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sex hormones-drugs
Question | Answer |
---|---|
ESTRADIOL | Natural Estrogens |
ETHINYL ESTRADIOL | Synthetic Estrogens |
Effects of Estrogens | Required for the normal sexual maturation and growth. Stimulate the development of the vagina, uterus, and uterine tubes Stimulate the development of the secondary sex characteristics. |
Effects of Estrogens on endomtrium | Growth effects on uterine smooth muscle With progesterone, regulates normal human menstrual cycle -Continuous exposure to estrogens for prolonged periods leads to hyperplasia of the endometrium -Associated with abnormal bleeding patterns |
Effects of Estrogens on blood vessels | Maintenance of the normal structure and function blood vessels |
Effects of Estrogens on BONE | DECREASE THE RATE OF RESORPTION OF BONE |
Effects of Estrogens on liver | Stimulates the production of: Corticosteroid-binding globulin, Thyroxine-binding globulin, (TBG): Increased circulating levels of thyroxine,SHBG: Increased circulating levels estrogen, testosterone,Transferrin: increased circulating levels of iron and co |
Estrogen EFFECTS ON PLASMA LIPIDS | Increase in the High-Density Lipoproteins (HDL) Slight reduction in the low-density lipoproteins (LDL) Reduction in total plasma cholesterol levels. Increased Plasma triglyceride |
Estrogen Effects on Blood Coagulation | Enhance coagulation |
ANASTROZOLE | Inhibitors of Estrogen Synthesis, Reversible Aromatase Inhibitors (Non steroidal type II) |
Serious estrogen-lacking side-effects | Increased risk of osteoporosis |
anastrozole Adverse Effects | Dramatically reduce levels of estrogens Produce hot flashes They lack the beneficial effect of tamoxifen to maintain bone density |
FORMESTANE | IRREVERSIBLE inhibition of aromatase (steroidal type I) |
Adverse Effects of FORMESTANE | Dramatically reduce levels of estrogens Produce hot flashes They lack the beneficial effect of tamoxifen to maintain bone density |
TAMOXIFEN | Competitive PARTIAL AGONIST of Estrogen Receptor (ER) |
Tamoxifen action | ER ANTAGONIST IN BREAST TISSUES PARTIAL AGONIST IN ENDOMETRIUM AND BONE Used for the treatment of breast cancer |
adverse effects Tamoxifen | Hot flashes atrophy of the lining of the vagina with bleeding and discharge hair lossN/V Menstrual irregularities increases the incidence of endometrial cancer in postmenopausal women. |
RALOXIFENE description and action | Selective Estrogen Receptor Modulators (SERMs) ER AGONIST IN BONE ANTAGONIST IN BOTH BREAST AND ENDOMETRIUM |
Raloxifene adverse effects | Hot flashes Deep vein thrombosis leg cramps |
CLOMIFENE | ANTAGONIST IN HYPOTHALAMUS AND ANTERIOR PITUITARY PARTIAL AGONIST IN OVARIES |
Adverse Effects of clomifene | ovarian hyperstimulation, increased incidence of multiple births, ovarian cysts, hot flashes, and blurred vision. Prolonged use (e.g., ≥12 cycles) increase the risk of ovarian cancer. |
DROSPIRENONE (1, 2-DIHYDROSPIRORENONE) | Type of progesterone |
Effects of Progesterone | Little effect on protein metabolism. Stimulates lipoprotein lipase activity |
progesterone effects on liver | Promotes glycogen storage |
effects of progesterone on reproductive tract | Progesterone decreases estrogen-driven endometrial proliferation -> development of a secretory endometrium Abrupt decline in progesterone at end of cycle= main determinant of onset of menstruation long duration -> changes in the endometrium similar to tho |
MIFEPRISTONE | Antiprogetins :Available for the termination of pregnancy |
MIFEPRISTONE MOA | Competitive receptor antagonist for PR-A and PR-B Also competes with glucocorticoid receptor |
ULIPRISTAL ACETATE | PARTIAL AGONIST AT THE PR |
ULIPRISTAL ACETATE MOA | Inhibit ovulation Used for emergency contraception |
testosterone | is the principal secreted androgen in men |
Testosterone effects | Puberty: 2° sexual characteristics in male TESTOSTERONE WHEN GIVEN TO ADULTS: In Adult Males, large doses lead to testicular atrophy In Adult Women, androgens lead to changes seen in pre-pubertal males |
Testosterone MOA | The effects of testosterone are mediated via the Androgen Receptor (AR) and estrogen |
KETOCONAZOLE | Antiandrogen, Synthesis Inhibitor |
KETOCONAZOLE effects | Inhibitor of adrenal and gonadal steroid synthesis Does not affect ovarian aromatase Reduces human placental aromatase activity. Increases the estradiol:testosterone ratio in plasma. Men treated with ketoconazole often develop reversible gynecomastia du |
FINASTERIDE | 5α-reductase inhibitor |
FINASTERIDE effects | Effective in reducing prostate size in men with benign prostatic hyperplasia |
FLUTAMIDE | Androgen Receptor Antagonists |
FLUTAMIDE effect | Limited efficacy when used alone because the increased LH secretion Stimulates higher serum testosterone concentrations |