Vasodilators/Angiotensin system inhibitors Flashcards
1
Q
What are 2 classes of Ca-Channel blockers?
A
- Dihydropyridines (DHPs)
2. non- dihydropryridines
2
Q
name drugs that are dihydropyrdines (DHP)
A
Amlodipine
3
Q
name drugs that are non-dihydropyridines
A
Diltiazem
Verapamil
4
Q
MOA for Ca-channel blockers
A
- decrease Ca influx through L-type Ca-channels
5
Q
Ca- channel blockers have their major effects on what sytsems
A
blood vessels
heart
6
Q
what are calcium channel blockers vascular effects
A
- decrease [Ca] in cell, decrease contractile elements, vasodilation ( arteries )
- decrease TPR, decrease BP
7
Q
what class of calcium channel blocker drugs have a better impact on the vascular system
A
dihydropryridines better than non-dihydropryridines
8
Q
What ca-channel blockers are best for use on the heart
A
Verapamil greater than Diltiazem
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
10
Q
how do ca-channel blockers depolarize in SA and AV nodes
A
inhibit phase 0:
- decrease firing rate of Sa node, decreases heart rate
- decreases conduction velocity in AV node, AV block
11
Q
Which Ca-channel blocker is the best vasodilator
A
DHPs
12
Q
Which Ca-chennel blocker is the best at reducing heart rate, worst?
A
best: Verapamil
worse: DHP
13
Q
Which Ca-chennel blocker is the best at reducing cardiac contractility, worst?
A
best: Verapamil
worse: DHP
14
Q
Which Ca-chennel blocker decreases AV nodal conduction
A
Verapamil
15
Q
pharmacokinetics for Ca-channel blockers
A
- hepatic metabolism
- effective orally
16
Q
What are 3 therapeutic uses for Ca-channel blockers
A
- chronic stable and variable angina
- supraventricular tachyarrhythmias - verapamil
- hypertension
17
Q
how do ca-channel blocker help with angina? specify which drugs
A
- increase coronary blood flow, all
- systemic artial vasodilation, decreases afterload, decreases O2 demand, all
- Verapamil and Diltiazem: decrease heart rate and contractilty
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
19
Q
How do Ca-channel blocker drugs help with hypertension and which drugs are used
A
- all decrease TPR
2. verapamil and Diltiazem decreased cardiac output
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
21
Q
drug interactions with Ca-channel blockers
A
- CYP3A4 inhibitors/induces
- concurrent Beta-blockers ( Verpamil, Diltiazem)
- Digoxin ( verpamil )
- antiarrhythmic drugs
22
Q
MOA for K-channel openers
A
- increase K efflux from vascular smooth muscle
- hyperpolarization
- relaxation
- decrease TPR
23
Q
Name K-channel opener drugs
A
Minoxidil
24
Q
What are the effects of Minoxidil
A
potent arterial vasodilator
- decrease TPR,
- increase HR, CO, fluid retention
25
Therapeutic uses of Minoxidil
- Hypertension refractory
| - promote hair growth to treat baldness
26
What are adverse effects of Minoxidil
1. fluid retention with loop diuretic use
2. tachycardia with beta blocker use
3. hypertrichosis (abnormal hair growth)
4. pericardial effusion/cardiac tamponade
27
What is the mechanism of action for Guanylyl cyclase activators
- increase guanylyl cyclase
- increase cGMP
- vasodilation, vascular smooth muscle relaxation
28
Name Guanylyl Cyclase activators
Sodium Nitroprusside
Organic nitrates
Hydralazine
Nitric Oxide
29
what are the effects of Sodium Nitroprusside
1. arteriodilation = venodilation
- arteriodilation: decreases TPR, BP, reflex increase HR
- venodilation: decrease LVEDV, CO, BP, reflex increase HR
30
what are the kinetics of sodium nitroprusside? expalin why
IV infusion only because of short half life
31
What are therapeutic uses for Sodium Nitroprusside
- hypertensive crisis
- acute CHF
- MI
32
What are adverse effects of Sodium Nitroprusside
- acute - excessive hypotension
| - chronic (days)- thiocyanate and/or cyanide toxicity
33
how does cyanide or thiocyanate toxicity occur?
- CN- and Thiosulfate makes thiocyanate, catalyzed by rhodanese in liver
34
what happens when there is sufficient thiosulfate? insufficient?
