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ENDO II Test I > Drugs Hypothalamus and Pituitary (linger) > Flashcards

Drugs Hypothalamus and Pituitary (linger) Flashcards

1
Q

Octreotide

A

somatostatin analog

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2
Q

lanreotide

A

somatostatin analog

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3
Q

Pegvisomant

A

GH antagonists

Inhibits binding of GH and prevents signal transduction

More effective than somatostatin analogs

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4
Q

Bromocriptine

A

Dopamine Agonists

coupled to Gαi/o, which inhibits adenylyl cyclase and decreases cAMP

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5
Q

Cabergoline

A

Dopamine Agonists

coupled to Gαi/o, which inhibits adenylyl cyclase and decreases cAMP

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6
Q

what are the vasopressin receptor agonists x2

A

vasopressin

desmopressin- longer half life

Peptide hormone released in response to rising plasma tonicity or failing blood pressure; antidiuretic and vasopressor properties
MOA: agonist at vasopressin (V1 and V2) receptors (GPCRs)

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7
Q

what are the vasopressin receptor antagonists x2

A

conivaptan
tolvaptan

antagonists at V2 receptors
Promotes the excretion of free water (without loss of serum electrolytes) resulting in net fluid loss, increased urine output, decreased urine osmolality, and subsequent restoration of normal serum sodium levels

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8
Q

mecasermin

A

Insulin Like growth factor 1 agonist (recombinant human IGF-1)

used for IGF-1 deficiency
and children with GH gene deletions who have developed neutralizing antibodies

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9
Q

most common adverse effect of mecasermin

A

hypoglycemia

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10
Q

what are the 2 strategies of growth hormone antagonists and which drugs represent the different strategies?

A

Reduce secretion of growth hormone
Somatostatin analogs: octreotide, lanreotide

Block action of growth hormone at receptors
Growth hormone receptor antagonist: pegvisomant

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11
Q

through what signalling pathway does prolactin act

A

JAK/STAT cytokine receptors

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12
Q

what is the clinical use of D2 receptor agonists

A

hyperprolactinemia (also acromegaly, Parkinson disease)

Shrink pituitary PRL-secreting tumors, lower circulating PRL levels, and restore ovulation in 70% of women with microadenomas and 30% of women with macroadenomas

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13
Q

what are the adverse effects of D2 receptor agonists

A

Nausea, headache, light-headedness, orthostatic hypotension, fatigue are most common adverse effects

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14
Q

clinical use of vasopressin agonists

A

pituitary diabetes insipidus, hemophilia A, von Willebrand disease

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15
Q

clinical use of vasopressin antagonists

A

Used in the treatment of clinically significant hypervolemic or euvolemic hyponatremia (associated with heart failure, cirrhosis, or SIADH)

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16
Q

which hormones activate kinase linked receptors of the JAK/STAT superfamily

A

GH and Prolactin

these are single chain protein hormones

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17
Q

which hormones act via GPCR’s

A

TSH
FSH
LH
ACTH

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18
Q

ACTH release is regulated by what

A

corticotropin releasing hormone (CRH)

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19
Q

what inhibits ACTH and CRH

A

cortisol

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20
Q

what stimulates and prohibits production of GH

A

stimulates–> GHRH

inhibited –> Somatostatin

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21
Q

which hormones of the pituitary act directly on target tissues

A

prolactin, vasopressin, ADH

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22
Q

what happens with disruption of the pituitary stalk and the hypothalamohypohysial portal vessels

A

prolactin levels will increase

ACTH, TSH, FSH, LH, GH levels will decrease

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23
Q

what are the target organs for GH and what is the primary target organ hormone or mediator

A

liver, muscle, bone, kidneys

IGF-1 is the primary target organ hormone/mediator

24
Q

what does somatostatin do

A

inhibits release of GH

25
Q

what it the recombinant human form of GH

A

somatropin (rhGH)

26
Q

what metabolizes GH

A

liver—> GH induces activity of P450’s

27
Q

growth hormone growth promoting effects are mediated through what?

A

an increase in IGF-1 transcription

28
Q

how do GH and IGF-1 differ in their effects on insulin

A

GH
-reduces insulin sensitivity (Causes mild hyperinsulinemia)

IGF-1
-act through IGF-1 and insulin receptors to lower serum glucose and reduce insulin

29
Q

how does GH affect muscle and lipid cells

A

muscle–> anabolic effects

lipids–> catabolic effects

30
Q

what are the adverse effects of GH in children

H
S
O
P
G
A

well tolerated in children

rare adverse effects include intracranial HTN (vision changes, headache, nausea, vomiting)

scoliosis

otitis media in pt’s with Turner syndrome
hypothyroidism

pancreatitis

gynecomastia

31
Q

what are the adverse effects of GH in adults?

