3.4.2 Reproductive Pharmacology

Question 1

What are the aromatase inhibitors?

Answer 1

competitive (anastrozole, letrozole)

Irreversible (exemestane, formestane)

Question 2

What are the three SERMs?

Answer 2

Tamoxifen (antagonist in breast), clomiphene (antagonist in hypothalmus/pituitary), raloxifene (antagonist in ___)

Question 3

What does the hypothalmus use to upregulates anterior pituitary production of LH/FSH?

Answer 3

GnRH

Question 4

What are some of the anti-androgens?

Answer 4

Question 5

What are the uses of aromatase inhibitors?

Answer 5

Early/advanced breast carcinoma

Question 6

Where is LH and FSH clinical pharmacology typically used?

Answer 6

Ovulation induction

Male infertility

Question 7

What are the different receptor agonists of estrogen?

Answer 7

Natural

Synthetic - Steriodal (ethinyl E2, mestronol, quinestrol) and Non-steriodal (Diethylstilbestrol, chlorotrianisene, methallenestrill)

Question 9

In what medical condition is there a lack of release of GnRH from the hypothalmus?

Answer 9

Kallman Syndrome

Question 10

Describe the release of GrRH

Answer 10

Pulsatile

Question 11

When is GnRH clinical pharmacology used?

Answer 11

Progressive precocious puberty

Prostate cancer

Endometriosis

Assisted reproduction

Uterine leiomyomata (fibroids)

Male/female infertility

Question 12

What are the uses of estrogen agonists?

Answer 12

Question 13

What are the clinical toxicity effects of GnRH in females? males?

Answer 13

Females: symptoms of menopause, ovarian cysts (temporary), osteoporosis

Males: Hot flushes, sweats, edema, gynecomastia, osteoporosis

Question 14

What are the two forms of progesterone and their functions?

Answer 14

Question 15

What are the 8 functions of estrogens?

Answer 15

Question 16

What are the receptor agonist/antagonists of progesterone?

Answer 16

Question 17

What are the four potential sites of pharmacological intervention?

Answer 17

The highlighted

Question 18

Clinical uses of progesterone?

Answer 18

Question 19

What are the 3 areas of reproductive pharm applications?

Answer 19

Replacement therapy for hormone deficiency

As antagonists for dz’s caused by excess production of pituitary hormones

As diagnostic tools for identifying several endocrine abnormalities

Question 20

What are the four different receptor antagonists of estrogen?

Answer 20

Tamoxifen, clomiphene, raloxifene, fulvestrant

Question 21

What are the agonists of FSH?

Answer 21

Menotropins, Urofollitropin, Follitropin alpha/beta

Question 22

What are the roles of FSH/LH in males and females? What are their feedback regulation mechanisms?

Answer 22

Question 23

What are the adverse effects and contraindications of estrogen?

Answer 23

Estrogen dependent neoplasm (breast, endometrium)

Undiagnosed genital bleeding

Hx of thromboembolitic disorders

Pregnant women

Question 24

What are the toxicities and contraindications of FSH/LH?

Answer 24

OHSS and multiple pregnancies

HA, depression, edema, precocious puberty

hot flushes, sweats, edema, typical symptoms of menopause

Question 25

What is the androgenic effect?

Answer 25

Question 26

How would agonists/antagonists work on GnRH?

Answer 26

Question 27

What is changed in the GnRH agonists?

Answer 27

The glycine residue is changed to prevent cleavage

Question 28

What is the therapeutic use of androgens?

Answer 28

Androgen replacement therapy: mimic the normal testosterone concentration?

Question 29

What are the three different forms of estrogen and their potency?

Answer 29

Estradiol - E2 (100%), Estriol - E3 (10%), Estrone - E1 (1%)

Question 30

What are some of the adverse effects of androgens?

Answer 30

Question 31

What is the agonist of LH? (taken off US market in 2012 b/c the drug company didn’t want to produce it)

Answer 31

Lutropin alpha

Question 32

What two ways can GnRH be manipulated pharmacologically?

Answer 32

Control pulstile release or inhibit receptor