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Pharmacology > Estrogen and Progesterone > Flashcards

Estrogen and Progesterone Flashcards

1
Q

What estrogen has the most estrogenic action?

A

Estradiol (E2)

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2
Q

What does LH target in females?

A

LH acts on Theca cells to synthesize androgen which is aromatized to E1 and E2 in Granulosa cells from FSH action

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3
Q

What does LH target in males?

A

LH stimulates testosterone production in the Leydig cells

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4
Q

What is the function of inhibins?

A

Inhibit FSH release

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5
Q

What is the function of activins?

A

Stimulate release of FSH

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6
Q

What is the function of aromatase?

A

Converts androgens to estrogen

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7
Q

What type of cervical mucus is secreted under estrogen control?

A

Thin mucus

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8
Q

What type of mucus is secreted under progesterone control?

A

Thick mucus

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9
Q

What is the effect of E2 on HDL and LDL?

A

Increases HDL

Decreases LDL

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10
Q

What are the main clinical uses of estrogens?

A
  • Oral contraceptive
  • HRT
  • Acne
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11
Q

What is the main SE of estrogen?

A

Endometrial hyperplasia and increased risk of endometrial carcinoma

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12
Q

Estrogen Contraindications

A
  • Breast and endometrial cancer
  • Pregnancy
  • Thrombotic disorders
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13
Q

What are SERMs?

A

Selective Estrogen Receptor Modulators

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14
Q

What are the actions of SERMs?

A

They bind estrogen receptors throughout the body and can act as an agonist OR antagonist depending on the tissue

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15
Q

Tamoxifen Indications

A

Use to treat and prevent breast cancer

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16
Q

Tamoxifen MOA

A

Estrogen receptor antagonist in breast tissue as a partial agonist in endometrium and bone

17
Q

Tamoxifen SE

A
  • Neoplasm of endometrium
  • Hot flashes
  • Abnormal menstruation
18
Q

Tamoxifen Contraindications

A
  • DVT

- Pregnancy

19
Q

Clomiphene MOA

A

Estrogen receptor antagonist in the hypothalamus and pituitary and partial agonist in the ovaries which disinhibits the release of GnRH and increases FSH and LH

20
Q

Clomiphene Indications

A

Female infertility from an ovulatory disorder

21
Q

Clomiphene SE

A
  • Thromboembolism
  • Ovarian cysts and hypertrophy
  • Abdominal discomfort
22
Q

Raloxifene Indications

A

Osteoporosis prevention and treatment

23
Q

Raloxifene MOA

A

Estrogen receptor agonist in bone and antagonist in the uterus and breast

24
Q

Fulvestrant Indications

A

Treat estrogen receptor positive metastatic breast cancer in post-menopausal women

25
Q

Fulvestrant MOA

A

Competitively inhibit estrogen binding to receptor and blocks the action of estrogen on its target tissues - pure antagonist

26
Q

Fulvestrant Contraindication

A

Pregnancy

27
Q

What are examples of aromatase inhibitors?

A
  • Anastrozole
  • Letrozole
  • Exemestane
  • Formestane
28
Q

Anastrozole/Letrozole Indications

A

Treatment and prevention of estrogen receptor positive early stage, locally advanced metastatic breast cancer

29
Q

Exemestane/Formestane Indications

A

Treatment and prevention of estrogen receptor positive early stage, locally advanced metastatic breast cancer

30
Q

Anastrozole/Letrozole MOA

A

Competitive inhibition of aromatase

31
Q

Exemestane/Formestane MOA

A

Irreversible inhibition of aromatase

32
Q

What is the main SE of all aromatase inhibitors?

A

Osteoporosis and fractures

33
Q

Norgestrel MOA

A

Alter GnRH pulsing and responsiveness of the anterior pituitary gland to GnRH

34
Q

Norgestrel Indications

A

Contraception

35
Q

Mifepristone MOA

A

Inhibits progesterone binding to receptor

36
Q

Mifepristone Indications

A

Abortion - up to day 49

37
Q

What is the idea of the combination of progestin with estrogen for HRT?

A

It is thought that progestin can protect the endometrium from the bad effects of estrogen

38
Q

Is the effectiveness of the combination OCPs greater than progestin alone?

A

Still inconclusive

Pharmacology (74 decks)

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