A

adults have more adverse effects than children

peripheral edema

myalgias

arthralgias

carpal tunnel syndrome

32
Q

in what pt’s is GH contraindicated

A

active malignancy

33
Q

when is the use of mecasermin indicated

A

in pt’s with growth failure that is not responsive to exogenous GH (Due to mutations in GH receptor of GH signaling pathway, or IGF-1 gene defects)

34
Q

what is the most common side effect of mecasermin

A

hypoglycemia (eating 20 min before administration prevents hypoglycemia)

IGF-1 lowers serum glucose and reduces insulin

35
Q

what are the clinical uses of GH antagonists

A

utilized to treat anterior pituitary adenomas that secrete GH–> cause acromegaly and gigantism

36
Q

how does pegvisomant work

A

direct inhibition of the GH receptor (helps with GH secreting adenoma)

so the GH receptor cannot stimulate downstream JAK/STAT signaling

37
Q

what does somatostatin inhibit

A

GH, TSH, glucagon, insulin, gastrin

must use longer acting analogs b/c the real stuff is too short acting

38
Q

what are the clinical uses of Octreotide

A

this is a somatostatin analog

acromegaly
carcinoid syndrome
gastrinoma
glucagonoma 
nesidioblastosis
diabetic diarrhea
watery diarrhea
hypokalemia
achlorhydria
39
Q

what are the adverse effects of octreotide

A

nausea/vomting
abdominal cramps
flatulence
steatorrhea with bulky bowel movements

gallstones 
cardiac effects (bradycardia, conduction disturbances)

vitamin B12 deficiency

40
Q

how do men and women present who have hyperprolactinemia and why do they have these symptoms?

A

women- amenorrhea, galactorrhea

men- loss of libido and infertility

hypogonadism and infertility associated with hyperporlactinemia result from inhibition of GnRH release

41
Q

what are the uses of dopamine agonists

A

D2 receptor agonist

hyperprolactinemia - shrink pituitary PRL-secreting tumors

higher doses–> acromegaly (b/c GH release is also reduces) and parkinson disease

42
Q

which dopamine agonist has a longer half life, higher affinity and greater selectivity for the D2 receptor and lower incidence of side effects

A

Cabergoline

NOT bromocriptine

43
Q

which D2 agonist is used in pregnancy

A

Bromocriptine

44
Q

which pregnant pt’s should discontinue therapy

A

those with microadenomas b/c microadenoma growth during pregnancy is rare

45
Q

why shouldn’t you use Dopamine agonists to suppress postpartum lactation

A

due to increased risk of stroke or coronary thrombosis

46
Q

what are the adverse effects of dopamine agonists

A

nausea, headache, light-headed, orthostatic hypotension, fatigue

psychiatric manifestations

pulmonary infiltrates (chronic high doses)

47
Q

how is oxytocin administered for control of postpartum bleeding

A

IM

48
Q

how is oxytocin administered for initiation and augmentation of labor

A

IV

49
Q

what does oxytocin do

A

stimulates uterine contraction and elicits milk ejection in lactating women

50
Q

what stimulates release of ADH

A

falling blood pressure and rising plasma osmolality

ADH possesses Antidiuretic and vasopressor properties

51
Q

via what receptors do Vasopressin and Desmopressin work

A

V1 and V2 receptors which are GPCR

52
Q

V2 receptors

A

found on renal tubule cells and reduce diuresis through increased water permeability and water resorption in the collecting tubules

53
Q

what are vasopressin and desmopressin used as treatments of choice for

A

Pituitary diabetes insipidus

54
Q

what other ways can desmopressin be used?

A

for treatment of coagulopathy in hemophilia A and VWD

55
Q

Adverse effects of vasopressin and desmopressin

A

headache, nausea, abd cramps, agitation, allergic rxns

overdose –> hyponatremia, seizures

56
Q

in which patients must you be careful when administering vasopressin

A

coronary artery disease patients due to vasoconstriction

57
Q

what are the uses of vasopressin antagonists

A

used to relieve symptoms and reduce signs of hyponatremia and heart failure

ENDO II Test I (4 decks)

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