Kruse DSA: Hypothalamic and Pituitary Hormones Flashcards

1
Q

GH

A

somatropin

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2
Q

IGF-1

A

Mecasermin

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3
Q

Somatostanin analogs

A
  • Octreotide

- Lanreotide

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4
Q

GH antagonists

A

Pegvisomant

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5
Q

Dopamnine agonists

A
  • bromocriptine

- cabergoline

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6
Q

Vasopressin receptor agonists

A

Vasopressin

Desmopressin

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7
Q

Vasopressin receptor antagonists

A
  • cconivaptan

- Tolvaptan

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8
Q

What kind of hormones are from the ant pit?

A

-peptide hormones

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9
Q

What provides the blood flwo to the ant pit

A

-the portal venous system that drains the hypothalamus

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10
Q

What negatively regulates the ant pit?

A
  • somatostatin
  • dopamine
  • both from hypothalamus
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11
Q

the posterior pituitary is an extension of neurons from the hypothalamus…. from what 2 nuclei do they originate in?

A
  • Supraoptic: Vasopressin

- paraventricular: Oxytocin

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12
Q

What do GH and PRL activate?

A
  • JAK/STAT kinase linked receptors

- they are single-chain protein hormones

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13
Q

What ant pit hormones activate GPCRs?

A
  • TSH
  • FSH
  • LH
  • they are dimeric ptns
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14
Q

What ant pit hormone is a single peptide that is cleaved froma larger precursor containg the peptide B-endorphin?

A

ACTH

-it also binds GPCRS

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15
Q

What feeds back and inhibits TSH and TRH?

A

-T3 and 4

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16
Q

What feeds back to inhibit FSH, LH, and GnRH?

A
  • estrogen and progesterone in women

- androgens in men

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17
Q

What inhibits ACTH and CRH

A

cortisol

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18
Q

Growth hormone

A
  • stimulated by GHRH
  • inhibited by SST
  • GH and IGF feed back to inhibiti GH release
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19
Q

Prolactin

A
  • inhibited via the D2 dopamine receptors (Gi)
  • so, disruption of pitutary stalk and hypothalamohypophysial portal vessels will increase PRL levels while the other hormones will decrease***
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20
Q

What is weird about GnRH?

A
  • When released in pulses, stimulates LH and FSH release

- when administered continuously, it inhibits LH and FSH release

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21
Q

What does ACTH target (organ)

A

Adrenal gland

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22
Q

What is GH metabolized by?

A
  • liver

- CYP450

23
Q

What receptor does GH get?

A

Jak/STAT

-IFG-1 production

24
Q

What do we give ppl who have a GH deficiency?

25
GH toxicity and contraindications
- well tolerated in children - adults: peripheral edema, myalgias, arthralgia, carpal tunnel syndrome - contraindicated in patients with a known malignancy
26
Mecasermin
- when children are unresponsive to exogenous GH, use this - it's a complex of recombinant human IGF-1 and IGFBP-3 (that incrases the half-life of rhIGF-1) - subcue
27
What is the most common adverse effect of Mecasermin?
- hypoglycemia | - so eat 20 minutes before and you'll be good to go
28
What are GH antagonists use for?
- ant pit adenomas that secret GH | - remember, acromegaly in adults, gigantism in children
29
Somatostatin analogs
- inhibits GH, glucagon, insulin ,and gastrin release - exogenous SST has a really short half life - found in hypothalamus, pancrease, and GI tract
30
What are the longer acting SST analogs?
- octreotide | - Lanreotide
31
Which drug is approved for the treatment of acrogmegaly?
-Lanreotide
32
Adverse effects of SST analogs
- GI: diarrhea, nausea, ab pain - Gallbladder sludge and gallstones.. because decreased gallbladder contraction and bile secretion - Cardiac effects (sinus bradycardia, conduction disturbances), Vitamin B12 deficiency
33
What is Pegcisomant?
- GH receptor antagonist - a PEG derivative of a mutant GH that binds to GH receptor and allows receptor to dimerize, but does not activate the JAK-STAT signaling cascade or stimulate IGF-1 secretion - used to treat acromegaly as well
34
Prolactin
- lactation - no preparations are available for use in PRL-deficient patients - if they have hyperprolactinemia, just give them a dopamine agonist
35
How does hyperprolactinemia present in women and men?
- Women: amenorrhea and galactorrhea | - Men: decreased libido and headaches)
36
How is inhibition of PRL secretion achieved?
by use of dopamine agonists | -dopamine= Prolactin inhibiting factor (PIF)
37
What are the 2 dopamine agonists?
- Bromocriptine | - Cabergoline
38
What else can dopamine agonists be use for?
-to shrink a prolactin-secreting tumor
39
Toxicity and contraindications of dopamine agonists
- nausea, headache, light-headedness, orthostatic hypotension, fatigue are most common - psych... takes months to resolve - pts with macroadenomas and preggo continue therapy - pts w. microadenomas and preggo discontinue therapy b/c microadenoma growth during pregnancy is rare - not recommended to suppress postpartum lactation due to increased indcidence of stroke or coronary thrombosis
40
Oxytocin
- stimulates uterine contraction and elicits milk ejection in lactating women - administered IV for initiation and augmentation of labor and IM for control of postpartum bleeding - this is a post pit thing remember
41
Vasopressin (ADH)
-releases in response to rising plasma osmolality or falling bp -
42
Desmopressing
long acting synthetic analog of casopressin with minimal Va receptor activity -mainly a good antidiuretic
43
What receptors does vasopressin get?
- GPCR's V1 receptors found on vascular smooth muscle... vasoconsriction - V2 receptors found on renal tubule cells... increases water permeability in collecting tubules
44
What else will activation of the V2 receptor do?
release factor VIII and VWF
45
What do we use vaso and desmopressin for?
- diabetes insipidus (the central kind) | - remember, that's the test to see if it's central or nephrogenic.... if desmopressin makes it better
46
Which one has higher V2 receptor affinity?
desmopressin
47
What else could desmopressin be used for since it activates those V2 receptors?
-Hemophilia A (factor VIII deficiency) and VWD
48
Toxicity and contraindications for vaso/desmopressin?
- headache, nausea, ab cramps, agitation, allergic rxns rarely - overdose can result in hyponatremia and seizures - vasopressin should be used with caution in patients with coronary artery disease due to vasoconstriction
49
Vasopressin antagonists
- Conivaptan | - Tolvaptan
50
MOA of the Vaptans
- antagonists of vasopressin receptors - Tol for V2 - Coni gets both
51
What is unique about the vasopressin antagonists?
they increase renal free water excretion with little or no change in electrolyte excretion (as opposed to diuretics)
52
What would we use vasopressin antagonists for?
-tx of euvolemic and hypervolemic hyponatremia
53
In CHF, which drug increases renal free water excretion without a change in systemic vascular resistance?
Conivaptan
54
What metabolizes coni/tolvaptan?
CYP3A4