Comparative Pharmacology
Head-to-head clinical analysis: BRETYLIUM TOSYLATE IN DEXTROSE 5 versus BRETYLOL.
Head-to-head clinical analysis: BRETYLIUM TOSYLATE IN DEXTROSE 5 versus BRETYLOL.
BRETYLIUM TOSYLATE IN DEXTROSE 5% vs BRETYLOL
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.
Bretylium tosylate is an adrenergic neuron blocking agent that inhibits norepinephrine release and enhances its reuptake, resulting in postganglionic sympathetic blockade. It also has direct antiarrhythmic effects by increasing the ventricular fibrillation threshold.
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.
Intravenous: 5-10 mg/kg over 10 minutes, then 5-10 mg/kg every 6-8 hours as needed for arrhythmias. Intramuscular: 5-10 mg/kg, may repeat every 6-8 hours.
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 elimination half-life is 7-11 hours in normal renal function; prolonged in renal impairment (up to 30 hours)
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 renal excretion of unchanged drug (80-90%); minor biliary/fecal elimination (10-20%)
Category C
Category C
Antiarrhythmic (Class III)
Antiarrhythmic (Class III)