Sotalol

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Contraindications 4 Dosage 5 Dosage-adjustment-in-renal-failure 6 Pharmacokinetics 7 Adverse-effects 8 Drug-interactions 9 Mechanism-of-action 10 More General Terms 11 Internet Database 12 References

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 severe LV systolic dysfunction
  

• pregnancy category = b
• safety in lactation = ?

Dosage

• intiate 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

*  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%)

• bradycardia, depression, sexual dysfunction

• less common (1-10%)

• dyspnea, confusion, congestive heart failure, hallucinations, reduced peripheral circulation, anxiety, constipation, diarrhea, dizziness, drowsiness, itching, nausea/vomiting, nightmares, epigastric discomfort, insomnia, weakness, tiredness

• 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

• hypokalemia
• hypomagnesemia
• diuretic use

• 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 antiarrhythmic agent, Group III

Drug-interactions

• cardiac effects additive with Ca+2-channel blockers
• excessive reduction of sympathetic tone when used with:

• reserpine
• bretylium
• guanethidine

• 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 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 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 ACE inhibitors, angiotensin II receptor antagonists & beta-blockers

Mechanism-of-action

• class III antiarrhythmic agent
• non-selective beta adrenergic antagonist
• delays repolarization by blocking K+ channels

More General Terms

• antiarrhythmic agent, Group III
• non-specific beta-adrenergic receptor antagonist

Internet Database

PubChem: 5253
PubChem: 66245
PubChem: 165245

References

1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
2. Harrison's Principles of Internal Medicine, 13th ed. Isselbacher et al (ed), Companion Handbook, McGraw Hill, NY, 1994
3. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 160-61
4. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
5. Kaiser Permanente Northern California Regional Drug Formulary, 1998
6. Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
7. Prescriber's Letter 12(1): 2005 "Pill-in-the-Pocket" Approach to Treating Atrial Fibrillation Detail-Document#: [1] (subscription needed) [2]

sotalol (Betapace, Sotacor)