GnRH antagonists
- Immediately block pituitary GnRH signaling
- No initial hormone flare
- Prostate cancer: degarelix/relugolix
- Endometriosis/fibroids: oral antagonists
- Hot flashes + bone loss are common
- Relugolix has important P-gp interactions
- Combination products may include add-back hormones
Class at a glance
- Immediately block pituitary GnRH signaling
Practical pearls
- Combination products may include add-back hormones
Pharmacology
- Endometriosis/fibroids: oral antagonists
Clinical role
- No initial hormone flare
- Prostate cancer: degarelix/relugolix
- Hot flashes + bone loss are common
- Relugolix has important P-gp interactions
Self-check
- What is the main pharmacologic action of GnRH antagonists?
Immediately block pituitary GnRH signaling.
- What clinically distinguishes Relugolix within GnRH antagonists?
important P-gp interactions.
Drugs in this class (2)
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