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D&T3 Test 1 > Vasodilators/Angiotensin system inhibitors > Flashcards

Vasodilators/Angiotensin system inhibitors Flashcards

1
Q

What are 2 classes of Ca-Channel blockers?

A
  1. Dihydropyridines (DHPs)

2. non- dihydropryridines

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2
Q

name drugs that are dihydropyrdines (DHP)

A

Amlodipine

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3
Q

name drugs that are non-dihydropyridines

A

Diltiazem

Verapamil

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4
Q

MOA for Ca-channel blockers

A
  • decrease Ca influx through L-type Ca-channels
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5
Q

Ca- channel blockers have their major effects on what sytsems

A

blood vessels

heart

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6
Q

what are calcium channel blockers vascular effects

A
  1. decrease [Ca] in cell, decrease contractile elements, vasodilation ( arteries )
  2. decrease TPR, decrease BP
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7
Q

what class of calcium channel blocker drugs have a better impact on the vascular system

A

dihydropryridines better than non-dihydropryridines

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8
Q

What ca-channel blockers are best for use on the heart

A

Verapamil greater than Diltiazem

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9
Q

how do ca-channel blockers work compared to the ventricular and atrial action potential

A
  • inhibits phase 2 (plateau): decreases calcium entry, decreases sarcoplasmic Ca release , decreases contractility
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10
Q

how do ca-channel blockers depolarize in SA and AV nodes

A

inhibit phase 0:

  1. decrease firing rate of Sa node, decreases heart rate
  2. decreases conduction velocity in AV node, AV block
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11
Q

Which Ca-channel blocker is the best vasodilator

A

DHPs

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12
Q

Which Ca-chennel blocker is the best at reducing heart rate, worst?

A

best: Verapamil
worse: DHP

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13
Q

Which Ca-chennel blocker is the best at reducing cardiac contractility, worst?

A

best: Verapamil
worse: DHP

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14
Q

Which Ca-chennel blocker decreases AV nodal conduction

A

Verapamil

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15
Q

pharmacokinetics for Ca-channel blockers

A
  • hepatic metabolism

- effective orally

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16
Q

What are 3 therapeutic uses for Ca-channel blockers

A
  1. chronic stable and variable angina
  2. supraventricular tachyarrhythmias - verapamil
  3. hypertension
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17
Q

how do ca-channel blocker help with angina? specify which drugs

A
  1. increase coronary blood flow, all
  2. systemic artial vasodilation, decreases afterload, decreases O2 demand, all
  3. Verapamil and Diltiazem: decrease heart rate and contractilty
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18
Q

how do Ca-channels blockers help with supraventricular tachyarrhythmias and which drug does this

A

Verapamil

  • decrease AV nodal conduction
    • control V rate in A flutter and A fib
    • terminates paroxysmal supraventricular tachycardia
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19
Q

How do Ca-channel blocker drugs help with hypertension and which drugs are used

A
  1. all decrease TPR

2. verapamil and Diltiazem decreased cardiac output

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20
Q

what are adverse effects, contraindicationa of Ca-channel blockers and which drug has the most impact on each side effect

A
  • increase mortality and risk MI with short acting DHPs
  • hypotension, DHP
  • CHF , Verapmil
  • AV block , Verapmail
  • hypotension , all
  • severe hepatic disease, all
  • LV dysfunction, Verapamil
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21
Q

drug interactions with Ca-channel blockers

A
  • CYP3A4 inhibitors/induces
  • concurrent Beta-blockers ( Verpamil, Diltiazem)
  • Digoxin ( verpamil )
  • antiarrhythmic drugs
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22
Q

MOA for K-channel openers

A
  • increase K efflux from vascular smooth muscle
  • hyperpolarization
  • relaxation
  • decrease TPR
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23
Q

Name K-channel opener drugs

A

Minoxidil

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24
Q

What are the effects of Minoxidil

A

potent arterial vasodilator

  • decrease TPR,
  • increase HR, CO, fluid retention
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25
Q

Therapeutic uses of Minoxidil

A
  • Hypertension refractory

- promote hair growth to treat baldness

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26
Q

What are adverse effects of Minoxidil

A
  1. fluid retention with loop diuretic use
  2. tachycardia with beta blocker use
  3. hypertrichosis (abnormal hair growth)
  4. pericardial effusion/cardiac tamponade
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27
Q

What is the mechanism of action for Guanylyl cyclase activators

A
  • increase guanylyl cyclase
  • increase cGMP
  • vasodilation, vascular smooth muscle relaxation
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28
Q

Name Guanylyl Cyclase activators

A

Sodium Nitroprusside
Organic nitrates
Hydralazine
Nitric Oxide

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29
Q

what are the effects of Sodium Nitroprusside

A
  1. arteriodilation = venodilation
    - arteriodilation: decreases TPR, BP, reflex increase HR
    - venodilation: decrease LVEDV, CO, BP, reflex increase HR
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30
Q

what are the kinetics of sodium nitroprusside? expalin why

A

IV infusion only because of short half life

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31
Q

What are therapeutic uses for Sodium Nitroprusside

A
  • hypertensive crisis
  • acute CHF
  • MI
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32
Q

What are adverse effects of Sodium Nitroprusside

A
  • acute - excessive hypotension

- chronic (days)- thiocyanate and/or cyanide toxicity

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33
Q

how does cyanide or thiocyanate toxicity occur?

A
  • CN- and Thiosulfate makes thiocyanate, catalyzed by rhodanese in liver
34
Q

what happens when there is sufficient thiosulfate? insufficient?

