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Flashcards in CARDIOVASCULAR- Pharmacology Deck (153):
1

Drugs used for Primary (essential) hypertension

Diuretics, ACE inhibitors, angiotensin II recetor blockers (ARBs), calcium channel blockers

2

For Hypertension with Cardiac Heart failure, which drugs are recommended?

Diuretics, ACE inhibitors/ ARBs, β blockers (compensated CHF), aldosterone antagonists

3

Which drugs must be used cautiously in decompensated CHF?

β blockers

4

When are β blockers contraindicated?

Cardiogenic shock

5

For patients with hypertension with Diabetes, which antihypertensive drugs are recommended?

ACE inhibitors/ ARBs. Calcium channel blockers, diuretics, β blockers, α blockers

6

Which antihypertensive drugs work as protective against diabetic nephropathy?

ACE inhibitors/ ARBs

7

Dihydropyridine Calcium channel blockers

Amlodipine, nimodipine, nifedipine

8

Non Dihydropyridine Calcium channel blockers

Diltiazem, Verapamil

9

Mechanism of action of Calcium channel blockers

Block voltage dependent L type calcium channels of cardiac and smooth muscle, thereby reduce muscle contractility

10

Which Calcium channel blockers have more effect in vascular smooth muscle?

Amlodipine= nifedipine> diltiazem> verapamil

11

Which Calcium channel blockers have more effect in heart?

Verapamil> diltiazem> amlodipine= nifedipine

12

Clinical use for Dihydropyridine Calcium channel blockers

(Except nimodipine)
Hypertension, angina (including prinzmetal), Raynaud phenomenom

13

Clinical use for Non Dihydropyridine Calcium channel blockers

Hypertension, angina, atrial fibrilation/ flutter

14

Clinical use for Nimodipine

Subarachnoid hemorrhage (prevents cerebral vasospasm)

15

These are Toxic effects of Calcium channel blockers

Cardiac depression, AV block, peripheral edema, flushing, dizziness, hyperprolactinemia, and constipation

16

Mechanism of Action of Hydralazine

↑ cGMP→ smooth muscle relaxation
Vasodilates arterioles> vein

17

Which effect does Hydralazine has?

Afterload reduction

18

Clinical use for Hydralazine

Severe hypertension, CHF
First line therapy for hypertension in pregnancy

19

First line therapy for hypertension in pregnancy

Metildopa
Hydralazine

20

Which drug is coadministered with hydralazine to prevent reflex tachycardia?

β blockers

21

Why are β blockers coadministered with hydralazine?

To prevent reflex tachycardia

22

Toxic effects of Hydralazine?

Compensatory tachycardia, fluid retention, nausea, headache, angina
Lupus like syndrome

23

When is Hydralazine contraindicated?

In angina/ Coronary artery disease

24

In hypertensive emergency which are the common used drugs?

Nitroprusside, nicardipine, clevidipine, labetalol, fenoldopam

25

How long does it takes for Nitroprusside to act?

Short acting

26

Which is the mechanism of action of Nitroprusside

↑ cGMP via direct release NO

27

Possible secondary effect of Nitroprusside

Can cause cyanide toxicity (releases cyanide)

28

Mechanism of Action of Fenoldopam

Dopamine D1 receptor agonist

29

Effect of Fenoldopam

Coronary, peripheral, renal, and splanchic vasodilation

30

Clinical effect of Fenoldopam

↓ BP
↑ natriuresis

31

Which is the mechanism of action of Nitroglycerin, isosorbide dinitrate?

Vasodilate by ↑ NO in vascular smooth muscle→ ↑ in cGMP and smooth muscle relaxation.

32

Which vessels are more dilated with Nitroglycerin, isosorbide dinitrate?

Dilates veins >> arteries

33

What is the effect of Nitroglycerin, isosorbide dinitrate?

↓ preload

34

Clinical use for Nitroglycerin, isosorbide dinitrate

Angina, acute coronary syndrome, pulmonary edema

35

Toxic effect of Nitroglycerin, isosorbide dinitrate

Reflex tachycardia, hypotension, flushing, headache, "Monday disease" in industrial exposure

36

Which drug helps with the reflex tachycardia caused by Nitroglycerin, isosorbide dinitrate?

β blockers

37

What is the "Monday disease" ?

Development of tolerance for the vasodilating action during the work week and loss of tolerance over the weekend results in tachycardia, dizziness, and headache upon reexposure

38

Which is the goal in antianginal therapy?

