Drugs for Cardiac Arrhythmias Flashcards

1
Q

What are the class 1A drugs?

A
  • Quinidine
  • Procainamide
  • Disopyramide
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2
Q

What are the class 1B drugs?

A
  • Lidocaine

- Mexiletine

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3
Q

What are the class 1C drugs?

A
  • Flecanide

- Propafenone

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4
Q

What are the class 2 beta blockers?

A
  • Esmolol

- Propranolol

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5
Q

What are the class 3 potassium channel-blocking drugs?

A
  • Amiodarone
  • Sotalol
  • Dofetilide
  • Ibutilide
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6
Q

What are the class 4 cardioactive calcium channel blocking drugs?

A
  • verapamil

- Diltiazem

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7
Q

What do class 1A drugs do?

A
  • block Na+ channels: (preferentially bind to open Na+ channels)
  • block K+ channels
  • prolong QRS and QT intervals
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8
Q

What does Procainamide do in addition to sodium channel block?

A
  • directly depresses the activities of SA and AV nodes
  • possesses antimuscarinic activity
  • has ganglion-blocking properties (reduces peripheral vascular resistance)
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9
Q

What are the adverse effects of Procainamide?

A
  • QT interval prolongation
  • induction of torsade de pointes arrhythmias and syncope
  • excessive inhibition of conduction
  • Lupus erythematosus syndrome with arthritis, pleuritis, pulm disease
  • nausea, diarrhea
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10
Q

What are the pharmacodymanics and clinical use of Quinidine?

A
  • affords antimuscarinic effect on the heart
  • beta-blocking activity
  • may cause hypotension -> tachycardia

NOTE: rarely used d/t adverse effects

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11
Q

What are the adverse effects of Quinidine?

A
  • QT interval prolongation
  • torsades de pointes arrhythmia
  • excessive conduction slowing
  • NVD
  • HA, dizziness, tinnitus
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12
Q

What is the clinical use of Disopyramide?

A

recurrent ventricular arrhythmias

- affords potent antimuscarinic effect on heart

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13
Q

What are the adverse effects of Disopyramide?

A
  • QT interval prolongation
  • torsade de points
  • negative inotropy
  • atropine-like symptoms (urinary retention, dry mouth, blurred vision, constipation)
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14
Q

What do class 1B drugs do?

A
  • block sodium channels (**preferentially bind to depolarized cells/inactivated sodium channels)
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15
Q

What class of drugs dissociates from the channels with fast kinetics?

A

class 1B

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16
Q

What drug class has a more specific action on sodium channels, does not block potassium channels, and does not prolong action potential or QT duration?

A

class 1B

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17
Q

What does Lidocaine do?

A

blocks inactivated sodium channels

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18
Q

What drug selectively blocks conduction in depolarized tissue, making damaged tissue “electrically silent”?

A

Lidocaine
- fast kinetics of dissociation from sodium channel results in recovery from block between action potentials, with no effect on cardiac conductivity in normal tissue

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19
Q

What is the clinical use of Lidocaine?

A

termination of ventricular tachycardia in the setting of acute myocardial ischemia

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20
Q

What are the adverse effects of Lidocaine?

A
    • it is the least toxic of all class 1 drugs **
  • may cause hypotension in patients with heart failure by inhibiting cardiac contractility
  • paresthesias, tremor, slurred speech, convulsions
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21
Q

What drug is the orally active congener of lidocaine, and has similar electrophysiological/antiarrhythmic effects to lidocaine?

A

Mexiletine

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22
Q

What is the clinical use of Mexiletine?

A
  • ventricular arrhythmias

- relieves chronic pain, especially pain due to diabetic neuropathy and nerve injury

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23
Q

What are the adverse effects of Mexiletine?

A
  • tremor
  • blurred vision
  • nausea
  • lethargy
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24
Q

What do class 1C drugs do?

A
  • block sodium channels (slow impulse conduction)
  • state dependent (preferentially bind open sodium channels)
  • blocks certain potassium channels
  • prolong QRS interval
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25
Q

What drug blocks sodium and potassium channels, and has no antimuscarinic effects?

A

Flecainide

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26
Q

What is the clinical use of Flecainide?

A

in patients with otherwise normal hearts who have supraventricular arrhythmias

27
Q

What are the adverse effects of Flecainide?

A

may be ver effective in supressing premature ventricular contractions

28
Q

When might Flecainide cause severe exacerbation of ventricular arrhythmias?

A

when administered to patients with preexisting ventricular tachyarrhythmias

  • patients with previous MI
  • patients with ventricular ectopic rhythms
29
Q

What drug class causes ventricular arrhythmias, such as PVCs and sustained VT and VF?

A

class 1C

NOTE: CAST trial was terminated early because 1C drugs were shown to increase mortality 2.5 fold

30
Q

What drug has sodium blocking kinetics similar to flecaininde, and possesses weak beta-blocking activity?

A

propafenone

31
Q

What is the clinical use of propafenone?

A

supraventricular arrhythmias in patients without structural disease

32
Q

What are the adverse effects of propafenone?

A
  • exacerbation of ventricular arrhythmias
  • a metallic taste
  • constipation
33
Q

What is the sympathetic effect of class 2 drugs on SA nodal cells?

