Estrogens, Progestrins, And Androgens

Question 1

What is the main estrogen made by the ovary?

Answer 1

Estradiol

Question 2

What 2 estrogens are made by conversion from androgens in the liver and adrenal glands?

Answer 2

Estrone and estriol

Question 3

Which estrogen is high is high in pregnancy?

Answer 3

Estriol

Question 4

Where is estrogen made in the male?

Answer 4

Made by Sertoli cells in the testis

Question 5

What is the enzyme used to convert testosterone to estrogen in the testis?

Answer 5

Aromatase

Question 6

What are the physiological effects of estrogen?

Answer 6

1. Development of sex organs and secondary sex characteristics
2. Closure of the epiphyseal plates
3. Stimulate ductal development in breast
4. Pigmentation in the skin
5. Increase binding globulins
6. Increase HDL, decrease LDL
7. Reduce bone resorption
8. Enhance coaguability
9. Libido, mood

Question 7

Where is progesterone produced in the female?

Answer 7

By the corpus luteum

During pregnancy: placenta

Question 8

What are the physiological effects of progesterone?

Answer 8

1. Matures endometrium
2. Development of secretory apparatus of the breast
3. Increases body temp
4. Depressants effects, sedatives

Question 9

How does progesterone or its metabolites make inhibitory effects?

Answer 9

Hits GABBA A receptor

Question 10

How much testosterone is freely circulating?

Answer 10

2%

Question 11

What are the effects of testosterone?

Answer 11

1. Growth of pubic hair, axillary hair, beard
2. Growth of larynx, thickening of vocal chordsSebum secretion
3. Decrease binding globulin
4. Stimulate EPO secretion
5. Anabolic effects

Question 12

What is oxymetholone?

Answer 12

17-alkyl deriv of testosterone

Question 13

What oxymetholone used to treat?

Answer 13

Bone marrow hypoplasia, myelofibrosis

Question 14

What are 17-alkyl derivatives associated with?

Answer 14

Hyperbilirubinemia, increased hepatic enzymes, cholestatic hepatitis,

Question 15

What is the bioavailability of estradiol?

Answer 15

10%

Question 16

What may alter the efficacy of oral estrogens?

Answer 16

Broad spectrum antibiotics that alter intestinal flora

Question 17

What drugs might estrogens alter the metabolism of?

Answer 17

Drugs metabolized by glucoronidases. Like acetaminophen

Question 18

What is the MOA of oral contraceptives?

Answer 18

Exert negative feedback on the hypothalamus and pituitary –

1. Reduce GnRH
2. Reduce FSH secretion - incomplete follicular development
3. Reduce LH secretion - no ovulation

Question 19

How do OCs affect sperm and endometrium?

Answer 19

It thickens the cervical mucous to reduce sperm.

It alters the endometrial structure makes the uterus unreceptive for implantation

Question 20

What is the most commonly used estrogen in OCs?

Answer 20

Ethinyl estradiol

Question 21

What are th most commonly used progesterones?

Answer 21

Norethindrone
Levonorgestrel
Norgestimate
Desogestrel

Question 22

What is the potency of the progesterones used?

Answer 22

1. Desogestrel
2. Norgestrel
3. Norgestimate, norethindrone

Question 23

Which progesterone has an increased risk of thromboembolism?

Answer 23

Desogestrel

Question 24

Which estrogen has androgenicity that is similar to spironolactone?

Answer 24

Drospirenone in Yasmin

Question 25

What are the advantages of triphasic OCs?

Answer 25

Less spotting, breakthrough bleeding and amenorrhea

Question 26

Who do we use progestin only on?

Answer 26

Women at risk for certain estrogen-dependent cancers or who don't tolerate the estrogen portion in OCs or who are breast feeding

Question 27

What is the disadvantage of using progestin only?

Answer 27

It is not as effective at inhibiting ovulation

Question 28

What is injectable progestin for?

