ACEs and ARBs

Question 1

What does renin do?

Answer 1

Works on angiotensinogen to produce angiotensin I

Question 2

What does the Angiotensin Converting Enzyme (ACE) do?

Answer 2

Works on Angiotensin I to produce Angiotensin II

Question 3

What do ARBs target?

Answer 3

Angiotensin II

Question 4

What are the 2 functions of angiotensin II that are blocked by ARBs?

Answer 4

-Vasoconstriction

-Aldosterone secretion

Question 5

What is the main effect of Angiotensin II that ARBs want to block?

Answer 5

Increased blood pressure

Question 6

What else does ACE work on and what is its effect?
(Another reason why we want to block ACE)

Answer 6

Besides Angiotensin I, Ace also works on Bradykinin

ACE inactivates bradykinin

Bradykinin produces decreased blood pressure so we do NOT want it inactivated. By using ACE inhibitors, we block the degradation of bradykinin

Question 7

What drug is a renin inhibitor?

Answer 7

Aliskiren

Question 8

How does Aliskiren work?

Answer 8

Direct inhibitor of renin

-Decreases formation of angiotensin I from angiotensinogen

**Not first line for hypertension

Question 9

What is a contraindication of Aliskiren?

Answer 9

Cannot be used in pregnant or nursing mothers

Question 10

What word ending signifies that a drug is an ACE Inhibitor?

Answer 10

“pril”

Question 11

What are the 3 classes of ACE inhibitors?

Answer 11

-Sulfhydryl-containing (similar to Captopril)
-Dicarboxyl-containing (similar to enalapril) *most potent
-Phosphorus-containing (similar to fosinopril)

Question 12

What two ACE inhibitors are not pro-drugs?

Answer 12

Lisinopril

Captopril

Question 13

What is the first-line hypertension treatment?

Answer 13

ACE and ARB

Question 14

What is the function of Captopril and Lisinopril?

Answer 14

ACE inhibitors

-First line monotherapy for hypertension

Question 15

What are some important considerations with Captopril and Lisinopril?

Answer 15

-Useful in whites but not people of African descent

-Beneficial in patients with heart failure or chronic kidney disease

-Better for patients with diabetes than thiazides

-Better for patients with ischemic heart disease than vasodilators

Question 16

What are some side effects of Lisinopril and Captopril?

Answer 16

-Cough
-Angioedema
-Hyperkalemia

Question 17

What are the contraindications for Captopril and Lisinopril?

Answer 17

-Pregnancy

-Do not use if GFR drops by more than 30%

Question 18

What affect can NSAIDs have on ACE inhibitors?

Answer 18

-Block production of prostaglandins which mediate the vasodilation produced by bradykinin

-Because of this, NSAIDs decrease the effect of ACE inhibitors

Question 19

What causes ACE inhibitors to have cough and angioedema as a side effect?

Answer 19

Accumulation of bradykinin

Question 20

Why can ACE inhibitors cause hyperkalemia?

Answer 20

Decreased production of aldosterone

(Aldosterone secretion is a function of Angiotensin II)

Question 21

What word-ending is indicative of ARBs?

Answer 21

“sartan”

Question 22

What drug is prototypical for ARBs?

Answer 22

Losartan

Question 23

What ARB has the lowest potency?

Answer 23

Losartan

*drug itself does not have much activity, but its metabolite is potent

Question 24

What ARB has the highest potency?

Answer 24

Candesartan

Question 25

What is the angiotensin II receptor?

Answer 25

AT1

Question 26

When are ARBs used?

Answer 26

First-line treatment for hypertension *Often used in patients who do not tolerate ACE inhibitors

Question 27

What are the adverse effects of ARBs?

Answer 27

-Hypotension -Hyperkalemia -Low rate of angioedema -Fetal pathologies -Reduction in GFR

Question 28

What is the function of spironolactone and eplerenone?

Answer 28

Aldosterone Receptor Antagonists (block reabsorption of sodium and decrease blood pressure) -Potassium-sparing diuretics

Question 29

What are spironolactone and eplerenone used for?

Answer 29

Chronic heart failure *not monotherapy for hypertension but used to reduce hypokalemia

Question 30

What are the adverse effects associated with spironolactone and eplerenone?

Answer 30

-Hyperkalemia -Antiandrogen effects

Question 31

What are all of the first-line treatment options for hypertension?

Answer 31

-Diuretics (thiazides) -ACE Inhibitors -ARBs -L-Type Ca++ Channel Antagonists (CCBs)

Question 32

What drug is the one thiazide mentioned?

Answer 32

Chlorthalidone

Question 33

How does Chlorthalidone work?

Answer 33

-Blocks sodium-chloride symporter on the distal convoluted tubule

Question 34

What are 2 important notes with use of chlorthalidone?

Answer 34

**Effective in people of African ancestry *Not the drug of choice for people with diabetes, hyperlipidemia, or gout

Question 35

What drugs can be used to treat hypertension in pregnancy?

Answer 35

-Methyldopa -Labetalol -Metoprolol *other beta blockers

Question 36

What hypertension drugs should be avoided in pregnancy?

Answer 36

-ACE inhibitors -ARBs -Direct renin inhibitors -Aldosterone receptor antagonists