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Spring Pharm Exam 3 > Estrogens and Progestins > Flashcards

Estrogens and Progestins Flashcards

1
Q

Hormone domino for estrogen release

A

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

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2
Q

Pharm use of estrogens/progestins

A

for contraception - supression of HPO axis via negative feedback

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3
Q

Physiologic use of estrogens/progestins

A

Menopausal hormone therapy (MHT)

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4
Q

granular cells secrete

A

estradiol - allows endometrium to proliferate

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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

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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

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7
Q

Pulsatile GnRH agonist administration

A

Increases LH and FSH release from pituitary

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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

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9
Q

Continuous GnRH antagonist administration

A

reduces testosterone levels in one week without initial rise

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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

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11
Q

Exogenous FSH MOA

A

stimulates gametogenesis and follicular development in women and spermatogenesis in men

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12
Q

Exogenous LH MOA

A

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

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13
Q

Gonadotropin clinical uses

A

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

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14
Q

Side effects of exogenous gonadotropin use

A

ovarian enlargement, multiple births, spontaneous abortion, gynecomastia

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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

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16
Q

hCG uses

A

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

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17
Q

hCG Side Effects

A

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

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18
Q

Estrogen MOA

A

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

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19
Q

Estrogen antagonist MOA

A

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

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20
Q

Estrogen Physiologic Effect

A

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

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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

A

:)

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
Q

Estrogen menopausal hormonal therapy - prevention of cardiovascular disease

A

NO LONGER APPROVED FOR HD PREVENTION

26
Q

Menopausal hormonal replacement therapy Contraindications

A

undiagnosed vaginal bleeding, acute liver disease, active thrombosis, recent hx of breast or endometrial CA

27
Q

Exogenous estrogen used in primary hypogonadism for…

A

~11-13 yo; sexual development, growth, avoid psychological aspects of delayed puberty

28
Q

Adverse effects of Estrogen use

A

post-menopausal bleeding, N/V/D, breast tenderness, migraines, HTN

29
Q

Progesterone is the most important progestin: precursor to estrogens, androgens, adrenocorticoids

A

:)

30
Q

Progesterone is synthesized…

A

in the ovary (corpus luteum), testis, adrenal gland and placenta

31
Q

Progesterone physiologic effects

A

Favors fat deposition, promotes liver glycogen storage, increases insulin levels, may compete with aldosterone

32
Q

Progesterone clinical uses

A

Oral and implant contraceptives

Menopausal hormone therapy (MUST be added to estrogen in women with a uterus)

33
Q

Progesterone side effects

A

mental depression, somnolence, H/A, breast enlargement, weight gain

34
Q

Hormonal controceptives contain either estrogen plus progestin (COC) or Progestin alone

A

:)

35
Q

COC MOA (estrogen and progestin in synergistic)

A

inhibition of ovulation via supression of FSH and follicle development (estrogen) and prevention of ovulatory surge of LH (progestin)

36
Q

If nausea, breast tenderness, edema occur…

A

decrease estrogen in COC

37
Q

If early/mid-cycle spotting, decreased flow/amenorrhea occur…

A

Increase estrogen, decrease the progestin dose

38
Q

If weight gain, hair growth, depression, fatigue, adverse lipid changes…

A

Decrease Progestin

39
Q

if excessive bleeding or late cycle spotting occur..

A

increase progestin and decrease estrogen dose

40
Q

COC use Contraindicated in

A

smokers >35 years old, uncontrolled HTN, DM with end organ damage, hx of VTE, hx of breast cancer or migraines with aura

41
Q

EC: Plan B MOA

A

altered oviduct motility or endometrial changes. Preventing from implanting

42
Q

Tamoxifen (Nolvadex) Use

A

SERM - used for treatment and prevention of breast CA. Induce hot flashes

43
Q

Raloxifene (Evista) Use

A

SERM - approved for prevention of breast cancer and prevention/treatment of postmenopausal osteoporosis. Induce hot flashes

44
Q

Clomiphene (Clomid)

A

Partial estrogen receptor agonist. Stimulates ovulation

45
Q

MIfepristone

A

Antagonist of progesterone receptor, terminate early pregnancy

46
Q

Medroxyprogesterone (Provera)

A

Progesterone derivatives with little effect on gonadotropin release

47
Q

Norethindrone OCP

A

1st generation. Lower progestin activity than 2nd gen. also have higher risk of unscheduled bleeding

48
Q

Levonorgestreal/norgestrel OCP

A

2nd generation. MOre progestin activity than 1st gen, improved libido, acne, hirsutism, dyslipidemia

49
Q

Desogestrel OCP

A

3rd generation. May be helpful in those with acne. slightly higher risk of VTE

50
Q

Drospirenone (Yasmin) OCP

A

4th Generation. Antimineralocorticoid and antiandrogenic activity, increased risk of VTE

Spring Pharm Exam 3 (8 decks)

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