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
what it the recombinant human form of GH
somatropin (rhGH)
26
what metabolizes GH
liver---> GH induces activity of P450's
27
growth hormone growth promoting effects are mediated through what?
an increase in IGF-1 transcription
28
how do GH and IGF-1 differ in their effects on insulin
GH -reduces insulin sensitivity (Causes mild hyperinsulinemia) IGF-1 -act through IGF-1 and insulin receptors to lower serum glucose and reduce insulin
29
how does GH affect muscle and lipid cells
muscle--> anabolic effects lipids--> catabolic effects
30
what are the adverse effects of GH in children ``` H S O P G ```
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
what are the adverse effects of GH in adults?
adults have more adverse effects than children peripheral edema myalgias arthralgias carpal tunnel syndrome
32
in what pt's is GH contraindicated
active malignancy
33
when is the use of mecasermin indicated
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
what is the most common side effect of mecasermin
hypoglycemia (eating 20 min before administration prevents hypoglycemia) IGF-1 lowers serum glucose and reduces insulin
35
what are the clinical uses of GH antagonists
utilized to treat anterior pituitary adenomas that secrete GH--> cause acromegaly and gigantism
36
how does pegvisomant work
direct inhibition of the GH receptor (helps with GH secreting adenoma) so the GH receptor cannot stimulate downstream JAK/STAT signaling
37
what does somatostatin inhibit
GH, TSH, glucagon, insulin, gastrin must use longer acting analogs b/c the real stuff is too short acting
38
what are the clinical uses of Octreotide
this is a somatostatin analog ``` acromegaly carcinoid syndrome gastrinoma glucagonoma nesidioblastosis diabetic diarrhea watery diarrhea hypokalemia achlorhydria ```
39
what are the adverse effects of octreotide
nausea/vomting abdominal cramps flatulence steatorrhea with bulky bowel movements ``` gallstones cardiac effects (bradycardia, conduction disturbances) ``` vitamin B12 deficiency
40
how do men and women present who have hyperprolactinemia and why do they have these symptoms?
women- amenorrhea, galactorrhea men- loss of libido and infertility hypogonadism and infertility associated with hyperporlactinemia result from inhibition of GnRH release
41
what are the uses of dopamine agonists
D2 receptor agonist hyperprolactinemia - shrink pituitary PRL-secreting tumors higher doses--> acromegaly (b/c GH release is also reduces) and parkinson disease
42
which dopamine agonist has a longer half life, higher affinity and greater selectivity for the D2 receptor and lower incidence of side effects
Cabergoline | NOT bromocriptine
43
which D2 agonist is used in pregnancy
Bromocriptine
44
which pregnant pt's should discontinue therapy
those with microadenomas b/c microadenoma growth during pregnancy is rare
45
why shouldn't you use Dopamine agonists to suppress postpartum lactation
due to increased risk of stroke or coronary thrombosis
46
what are the adverse effects of dopamine agonists
nausea, headache, light-headed, orthostatic hypotension, fatigue psychiatric manifestations pulmonary infiltrates (chronic high doses)
47
how is oxytocin administered for control of postpartum bleeding
IM
48
how is oxytocin administered for initiation and augmentation of labor
IV
49
what does oxytocin do
stimulates uterine contraction and elicits milk ejection in lactating women
50
what stimulates release of ADH
falling blood pressure and rising plasma osmolality ADH possesses Antidiuretic and vasopressor properties
51
via what receptors do Vasopressin and Desmopressin work
V1 and V2 receptors which are GPCR
52
V2 receptors
found on renal tubule cells and reduce diuresis through increased water permeability and water resorption in the collecting tubules
53
what are vasopressin and desmopressin used as treatments of choice for
Pituitary diabetes insipidus
54
what other ways can desmopressin be used?
for treatment of coagulopathy in hemophilia A and VWD
55
Adverse effects of vasopressin and desmopressin
headache, nausea, abd cramps, agitation, allergic rxns overdose --> hyponatremia, seizures
56
in which patients must you be careful when administering vasopressin
coronary artery disease patients due to vasoconstriction
57
what are the uses of vasopressin antagonists
used to relieve symptoms and reduce signs of hyponatremia and heart failure