Bretylium Tosylate

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Cat Number

API0231559

CAS Number

61-75-6

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Product Detail Description Customer Q&A

CAS Number

61-75-6

EINECS

200-516-8

Storage

Store at room temperature

Synonyms

Bretylol; Bretylium tosilate; Darentin; Tosilato de bretilio; Tosilate de bretylium; Bretylii tosilas; ASL-603; Bretilio tosilato

Molecular Formula

C18H24BrNO3S

Molecular Weight

414.4

Smiles

CC[N+](C)(C)CC1=CC=CC=C1Br.CC1=CC=C(C=C1)S(=O)(=O)[O-]

Appearance

White to off-white crystalline powder

Melting Point

97-99℃

General Description

Bretylium tosylate is a class III antiarrhythmic agent that also exhibits class II (antiadrenergic) properties, used primarily in emergency settings for the treatment of life-threatening ventricular arrhythmias. It is administered intravenously or intramuscularly and acts by suppressing ventricular fibrillation and ventricular tachycardia. The drug is a quaternary ammonium compound that accumulates in sympathetic ganglia and nerve terminals.

Mechanism of Action

Bretylium initially causes release of norepinephrine from adrenergic nerve endings, transiently increasing heart rate and blood pressure. This is followed by blockade of norepinephrine release, resulting in chemical sympathectomy. The antiarrhythmic effect is due to prolongation of the cardiac action potential duration and refractory period in the ventricles, suppressing reentry circuits. It also raises the ventricular fibrillation threshold.

Application

It is indicated for the treatment of ventricular fibrillation and hemodynamically unstable ventricular tachycardia that is unresponsive to other antiarrhythmics, particularly in the setting of acute myocardial infarction. However, its use has declined significantly due to the availability of more effective and safer agents such as amiodarone. It remains available as a second-line agent in advanced cardiac life support protocols.

Does Bretylium Tosylate require protection from light during long-term storage?

Yes, it is photosensitive. Prolonged UV exposure can cause photodegradation. Store in light-resistant containers, preferably amber glass or opaque packaging.

What is the recommended storage temperature for Bretylium Tosylate?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can cause discoloration and accelerate decomposition.

Is Bretylium Tosylate hygroscopic, and how is this managed?

It is moderately hygroscopic. Storage in tightly sealed containers with desiccant is recommended, especially in high-humidity environments, to prevent caking.

How is the impurity 2-bromoethyl tosylate monitored during stability?

This genotoxic impurity is controlled using a highly sensitive GC-MS method, ensuring levels are below the threshold of toxicological concern (TTC).