Sex Steroids + Androgens Flashcards
What are the u/e of estrogen?
- Nausea and breast tenderness, most common.
- endometrial hyperplasia and endometrial carcinoma.
- edema and weight gain.
- breast carcinoma.
- hyperpigmentation.
- thromboembolic events, Myocardial Infarction.
What are the uses of estrogens?
most common: oral contraceptives, then post-menopausal women experiencing vasomotor symptoms and vaginal atrophy. Also, replacement therapy in hypogonadism and osteoporosis.
What is combined with estrogen to prevent endometrial hyperplasia and endometrial carcinoma?
progestin
What is the most common estrogen drug?
estradiol
What estrogen drug has been associated with cervical and vaginal carcinoma in daughters of women who took it during pregnancy?
diethylstilbestrol
What is a SERM?
Selective estrogen receptors modulators.
mixed agonist-antagonist of estrogens. They interact at estrogen receptors but have selective agonism or antagonism according to the tissue type.
Which SERM is an antagonist to estrogen receptors in breast tissue, but estrogen-agonist in the uterus and bone? It prevents endogenous estrogens from stimulating tumor grownth
Tamoxifen -
used to treat estrogen receptor-positive breast cancer in postmenopausal women. u/e INCREASED risk of uterine cancer
Which SERM has agonist activity in bone and antagonist activity in breast and endometrial tissue? It binds to estrogen receptors and induces expression of genes that maintain bone density.
Raloxifene -
Used to treat and prevent osteoporosis.
Which SERM interferes w the negative feedback of estrogens by acting as a partial estrogen receptor agonist in the hypothalamus? It binds w the estrogen receptors and causes the hypothalamus to sense a lack of estrogen resulting in release of GnRH and Gonadatropins leading to a stimulation of ovulation.
Clomiphene. -
treats infertility in women
What is the drug used in oral contraceptives, replacement therapy and in the treatment of dysfunctional uterine bleeding, dysmenorrhea and management of endometriosis?
Progestins -
Medroxyprogesterone
What are the u/e of Progestins?
weight gain, edema, depression. Also increased clotting leading to thrombophlebitis or pulmonary embolism.
What works to terminate pregnancy by breaking down the uterine lining?
Mifepristone
who is most at risk for u/e of increased abnormal clotting when taking oral contraceptives?
women who smoke and are over age 35
What diseases can be caused by Androgens?
Prostate Cancer and Benign Prostatic Hyperplasia
What are the primary and unapproved uses of androgens?
Primary therapeutic use is for replacement therapy in patients w testicular deficiency. Unapproved use: anabolic steroids to increase lean body mass, muscle strength and endurance.
What are the side effects of Androgens in women?
virilization including acne, growth of facial hair, deepening of the voice and excessive muscle development
Name two testosterone derivatives:
testosterone propionate - palliative for breast cancer.
fluxymesterone - treats hypogonadism in male children
What is an example of Anabolic steroids?
DHEA - precursor of testosterone and estrogen.
What is the MOA of anti androgens?
they counter male hormonal action by interfering with the synthesis of androgens or by blocking their receptors
What is the MOA of 5-alpha-reductase inhibitors?
inhibit the enzyme which converts testosterone to DHT which is the major intracellular androgen in most target tissues. This results in decrease formation of DHT and reduction of prostate size. FINASTERIDE.
What drug is used to treat benign prostatic hyperplasia?
Finasteride - and at lower doses, stimulates hair growth.
5-alpha-reductase inhibitor
androgen
What is the MOA of Androgen receptor antagonists?
competitive inhibitors of androgens in target cells. FLUTAMIDE
What treats prostate carcinoma in males?
Flutamide
