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?

A

rhGH

25
Q

GH toxicity and contraindications

A
  • well tolerated in children
  • adults: peripheral edema, myalgias, arthralgia, carpal tunnel syndrome
  • contraindicated in patients with a known malignancy
26
Q

Mecasermin

A
  • 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
Q

What is the most common adverse effect of Mecasermin?

A
  • hypoglycemia

- so eat 20 minutes before and you’ll be good to go

28
Q

What are GH antagonists use for?

A
  • ant pit adenomas that secret GH

- remember, acromegaly in adults, gigantism in children

29
Q

Somatostatin analogs

A
  • inhibits GH, glucagon, insulin ,and gastrin release
  • exogenous SST has a really short half life
  • found in hypothalamus, pancrease, and GI tract
30
Q

What are the longer acting SST analogs?

A
  • octreotide

- Lanreotide

31
Q

Which drug is approved for the treatment of acrogmegaly?

A

-Lanreotide

32
Q

Adverse effects of SST analogs

A
  • 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
Q

What is Pegcisomant?

A
  • 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
Q

Prolactin

A
  • lactation
  • no preparations are available for use in PRL-deficient patients
  • if they have hyperprolactinemia, just give them a dopamine agonist
35
Q

How does hyperprolactinemia present in women and men?

A
  • Women: amenorrhea and galactorrhea

- Men: decreased libido and headaches)

36
Q

How is inhibition of PRL secretion achieved?

A

by use of dopamine agonists

-dopamine= Prolactin inhibiting factor (PIF)

37
Q

What are the 2 dopamine agonists?

A
  • Bromocriptine

- Cabergoline

38
Q

What else can dopamine agonists be use for?

A

-to shrink a prolactin-secreting tumor

39
Q

Toxicity and contraindications of dopamine agonists

A
  • 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
Q

Oxytocin

A
  • 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
Q

Vasopressin (ADH)

A
42
Q

Desmopressing

A

long acting synthetic analog of casopressin with minimal Va receptor activity
-mainly a good antidiuretic

43
Q

What receptors does vasopressin get?

A
  • GPCR’s V1 receptors found on vascular smooth muscle… vasoconsriction
  • V2 receptors found on renal tubule cells… increases water permeability in collecting tubules
44
Q

What else will activation of the V2 receptor do?

A

release factor VIII and VWF

45
Q

What do we use vaso and desmopressin for?

A
  • diabetes insipidus (the central kind)

- remember, that’s the test to see if it’s central or nephrogenic…. if desmopressin makes it better

46
Q

Which one has higher V2 receptor affinity?

A

desmopressin

47
Q

What else could desmopressin be used for since it activates those V2 receptors?

A

-Hemophilia A (factor VIII deficiency) and VWD

48
Q

Toxicity and contraindications for vaso/desmopressin?

A
  • 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
Q

Vasopressin antagonists

A
  • Conivaptan

- Tolvaptan

50
Q

MOA of the Vaptans

A
  • antagonists of vasopressin receptors
  • Tol for V2
  • Coni gets both
51
Q

What is unique about the vasopressin antagonists?

A

they increase renal free water excretion with little or no change in electrolyte excretion (as opposed to diuretics)

52
Q

What would we use vasopressin antagonists for?

A

-tx of euvolemic and hypervolemic hyponatremia

53
Q

In CHF, which drug increases renal free water excretion without a change in systemic vascular resistance?

A

Conivaptan

54
Q

What metabolizes coni/tolvaptan?

A

CYP3A4