The unique propey of SERMs is that they:
SERM: 1. Raloxifene- Agonist at bone - Agonist in blood : Increase HDL level- Antagonist at breast: Decrease breast carcinoma risk- Antagonist at endometrium: Decrease endometrium carcinoma- Agonist at liver: Increase thromboembolism risk 2. Tamoxifen- Agonist at bone - Agonist in blood : Increase HDL level- Antagonist at breast: Decrease breast carcinoma risk- Agonist at endometrium: Increase endometrium carcinoma- Agonist at liver: Increase thromboembolism risk Tamoxifen, Doloxifen and toremifene are beneficial on: - Bone - Blood - Breast 3. Clomifene Antagonist at pituataryHypothalamus - GnRHPituatary - LH/FSHOvary - E/P
Have both estrogenic and progestational agonistic activity
Inhibits the aromatase enzyme that is required for estrogen synthesis
Produces estrogenic effect without binding to estrogen receptors
Act as agonist in some tissues and antagonist in other tissues
Osteoporosis, Sex Hormones and OCPs