Arzneistoffe
- Buserelin (Profact®)
- Deslorelin
- Histrelin (Vantas®)
- Goserelin (Zoladex®)
- Leuprorelin (Enantone®)
- Nafarelin
- Peforelin
- Triptorelin (Decapeptyl®)
Wirkmechanismus
GnRH-Agonisten sind synthetische Analoga des Gonadotropin-releasing-Hormon (GnRH). Nach Konstante unphysiologische Stimmulation der GnRH-Rezeptoren in der Hypophyse kommt es zu einem initialen Anstieg der LH- und FSH Sekretion mit anschließender Downregulation der GnRH-Sekretion. Innerhalb von 2-3 Wochen werden keine Sexualhormone mehr gebildet und der für die Erkankung wichtiger Stimulus entfällt.
Aminosäuresequenz der GnRH-Agonisten
| Table 1. Amino acid sequence of GnRH agonists 1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 | 9 | 10 | ||||||||||
| GnRH | pGlu | His | Trp | Ser | Tyr | Gly | Leu | Arg | Pro | Gly NH2 | |||||||||
| Triptorelin | pGlu | His | Trp | Ser | Tyr | D-Trp | Leu | Arg | Pro | Gly NH2 | |||||||||
| Nafarelin | pGlu | His | Trp | Ser | Tyr | D-Nal | Leu | Arg | Pro | Gly NH2 | |||||||||
| Deslorelin | pGlu | His | Trp | Ser | Tyr | D-Trp | Leu | Arg | Pro | NHEt | |||||||||
| Leuprolide | pGlu | His | Trp | Ser | Tyr | D-Leu | Leu | Arg | Pro | NHEt | |||||||||
| Buserelin | pGlu | His | Trp | Ser | Tyr | D-ser(Tbu) | Leu | Arg | Pro | ethylamide | |||||||||
| Peforelin | pGlu | His | Trp | Ser | His | Asp | Trp | Lys | Pro | Gly NH2 | |||||||||
Synonyme
- GnRH-Analoga
Literatur & Quellen
- European public MRL assessment report (EPMAR) – triptorelin Acetate EMA/CVMP/382140/2013; Stand July 2013