Answer 28

For long term contraception

Question 29

Who is injectable progestin not good for?

Answer 29

Women who want to get pregnant soon after treatment

Question 30

What are the disadvantages of implantable progestin?

Answer 30

Need for surgical implantation and removal | Irregular bleeding

Question 31

What can lower the efficacy of OCs?

Answer 31

Phenytoin Rifampin Antibiotics

Question 32

What are the side effects of estrogen?

Answer 32

TE - increases clotting factors and decreases antithrombin III Increase risk of MI HTN Nausea - heightened sense of smell Edema Headache or worsens migraines - converts tryptophan to nicotinic acid Cancer of breast, cervix, liver

Question 33

What are the side effects of progestin?

Answer 33

``` Increased appetite - increase in the amount of insulin Weight gain Depression Increased bp Increase acne and CV disease ```

Question 34

What are the contraindications to OCs?

Answer 34

``` Pregnancy Women with history of estrogen-dependent neoplasm or breast cancer TE disorders Liver disease Smokers ```

Question 35

What is plan b?

Answer 35

It is a high dose of levonorgestrel

Question 36

What is RU486?

Answer 36

Mifepristone - has a luteolytic effect, usually combined with a prostaglandin which may trigger uterine contraction

Question 37

What is DES?

Answer 37

May interfere with timing of uterine maturation

Question 38

What are the post coital contraceptives?

Answer 38

Plan B Mifepristone DES

Question 39

What is hormone replacement used for?

Answer 39

Reducing menopause symptoms Reducing osteoporosis Treating primary hypogonadism (ovarian failure, hypopituitarism)

Question 40

What is the treatment for menopause?

Answer 40

Low dose estrogen and a progestin

Question 41

What are the HRTs for menopause?

Answer 41

Conjugated equine estrogen Metroxy-progesterone acetate (provera) Estradiol Prempro (CEE + MPA)

Question 42

What are progestins given for in menopause?

Answer 42

For reducing endometrial and uterine cancer

Question 43

What are the benefits of HRT?

Answer 43

Reduces heart attacks and strokes Reduces hot flashes Decreases bone loss

Question 44

What are the problems with HRT?

Answer 44

Poor compliance because of bleeding and fear of cancer. | Hypogonadism

Question 45

What are the side effects with estrogen in HRT.

Answer 45

``` Hyper pigmentation Increased migraines Breast tenderness Nausea Bleeding Cancer ```

Question 46

What are the contraindications to HRT?

Answer 46

Hx of estrogen dependent cancers TE Liver disease Smoking

Question 47

What are the advantages of transdermal estradiol?

Answer 47

Reduced conversion of estradiol to estrone Little risk for TE No effect of SHBG

Question 48

What is the disadvantage of transdermal estradiol?

Answer 48

May not cause increase in HDL or lower LDL

Question 49

What is can androgen therapy be used for?

Answer 49

Hypogonadal men Reverse atrophy following trauma, surgery, disease Anemia Osteoporosis

Question 50

What are the side effects of androgen therapy?

Answer 50

``` Masculinizing effects or gynecomastia Hirsutism Acne Hepatic dysfunction Azospermia Abuse ```

Question 51

What are the contraindications to androgens?

Answer 51

Hx of prostate or breast cancer | Pregnant women

Question 52

What are the disorders or androgen excess?

Answer 52

``` Hirsutism Acne Amenorrhea Gynecomastia Prostatic hyperplasia - urinary retention PCOS Cushing's ```

Question 53

What drugs can be used for hirsutism?

Answer 53

OCs AR antagonist - spironolactone, flutamide DHT synthesis inhibitors - finasterides, dutasteride GnRh analogs Eflornithine cream - ornithine decarbox inhibitor

Question 54

What is clomiphene?

Answer 54

A partial estrogen agonist - reduces negative feedback so increases gonadotropins and estrogens

Question 55

What is Faslodex?

Answer 55

Pure anti- estrogen