Reduction of myocardial O2 consumption (MVO2) by ↓ 1 or more of the determinants of MVO2

39

Which are determinants of myocardial O2 consumption?

End diastolic volume
Blood pressure
Heart rate
Contractility

40

Which are the main medications in Antianginal therapy?

Nitrates
β Blockers
Nitrates + β blockers

41

What is affected with nitrates?

Preload

42

Which effects do Nitrates have as Antianginal therapy?

↓ End diastolic volume
↓ Blood pressure
↑ Contractility (reflex response)
↑ Heart rate (reflex response)
↓ Ejection time
↓ MVO2

43

Effects of β Blockers as Antianginal Therapy

↑ End diastolic volume
↓ Blood pressure
↓ Contractility
↓ Heart rate
↑ Ejection time
↓ MVO2

44

What effect do Nitrates + β blockers have as Antianginal Therapy?

No effect or ↓ End diastolic volume
↓ Blood pressure
Little/ no effect in Contractility
↓ Heart rate
Little/ no effect on Ejection time
↓↓ MVO2

45

Which calcium channel blocker has similar effects to nitrates in Antianginal therapy?

Nifedipine

46

Which drugs are contraindicated in Angina?

partial β agonists

47

Which partial β agonists are contraindicated in Angina?

Pindolol and Acetabutol

48

Lipid lowering agents

HMG- CoA reductase inhibitors
Niacin (vitamin B3)
Bile acid resins
Cholestherol absorption blockers
Fibrates

49

HMG-CoA reductase inhibitors

Lovastatin
Pravastatin
Simvastatin
Atorvastatin
Rosuvastatin

50

Which effects do HMG-CoA reductase inhibitors have?

↓↓↓ LDL
↑ HDL
↓ Tiglycerides

51

What is the mechanism of action of Pravastatin?

Inhibit conversion of HMG- CoA to mevalonate, a cholesterol precursor

52

Side effect of HMG-CoA reductase inhibitors

Hepatotoxicity (↑ LFTs), rhabdomyolisis

53

When do HMG-CoA reductase inhibitors have increased risk for rhabdomyolisis?

When used with fibrates and niacin

54

Effect of Niacin

↓↓ LDL
↑↑ HDL
↓ Tiglycerides

55

What vitamin is Niacin?

Vitamin B3

56

Which mechanism of action does Niacin has?

Inhibits lipolysis in adipose tissue, reduces hepatic VLDL synthesis

57

Possible side effects of Niacin

Red, flushed face
Hyperglycemia
Hyperuricemia

58

How do you decreased the probability of flushed face as a side effect of Niacin?

With aspirin or long term use

59

How is hyperglycemia manifested in Niacin administration?

Acanthosis nigricans

60

Which vitamin can exacerbate Gout?

Vitamin B3 (Niacin) because increases Hyperuricemia

61

Bile Acid Resins

Cholestyramine
Colestipol
Colesevelam

62

Effect of Bile Acid Resins

↓↓ LDL
Slightly ↑ HDL
Slightly ↑ Tiglycerides

63

Which is the mechanism of action of Bile acid resins?

Prevent intestinal reabsorption of bile acids; liver mistuse cholesterol to make more

64

What needs to be in mind before administering Bile acid resins?

Patients hate it- tastes bad and causes GI discomfort, ↓ absorption of fat soluble vitamins

65

Another side effect of Bile acid resins

Cholesterol gallstones

66

Cholesterol absorption blockers

Ezetimibe

67

What is the effect of Ezetimibe?

↓↓ LDL

68

Mechanism of action of Ezetimibe

Prevent cholesterol absorption at small intestine brush border

69

Side effect of Cholesterol absorption blockers

Rare ↑ LFTs, diarrhea

70

Name Fibrates

Gemfibrozil
Clofibrate
Bezafibrate
Fenofibrate

71

Effect of Fibrates

↓ LDL
↑ HDL
↓↓↓ Tiglycerides

72

Mechanism of action of Fibrates

Upregulate LPL → ↑ TG clearance
Activates PPAR α to induce HDL synthesis

73

Side effects of Fibrates

Myositis (↑ risk with concurretn statins)
Hepatotoxicity (↑ LFTs)
Cholesterol gallstones

74

When is increased the risk for Cholesterol gallstones when using fibrates?

