Progesterone

Question 1

What are the 2 types of mechanism of action of progesterone?

Answer 1

• slow classic genomic mechanism
• rapid non-genomic mechanism

Question 2

Explain the slow classic genomic mechanism of progesterone.

Answer 2

• progesterone binds to nuclear receptors that are TFs

Question 3

What are the major receptors involved in the slow classic genomic mechanism of progesterone? Which one acts as an activator/repressor?

Answer 3

• PR-A = repressor
• PR-B = activator

Question 4

What may disrupted balance between PR-A and PR-B receptors lead to?

Answer 4

• endometriosis
• endometrial hyperplasia
  (i.e. gynecological pathologies)

Question 5

Explain the rapid non-genomic mechanism of progesterone.

Answer 5

activation of many signal transduction pathways

Question 6

What are some abnormal progesterone responses?

Answer 6

• fibroids
• endometriosis and adenomyosis
• abnormal uterine bleeding
• miscarriage

Question 7

What are some pharmacological uses of progesterone?

Answer 7

• hormonal contraception
• menopausal hormonal therapy
• dysmenorrhea
• endometriosis

Question 8

What are some pharmacological uses of SPRMs?

Answer 8

• uterine fibroids
• tumors
• medical abortion
• emergency contraception

Question 9

What is the mechanism of action of selective progesterone receptor modulators (SPRMs)?

Answer 9

• agonist/antagonist/mixed effects on progesterone target tissues
• interaction with CoA (agonist/transactivation) or CoR (antagonist/transrepression)

Question 10

What are the 2 SPRMs currently licensed for gynecological use?

Answer 10

• mifepristone
• ulipristal acetate (UPA)

Question 11

List the following for mifepristone:
- class of drug
- MOA
- uses

Answer 11

• class: SPRM
• MOA: progesterone antagonist –> relax cervix
• uses: emergency contraception, medical abortion

Question 12

How does mifepristone act as emergency contraception?

Answer 12

inhibit LH surge and ovulation in late follicular phase

Question 13

List the following for ulipristal acetate (UPA):
- class of drug
- uses

Answer 13

• class: SPRM
• uses: uterine fibroids, emergency contraception

Question 14

which hormone do all hormonal contraceptives contains?

Answer 14

progestin

Question 15

What is the effect of progestins in hormonal contraception?

Answer 15

progestin PROVIDE contraceptive effect by:
- decrease GnRH and LH + prevent ovulation
- direct negative effects on cervical mucus permeability
- reduce endometrial receptivity and sperm survival

Question 16

What is the effect of estrogens in hormonal contraception?

Answer 16

estrogens ENHANCE contraceptive effect by:
- reducing GnRH
- preventing the development of a dominant follicle

Question 17

What is the advantage of taking combined hormonal contraception instead of progestin-only contraception?

Answer 17

consistent, regular bleeding pattern

Question 18

What are some non-contraceptive health effects of hormonal contraception?

Answer 18

• reduce ovarian tumors and cysts
• diminish PMS symptoms
• estrogen improves androgen-sensitive conditions (acne and hirsutism)
• progestin reduces menstrual blood loss and menstrual pain

Question 19

What are some emergency hormonal contraceptives?

Answer 19

• emergency contraception pills (ECPs)
• Yuzpe method (estrogen + progestin)
• SPRM (UPA)

Question 20

How do emergency contraception pills work? What are the components of ECPs?

Answer 20

• progestin : levonorgestrel
• prevent/delay ovulation
• impair luteal function

Question 21

How does the Yuzpe method work?

Answer 21

• inhibit implantation of fertilized egg (by changing endometrium)
• delay/suppress ovulation
• impair luteal function

Question 22

How does UPA work as an emergency hormonal contraceptive?

Answer 22

inhibit/delay ovulation

Question 23

What happens to estrogen during menopause? What are some symptoms? What can the symptoms be treated with?

Answer 23

• menopause: decrease estrogen levels
• symptoms: irregular/absent period, hot flashes, night sweats, sleep/mood disorders
• treatment: estrogen+ progesterone (with uterus); only estrogen (without uterus)

Question 24

Does menopause decrease or increase the rate of chronic conditions?

Answer 24

increase