Pharm Test 3 Gonadal Hormones Flashcards
Estrone (fat) Ethinyl Estradiol (Ovary) also most potent Estriol Diethylstilbestrol***TEST Conjugated Estrogen Mestranol Quinestrol (prodrug for Estradiol)
Physiological effects: Sexual development: growth/development of vagina, uterus, fallopian tubes and 2* sex characteristics in female.
-Decrease bone resorption, closure of the growth plate, increase factor2,7,9,10,12 and decrease factor 3,c,s
-increase cholesterol in bile=stones
INDICATION: hypogonadism in female, OCP, Post menopausal HRT, Prostate CA, acne, dysmenorrhea, dysfunctional uterine bleeding
AE: increase thromboembolism, risk of CVD, breast/endometrial cancer, Migraine, cholestasis, mood changes
DES–> infertility and vaginal cancer
Tamoxifen
Selective Estrogen Receptor Modulators (SERMS)
PE: Antag:Breast. Agonist: Liver, endometrial, bone
I: Breast Cancer
AE: Hot Flush (Antag), Thrombosis (agonist), increase risk of endometrial cancer
Raloxifene
SERM
PE: Antag: breast Agonist: bone
I: breast cancer prophylaxis, prevention of osteoporosis
NO EFFECT ON ENDOMETRIUM
Toremifene
SERM
I:post menopausal breast mets
AE:hot flush, nausea, increase ALP
Decrease DNA synthesis
Clomiphene
SERM
PE: Blocks -ve feedback of GnRH @ hypothalamus-> increase pulsitile release-> increaseFSH/LH-> growth of follicle and ovulation
I: Infertility
PK: t.5= 5-7 days
AE: Ovarian hyperstimulation, ovarian enlargement, multiple pregnancies, visual disturbances
*Interferes with receptor recycling effectively depleting hypothalamic ERs–> loss of -ve feedback
Clomiphene
SERM
PE: Blocks -ve feedback of GnRH @ hypothalamus-> increase pulsitile release-> increaseFSH/LH-> growth of follicle and ovulation
I: Infertility. Half life is about a week
AE: Ovarian overstimulation/enlargement, multiple pregnancies, visual disturbances
**Interferes with receptor recycling effectively depleting hypothalamic ERs –> loss of -ve feedback
Fulvestrant
Estrogen Receptor Antagonist SERD
Indication: Breast CA in tamoxifen resistant pt’s
AE: Hot Flush, HA, Injection site reaction
Letrozole
Anastrozole
Exemestane (irreversible)
Aromatase inhibitors
PE: Blocks conversion of androgen to estrogen
I: 2nd line treatment for breast CA after tamoxifen
AE: Hot flush, decrease bone mineral density
Progesterone Medroxyprogesterone Norgestrel Norethindrone Desogestrel Norelgestromin Etonogestrel Norgestimate Drospirenone: spironolactone derivative with antimeneralocorticoid and antiandrogenic activity -> Endometrial thinning and treatment of acne
Progestins
PE: Elevation=ovulation, regulation for gestation and maintenance of pregnancy, Induces secretory changes in the endometrium, Decreases uterine and gallbladder contractions, High dose-> suppresses FSH and LH leading to anovulation
I: Contraception, HRT, Promote and maintain pregnancy, suppress ovaries in the treatment of dysmenorrhea and endometriosis, Diagnose estrogen secretion when menstruation occurs after progesterone administration in a patient with amenorrhea
AE: /long term use: weight gain, depression, edema, acne, decreased HDL, HTN, Thrombophlebitis, Cholestatic jaundice
Mifepristone
Competative inhibitor of preogesterone and glucocorticoid receptors
I: morning after pill-abortifacient
AE: Excess bleeding, N/V/Pain/anorexia
**Given with with PGE or PGF to increase myometrial contraction
Danazol
Partial agonist @ progestin, androgen, glcocorticoid receptors
I: /endometriosis, Fibrocystic change in the breast
Inhibits CYP450
AE:hepatitis
**Modified Testosterone->masculinization/hirsutism
Testosterone Oxandrolone Stanozolol Fluoxymesterone Nandrolone Oxymetholone
Androgens, DHT is more potent than testosterone and androstenedione
PE: testosterone: Wolffian duct, spermatogenesis, bone formation and muscle growth
DHT: External genitalia, prostate, male pattern baldness, Acne, Facial/Body hair
I: Hypogonadism, Increase bone density in osteoporosis, increase muscle mass (+N balance), aplastic anemia
AE:
Testosterone Oxandrolone Stanozolol Fluoxymesterone Nandrolone Oxymetholone
Androgens, DHT is more potent than testosterone and androstenedione
PE: testosterone: Wolffian duct, spermatogenesis, bone formation and muscle growth
DHT: External genitalia, prostate, male pattern baldness, Acne, Facial/Body hair
I: Hypogonadism, Increase bone density in osteoporosis, increase muscle mass (+N balance), aplastic anemia
AE: Over-masculinization, Hirsutism, suppress menses, acne, clitoral enlargment, BPH, Premature closure of epiphyseal plate
**Excess use–>feminization due to feedback inhibition and conversion of exogenous testosterone into estrogen
Flutamide
Bicalutamide
Nilutamide
Androgen receptor blocker
I: used in conjuction with GnRH to reduce initial tumor flare ups
Finasteride
Dutasteride
5a reductase inhibitor
PE: Block conversion of testosterone to DHT
I: BPH, Male pattern baldness
AE: Gynecomastia, Impotence
