GnRH receptor antagonist
GnRH receptor antagonist — mechanism card
- Immediate gonadotropin/sex-hormone suppression with no initial flare
- Prostate cancer, endometriosis, uterine fibroids
- Sex-hormone deprivation → hot flashes, ↓ bone density
Drugs with this mechanism (3)
- Danazol — Weak androgen suppressing gonadotropins; used for endometriosis and hereditary angioedema.
- Degarelix — GnRH receptor ANTAGONIST for prostate cancer — castration without the testosterone flare.
- Elagolix — Oral non-peptide GnRH antagonist; suppresses without the initial flare of leuprolide.
Self-check
- Do GnRH antagonists cause an initial hormone flare?
No; suppression is immediate. - What skeletal effect can sex-hormone deprivation cause?
Reduced bone density.
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