Agents Used in Cardiac Arrhythmias

AGENTS USED IN CARDIAC ARRHYTHMIAS (cont.
Arrhythmias
▪ These are caused by abnormal pacemaker activity or abnormal impulse propagation.
▪ A problem with the rate or rhythm of your heartbeat. It means that your heart beats too quickly, too
slowly, or with an irregular pattern.
Example: When the heart beats faster than normal, it is called Tachycardia.
The aim of the therapy of arrhythmias is to reduce ectopic pacemaker activity and modify conduction or
refractoriness in reentry circuits to disable movements.
Mechanism of Actions
I. Sodium Channel Blockade
 Sodium potassium pump

II. Blockade of sympathetic autonomic effects in the heart
 Anti-sympathetic.
 Because sympathetic activity can precipitate arrhythmias, drugs that block beta1-
adrenoceptors are used to inhibit sympathetic effects on the heart. Because beta-
adrenoceptors are coupled to ion channels through defined signal transduction
pathways, beta-blockers indirectly alter membrane ion conductance, particularly
calcium and potassium conductance.
III. Prolongation of the effective refractory period
 Refractory/Repolarization – means “Resting Period”

 Ang heart ky mo rest gamay then mo beat, rest then beat.
 Dropping of beats will prolong the resting period of the heart
IV. Calcium channel blockade
Sodium Channel Blocking Drugs

▪ Drugs with local anaesthetic actions
▪ They are the oldest group of anti-arrhythmic drugs and are still widely used.
▪ Prolong the action potential duration
Sodium Channel Blockade

Four responses with Na+ channel blockers:
1. Decrease the velocity – velocity meaning “speed”, by blockade of sodium it can decrease the
speed of heart during contraction.
 Decreasing conduction velocity can help to abolish tachyarrhythmias caused by reentry circuits
2. Suppress the automaticity – Ang heart automatic siya nga mo beat, if for example ang heart
nadaot or nagka arrhythmia mag cause na siyag beating like every second. 60 seconds or 60
bts/min ang normal beating sa heart, in order to suppress its automaticity you will drop some
of its beats to prolong making it from 60 bts/min to 50 bts/min.
3. Decrease ectopic focus – ectopic meaning outside of the normal position. Example: in
pregnancy instead na mo grow ang baby inside sa uterus, toa siya nigrow sa gawas w/c is
abnormal. Blockade of sodium decreases ectopic focus because these are an excitable group of cells
that causes a premature heart beat outside the normally functioning SA node of the heart.
SA node – the heart’s natural pacemaker. Serves to establish and maintain the rhythmic activity of the
heart
4. Increase recovery time

NOTE: Not all sodium are blocked but some. By blocking of sodium it will decreases the chances of
the heart to beat fast resulting in a prolong rest until the next heartbeat. It will prolong the Action
potential duration.
Action potential duration – “ang kadugayon sa beat” prolonging APD, maka cause siya og forceful
contraction sa heart, so mas chada ang mugawas na dugo og mas ma release tanan throughout the
body.
Sodium Channel Blocking Drugs

i. Class IA – prolongs action potential duration
▪ Procainamide
▪ Quinidine
▪ Disopyramide
ii. Class IIB – shortens action potential duration

▪ Lidocaine
▪ Mexiletine
iii. Class IIIC - have minimal effects on the action potential duration
▪ Flecainide –
Cardiac Arrhythmia Suppression Test (CAST trial): When flecainide and other Class 1C was given
prophylactically to patients convalescing to myocardial infarction it increased mortality to 2 ½
fold. Therefore the trial had to be prematurely terminated.
▪ Propafenone
▪ Morcizine
Class II: Beta-Adrenoceptor Blocking Drugs

▪ Action is sympatholytic. (anti-sympathetic)
▪ Drugs with this action reduce β-adrenergic activity in the heart.

