Esmolol hydrochloride

Описание

Esmolol is an ultra-short acting, cardioselective P-blocker with no intrinsic sympathomimetic activity. The capability of rapid reversal makes esmolol uniquely suitable for the acute management of supraventricular tachycardia and the control of blood pressure and heart rate during surgery or other cardiac emergencies.

Химические свойства

Esmolol Hydrochloride is a white to off-white crystalline powder. It is a relatively hydrophilic compound which is very soluble in water and freely soluble in alcohol. Its partition coefficient (octanol/water) at pH 7.0 is 0.42 compared to 17.0 for propranolol.
Esmolol Hydrochloride has the empirical formula C16H26NO4Cl and a molecular weight of 331.8. It has one asymmetric center and exists as an enantiomeric pair.

Использование

Esmolol hydrochloride is indicated for paroxysmal supraventricular tachycardia, the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. Esmolol hydrochloride is also indicated in noncompensatory sinus tachycardia where, in the physician's judgment, the rapid heart rate requires specific intervention. Esmolol hydrochloride is not intended for use in chronic settings where transfer to another agent is anticipated.

Определение

ChEBI: The hydrochloride salt of esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used in the management of su raventricular arrhythmias, and for the control of hypertension and tachycardia during surgery.

Фармакокине?тика

Esmolol Hydrochloride is a beta1-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Its elimination half-life after intravenous infusion is approximately 9 minutes. Esmolol Hydrochloride inhibits the beta1 receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit beta2 receptors located chiefly in the bronchial and vascular musculature.
Esmolol Hydrochloride is rapidly metabolized by hydrolysis of the ester linkage, chiefly by the esterases in the cytosol of red blood cells and not by plasma cholinesterases or red cell membrane acetylcholinesterase. Total body clearance in man was found to be about 20 L/kg/hr, which is greater than cardiac output; thus the metabolism of Esmolol Hydrochloride is not limited by the rate of blood flow to metabolizing tissues such as the liver or affected by hepatic or renal blood flow. Esmolol Hydrochloride has a rapid distribution half-life of about 2 minutes and an elimination half-life of about 9 minutes.

Побочные эффекты

Hypotension (in 20-50% of pts), diaphoresis, pallor, flushing, peripheral ischemia, bradycardia, heart block, heart failure, sudden cardiac death.
Dizziness, confusion, headache, fatigue, anxiety.
Nausea, vomiting, fever.
Bronchospasm, cough, wheeziness, nasal stuffiness.
Urinary retention.
Inflammation and induration at injection site.