Progesterone Flashcards
What are the 2 types of mechanism of action of progesterone?
- slow classic genomic mechanism
- rapid non-genomic mechanism
Explain the slow classic genomic mechanism of progesterone.
- progesterone binds to nuclear receptors that are TFs
What are the major receptors involved in the slow classic genomic mechanism of progesterone? Which one acts as an activator/repressor?
- PR-A = repressor
- PR-B = activator
What may disrupted balance between PR-A and PR-B receptors lead to?
- endometriosis
- endometrial hyperplasia
(i.e. gynecological pathologies)
Explain the rapid non-genomic mechanism of progesterone.
activation of many signal transduction pathways
What are some abnormal progesterone responses?
- fibroids
- endometriosis and adenomyosis
- abnormal uterine bleeding
- miscarriage
What are some pharmacological uses of progesterone?
- hormonal contraception
- menopausal hormonal therapy
- dysmenorrhea
- endometriosis
What are some pharmacological uses of SPRMs?
- uterine fibroids
- tumors
- medical abortion
- emergency contraception
What is the mechanism of action of selective progesterone receptor modulators (SPRMs)?
- agonist/antagonist/mixed effects on progesterone target tissues
- interaction with CoA (agonist/transactivation) or CoR (antagonist/transrepression)
What are the 2 SPRMs currently licensed for gynecological use?
- mifepristone
- ulipristal acetate (UPA)
List the following for mifepristone:
- class of drug
- MOA
- uses
- class: SPRM
- MOA: progesterone antagonist –> relax cervix
- uses: emergency contraception, medical abortion
How does mifepristone act as emergency contraception?
inhibit LH surge and ovulation in late follicular phase
List the following for ulipristal acetate (UPA):
- class of drug
- uses
- class: SPRM
- uses: uterine fibroids, emergency contraception
which hormone do all hormonal contraceptives contains?
progestin
What is the effect of progestins in hormonal contraception?
progestin PROVIDE contraceptive effect by:
- decrease GnRH and LH + prevent ovulation
- direct negative effects on cervical mucus permeability
- reduce endometrial receptivity and sperm survival
What is the effect of estrogens in hormonal contraception?
estrogens ENHANCE contraceptive effect by:
- reducing GnRH
- preventing the development of a dominant follicle
What is the advantage of taking combined hormonal contraception instead of progestin-only contraception?
consistent, regular bleeding pattern
What are some non-contraceptive health effects of hormonal contraception?
- reduce ovarian tumors and cysts
- diminish PMS symptoms
- estrogen improves androgen-sensitive conditions (acne and hirsutism)
- progestin reduces menstrual blood loss and menstrual pain
What are some emergency hormonal contraceptives?
- emergency contraception pills (ECPs)
- Yuzpe method (estrogen + progestin)
- SPRM (UPA)
How do emergency contraception pills work? What are the components of ECPs?
- progestin : levonorgestrel
- prevent/delay ovulation
- impair luteal function
How does the Yuzpe method work?
- inhibit implantation of fertilized egg (by changing endometrium)
- delay/suppress ovulation
- impair luteal function
How does UPA work as an emergency hormonal contraceptive?
inhibit/delay ovulation
What happens to estrogen during menopause? What are some symptoms? What can the symptoms be treated with?
- menopause: decrease estrogen levels
- symptoms: irregular/absent period, hot flashes, night sweats, sleep/mood disorders
- treatment: estrogen+ progesterone (with uterus); only estrogen (without uterus)
Does menopause decrease or increase the rate of chronic conditions?
increase
