GnRH receptor agonist
- Continuous exposure: initial hormone surge (“flare”), then receptor desensitization → gonadotropin suppression
- A tumor flare risk in prostate cancer
- ↓ sex steroids → used for prostate cancer, endometriosis and precocious puberty
- Hypogonadal effects: hot flashes, ↓ libido, bone loss
Drugs with this mechanism (2)
- Goserelin — GnRH receptor AGONIST implant; flare first, then downregulation.
- Leuprolide — GnRH agonist causing an initial flare then suppression of sex hormones.
Self-check
- What follows the initial hormone flare during continuous GnRH agonist exposure?
Receptor desensitization and gonadotropin suppression. - In which cancer is the initial GnRH-agonist flare a concern?
Prostate cancer.
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