A

Sufficient: thiocyanate toxicity: weakness, nausea, disorientation, delerium

insufficient: CN- toxicity: cytoxic anoxia, hypoxia, convulsions, respiratory arrest

35
Q

what are the 2 categories for organic nitrates

A

nitroglycerin

Isosorbide Dinitrate

36
Q

What vessels do organic nitrates work on

A

venodilation

37
Q

what are effects of organic nitrate at low doses

A
  • venodilation: decreases LVEDV, SV, CO
  • reflex to increase HR and TPR
  • No change to BP
38
Q

what are effects of organic nitrate at high doses

A
  • venodilation: decrease CO, BP
  • arteriodilation: decrease TPR, BP
  • reflex increase HR
39
Q

What are kinetics of organic nitrates

A
  • HM: extensive first pass metabolism
  • glutathione-organic nitrate reductase, denitration, decrease activity
  • IV, sublingual, and transdermal
40
Q

Therapeutic uses for organic nitrates

A
  • angina
  • CHF
  • acute MI
41
Q

Adverse effects of organic nitrates

A
  • excessive hypotension

- tolerance

42
Q

What are the kinetics of nitric oxide

A
  • inhalational

- short half life

43
Q

therapeutic uses of nitric oxide

A

-hypoxic respiratory failure in term/near-term neonates with associated pulmonary hypertension

44
Q

Adverse effects of nitric oxide

A
  • pulmonary edema

- hypoexmia upon sudden withdrawal

45
Q

What are the effects of Hydralazine

A
  • arterial vasodilation, decreases TPR, BP
46
Q

Therapeutic uses of Hydralazine

A

CHF

hypertension

47
Q

what are adverse effects of Hydralazine

A
  • fluid retention
  • tachycardia
  • +ANA, lupus like syndrome
48
Q

MOA for Fenoldopam

A
  • D1 receptor agonist
49
Q

what are the effects of Fenoldopam

A

peripheral vasodilation, decrease TPR, BP

50
Q

How is Fenoldopam administered

A

IV- rapidly acting, moderate duration

51
Q

therapeutic uses of Fenoldopam

A

hypertensive emergency

52
Q

adverse effects of Fenoldopam

A
  • hypersensitivity - sodium metabisulfite in formulation
  • tachycardia
  • hypotension
53
Q

Phosphodiesterase PDE inhibitors, name the drugs

A

Sildenafil

Tadalafil

54
Q

MOA for PDE inhibitors

A

inhibits PDE type 5, NO induced, increase cGMP, smooth muscle relaxation

55
Q

what are the effects of Sildenafil and Tadalafil

A
  • relaxation of smooth muscle in corpus cavernosum, erection

- relaxation of lower urinary tract smooth muscle facilities urination

56
Q

Therapeutic uses of PDE inhibitors

A
  • erectile dysfunction

- Tadalafil beneficial in Benign prostatic hypertrophy

57
Q

Kinetics for Sildenafil and Tadalafil

A

mainly hepatic metabolism

58
Q

Adverse effects of PDE inhibitors

A

hypotension

59
Q

Contraindication for Sildenafil and Tadalafil

A
  • concurrent organic nitrates
  • concurrent alpha-blockers
  • CYP3A4 interacting drugs
60
Q

ACEI MOA

A

inhibit ACE, decrease angiotension II, aldosterone

- inhibits metabolism of bradykinin

61
Q

ACEI block angiotension II which causes

A
  • vasoconstriction
  • facilitation of adrenergic mediated vasoconsrtiction
  • mediated CV remodeling
62
Q

ACEI decreases aldosterone secretion

A

sodium and water retention

63
Q

what are the effects of ACEI

A

decrease TPR, NA and fluid retenetion, blood pressure

64
Q

Name 2 drugs that are ACEI

A

Lisinopril

Enalapril

65
Q

Kinetics of ACEI

A

prodrugs

66
Q

Therapeutic uses of ACEI

A
  1. hypertension
  2. CHF
  3. post MI
  4. prevent diabetic nephropathy
67
Q

Adverse effects of ACEI

A
  • fetopathic potential
  • cough
  • hyperkalemia
  • hypotension
  • hypersensitivity - rashes
68
Q

contraindications of ACEI

A
  • pregnancy
  • K supplements
  • hypersensitivity
69
Q

Name 2 drugs that are angiotensin II receptor blockers

A

Losartan

Valsartan

70
Q

MOA of angiotensin II receptor blockers

A

competitive antagonist at AT1 receptors

71
Q

effects of Losartan and Valsartan

A

similar to ACE I

- less cough and angioedema

72
Q

therapeutic uses of Losartan and Valsartan

A
  • hypertension
  • CHF
  • post MI
  • prevent diabetic nephropathy
73
Q

Adverse effects of angiotensin II receptor blockers

A
  • fetopathic potential
  • hyperkalemia
  • hypotension
  • hypersensitivity - rashes
74
Q

contraindications of Losartan and Valsartan

A
  • pregnancy
  • bilateral renal vascular stenosis
  • K supplements
  • hypersensitivity
75
Q

Name a renin inhibitors

A

Aliskiren

76
Q

MOA for Aliskiren

A

inhibits renin, decreases ATI

77
Q

effects of Aliskiren

A
  • similar to ACEi

- less cough

78
Q

therapeutic uses of Aliskiren

A

hypertension

79
Q

adverse effects of Aliskiren

A
  • fetopathic potential
  • hyperkalemia
  • hypotension
  • hypersensitivity reactions
80
Q

contraindications of Aliskiren

A
  • pregnancy
  • bilateral renal vascular stenosis
  • K supplements, K-sparing diuretics
  • hypersensitivity

D&T3 Test 1 (11 decks)

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