Anti-arrhythmics Flashcards
What is the function of Class 1 arrhythmics?
- Rhythm control
- They block sodium channels that are responsible for the rising phase (Phase 0) of cardiac action potentials.
- They are frequency dependent and voltage dependent.
What are the primary effects of Class 1 AADs on the cardiac action potential?
- They increase the threshold for activation of a cell
- They reduce Vmax, the rate of the rise of the action potential.
- They increase the effective refractory period.
What is the function of Class 1A AADs?
- Reduction in repetitive firing through increased threshold and frequency dependent block.
- Reduces Vmax
- Prolongs APD and ERP
- Binding/unbinding is immediate``
What is the function of Class 1B AADs?
- Reduction in repetitive firing by increased threshold and frequency dependent block.
- Little effect on Vmax
- Binding/unbinding is rapid
What is the funciton of Class 1C AADs?
- Reduction in repetitive firing by increased threshold and frequency dependent block
- Larger reduction in Vmax than Class 1A
- Little effect on ERP
- Binding/unbinding is slow
Toxicities of Class 1 AADs
- TI is low in most Class 1 drugs.
- Reduced Vmax can cause slowed conduction/arrhythmic APs
- Ventricular arrythmias are a dangerous SAE
Which Class 1 drugs have the most toxicities?
Class 1C > Class 1A > Class 1B
What are the Class 1A Drugs?
Procainamide
Quinidine
Disopyramide
Procainamide
- increases threshold, reduces repetitive firing, reduces Vmax, and increases ERP
- used for A-flutter, A-fib, PSVT, V-tach, and V-fib
- SAE: Arganulocytosis, SLE-like Syndrome, nausea, hypotension
Quinidine
- increases threshold, reduces repetitive firing, reduces Vmax, and increases ERP
- used for A-flutter, A-fib, and PSVT, can be used to prevent V-tachyarrythmias
- SAE: diarrhea, cinchonism - including headaches and tinnitus
Disopyramide
- similar to quinidine
- used to maintain sinus rhythm in pts with A-flutter, A-fib or to prevent the recurrence of V-tach or V-fib
What are the Class 1B antiarrhythmics?
Lidocaine
Tocainide
Mexiletine
Lidocaine
- increases threshold, reduces repetitive firing
- little effect on Vmax or ERP
- IV only
- used for IV control of ventricular arrhythmias
- SAE: rare at therapeutic levels; can include CNS symptoms at high plasma levels
Tocainide/Mexiletine
- similar to lidocaine but can be used orally
What are the Class 1C AADs?
Flecainide
Propafenone
Flecainide
- increases threshold and reduces repetitive firing, reduces Vmax
- little effect on ERP
- used for atrial arrhythmias only
- SAE: serious cardiac toxicity
Propafenone
- increases threshold and reduces repetitive firing, reduces Vmax
- little effect on ERP
- used in chronic oral therapy for pts with SVTs including A-fib
- metabolized by P450: drug-drug interactions!!!
What is the function of Class III AADs?
Used for rhythmcontrol and have three common effects:
- K+ channel blockade
- Delayed repolarization
- Prolonged action potential and prolonged ERP
Amiodarone
- Class III/Class I hybrid
- blocks Na+ and K+ channels
- prolongation of action potential duration, increased ERP, reduced Vmax and reduced conduction velocity at high doses
- LONG half life - accumulates in lipids and can cause serious side effects
- used IV for conversion to sinus rhythm as well as orally for ventricular arrythmias and SVTs.
- SAE: pulmonary fibrosis (most serious), headaches, tremor, ataxia, paresthesias, also rare CV side effects
Dronedarone
- Class III/Class I hybrid similar to amiodarone
- used for a-tach, a-fib, and v-tach
- SAE: more rare than with amiodarone
Dofetilide
- Class III AAD that blocks K+ channel responsible for the early phase of the AP via the IKr current
- prolongs AP duration and ERP
- used to maintain sinus rhythm in A-flutter and A-fib
Ibutilide
- Class III AAD that is similar to dofetilide
- IV only
- used for conversion of A-flutter and A-fib
- SAE: can cause prolonged QT
Sotalol
- beta antagonist and K+ channel blocker
- prolongs action potential duration and ERP
- used to treat ventricular tachycardias and SVTs
- SAE: can be arrythmogenic, long QT syndrome, and V-tach
What are Class II and Class IV AADs used for?
Rate control