ACE-Is and ARBs

Question 1

What are three actions of angiotensin II?

Answer 1

• potent vasoconstriction
• secretion of aldosterone retaining renal Na and H2O
• stimulates cardiac and vascular smooth muscle proliferation –> hypertrophy and dec efficiency

Question 2

What is the mechanism of action of ACE Inhibitors (ACEi) and angiotensin receptor blockers (ARB)?

Answer 2

ACEi prevents conversion of angiotensin I to angiotensin II. ARB prevents angiotensin II from binding to receptors.

Question 3

In addition to HTN, what other disesase benefits greatly from ACEi?

Answer 3

CHF - almost all CHF patients are on an ACEi

Question 4

All ACEi drugs end in what suffix? List examples.

Answer 4

“pril” - elanapril, captopril, lisinopril, quinapril

Question 5

What action of ACEi drugs may cause a dry, hacking cough?

Answer 5

Inhibition of kinase which increase bradykinin in lungs. Bradykinin is a vasodilator and promotes production of other vasodilators. Inc bradykinin in the lungs can also cause a cough.

Question 6

How is a cough caused by an ACEi treated?

Answer 6

Possibly ASA or by removing the ACEi drug. DO NOT treat with cough suppressants.

Question 7

Name three cough suppressants.

Answer 7

Benzonatate, codeine, dextromethorphan

Question 8

Other than a dry cough, what other adverse effects exist with ACEi drugs?

Answer 8

HyperK, Angioedema (may also be caused by NSAIDs), avoid in pregnancy (especially 3rd trimester)

Question 9

What is the caution in prescribing ACEi drugs to patients with renal disease?

Answer 9

Must r/o renal artery stenosis. RAS reduces blood flow to the kidney causing the efferent arteriole to constrict as a compensatory mechanism. ACEi drugs prevent the compensatory constriction of the efferent arteriole and renal function decreases.

Question 10

What was the first ACEi?

Answer 10

Captopril

Question 11

Define prodrug and state which ACEi is a prodrug.

Answer 11

prodrug: not in active form when swallowed. Liver coverts drug to its active form. Enalapril is an ACEi prodrug.

Question 12

What is the only IV ACEi and how often is it used?

Answer 12

Enalaprilat - rarely used bc it is expensive

Question 13

ARB drugs end in what suffix? List some examples.

Answer 13

“sartan” - losartan, valsartan, telmisartan

Question 14

Why are renin inhibitors never used?

Answer 14

They are too nephrotoxic

Question 15

What is the function of neprilysin?

Answer 15

Pac man like enzyme that chews up chemicals in the blood stream that cause vasodilation

Question 16

What is the action of neprilysin inhibitors?

Answer 16

Inhibit neprilysin enzyme so the chemicals in the blood that promote vasodilation stay around longer.

Question 17

What is the only neprilysin inhibitor on the market?

Answer 17

Sacubitril combined with Valsartan –> brand name Entresto.

Question 18

What is the only indication for Entresto?

Answer 18

Severe heart failure

Question 19

What is the black box warning for Entresto?

Answer 19

Fetal toxicity –> pregnancy category X