Pharmacology of sex hormones

Question 1

What are the most widely used form of hormonal contraception due to their ease of use and effectiveness

Answer 1

Oral contraceptives

Question 2

What are the estrogen components of oral contraceptives, which is metaobolized to other

Answer 2

Ethyinyl estradiol and mestranol, mestranol is metabolized to ethinyl estradiol in liver and gut

Question 3

What allows the estrogen components to be orally available in oral contraceptives

Answer 3

Ethinyl group (C triple bond C)

Question 4

What are the first generation progestins

Answer 4

norethindrone, ethynodiol diacetate, norgestrel, norethindrone acetate

Question 5

What is the 2nd generation progestin

Answer 5

Levonorgestrel

Question 6

What are the 3rd generation progestin

Answer 6

Norgestimate and Desogestrol

Question 7

What is the 4th generation progestin, what is interesting about this agent

Answer 7

Drospirenone, has no estrogenic or androgenic activity with low to no progestational activity

Question 8

What is the biggest setback of first generation progestins

Answer 8

They have estrogenic activity causing side effects

Question 9

Which progestin agents has the most progestational activity, which has the most androgenic activity, little to no estrogenic activity

Answer 9

Levonorgestrel and Desogestrel, Levonorgestrel has the most androgenic activity while Desogestrel has little to no estrogenic activity

Question 10

What is the mechanism of action of combination oral contraceptives

Answer 10

Suppress LH and FSH causing no mid-cycle LH surge thus preventing ovulation

Question 11

T/F: Having only a estrogen component or a progestin component alone prevents ovulation but a combination acts synergistically and consistently

Answer 11

True

Question 12

What is the MOA of estrogens in oral contraceptives

Answer 12

Primary effect is stabilize endometrial lining and provide cycle control causing less bleeding, suppress FSH release, possibly block LH surge and ovulation

Question 13

What is the MOA of progestins in oral contraceptives

Answer 13

Primary effect is it diminshes the frequency of GnRH pulses and blocks LH surge preventing ovulation, produces thick mucus

Question 14

T/F: Estrogens provide the most contraceptive effect

Answer 14

False: Progestins provide the most contraceptive effect

Question 15

What does it mean if an Oral contraceptive is combined monophasic

Answer 15

One concentration of etrogenic component and one concentration of progestin component

Question 16

T/F: If an oral contraceptive is triphasic that means it has diffferent concentrations of components scheduled for different days

Answer 16

True

Question 17

What are risk in taking oral contraceptives

Answer 17

Cardiovascular, increased risk of venous thromboembolism, acute heart attack in smokers with hypertension over the age of 35

Question 18

What is perimenopause, how long is it

Answer 18

Period preceding to menopause, 2-8 years

Question 19

What are symptoms of perimenopause/menopause

Answer 19

Vasomotor symptoms, Hot flashes, night sweats, irregular bleeding, vaginal dryness

Question 20

What is hormone replacement therapy

Answer 20

Medications containing female hormones to replace the ones the body no longer makes after menopause

Question 21

Why would estrogen-based hormone replacement therapy be used

Answer 21

Primarily used for treatment of vasomotor and urogenital symptoms of menopause and for prevention of osteoporosis

Question 22

When would progestin be added hormone replacement therapy, when would a patient only take estrogen-based HRT

Answer 22

Endometrail hyperplasia and carcinoma, Hypersectomy

Question 23

What is the biggest risk for using hormone replacement therapy

Answer 23

Endometrial (uterine) cancer, venous thromboembolism, breast cancer, gallbladder disease

Question 24

What are the two most common Selective estrogen receptor modulators (SERMs), what is their MOA

Answer 24

Tamoxifen and Raloxifene, bind to estrogen receptors but cause their conformation to no longer support cancer growth

Question 25

Why are aromatase inhibitors used

Answer 25

Prevent testosterone from being converted to estrogen thus preventing more tumor growth in breast cancer

Question 26

What is an irreversible aromatase inhibitor, what is a reversible aromatase inhibitor

Answer 26

Exemestane/ Anastrozole and Letrozole

Question 27

T/F: Reversible aromatse inhibitors can also be used in female infertility and gynecomastia in children and adolescents

Answer 27

True

Question 28

What is the MOA of antiandrogens

Answer 28

inhibit circulating androgens by blocking androgen receptors and/or suppressing androgen synthesis, inhibits gonadotropin secretion reducing LH and FSH and testosterone

Question 29

What is the most common antiandrogens, when would it be used, side effects

Answer 29

Cyproterone acetate/ prostate cancer/ feminization, reversible infertility sexual dysfucntion, fatigue, irritability

Question 30

When are gonadotropins given to patients, what are they, who are they purified from

Answer 30

Treat infertility in patients with gonadotropin deficiency, Human menopausal gonadotropin (hMG): urine of postemopausal women, Human chorionic goadotropin (hCG): from urine of pregnant women

Question 31

T/F: hMG has mostly LH while hCG has a mixture of FSH and LH

Answer 31

False: Human menopausal gonadotropin has a mixture of FSH and LH while Human chorionic gonadotropin is mostly LH

Question 32

How do GnRH (LHRH) lead to less LH and FSH, what is a risk of this therapy

Answer 32

Initially promote LH and FSH but after longer exposure (10 days) the receptors undergo desensitization and internalize causing a decrease in FSH and LH, tumor growth due to increase testosterone and Estrogens

Question 33

What is a typical GnRH agonist

Answer 33

Goserelin

Question 34

What is MOA GnRH antagonists

Answer 34

Competitively and reversibly bind to GnRH receptor thereby LH and FSH relase from the pituitary