4.4 Antiarrhythmic Drugs Flashcards
Which generates slower + shorter impulses; SAN or Purkinje Fibers?
SAN
Which contracts 1st, atria or ventricles?
Atria contracts before the ventricles, causing the characteristic rhythm of the heart
Arrhythmia is an abnormal cardiac rhythm from…
- Abnormal impulse …
- Generation
- Conduction
What is Atrial Fibrillation?
Irregular heartbeat
What are the Class I Antiarrhythmic Drugs?
Sodium Channel Blockers
What are the Class II Antiarrhythmic Drugs?
β-adrenergic receptor blockers
What are the Class III Antiarrhythmic Drugs?
Potassium Channel Blockers
What are the Class IV Antiarrhythmic Drugs?
Calcium Channel Blockers
What are the Unclassified Antiarrhythmic Drugs?
Adenosine, Magnesium, Potassium
What class of antiarrhythmic drugs preferentially bind to the activated sodium channels?
Class 1A + 1C
What class of antiarrhythmic drugs preferentially bind to the inactivated sodium channels?
Class 1B
What are the 3 Class IA drugs?
- Procainamide
- Disopyramide
- Quinidine
What are the cardiac effects of Class IA antiarrhythmic drugs? (3)
- Slow 0 phase of AP
- When MP is actively rising
- Slow impulse conduction
- Prolong action of potential duration
What is procasinamide metabolized to?
N-acetylprocainamide (NAPA)
Both NAPA + dysopyramide are eliminated by the …
kidneys
What is the therapeutic use of Procainamide (Class IA)?
Atrial + Ventricular Arrhythmias
What is the therapeutic use of Disopyramide (Class IA)?
Ventricular Arrhythmia (USA)
What is the toxicity associated with Procainamide (Class IA)? (3)
- Hypotension due to ganglion-blocking
- Excessive cardiac effects (torsadogenesis)
- Lupus-related effects (erythematosus)
What is the toxicity associated with Disopyramide (Class IA)? (3)
- Negative iontropic effects on the heart
- May precipitate heart failure
- Atropine-like activitives
What are the Class IB antiarrhythmic drugs? (2)
- Lidocaine (LA)
- Mexiletine
What are the cardiac effects of Class IB antiarrhythmic drugs? (2)
-
Bind to inactivated state of sodium channels
- Prolongs the inactiviety of Na channels
-
Depresses conduction in depolarized cells
- Slows down the rate at which impulses are being initiated
Which Class IB antiarrhythmic drug has the longest half life?
-
Mexiletine = 8-20 hrs
- Orally administered
- Lidocaine = 1-2 hrs
Where are the Class IB antiarrhythmic drugs metabolized?
Liver
What is the therapeutic use of the Class IB drugs?
Ventricular Tachycardia
What is the therapeutic use of Mexiletine (Class IB)?
Pain release for diabetic neurology
Which class of sodium channel blockers is the least toxic?
Class IB
What is the toxicity associated with Class IB sodium channel blockers? (2)
- Large doses may cause hypotension
- LA neurologic effects
What are the Class IC sodium channel blockers? (2)
- Flecainide
- Propafenone
What are the cardiac effects of Class IC sodium channel blockers? (2)
- Blocks sodium channels with slow kinetics
- Blocks potassium channels with slow kinetics
How are Class IC drugs administered?
orally, and well absorbed
How are Class IC drugs eliminated and metabobilized?
- Eliminated by liver
- Metabolized in kidneys
What are the therapeutic uses of Class IC drugs? (2)
- Supraventricular arrhythmias
- Premature ventricular conductions
What is the toxicity associated with Class IC drugs?
Severe exacerbation of arrhythmias in preexisiting conditions
What is the toxicity associated with Propafenone (Class IC)?
Constipation
What are the Class II antiarrhytmic drugs?
- Propranolol
- Esmolol
- Sotalol
What are the Class II nonselective β-blockers?
- Propranolol
- Sotalol
What Class II drug is β1-selective?
Esmolol
What antiarrhythmic drugs are contraindicated in pts with Asthma?
Class III = non-selective β-blockers (propranolol, sotalol)
These pts require β2 stimulation
What are the cardiac effects of Class II drugs?
Slows AP duration
- Propranolol - also slows impulse conduction
What is the therapeutic use of Esmolol (Class II)?
Intraoperative acute arrhytmias
What are the Class III antiarhythmic drugs? (4)
- Amiodarone
- Dronedarone
- Dofetilide
- Ibutilide
What are the cardiac effects of Amiodarone (Class III) antiarrhythmic drugs? (3)
- Shows complex effects (class I, II, III, IV actions)
- Prolongs AP duration
- Prolongs duration of refractory period
How is Amiodarone (class III) administered?
Oral + IV
How is amiodarone (Class III) metabolized?
Liver (CYP3A4)
What are the therapeutic uses of Amiodarone (Class III)? (2)
- Recurrent ventricular tachycardia
- Atrial fibrillation
What drug is structurally related to thyroxine, and inhibits conversion of T4 to T3?
Amiodarone (Class III)
What is the toxicity associated with Amiodarone (Class III)? (3)
- Bradycardia + heart block
- Pulmonary toxicity (fibrosis)
- Abnormal liver function (b/c extensive metab) + hepatitis
What Class III drug is an amidarone analog, without iodine in it?
Dronedarone
What are the cardiac effects of Dronedarone (Class III)? (2)
- Prolongs AP duration
- Weak β-blocking activity
Which Class III drug has increased absorption by 2-3 fold when taken with food?
Dronedarone
What is the therapeutic use of Dronedarone (Class III)?
Atrial Fibrillation
What is the toxicity associated with Dronedarone (Class III)?
Abnormal liver function + hepatitis
What Class III drug is only administered orally, with 100% bioavailability?
Dofetilide
What is the toxicity associated with Dofetilide (Class III)?
Ventricular pro-arrhythmias
What Class III drug is administered only by IV?
Ibutilide
What is the therapeutic use for Ibutilide, besides the typical use of Class III drugs to atrial fibrillation?
Atrial flutter
What is the toxicity associated with Ibutilide (Class III)?
Excessive QT prolongation + torsadogenesis
What are the Class IV antiarrhythmic drugs? (2)
- Verapamil
- Diltiazem
What are the cardiac effects of Class IV drugs?
- Prolongs effective refractory period
- Supresses early + delayed afterdepolarization
What is Verapamil (Class IV) useful in treating?
Supraventricular tachycardia
Which Class IV drug is available in Intraventricular form?
Diltiazem
What are the cardiac effects of Adenosine? (4)
- Increases potassium conductance
- Inhibits calcium current
- Hyperpolarization
- Suppression of calcium-dependent AP
What is the effect of Adenosine at a high bolus dose?
Inhibits AV node conduction
What is the 1/2 life of Adenosine?
1/2 life in the blood = 10 seconds
Not good for long term use
What is the drug of choice for supraventricular tachycardia?
Adenosine
Verapamil is also used for SVT
What is the toxicity/symptoms associated with Adenosine? (3)
- Flushing
- Shortness of breath
- Chest burning
What drugs are at risk for drug-drug interactions with Antiarrhytmic drugs? (2)
- Catecholamines
- Antiarrhythmic drugs