Bretylium (Tosylate)

Drug #103

Bretylium (Tosylate) is a potassium channel blocking agent. Bretylium (Tosylate) is a quaternary salt and is an adrenergic neurona blocking agent. It was first introduced as an antihypertensive agent.Bretylium (Tosylate) is now used as an antiarrhythmic agent. It interferes with the neuronal release of catecholamines but also has direct antiarrhythmic properties.

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Primary Characteristics

It is of Synthetic origin and belongs to Toluene sulphonate.

It belongs to Adrenergic Neurone Blockade pharmacological group on the basis of mechanism of action and also classified in Anti arrhythmic agents pharmacological group.

Molecular Weight: 414.4 · pK_a: not relevant · Solubility in Water: 1 in 1 · Solubility in Alcohol: 1 in 0.4 · Non-proprietary name: Bretylium (Tosylate).

Molecular structure of Bretylium (Tosylate)

Pharmacokinetics

Absorption: Bretylium (Tosylate) has an oral bioavailability is 15% (±10%), pre-systemic (first-pass) metabolism accounts for 3% (±2%).

Distribution: Bretylium (Tosylate) has a volume of distribution is 3.4-8.2 l/kg. plasma protein binding is < 10%.

Elimination: it is metabolised via Insignificant, plasma half-life is 10 hr, renal excretion is 100%.

Indications

Bretylium (Tosylate) is primarily indicated in conditions like Prophylaxis of acid aspiration in obstetrics, Ventricular arrhythmias.

Contraindications

Bretylium (Tosylate) is contraindicated in conditions like Cardiac arrhythmia, Myocardial infarction, Digitalis induced arrythmias.

Dosage

Bretylium (Tosylate)'s dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
7.5 mg/kg	7.5 mg/kg	—	IM	Maintenance, Every 6-8 Hours, As Required
7.5 mg/kg	7.5 mg/kg	—	IV	Load for every 15-30 minutes for 3 doses
0.021 mg/kg.min	0.021 mg/kg.min	—	IV Inf	Maintenance, As Required
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown4 interactions

1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Bretylium (Tosylate) produces potentially life-threatening effects which include Hypotension. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Bretylium (Tosylate) are Severe hypotension.

Bretylium (Tosylate) is known to cause more or less tolerable side effects which are usually transient. These include Facial flushing, Nausea and vomiting, Parotid pain and swelling, Transient diplopia, Transient increase in blood pressure.

Warnings / Precautions

Increase dose interval of bretylium in renal dysfunction. Dilute for IV use except in treating existing ventricular fibrillation where it should be given as rapidly as possible.

Available Brands

None recorded.

Storage Conditions

Bretylium (Tosylate) should be stored Inj.

Drug Classification

1.12.2 — Antiarrhythmic drugs