Estrogens and Progestins Flashcards

(50 cards)

1
Q

Hormone domino for estrogen release

A

At puberty: hypothalamus GnRH –> anterior pituitary FSH/LH –> estrogen from ovaries

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Pharm use of estrogens/progestins

A

for contraception - supression of HPO axis via negative feedback

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Physiologic use of estrogens/progestins

A

Menopausal hormone therapy (MHT)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

granular cells secrete

A

estradiol - allows endometrium to proliferate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

leuteal cells secrete

A

progesterone - early, with estrogen, suppress LH/FSH. later at higher levels, has anti-estrogen effects to halt proliferation of endometrium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

clinical use of synthetic GnRH

A

Test for delayed puberty
Replacement (pulsatile) therapy: male and female infertility or abnormal function of hypothalamus
Continuous administration: prostate cancer, endometriosis, idiopathic precocious puberty

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Pulsatile GnRH agonist administration

A

Increases LH and FSH release from pituitary

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Continuous GnRH agonist administration

A

blocks release of gonadotropins after 3-4 weeks (downregulation of receptors) after an initial rise of gonadotropin release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Continuous GnRH antagonist administration

A

reduces testosterone levels in one week without initial rise

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

SIde effects of GnRH

A

vasodilation, headache, multiple pregnancies, hypoestrogenic SSX. If using continuously, can have “flare symptoms” secondary to surge in testosterone. NO flare symptoms with antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Exogenous FSH MOA

A

stimulates gametogenesis and follicular development in women and spermatogenesis in men

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Exogenous LH MOA

A

stimulates testosterone production in testicular Leydig cells and (w/FSH) stimulates follicular developement in ovary

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Gonadotropin clinical uses

A

hypogonadism with infertility. FSH used with LH sequentially in women and together in males

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Side effects of exogenous gonadotropin use

A

ovarian enlargement, multiple births, spontaneous abortion, gynecomastia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Human Chorionic Gonadotropin (from urine of preggos) MOA

A

Stimulates corpus luteum to produce and maintain placenta.

Stmulates Leydig cells to produce testosterone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

hCG uses

A

action similar to LH, some FSH action. For infertility in M and F

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

hCG Side Effects

A

H/A, depression, edema, gynecomastia, Ab production

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Estrogen MOA

A

diffuse through PM, enter nucleus and bind estrogen receptor (ERa, ERb) to ultimately initiate gene transcription

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Estrogen antagonist MOA

A

Will enter cells and bind ER, but reduce transcription of genes.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Estrogen Physiologic Effect

A

Maintain CT structure, alter liver metabolism, enhance blood coagulability, alter plasma lipid composition (cardioprotective)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Estrogen menopausal hormonal therapy - symptomatic TX

A

Treats the vasomotor symptoms and vulvovaginal/urogenital complaints. Use for a short period of time at lowest possible dose

22
Q

Non-hormonal therapy for hot flashes is an alternative for women with E+ breast cancer or history of blood clots

23
Q

Estrogen menopausal hormonal therapy - Prevention of osteoporosis

A

ONLY for patients at significant risk of osteoporosis. Worry for breast cancer risk, MI, blood clots.
Selective estrogen receptor modulators (SERMs) have less risks

24
Q

Raloxifene (Evista) SERM

A

Estrogen like activity on bone (increase mineral density) and liver (decrease LDL and total cholesterol)
Lack agonist activity (growth) in breast and uterine tissue.
Retain risk of clots d/t increase in hepatic clotting factor synthesis

25
Estrogen menopausal hormonal therapy - prevention of cardiovascular disease
NO LONGER APPROVED FOR HD PREVENTION
26
Menopausal hormonal replacement therapy Contraindications
undiagnosed vaginal bleeding, acute liver disease, active thrombosis, recent hx of breast or endometrial CA
27
Exogenous estrogen used in primary hypogonadism for...
~11-13 yo; sexual development, growth, avoid psychological aspects of delayed puberty
28
Adverse effects of Estrogen use
post-menopausal bleeding, N/V/D, breast tenderness, migraines, HTN
29
Progesterone is the most important progestin: precursor to estrogens, androgens, adrenocorticoids
:)
30
Progesterone is synthesized...
in the ovary (corpus luteum), testis, adrenal gland and placenta
31
Progesterone physiologic effects
Favors fat deposition, promotes liver glycogen storage, increases insulin levels, may compete with aldosterone
32
Progesterone clinical uses
Oral and implant contraceptives | Menopausal hormone therapy (MUST be added to estrogen in women with a uterus)
33
Progesterone side effects
mental depression, somnolence, H/A, breast enlargement, weight gain
34
Hormonal controceptives contain either estrogen plus progestin (COC) or Progestin alone
:)
35
COC MOA (estrogen and progestin in synergistic)
inhibition of ovulation via supression of FSH and follicle development (estrogen) and prevention of ovulatory surge of LH (progestin)
36
If nausea, breast tenderness, edema occur...
decrease estrogen in COC
37
If early/mid-cycle spotting, decreased flow/amenorrhea occur...
Increase estrogen, decrease the progestin dose
38
If weight gain, hair growth, depression, fatigue, adverse lipid changes...
Decrease Progestin
39
if excessive bleeding or late cycle spotting occur..
increase progestin and decrease estrogen dose
40
COC use Contraindicated in
smokers >35 years old, uncontrolled HTN, DM with end organ damage, hx of VTE, hx of breast cancer or migraines with aura
41
EC: Plan B MOA
altered oviduct motility or endometrial changes. Preventing from implanting
42
Tamoxifen (Nolvadex) Use
SERM - used for treatment and prevention of breast CA. Induce hot flashes
43
Raloxifene (Evista) Use
SERM - approved for prevention of breast cancer and prevention/treatment of postmenopausal osteoporosis. Induce hot flashes
44
Clomiphene (Clomid)
Partial estrogen receptor agonist. Stimulates ovulation
45
MIfepristone
Antagonist of progesterone receptor, terminate early pregnancy
46
Medroxyprogesterone (Provera)
Progesterone derivatives with little effect on gonadotropin release
47
Norethindrone OCP
1st generation. Lower progestin activity than 2nd gen. also have higher risk of unscheduled bleeding
48
Levonorgestreal/norgestrel OCP
2nd generation. MOre progestin activity than 1st gen, improved libido, acne, hirsutism, dyslipidemia
49
Desogestrel OCP
3rd generation. May be helpful in those with acne. slightly higher risk of VTE
50
Drospirenone (Yasmin) OCP
4th Generation. Antimineralocorticoid and antiandrogenic activity, increased risk of VTE