Comparative Pharmacology
Head-to-head clinical analysis: BRETYLIUM TOSYLATE IN DEXTROSE 5 IN PLASTIC CONTAINER versus DOFETILIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BRETYLIUM TOSYLATE IN DEXTROSE 5 IN PLASTIC CONTAINER versus DOFETILIDE.
BRETYLIUM TOSYLATE IN DEXTROSE 5% IN PLASTIC CONTAINER vs DOFETILIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bretylium tosylate inhibits norepinephrine release from adrenergic nerve terminals by blocking neuronal reuptake and causing initial norepinephrine release followed by depletion. It also exhibits class III antiarrhythmic activity by prolonging the action potential duration and refractory period in cardiac Purkinje fibers and ventricular muscle.
Selectively blocks the rapid component of the delayed rectifier potassium current (Ikr) in cardiac myocytes, prolonging repolarization and the effective refractory period.
For ventricular tachycardia/fibrillation: 5 mg/kg IV over 8-10 minutes, then 5-10 mg/kg IV q6-8h. For continuous infusion: 1-2 mg/min IV.
250-500 mcg orally twice daily, based on creatinine clearance and QTc response.
None Documented
None Documented
Clinical Note
moderateDofetilide + Levofloxacin
"Dofetilide may increase the QTc-prolonging activities of Levofloxacin."
Clinical Note
moderateDofetilide + Norfloxacin
"Dofetilide may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderateDofetilide + Gemifloxacin
"Dofetilide may increase the QTc-prolonging activities of Gemifloxacin."
Clinical Note
moderateDofetilide + Torasemide
"Dofetilide may increase the QTc-prolonging activities of Torasemide."
Terminal half-life: 7-11 hours (normal renal function); prolonged in renal impairment (up to 16-32 hours in anuria)
Terminal elimination half-life: 10 hours (range 7–13 hours) in patients with normal renal function; prolonged in renal impairment, up to 20 hours in moderate impairment and >30 hours in severe impairment.
Renal: >80% unchanged; biliary/fecal: minimal (<5%)
Renal: 80% unchanged; biliary/fecal: 20% as metabolites and unchanged drug.
Category C
Category C
Antiarrhythmic (Class III)
Antiarrhythmic (Class III)