Pharmacol of Repro Hormones (Ascoli)

Question 1

What do the ligand and DNA binding domains of steroid receptors recognize?

Answer 1

ligand binding domain recognizes the steroid; DNA binding domain recognizes a gene specific sequence of the steroid

Question 2

Progesterone Receptor A is mostly a transcriptional _____ whereas Progesterone Receptor B is mostly a transcriptional _______.

Answer 2

activator; repressor

Question 3

True or false: Estrogen Receptors A and B are products of the same gene but use different promoters and start sites.

Answer 3

False. It is progesterone receptors A and B that are the products of the same gene.

Question 4

(oral) progestin with enhanced activity as mineralocorticoid antagonist and androgen antagonist

Answer 4

drospirenone

Question 5

(oral) selective progesterone receptor modulator (PRM) that can be an agonist or an antagonist, depending on the tissue

Answer 5

ulipristal

Question 6

(oral) progesterone antagonist

Answer 6

mifepristone

Question 7

among the first non-steroidal estrogens, this drug is no longer in use

Answer 7

DES (diethylstilbestrol)

Question 8

an environmental contaminant with estrogen-like effects

Answer 8

BPA

Question 9

selective estrogen receptor modulator (SERM) that can be an agonist or an antagonist depending on the tissue

Answer 9

tamoxifen

Question 10

All of these may be given orally except:
A. medroxyprogesterone
B. norethindrone
C. ulipristal
D. drospirenone
E. mifepristone

Answer 10

A. Medroxyprogesterone is given as an IM injection.

Question 11

ovulation may be induced by what type of inhibitor or antagonist?

Answer 11

aromatoase inhibitor or estrogen antagonist

Question 12

type of antagonsit that is effective in stimulating abortion

Answer 12

progesterone

Question 13

True or false: selective estrogen receptor modulators are effective in both breast cancer and hormone replacement therapy.

Answer 13

True. Aromatase inhibitors may also be used to treat breast cancer.

Question 14

_____ work by inhibiting gonadotropin secretion and, more importantly, by increasing the viscosity of the cervical mucus.

Answer 14

Progestins

Question 15

Adverse effects of this type of contraception include headaches, nausea, weight gain, and in some cases, thromboembolism.

Answer 15

combination-type

Question 16

Health benefits of this type of contraception include decreased risk of ovarian and endometrial cancers and increased HDL production.

Answer 16

combination-type

Question 17

this type of contraception includes preparations such as high dose oral progestin (norgestrel) and selective PRMs (ulipristal)

Answer 17

postcoital

Question 18

describe 2 mechanisms of action of selective progesterone receptor modulators (PRMs) such as ulipristal

Answer 18

1. works as an antagonist to progesterone receptors in granulosa cells, which are stimulted by progesterone prior to follicular rupture
2. works as an agonist of progesterone receptors in the pituiatary and hypothalamus, inhibiting gonadotropin secretion

Question 19

type of highly effective, non-hormonal contraception that acts as a spermicidal agent

Answer 19

copper IUD

Question 20

True of false: though both of these SERMs are used in the treatment of postmenopausal symptoms, osteoporosis and estrogen-dependent breat cancer, one advantage of tamoxifen over raloxifene is that it does not stimulate endometrial proliferation.

Answer 20

False. It is raloxifene that does not stimulate endometrial proliferation.

Question 21

estrogen receptor antagonist that is used to stimulate ovulation by preventing the early inhibitory effects of estrogen on gonadotropin secretion early in the follicular phase of the menstrual cycle

Answer 21

clomiphene

Question 22

SERM that acts as an agonist on the vaginal epithelium and is approved for the treatment of vaginal atrophy in post-menopausal women.

Answer 22

ospemifene

Question 23

SERM that has estrogenic effects on bone (preventing bone loss) but no estrogen effects on the breast or endometrium

Answer 23

bazedoxifene

Question 24

these steroidal or non-steroidal inhibitors are used in postmenopausal women for the the treatment of breast cancer or other disorders where estrogen action needs to be inhibited - also used to induce ovulation

Answer 24

aromatase inhibitors

Question 25

steroidal aromatase inhibitor

Answer 25

exemstane

Question 26

non-steroidal aromatase inhibitor

Answer 26

anastrozole

Question 27

progesterone receptor antagonist indicated for abortions, postcoital contraception, and as a glucocorticoid antagonist for the treatment of individuals with Cushing’s and type 2 diabetes

Answer 27

mifepristone (RU486)

Question 28

Inhibitors of this enxyme can be effectively used as “antiandrogens”

Answer 28

5α-reductase

Question 29

True or false: the affinity of the one and only androgen receptor for DHT is higher than its affinity for testosterone

Answer 29

True

Question 30

17-alkylated derivatives of testosterone (ie, danazol and methyltestosterone) give theses androgens what advantage? What is the disadvantage?

Answer 30

allows the steroid to survive its first pass through the liver and into the bloodstream, so that it can be taken orally; disadvantage = more side effects, particularly hepatic toxicity

Question 31

True or false: testosterone is ineffective when given orally.

Answer 31

True. Testosterone analogs such as danazol or methyltestosterone may be given orally, but testosterone must be administered transdermally or intramuscularly, and is sometimes given as a buccal tablet.

Question 32

2 antiandrogens that inhibit 5α-reductase, preventing the conversion of testosterone to its more potent form DHT

Answer 32

finasteride or dutasteride

Question 33

Flutamide, bicalutamide, and nilutamide are all antiandrogens that work by what mechanism of action?

Answer 33

androgen receptor antagonists

Question 34

2 antiandrogens that work by inhibiting steroid synthesis, disrupting testicular, adrenal and ovarian steroidogenesis

Answer 34

ketoconazole and spiranolactone

Question 35

gynecomastia and sexual dysfunction are side effects of what class of drugs?

Answer 35

antiandrogens

Question 36

True or false: pulastile GNRH increases gonadotropin secretion while continuous GNRH decreases it

Answer 36

True

Question 37

synthetic GNRH used to treat delayed puberty in boys or girls and anovulatory disorders, endometriosis and dysmenorrhea in women; may be administered as a single injection or with a pump in a pulsatile fashion

Answer 37

gonadorelin