Pharm Gonadal Hormones And Inhibitors

Front 1

Question: The estrogen that is used in most combined hormonal contraceptives is?

Back 1

Ethinyl estradiol

Front 2

Question: A 23 year old woman desires a combined oral contraceptive for pregnancy protection. What is a factor that would lead a health professional to recommend an alternative form of a contraception in a women that has?

Back 2

A history of migraine headache; estrogen-containing hormonal contraceptives increases the risk of episodes of migraine headache.

Front 3

Question: Men who use large doses of anabolic steroids are at increased risk of:

Back 3

Large doses of anabolic steroids are associated with liver impairment, including cholestatic jaundice and elevation of aspartate transaminase

Front 4

Question: A 50 year old woman with a positive mammogram undergoes lumpectomy and a small carcinoma is removed. Biochemical analysis of the cancer reveals the presence of estrogen and progesterone receptors. After this procedure, she will probably receive?

Back 4

Tamoxifen, an antiandrogen (receptor antagonist) which decreases the rate of recurrence of cancer.

Front 5

Question: A young woman complains of abdominal pain at the time of menstruation. Careful evaluation indicates the presence of significant endometrial deposits on the pelvic peritoneum. The most appropriate therapy for this patient is?

Back 5

Medroxyprogesterone acetate by intramuscular injection.

In endometriosis, suppression of ovarian function and production of gonadal steroids are useful.

Front 6

Question: Diethylstilbestrol (DES) should never be used in pregnant women because it is associated with?

Back 6

Infertility and development of vaginal cancer in female offspring. Also result in fetal damage.

DES is a nonsteroidal estrogen agonist.

Front 7

Question: The unique property of SERMs is that they?

Back 7

Act as agonists in some tissues and antagonists in other tissues. Tamoxifen and raloxifene are examples of SPERMs.

Front 8

Finasteride has efficacy in the prevention of a male-pattern baldness by virtue of its ability to?

Back 8

Reducing the production of DHT by inhibiting 5-alpha-reductase (which converts testosterone to DHT).

Note: used to treat BPH and male-pattern hair loss

Front 9

Question: A 60 year old man is found to have a prostate lump and an elevated prostate-specific antigen (PSA) blood test. Magnetic resonance imagining suggests several enlarged lymph nodes in the lower abdomen, and x-ray film reveals 2 radiolucent lesions in the body pelvis. This patient is likely to be treated with?

Back 9

Flutamide, a competitive antagonist of the androgen receptor.

Note: used to treat advanced prostate cancer.

Front 10

Question: A 52 year old postmenopausal PT has evidence of low bone mineral density. She and her physician are considering therapy with raloxifene or a combination of conjugated estrogens and medroxyprogesterone acetate. What characteristic of the PT will lead to the selection of raloxifene?

Back 10

Strong family of history of breast cancer.

Conjugated estrogens and raloxifene both improve bone mineral density and protect against osteoporosis. The 2 advantages of raloxifene over full estrogen receptor agonists is that raloxifene has antagonist effects in breast tissue and lacks an agonistic effect in endometrium.

With a strong family history of breast cancer, raloxifene may be a better choice than a full estrogen agonist because it will not further increase the woman's risk of breast cancer and may even lower her risk.

Front 11

What is a synthetic estrogen with high bioavailability used in hormonal contraceptives?

Back 11

Ethinyl estradiol

Front 12

What are the effects of estrogen?

Back 12

Growth of genital structures; secondary sexual characteristics; growth spurt during puberty; modifies serum protein level; reduce bone resorption; enhances coagulability of blood; increases plasma triglyceride while reducing LDLD and increasing HDL.

Front 13

What effect is produced from continuous administration of estrogen with progestin?

Back 13

Inhibits secretion of gonadotropins form the anterior pituitary .

Front 14

What are the clinical uses of estrogen?

Back 14

Hypogonadism in young females; HRT in women with estrogen deficiency from premature ovarian failure; menopause; surgical removal of ovaries; HRT ameliorates hot flushes and atrophic changes in the urogenital tract; prevents bone loss and osteoporosis.

