Gonadal Hormones Flashcards
Esthinyl estradiol
Synthetic steroidal estrogen
Component of OCP
Mestranol
Synthetic steroidal estrogen
Quinestrol
Synthetic steroidal estrogen
Diethylstilbestrol (DES)
Synthetic non-steroidal estrogen
SE: Adenocarcinoma of the vagina
Chlorotrianisene
Synthetic non-steroidal estrogen
Methallenestril
Synthetic non-steroidal estrogen
Tamoxifen
SERM (estrogen receptor antagonist in breast, partial agonist in endometrium and bone)
Prevention, palliative, adjuvant therapy for breast CA
SE: malignant neoplasm of endometrium (give for
Clomiphene
SERM (estrogen receptor antagonist in hypothalamus and pituitary, partial agonist in ovaries) Disinhibits GnRH release and increases LH and FSH
Female infertility dt ovulatory disorder
SE: Thromboembolism, ovarian cysts and hypertrophy, flushing/vasomotor symptoms
Raloxifene
SERM (estrogen receptor antagonist in uterus and breast, agonist in bone)
Osteoporosis prevention and tx
SE: retinal vascular occlusion, venous thromboembolism, hot flashes, leg cramps
Decreases risk of invasive breast CA in postmenopausal women with osteoporosis
Fulvestrant
SERM (competitively inhibits estrogen binding to receptor. No agonist activity)
Tx of E2 receptor+ metastatic breast CA with disease progression
SE: nausea, asthenia, pain, hot flashes, HA
Anastrozole
Competitive aromatase inhibitor
Tx and prevention of E2 receptor+ early metastatic breast cancer
SE: osteoporosis, thrombophlebitis, profuse vaginal bleeding, hypercholestrerolemia, edema, rash, nausea, HA, depression, dyspnea
Letrozole
Competitive aromatase inhibitor
Tx and prevention of E2 receptor+ early metastatic breast cancer
SE: osteoporosis, thrombophlebitis, profuse vaginal bleeding, hypercholestrerolemia, edema, rash, nausea, HA, depression, dyspnea
Exemenstane
Irreversible aromatase inhibitor
Tx and prevention of E2 receptor+ early metastatic breast cancer
SE: osteoporosis, thrombophlebitis, profuse vaginal bleeding, hypercholestrerolemia, edema, rash, nausea, HA, depression, dyspnea
Formestane
Irreversible aromatase inhibitor
Tx and prevention of E2 receptor+ early metastatic breast cancer
SE: osteoporosis, thrombophlebitis, profuse vaginal bleeding, hypercholestrerolemia, edema, rash, nausea, HA, depression, dyspnea
Norgesterel
Progestin only contrceptive (decreases pulsation of GnRH, slows tubal peristalsis, decreases endometrial receptivity, thickens cervical mucus)
Norethindrone
Progestin only contrceptive (decreases pulsation of GnRH, slows tubal peristalsis, decreases endometrial receptivity, thickens cervical mucus)
Medroxyprogesterone acetate
Progestin only contrceptive (decreases pulsation of GnRH, slows tubal peristalsis, decreases endometrial receptivity, thickens cervical mucus)
Given parenterally q 3 months
Etonogestrel
Progestin only contrceptive (decreases pulsation of GnRH, slows tubal peristalsis, decreases endometrial receptivity, thickens cervical mucus)
Implant - effective for 3 years
Combined birth control
Suppress GnRH, LH, FSH, and follicular development, slows tubal peristalsis, decreases endometrial receptivity, thickens cervical mucus
CX: Breast/endometrial CA, CVA or CAD, cholestatic jaundice of pregnancy, liver tumors, severe HTN, prolonged immobilizaiton, female smokers over 35, thrombotic disorders
SE: AV thromboembolism, PE, cerebral thrombosis, gallbladder disease, HTN, hepatic neoplasm, breast tenderness, bloating, migraine, weight chage
Norgestrel and levonorgestrel have highest androgenic activity
Mifepristone
Inhibits progesterone binding to receptor
Abortion (through day 49)
SE: prolonged bleeding time, bacterial infections, sepsis, N/V/D, cramps, headaches
Levonorgestrel
Progestin that blocks LH surge to disrupt normal ovulation, produce endometrial changes, prevent implantation
Prevention of unwanted pregnancy
SE: N/V, HA, dizziness, mastalgia
Premarine
Conjugated equine estrogen
HRT Therapy
CX: Breast cancer
Estrace
Micronized estradiol
HRT Therapy
CX: Breast cancer
Cenestrin
Conjugated synthetic estrogens
HRT Therapy
CX: Breast cancer
Vivelle, estraderm, estrogel
Transdermal estrogens
HRT Therapy
CX: Breast cancer
Testosterone enanthate
Replacement of testosterone to produce androgenic effects
Tx: hypogonadism
SE: cholestatic jaundice, liver carcinoma, BPH, prostate cancer, gynecomastic, acne, HA
Testosterone cypionate
Replacement of testosterone to produce androgenic effects
Tx: hypogonadism
SE: cholestatic jaundice, liver carcinoma, BPH, prostate cancer, gynecomastic, acne, HA
Flutamide
Competitive inhibitor of DHT and testosterone binding to receptor
For metastatic prostate CA, BPH
SE: hepatotoxicity, hematopoeitic disorder, diarrhea, nausea, rash, hot flashes
Spironolactone
Competitive inhibitor of DHT and testosterone binding to the receptor
Hirsutism, HTN, acne, edema with CHF, cirrhosis or nephrotic syndrome, hypokalemia
SE: GI hemorrhage, hyperK, metabolic acidosis, agranulocytosis SLE, gynecomastic, dyspepsia, lethargy, impotence, rash
Finasteride
Selective inhibitor of 5 a-reductase (T to DHT) in prostate, liver, and skin
BPH, androgenic alopecia
SE: neoplasm of male breast, breast tenderness, decreased libido, erectile dysfunction, ejaculatory disorder
DO NOT USE IN WOMEN