Pharmacology - ACE inhibitors + ARBs

Question 1

____ releases angiotensinogen

____ releases renin

what is the relationship between the 2?

Answer 1

liver produces angiotensinogen

kidney produces renin

renin is the enzyme that converts angiotensinogen into angiotensin I

Question 2

what does aldosterone do

Answer 2

leads to sodium and water retention and decreased potassium

fluid retension causes increased BP

Question 3

corticosteroids ____ the production of angiotensinogen

Answer 3

increase

Question 4

renin is secreted in response to what 3 things

Answer 4

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

TO INCREASE BP BY CONVERTING ANGIOTENSINOGEN INTO ANGIOTENSIN 1

Question 5

____ stimulates aldosterone secretion from the adrenal cortex

Answer 5

angiotensin II

causing increased BP

Question 6

____ is a potent vasoconstrictor which leads to increased BP

Answer 6

angiotensin II

Question 7

***ACE inhibitors reverse………

Answer 7

cardiac and vascular hypertrophy and remodeling

Question 8

**______ reverse cardiac and vascular hypertrophy and remodeling

Answer 8

ACE inhibitors

Question 9

3 bad effects of angiotensin II

Answer 9

high BP
myocardial infarction
renal damage

Question 10

true or false

ACE inhibitors decrease peripheral resistance

Answer 10

TRUE

by blocking vasoconstriction caused by angiotensin II

Question 11

***major side effect of ACE inhibitors

explain how it happens

Answer 11

COUGH

bc bradykinin and substance P breakdown is INHIBITED in the lungs

Question 12

true or false

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

Answer 12

true

Question 13

what do ACE inhibitors do to potassium levels

Answer 13

increase potassium levels

Question 14

**true or false

enalapril is a prodrug

Answer 14

TRUE

active form is enalaprilat

Question 15

what is the advantage of enalapril over captopril

Answer 15

less side effects

Question 16

***true or false

ramipril is not a prodrug

Answer 16

FALSE - it is

Question 17

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

Answer 17

ramipril

Question 18

***true or false

lisinopril is not a prodrug

Answer 18

TRUE - not a prodrug

Question 19

**TRUE OR FALSE

fosinopril is not a prodrug

Answer 19

FALSE - it is

active form is fosinoprilat

Question 20

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

Answer 20

FOSINOPRIL

it produces adequate blood pressure reduction and reversal of the hypertrophy

Question 21

true or false

ACE inhibitors are considered first line for hypertension

Answer 21

TRUE

Question 22

true or false

ACE inhibitors do not cause hyperuricemia like diuretics do

Answer 22

true

Question 23

explain the MOA of ARBs

Answer 23

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

Question 24

what does angiotensin II do to urine output?

Answer 24

decreases urine output and decreased GFR

Question 25

where is the AT 1 receptor expressed

Answer 25

in the heart and blood vessels

Question 26

where is the ACE enzyme released from

Answer 26

the lungs

Question 27

through what kind of receptor do AT1 receptors work

Answer 27

the phospholipase C-IP3/DAG intracellular calcium type -- Gq!!!!! incresed calcium causes vasoconstriction and muscle contraction - thereby increasing BP when angiotensin II binds

Question 28

WHAT IS THE SPECIFIC AT1 BLOCKER

Answer 28

Losartan

Question 29

true or false ARBS block AT2 more than AT1

Answer 29

FALSE - AT1 more than AT2

Question 30

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

Answer 30

losartan and valsartan

Question 31

explain the pharmacology of losartan competiive? agonist? what receptor?

Answer 31

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)

Question 32

true or false losartan inhibits ACE

Answer 32

FALSE

Question 33

give 3 reasons why we need ARBs over ACE inhibitors

Answer 33

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

Question 34

true or false losartan can be used in pregnancy

Answer 34

FALSE ACE inhibitors and ARBS are not safe in pregnancy

Question 35

true or false valsartan is selective for AT1

Answer 35

TRUE

Question 36

true or false valsartan is a noncompetitive inhibitor of angiotensin II

Answer 36

FALSE - competitive inhibitor

Question 37

___ causes the release of aldosterone from the adrenal cortex of the kidney what is the effect of this

Answer 37

angiotensin II causes water and sodium retention and thus increased BP

Question 38

name 2 side effects of valsartan

Answer 38

hypotension dizziness

Question 39

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

Answer 39

angioedema cough

Question 40

what do ARBS do to potassium levels

Answer 40

increased

Question 41

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

Answer 41

losartan

Question 42

***name an ARB that is metabolized by CYP2C9

Answer 42

irbesartan

Question 43

name an ARB that has low liver metabolism

Answer 43

valsartan

Question 44

**true or false candesartan is a prodrug

Answer 44

TRUE activated in GI by esterases through hydrolysis

Question 45

**true or false azilsartan is not a prodrug

Answer 45

FALSE - it is

Question 46

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

Answer 46

azilsartan not good

Question 47

what CYP is azilsartan metabolized by

Answer 47

CYP2C9

Question 48

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

Answer 48

TELMISARTAN

Question 49

which ARB has the longest half life and highest lipophilicity

Answer 49

telmisartan

Question 50

which ARB is good for patients with diabetes and why?

Answer 50

telmisartan bc it can improve insulin sensitivity and help with hypertension additive PPARy agonistic action

Question 51

true or false ARBS can cause decreased potassium

Answer 51

FALSE increase

Question 52

what do ARBS do to lithium levels

Answer 52

increase - bc it follows potassium

Question 53

what class of drugs decreases the effect of ARBs

Answer 53

NSAIDS bc they cause sodium retension

Question 54

recap - how do spironolactone and eplerenone decrease BP

Answer 54

bc they antagonize aldosterone aldosterone would normally cause sodium and water retention and thus increase BP