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SERMs Dr Sarvesh Singh Associate Professor E-mail: drsarveshsingh@gmail

SERMs Dr Sarvesh Singh Associate Professor E-mail: drsarveshsingh@gmail.com. ESTROGEN RECEPTORS (ERS). Demonstrated in female sex organs Two types: ER α : Predominates in uterus, vagina, breast, hypothalamus and blood vessels ER ᵝ :

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SERMs Dr Sarvesh Singh Associate Professor E-mail: drsarveshsingh@gmail

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  1. SERMs DrSarvesh Singh Associate Professor E-mail: drsarveshsingh@gmail.com

  2. ESTROGEN RECEPTORS (ERS) • Demonstrated in female sex organs • Two types: • ERα: • Predominates in uterus, vagina, breast, hypothalamus and blood vessels • ERᵝ: • Predominates in prostate gland of males and ovaries in females

  3. SERMs • Selective estrogen receptor modulators • Actions are in a tissue selective manner • Agents that act as: • Estrogen agonists in some tissues • Antagonists in other tissues • TWO SERMs: • Raloxifene • Tamoxifen

  4. RALOXIFENE • High affinity for both ERα and Erβ • Distinct DNA target the ‘raloxifene response element’ (RRE) • Partial agonistic actions in: • Bone • CVS • Antagonistic actions in: • Endometrial • Breast

  5. RALOXIFENE PARTIAL AGONISTIC ACTIONS IN: • Bone • Prevents bone loss in postmenopausal women • CVS • It reduces LDL cholesterol ANTAGONISTIC ACTIONS IN: • Endometrial • No increase in the risk of endometrial carcinoma • Breast • It reduces the risk of breast cancer

  6. RALOXIFENE FIRST LINE DRUG FOR POSTMENOPAUSAL OSTEOPOROSIS ? BISPHOSPHONATE

  7. RALOXIFENE BONE: • Bone mineral density (BMD) may increase by 0.9–3.4% in different bones (particularly the lumbar vertebrae) • Risk of vertebral fracture is reduced to half, but not that of long bones • Ca2+ and vit D supplements enhance the benefit • It is less efficacious than bisphosphonatesin preventing fractures • Raloxifene is a second line drug for prevention and treatment of osteoporosis in postmenopausal women

  8. RALOXIFENE • It reduces LDL cholesterol(by upregulating hepatic LDL receptors) • In contrast to estrogen HRT: • No increase in HDL and triglyceride levels DISADVANTAGES: • No relief of menopausal vasomotor symptoms • Hot flushes may occur

  9. RALOXIFENE SERIOUS DISADVANTAGE 3-fold increase in risk of deep vein thrombosis and pulmonary embolism

  10. TAMOXIFEN Estrogenic (agonist) action: • Uterus (increased risk of endometrial carcinoma) • Bone (Improvement in bone mass) Anti-estrogenic (antagonist) action – • Breast (used for treatment of breast cancer) • Blood (Improvement in lipid profile & increased risk of venous thromboembolism )

  11. RALOXIFENE & TAMOXIFENE Similarities b/w Raloxifene & Tamoxifene • Improvement in lipid profile • Increased risk of venous thromboembolism Differences b/w raloxifene & tamoxifene Raloxifene: • Antiestrogenic action on endometrium so NO RISK of carcinoma endometrium Tamoxifene: • Estrogenic action on endometrium so increased risk of carcinoma endometrium

  12. TAKE HOME MESSAGES • Tamoxifen: used for treatment of breast cancer • Raloxifene: used for treatment of osteoporosis NOTE Increased risk of venous thromboembolism with BOTH

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