Pharmacology - ACE inhibitors + ARBs Flashcards

1
Q

____ releases angiotensinogen

____ releases renin

what is the relationship between the 2?

A

liver produces angiotensinogen

kidney produces renin

renin is the enzyme that converts angiotensinogen into angiotensin I

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2
Q

what does aldosterone do

A

leads to sodium and water retention and decreased potassium

fluid retension causes increased BP

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3
Q

corticosteroids ____ the production of angiotensinogen

A

increase

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4
Q

renin is secreted in response to what 3 things

A

-decrease in arterial BP
-decreased sodium
-increased sympathetic NS activity

TO INCREASE BP BY CONVERTING ANGIOTENSINOGEN INTO ANGIOTENSIN 1

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5
Q

____ stimulates aldosterone secretion from the adrenal cortex

A

angiotensin II

causing increased BP

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6
Q

____ is a potent vasoconstrictor which leads to increased BP

A

angiotensin II

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7
Q

***ACE inhibitors reverse………

A

cardiac and vascular hypertrophy and remodeling

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8
Q

**______ reverse cardiac and vascular hypertrophy and remodeling

A

ACE inhibitors

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9
Q

3 bad effects of angiotensin II

A

high BP
myocardial infarction
renal damage

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10
Q

true or false

ACE inhibitors decrease peripheral resistance

A

TRUE

by blocking vasoconstriction caused by angiotensin II

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11
Q

***major side effect of ACE inhibitors

explain how it happens

A

COUGH

bc bradykinin and substance P breakdown is INHIBITED in the lungs

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12
Q

true or false

ARBS do not cause the side effect of cough seen in ACE inhibitors

A

true

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13
Q

what do ACE inhibitors do to potassium levels

A

increase potassium levels

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14
Q

**true or false

enalapril is a prodrug

A

TRUE

active form is enalaprilat

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15
Q

what is the advantage of enalapril over captopril

A

less side effects

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16
Q

***true or false

ramipril is not a prodrug

A

FALSE - it is

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17
Q

which ACE inhibitor is tissue specific and thus protective of the heart and kidney?

A

ramipril

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18
Q

***true or false

lisinopril is not a prodrug

A

TRUE - not a prodrug

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19
Q

**TRUE OR FALSE

fosinopril is not a prodrug

A

FALSE - it is

active form is fosinoprilat

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20
Q

***which medication has beneficial effects for patients with hypertension and left ventricular hypertrophy and why?

A

FOSINOPRIL

it produces adequate blood pressure reduction and reversal of the hypertrophy

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21
Q

true or false

ACE inhibitors are considered first line for hypertension

A

TRUE

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22
Q

true or false

ACE inhibitors do not cause hyperuricemia like diuretics do

A

true

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23
Q

explain the MOA of ARBs

A

they block the angiotensin II RECEPTOR (AT I receptor) and thus prevent angiotensin II from binding to it and exerting its effects of vasoconstriction

24
Q

what does angiotensin II do to urine output?

A

decreases urine output and decreased GFR

25
Q

where is the AT 1 receptor expressed

A

in the heart and blood vessels

26
Q

where is the ACE enzyme released from

A

the lungs

27
Q

through what kind of receptor do AT1 receptors work

A

the phospholipase C-IP3/DAG intracellular calcium type – Gq!!!!!

incresed calcium causes vasoconstriction and muscle contraction - thereby increasing BP when angiotensin II binds

28
Q

WHAT IS THE SPECIFIC AT1 BLOCKER

A

Losartan

29
Q

true or false

ARBS block AT2 more than AT1

A

FALSE - AT1 more than AT2

30
Q

**___ AND ___ were the first marketed blockers of the angiotensin II type 1 (AT1) receptor

A

losartan and valsartan

31
Q

explain the pharmacology of losartan

competiive?
agonist?
what receptor?

A

competitive antagonist and inverse agonist of the AT1 receptor

meaning it either binds and has NO EFFECT or binds and does the OPPOSITE EFFECT (vasodilation)

32
Q

true or false

losartan inhibits ACE

A

FALSE

33
Q

give 3 reasons why we need ARBs over ACE inhibitors

A

ARBS do not have the persistent cough side effect
(VERY rarely if they do)

completely inhibiting AT1

indirectly activate AT2 and cause vasodilation! additional benefit

34
Q

true or false

losartan can be used in pregnancy

A

FALSE

ACE inhibitors and ARBS are not safe in pregnancy

35
Q

true or false

valsartan is selective for AT1

A

TRUE

36
Q

true or false

valsartan is a noncompetitive inhibitor of angiotensin II

A

FALSE - competitive inhibitor

37
Q

___ causes the release of aldosterone from the adrenal cortex of the kidney

what is the effect of this

A

angiotensin II

causes water and sodium retention and thus increased BP

38
Q

name 2 side effects of valsartan

A

hypotension
dizziness

39
Q

name 2 side effects that are more common in ACE inhibitors than ARBS

A

angioedema
cough

40
Q

what do ARBS do to potassium levels

A

increased

41
Q

*****name an ARB that is metabolized by CYP3A4

A

losartan

42
Q

***name an ARB that is metabolized by CYP2C9

A

irbesartan

43
Q

name an ARB that has low liver metabolism

A

valsartan

44
Q

**true or false

candesartan is a prodrug

A

TRUE

activated in GI by esterases through hydrolysis

45
Q

**true or false

azilsartan is not a prodrug

A

FALSE - it is

46
Q

____ has an ability to remain tightly bound to ATI receptors for very long periods after drug washout

A

azilsartan

not good

47
Q

what CYP is azilsartan metabolized by

A

CYP2C9

48
Q

WHICH ARB HAS THE STRONGEST RECEPTOR BINDING AFFINITY IN THE ENTIRE CLASS???

A

TELMISARTAN

49
Q

which ARB has the longest half life and highest lipophilicity

A

telmisartan

50
Q

which ARB is good for patients with diabetes and why?

A

telmisartan

bc it can improve insulin sensitivity and help with hypertension

additive PPARy agonistic action

51
Q

true or false

ARBS can cause decreased potassium

A

FALSE increase

52
Q

what do ARBS do to lithium levels

A

increase - bc it follows potassium

53
Q

what class of drugs decreases the effect of ARBs

A

NSAIDS

bc they cause sodium retension

54
Q

recap - how do spironolactone and eplerenone decrease BP

A

bc they antagonize aldosterone

aldosterone would normally cause sodium and water retention and thus increase BP

55
Q
A