symptoms and treatment for the most common diseases and injuries.

The contents shown do not replace the original package insert of the medicinal product, especially with regard to dosage and effect of the individual products. We cannot assume any liability for the correctness of the data, as the data was partly converted automatically. A doctor should always be consulted for diagnoses and other health questions. Further information on this topic can be found here.