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Anti-Arrhythmic Drugs
Use, MOA and ADR's
33
Medical
Graduate
03/14/2013

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Cards

Term
What are the classes of Antiarrhythmic Drugs?
Definition

Class Ia, Ib, Ic

Class II

Class III

Class IV

Term
What is the general mechanism of Class Ia antiarrhythmics?
Definition

Na+ Channel Blockade

 

Moderately blocks phase 0 upstroke rate

Prolongs repolarization

 

Ex. Qunidine, Procainamide and Disopyramide

Term
What is the general mechanism of action of Class Ib antiarrhytmic drugs?
Definition

Mild block of Na+ channel

 

Mild decrease in phase 0 upstroke rate

Shorten repolarization

 

Ex. Lidocain, Tocainide, Mexiletine and Phenytoin

Term
What is the general mechanism of action of Class Ic antiarrhythmic drugs?
Definition

Marked Na+ Channel Blockade

 

Marked decrease in phase 0 upstroke rate

-no change in repolarization

 

Ex. Flecainide, Propafenone

Term
What is the general mechanism of action of Class II antiarrhytmic drugs?
Definition

Class II are the Beta-Blocking agents.

 

Propanolol, Esmolol, Metaprolol and many more.

 

*all end in "ol"*

Term
What is the general mechanism of action of Class III antiarrhytmic drugs?
Definition

Class III antiarrythmics are K+ channel blocking agents.

 

Marked prolongation of repolarization.

 

Ex. Amiodarone, Bretylium, Sotolol

Term
What is the general mechanism of action of Class IV antiarrhytmic drugs?
Definition

Class IV antiarrhythmic drugs are Ca2+ channel blocking agents.

 

Ex. Verapamil and Dilitazem

Term
What are the main cardiac effects of Class IA antiarrythmic drugs?
Definition

1. Prolong QRS wave (decrease slope of phase 0)

2. Prolong ventricular repolarization (inc. Phad 1-3 of RP)

3. Prolong QT interval

4. decrease automaticity of slow and fast fibers

5. initial anticholinergic effects at SA/AV nodes

Term
What are the main toxicities of Class IA antiarrythmic drugs?
Definition

1. Widening of QRS may lead to ventricular tachycardia

2. Torsades de Points

-proarrhythmia

-caused by drugs that prolong QT

-can lead to tachychardia and syncope (fainting)

Term
What are the main clinical indicatoins for use of Class IA antiarrythmic drugs?
Definition

1. SVT - Supra-ventricular tachychardia arrhythmias

ex.) atrial flutter or fibrillation

Term
What is the drug of choice for the Class IA antiarrythmic drugs?
Definition
Qunidine, Procainamide and Disopyramide
Term
What are the main cardiac effects of Class IB antiarrythmic drugs?
Definition

1. Shortens QT interval

-slight decrease in slope of phase 0

2. Decreases ventricular automaticity

-especially in ischemic cardiocytes

Term
What are the toxicities of Class IB antiarrythmic drugs?
Definition

1. Dose related CNS effects

-dizziness, tremor, psychosis, convulsions

-CNS depression can have anesthetic action (pain suppression)

Term
What are the clinical indications for Class IB antiarrythmic drugs?
Definition

1. Ventricular arrhthmias only

-especially post MI to reduce ventricular fibrillation

Term
What are the drugs of choice for Class IB antiarrhythmic drugs?
Definition

1. Lidocaine

-extensive 1st pass metabolism

-cannot be giving PO

-hepatic metabolism converts to active metabolites

-IV loading and maintenance dose follows 2 compartment model

 

2. Lidocaine analogs

-Mexiletine and Tocainide

 

3.Phenytoin

-used in digitalis-induced arrhythmias

Term
What are the main cardiac effects of Class IC antiarrythmic drugs?
Definition

Widening of QRS and PR interval

-minimal effect on QT interval

Term
What are the toxicities of Class IC antiarrythmic drugs?
Definition

1. Aggrevation of AV block

-can lead to ventricular tachycardia

2. increased mortality in CAST with encainide, flecainide

Term
What are the clinical indications of Class IC antiarrythmic drugs?
Definition

1. AV nodal reentry

Term
What are the drugs of choice for the Class IC antiarrythmic drugs?
Definition
Flecainide, Propafenone, Moricizine
Term
What are the toxicities of Class IC antiarrythmic drugs?
Definition
Term
What are the main cardiac effects of Class II antiarrythmic drugs?
Definition

Beta-Blocking Agents

1. Effects Pacemaker cells: SA, AV and purkinje fibers 

2. Decrease HR, slowed AV conduction, increased PR interval, decreased automaticity (especially related to SNS)

3. Decreases cardia work and oxygen consumption

4. Post MI reduction of reinfarction and sudden death

Term
What are the clinical indications for Class II antiarrythmic drugs?
Definition

1. Supraventricular arrhythmias

-some ventricular arrhythmias

Term
What are the drugs of choice and selectivity of Class II antiarrhythmic drugs?
Definition

1. Propranolol - non-selective blocking

2. Acebutolol - Beta 1 

3. Esmolol - Beta 1 

4. Metoprolol - Beta 1

Term

What do Beta receptors do?

 

Definition
Beta blockers target the beta receptor. Beta receptors are found on cells of the heart muscles, smooth muscles, airways, arteries, kidneys, and other tissues that are part of the sympathetic nervous system and lead to stress responses, especially when they are stimulated by epinephrine(adrenaline). Beta blockers interfere with the binding to the receptor of epinephrine and other stress hormones, and weaken the effects of stress hormones
Term
What are the 3 beta receptors and their actions?
Definition
 β1-adrenergic receptors are located mainly in the heart and in the kidneys.[7] β2-adrenergic receptorsare located mainly in the lungs, gastrointestinal tract, liver, uterus, vascular smooth muscle, and skeletal muscle.[7] β3-adrenergic receptors are located in fat cells
Term
What are the cardiac effects of Class III antiarrhythmic drugs?
Definition

K+ Channel Blockers = Class III

 

1. Increase effective refractive period

- decreases re-entry arrhythmias

-Prolong RP (phase 1-3) and AP duration, w/o significant Na+ channel blockade

2 Amiodarone specific

- decreased conduction velocity = decrease re-entry

-decreased rate of firing (Phase 4 slope)

-causes decreased automaticity

Term
What are the clinical indications for Class III antiarrhythmic drugs?
Definition

Atrial, nodal and ventricular arrhythmias

very broad use

Term
What are the toxicities of Class III antiarrhythmic drugs?
Definition

1. microdeposits in cornea skin and other tissues

2. pulmonary toxicity - fibrosiss

3. peripheral neuroapthy and myopathy

4. abnormal liver function

5. thyroid dysfunction

6. photosensativity - blue-gray skin discoloration in sun exposed areas

Term
What are the drugs of choice for Class III antiarrhythmic drugs?
Definition
Bretylium, Sotalol, Amiodarone, Ibutilide, Dofetilide
Term
What are the cardiac effects of Class IV antiarrhythmic drugs?
Definition

1. decreased conduction velocity of AV node

2. increased refractory period of AV node

 

Both lead to decreased re-entry

Term
What are the drugs of choice for Class IV antiarrhythmic drugs?
Definition
Verapamil and Dilitazem
Term
What are the toxicities of Class IV antiarrhythmic drugs?
Definition

GI - constipation with verapamil

Hypotension

decreased HR

AV block

potential for CHF

Term
What are the clinical indications for Class IV antiarrhythmic drug use?
Definition

suppresses ventricular rate in atrial flutter and fibrillation

compare to digitlis and beta-blockers

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