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IDT Spring > HPG Axis, Gonadal Hormones And Inhibitors > Flashcards

HPG Axis, Gonadal Hormones And Inhibitors Flashcards

1
Q

What are primary endocrine organs?

A

Pineal gland
Hypothalamus
Pituitary gland
Thyroid/parathyroid glands
Thymus
Adrenal gland
Pancreas
Testes/ovaries
Placenta

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2
Q

What are secondary endocrine organs?

A

Skin
Heart
Liver
Stomach
Kidney
Small intestine

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3
Q

The control of metabolism, growth, and reproduction is mediated by a combo of neural and endocrine systems located in the ________ and ________

A

Hypothalamus, pituitary gland

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4
Q

Which endocrine organ consists of an anterior and posterior lobe?

A

Pituitary

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5
Q

Which sole anterior pituitary hormone acts directly on target tissues?

A

Prolactin (PRL)

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6
Q

GH, TSH, ACTH, LH, and FSH are secreted by? What two hormones do they stimulate?

A

Anterior pituitary
Estrogen and testosterone

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7
Q

Which two hormones are secreted by the posterior pituitary?

A

ADH and oxytocin

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8
Q

ADH:
Where is it produced?
Released?
Targets?
Effects?

A

Hypothalamus
Posterior Pituitary hormone
Kidneys, sweat glands, and circulatory system
Water balance

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9
Q

Oxytocin:
Where is it produced?
Released?
Targets?
Effects?

A

Hypothalamus
Posterior pituitary hormone
Female reproductive system
Uterine contractions during birth

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10
Q

Which hormone is released by the hypothalamus to stimulate sex hormone/gamete production? Which anterior pituitary hormone?

A

GnRH
FSH/LH

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11
Q

Which hormone is released by the hypothalamus to stimulate thyroid hormone production? Which anterior pituitary hormone?

A

TRH
TSH

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12
Q

Which hormone is released by the hypothalamus to stimulate milk production? Which anterior pituitary hormone?

A

PRH
PRL

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13
Q

Which hormone is released by the hypothalamus to stimulate IGF production? Which anterior pituitary hormone?

A

GHRH
GH

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14
Q

Which hormone is released by the hypothalamus to stimulate glucocorticoid production? Which anterior pituitary hormone?

A

CRH
ACTH

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15
Q

What is LH’s effect in females in the ovaries?

A

Increased estrogen and progesterone production

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16
Q

What is LH’s effect in males in the testes?

A

Testosterone production

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17
Q

Gonadotropin releasing hormone (GnRH) causes secretion of which two gonadotropins?

A

FSH and LH

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18
Q

Pulsation GnRH release occurs and is responsible for stimulating LH and FSH production during the ____ and ________ period.
Year 2-puberty: GnRH ____________ and pituitary has ____ sensitivity.
Just before puberty, there is ___________ frequency and amplitude of GnRH, and in early puberty, pituitary sensitivity to GnRH _______.

A

Fetal, neonatal
Falls off, low
Increased, increases

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19
Q

what is gonadorelin?
how is it used?

A

a more potent, synthetic acetate salt of GnRH
when used as a single dose helps initiate puberty. as a pulsatile dose treats GnRH-deficient infertility by stimulating FSH and LH secretion. as a sustained long-acting dose inhibits gonadal function in children with early puberty and women who require ovarian suppression

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20
Q

what are the names of the drugs that are GnRH agonists?
what is the MoA?

A

Leuprolide
Goserelin
Histrelin
Nafarelin
Triptorelin
inhibits gonadotropin release to suppress:
ovulation
gynecologic disorders
advanced prostate cancer
early pubertal transgender adolescents

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21
Q

what are adverse effects of GnRH agonists?

A

symptoms of menopause
long-term treatment bone loss and osteoporosis
gynecomastia
reduced libido

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22
Q

In men with prostate cancer and children with precocious puberty, the first few weeks of GnRH therapy can temporarily ___________ the condition (cause a _____)

A

exacerbate, flare

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23
Q

What are the GnRH antags?

A

Ganirelix
Cetrorelix
Degarelix

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24
Q

which GnRH antags suppress endogenous gonadotropin production during ovulation induction?

A

Ganirelix and Cetrorelix

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25
Q

which GnRH antag treats advanced prostate cancer?

