Progestins
The progestins (also called progestogens and progestogens ) are synthetic analogues of the progestins . They are used as active ingredients, for example, in hormonal contraception and in hormone replacement therapy .
Progestins are derived from the naturally occurring sex hormones nortestosterone or testosterone or progesterone .
Partial effects
The derivatives of nortestosterone such as norethisterone acetate , levonorgestrel and gestodene have, in addition to their gestagenic effect, also a partial androgenic effect, which can increase the tendency to oily skin and body hair. The androgenic effects of norgestimate and etonogestrel are only minimally pronounced ; Dienogest has no activity on androgen receptors. In addition to an anti-androgenic activity, drospirenone also has an antimineralcorticoid activity that counteracts the increased water retention caused by the estrogen component of the “ pill ”. Further drugs from the nortestosterone group are desogestrel , a precursor of etonogestrel, and norelgestromin , the active metabolite of norgestimate.
The descendants of progesterone, chlormadinone acetate and cyproterone acetate , have a marked anti-androgenic effect. Nomegestrol is only mildly antiandrogenic; There is inconsistent information on medroxyprogesterone .
| Trunk connection | connection | Antiestrogenic effect | Androgenic effects | Antiandrogenic effect | Glucocorticoid effect | Antimineral corticoid effect |
|---|---|---|---|---|---|---|
 |
progesterone | + | - | (+) ± | ± | + |
| Medroxyprogesterone | + | (+) | - + | + | - | |
| Cyproterone acetate | + | - | + | + | - | |
| Chlormadinone acetate | + | - | + | + | - | |
| Medrogestone | + | - | - | - | ||
| Megestrol | + | - | - | + | - | |
 |
Norethisterone acetate | + | + | - | - | - |
| Levonorgestrel | + | + | - | - | - | |
| Gestoden | + | + | - | ± | - | |
| Norgestimate | + | + | - | - | - | |
| Etonogestrel | + | + | - | - | ||
| Dienogest | + | - | + | - | - | |
| Drospirenone | + | - | + | - | + | |
| + present ± partially present (+) weakly / partially present - not present | ||||||
Generations
Depending on how they are introduced into therapy, synthetic gestagens are also divided into generations:
- 1st generation: norethisterone
- 2nd generation: Levonorgestrel
- 3rd generation: Gestoden, Desogestrel, Norgestimate
Some authors attribute drospirenone, which contains structural elements of spironolactone , to a 4th generation.
Risk of venous thrombosis
A known, rare side effect of the use of combined oral contraceptives is the occurrence of venous thromboembolic events (VTE), which is pointed out in the product information. The risk is higher for birth control pills with certain 3rd and 4th generation progestogens compared to those that contain norethisterone or levonorgestrel. In January 2014, the European Medicines Agency published the result of a risk assessment process for combined oral contraceptives containing desogestrel, gestodene, norgestimate, etonogestrel, drospirenone, dienogest, chlormadinone, nomegestrol or norelgestromin. Hence, the estimated risk of venous thromboembolic events occurring per 10,000 women per year
- About 5 to 7 cases in women taking a combination containing levonorgestrel, norgestimate, or norethisterone
- About 6 to 12 cases in women taking a combination containing etonogestrel or norelgestromin
- About 9 to 12 cases in women who take a combination containing gestodene, desogestrel or drospirenone.
The available data on combination preparations containing chlormadinone, dienogest or nomegestrol are not sufficient to be able to assess the risk. For comparison: women who do not use oral contraceptives (non-users) and are not pregnant have about 2 cases of VTE per 10,000 women annually.
Individual evidence
- ↑ a b c d e f g h E. Mutschler, G. Geisslinger, HK Kroemer, S. Menzel, P. Ruth: Mutschler drug effects. Pharmacology - Clinical Pharmacology - Toxicology. 10th edition. Wissenschaftliche Verlagsgesellschaft mbH, Stuttgart 2012, ISBN 3-80-472898-7 ; P. 419 ff.
- ↑ a b c d e f g h i j k FA Leidenberger, T. Strowitzki, O. Ortmann: Clinical endocrinology for gynecologists. Springer, 4th ed. 2009, p. 227.
- ↑ Product information Sayana suspension for injection , as of April 2012.
- ↑ K. Münstedt, M. Kirschbaum: Checklist gynecology and obstetrics ; Georg Thieme Verlag 2005, p 411. Here viewable online
- ↑ Combined hormonal contraceptives , risk assessment procedure EMEA / H / A-31/1356. Retrieved October 24, 2019.