Gonadal Hormones Flashcards

1
Q

inhibin produced by the ovaries/testes inhibits ______

A

FSH

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2
Q

in females, LH acts on _____ cell and converts ____ to ____ via _____ (enzyme)

A

LH acts on the thecae called and ↑ desmolase which converts cholesterol to androgens

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3
Q

androgens are converted into estrogen in ______ cells via _____ (enzyme) and the hormone that ↑ the activity of this enzyme is _____

A

granulosa cells; aromatase; aromatase activity ↑ by FSH

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4
Q

LH in males ↑ desmolase activity in _____ cells

A

Leydig cells

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5
Q

desmolase in both males and females is stimulated by _____ (hormone) in the _____ or ____ cells

A

LH in theca (females) and Leydig (males) cells

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6
Q

FSH in males ↑ the activity of what enzyme?

A

androgen binding protein

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7
Q

what occur in the Sertoli cells in male gonands due to FSH being secreted?

A

↑ the activity of ABP so you get more testoserone-ABP which ↓ the lipophilicity of the testosterone so that it stays within the seminiferous tubules so that spermatogenesis can occur

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8
Q

testosterone binding to ABP makes the testosterone more/less lipophilic

A

less

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9
Q

meatranol is a __________

A

pro drug that is converted to ethinyl estradiol (synthetic estrogen)

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10
Q

estrogens ↑/ ↓ bone resorption

A

↓ (increases bone mass and thus is protective against osteoporosis and why it is more likely to get osteoporosis in menopause)

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11
Q

what is the effect of estrogen on lipids?

A

↑ HDL and ↓ LDL (good effects) but cannot be used to treat CVD

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12
Q

what is the risk of giving estrogen to patients?

A

↑ risk for thromboembolic events due to

  1. ↑ hepatic production of factors 2, 7, 9, 10 and fibrinogen
  2. ↓ antithrombin III activity
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13
Q

estrogen ↑/ ↓ the activity of antithrombin III

A

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14
Q

what are the effects of estrogen on the vasculature?
NO production
prostacyclin production

A

↑ NO production

↑ prostacyclin production

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15
Q

how is estrogen metabolized?

A

conjugated by cytochrome enzymes in the liver and then excreted in the bile and hydrolyzed by intestinal bacterial and then reabsorbed as an active drug

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16
Q

what are some of the more moderate/severe AE of estrogens?

A
  • ↑ risk for endometrial cancer (offset risk by giving estrogen with progestin)
  • ↑ frequency of migraines
  • choelstatis/gallbladder isease
  • thromboembolism
  • depression
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17
Q

what are the SERMs (selective estrogen receptor modulators)

A
  • tamoxifen
  • raloxifene
  • clomiphene
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18
Q

SERMs bind to ______

A

estrogen receptors and can have agonist or antagonist effects

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19
Q

________ is a SERM that can be used in the treatment of infertility associated with anovulatory cycles (try this before IVF)

A

clomiphene

20
Q

tamoxifen is a _____ (type of estrogen drug). what is its MOA and what is it used for?

A

SERM
- antagonist in breast tissue and against in non breast tissue (endometrium, liver, bone)

used in prevention AND treatment of hormone responsive breast cancer

21
Q

______ is a SERM used in the prevention of hormone responsive breast cancer

A

Raloxifene; (tamoxifen is used for prevention and treatment of hormone responsive breast cancer)

22
Q

raloxifene is used in the prevention and treatment of ________

A

osteoporosis in post menopausal women

acts as an agonist in bone (inhibits resorption)

23
Q

what is the MOA of clomiphene?

A

antagonist in the hypothalamus and thus inhibits the normal feedback inhibition

24
Q

_______ is a SERM used in the treatment and prevention of osteoporosis in post menopausal women

A

raloxifene

25
Q

_______ is a SERM with a ↑ risk for endometrial cancer

A

tamoxifen because it is an agonist at the endometrial tissue

26
Q

and example of an SERD is _______

A

fulvestrant; causes estrogen receptors to be degraded and down regulated in all tissues

27
Q

a patient is found to have hormone receptor positive metastatic breast cancer. the first line treatment of ______ was not useful. What should be given next

A

first line: tamoxifen (SERM)

now give fulvestrant (SERD)

28
Q

what are the non steroidal aromatase inhibitors?

A
  • anastrozole
  • letrozole

they are competitive, reversible inhibitors

29
Q

what is the steroidal aromatase inhibitor?

A
  • exemestrane

irreversible inhibitor

30
Q

what are the main effects of progestins (4)

A
  • prevents endometrial hyperplasia by ↓ growth and ↑ vascularization of endometrium
  • thickening of cervical mucus which inhibits moment of sperm
  • associated with ↑ in body temp
  • maintenance of pregnancy
31
Q

which is associated with ↑ risk of endometrial cancer: tamoxifen or raloxifene

A

tamoxifen

32
Q

what are some of the major AE of progestins?

A
  • uterine bleeding (even though it is given to treat uterine bleeding)
  • weight gain
  • ↓ HDL levels (especially in androgens progestins)
  • thromboembolic events (extremely rare)
33
Q

_____ is an anti progestin

A

mifepristone which is a competitive inhibitor at the progesterone receptor and can be used in combination with misoprostol as an abortifacient

34
Q

what type of drug is danazol

A

androgen that also has anti estrogen activity

35
Q

what are 3 AE of using high dose testosterone

A
  • reduction in testicular size
  • hepatic abnormalities
  • ↑ aggression
36
Q

spironolactone is a ______ antagonist

A

androgen receptor antagonist

37
Q

what kind of drug is finasteride

A

5 α reductase inhibitor

38
Q

spironolactone and _______ are androgen receptor antagonists

A

flutamide

39
Q

ketoconazole inhibits ______

A

steroid synthesis

40
Q

flutamide is used for the treatment of ______

A

prostate carcinoma (it is a androgen receptor antagonist)

41
Q

_______ is one of the main treatments for BPH (benign prostatic hyperplasia) and also male pattern baldness

A

finasteride (5 α reductase inhibitor)

42
Q

what are some of the clinical uses of ketoconazole?

A
  • treat non operable Cushing’s syndrome and prostate cancer

non selective inhibitor of adrenal and gonadal steroid synthesis

43
Q

______ is the form of estrogen in post menopausal

A

estrone (E1)

44
Q

______ is the form of estrogen in reproductive years

A

estradiol (E2)

45
Q

______ is the form of estrogen in pregnancy

A

estriol (E3)