With concurrent bile acid resins

75

Cardiac glycoside

Digoxin

76

How are the pharmacologic properties of Digoxin

75% bioaviailability
20-40 % protein bound
t1/2= 40 hours, urinary excretion

77

Mechanism of action of digoxin

Direct inhibition of Na+/ K+ ATPase leads to indirects inhibition of Na+/ Ca2+ exchanger/ antiport.
↑ Ca2+ intracellular →positive inotropy. Stimulates vagus nerve → ↓ Heart rate

78

Clinical use for Digoxin

CHF (↑ contractility)
Atrial Fibrilation

79

What effect does Digoxin has in Atrial Fibrilation?

↓ conduction at AV node and depression of SA node

80

Cholinergic side effects of Cardiac glycosides

Nausea, vomiting, diarhea, blurry yellow vision

81

ECG changes due to use of Digoxin

↑ PR, ↓ QT, ST scooping, T wave inversion, arrhytmia, AV block

82

Which electrolyte changes can Digoxin produce?

Hyperkalemia

83

What does Hyperkalemia caused by Cardiac glycosides indicate?

Poor prognosis

84

Which factros predispose to Digoxin toxicity?

Renal failure, hypokalemia, verapamil, amiodarone, quinidine

85

Why verapamil, amiodarone, quinidine increase the possibility of Digoxin toxicity?

↓ Digoxin clearance; displaces digoxin from tissue binding sites

86

Why does hypokalemia can increase the risk of toxic effects of Digoxin?

Permissive for digoxin binding at K+ binding site on Na+/ K+ ATPase

87

Antidote for Digoxin toxicity

Slowly normalize K+, cardiac pacer, anti digoxin Fab fragments, Mg2+

88

Class I Antiarrhytmics mechanism of Action

Na+ channel blockers

89

What effect do Class I Antiarrhytmics have?

Slow or Block (↓) conduction (especially in depolarized cells)
↓ slope of phase 0 depolarization and ↑ threshold for firing in abnormal pacemaker cells

90

Which is the dependant to use Class I Antiarrhytmics?

Are state dependent (selectively depress tissue that is frequently depolarized (eg. tachycardia))

91

Which state ↑ toxicity for all class I drug?

Hyperkalemia

92

How many classes of Antiarrythmics class I exist?

Class IA
Class IB
Class IC

93

Class IA Antiarrythmics

Quinidine
Procainamide
Disopyramide

94

Mechanism of Action of Class IA Antiarrythmics

↑ Action Potential duration, ↑ effective refractory period (ERP), ↑ QT interval

95

Clinical use for Class IA Antiarrythmics

Both atrial and ventricular arrythmias, especially re-entrant and ectopic Supraventricular tachycardia and VT

96

Toxic effect of Class IA Antiarrythmics

Thrombocytopenia
Torsades de pointes

97

What is cinchonism?

Headache
Tinnitus

98

Which Class IA Antiarrythmic causes cinchonism?

Quinidine

99

Class IA Antiarrythmics that can cause reversible SLE like syndrome

Procainamide

100

Class IA Antiarrythmic related to cause heart failure

Disopyramide

101

How Class IA Antiarrythmics can cause torsades de pointes?

Due to ↑ QT interval

102

Class IB Antiarrythmics

Lidocaine, Mexiletine

103

Class IB Antiarrythmics mechanism of Action

↓ Action Potential

104

Which tissue is preferentially affected with Class IB Antiarrythmics?

Ischemic or depolarized Purkinje and ventricular tissue

105

Another drug that can also fall into the Class IB Antiarrythmics

Phenytoin

106

Clinical use for Class IB Antiarrythmics

Acute ventricular arrhytmias (especially post MI)
Digitalis induced arrhytmias

107

Which Antiarrythmics are better for post MI?

Class IB Antiarrythmics

108

Toxic effects of Class IB Antiarrythmics

CNS stimulation/depression
Cardiovascular depression

109

Class IC Antiarrythmics

Flecainide
Propafenone

110

Which is the mechanism of action of Class IC Antiarrythmics?

Significantly prolongs refractory period in AV node
Minimal effect in Action potential duration

111

Clinical use for Class IC Antiarrythmics

Supraventricular Tachycardia, including atrial fibrilation

112

Antiarrythmics used as last resort in refractory Ventricular Tachycardia

Class IC Antiarrythmics

113

When are Class IC Antiarrythmics contraindicated?

post MI
Structural and ischemic heart disease

114

Toxic effect of Class IC Antiarrythmics

Proarrhytmic

115

Who are Antiarrhytmics class II?