Front 15

What can estrogen therapy be used with in men?

Back 15

Men with androgen-dependent prostate cancer

Front 16

What are the SE of estrogen therapy?

Back 16

Premature closure of the epiphyses of long bones and short statue (when used with hypogonadal girls); increase risk of endometrial cancer, breast cancer; MI, stroke, DVT.

Also: migraine headache, gallbladder disease, hypertriglyceridemia, and hypertension.

Front 17

How can you prevent the risk of endometrial cancer with treatment of estrogen therapy?

Back 17

When estrogen is combined with progestin.

Front 18

Diethylstilbestrol (DES) increases the risk of?

Back 18

Is a nonsteroidal estrogen. Associated with infertility, ectopic pregnancy, vaginal adenocarcinoma in daughters of women treated with DES during pregnancy.

Front 19

What is the major progestin in humans?

Back 19

Progesterone

Front 20

What are the effects of progesterone?

Back 20

Induces secretory changes in the endometrium; increases the vascularization of the endometrium; affect carbohydrate metabolism and stimulate the deposition of fat.

Front 21

What is the effect of high doses of progesterone?

Back 21

Suppresses gonadotropin secretion and causes anovulation in women.

Front 22

What are the clinical uses of progestin?

Back 22

Contraceptive alone or with estrogen; used with estrogen to prevent estrogen-induced endometrial cancer; to promote and maintain pregnancy.

Front 23

What is the SE of progestin?

Back 23

Weight gain, reversible decrease in bone density

Front 24

Hormonal contraceptives include what in them?

Back 24

Combination of estrogen and progestin or a progestin alone.

Front 25

Postcoital contraceptives can include progestin (L-norgestrel) alone, estrogen alone, or estrogen and progestine together. Which one produces the fewer SE?

Back 25

Progestin (L-norgestrel) alone.

Front 26

What is the MOA of hormonal contraceptives?

Back 26

When administered before the LH, they inhibit ovulation. THey affect the cervical mucus, tubal function, and endometrial lining.

Front 27

What are some other clinical uses of hormonal contraceptives?

Back 27

To prevent hypogonadism to prevent estrogen deficiency; treat acne, hirsutism, dysmenorrhea, and endometriosis; reduce risk of ovarian cysts, ovarian and endometrial cancer, benign breast disease, and pelvic inflammation; lowers the incidence of ectopic pregnancy, iron deficiency anemia, and rheumatoid arthritis.

Front 28

What are the SE of hormonal contraceptive therapy?

Back 28

Thromboembolism (increases with smokers); earlier onset of breast cancer if predispose; increase triglycerides, depression, weight gain, hypertension.

Front 29

What are selective estrogen receptor modulators (SERMs) and what are three examples.

Back 29

Mixed estrogen agonist in some tissues and partial agonists or antagonists in other tissues.

Tamoxifen, Raloxifene, Clomiphene.

Front 30

Describe the antagonist/agonist effect of tamoxifen and its uses.

Back 30

Antagonist: on breast tissue; therefore, used for hormone-responsive breast cancer.

Agonist: on endometrial tissues; therefore increase risk of endometrial cancer. On bone tissue; therefore, prevents osteoporosis.

Front 31

What are the SE of tamoxifen and raloxifene?

Back 31

Hot flushes (antagonist effect), increase risk of venous thrombosis (agonist effect).

Front 32

Describe the antagonist/agonist effect of raloxifene and its uses.

Back 32

Partial agonist: on bone; therefore, used to prevent osteoporosis.

Antagonist: on breast tissue; therefore, reduces risk of breast cancer.

Front 33

How is Raloxifene different than tamoxifen?

Back 33

Has no estrogenic effects on endometrial tissue; therefore, no risk of endometrial cancer.

Front 34

Describe the partial agonist effect of clomiphene and its uses.

Back 34

Partial agonist: on estrogen receptors in hypothalamus. It reduces the negative feedback from estrogen and increases the release of LH and FSH to stimulate ovulation.

Front 35

What is a pure estrogen receptor antagonist in all tissue, and what is it used for?

