John Vincent A. Yangco ANTI-ARRHYTHMIC DRUGS Drugs used for Tachyarrhythmias 1. Class IA a. b. c. Quinidine Procainamide Disopyramide a. b. c. d. 2. Class IB Lidocaine Phenytoin Tocainide Mexiletine 3. a. b. c. Class IC Flecainide Encainide Propaferone a. b. c. d. e. f. 4. Class II Propanolol Atenolol Esmolo Metoprolol Nadolol Pindolol 5. Class III a. Bretylium b. Amiodarone c. Sotalol 6. Class IV a. Verapamil b. Diltiazem Drugs used for Bradyarrhytmias 7. Atropine 8. Glycopyrrolate 9. Propantheline bromide Procainamide -Brand name: Pronestyl® -Action: A class IA antiarrhythmic agent, exhibits cardiac action similar to that of quinidine. It is considered both a supraventricular and ventricular antidysrhythmic. It prolongs the refractory times in both the atria and ventricles, decreases myocardial excitability, and depresses automaticity and conduction velocity. It has anticholinergic properties. -Clinical uses: Useful for the treatment of ventricular premature complexes (VPC’s), ventricular tachycardia, or supraventricular tachycardia associated with Wolff-ParkinsonWhite (WPW) syndrome with wide QRS complexes. -Adverse effect: Gastrointestinal effects may include anorexia, vomiting, or diarrhea. Effects related to the cardiovascular system can include weakness, hypotension, negative inotropism, widened QRS complex and QT intervals, AV block, multiform ventricular tachycardias. There is also a possibility of fever and leukopenias. -Contraindication: Contraindicated in patients with myasthenia gravis. Also in patients hypersensitive to it, procaine or other chemically related drugs. In humans, it is contraindicated in patients with systemic lupus erythematous (SLE). It should not be used in patients with torsade de pointes, or with 2 or 3 degree heart block. nd rd -Drug Interaction: Use with Amiodarone Anticholinesterase agents Cimetidine Hypotensive drugs Lidocaine Neuromuscular blocking agents Quinidine Phenytoin Propanolol Ranitidine Trimethoprim -Dosage: Dogs - 10-30 mg/kg q6h PO, to a maximum dose of 40 mg/kg 8-20 mg/kg IV or IM Constant rate infusion (CRI): Initial loading dose of 10 mg/kg, followed by 20 mcg/kg/min IV CRI; the CRI rate can be increased to 25-50 mcg/kg/min if needed for refractory arrhythmias Cats – 3-8 mg/kg q6-8h IM or PO CRI: 1-2 mg/kg IV slowly, then 10-20 mcg/kg/min IV Horses – 25-35 mg/kg q8h PO Up to 20 mcg/kg IV -Formulation: Available in 250-, 375-, and 500-mg tablets or capsules and a 100- and 500mg/ml injection. Lidocaine -Brand name: Xylocaine® -Action: A class IB antidysrhythmic agent. At therapeutic levels, lidocaine causes phase 4 diastolic depolarization attenuation, decreased automaticity, and either a decrease or no change in membrane responsiveness and excitability. -Clinical uses: Use as a local and topical anesthetic agent. It is also used to treat ventricular arrhythmias, principally ventricular tachycardia and ventricular premature complexes in all species. -Adverse effect: CNS signs include drowsiness, depression, ataxia, muscle tremors, etc. Nausea and vomiting may occur, but are usually transient. -Contraindication: Cats tend to be more sensitive to the CNS effects of lidocaine. Contraindicated in patients with known hypersensitivity to the amide-class local anesthetics, a severe degree of SA, AV or intraventricular heart block, or Adams-Stokes syndrome. Used with caution in patients with liver disease, congestive heart failure, shock, hypovolemia, severe respiratory depression, or marked hypoxia. -Drug interaction: Use with Antiarrhythmics Cimetidine Phenytoin Propranolol Succinylcholine -Dosage: Dogs – Antiarrhythmic: 2-4 mg/kg IV (to a maximum dose of 8 mg/kg over 10minute period) Antiarrhythmic: 25-75 mcg/kg/min IV, CRI