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PHRM 825 Steroids Exam 2 > Estrogens > Flashcards

Estrogens Flashcards

1
Q

What is estrogen and what does it do?

A
  1. development and maintenance of reproductive tissues
  2. regulate CNS
  3. effects in peripheral tissues
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2
Q

what is progesterone and what does it do?

A
  1. development and maintenance of reproductive tissues
  2. maintenance of pregnancy
  3. effects in other tissues
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3
Q

what is the change in estrogen/ progesterone levels during the early follicular phase?

A

estrogen suppresses the production of FSH

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4
Q

what is the change in estrogen/ progesterone levels during the late follicular phase?

A

estrogen stimulates the surge of LH & FSH –> ovulation and formation of corpus luteum

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5
Q

what is the change in estrogen/ progesterone levels during the luteal phase?

A

estrogen and progesterone suppress production of LH and FSH

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6
Q

describe the regulation of estrogen synthesis?

A
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7
Q

list the physiological effects of estrogen?

A
  1. female maturation
  2. endometrial effects
  3. metabolic and cardiovascular effects
  4. blood coagulation
  5. CNS
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8
Q

what effects go with female maturation?

A
  1. development in vagina
  2. stromal development and duct growth in breast
  3. accelerated growth phase
  4. growth of pubic and armpit hair
  5. alteration in body fat
  6. pigment in places
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9
Q

what effects go with endometrial effects?

A
  1. development of lining in menstrual cycle
  2. prolonged exposure leads to hyperplasia of endometrium and abnormal bleeding
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10
Q

what is the consequence of enterohepatic recirculation in estrogen metabolism?

A

if orally administered there can be hepatic and peripheral adverse effects due to reabsorption back into the liver thats why we use other routes to avoid this

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11
Q

what are the clinical uses for estrogens?

A

hormone replacement therapy, osteoporosis, and hormonal contraception, replacement therapy for hypogonadism

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12
Q

why do we use estrogen for hormone replacement therapy?

A
  1. relief in CNS (hot flashes, sweating, flushing)
  2. relief in atrophy ( vag dryness, inc. risk of infections)
  3. physiological effects ( mood swings, insomnia, depression, nervous)
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13
Q

why do we use estrogens for osteoporosis?

A
  1. post menopausal women only
  2. dec. reabsorption rate of bone
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14
Q

why do we use estrogen in people with hypogonadism?

A
  1. failure of development of ovaries
  2. chromosomal disorders
  3. castration
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15
Q

what are the adverse effects of estrogens?

A

uterine bleeding, endometrial carcinoma, breast cancer, nausea, headache, weight gain, and fluid retention

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16
Q

tell me why estrogen causes uterine bleeding?

A
  1. major cause for post menopausal bleeding
  2. endometrial hyperplasia
  3. can be prevented by admin of progestin in each cycle
17
Q

tell me why estrogen causes breast cancer?

A
  1. long term use
  2. can promote growth if hormones aren’t normal –> additional progestin
18
Q

tell me why estrogen has an effect of endometrial carcinoma?

A

concomitant use of progestin reduces the risk
1. if given more than normal can result in hyperplasia

19
Q

what is the mechanism of action for SERMs?

A
  1. designer estrogen; partial agonist
  2. if the ligand binding is bound with an agonist then helix 12 will allow confirmation and coactivator binding
  3. has estrogenic and antiestrogenic effects
20
Q

what is the mechanism of action for antagonists?

A

if ligand is a SERM modulator bound then helix 12 will block coactivator and have antagonist effect

21
Q

what drugs are aromatase inhibitors?

A
22
Q

what are aromatase inhibitors used for?

A
  1. block biosynthesis of estrogens
  2. gynecomastia
  3. off label: ovulation induction
  4. used in breast cancer if resistant to tamoxifen
23
Q

what drugs are used as SERMs?

A
  1. tamoxifen
  2. toremifene
  3. ospemifene
  4. raloxifene/bazedoxifene
  5. clomiphene
24
Q

What is tamoxifen?

A
  1. pro drug and partial agonist
  2. antiestrogen actions: breast cancer
  3. estrogenic action: osteoporosis, increase blood clots, weak estrogen agonist
25
Q

what is toremifene?

A
  1. similar to tamoxifen structure
  2. serm
  3. advanced breast cancer
26
Q

what is ospemifene?

A
  1. serm
  2. estrogenic effects on vaginal epithelium
  3. treat dyspareunia in post-menopausal women
27
Q

what is raloxifene/ bazedoxifene?

A
  1. SERM/ partial agonist
  2. estrogenic actions: osteoporosis in postmenopause, dec. LDL, inc. blood clots
  3. antoestrogenic actions: dec. breast cancer, doesn’t stimulate endometrial cells, may cause hot flashes
28
Q

what is clomiphene?

A
  1. SERM/ partial agonist
  2. inc. secretion of FSH and LH by inhibiting negative estradiol feedback
  3. stiulate ovulation in women with amenorrhea, oligomenorrhea, and ovulatory dysfunction
  4. PCOS
29
Q

what is Fulvestrant?

A
  1. SERD
  2. pure estrogen antagonist
  3. breast cancer treatment
  4. more effective than SERM if tolerance to tamoxifen
30
Q

what do steroidal estrogens look like?

A
31
Q

what do non-steroidal estrogens look like?

A
32
Q

what are estrogenic esters?

A
  1. esterification dec. solubility and slow absorption
  2. slow absorption (IM) –> prolong action –> less injections
  3. examples:
    –> estradiol valerate and estradiol cypionate
33
Q

what are conjugated esters?

A
  1. collected from pregnant mares urine (premarin)
  2. mix of estrogens
    –> 50-60% (estrone sulfate)
    –> other (equilin sulfate)
34
Q

what is 17a- alkylated estrogens?

A
  1. prevents conversion to estrone–> enhance bioavailability and inc. half life
  2. 3-alkylated ether is dealkylated quickly in vivo
  3. examples:
    – mestranol, quinestrol, ethinyl estradiol
35
Q

what happens if there is no pregnancy in the menstrual cycle?

A
  1. corpus luteum degenerates
  2. production of estrogen and progesterone by corpus luteum declines –> menstruation
36
Q

what happens if you become pregnant in the menstrual cycle?

A
  1. fertilized egg secretes hCG
  2. hCG act like LH to stimulate corpus luteum to produce progesterone in 1st trimester
  3. assays can be used to test hCG for pregnancy tests
37
Q

what are the metabolic and cardiovascular effects of estrogen?

A
  1. dec. in rate of reabsorption to bone
  2. stimulate transcortin and SHBG
  3. alteration in plasma levels ( inc. HDL, dec. LDL)

PHRM 825 Steroids Exam 2 (8 decks)

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