Profile of the progesterone derivative chlormadinone acetate - pharmocodynamic properties and therapeutic applications

Contraception
René Druckmann

Abstract

Chlormadinone acetate (CMA) is a derivative of progesterone (17alpha-acetoxy-6-chloro-4,6-pregnadiene-3,20-dione), first synthesized in 1961 and is used as an orally effective progestogen in hormone replacement therapy (HRT), and in combination with ethinyl estradiol (EE) in contraception since 1999. Chlormadinone acetate has a strong progestogenic effect - about one-third higher than that of progesterone - and may vary depending on the previous effect of an estrogen, i.e., estrogens may promote the formation of progesterone receptors and proliferation of the endometrium. Like progesterone, it is anti-estrogenic and has no partial androgenic effect (at the doses used for contraception and HRT). In contrast to progesterone, it has a slight glucocorticoid effect, a pronounced anti-androgenic effect and no anti-mineralocorticoid effect. No pregnancy-maintaining effect of CMA has been demonstrated in humans. The anti-androgenic effect of CMA is presumed to be the result of both its binding to androgen receptors - competitively inhibiting the effect of endogenous testosterone and dihydrotestosterone - and the competitive inhibition of 5alpha-reductase. In this respect, dosing of CMA is crucial; agonistic effects are observed when do...Continue Reading

References

Jan 1, 1987·American Journal of Obstetrics and Gynecology·C Jung-Hoffmann, H Kuhl
Dec 1, 1987·British Journal of Obstetrics and Gynaecology·B BazinJ Paris
Jul 1, 1985·Contraception·J Newburger, J W Goldzieher
Jan 1, 1973·Contraception·Y G DugwekarK R Laumas
May 20, 1998·Contraception·H P ZahradnikJ O Andreas
Aug 12, 1998·Journal of Endocrinological Investigation·Y SahinI Müderris
Nov 24, 1999·The Journal of Clinical Endocrinology and Metabolism·B CouzinetG Schaison
Sep 11, 2001·Dermatology : International Journal for Clinical and Investigative Dermatology·I WorretNatascha Binder
Feb 22, 2002·Primary Care·Wilhelm H Cronje, John W W Studd
Jun 6, 2002·Proceedings of the National Academy of Sciences of the United States of America·Zheng LiuBert W O'Malley
Feb 8, 2003·Molecular and Cellular Endocrinology·Béatrice TérouanneCharles Sultan
Feb 26, 2003·Drugs·Daniel Raudrant, Thomas Rabe
Oct 15, 2003·European Journal of Obstetrics, Gynecology, and Reproductive Biology·Ernest H Y NgPak-Chung Ho
Dec 13, 2003·Maturitas·Adolf E SchindlerJos H H Thijssen
Jul 21, 2004·The Journal of Steroid Biochemistry and Molecular Biology·Rocio García-BecerraFernando Larrea
Nov 16, 2004·Contraception·Jacqueline ConardJean-Christophe Thalabard
Jan 27, 2005·Climacteric : the Journal of the International Menopause Society·Regine Sitruk-WareRené Druckmann
Apr 2, 2005·Obstetrics and Gynecology·Julia B GreerRoberta B Ness
Jun 23, 2005·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·Ramazan DansukCem Turan
Dec 24, 2005·Contraception·Johannes Huber, Katharina Walch
Sep 15, 2006·Archives of Medical Research·Carlos M ContrerasMinerva Hernández-Lozano
May 17, 2007·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·Françoise ParisCharles Sultan
Jun 15, 2007·The European Journal of Contraception & Reproductive Health Care : the Official Journal of the European Society of Contraception·Francisca Martínez, Angels Avecilla
Dec 6, 2007·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·René Druckmann
May 13, 2008·Archives of Gynecology and Obstetrics·Sayed BakryFrederick Naftolin

Citations

Dec 1, 2010·Molecular Human Reproduction·Wolfgang R SchäferH P Zahradnik
Nov 10, 2015·Expert Opinion on Therapeutic Targets·Manuel Luque-Ramírez, Héctor Francisco Escobar-Morreale
Jul 10, 2012·Fertility and Sterility·Aida Hanjalic-BeckH P Zahradnik
Mar 20, 2020·The European Journal of Contraception & Reproductive Health Care : the Official Journal of the European Society of Contraception·Giuseppe MorganteVincenzo De Leo
Dec 1, 2010·Hormone Molecular Biology and Clinical Investigation·Réne Druckmann
Mar 29, 2020·Journal of Endocrinological Investigation·F TorreS La Vignera
Apr 12, 2020·Neuro-Chirurgie·Alexandre RouxJohan Pallud

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Spatio-Temporal Regulation of DNA Repair

DNA repair is a complex process regulated by several different classes of enzymes, including ligases, endonucleases, and polymerases. This feed focuses on the spatial and temporal regulation that accompanies DNA damage signaling and repair enzymes and processes.

Glut1 Deficiency

Glut1 deficiency, an autosomal dominant, genetic metabolic disorder associated with a deficiency of GLUT1, the protein that transports glucose across the blood brain barrier, is characterized by mental and motor developmental delays and infantile seizures. Follow the latest research on Glut1 deficiency with this feed.

Hereditary Sensory Autonomic Neuropathy

Hereditary Sensory Autonomic Neuropathies are a group of inherited neurodegenerative disorders characterized clinically by loss of sensation and autonomic dysfunction. Here is the latest research on these neuropathies.

Separation Anxiety

Separation anxiety is a type of anxiety disorder that involves excessive distress and anxiety with separation. This may include separation from places or people to which they have a strong emotional connection with. It often affects children more than adults. Here is the latest research on separation anxiety.

Neural Activity: Imaging

Imaging of neural activity in vivo has developed rapidly recently with the advancement of fluorescence microscopy, including new applications using miniaturized microscopes (miniscopes). This feed follows the progress in this growing field.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.