Estogen, Progestins And Combinations Flashcards
What are the major female hormones?
Estrogen (primary for developing and regulating the female reproductive system and secondary sex characteristics)
3 Major endogenous estrogens
- Estrone
- Estradiol (most potent)
- Estriol
Progestogen (primary for maintaining pregnancy (growth and maintenance of endometrium of the uterus))
1 major endogenous progestogen in females
1. Progesterone
What is menopause?
A condition in females when estrogen production reduces later in life
What are progestins?
Synthetic progestogen / progesterone (drugs) used in medicine
Where on the steroid hormone do side chains bind in order to cause different type of hormones?
The 17th carbon at the D ring (5 member ring_)
By changing the side chain there you will get different types of hormones created
is the steroid neucleus necessary for estrogenic and progestahenic activity?
It is NOT necessary for estrogenic activity!
It IS necessary for progestagenic activity
What can be done to estradiol in order to increase oral bioavailability?
Oral estradiol is usually rapidly inactivated by the liver
Adding an ethanol group (ester) at C17 or methylation at the C3 group will improve oral bioavailability by decreasing liver metabolism
How does estrogen and progesterone regulation in normal reproductive age females work?
- Hypothalamus releases GnRH
- GnRH binds to anterior pituitary and releases LH and FSH into the blood
- LH and FSH bind to ovary which produced estrogen and progesterone
- Progesterone effects the uterus
Regulation
- Negative feedback of estrogen and progesterone binds to AP and Hypothalamus to shut it down. THIS HAPPENS THROUGH MOST OF THE CYCLE!!
- Positive feedback of estrogen and progesterone to AP and hypothalamus to increase the release of hormones. THIS HAPPENS DURING DAYS 12-14 (once a month during ovulation)
What is the function of an acetylated chromatin?
It will turn gene transcription ON
What is the function of a deacetylated chromatin?
It will turn gene transcription OFF
What happens when a steroid diffuses thro a cell membrane>
- Binds to receptors that are monomers which are bound to heat shock proteins.
- The binding of the steroid to the monomer causes it to have a conformation change and disassociates from the heat shock proteins
- The receptors will then form a DIMER and become acetylated
- This will cause the his tone (chromatin) to also be acetylated
- This will allow the dimers to bind to the DNA (hormone response elements HRE)
- Will cause co-activator proteins top turn ON gene transcription of some genes
- Co-repression proteins - turn OFF gene transcription of some genes
Why are estrogen receptors so complicated?
One estrogen molecule can bind and have 6 different effects depending on where it binds
**the same ligand can generate different effects in different tissues
What is the physiologic function of estradiol and progesterone on the uterine lining (endometrium)?
Estradiol = Build up
Progesterone = maintain, when progesterone levels drop it causes shedding/promote loss (menaces)
What are the effects of estradiol and progesterone on bone growth during puberty?
Estradiol = promote; closure of epiphysis (ending bone growth)
Progesterone = no effect
What are the effects of estradiol and progesterone on bone density?
Estradiol =
Increase (early in life)
Maintain (later in life)
Progestogen = no effect
What are the physiologic functions of estradiol and progesterone on cholesterol?
Estradiol = inc HDL and dec LDL
Progesterone = variable
What are the physiologic functions of estradiol and progesterone on cancer?
Estradiol = inc risk of endometrial, breast CA
Progesterone = dec risks of endometrial, breast CA
What is important to know about estrone in terms of major production and function ?
A form of endogenous estrogen
Maintains healthy thin uterine lining during menopause
Produced in adipose tissue
E1
What is important about estradiol in terms of production and function
Most potent and common form
Produced in ovary - follicles
Maintains healthy uterine lining for possible pregnancy during reproductive years
E2
What is important to note about estriol in terms of major production sites and functions?
Most potent when pregnant
Made in placenta
Maintains healthy thick uterine lining providing blood to the placenta during pregnancy
E3
What is an overview of the menstrual cycle in terms of phases and how long they last?
Typically 28 days
Follicular phase
Low progesterone, menaces (when bleeding first occurs about a week long) happens around days 1-13
Ovulation phase
Days 13-15
High levels of LH and FSH
Luteal phase
Days 16-28 (build up phase) Large amount of progesterone and estrogen
For the menstrual cycle what are the interactions between LH, FSH and the follicle
- LH will bind to LHR in the THECA CELL which will cause the conversion of cholesterol to androstenedione
- Androstenedione then leaves the theca cell and goes into the granulosa cell. FSH will bind to FSHR which will activate aromatase with will cause androstenedione into estrone which can then become estradiol
***Granulosa cell is for FSH and produced estrogen
***Theca cell is for LH and coverts cholesterol to androstenedione
MUST HAVE enough LH and FSH for this to work
What hormone is most predominantly active in the follicular phase, ovulation and luteal phase?
Follicular phase = FSH and LH as well as estradiol levels are high
Ovulation = LH is highest then FSH follows
Lethal Phase = progesterone, also a lot fo estrogen
When does a women’s body temp rise during the menstrual cycle?
Luteal phase is when body temp is high
How many peaks of estrogen are there in the menstrual cycle as well as progesterone peaks?
Estrogen peaks twice
Progesterone only once
