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Sex hormones

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Pharmacology

Publié dans : Santé & Médecine
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Sex hormones

  1. 1. Endocrine Pharmacology Adrenal Steroids & The Sex Hormones Dr. Salman Iftikhar
  2. 2. Adrenal Steroids Glucocorticoids: prednisone, dexamethasone Mineralocorticoid: fludrocortisone
  3. 3. Adrenal Steroids • Nonendocrine uses: Used in inflammatory disorders • Endocrine uses of glucocorticoids (e.g., prednisone, dexamethasone), mineralocorticoids (fkudrocortisone): 1. Addison disease – replacement therapy 2. Adrenal insufficiency staes (infection, shock, trauma) – supplementation 3. Premature delivery to prevent respiratory distress syndrome – supplementation 4. Adrenal hyperplasia – feedback inhibition of ACTH
  4. 4. Adrenal Steroids • Adrenal steroid antagonists: 1. Spironolactone:  Blocks aldosterone and androgen receptos 2. Mifepristone:  Blocks glucocorticoid and progestin receptors 3. Synthesis inhibitors  Metyrapone (blocks 11-hydroxylation)  Ketoconazole
  5. 5. SEX hormones
  6. 6. Contraception
  7. 7. Estrogens • Estradiol is the major natural estrogen • Conjugated equine estrogens (premarin)– natural • Ethinyl estradiol and mestranol – steroidal • Diethylstilbestrol (DES) – nonsteroidal
  8. 8. Estrogens • Clinical Uses 1. Female hypogonadism 2. Hormone replacement therapy (HRT) in menopause 3. Contraception –feedback  of gonadotropins 4. Dysmenorrhea 5. Uterine bleeding 6. Prostate CA
  9. 9. Estrogens • Adverse Effects 1. General  Nausea  Breast tenderness  Endometrial hyperplasia   gallbladder disease, cholestasis  Migraine
  10. 10. Estrogens • Adverse effects 2.  blood coagulation (only high doses) 3. Cancer risk •  endometrial cancer (unless progestins are added) •  breast cancer – questionable, but caution if other risk factors are present • DES given during breast feeding  vaginal adenocarcinoma cancer in offspring
  11. 11. Estrogens 1. Anastrozole • Aromatase inhibitor  estrogen synthesis • Use: Estrogent – dependant postmenopausal breast cancer 2. Clomiphene (fertility pill) •  feedback inhibition  FSH and LH  ovulation  pregnancy • Use: fertility drug • Adverse effect:  multiple births
  12. 12. Estrogens • Selective estrogen – receptor modulators (SERMs) 1. Tamoxifen • Action is variable depending on “target” tissue • E-receptor agonist (bone), antagonist (breast), partial agonist (endometrium) • Possible inc. risk of endometrial cancer • Used in estrogen-dependant breast cancer and for prophylaxis in high – risk patients
  13. 13. Estrogens • Selective estrogen – receptor modulators (SERMs) 2. Raloxifene • E-receptor agonist (bone), antagonist breast and uterus • When used in menopause there is no inc. risk of cancer • Use: prophylaxis of post menopausal osteoporosis
  14. 14. Progestin • Progesterone is the major natural progestin • Drugs: 1. Levonorgestril 2. Medroxyprogesterone 3. Norethindrone 4. Desogestrel – a synthetic progestin devoid of androgenic and anti-estrogenic activities, common to other derivative
  15. 15. Progestin • Clinical uses: 1. Contraception (oral with estrogens) 2. HRT with estrogens to decrease endometrial CA • Adverse effects 1. HDL and  LDL 2. Glucose intolerance 3. Breakthrough bleading 4. Androgenic (hirsutism) 5. Antiestrogenic (block lipid changes)
  16. 16. Progestin • Antagonist: mifeprostone – abortifacient (used with PGs)
  17. 17. Oral Contraceptives • Pharmacology: 1. Combination of estrogens (ethinyl estradiol, mestranol) with progestins (norgestrel, norethindrone) in varied dose with mono-, bi-, and triphasic variants 2. Supress gonadotropins, esp. midcycle LH surge • Adverse effects 1. Estrogen • Nausea, bloating, headache, mastalgia 2. Progestins • Weight gain, hirsutism, acne, tiredness, depression, dec. HDL and inc. LDL 3. Liver adenoma
  18. 18. Oral Contraceptives • Interactions: Dec. contraceptive effectiveness when used with antimicrobials and enzyme inducers • Benefits 1.  risk of endometrial and ovarian cancer 2.  Dysmenorrhea 3.  endometriosis 4.  PID 5.  osteoporosis
  19. 19. • The combination agents are divided into monophasic forms (constant dosage of both components during the cycle) and biphasic or triphasic forms (dosage of one or both components is changed once or twice during the cycle)
  20. 20. Androgens • Methyltestosterone and 17-alkyl derivatives with increased anabolic actions, e.g., oxandrolone, nandrolone • Uses: 1. Male hypogonadism and for anabolic actions 2. Illicit use in athletics
  21. 21. Androgens • Adverse effects 1. Excessive masculinization 2. Premature closure of epiphysis 3. Cholestatic jaundice 4. Aggression – “roid rage” 5. Dependence
  22. 22. Androgens • Antagonists: 1. Flutamide: androgen receptor blocker – used for prostate cancer 2. Leuprolide: GnRH analog: repository form used for CA prostate
  23. 23. Androgens • Antagonists: 3. Finasteride: • 5- alpha reductase inhibitor, preventing conversion of testosterone to dihydrotestosterone (DHT) • DHT is responsible for hair loss and prostate enlargement • Uses: BPH, male pattern baldness • CAUTION: Teratogenicity
  24. 24. Androgens • Antagonists: 4. Ketoconazole • Synthesis inhibitor – used in androgen receptor positive prostate cancer

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