Estrogens, Progestins, And Hormone Replacement

Question 0

List 4 progestins

Answer 0

Progesterone
Medroxyprogesterone
Norethindrone
Norgestimate

Question 1

List 3 estrogens

Answer 1

Estradiol
Conjugated Estrogens
Ethinyl estradiol

Question 2

SERMS

Answer 2

• Tamoxifen

- Raloxifene

Question 3

Bisphosphates

Answer 3

Alendronate

Ibandronate

Question 4

1) Estrogens do what to the endometrium?

2) Progesterone does what to endometrium?

Answer 4

1) Stimulate growth
2) Inhibits endometrial growth, maintains vascular supply and secretory capacity, an its withdrawal leads to menstruation.

Question 5

Metabolic effects of estrogen includes:

Answer 5

• Decreased bone resorption
• Decreased total and LDL cholesterol, increased HDL and Trigs
• Increased synthesis of blood clotting factors and angiotensinogen
• Increased levels of binding globulins for thyroxine, cortisol, sex steroids

Question 6

What has rapid first pass metabolism in the liver when given orally and is mainly used in hormone replacement therapy (HRT) and hypogonadism?

Answer 6

Estradiol- Can be in slow-release depot forms for IM injection, Topical preps, micronized oral prep.

Question 7

Most common of several natural estrogen preparations, containing ester conjugates and salts of estrone and estriol. Major use is in HRT. What is it?

Answer 7

Conjugated Estrogens

Question 8

What is a synthetic estradiol analog?

Answer 8

Ethinyl estradiol

Question 9

What does the Ethinyl group do in ethinyl estradiol?

Answer 9

Slows metabolism, increases potency and oral effectiveness.

Question 10

What is a prodrug of ethinyl estradiol?

Answer 10

Mestranol

Question 11

Therapeutic uses of estrogens include:

Answer 11

-Hypogonadism, hypopituitarism.
A) Replacement therapy to promote normal growth and development of secondary sexual characteristics.
B) Low dose for growth stimulation, higher doses for epiphysial closure and sexual development. Gonadotropins (LH and FSH) required for fertility.

• Post-menopausal replacement therapy
• In oral contraceptives

Question 12

SE of estrogens

Answer 12

• Nausea, edema, breast tenderness, hyperpigmentation
• Migraine, cholestasis, insulin resistance, liver and gallbladder disease
• Thromboembolic complications
• Endometrial hyperplasia- increase risk of cancer
• Gynecomastia, feminization in men
• Teratogenesis occurred with long-ago use of DES early in pregnancy
• Metabolic changes in cholesterol, bone, clotting factors, esp. high dose oral preps.

Question 13

What progestins are available?

Answer 13

• Progesterone
• Medoxyprogesterone
• Norethindrone
• Norethindrone
• Norgeastimate

Question 14

What may be safer for long-term HRT for progesterone? Available in IM, creams, suppositories, slow release IUD.

Answer 14

Progesterone (generic)

Question 15

What is the prototype of synthetic progestins structurally related to progesterone (21 carbons)? Used as the acetate ester.

Answer 15

Medoxyprogesterone

Question 16

T/F: Medoxyprogesterone has mainly progesterone-like effects, with little or no concern about androgen or estrogen activity?

Answer 16

True

Question 17

What is the prototype of synthetic progestins structurally related to testosterone (18 carbons)?

Answer 17

Norethindrone

Question 18

T/F: Norethindrone retains some androgenic activity, causing beneficial effects?

Answer 18

False- causing unwanted side effects.

Question 19

How is Norethindrone administered and how are the used?

Answer 19

Oral- used in oral contraceptives, some now for HRT.

Question 20

What is a new derivative of northindrone with essentially no androgenic effect and are used only in combo oral contraceptives?

Answer 20

Norgestimate

Question 21

Adverse effects of androgenic progestins are…

-SE for all progestins include…

Answer 21

Acne, wt. gain, masculinization, altered libido, decreased HDl and increased LDL.

-All progestins: Menstrual changes, nausea, bloating, teratogenesis, others

Question 22

The women’s health initiative (WHI) found that HRT for long term use does what?

Answer 22

-Increase risk of coronary heart disease, strokes, and pulmonary embolisms.Reduced osteoporosis and colorectal cancer. Both estrogen and progestin increase risk of breast CA.

Question 23

If a patient has no uterus, what would you use for HRT?

Answer 23

Just estrogen

Question 24

Side effects of HRT include…

Answer 24

-Return to vaginal bleeding, breast swelling and tenderness, plus disease risk of endometrial cancer, breast ca, CV effects.

Question 25

What is used for its agonist effect on bone in osteoporosis?

Answer 25

Raloxifene

Question 26

What is used for its antagonist effect in breast CA?

Answer 26

Tamoxifen

Question 27

What has agonist actions to increase uterine cancer risk and risk of thrombotic disease?

Answer 27

Tomoxifen. Raloxifene has antagonist effect in uterine cancer (good).

Question 28

T/F: Tamoxifen and Raloxifene both have antagonistic effects on menopausal symptoms which may cause hot flashes and other menopausal symptoms.

Answer 28

True

Question 29

T/F: Tamoxifen (and Raloxifene) have beneficial agonist effects on bone resorption?

Answer 29

True

Question 30

T/F: Tamoxifen and Raloxifine have agonist effects on blood lipid profiles to increase heart disease risk?

Answer 30

False- decrease