Exam 5 - ACEs/ARBs, Diuretics Yang

Question 1

when is the RAAS system activated?

Answer 1

when blood pressure is low (reduced blood volume)

Question 2

target for ACE inhibitors

Answer 2

angiotensin-converting enzyme

Question 3

target for ARBs

Answer 3

angiotensin II receptor

Question 4

what is the only direct renin inhibitor drug?

Answer 4

Aliskiren (dec Ang I formation from angiotensinogen)

Question 5

_____ is released by juxtaglomerular cells in the kidney due to low BP, low NaCl in the distal tubule of the kidney, and increased SNS activity (beta-1)

a. angiotensin
b. angiotensinogen
c. renin
d. aldosterone

Answer 5

c. renin

Question 6

renin is what kind of protease?

Answer 6

aspartic acid

Question 7

angiotensin converting enzyme (ACE) converts __________ to __________

Answer 7

angiotensin I to angiotensin II

Question 8

what bond does renin cleave in angiotensinogen to make angiotensin I?

a. leu-val
b. phe-his
c. asp-arg
d. val-tyr

Answer 8

a. leu-val

Question 9

what bond does ACE cleave in angiotensin I to make angiotensin II?

a. leu-val
b. phe-his
c. asp-arg
d. val-tyr

Answer 9

b. phe-his

Question 10

ACE is also responsible for inactivation of __________, a nonapeptide (9 AAs) which promotes vasodilation and other physiological effects through prostaglandin release

Answer 10

bradykinin

Question 11

aliskiren clinical use

Answer 11

not first-line for hypertension –
effective in reducing renin leading to a drop in
blood pressure

Question 12

true or false: aliskiren can be used in pregnancy

Answer 12

false

Question 13

drugs that block _____ receptors inhibit release of renin due to interaction with receptors on juxtaglomerular cells in kidney

a. alpha 1
b. alpha 2
c. beta 1
d. beta 2

Answer 13

c. beta 1

Question 14

ACE inhibitor drugs ending

Answer 14

“-pril”

Question 15

3 ACE inhibitor classes

Answer 15

1. sulfylhydryl-containing
2. dicarboyxl-containing
3. phosphorus-containing

Question 16

dicarboyxl-containing ACE inhibitors are structurally related to __________

Answer 16

enalapril (one of most potent ACE inhibitors)

Question 17

sulfhydryl-containing ACE inhibitors are structurally related to __________

Answer 17

captopril

Question 18

phos-containing ACE inhibitors are structurally related to __________

Answer 18

fosinopril

Question 19

many ACE inhibitors are ester-containing ___ ___ that are much less potent than the active drug

Answer 19

pro drugs

Question 20

most commonly used ACE inhibitor

Answer 20

lisinopril

Question 21

true or false: lisinopril is a pro-drug

Answer 21

false

Question 22

which of the following is a prodrug?

a. lisinopril
b. enalapril
c. captopril

Answer 22

b. enalapril

Question 23

enalapril is hydrolyzed to active diacid ______

Answer 23

enalaprilat (pronounced enalapril-ate)

Question 24

true or false: fosinopril is a prodrug

Answer 24

true (requires hydrolysis to become active)

Question 25

clinical use of ACE inhibitors

Answer 25

first line monotherapy for HTN, heart failure

Question 26

dry cough from ACE inhibitors is due to accum of __________

Answer 26

bradykinin

Question 27

what class of drugs can dec ACE inhibitor hypotensive effects bc they work on the renin-bradykinin pathways?

Answer 27

NSAIDs

Question 28

3 main side effects of captopril, lisinopril

Answer 28

dry cough angioedema hyperkalemia

Question 29

prototypical ARB drug

Answer 29

losartan

Question 30

ARBs block Ang II receptors w/ much higher affinity for a. AT1 receptor b. AT2 receptor

Answer 30

a. AT1

Question 31

ARBs are largely excreted in _____ a. feces b. urine

Answer 31

a. feces

Question 32

ARB drug ending

Answer 32

"-sartan"

Question 33

rank the order of potency for these agents (some are equal): losartan EXP 3174 (active metabolite of losartan) omesartan eprosartan candesartan valsartan telmisartan irbesartan

Answer 33

candesartan = omesartan > irbesartan = eprosartan > telmisartan = valsartan = EXP 3174 > losartan

Question 34

clinical use of ARBs

Answer 34

first-line monotherapy for HTN (often for those who don't tolerate ACE inhibitors)

Question 35

true or false: ACE inhibitors and ARBs are LESS effective in African Americans

Answer 35

true

Question 36

two aldosterone receptor antagonist drugs

Answer 36

spironolactone eplerenone

Question 37

common adverse effect of aldosterone receptor antagonists

Answer 37

hyperkalemia (they are potassium-sparing)

Question 38

clincal uses of aldosterone receptor antagonist (3)

Answer 38

-chronic heart failure (reduces mortality) -aldosteronism -HTN (not monotherapy but used to reduce hypokalemia)

Question 39

which drug has antiandrogen effects and can cause gynecomastia and impotence?

Answer 39

spironolactone

Question 40

two thiazide drugs

Answer 40

chlorthalidone, HCTZ

Question 41

thiazides MOA

Answer 41

diuretic blocking Na-Cl symporter on DCT

Question 42

true or false: thiazides are NOT effective in African Americans

Answer 42

false

Question 43

clinical use of thiazides

Answer 43

first-line monotherapy for mild-moderate HTN

Question 44

thiazides are not a drug of choice for pts with what 3 conditions?

Answer 44

diabetes, hyperlipidemia, gout

Question 45

long term thiazides lower _______ _______ _______

Answer 45

peripheral vascular resistance

Question 46

loop diuretics can be used _____ line monotherapy for HTN a. first b. second

Answer 46

b. second

Question 47

true or false: K+ sparing diuretics are used first line for HTN

Answer 47

false (bc they are weak and associated with hyperkalemia)

Question 48

which of the following are safe to use for HTN in pregnancy? SELECT ALL THAT APPLY a. ACE inhibitors b. ARBs c. labetalol d. methyldopa e. aldosterone receptor antagonists f. metoprolol g. direct renin inhibitors

Answer 48

c, d, f