Inotropic Agents - Dr. Stevens Flashcards

1
Q

Which is more hydrophobic, digoxin or digitoxin? Why?

A

Digitoxin is more hydrophobic because it is missing the 12-OH group that digoxin has. It is the most lipophilic cardiac glycoside.

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2
Q

Which has the longer half-life, digoxin or digitoxin? How do the metabolisms compare?

A

Digitoxin has the longer half-life. It is extensively metabolized by the liver. Digoxin is eliminated 80% unchanged, and is metabolized by the liver as well.

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3
Q

How does quinidine interact with digoxin? (How does blocks P-gp in the renal tube affect digoxin?)

A

It increases plasma levels of digoxin.

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4
Q

How does verapamil interact with digoxin? (How does inhibiting P-gp efflux of digoxin affect digoxin?)

A

Digoxin absorption is increased.

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5
Q

How does rifampin affect digoxin? (How does inducing P-gp efflux affect digoxin?)

A

The absorption of digoxin is decreased.

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6
Q

How does bile acid binding resins affect digoxin? (cholestyramine?)

A

Less digoxin absorption.

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7
Q

How does furosemide interact with digoxin?

A

It decreased extracellular K, which makes it more difficult for the Na/K ATPase to pump K back into the cell to reset the chemical gradient. This increases phosphorylation of the ATPase, which allows digoxin to have a higher binding affinity to the extracellular site. This makes the drug work more effectively.

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8
Q

What are some common side effects of cardiac glycosides?

A

Blurred vision, loss of appetite. Can also be pro-arrhythmic.

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9
Q

What does GI side effects of digoxin often indicate?

A

Digitalis toxicity

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10
Q

What can you treat digitalis toxicity with?

A

Digifab, or Digibind. This will help prevent cardiac arrest.

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11
Q

How do phosphodiesterase inhibitors work?

A

Block degradation of cAMP to AMP

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12
Q

Should PDE3 inhibitors be used for treating acute or chronic CHF?

A

Acute CHF. Chronic use increases the mortality rate.

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13
Q

What type of medication is Levosimendan? When is it used?

A

A Ca-sensitizing agent. It is used in acute CHF patients with no risk of arrhythmias.

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14
Q

How does levosimendan work?

A

It increases contractility by binding the N-terminus of troponin C and stabilizing the Ca-bound conformation. It also activates ATP-regulated K channels and causes vasodilation in smooth muscles.

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15
Q

What B-adrenergic agent is used as an inotropic agent?

A

Dobutamine.

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16
Q

How does dobumatine act?

A

It is sold as a racemate, which is important in it’s action. The inotropic effect is a result of B1-agonism by the (+)dobutamine and alpha-agonism by the (-) dobutamine. There is no vasodilation by the alpha-agonism because it is negated by the +dobutamine’s alpha-antagonism. The overall effect is an increase in stroke volume and little heart rate increase.

17
Q

How is dobumatine metabolized?

A

By COMT

18
Q

What is the only orally metabolized inotropic agent?

A

Digoxin. Others are IV.