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Therapeutics 2 - Exam 5 > ? > Flashcards

? Flashcards

1
Q

what is aliskiren?

A

anti HTN medication that prevents conversion of angiotensinogen to angiotensin I
nonpeptidic direct inhibitor of renin –> decreases the formation of angiotensin I from angiotensinogen

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2
Q

what is renin?

A

aspartic acid protease that converts angiotensinogen to angiotensin I

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3
Q

what is ACE?

A

angiotensin converting enzyme
metallo dipeptidase that converts angiotension I to angiotensin II

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4
Q

what is angiotensinogen?

A

60 kD glycoprotein circulating in the plasma

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5
Q

what is angiotensin I?

A

inactive decapeptide precursor to angiotensin II

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6
Q

what is angiotensin II?

A

octapeptide responsible for pressor, sodium, and fluid retention response

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7
Q

what is the effect of ACE?

A

inactivates bradykinin
vasodilator

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8
Q

what do angiotensin II receptors activate?

A

the AT1-subtype

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9
Q

what happens in the degradation of angiotensinogen?

A

angiotensinogen to angiotensin I via renin to angiotensin II via ACE-1 to angiotensin III via aminopeptidase A to angiotensin IV via aminopeptidase N

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10
Q

what is the indication of aliskiren?

A

HTN (not first line)
helps reduce renin to reduce BP

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11
Q

what is the CI of aliskiren?

A

pregnancy and breastfeeding

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12
Q

how does beta-1 receptor blockers act on juxtaglomerular cells?

A

inhibit the release of renin due to interaction with receptors in the kidney

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13
Q

what drugs are sulfhydryl-containing ACE inhibitors and structurally related to captopril?

A

fentiapril
pivalopril
zofenopril
alacepril

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14
Q

what drugs are dicarboxyl-containing ACE inhibitors and structurally similar to enalapril?

A

lisinopril
benazepril
quinapril
moexipril
ramipril
trandolapril
perindopril
spirapril
pentopril
cilazapril

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15
Q

what drugs are phosphorus containing ACE inhibitors?

A

fosinopril sodium

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16
Q

what is lisinopril?

A

prinivil, zestril
dicarboxyl containing ACEi that is well-tolerated
not a prodrug

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17
Q

what is the half life of lisinopril?

A

12 hours

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18
Q

what is enalapril?

A

vasotec
dicarboxyl containing ACEi and prodrug that is hydrolyzed to active diacid enalaprilat (IV)

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19
Q

what is quinapril?

A

accupril
dicarboxyl containing ACE inhibitor and prodrug

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20
Q

what is captopril?

A

sulfonhydryl containing ACE i that contains a thiol and is not a prodrug

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21
Q

what is the indication of captopril?

A

supine HTN-orthostatic hypotension

22
Q

what is the half life of captopril?

A

under 3 hours

23
Q

what is the SE of captopril?

A

rash
neutropenia
agranulocytosis

24
Q

what is fosinopril sodium?

A

monopril
phosphorous containing ACei that is a prodrug and cascade ester

25
Q

what are the actions of ACEi?

A

reduce vasoconstriction due to angiotensin II
reduce myocardial activity
decrease myocardiac hypertrophy and remodeling
reduce sodium and water retention caused by aldosterone release
reduce TPR

26
Q

what is the indication of ACEi?

A

first line monotherapy for HTN
HF
particularly useful in white people, those with HF, CKD, diabetes, and ischemic heart failure (not AA)

27
Q

what is the problem with ACEi?

A

cough
angioedema of lips and tongue from bradykinin accumulation (higher risk in AA)
hyperkalemia from less aldosterone production
reduced effectiveness via NSAIDs

28
Q

what is the CI of ACEi?

A

pregnancy (fetal hypotension, renal failure, mortality)
stop use if renal artery stenosis if GFR drops by over 30%

29
Q

where is angiotensin II receptor blockers excreted?

A

in the feces

30
Q

how are ARBs administered?

A

oral

31
Q

what is the action of ARBs?

A

block angiotensin II receptors with much higher affinity for AT1 receptor than AT2 receptors

32
Q

what is the potency of ARBs?

A

candesartan and olmesartan then irbesartan and eprosartan then telmisartan and valsartan and exp 3174 then losartan

33
Q

what is prototypical ARB?

A

losartan

34
Q

what is the affect of ARBs?

A

reduce angiotensin II mediated vasoconstriction
peripheral resistance
afterload
aldosterone secretion
salt and water retention
preload
SNS activity from angiotensin II stimulation
renin release
myocardial and vascular remodeling
cardiomyocyte apoptosis
TPR

35
Q

what is the indication of ARBs?

A

first line monotherapy for HTN

36
Q

what is the AE of ARBs?

A

hypotension
high K
lower rate of angioedema (but still may occur)
fetal pathologies
reduced GFR

37
Q

why do ARBs not have a cough associated?

A

they dont inhibit the breakdown of bradykinin like ACEi do

38
Q

what populations benefit from ARBs?

A

diabetes (comapred to thiazides)
ischemic heart disease (compared to direct vasodilators)
CKD (diminish proteinuria and stabalize renal function)
not AA

39
Q

what drugs are aldosterone antagonists?

A

sprinolactone and eplerenone

40
Q

what is MOA of aldosterone antagonists?

A

block reabsorption of sodium to mildly reduce BP

41
Q

why are aldosterone antagonists useful in HF?

A

increase the production of aldosterone –> promotes development of cardiac hypertrophy, remodeling, and fibrosis
also maintains normal K levels –> reduces the risk of arrhythmias

42
Q

what is the clinical uses of aldosterone antagonists?

A

chronic HF (reduced mortality)
aldosteronism
HTN (not monotherapy, but used to reduce hypokalemia)

43
Q

what are the AE of aldosterone antagonists?

A

high K

44
Q

what is the SE of spironolactone?

A

gynecomastia and impotence (due to anti-androgen effects and lack of receptor specificity)

45
Q

what is the action of thiazides?

A

diuretics that block the NaCL symporter on the DCt to initiatlly reduce blood volume and CO

46
Q

what are the long-term effects of thiazide?

A

lower peripheral vascular resistance

47
Q

what drugs are thiazides?

A

chlorothalidone
HCTZ

48
Q

what populations benefit from thiazides?

A

AA

49
Q

what is the problem with thiazides?

A

low K
metabolic alkalosis
hyperuricemia
high Ca
hyperglycemia
hyperlipidemia

50
Q

what diuretics are not recommend as first line monotherapy?

A

loop (due to short acting/higher risk of SE)
K-sparing (weak and associated with hyperkalemia)

51
Q

what HTN drugs are used in pregnancy?

A

methyldopa
labetolol
metoprolol

52
Q

what HTN drugs should be avoided in pregnancy?

A

ACEi
ARBs
direct renin inhibitors
aldosterone receptor antagonists

Therapeutics 2 - Exam 5 (14 decks)

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