BRETYLIUM TOSYLATE C화학적 특성, 용도, 생산
화학적 성질
White Solid
용도
Bretylium tosylate has a biphasic response, initially inducing norepinephrine release followed by sympathetic ganglionic blockade. Bretylium tosylate is a class III antiarrhythmic agent and a competitive inhibitor of acetylcholinesterase.
정의
ChEBI: The tosylate salt of bretylium. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibril
ation.
일반 설명
Bretylium tosylate, (o-bromobenzyl)ethyl dimethylammonium p-toluenesulfonate(Bretylol), is an extremely bitter, white, crystalline powder.The chemical is freely soluble in water and alcohol.Bretylium tosylate is an adrenergic neuronal-blockingagent that accumulates selectively in the neurons anddisplaces norepinephrine. Because of this property,bretylium was used initially, under the trade name ofDarenthin, as an antihypertensive agent. It caused posturaldecrease in arterial pressure. This use was discontinuedbecause of the rapid development of tolerance, erratic oralabsorption of the quaternary ammonium compound, andpersistent pain in the parotid gland on prolonged therapy.
Clinical Use
Currently, bretylium is reserved for use in ventriculararrhythmias that are resistant to other therapy. Bretyliumdoes not suppress phase 4 depolarization, a common actionof other antiarrhythmic agents. It prolongs the effectiverefractory period relative to the action potential durationbut does not affect conduction time and is categorized asa class III antiarrhythmic agent. Because bretylium doesnot have properties similar to those of the other antiarrhythmicagents, it has been suggested that its action is aresult of its adrenergic neuronal-blocking properties; theantiarrhythmic properties of the drug, however, are notaffected by administration of reserpine. Bretylium is also alocal anesthetic, but it has not been possible to demonstratesuch an effect on atria of experimental animals, except atvery high concentrations. Therefore, the precise mechanismof the antiarrhythmic action of bretylium remains tobe resolved.
부작용
The major adverse effect associated with bretylium tosylate is hypotension, including
orthostatic hypotension, which may be very severe.
BRETYLIUM TOSYLATE 준비 용품 및 원자재
원자재
준비 용품
