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sex hormones-drugs

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 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 loss N/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
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.
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 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
Created by: ksoul6



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