Comparative Pharmacology
Head-to-head clinical analysis: BRETYLIUM TOSYLATE IN DEXTROSE 5 versus CORDARONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BRETYLIUM TOSYLATE IN DEXTROSE 5 versus CORDARONE.
BRETYLIUM TOSYLATE IN DEXTROSE 5% vs CORDARONE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bretylium tosylate is an antiarrhythmic agent that prolongs the action potential duration and refractory period in cardiac tissue. It initially causes release of norepinephrine from sympathetic nerve endings, followed by inhibition of norepinephrine release. It has class III antiarrhythmic properties and also exhibits adrenergic blockade.
Class III antiarrhythmic agent; prolongs action potential duration and refractory period via blockade of potassium channels; also exhibits class I, II, and IV properties including sodium channel blockade, non-competitive beta-adrenergic blockade, and calcium channel blockade.
Intravenous: 5-10 mg/kg infused over 10-30 minutes, may repeat at 30-minute intervals up to a total of 30 mg/kg; maintenance: 1-2 mg/min as continuous IV infusion or 5-10 mg/kg every 6 hours by intermittent infusion. Intramuscular: 5-10 mg/kg undiluted, repeat every 1-2 hours as needed.
Loading dose: 800-1600 mg/day orally in divided doses for 1-3 weeks, then 600-800 mg/day for 1 month, then maintenance: 200-400 mg/day. IV: Loading 150 mg over 10 minutes, then 1 mg/min for 6 hours, then 0.5 mg/min.
None Documented
None Documented
Terminal elimination half-life is approximately 7-11 hours in patients with normal renal function, but can be prolonged to >24 hours in renal impairment or anuria, necessitating dose adjustment.
Terminal half-life ranges 40–70 days (mean 55 days) due to extensive tissue accumulation, particularly in adipose tissue. Prolonged half-life necessitates loading doses and long washout periods.
Primarily excreted unchanged by the kidneys via glomerular filtration and tubular secretion; >70% of an administered dose recovered in urine within 24 hours; negligible biliary/fecal elimination.
Primarily hepatic metabolism with biliary excretion; minimal renal elimination (<1% unchanged). Fecal excretion accounts for ~70% of the dose. Less than 10% excreted in urine.
Category C
Category C
Antiarrhythmic (Class III)
Antiarrhythmic (Class III)