Esmolol Hydrochloride Injection

Esmolol hydrochloride injection is a selective beta-1 adrenergic receptor blocker with rapid onset and short duration of action. It mainly acts on beta-1 adrenergic receptors of the myocardium, and also has a blocking effect on beta-2 adrenergic receptors of tracheal and vascular smooth muscle at high doses. It has no intrinsic sympathomimetic effect or membrane stabilizing effect at therapeutic doses. It can reduce the heart rate of normal people during exercise and rest, and counteract the heart rate increase caused by isoproterenol. Its antihypertensive effect is correlated with the degree of beta-adrenergic receptor blockade. The beta-adrenergic receptor blocking effect basically disappears 10 to 20 minutes after the intravenous injection is stopped. Electrophysiological studies suggest that esmolol hydrochloride injection has typical beta-adrenergic receptor blocker effects: reducing heart rate, reducing sinoatrial node automaticity, prolonging sinoatrial node recovery time, prolonging the AH interval during sinus rhythm and atrial rhythm, and prolonging the forward Wen-style conduction cycle. Radionuclide cardiac blood pool angiography suggests: At a dose of 0.2 mg/kg/min, this product can reduce resting heart rate, systolic blood pressure, heart rate-blood pressure product, left and right ventricular ejection fraction and cardiac index, and its effect is similar to that of intravenous injection of 4 mg propranolol (propranolol). Under exercise, esmolol hydrochloride injection is similar to propranolol, both of which can slow down heart rate, reduce heart rate-blood pressure product and cardiac index, but the effect of reducing systolic blood pressure is more obvious. Cardiovascular angiography suggests: At a dose of 0.3 mg/kg/min, in addition to causing the above effects, this product can also cause a slight increase in left ventricular end-diastolic pressure and pulmonary artery wedge pressure. Hemodynamic parameters will be completely restored 30 minutes after stopping the drug.

Main ingredients and chemical name: 4-(3-isopropylamino-2-hydroxypropoxy)phenylpropanoic acid methyl ester hydrochloride Molecular formula: C16H25NO4HCl Molecular weight: 331.84

1. Used to control ventricular rate in atrial fibrillation and atrial flutter. 2. Perioperative hypertension. 3. Sinus tachycardia.

1. To control the ventricular rate of atrial fibrillation and atrial flutter, adults should first receive a loading dose of 0.5 mg/kg/min intravenously for about 1 minute, followed by an intravenous drip maintenance dose: starting from 0.05 mg/kg/min, and continuing to maintain after 4 minutes if the therapeutic effect is satisfactory. If the therapeutic effect is not good, the loading dose can be repeated and the maintenance dose can be increased by 0.05 mg/kg/min. The maintenance dose can be increased to a maximum of 0.3 mg/kg/min, but doses above 0.2 mg/kg/min have not been shown to bring significant benefits. 2. The immediate control dose for perioperative hypertension or tachycardia is: 1 mg/kg intravenously within 30 seconds, and then 0.15 mg/kg/min intravenously, with a maximum maintenance dose of 0.3 mg/kg/min. Gradually control the dose with the same treatment of supraventricular tachycardia. The dose used to treat hypertension is usually larger than that used to treat arrhythmias.

Most adverse reactions are mild and transient. The most important adverse reaction is hypotension. There have been reports of death from the use of esmolol simply to control ventricular rate. 1. Incidence; 1% adverse reactions: hypotension during injection (63%), persistent hypotension after stopping medication (80%), asymptomatic hypotension (25%), symptomatic hypotension (sweating, dizziness) (12%), sweating with hypotension (10%), injection site reactions including inflammation and intolerance (8%), nausea (7%), dizziness (3%), drowsiness (3%). 2. Adverse reactions with an incidence of 1%: peripheral ischemia, confusion, headache, irritability, fatigue, vomiting. 3. Incidence: 1% adverse reactions: hemiplegia, weakness, depression, abnormal thinking, anxiety, lack of appetite, mild headache, epileptic seizure, bronchial spasm, snoring, dyspnea, nasal congestion, dry rales, wet rales, indigestion, constipation, dry mouth, abdominal discomfort, taste perversion, injection site edema, erythema, skin discoloration, burning sensation, thrombophlebitis and extravasation skin necrosis, urinary retention, speech disorders, visual abnormalities, mid-scapular pain, chills, fever.

1 Bronchial asthma or history of bronchial asthma. 2 Severe chronic obstructive pulmonary disease. 3 Sinus bradycardia. 4 Second to third degree atrioventricular block. 5 Refractory heart failure. 6 Cardiogenic shock. 7 Allergic to this product.

When used in combination with sympathetic ganglion blockers, there will be a synergistic effect, and hypotension, bradycardia, and syncope should be prevented. When used in combination with warfarin, the blood concentration of this product seems to increase, but it has little clinical significance. When used in combination with digoxin, the blood concentration of digoxin can increase by 10%-20%. When used in combination with morphine, the steady-state blood concentration of this product will increase by 46%. When used in combination with succinylcholine, the neuromuscular blocking effect of succinylcholine can be prolonged by 5 to 8 minutes. This product will reduce the efficacy of adrenaline. This product combined with verapamil in patients with poor heart function will cause cardiac arrest.

Keep away from light and store in sealed container.

1ml:0.1g

Beijing Tide Pharmaceutical Co., Ltd.

• Founded in:

  1995-05-29

• Address:

  No. 8 Rongjing East Street, Beijing Economic and Technological Development Zone, Beijing

• Tax NO.:

  911103026000314683

• Registered Funds:

  500 million yuan

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