Gonadal Hormones

Question 1

Prolactin feed back inhibits the release of what? leading to what?

Answer 1

GnRH - leading to decreased spermatogenesis or ovulation

Question 2

ACTH acts on what enzyme to increase synthesis of cortisol?

Answer 2

desmolase (cholesterol to pregnenolone)

Question 3

Name 2-6 important physiological functions of estrogen that are NON-reproductive

Answer 3

prevent bone loss
lead to closure of epiphyseal plates in long bones
pro-coagulation state (+)
increase HDL and lower LDL
increase binding protein levels of some hormones (free levels are unaffected)
increase cholesterol in bile (form gallstones)

Question 4

Which estrogen is a prodrug that gets converted to ethinyl estradiol and is present in some contraceptives?

Answer 4

Mestranol

Question 5

How are oral contraceptives metabolized? What drugs can decrease their efficacy?

Answer 5

P450 system - CYP inducers decrease their efficacy by leading to more rapid breakdown

Question 6

exposure to diethylstilbestrol in utero can lead to what complications in the fetus?

Answer 6

(DES) if female, fetus can have infertility and vaginal cancer

Question 7

Name the 4 ABSOLUTE contraindications of estrogen use

Answer 7

1. history of thromboembolism
2. breast and endometrial cancer
3. pregnancy
4. liver disease

Question 8

Which SERM has an increased risk of endometrial cancer due to agonist affects there?

Answer 8

Tamoxifen

Question 9

Which SERM can be used as prophylaxis for breast cancer in high risk patients? What does it also help prevent?

Answer 9

Raloxifene

also agonistic on bone - prevents osteoporosis

Question 10

Patient at high risk of breast cancer who has had endometrial cancer in the past can be treated with which SERM?

Answer 10

Raloxifene - antagonistic in breast with no effects on endometrium

Question 11

Which drug can be given IM in the treatment of breast cancer that is resistant to Tamoxifen? What class of drug is this?

Answer 11

Fulvestrant - SERD (selective estrogen receptor downregulator)

Question 12

What does the enzyme aromatase do? Name three drugs that inhibit it. Which is irreversible?

Answer 12

Converts androgens to estrogen

Letrozole, Anastrozole, and Exemestane (irreversible)

Question 13

Which drug helps treat female infertility by acting as an estrogen antagonist in the hypothalamus and anterior pituitary? How does this work?

Answer 13

Clomiphene - prevents feedback inhibition of GnRH release in hypothalamus so anterior pituitary releases LH and FSH

Question 14

Clomiphene - type of drug and side effects (4)

Answer 14

SERM in hypothal and ant pituitary

ovarian hyper-stimulation syndrome
ovarian enlargement
multiple pregnancy
visual disturbances

Question 15

Which drug is a spironolactone derivative that is used in OC to treat acne in females? How does it work?

Answer 15

Drospirenone - antagonizes aldosterone effects

Question 16

Name 4 of the new preparation progestins. What advantage do they have over the old?

Answer 16

Desogestrel, Norelgestromin, Etonogestrel, Norgestimate

fewer androgenic effects

Question 17

Which drug is used as the “morning after” pill or as an abortifacient? what type of drug is it?

Answer 17

Mifepristone - antiprogestin

Question 18

Which androgen is most potent in males that leads to male pattern baldness and BPH? What enzyme is responsible for its creation?

Answer 18

DHT

made from testosterone by 5-alpha-reductase

Question 19

What are the two synthetic androgens that are more potent and have less andorgenic effects? What do they treat? How are they given?

Answer 19

Oxandrolone and Stanozolol

treats hypogonadism and increase bone density (osteoporosis)

transdermal, buccal, or subcutaneous implant

Question 20

Excess use of androgens in males can lead to what adverse effects?

Answer 20

feminization (lolololol) - gynecomastia, testicular shrinkage, infertility (due to feedback inhibition)

Question 21

Androgen receptor antagonist drugs have what ending? Name 3

Answer 21

• lutamide

Flutamide, Bicalutamide, Nilutamide

Question 22

Name the 5-alpha-reductase inhibitor. What is it used for?

Answer 22

finasteride - treats BPH

Question 23

Name the steroid synthesis inhibitor that is used to treat advanced prostate cancer that is resistant to first line drugs

Answer 23

Ketoconazole

Question 24

What drugs can be used to produce reversible medical castration? (name and class) - what is important to remember about giving them?

Answer 24

Leuprolide and gonadorelin (antiandrogens - GnRH analogs)

must be given continuously (pulsatile has the opposite effect)

Question 25

What drug treats hirsutism? what type of drug is it?

Answer 25

spironolactone (androgen receptor antagonist)

Question 26

What two antiandrogens are used to treat prostate cancer? What type of drugs?

Answer 26

Leuprolide - GnRH analog

Flutamide - Androgen receptor antagonist

Question 27

Randy wants to become Sandy. What hormone can you give? What type of drug is it?

Answer 27

Cyproterone - androgen receptor antagonist

Question 28

what drug treats BPH and male pattern baldness? type of drug?

Answer 28

Finasteride - 5-alpha-reductase inhibitor

Question 29

What drug can treat both Cushing’s disease and metastatic prostatic cancer? How does it work?

Answer 29

Ketoconazole - steroid synthesis inhibitor

Question 30

When do you give Aromatase Inhibitors

Answer 30

2nd line for Breast CA after Tamoxifen

Question 31

What do you give for Post-menopausal Breast CA mets

Answer 31

Toremifene

Question 32

What is a partial agonist at progestin, androgen and glucocorticoid

Answer 32

Danazol

Question 33

What do you give Danazol for

Answer 33

Endometriosis

FCC

Question 34

Danazol AE

Answer 34

Hep

Masculinization/Hirsutism