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  1. Selective Estrogen Receptor Modulator By Dr Zarish Ghafoor
  2. Estrogens • Estrogen is a category of sex hormone responsible for the development and regulation of the reproductive system and secondary sex characteristics.
  3. Source of estrogen • Ovaries (max) • Fat tissue • Adrenal gland
  4. Mechanism of action Receptor sites • Hypothalamus • Pituitary • Breast • Bone • Uterus • Heart
  5. Effect of estrogen drugs • Estrogen agonist • Antagonist • Mixed agonist antagonist
  6. Selective estrogen receptor modulators (SERMS) • Functions of SERMs • Tissue selective action • Estrogenic action in some tissues • Antiestrogenic action in other tissues
  8. SERMs
  9. Pharmacological Effects of SERMs Estrogenic effects • Bone………Decrease resorption……Decreases chances of fracture • Liver…..decrease LDL increase HDL, • Protein…….increase protein synthesis • Blood…..increase coagulation…. Increase deep venous thrombosis
  10. Pharmacological Effects of SERMs • Estrogenic effects • Uterus….increase endometrial proliferation except clomiphene • Ovary …….increase ovarian stimulation.(Clomiphen) Anti estrogenic effects • Breast…..decrease breast cell proliferation
  11. CLINICAL USES of SERMs 1)As Replacement therapy Primary Hypogonadism (Turner’s syndrome) Premature ovarian failure Surgical removal of the ovaries. Menopause
  12. CLINICAL USES of SERMs 1)Other uses: Contraception Dysfunctional uterine bleeding (DUB) Prostate cancer Dysmenorrhea Osteoporosis Amenorrhea Hirsutism Breast cancer Gynecomastia
  13. ADVERSE EFFECTS of SERMs 1) Ovarian hyper stimulation-Multiple pregnancies 2) Polycystic ovaries 3) Increase risk of endometrial cancer 4) Increase risk of deep venous thrombosis 5) Pulmonary embolism 7) Retention of salt and water Hypertension 8) Hot Flushes 9) Leg cramps 10) Nausea 11)Vomiting
  14. Hormonal Oral Contraceptives OCPs
  15. Hormonal Oral Contraceptives (OCPs) • Preparations of OCPs: • Combined oral contraceptive pills • Monophasic • Multiphasic • Progesterone only pills (Mini pills) • Emergency Pills (Post coital pills)
  16. Hormonal Oral Contraceptives (OCPs) Routes of administration of OCPs: Oral pills S/C Implants Transdermal patches Injections (long acting) Intra-uterine devices (IUDs) Vaginal rings.
  17. Hormonal Oral Contraceptives (OCPs) Mechanism of action • Inhibition of ovulation (feedback inhibition of pituitary (causing abolition of LH surge) • Thickening of cervical mucus • Decreased motility and secretions of the fallopian tubes • Making endometrium unfavourable for implantation
  18. Hormonal Oral Contraceptives (OCPs) Clinical uses: 1) Osteoporosis 2) Ovarian Cysts 3) Menstrual Cycle Irregularities 4) Dysmenorrhea 5) Benign Breast Disease 6) Menorrhagia 7) Ectopic Pregnancy 8) Pelvic Inflammatory Disease (PIDs)
  19. Hormonal Oral Contraceptives (OCPs) Adverse effects: Mild: • Nausea, edema, break through bleeding, Migraine, Breast discomfort Moderate: • Break through bleeding, Weight gain, Hyper pigmentation, Acne, Hirsutism, Vaginal infection, Amenorrhea
  20. Hormonal Oral Contraceptives (OCPs) Adverse effects: Severe: • Venous thromboembolic disease • Cerebrovascular disease • cholelithiasis • hepatic adenoma • Breast cancer • Alopecia