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PHRM 844 Therapeutics > Exam 5 - ACEs/ARBs, Diuretics Yang > Flashcards

Exam 5 - ACEs/ARBs, Diuretics Yang Flashcards

1
Q

when is the RAAS system activated?

A

when blood pressure is low (reduced blood volume)

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2
Q

target for ACE inhibitors

A

angiotensin-converting enzyme

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3
Q

target for ARBs

A

angiotensin II receptor

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4
Q

what is the only direct renin inhibitor drug?

A

Aliskiren (dec Ang I formation from angiotensinogen)

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5
Q

_____ 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

A

c. renin

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6
Q

renin is what kind of protease?

A

aspartic acid

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7
Q

angiotensin converting enzyme (ACE) converts __________ to __________

A

angiotensin I to angiotensin II

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8
Q

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

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

A

a. leu-val

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9
Q

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

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

A

b. phe-his

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10
Q

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

A

bradykinin

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11
Q

aliskiren clinical use

A

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

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12
Q

true or false: aliskiren can be used in pregnancy

A

false

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13
Q

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

A

c. beta 1

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14
Q

ACE inhibitor drugs ending

A

“-pril”

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15
Q

3 ACE inhibitor classes

A
  1. sulfylhydryl-containing
  2. dicarboyxl-containing
  3. phosphorus-containing
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16
Q

dicarboyxl-containing ACE inhibitors are structurally related to __________

A

enalapril (one of most potent ACE inhibitors)

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17
Q

sulfhydryl-containing ACE inhibitors are structurally related to __________

A

captopril

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18
Q

phos-containing ACE inhibitors are structurally related to __________

A

fosinopril

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19
Q

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

A

pro drugs

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20
Q

most commonly used ACE inhibitor

A

lisinopril

21
Q

true or false: lisinopril is a pro-drug

A

false

22
Q

which of the following is a prodrug?

a. lisinopril
b. enalapril
c. captopril

A

b. enalapril

23
Q

enalapril is hydrolyzed to active diacid ______

A

enalaprilat (pronounced enalapril-ate)

24
Q

true or false: fosinopril is a prodrug

A

true (requires hydrolysis to become active)

25
Q

clinical use of ACE inhibitors

A

first line monotherapy for HTN, heart failure

26
Q

dry cough from ACE inhibitors is due to accum of __________

A

bradykinin

27
Q

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

A

NSAIDs

28
Q

3 main side effects of captopril, lisinopril

A

dry cough
angioedema
hyperkalemia

29
Q

prototypical ARB drug

A

losartan

30
Q

ARBs block Ang II receptors w/ much higher affinity for

a. AT1 receptor
b. AT2 receptor

A

a. AT1

31
Q

ARBs are largely excreted in _____

a. feces
b. urine

A

a. feces

32
Q

ARB drug ending

A

“-sartan”

33
Q

rank the order of potency for these agents (some are equal):

losartan
EXP 3174 (active metabolite of losartan)
omesartan
eprosartan
candesartan
valsartan
telmisartan
irbesartan

A

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

34
Q

clinical use of ARBs

A

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

35
Q

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

A

true

36
Q

two aldosterone receptor antagonist drugs

A

spironolactone
eplerenone

37
Q

common adverse effect of aldosterone receptor antagonists

A

hyperkalemia (they are potassium-sparing)

38
Q

clincal uses of aldosterone receptor antagonist (3)

A

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

39
Q

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

A

spironolactone

40
Q

two thiazide drugs

A

chlorthalidone, HCTZ

41
Q

thiazides MOA

A

diuretic blocking Na-Cl symporter on DCT

42
Q

true or false: thiazides are NOT effective in African Americans

A

false

43
Q

clinical use of thiazides

A

first-line monotherapy for mild-moderate HTN

44
Q

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

A

diabetes, hyperlipidemia, gout

45
Q

long term thiazides lower _______ _______ _______

A

peripheral vascular resistance

46
Q

loop diuretics can be used _____ line monotherapy for HTN

a. first
b. second

A

b. second

47
Q

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

A

false (bc they are weak and associated with hyperkalemia)

48
Q

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

A

c, d, f

PHRM 844 Therapeutics (28 decks)

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