Bretylium

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Bretylium
Systematic (IUPAC) name
N-(2-bromobenzyl)-N,N-dimethylethanaminium
Clinical data
MedlinePlus a682861
Pregnancy cat. C (AU) C (US)
Legal status -only (US)
Routes IV, IM
Pharmacokinetic data
Bioavailability NA
Protein binding NA
Metabolism None
Half-life 7-8 hours
Excretion Renal
Identifiers
CAS number 59-41-6 YesY
ATC code C01BD02
PubChem CID 2431
DrugBank DB01158
ChemSpider 2337 YesY
UNII RZR75EQ2KJ YesY
KEGG D00645 N
ChEBI CHEBI:3172 YesY
ChEMBL CHEMBL1199080 N
Chemical data
Formula C11H17BrN+
Mol. mass 243.163 g/mol
 N (what is this?)  (verify)

Bretylium (also bretylium tosylate) is an antiarrhythmic agent.1 It blocks the release of noradrenaline from nerve terminals. In effect, it decreases output from the peripheral sympathetic nervous system. It also acts by blocking K+ channels and is considered a class III antiarrhythmic. The dose is 5-10 mg/kg and side effects are hypertension followed by hypotension and ventricular ectopy.

It was patented in 1978 by Marvin Bacaner at the University of Minnesota.2

Uses

It is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. 3

It is contraindicated in patients with AV (atrioventricular) heart block or digoxin toxicity.

Bretylium should be used only in an ICU or Emergency Department setting and should not be used elsewhere due to its dramatic actions and its predominant side effect of hypotension.

References

  1. ^ Tiku PE, Nowell PT (December 1991). "Selective inhibition of K(+)-stimulation of Na,K-ATPase by bretylium". Br. J. Pharmacol. 104 (4): 895–900. PMC 1908819. PMID 1667290. 
  2. ^ "University of Minnesota: Scholars Walk". Retrieved 2008-09-23. 
  3. ^ "ACS". Retrieved 2008-09-23. dead link