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Cardio II > Pharm-angiotensins > Flashcards

Pharm-angiotensins Flashcards

1
Q

Potent renin inhibitor
Orally active
Low bioavailability
Half life?

A

Aliskiren

>24 hrs

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2
Q

MOA:

Aliskiren

A

Suppression of plasma renin activity, thus decreasing levels of Ang I and II

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3
Q

Uses:

Aliskiren

A

HTN, but not 1st line

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4
Q

Contraindications:

Aliskiren

A

Pregnancy

Bilateral renal artery stenosis

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5
Q

MOA:
ACEI
Consequences?

A

Inhibition of the conversion of Ang I to Ang II

  • decrease in aldosterone
  • renal retention of Na, but K increases
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6
Q

What is “aldosterone escape”?

A

Due to ACEI, aldosterone levels decrease, but can then increase over time

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7
Q

Beneficial effects of ACEI

A
  • Lower BP by decreasing PVR
  • Improve arterial compliance
  • decrease afterload
  • decrease preload through venodilation
  • improve renal perfusion
  • improve insulin sensitivity and glucose metabolism
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8
Q

Examples of ACEI

A

-prils

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9
Q

ACEI:

Prodrugs

A

Enalapril
Fosinopril
Ramipril

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10
Q

ACEI:

Non prodrugs

A

Captopril

Lisinopril

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11
Q

Clinical uses for ACEI

A 
HTN 
HF
Acute MI
Chronic renal failure 
Reduce adverse cardiovascular events
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12
Q

Contraindications:

ACEI

A

Pregnancy

Bilateral renal a. stenosis

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13
Q

Adverse effects:

ACEI

A 
Hyperkalemia
Hypotension
Renal function impairment 
Dry cough
Angioedema
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14
Q

Drug interactions:

ACEI

A

NSAIDs

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15
Q

MOA:

ARB

A

AT1 receptor blockers (NOT AT2)

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16
Q

Examples:

ARB

A

-sartans

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17
Q

Orally active ARB
Extensive first pass metabolism
Has an active metabolite with a longer half life than the parent compound

A

Losartan

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18
Q

True or false:

ARBs cross the BBB

A

False

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19
Q

Clinical uses:

ARB

A

Similar to ACEI for pts who can’t tolerate ACEI

20
Q

Contraindications:

ARB

A

Same as ACEI (so avoid combo)

21
Q

Adverse effects:

ARB

A

Similar to ACEI except no dry cough

22
Q

Examples of Kallikrein inhibitors

A

Aprotinin

Ecallantide

23
Q

MOA

Kallikrein inhibitors

A

Inhibit synthesis of kinins

24
Q

How do ACEI affect the kallikrein-kinin system?

A

They prolong the actions of bradykinin by inhibiting its degradation

25
Q

___ is a bradykinin B2 receptor antagonist that reduces vascular permeability

A

Icatibant

26
Q

Clinical uses:

Icatibant

A

Hereditary angioedema

ACEI associated angioedema

27
Q

ET-1 has a biphasic effect on blood vessels:

A

Transient vasodilation followed by prolonged vasoconstriction

28
Q

Under normal physiologic conditions, what effect does ET1 have on the heart?

A

Positive inotropic and chronotropic

29
Q

ET1 causes ___ of airway smooth muscle

A

Contraction(bronchoconstriction)

30
Q

MOA:

Endothelin receptor antagonists

A

Block ET receptors thus relax vascular smooth muscle

31
Q

Examples:

ET receptor antagonists

A

-entans

32
Q
  1. Orally active, nonselective ETA/ETB receptor antagonists

2. Selective ETA receptor blocker

A
  1. Bosentan, macitentan

2. Ambrisentan

33
Q

Clinical uses:

ET antagonists

A

Pathological and physiological pulmonary arterial BP control

  • vasoconstriction
  • also relaxation through PGI2 and NO
34
Q

Adverse effects of ETA receptor antagonists

A 
Headache
Flushing
Peripheral edema
Palpitations
Elevated liver enzymes
35
Q

Contraindications:

ETA receptor antagonists

A

Pregnancy

36
Q

Examples of natriuretic peptides

A

Atrial and brain type
ANP
BNP

37
Q

___ is a recombinant of human BNP. It relaxes arteries and veins and promotes diuresis and natriuresis, leading to reduced cardiac workload. What else does it do?

A

Nesiritide
Decrease remodeling
Lower BP

38
Q

Clinical uses:

Nesiritide

A

Acute decompensated congestive HF, given IV

39
Q

___ is a neprolysin inhibitor

A

Sacubitril (prodrugs activated to LBQ657 by esterases)

40
Q

MOA:

Sacubitril

A

Inhibits neprilysin, which is responsible for the degradation of ANP and BNP
-also increases Ang II levels which may counteract the effects listed above. SO it must be COMBINED with AT1 receptor blocker in treating chronic HF

41
Q

LCZ696 (entresto) =

A

Sacubitril + valsartan

42
Q

Clinical uses:

LCZ696

A

Chronic HF in pts with reduced EF (CHFrEF)

43
Q

MOA:

LCZ696

A

Enhance effects of ANP and BNP

Block Ang II

44
Q

Adverse effects:

LCZ696

A

Hypotension
Hyperkalemia
Renal impairment
Angioedema (rare but severe)

45
Q

Contraindications:

LCZ696

A

Hx of angioedema

Use of ACEI, ARB, or aliskiren

Cardio II (16 decks)

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