A

Degarelix

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26
Q

GnRH antags __________ a tumor flare when used for prostate cancer and may be less likely to cause ______________ syndrome when used for ovulation induction

A

do not cause, ovarian hyperstimulation

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27
Q

what is FSH’s function in male/female?

A

male: regulates spermatogenesis
female: follicle development

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28
Q

what is LH’s function in male/female?

A

Male: stimulates testicular androgen production
female: works with FSH to regulate ovarian steroidogenesis

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29
Q

all ovulation induction protocols that use gonadotropins include:
Gonadotropin production is _______ by administration of a GnRH agonist or antag
Follicle development is driven by daily injections of a preparation with ____ activity
The final stage of oocyte maturation is induced with an injection of ___ or __________

A

inhibited
FSH
LH, human chorionic gonadotropin (hCG)

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30
Q

what is menotropin and how is it produced?

A

mixture of FSH and LH purified from the urine of postmenopausal women

31
Q

what is Urofollitropin and how is it produced?

A

a FSH analog produced from purified urine of postmenopausal women

32
Q

what are the 2 recombinant forms of human FSH?

A

follitropin alpha and follitropin beta

33
Q

what is the role of hCG and how is it produced?

A

supports the fetus in early pregnancy by activating LH receptors
purified from human urine

34
Q

what is Lutropin?

A

a recombinant form of human LH

35
Q

what is the main antagonist of prolactin?

A

dopamine

36
Q

what are the D2 R agonists used as prolactin antagonists? why do we use them?

A

**Bromoctriptine, cabergoline, and pergolide
prolactin-secreting adenomas cause hyperprolactinemia which leads to infertility and galactorrhea (milk production). D2 agonists help reduce prolactin concentrations. they can also treat acromegaly (excessive growth hormone)

37
Q

what are the two posterior pituitary gland (neurohypophysis) hormones?

A

ADH and oxytocin

38
Q

how do we use oxytocin?
how do we use atosiban?

A

it stimulates uterine contraction and can induce labor
blocks the oxytocin receptor to suppress preterm labor (not FDA approved)

39
Q

what is the ADH hormone and it’s MoA?

A

Vasopressin binds to V2 Rs to increase insertion of water channels in the kidney to have a antidiuretic effect

40
Q

what is Desmopressin and it’s use?
what are conivaptan and tolvaptan and their use?

A

V2 R agonist: used for pituitary diabetes insipidus (inability to regulate the body’s level of water)
V2 R antags: offset fluid retention due to excess vasopressin

41
Q

Summary:
what are the gonadal hormones?
what are SERMS?
what do antiandrogenic drugs do?

A

estrogen, progestin, and testosterone
selective estrogen receptor modulators: modify function of estrogen
treat prostate cancer and benign prostatic hyperplasia in men and androgen excess in women

42
Q

what is tamoxifen?
what is it used for?
how is it used prophylactically?
SEs?

A

a SERM: estrogen R antag
treating breast cancer - blocking estrogen R prevents cell proliferation by inhibiting the estrogen response element
can reduce the chance of breast cancer for very high risk women
hot flushes and increased risk of venous thrombosis

43
Q

what is fulvestrant?
why/when do we use it?

A

a full estrogen antag
treat breast cancer if pt is resistant to tamoxifen

44
Q

what drug class is anastrozole?
use?

A

competitive aromatase inhibitor
treat breast cancer

45
Q

how can GnRH agonists effect estrogen?
androgen?

A

inhibit estrogen production
inhibit androgen production

46
Q

what is flutamide? what is it used for?

A

non-steroidal competitive antagonist of androgen receptors which treats prostate carcinoma

47
Q

what is finasteride’s effect on androgen?
uses?

A

inhibit androgen R to inhibit dihydrotestosterone production
treats benign prostatic hyperplasia and prevents hair loss in men

48
Q

what is ketoconazole’s effect on androgen/gonads? what can it treat?

