Hypothalamic And Pituitary Hormones (Kruse)

Question 1

Somatotropin is also known as ___

Answer 1

GH

Question 2

Receptor type and signaling pathway for somatotropin (GH)?

Answer 2

Kinase-linked receptor super family

JAK/STAT signaling pathway

Question 3

Contraindications for GH/Somatotropin?

Answer 3

Malignancy

Question 4

Mecasermin is what type of hormone? Route of admin? Most common adverse effect?

Answer 4

Complex of recombinant human IGF-1 (rhIGF-1) and recombinant human insulin-like growth factor binding protein-3 (IGFBP-3) –> need rhIGFBP-3 to increase t1/2 of rhIGF-1

SubQ

Hypoglycemia (eating 20 mins before admin prevents hypoglycemia)

Question 5

Octreotide and lanreotide are what type of drugs/hormones?

Answer 5

Somatostatin analog (GH antagonist)

Question 6

Adverse effects of somatostatin analogs?

Answer 6

GI: diarrhea, nausea, abdominal pain
Gallbladder sludge and gallstones
Cardiac effects: sinus bradycardia, conduction disturbances
Vitamin B12 deficiency

Question 7

___ is approved for tx of acromegaly and is a somatostatin analog

Answer 7

Lanreotide

Question 8

__ is a GH receptor antagonist used to tx acromegaly

Answer 8

Pegvisomant

Question 9

Pegvisomant is a PEG derivative of a mutant GH that binds to GH receptor and allows receptor to dimerize, but does not activate __ signaling cascade or stimulate IGF-1 secretion

Answer 9

JAK-STAT

Question 10

For pts with symptomatic hyperprolactinemia, inhibition of prolactin secretion can be achieved with __

Answer 10

Dopamine agonists

Question 11

Bromocriptine and cabergoline are __ hormones/drugs used to tx hyperprolactinemia. What is their MOA?

Answer 11

Dopamine agonists

D2 receptor agonist

Question 12

Which dopamine agonist has a longer half life?

Answer 12

Cabergoline (65 hrs)

Bromocriptine is 15 hrs

Question 13

Most common side effects of dopamine agonists?

Answer 13

Nausea, headache, light-headedness, orthostatic hypotension, fatigue

Question 14

List the ADH agonists:

Answer 14

Vasopressin and desmopressin

These are peptide hormones

Question 15

__ is a long-acting synthetic analog of vasopressin with minimal V1 receptor activity and an antidiuretic-to-pressor ration 3000x that of vasopressin

Answer 15

Desmopressin

Question 16

MOA of vasopressin?

Answer 16

Activates GPCR V1 receptors (vascular smooth m., and mediate vasoconstriction) and V2 receptors (renal tubule cells and reduce diuresis)

Question 17

__ are the tx of choice for pituitary (central) diabetes insipidus

Answer 17

Vasopressin and desmopressin

Desmopressin is preferred d/t selectivity of V2 receptors

Question 18

__ is used in the tx of coagulopathy in hemophilia A and VW disease

Answer 18

Desmopressin

Question 19

Toxicity and contraindications with vasopressin and desmopressin?

Answer 19

Headache, nausea, abdominal cramps, agitation, allergic rxns occur rarely
OD can lead to hyponatremia and seizures

Used with caution in pts with CAD d/t vasoconstriction

Question 20

Conivaptan and tolvaptan are what types of drugs?

Answer 20

Vasopressin antagonists

Question 21

MOA of Tolvaptan?

MOA of Conivaptan?

Answer 21

Selective for V2 receptors

Nonselective and blocks V1 and V2 receptors

Question 22

Conivaptan and tolvaptan are utilized in the tx of what?

Answer 22

Euvolemic and hypervolemic hyponatremia (in cases of CHF and SIADH)

Question 23

How are conivaptan and tolvaptan metabolized?

Answer 23

CYP3A4