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pharm II, exam 3 > sex hormones > Flashcards

sex hormones Flashcards

1
Q

List the long acting agonist GnRH drugs

A
  • Leuprolide
  • Goserelin
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2
Q

continuous administration of long acting GnRH agonists, Leuprolide and Goserelin suppresses release of

A

LH and FSH

  • after initial surge
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3
Q

testosterone and progesterone has what type of feedback

A

negative feedback on hypothalamus release of GnRH and pituitary release of LH and FSH

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4
Q

GnRH is released in what manner

A

pulsatile

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5
Q

Tonic GnRH administration leads to what

A

suppressed gonadotropin release

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6
Q

use of long acting GnRH agonists

A
  • IVF
  • sex-steroid-dependent CA
  • endometriosis
  • precocious puberty
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7
Q

List the GnRH antagonist

A
  • cetrorelix
  • ganirelix
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8
Q

MOA of GnRH antagonist

A

suppress LH and FSH

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9
Q

what is the difference between long acting GnRH agonists and antagonists

A
  1. only 4-5 days of antagonist treatment vs 3 weeks of agonist tx to suppress gonadotropins
  2. no initial surge of gonadotropins in antagonist tx
  3. agonist only (metastatic prostate CA- problems during start of tx: use antiandrogen)
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10
Q

when treating metastatic prostate CA with GnRH long acting agonist, what should be given to prevent bone pain

A

antiandrogen

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11
Q

mutual side effects of long acting GnRH agonist or antagonist

A
  • menopausal symptoms
  • testicular atrophy
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12
Q

what gonadotropin drives folliculogenesis?

A
  • FSH
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13
Q

as follicles grow, what hormone increases? What is its function?

A
  • estrogen
  • endometrial development and thickening
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14
Q

high, sustained levels of estrogen after the follicular phase cause what type of feedback? effect?

A
  • positive feedback
  • LH surge ->
    • Ovulation
    • Luteinization : packed in cholesterol
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15
Q

During the luteal/secretory phase, what hormone produced by the corpus luteum maintaines the endometrium

A

progesterone and estrogen

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16
Q

primary function of FSH in women and men

A
  • women: develops ovarian follicle and supports esterogen synthesis
  • men: stimulates spermatogenesis (also need testosterone)
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17
Q

What are the FSH drugs

A
  1. human menopausal gonadotropins (aka menotropins): FSH and LH but used for FSH
  2. Urofollitropin: purified FSH
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18
Q

List the primary function of Luteinizing hormone

A
  • stimulates ovulation
  • stimulates luteinization of follicles
  • steroid production
    • women: progesterone synthesis
    • men: testosterone synthesis
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19
Q

What is the LH drug

A
  • hCG: used instead of LH, has same actions
    • get from urine of pregnant women fyi
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20
Q

what are the uses for gonadotropin drugs in men

A

reversing infertility

  • men: induce spermatogenesis
    1. LH increases testosterone (give LH for a year)
    2. FSH then induces permatogenesis (give FSH for a few months)
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21
Q

what are the uses for gonadotropins in females

A
  • women: IVF: reduce infertility
  1. give FSH (9-12 days) stimulates ovaries and estrogen production,
  2. single dose of LH given to induce ovulation
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22
Q

adverse effects of gonadotropins

A
  • ovarian hyperstimulation syndrome
    • vascular permeability, shock
  • multiple births: 20%
  • gynecomastia
23
Q

contraindications of gonadotropins

A
  • sex steroid-dependent cancers
24
Q

what are the major endogenous estrogens

A
  • estradiol
  • estriol
  • estrone
25
MOA of endogenous estrogens
* bind to **nuclear receptors** and cause change in transcription * will not have immediate effect, takes time to have an effect
26
metabolism of estrogens
* conjugated in liver and excreted in bile * underogoes **enterohepatic circulation** * flora in GI tract will reverse conjugation and increase bioavailability
27
estrogen function in the uterus
* endometrial growth
28
estrogen function in puberty
closes epiphyses
29
estrogen function in bone
maintenance of bone mineral density
30
estrogen function in blood clotting
* increase synthesis of clotting proteins, increase platelet adhesiveness
31
function of estrogen on hormone binding proteins and HDL and LDL
* increases sex hormone binding globulin, corticosteroid binding globulin, thyroid binding globulin * increases HDL * decreases LDL
32
synthetic estrogens used in
oral contraceptives
33
conjugated estrogens used in
hormone replacement therapy
34
estradiol is given via what route of administration
creams/patches
35
uses of exogenous estrogens
* **oral contraceptives** * **hormone replacement therapy** * **stimulating pubertal development** in hypogonadic girls
36
adverse effects of exogenous estrogen
* migraines * gallbladder dz * thromboembolism * **accelerated blood clotting**
37
contraindications to taking exogenous estrogens
* estrogen dependent neoplasma (e.g. breast CA) * thromboembolic disorders
38
MOA of **Tamoxifen**
* selective estrogen receptor modulator * in some tissues, it acts as an estrogen antagonist and in other tissues it acts as an estrogen agonist
39
In what tisses does tamoxifen act as an estrogen antagonist
* breast * used as palliative and prophylactic tx in breast CA (DOC in premenopausal women)
40
in what tissues does Tamoxifen act as an estrogen agonist
* **Bone:** limits bone loss * **Uterus:** may increase risk of uterine CA
41
DOC for palliative and prophylactic tx of estrogen dependent breast CA in **pre**menopausal women
Tamoxifen
42
Raloxifene MOA and use
* SERM: estrogen antagonist in uterus and breast and agonist in bone * Use: **osteoporosis**
43
Tamoxifen has what effect on HDL? Toremifene has what effect on HDL?
* Tamoxifen: decrease HDL * Toremifene: increase HDL
44
MOA and Use of Clomiphene
* SERM used for infertility * antagonizes negative feedback of estrogen in hypothalamus * **stimulates LH and FSH**, inducing ovulation
45
List the Antiestrogens
* Tamoxifen * Toremifene * Raloxifene * Clomiphene * Fulvestrant
46
first line drug for infertility? what is the obvious side effect
* clomiphene * multiple pregnancies
47
which antiestrogen is a full estrogen receptor antagonist
Fulvestrant
48
protein hormones have what route of administration
Injections
49
**List the Aromatase inhibitors:** function: inhibit estrogen synthesis
* Anastrozole * Letrozole * Exemastane
50
which Aromatase inhibitor is irreversible
exemastane
51
DOC for breast CA treatment in postmenopausal women
aromatase inhibitors
52
which drug is used in advanced breast CA after tamoxifen failure in postmenopausal women
aromatase inhibitors
53
adverse effects of aromatase inhibitors
* women goes through menopause again * N/V, hot flashes, joint pain
54
contraindication of aromatase inhibitors
* premenopausal women * pregnancy: category X

pharm II, exam 3 (8 decks)

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