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rough overview of HF: RAS drugs and ADrenergic Receptor....
951 - Block 3
30
Science
Pre-School
11/09/2011

Additional Science Flashcards

 


 

Cards

Term
I am a tissue protease that converts ANGI to ANg II.  I am not induced in HF.  Who am I?
Definition
chymase
Term

I am expressed in:

cardiac myocytes

fibroblasts

vascular smooth muscle cells

endothelial cells

 

Definition
ACE
Term

I am expressed in:

mast cells 

other interstitial cells

Definition
Chymase
Term
What are the four therapeutic effects of ACEi in HF?
Definition

1. inhibit formation of ANG II

12. arterial and venous dilation, decreasing both afterload and preload

3. decrease aldosterone release

4. decrease LV hypertrophy (growth mediated effect)

Term
What role does the AT1 receptor play?  (What effects does it have?)
Definition

cell growth

increased NE

Term
What effects does the AT2 receptor have?
Definition
unknown
Term
ACEi have been porven in clinical trials to improve what fourthings in HF?
Definition

1. hemodynamics

2. clinical status

3. lessen symtpoms of HF

4. decrease mortality

Term
What stages of HF may you use ACEi? 
Definition
Used in all stages/classes, slow progression of the disease
Term

What is bradykinin?

 

What degrades bradykinin?

Definition

potent vasodilator

 

ACE also degrades bradykinin

Term
When you give an ACEi, you block the degradation of bradykinin. ...What effects are caused by the increased bradykinin levels?
Definition

edema of the skin (wheals)

 

increased coughing

Term
What are the adverse effects of ACEi in the treatment of HF?
Definition

1. hypotension (dizziness, syncope)

 

2. renal insufficiency, renal perfusion pressur in people with reduced CO is maintained by the effect of ANG II to contrict the efferent arteriole

 

3.  elimination of ANG II in maintaing the GFR

Term

What receptor is responsible for the adverse effects of increased ANG II?

 

what are the effects?

Definition

AT 1

 

vasoconstriction

myocyte apoptosis

cardiac myocyte growth

NE release

aldosterone release 

 

Term
What is the predominant Ang II receptor in the vasculature?
Definition
AT 1
Term
What two ARBs are approved for heart failure when an ACEi is not well tolerated?
Definition
Valsartan and candesartan 
Term
What did ELITE 1 show?
Definition
losartan superior to ACEi in elderly with HF
Term
What did ELITE 2 prove?
Definition
ACE i was equal to or superior to AT1 receptor antagonist in all endpoints measured
Term
VALIANT was the first trial to show what result?
Definition
comparable efficacy of AT1 receptor antagonist and ACe i
Term
What happens to aldosterone levels after long term use of ACEi?
Definition

They increase back to normal or elevated levels.

 

This is called aldosterone escape.

Term

I cause:

sodium retention, increasing preload

myocardial fibrosis by stimulating collagen production

inhibit uptake of NE (elevates NE in heart)

cause baroreceptor dysfunction

 

who am I?

Definition
aldosterone
Term
T/F: there is normally no adrenergic stimulation in left ventricle during restiing state.
Definition
true 
Term
The chronic increases in sympathetic activity  are caused by what four reasons?
Definition

1. reduction in CO

2. increased HR

3. excessive vasoconstriction

4. excessive retention of salt and water

Term
Long term sympathetic stimulation...
Definition

further depresses ventricular function and increases the heart's demand for energy

 

not goooood 

Term
What is the normal expression of beta 1 and beta 2 in the ventricles?
Definition

80/20

 

during HF beta 2 can increase up to 40%

Term
Why are second and third generation BBs effective?
Definition

1. reverses downregulation of beta 1

2. produces more normal cardiac performance

- increases reserve capacity

3. restores normal coupling of receptor to adenylate cyclase

4. reduces cardiac remodeling and myocardial death resulting from apoptosis

5. reverses hyper-phosphorylation of the calcium release channel in the ER (ryanodine receptor) 

Term
You may not use class 1 bb in HF.
Definition

You may not use class 1 bb in HF.

Term
Further description of the beneficial effects:
Definition
Beta blockers reduce the adverse effects of excessive NE by blocking the receptor from NE.  BB bind the receptor but do not trigger signal transduction. BB also stabilize cardiac rhythm and reduce HR. 
Term

Name the single, third gen BB approved for HF:

 

it is a non-selective BB and has potent vasodilator effects due to alpha 1 antagonism...must titrate up slowly.

 

also reduces afterload

Definition
carvedilol
Term
Etanercept has recently entered phase III trials for HF treatment....how does this drug work in HF?
Definition
It is a TNF- alpha receptor fusion protein, which would block the pro-inflammatory TNF-alpha (which produces a negative ionotropic effect). 
Term
I am a small molecule TNF-alpha inhibitor that is used to treat other disorders, but I recently show that I can increase left ventricular funtion in a controlled trial.  Who am I?
Definition
pentoxifylline. 
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