sotalol (Betapace, Sotacor)
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Introduction
Tradename: Betapace. Class III antiarrhythmic agent.
Indications
- prevents recurrence of sustained ventricular tachycardia (70%)
- decreases frequency & duration of non-sustained ventricular tachycardia (40%)
- prevents recurrence of atrial fibrillation/flutter, but benefits outweighed by proarrhythmic effects
Contraindications
- avoid in patients with acute heart failure[6]
- avoid in patients with severe LV systolic dysfunction
Dosage
- initiate therapy while patient is hospitalized
- start 80 mg PO BID
- increase at 2-3 days intervals
- max 640 mg/day
- usual maintenance dose is 160-320 mg/day
- PRN dosing for paroxysmal atrial fibrillation[7]
Dosage adjustment in renal failure
Table
| creatinine clearance | dosage interval |
|---|---|
| 30-60 mL/min | every 24 hours |
| 10-30 mL/min | every 36-48 hours |
| < 10 mL/min | NOT recommended |
Tabs: 80, 160, 240 mg
Pharmacokinetics
- bioavailability is 90-100%
- minimal 1st pass hepatic metabolism
- not bound to plasma proteins
- onset of activity is 1-3 hours
- elimination 1/2life is approximately 7.5 hours
- increased with renal insufficiency
- duration of action is 12-20 hours
- excreted unchanged in the urine
elimination via kidney 90 %
1/2life = 12 hours
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- rash, chest pain, leukopenia, hypotension, diaphoresis, phlebitis, Raynaud's phenomenon, skin necrosis after extravasation, cold extremities, life-threatening ventricular arrhythmias, torsades de pointes, retroperitoneal fibrosis (rare), red & crusted skin
- cardiac
- prolongation of QT interval
- torsades de pointes, especially with
- bradyarrhythmias
- prolongs AV conduction
- sinus bradycardia
- contraindicated in patients with sinus bradycardia, 2nd or 3rd degree AV block
- exacerbation of ventricular arrhythmia
- heart failure (3%)
- non cardiac
- fatigue
- bronchospasm
- may mask symptoms of hypoglycemia
- drug adverse effects of beta-adrenergic receptor antagonists
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antiarrhythmic agent, Group III
- drug adverse effects of antihypertensive agents
Drug interactions
- cardiac effects additive with Ca+2-channel blockers
- excessive reduction of sympathetic tone when used with:
- avoid concurrent use of:
- clonidine, insulin, sulfonylureas, verapamil, class 1A antiarrhythmic agents, digoxin, terfenadine, astemizole, cisapride
- drug interaction(s) of antiarrhythmic agents in combination with diuretics
- drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of beta-adrenergic receptor antagonists with thyroid hormone
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfinpyrazone
- drug interaction(s) of beta-adrenergic receptor antagonists with salicylate
- drug interaction(s) of beta-adrenergic receptor antagonists with rifampin
- drug interaction(s) of beta-adrenergic receptor antagonists with ampicillin
- drug interaction(s) of beta-adrenergic receptor antagonists with colestipol
- drug interaction(s) of beta-adrenergic receptor antagonists with cholestyramine
- drug interaction(s) of beta-adrenergic receptor antagonists with barbiturates
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium salts
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum carbonate
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum hydroxide
- drug interaction(s) of beta-adrenergic receptor antagonists with prazosin
- drug interaction(s) of beta-adrenergic receptor antagonists with lidocaine
- drug interaction(s) of beta-adrenergic receptor antagonists with ergot alkaloids
- drug interaction(s) of beta-adrenergic receptor antagonists with clonidine
- drug interaction(s) of beta-adrenergic receptor antagonists with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists (except atenolol) with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with quinolones
- drug interaction(s) of beta-adrenergic receptor antagonists with quinidine
- drug interaction(s) of beta-adrenergic receptor antagonists with propafenone
- drug interaction(s) of beta-adrenergic receptor antagonists with phenothiazines
- drug interaction(s) of beta-adrenergic receptor antagonists with MAO inhibitors
- drug interaction(s) of beta-adrenergic receptor antagonists with loop diuretics
- drug interaction(s) of beta-adrenergic receptor antagonists with hydralazine
- drug interaction(s) of beta-adrenergic receptor antagonists with histamine H2 receptor antagonists
- drug interaction(s) of beta-adrenergic receptor antagonists with haloperidol
- drug interaction(s) of beta-adrenergic receptor antagonists with flecainide
- drug interaction(s) of beta-adrenergic receptor antagonists with oral contraceptives
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium channel blockers
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of beta blockers with ACE inhibitors
- drug interaction(s) of spironolactone with beta blockers
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- class III antiarrhythmic agent
- non-selective beta adrenergic antagonist
- delays repolarization by blocking K+ channels
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Harrison's Principles of Internal Medicine, 13th ed. Isselbacher et al (ed), Companion Handbook, McGraw Hill, NY, 1994
- ↑ Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 160-61
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 6.0 6.1 Medical Knowledge Self Assessment Program (MKSAP) 11, 16. American College of Physicians, Philadelphia 1998, 2012
- ↑ 7.0 7.1 Prescriber's Letter 12(1): 2005 "Pill-in-the-Pocket" Approach to Treating Atrial Fibrillation Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210108&pb=PRL (subscription needed) http://www.prescribersletter.com