1-4 and 5 Flashcards
Which two drugs have a black box warning that state they cause myelination disorders?
Tolvaptan/Mozvaptan (V2 Receptor Antagonists)
Which drug class does Conivaptan belong to?
V1a/V2 Receptor Antagonists
Which drug class is best use for treating hypervolemic-hyponatremia due to SIADH?
Vasopressin Receptor Antagonists
Clinical indications for Vasopressin agonists?
1) Diabetes insipidus
2) Nocturia
What part of the kidney is critical for conserving water?
Collecting duct
When plasma Osm increases, so do vasopressin levels. How does this affect water permeability?
Increases water permeability by enhancing AQP2 localization in membrane
What is the major receptor in renal tissue (specifically: in the principal cells of the collecting duct and thick ascending limb)?
V2
How does vasopressin lead to translocation of AQP2 on membrane surface?
-Rise in cAMP and PKA
What drug class binds to NPR receptors, thereby triggering conversion of GTP to cyclic GMP?
Natriuretic Peptides (AMP, CMP, Urodilatin)
True or False: In the Natriuretic Peptide pathway, both cGMP and PKG inhibit the CNG (cyclic nucleotide gate channel) directly
True
True or False: In the Natriuretic Peptide pathway, PKG prevents Na exit via Na/K ATPase
True
___ is a recombinant BMPknown to inhibit cyclic nucleotide gated cation channel (CNGC)
Nesiritide
Regarding natriuretic peptides, what channel allows for Na/K/NH4 entry and is controlled by cGMP?
CNGC (cyclic nucleotide gated cation channel)
Where do Natriuretic Peptides act?
Inner medullary collecting duct
What drug is a MR specific antagonist with reduced non-specific effects?
Eplerenone
True or False: Since Thiazides can interfere w/other steroid receptors, they can cause impotence, hirsuitism, menstrual irregularities, etc.
False - Since MR Antagonists can interfere w/other steroid receptors, they can cause impotence, hirsuitism, menstrual irregularities, etc.
What drugs prevent aldosterone induced increased expression of ENaC mRNA and protein
A. Spironolactone/Eplerenone
B. Amiloride
A. Spironolactine/Eplerenone
How do MR Antagonists decrease mRNA expression of ENaC and promote degradation of ENaC
They stop NEDD 4/2 from being phosphoryalted - therefore ENaC is degraded
By inhibiting aldosterone, aldosterone cannot bind to MR, enter nucleus, and upregulate ENa
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