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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
Q

MOA of endogenous estrogens

A
  • bind to nuclear receptors and cause change in transcription
  • will not have immediate effect, takes time to have an effect
26
Q

metabolism of estrogens

A
  • conjugated in liver and excreted in bile
  • underogoes enterohepatic circulation
    • flora in GI tract will reverse conjugation and increase bioavailability
27
Q

estrogen function in the uterus

A
  • endometrial growth
28
Q

estrogen function in puberty

A

closes epiphyses

29
Q

estrogen function in bone

A

maintenance of bone mineral density

30
Q

estrogen function in blood clotting

A
  • increase synthesis of clotting proteins, increase platelet adhesiveness
31
Q

function of estrogen on hormone binding proteins and HDL and LDL

A
  • increases sex hormone binding globulin, corticosteroid binding globulin, thyroid binding globulin
  • increases HDL
  • decreases LDL
32
Q

synthetic estrogens used in

A

oral contraceptives

33
Q

conjugated estrogens used in

A

hormone replacement therapy

34
Q

estradiol is given via what route of administration

A

creams/patches

35
Q

uses of exogenous estrogens

A
  • oral contraceptives
  • hormone replacement therapy
  • stimulating pubertal development in hypogonadic girls
36
Q

adverse effects of exogenous estrogen

A
  • migraines
  • gallbladder dz
  • thromboembolism
  • accelerated blood clotting
37
Q

contraindications to taking exogenous estrogens

A
  • estrogen dependent neoplasma (e.g. breast CA)
  • thromboembolic disorders
38
Q

MOA of Tamoxifen

A
  • selective estrogen receptor modulator
    • in some tissues, it acts as an estrogen antagonist and in other tissues it acts as an estrogen agonist
39
Q

In what tisses does tamoxifen act as an estrogen antagonist

A
  • breast
    • used as palliative and prophylactic tx in breast CA (DOC in premenopausal women)
40
Q

in what tissues does Tamoxifen act as an estrogen agonist

A
  • Bone: limits bone loss
  • Uterus: may increase risk of uterine CA
41
Q

DOC for palliative and prophylactic tx of estrogen dependent breast CA in premenopausal women

A

Tamoxifen

42
Q

Raloxifene MOA and use

A
  • SERM: estrogen antagonist in uterus and breast and agonist in bone
  • Use: osteoporosis
43
Q

Tamoxifen has what effect on HDL? Toremifene has what effect on HDL?

A
  • Tamoxifen: decrease HDL
  • Toremifene: increase HDL
44
Q

MOA and Use of Clomiphene

A
  • SERM used for infertility
  • antagonizes negative feedback of estrogen in hypothalamus
    • stimulates LH and FSH, inducing ovulation
45
Q

List the Antiestrogens

A
  • Tamoxifen
  • Toremifene
  • Raloxifene
  • Clomiphene
  • Fulvestrant
46
Q

first line drug for infertility? what is the obvious side effect

A
  • clomiphene
  • multiple pregnancies
47
Q

which antiestrogen is a full estrogen receptor antagonist

A

Fulvestrant

48
Q

protein hormones have what route of administration

A

Injections

49
Q

List the Aromatase inhibitors: function: inhibit estrogen synthesis

A
  • Anastrozole
  • Letrozole
  • Exemastane
50
Q

which Aromatase inhibitor is irreversible

A

exemastane

51
Q

DOC for breast CA treatment in postmenopausal women

A

aromatase inhibitors

52
Q

which drug is used in advanced breast CA after tamoxifen failure in postmenopausal women

A

aromatase inhibitors

53
Q

adverse effects of aromatase inhibitors

A
  • women goes through menopause again
    • N/V, hot flashes, joint pain
54
Q

contraindication of aromatase inhibitors

A
  • premenopausal women
  • pregnancy: category X

pharm II, exam 3 (8 decks)

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