A

inhibits adrenal and gonadal synthesis to treat steroid-responsive prostate cancer

49
Q

when properly regulated by FSH and LH, each menstrual cycle consists of:

A

follicular phase: follicle in ovary matures and secretes estrogen
ovulation: release ovum and transforms to secrete progesterone
luteal phase: if ovum is not fertilized and implanted, egg degenerates
menstruation: the proliferated uterine endometrium is shed

50
Q

during most of the menstrual cycle, estrogen and progesterone have a negative feedback mechanism to inhibit the hypothalamus from producing _______ and the anterior pituitary from producing ________ which eventually prevents further production of ____________ by the ovary.
on the contrary, around day 12-14, estrogen and progesterone have a positive feedback mechanism to stimulate the production of these pathways

A

GnRH, FSH and LH, estrogen and progesterone

51
Q

Estrogen is produced by the _____, whereas progesterone is produced by the _________. Estrogen’s production is regulated by ___, whereas progesterone’s production is regulated by ___.
Estrogen cause enlargement of the _____ and _____ during pregnancy, whereas progesterone causes reduction in the contractility of the ______ and stimulates the growth of __________

A

follicle, corpus luteum
FSH, LH
uterus, breasts, uterus, mammary glands

52
Q

which CYP enzyme is essential for estrogen production?

A

CYP19 (aromatase)

53
Q

Estrogen is essential for female ___________ such as growth of the __________ during childhood and the __________ associated with puberty.
It modifies serum ______ levels and reduces bone ________.
It enhances the _________ of blood and increase plasma __________ levels while reducing _________ cholesterol and increasing _______ cholesterol

A

reproductive development, genital structures, growth spurt
protein, resorption
coagulability, triglyceride, LDL, HDL

54
Q

what is Premarin and how is it used?

A

mixture of estrogens that is used orally for hormone replacement therapy (HRT)

55
Q

which synthetic estrogens have high bioavailability?

A

ethinyl estradiol and mestranol

56
Q

why do we give women estrogen as HRT?

A

if they have estrogen deficiency caused by ovarian failure, menopause, or removed ovaries. it also prevents bone loss and osteoporosis

57
Q

T/F medroxyprogesterone has improved oral bioavailability compared to progesterone, but does not support pregnancy

A

True

58
Q

why is progestin always given with estrogen in HRT?

A

to prevent estrogen-induced endometrial cancer (breast cancer)

59
Q

what drug class are raloxifen and bazedoxifene?
what do they prevent/treat?
SEs?

A

SERM
osteoporosis in postmenopausal women and reduce the chance of breast cancer in very high risk women
hot flushes and venous thrombosis (same as tamoxifen)

60
Q

what is clomiphene used for? MoA?

A

induce ovulation in anovulatory women who wish to become pregnant by blocking estrogen Rs in pituitary to reduce negative feedback to increase FSH and LH output

61
Q

what is exemestane?
use?

A

an irreversible aromatase inhibitor to treat breast cancer

62
Q

what is danazol?
what does it treat?

A

inhibitor of several P450s and a weak partial agonist of progestin, androgen, and glucocorticoid Rs
treats endometriosis (uterine cells grow outside uterus) and fibrocystic disease of the breast (painful, lumpy breasts)

63
Q

what drug class is mifepristone?
use?
what is it combined with?

A

progesterone and glucocorticoids antag
abortifacient up to 49 days from last menstrual period
it is combined with misoprostol, a prostaglandin analog

64
Q

Testosterone is synthesized from ________ and ____________.
In the plasma, it is partly bound to _________, a transport protein.
It is converted in several organs to _________, which is the active hormone in those tissues

A

progesterone, dehydroepiandrosterone (DHEA)
sex hormone-binding globulin
dihydrotestosterone (DHT)

65
Q

what type of target genes does testosterone modulate?

A

AR target genes

66
Q

T/F testosterone attributes to male-pattern baldness

A

true

67
Q

testosterone is labeled as an androgen… what can androgens be used to treat?

A

RBC production in certain anemias and promote weight gain in pts with wasting syndromes (AIDS)

68
Q

T/F testosterone given orally can have long-lasting effects comparable to injectable formulations

A

false, little effect due to rapid hepatic metabolism

69
Q

how does excess androgen effect women?
what about men?

A

causes hirsutism, enlarged clitoris, deepened voice, and menstrual irregularity
causes gynecomastia, testicular shrinkage, and infertility

70
Q

high doses of anabolic steroids can cause?

A

cholestatic jaundice, elevated liver enzymes, and liver tumors

71
Q

how is spironolactone involved with androgen and what does it treat?

A

it inhibits androgen Rs to treat hirsutism (facial hair growth) in women

72
Q

suppression of gonadotropin secretion, especially ___, reduces the production of ________. This can be caused using the drug _____ which can treat _________.

A

LH, testosterone
leuprolide, prostatic carcinoma

73
Q

what two GnRH R antags are approved for advanced prostate cancer?

A

abarelix and degarelix

IDT Spring (22 decks)

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