Hypothalamic And Pituitary Hormones (Kruse) Flashcards
Somatotropin is also known as ___
GH
Receptor type and signaling pathway for somatotropin (GH)?
Kinase-linked receptor super family
JAK/STAT signaling pathway
Contraindications for GH/Somatotropin?
Malignancy
Mecasermin is what type of hormone? Route of admin? Most common adverse effect?
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)
Octreotide and lanreotide are what type of drugs/hormones?
Somatostatin analog (GH antagonist)
Adverse effects of somatostatin analogs?
GI: diarrhea, nausea, abdominal pain
Gallbladder sludge and gallstones
Cardiac effects: sinus bradycardia, conduction disturbances
Vitamin B12 deficiency
___ is approved for tx of acromegaly and is a somatostatin analog
Lanreotide
__ is a GH receptor antagonist used to tx acromegaly
Pegvisomant
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
JAK-STAT
For pts with symptomatic hyperprolactinemia, inhibition of prolactin secretion can be achieved with __
Dopamine agonists
Bromocriptine and cabergoline are __ hormones/drugs used to tx hyperprolactinemia. What is their MOA?
Dopamine agonists
D2 receptor agonist
Which dopamine agonist has a longer half life?
Cabergoline (65 hrs)
Bromocriptine is 15 hrs
Most common side effects of dopamine agonists?
Nausea, headache, light-headedness, orthostatic hypotension, fatigue
List the ADH agonists:
Vasopressin and desmopressin
These are peptide hormones
__ is a long-acting synthetic analog of vasopressin with minimal V1 receptor activity and an antidiuretic-to-pressor ration 3000x that of vasopressin
Desmopressin
MOA of vasopressin?
Activates GPCR V1 receptors (vascular smooth m., and mediate vasoconstriction) and V2 receptors (renal tubule cells and reduce diuresis)
__ are the tx of choice for pituitary (central) diabetes insipidus
Vasopressin and desmopressin
Desmopressin is preferred d/t selectivity of V2 receptors
__ is used in the tx of coagulopathy in hemophilia A and VW disease
Desmopressin
Toxicity and contraindications with vasopressin and desmopressin?
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
Conivaptan and tolvaptan are what types of drugs?
Vasopressin antagonists
MOA of Tolvaptan?
MOA of Conivaptan?
Selective for V2 receptors
Nonselective and blocks V1 and V2 receptors
Conivaptan and tolvaptan are utilized in the tx of what?
Euvolemic and hypervolemic hyponatremia (in cases of CHF and SIADH)
How are conivaptan and tolvaptan metabolized?
CYP3A4
