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Indications and Dosage
Parenteral
Ventricular arrhythmias Adult: Life-threatening cases: Initially, 5 mg/kg as rapid IV inj, may increase to 10 mg/kg and repeat at 15-30 min intervals if arrhythmia persists. Max: 30 mg/kg. Other ventricular arrhythmias: 5-10 mg/kg by IM or IV inj over >8 min, may repeat in 1-2 hr if arrhythmia persists. Maintenance: IM: 5-10 mg/kg 6-8 hrly. IV: 5-10 mg/kg over >8 min 6 hrly as intermittent infusion or 1-2 mg/min as continuous infusion.
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Contraindications
Prevention of arrhythmias in patients w/ recent MI. Concomitant use w/ digitalis glycosides, unless arrhythmia is unrelated to digitalis toxicity and resistant to other therapy.
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Special Precautions
Patient w/ fixed cardiac output (e.g severe aortic stenosis or pulmonary HTN), bradycardia. Renal impairment.
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Adverse Reactions
Hypotension, dizziness, light-headedness, vertigo, transient increase in BP and heart rate, worsening of cardiac arrhythmias, nausea, vomiting; local tissue necrosis and muscle atrophy (IM).
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Monitoring Parameters
Monitor ECG, BP and renal function.
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Drug Interactions
May enhance the effects of sympathomimetics.
Potentially Fatal: May exacerbate arrhythmias when used w/ digitalis glycoside. |
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Action
Description:
Mechanism of Action: Bretylium tosilate is a quaternary ammonium compound w/ class III antiarrhythmic activity that prolongs the duration of action potential and effective refractory period in Purkinje fibers and ventricular tissues. It accumulates in sympathetic ganglia and postganglionic adrenergic neurons, causing an initial release of norepinephrine and subsequent blockade of adrenergic transmission by preventing further release from adrenergic nerve endings. Onset: Delayed 20 min and up to 6 hr. Pharmacokinetics: Absorption: Well absorbed (IM). Distribution: Minimally distributed in CNS. Plasma protein binding: <5%. Excretion: Via urine (80-90% as unchanged drug). Elimination half-life: 5-10 hr. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Bretylium tosylate, CID=6100, https://pubchem.ncbi.nlm.nih.gov/compound/Bretylium-tosylate (accessed on Jan. 21, 2020) |
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Storage
Store between 15-30°C. Protect from light.
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MIMS Class
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ATC Classification
C01BD02 - bretylium tosilate ; Belongs to class III antiarrhythmics.
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References
Anon. Bretylium. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 19/08/2016. Buckingham R (ed). Bretylium tosilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/08/2016.
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