Estrogen Therapy Flashcards Preview

Female Repro Pharm > Estrogen Therapy > Flashcards

Flashcards in Estrogen Therapy Deck (21)
Loading flashcards...
1
Q

What is the main estrogen produced by the ovary

A

Estradiol-17B

2
Q

Name 2 weak natural estrogens

A
  1. Estriol

2. Estrone

3
Q

Tell me again how estradiol-17B is made?

A

Aromatization reaction of testosterone or androstenedione. Catalyzed by aromatase enzyme (CYP19)

4
Q

Where do you find aromatase?

A
  1. Granulosa cells of the ovary
  2. Sertoli and leydig cells
  3. Adipose stroma
  4. Bone
  5. Brain (interesting)
5
Q

In a premenopausal woman, where does most of the circulating estrogen come from?

A

The ovaries

6
Q

What type of estrogen does the liver make?

A

Estriol and estrone. Catalyzed by type II hydroxysteroid dehydrogenase.

7
Q

In a postmenopausal woman, where does most of the circulating estrogen come from?

A

Estrone produced by adipose tissue

8
Q

What are the effects of estrogen in utero?

A

Formation of the:

  1. Vagina
  2. Uterus
  3. Fallopian tubes
9
Q

What are the effects of estrogen when girls go through puberty, the best time of your life

A
  1. Pubic and axillary hair growth
  2. Distribution of body fat
  3. Ductal and stromal development of breast
  4. Endometrial development
  5. Long bone development and eventual epiphyseal plate closure
10
Q

What are some of the metabolic effects of estrogen?

A
  1. increased bone mass (cause we ladies gots the strongest bones)
  2. Increased triglycerides (cause you ladies are fat) and reduces serum cholesterol
11
Q

What modification is needed to make estrogen preparations orally action

A

17alpha

17a ethinyl estradiol is the pharm prep of estrogen that we need to know

12
Q

What kind of disease would you consider using estrogen therapy for? (a bit intuitive)

A
  1. Hypogonadism: being replacement therapy between 11-13 yo and then switch to a 12a ethinyl estoradiol/progesterione OCP
  2. Menopausal hormone therapy
13
Q

We know that estrogen helps treat the symptoms of menopause. What specifically is estrogen helping with?

A
  1. Decreasing bone fractures
  2. Hot flashes (vasomotor sx)
  3. Vaginal dryness
  4. Urogenital atrophy
  5. Memory problems
14
Q

What are the consequences of hormone replacement therapy

A

Increased risk for MI and endometrial carcinoma

15
Q

What is norethindrone acetate. Do we still use this drug?

A

Its a estrogen progesterone combined hormone replacement therapy. No, the study was halted in 2002 because of increased risks of MI, stroke, blood clots and breast cancer

16
Q

There are three SERMS we need to know. (Selective estrogen receptor modulators). What are they? (more details on them later)

A

Remember the FENce drugs (women are hopping back over the fence from menopause to their pre-menopause estrogen levels)

  1. TamoxiFEN
  2. RaloxiFENe
  3. OspemiFENe

(The FENce is now TORn, n=nothing)

17
Q

TamoxiFEN. How does it’s effect differ based on the tissue it acts on?

A

*Breast: antagonist, decreased risk of cancer
Bone: agonist, decreased risk of osteoporosis
Endometrium: agonist, increased risk of cancer
Liver: agonist, increase risk of venous thrombosis

18
Q

RaloxiFENe. Describe its effect on bone, breast, endometrium

A

*Breast: antagonist, decreased risk of cancer
Bone: partial agonist, decreased risk of osteoporosis
Endometrium: antagonist, decreased risk of cancer

19
Q

Ospemifene. Why is this SERM so special?

A

It is the ONLY SERM that has estrogen like effects on the vagina. In post-menopausal women there can be vaginal atrophy leading to dyspareunia (pain during intercourse). This drug can help with that and also:

Bone: agonist, decreased risk of osteoporosis
Endometrium: antagonist: decreased risk of cancer
Breast: antagonist, decreased risk of cancer

20
Q

What is the one estrogen synthesis inhibitor we are responsible for knowing?

A

Letrozole

21
Q

How does letrozole work and what do we use it for?

A

It is an aromatase inhibitor that is used to treat breast cancer. Used first line or second line with tamoxifen.

Side effect: hot flashes