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Gonadal hormones. Dr. Z. Kiani. Androgens Estrogens Progestins Gonadotropins. Testosterone. Testosterone is not suitable for oral use (high FPE) Active form of testosterone in several oragans is DHT Some synthetic forms have greater anabolic effects: Nandrolone Oxymetolone.
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Gonadal hormones Dr. Z. Kiani
Androgens • Estrogens • Progestins • Gonadotropins
Testosterone • Testosterone is not suitable for oral use (high FPE) • Active form of testosterone in several oragans is DHT • Some synthetic forms have greater anabolic effects: • Nandrolone • Oxymetolone
Mechanism of Action اتصال به گیرنده های داخل سلولی و تغییر بیان ژن های هدف
Effects • Androgenic effects: • Primary • Secondary • Anabolic effects: • Maintain bone density • increased muscle size and strength • increased RBC • کاربرد های غدد و غیر غدد مثل دوپینگ
Toxicity • سمیت کبدی- عوارض مردانگی در زنان و برعکس در مردان
Antiandrogens • مهار ساخت- مهار رسپتورها و مهار تبدیل تستوسترون به دی هیدروتستوسترون- مهار GnRH • ketoconazole • Flutamide • Spironolactone • Finasteride: uses in baldness & BPH • GnRH Analogs and Antagonists
Esterogenic drugs • Effects: • normal female reproductive development • Metabolic effects: • Enhances blood coagulability • Increase TGs • Decrease LDL • Increase HDL • Clinical Use: • In hypogonadism in young females • HRT • components of hormonal contraceptives
Esterogenic drugs • Toxicity: • Increases risk of endometrial cancer • Small increase in the risk of breast cancer • Nausea • breast tenderness • Increased risk of migraine headache • Thromboembolic events (deep vein thrombosis) • Gallbladder disease • Hyper triglyceridemia • Hypertension
Progestins • Progesterone • Synthetic progestins: some have androgenic effects • Medroxyprogesterone • L-norgestrel • Norethindrone • Norgestimate • Desogestrel • Clinical Use • used as contraceptives (OCPs) • HRT
Drug interaction is very important for OCPs users: • Cytochrome inducer drugs and herbs
Antiestrogens and Antiprogestins • مهار انتخابی گیرنده های استروژن در بافت های مختلف بدن- مهار کننده های سنتز استروژن و و آنتی پروژستین ها • Tamoxifen: uses in breast cancer • Raloxifene: uses in osteoprosis • Clomiphene: uses in infertility • Letrozole • Danazole • Mifepristone (RU 486)