β blockers
Metoprolol, propanolol, esmolol, atenolol, timolol, carvedilol

116

Mechanism of action Antiarrhytmics class II

Decrease SA and AV nodal activity by ↓ cAMP, ↓ Ca2+ currents
Suppress abnormal pacemakers by ↓ slope of phase 4

117

What effet do Antiarrhytmics class II have in AV node?

AV node particularly sensitive- ↑ PR interval

118

Which characteristic does Esmolol has as Antiarrhytmic?

Very short acting

119

Clinical use for Antiarrhytmics class II

Supraventricular Tachycardia
lowing ventricular rate during atrial fibrillation and atrial flutter

120

Toxic effects of β blockers

Incompetence, exacerbation of COPD and asthma
Cardiovascular effects (bradycardia, aV block, CHF)
CNS effects (sedation, sleep alterations)
May mask the signs of hipoglycemia

121

Which Antiarrhytmic class II can cause dyslipidemia?

Metoprolol

122

Side effect of Propanolol

Can excacerbate vasospasm in Prinzmetal angina

123

When are Antiarrhytmics class II contraindicated?

In cocaine users

124

Why are β blockers contraindicated for cocaine users?

Risk of unopposed α adrenergic receptor agonist activity

125

How is β blocker overdose treated?

With Glucagon

126

Antiarrhytmics class III

AIDS:
Amiodarone
Ibutilide
Dofelitide
Sotalol

127

How do Antiarrhytmics class III work

K+ channel blockers

128

Mechanism of action of Antiarrhytmics class III

↑ Action Potential duration, ↑ Effective refractory Potential

129

When are Antiarrhytmics class III used?

When other antiarrhytmics fail

130

Which ECG change do Antiarrhytmics class III cause?

↑ QT interval

131

Clinical use of Antiarrhytmics class III

Atrial fibrillation, atrial flutter

132

Antiarrhytmics class III used for Ventricular Tachycardia

Amiodarone
Sotalol

133

Toxic effects caused by Sotalol

Torsades de pointes
Excessive β blockade

134

Side effect of Ibutilide

Torsades de pointes

135

You need to be careful when using amiodarone because it can cause...

Pulmonary fibrosis
Hepatotoxicity
Hypothyroidism/Hyperthyroidism
Corneal deposits
Skin deposits (gray/blue) resulting in photodermatitis
Neurologic effects
Constipation
Cardivascular effects

136

Which is the reason amiodarone can cause Hypothyroidism/Hyperthyroidism?

Is 40% iodine by weight

137

Cardiac side effect of Amiodarone

Bradycardia
Heart block
CHF

138

When using amiodarone what do you need to check?

PFTs (pulmonary function tests)
LFTs (liver function tests)
TFTs (Tyroid function tests)

139

Which antiarrhytmic effects does amiodarone has?

Class I, II, III, IV effects and altered the lipid membrane

140

Class IV Antiarrhytmics

Verapamil
Diltiazem

141

Effect of Class IV Antiarrhytmics

Ca2+ channel blockers

142

Mechanism of Action of Class IV Antiarrhytmics

↓ Conduction velocity
↑ Effective refractory period

143

ECG changes with Ca2+ channel blockers

↑ PR interval

144

Clinical use for Class IV Antiarrhytmics

Prevention of nodal arrhytmias (eg. SPT)
Rate control on Atrial Fibrilation

145

Toxic effect of Class IV Antiarrhytmics

Constipation, flushing, edema, Cardiovascular effects

146

Which cardiovascular side effects do Class IV Antiarrhytmics have?

CHF
AV block
Sinus node depression

147

Which are other antiarrhythmics that aren't classified with other families?

Adenosine
Mg2+

148

Mechanism of action of Adenosine

↑ K+ out of cells → hyperpolarizing the cell and ↓ Ica

149

Drug of choice in diagnosing/ abolishing supraventricular tachycardia

Adenosine

150

How long does it takes for Adenosine to act?

Very short acting (15 seg)

151

Adverse effects of Adenosine

Flushing
Hypotension
Chest pain

152

Who block the effects of Adenosine?

Effects blocked by Theophylline and caffeine

153

When is Mg2+ used as Antiarrhythmic?

Effective in torsades de pointes and digoxin toxicity