A
  • lowers action potential threshold due to effect of L-type Ca channels
  • increases slope due to effects on funny current and T-type Ca channels
34
Q

What are the effects of propranolol and esmolol on SA and AV nodal cells?

A
  • SA node: decreases HR (increasing RR interval)

- AV node: decreases AV conductance (increasing PR interval)

35
Q

What are the clinical uses of propranolol in cardiac arrhythmias?

A
  • arrhythmias associated with stress and thyroid storm
  • atrial fibrilation and flutter
  • paroxysmal supraventricular arrhythmias
  • arrhythmias associated with MI (it decreases mortality in pt with MI)
36
Q

What short-acting selective beta-1 blocker has a half-life of 10 minutes (because of hydrolysis by blood esterases)?

A

Esmolol

37
Q

What is the clinical use of Esmolol?

A
  • supraventricular arrhythmias
  • arrhythmias associated with thyrotoxicosis
  • myocardial ischemia or acute MI with arrhythmias
  • as an adjunct drug in general anesthesia to control arrhythmias during surgery
38
Q

What are the adverse effects of beta-blockers?

A
  • reduced CO
  • bronchoconstriction
  • impaired liver glucose metabolism
  • increase VLDL, decrease HDL (unfavorable)
  • sedation, depression
39
Q

What are the contraindications of beta-blockers?

A
  • asthma
  • peripheral vascular disease
  • Raynaud’s syndrome
  • T1DM on insulin
  • bradyarrhythmias and AV conduction abnormalities
  • severe depression of cardiac function
40
Q

What do class 3 drugs block?

A

potassium channels

  • calcium activated
  • inward rectifying
  • tandem pore domain
  • voltage-gated
41
Q

When are inwardly rectifying potassium channels open?

A

in the resting state

42
Q

What contributes to the regulation of action potential?

A
  • voltage-gated potassium channels
43
Q
What class of drugs :
- block potassium channels
0 prolong action potential duration
- prolong QT interval
- prolong refractory period
A

class 3 drugs

44
Q

What drug is used to treat recurrent ventricular tachycardia and atrial fibrillation?

A

Amiodarone (class 3)

45
Q

What is Amiodarone metabolized by?

A

CYP3A4
- major metabolite is active, with very long elimination half-life (weeks-months)

NOTE: it inhibits many CYP enzymes, which may affect the metabolism of many other drugs, so all meds should be carefully reviewed, dose adjustments may be necessary

46
Q

What are the adverse effects of Amiodarone?

A
  • AV block and bradycardia
  • low incidence of torsades de points
  • fatal pulmonary fibrosis
  • hepatitis
  • photodermatitis
  • optical neuritis
  • hypo/hyperthyroidism (blocks peripheral conversion of T4->T3
47
Q

What drug is considered a class 2 (non-selective beta-blocker) and a class 3 agent (prolongs APD)

A

Sotalol

48
Q

What are the clinical uses of Sotalol?

A
  • treatment of life-threatening ventricular arrhythmias

- maintenance of sinus rhythm in patients with atrial fibrillation**

49
Q

What are the adverse effects of Sotalol?

A
  • depression of cardiac function

- provokes torsades de pointes

50
Q

What drug specifically blocks the rapid component of the delayed rectifier potassium current?

A

Dofetilide

NOTE: effect is more pronounced at lower heart rates)

51
Q

What is the clinical use of Dofetilide?

A
  • restore sinus rhythm in patients with atrial fibrillation

- maintains sinus rhythm after cardioversion (restoring normal HR) in patients with atrial fibrillation

52
Q

What are the adverse effects of Dofetilide?

A

QT interval prolongation and increased risk of ventricular arrhythmias

53
Q

What drug slows cardiac repolarization (similar to dofetilide) by blocking the rapid component of the delayed rectifier potassium current?

A

Ibutilide

54
Q

What is the clinical use of Ibutilide?

A

conversion of atrial flutter and atrial fibrillation to sinus rhythm

55
Q

What are the adverse effects of Ibutilide?

A

QT interval prolongation and increased risk of ventricular arrhythmias

56
Q

What drug class blocks both activated and inactivated L-type calcium channels?

A

class 4 drugs

57
Q

What do class 4 drugs do?

A
  • decrease the slope of phase 0 depolarization -> bradycardia
  • increase L-type calcium channel threshold potential -> prolong AP duration
  • prolong refractory period in the AV node
58
Q

What are the two class 4 drugs mentioned?

A

Verapamil, Diltiazem

59
Q

What is the clinical use of Verapamil and Diltiazem ?

A
  • termination and prevention of paroxysmal supraventricular tachycardia
  • ventricular rate control in atrial fibrillation and flutter
60
Q

What are the adverse effects of Verapamil and Diltiazem?

A
  • negative inotropy
  • AV block
  • SA node arrest
  • bradyarrhythmias
  • hypotension

NOTE: Verapamil also causes constipation

61
Q

What drug activates potassium current and inhibits calcium and funny currents, causing hyperpolarization and suppression of action potentials in slow cells?

A

Adenoside

- it also inhibits AV conduction and increases nodal refractory period

62
Q

What is the clinical use of Adenosine?

A

conversion of sinus rhythm in paroxysmal supraventricular tachycardia

63
Q

What are the adverse effects of Adenosine?

A
  • shortness of breath
  • bronchoconstriction
  • chest burning
  • AV block
  • hypotension