Эсмолол

Использование

Esmolol is a cardioselective beta1 receptor blocking agent.

Опасность

A reproductive hazard.

Клиническое использование

Esmolol (Brevibloc) is a short-acting intravenously administered β1-selective adrenoceptor blocking agent. It does not possess membrane-stabilizing activity or sympathomimetic activity.
Esmolol is used in the treatment of supraventricular tachyarrhythmias for rapid control of ventricular rate and reduction of myocardial oxygen consumption. Discontinuation of administration is followed by a rapid reversal of its pharmacological effects because of esmolol’s rapid hydrolysis by plasma esterases.

Побочные эффекты

The most frequently reported adverse effects are hypotension, nausea, dizziness, headache, and dyspnea.As with many β-blocking drugs, esmolol is contraindicated in patients with overt heart failure and those in cardiogenic shock.

Метаболизм

The -blocker esmolol (Brevibloc) is unusual in that it is very rapidly metabolized; its plasma half-life is only 9 minutes. It is subject to hydrolysis by cytosolic esterases in red blood cells to yield methanol and an acid metabolite, the latter having an elimination half-life of about 4 hours. Only 2% of the administered esmolol is excreted unchanged. Because of its rapid onset and short duration of action, esmolol is used by the intravenous route for the control of ventricular arrhythmias in emergencies.