GnRH receptor agonist
- Continuous exposure: initial hormone surge (“flare”), then receptor desensitization → gonadotropin suppression
- ↓ sex steroids → used for prostate cancer, endometriosis and precocious puberty
- Hypogonadal effects: hot flashes, ↓ libido, bone loss
- Continuous stimulation desensitizes the receptor, suppressing gonadotropins
- Initial testosterone surge — a tumor flare risk in prostate cancer
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.
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