Drugs Used in Cardiac Arrhythmias Flashcards
Class 1 Sodium Channel-blocking Drugs: 1A
– Quinidine (Cardioquin)
– Procainamide (Pronestyl)
– Disopyramide (Norpace)
Class 1 Sodium Channel-blocking Drugs: 1B
– Lidocaine (Xylocaine)
– Mexiletine (Mexitil)
Class 1 Sodium Channel-blocking Drugs: 1C
– Flecainide (Tambocor)
– Propafenone (Rythmol)
Class 2 Beta Blockers
– Esmolol (Brevibloc)
– Propranolol (Inderal)
Class 3 Potassium Channel-blocking Drugs
– Amiodarone (Cordarone)
– Sotalol (Betapace)
– Dofetilide (Tikosyn)
– Ibutilide (Corvert)
Class 4 Cardioactive Calcium Channel Blockers
– Verapamil (Isoptin)
– Diltiazem (Cardizem)
Miscellaneous agents
Adenosine (Adenocard)
Fast action potential in cardiac muscle: Which phase?
- Voltage-dependent fast Na+ channels open as a result of depolarization; Na+ enters the cells down its electrochemical gradient
Phase 0
Fast action potential in cardiac muscle: Which phase?
- K+ exits cells down its gradient, while fast Na+ channels close, resulting in some repolarization
Phase 1
Fast action potential in cardiac muscle: Which phase?
- plateau phase results from K+ exiting cells offset by and Ca2+ entering through slow voltage-
dependent Ca2+ channels
Phase 2
Fast action potential in cardiac muscle: Which phase?
- Ca2+ channels close and K+ begins to exit more rapidly resulting in repolarization
Phase 3
Fast action potential in cardiac muscle: Which phase?
- Resting membrane potential is gradually restored by Na+/K+ ATPase and the Na+/Ca2+
exchanger
Phase 4
Effects of Class 1A drugs
- Block sodium channels
- Bind to open (ACTIVATED) sodium channels
- Dissociate from channel with INTERMEDIATE kinetics
- Block POTASSIUM channels
- PROLONG AP duration **
- Prolong QRS and QT intervals of the ECG **
Class 1A: Procainamide
Clinical Use?
• Used infrequently (frequent dosing is required,
common occurrence of lupus-related side effects)
• Is effective in sustained VENTRICULAR TACHYCARDIAS and arrhythmias associated with myocardial infarction (not
a first choice drug for these indications)
• Sidenote: it directly depresses the activities of SA and AV nodes
Class 1A: Procainamide
Adverse effects?
• Cardiac – QT interval prolongation – Induction of torsade de pointes arrhythmias and syncope – Excessive inhibition of conduction
• Extracardiac
– Lupus erythematosus syndrome with arthritis, pleuritis, pulmonary disease, hepatitis and fever
– Nausea, diarrhea
– Agranulocytosis
Class 1A: Quinidine
Pharmacodynamics and clinical use?
– Affords antimuscarinic effect on the heart –> may ENHANCE AV conductance
– Exhibits beta-blocking activity (effect on PR interval is
variable)
– May cause HYPOTENSION –> tachycardia
Class 1A: Quinidine
Clinical use?
Rarely used because of cardiac and extracardiac adverse
effects and the availability of better-tolerated antiarrhythmic drugs
Class 1A: Quinidine
Adverse effects?
• Cardiac:
– QT interval prolongation
– Induction of torsade de pointes arrhythmia and
syncope
– Excessive slowing of conduction throughout the
heart
• Extracardiac:
– GI side effects (diarrhea, nausea, vomiting)
– Headache, dizziness, tinnitus (cinchonism)
– Thrombocytopenia, hepatitis, fever
Class 1A: Disopyramide
Clinical use?
Recurrent ventricular arrhythmias
Class 1A: Disopyramide
Adverse effects?
• Cardiac: QT interval prolongation, induction of torsade de pointes arrhythmia and syncope, negative inotropic effect – may precipitate heart failure, excessive depression of cardiac conduction
• Extracardaic: atropine-like symptoms – urinary
retention, dry mouth, blurred vision, constipation, exacerbation of glaucoma