Back 35

Fulvestrant is used in the treatment of women with breast cancer that has developed resistance to tamoxifen.

Front 36

What are two aromatase inhibitors, and what are they used for?

Back 36

Anastrozole (nonsteroidal competitive inhibitor) and exemestane (irreversible inhibitor).

They are used in the treatment of breast cancer.

Aromotase is used in the synthesis of estrogen.

Front 37

What drug inhibits CYP450 involved in gonadal steroid synthesis, is a weak partial agonist of progestin, androgen, and glucocorticoid receptors? What is it used for?

Back 37

Danazol is sometimes used for endometriosis and fibrocystic disease of the breast.

Front 38

What is a GnRH agonist used to suppress gonadotropin secretion and therefore, inhibit ovarian production of estrogen and progesterone? What is it used for?

Back 38

Leuprolide can be used for precocious puberty, and short-term treatment of endometriosis and uterine fibroids in women. It can be used with flutamide for prostate cancer.

When used in a pulsatile fashion (is an agonist now), can be used to treat infertility.

Front 39

What is the MOA of mifepristone (RU 486) and what is it used for and with what?

Back 39

It is a competitive inhibitor of progestins.

It is used with misoprostol (PGE1) for an abortifacient.

Front 40

What are the SE of mifepristone?

Back 40

Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain.

Front 41

How is dihydrotestosterone (DHT) formed?

Back 41

Testosterone is synthesized from progesterone and DHEA. Testosterone is converted to DHT, in several organs (e.g., prostate)

Front 42

In addition to sex characteristics produced from testosterone, what else does it do?

Back 42

Increase muscle mass and strength, increase RBC production, excretion of urea nitrogen is reduced, and nitrogen balance becomes more positive. Helps to maintain normal bone density.

Front 43

What are the clinical uses of testosterone?

Back 43

Hypogonadism, stimulate RBC, promote weight gain in wasting sydnromes (e.g., AIDS), stimulation of anabolism to promote recovery after burn or injury, treat ER-positive breast cancer (exemestane).

Front 44

What are the SE of testosterone?

Back 44

Virilization; menstrual irregularity, in men, can cause feminization (gynecomastia, testicular shrinkage, infertility) as a result of feedback inhibition of the pituitary and conversion of exogenous androgens to estrogens.

Cholestatic jaundice, elevation of liver enzymes, hepatocellular carcinoma, premature closure of epiphyseal plates; increase LDL, decrease HDL

Front 45

What are two antiandrogen receptor inhibitors?

Back 45

Flutaminde and spironolactone

Front 46

What is the MOA of flutamide and its what is it used for?

Back 46

Nonsteroidal competitive antagonists of androgen receptors.

Note: by blocking androgen receptor, flutamide causes the relief of testosterone's inhibition of GnRH; therefore, with lower levels of testosterone detected, there will be increase release of LH. To counteract this, leuprolide is always administered with flutamide.

Front 47

What is the MOA spironolactone and what is it used for?

Back 47

Inhibits androgen receptors.

K sparing diuretic, treatment of hirsutism in women.

Front 48

Ketoconazole and spironolactone are both used in the treatment of? What are their SE?

Back 48

Polycystic ovarian syndorme, prevent hirsutism.

Both cause gynecomastia and amenorrhea.

Front 49

What converts testosterone to DHT and in what tissues? What drug inhibits this enzyme and what is it used for? What is it less likely to cause then other antiandrogens?

Back 49

Finasteride inhibits 5-alpha-redcutase, which the enzyme is used in prostate cells and hair follicles.

Finasteride is used to treat prostatic hyperplasia and prevent hair lose.

It is less likely to cause impotence, infertility, and loss of libido.

Front 50

What is the MOA of combined hormonal contraceptives to treat hirsutism in females?

Back 50

The estrogen in the contraceptive acts in the liver to increase the production of sex hormone-binding globulin, which in turn reduces the concentration of the free androgen in the blood.

Front 51

What is the MOA of ketoconazole?

Back 51

It is an antifungal drug that inhibits gonadal and adrenal steroid synthesis.

Treatment of prostate cancer.