Antiarrhythmic: 6 mg/kg q1.5h IM Epidural: 4.4 mg/kg of 2% solution Cats – Antiarrhythmic: Start with 0.1 to 0.4 mg/kg initially, and then increase to 0.25-0.75 mg/kg IV slowly if there has been no response Antiarrhythmic: Loading dose of 0.5-1 mg/kg IV, followed by 1020 mcg/kg/min, (0.6-1.2 mg/kg/hr), IV, CRI Epidural: 4.4 mg/kg of 2% solution Horses – Antiarrhythmic: 0.25-0.5 mg/kg q5-15 min IV, for a total of 1.5 mg/kg, then as a CRI of 0.05 mg/kg/min (50 mcg/kg/min) Postoperative ileus: 1.3 mg/kg IV bolus administered over 15 min, followed by 0.05 mg/kg/min (50 mcg/kg/min) CRI Analgesia: 2 mg/kg IV, followed by 50 mcg/kg/min, CRI -Formulation: Available in 5-, 10-, 15-, and 20-mg/ml injection. Diltiazem -Brand name: Cardizem®, Dilacor XR® -Action: A calcium-channel blocker similar in action to drugs such as verapamil or nifedipine. It inhibits the transmembrane influx of extracellular calcium ions in myocardial cells and vascular smooth muscle, but does not alter serum calcium concentrations. It also slows AV node conduction and prolongs refractory time. -Clinical uses: Useful in treatment of hypertension, atrial fibrillation, and supraventricular tachycardias. -Adverse effects: Bradycardia is the most prominent side effect reported in dogs. In cats, vomiting is reported as the most common side effect. Potentially, lethargy, GI distress (anorexia), hypotension, heart block or other rhythm disturbances, CNS effects, rashes, or elevations in liver function tests could occur in other species. -Contraindication: Contraindicated in patients with severe hypotension (<90 mm Hg systolic), sick sinus syndrome or 2 or 3 degree AV block (unless a functioning pacemaker is in place), acute MI, radiographically documented pulmonary congestion, or when the patient is hypersensitive to it. nd rd -Drug interaction: Use with Anesthetics Benzodiapines Beta-blockers Buspirone Digoxin Cimetidine/ranitidine Cyclosporine Rifampin Quinidine -Dosage: Dogs – 0.5-1.5 mg/kg q8h PO. For atrial fibrillation 5 mg/kg q12h, PO and a combination of diltiazem (3 mg/kg q12h PO) plus digoxin (0.005 mg/kg q12h, PO) has been used Atrial fibrillation: 0.05-0.25 mg/kg IV administered q5min to effect Supraventricular tachycardia: 0.25 mg/kg over 2 min IV Acute renal failure: 0.2 mg/kg IV, followed by 3-5 mcg/kg/min constant rate infusion Cats – 1.75-2.4 mg/kg q8h PO Horses – 0.125 mg/kg IV over at least 2 minutes -Formulations: Available in 30-, 60-, 90- and 120-mg tablets; 60-, 90-, 120-, 180-, 240-, and 300-mg extended release capsules; and in a 5-mg/ml injection solution. Glycopyrrolate -Brand name: Robinul-V® -Action: Anticholinergic agent parasympatholytic. It produces atropine-like effects systemically. It has less effect on CNS compared to atropine because of lower penetration to CNS. It may produce a longer duration of action than atropine. -Clinical uses: Used to inhibit vagal effects and increase heart rate in animals. It also will decrease respiratory, salivary, and GI secretions. It may be used as an adjunct to anesthesia when it is necessary to override vagal stimulus. -Adverse effects: Antimuscarinic (anticholinergic) effects. Side effects of therapy include xerostomia, ileus, constipation, tachycardia, and urine retention. -Contraindication: Do not use in patients with glaucoma, intestinal ileus, gastroparesis, or tachycardia. -Drug interaction: No specific drug interactions. However, it is expected that glycopyrrolate will antagonize drugs that stimulate respiratory and GI secretions and GI motility. -Dosage: Dogs and cats: 0.005-0.01 mg/kg IV, IM or SQ Cattle and horses: use during anesthesia: 0.005-0.01 mg/kg IM or SQ or 0.00250.005 mg/kg IV -Formulation: Available as a 0.2-mg/ml injection.