Drugs under Class II are:
i. Propanolol – have antiarrhythmic properties by virtue of their β blocking action and direct membrane
effects.
ii. Esmolol – is a short-acting β blocker used primarily as an antiarrhythmic drug for inoperative and
other acute arrhythmias.
iii. Sotalol – a nonselective β blocking drug that prolongs the action potential (Class III action)
Class III: Prolongs Refractory Period

▪ Prolong repolarization or rest period.
“Repolarization – Rest”
“Depolarization – Contraction”
▪ Drugs that prolongs the action potentials, usually by blocking potassium channels in cardiac muscle by
enhancing inward current.
▪ Action potential prolongation by most of these drugs often exhibits the undesirable property of
“reverse use-dependence”. - meaning that, at lower heart rates the refractoriness of the ventricular
myocyte increases where then it can contribute to the risk of torsades de pointes.
Drugs under Class III are:

i. Amiodarone – resulted from its broad spectrum of anti-arrhythmic action, it is very extensively
used for wide variety of arrhythmias. It blocks K+ & Na+ channels and is a weak calcium and
adrenergic blocker.
ii. Dronedarone – like amiodarone, it has multichannel actions, including blocking of K+, Ca+ and
Na+ channels and also has β-adrenergic blocking actions.
iii. Vernakalant – is a multi-ion channel blocker that was developed for the treatment of atrial
fibrillation. It also produces use-dependent block of sodium channel.
iv. Sotalol – it has both Beta-adrenergic receptor blocking (class II) and action potential-prolonging
(class III) actions.
v. Dofetilide – it is a pure class III potassium channel blocker antiarrhythmic agent.
vi. Ibutilide – it is a potassium channel blocker that also activates the inward sodium current
(mixed class III and subclass IA action).
Class IV: Calcium channel Blocking Drugs

▪ Class IV drugs are the non-dihydropyridine calcium channel blockers.
▪ These drugs, of which Verapamil is the prototype were first introduced as anti-anginal agents.
Drugs under IV are:

i. Verapamil – blocks both activated and inactivated L-type calcium channels. It shows greater
action in the heart than on vascular smooth muscle.
ii. Diltiazem – appears to be similar in efficacy with verapamil in the management of
supraventricular arrhythmias, including rate control in atrial fibrillation.
Miscellaneous Antiarrhythmic Agents

Certain agents that are used for the treatment of arrhythmias do not fit the conventional Class 1-4
organization.
Which includes:
a. Digitalis - because of its ability to activate the vagus nerve (parasympathomimetic effect), can also be
used to reduce AV conduction velocity in an attempt to normalize ventricular rate during atrial flutter or
fibrillation.
b. Adenosine
c. Magnesium
d. Potassium
ADENOSINE
▪ It is a naturally occurring nucleoside throughout the body.
Mechanism of action: Activates inward rectifier K+ current and inhibits calcium current.
Intravenous adenosine is the drug of choice for abolishing acute supraventricular tachycardia. It has low
toxicity but causes flushing, chest pain, and hypotension.
▪ It has an extremely short duration of action (approx. 10-15 sec) and the drug is less effective in the
presence of adenosine receptor blockers such as theophylline or caffeine, and its effects are
potentiated by adenosine uptake inhibitors such as dipyridamole.
▪ Adenosine is effective in patients not responding to verapamil
MAGNESIUM
Originally used for patients with Digitalis-Induced arrhythmias who were hypomagnesemic, magnesium
infusion has been found to have antiarrhythmic effects in some patients with normal serum magnesium levels.
Mechanism of action:
Magnesium is recognized to influence Na+/K+ –ATPase, sodium channels, certain potassium channels and
calcium channels. It is multichannel.
POTASSIUM AND DIGITALIS
Mechanism of action:
Inhibits each other’s binding to Na+/K+ - ATPase.

Agents Used in Cardiac Arrhythmias

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AGENTS USED IN CARDIAC ARRHYTHMIAS (cont.

 Sodium potassium pump

 Refractory/Repolarization – means “Resting Period”

Sodium Channel Blocking Drugs

Sodium Channel Blockade

4. Increase recovery time

Sodium Channel Blocking Drugs

ii. Class IIB – shortens action potential duration

Class II: Beta-Adrenoceptor Blocking Drugs

▪ Drugs with this action reduce β-adrenergic activity in the heart.

Class III: Prolongs Refractory Period

Drugs under Class III are:

v. Dofetilide – it is a pure class III potassium channel blocker antiarrhythmic agent.

Class IV: Calcium channel Blocking Drugs

Drugs under IV are:

Miscellaneous Antiarrhythmic Agents

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