Sufficient: thiocyanate toxicity: weakness, nausea, disorientation, delerium
insufficient: CN- toxicity: cytoxic anoxia, hypoxia, convulsions, respiratory arrest
35
what are the 2 categories for organic nitrates
nitroglycerin
| Isosorbide Dinitrate
36
What vessels do organic nitrates work on
venodilation
37
what are effects of organic nitrate at low doses
- venodilation: decreases LVEDV, SV, CO
- reflex to increase HR and TPR
- No change to BP
38
what are effects of organic nitrate at high doses
- venodilation: decrease CO, BP
- arteriodilation: decrease TPR, BP
- reflex increase HR
39
What are kinetics of organic nitrates
- HM: extensive first pass metabolism
- glutathione-organic nitrate reductase, denitration, decrease activity
- IV, sublingual, and transdermal
40
Therapeutic uses for organic nitrates
- angina
- CHF
- acute MI
41
Adverse effects of organic nitrates
- excessive hypotension
| - tolerance
42
What are the kinetics of nitric oxide
- inhalational
| - short half life
43
therapeutic uses of nitric oxide
-hypoxic respiratory failure in term/near-term neonates with associated pulmonary hypertension
44
Adverse effects of nitric oxide
- pulmonary edema
| - hypoexmia upon sudden withdrawal
45
What are the effects of Hydralazine
- arterial vasodilation, decreases TPR, BP
46
Therapeutic uses of Hydralazine
CHF
| hypertension
47
what are adverse effects of Hydralazine
- fluid retention
- tachycardia
- +ANA, lupus like syndrome
48
MOA for Fenoldopam
- D1 receptor agonist
49
what are the effects of Fenoldopam
peripheral vasodilation, decrease TPR, BP
50
How is Fenoldopam administered
IV- rapidly acting, moderate duration
51
therapeutic uses of Fenoldopam
hypertensive emergency
52
adverse effects of Fenoldopam
- hypersensitivity - sodium metabisulfite in formulation
- tachycardia
- hypotension
53
Phosphodiesterase PDE inhibitors, name the drugs
Sildenafil
| Tadalafil
54
MOA for PDE inhibitors
inhibits PDE type 5, NO induced, increase cGMP, smooth muscle relaxation
55
what are the effects of Sildenafil and Tadalafil
- relaxation of smooth muscle in corpus cavernosum, erection
| - relaxation of lower urinary tract smooth muscle facilities urination
56
Therapeutic uses of PDE inhibitors
- erectile dysfunction
| - Tadalafil beneficial in Benign prostatic hypertrophy
57
Kinetics for Sildenafil and Tadalafil
mainly hepatic metabolism
58
Adverse effects of PDE inhibitors
hypotension
59
Contraindication for Sildenafil and Tadalafil
- concurrent organic nitrates
- concurrent alpha-blockers
- CYP3A4 interacting drugs
60
ACEI MOA
inhibit ACE, decrease angiotension II, aldosterone
| - inhibits metabolism of bradykinin
61
ACEI block angiotension II which causes
- vasoconstriction
- facilitation of adrenergic mediated vasoconsrtiction
- mediated CV remodeling
62
ACEI decreases aldosterone secretion
sodium and water retention
63
what are the effects of ACEI
decrease TPR, NA and fluid retenetion, blood pressure
64
Name 2 drugs that are ACEI
Lisinopril
| Enalapril
65
Kinetics of ACEI
prodrugs
66
Therapeutic uses of ACEI
1. hypertension
2. CHF
3. post MI
4. prevent diabetic nephropathy
67
Adverse effects of ACEI
- fetopathic potential
- cough
- hyperkalemia
- hypotension
- hypersensitivity - rashes
68
contraindications of ACEI
- pregnancy
- K supplements
- hypersensitivity
69
Name 2 drugs that are angiotensin II receptor blockers
Losartan
| Valsartan
70
MOA of angiotensin II receptor blockers
competitive antagonist at AT1 receptors
71
effects of Losartan and Valsartan
similar to ACE I
| - less cough and angioedema
72
therapeutic uses of Losartan and Valsartan
- hypertension
- CHF
- post MI
- prevent diabetic nephropathy
73
Adverse effects of angiotensin II receptor blockers
- fetopathic potential
- hyperkalemia
- hypotension
- hypersensitivity - rashes
74
contraindications of Losartan and Valsartan
- pregnancy
- bilateral renal vascular stenosis
- K supplements
- hypersensitivity
75
Name a renin inhibitors
Aliskiren
76
MOA for Aliskiren
inhibits renin, decreases ATI
77
effects of Aliskiren
- similar to ACEi
| - less cough
78
therapeutic uses of Aliskiren
hypertension
79
adverse effects of Aliskiren
- fetopathic potential
- hyperkalemia
- hypotension
- hypersensitivity reactions
80
contraindications of Aliskiren
- pregnancy
- bilateral renal vascular stenosis
- K supplements, K-sparing diuretics
- hypersensitivity
