Esmolol Hydrochloride for Injection

1 Pharmacological action This product is a selective beta-1 adrenergic receptor blocker with rapid onset and short duration of action. It mainly acts on the beta-1 adrenergic receptors of the myocardium, and also has a blocking effect on the beta-2 adrenergic receptors of the trachea and vascular smooth muscle at high doses. There is 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 that 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 that at a dose of 0.3 mg/kg/min, this product can cause a slight increase in left ventricular end-diastolic pressure and pulmonary artery wedge pressure in addition to the above effects, and the hemodynamic parameters will be completely restored 30 minutes after stopping the drug. 2 Carcinogenicity, mutagenicity and reproductive toxicity Due to the ultra-short-term use of esmolol hydrochloride injection, there are no research results on its carcinogenicity, mutagenicity and reproductive effects.

Esmolol hydrochloride Chemical name: 4-(3-isopropylamino-2-hydroxypropoxy)phenylpropanoic acid methyl ester hydrochloride Molecular formula: C16H25NO4HCl Molecular weight: 331.84

This product is freeze-dried powder injection

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

1. Control of ventricular rate during atrial fibrillation and atrial flutter: For adults, first give a loading dose of 0.5 mg/kg/min intravenously for about 1 minute, followed by intravenous drip maintenance dose: start with 0.05 mg/kg/min, and continue to maintain after 4 minutes if the effect is satisfactory. If the effect is not good, the loading dose can be repeated and the maintenance amplitude 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. Perioperative hypertension or tachycardia: (1) Immediate control dose: 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. (2) Gradually control the dose as for supraventricular tachycardia treatment. (3) The dose used to treat hypertension is usually larger than that used to treat arrhythmia.

Most adverse reactions are mild and transient. The most important adverse reaction is hypotension. There have been reports of death when esmolol was used simply to control ventricular rate. 1. Adverse reactions with an incidence of 1%: 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%), and drowsiness (3%). 2. Adverse reactions with an incidence of 1%: peripheral ischemia, confusion, headache, irritability, fatigue, and vomiting. 3. Adverse reactions with an incidence of <1%: hemiplegia, weakness, depression, abnormal thinking, anxiety, lack of appetite, mild headache,

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

Precautions for children: There is no data on the use of this product in children. Precautions for pregnancy and lactation: A teratogenicity study of this product on rats was conducted. A dose of 3mg/kg/min was given by intravenous drip for 30 minutes every day. No toxicity or teratogenicity was found on pregnant rats and fetuses. However, a dose of 10mg/kg/min was toxic and lethal to pregnant rats. A teratogenicity study on rabbits found that a dose of 1mg/kg/min was given by intravenous drip for 30 minutes every day. No toxicity or teratogenicity was found on pregnant rabbits and fetuses. However, a dose of 2.5mg/kg/min was toxic to pregnant rabbits and increased the mortality rate of fetuses. There is a lack of corresponding research data on the use of this product in pregnant women, but there are reports that the use of this product in the last three months of pregnancy or during delivery can cause fetal bradycardia, which cannot be stopped after stopping the drug. Therefore, this product can only be used in pregnant women when it is very necessary. It is not known whether this product can be secreted through breast milk. Lactating women who take the drug should stop breastfeeding. Precautions for the elderly: The use of this product in the elderly has not been fully studied. However, the elderly are sensitive to the antihypertensive and heart rate lowering effects and have poor renal function, so caution should be exercised when using this product.

1. When used in combination with sympathetic ganglion blockers, there will be a synergistic effect, and hypotension, bradycardia, and syncope should be prevented. 2. When used in combination with warfarin, the blood concentration of this product seems to increase, but it has little clinical significance. 3. When used in combination with digoxin, the blood concentration of digoxin can increase by 10%-20%. 4. When used in combination with morphine, the steady-state blood concentration of this product will increase by 46%. 5. When used in combination with succinylcholine, the neuromuscular blocking effect of succinylcholine can be prolonged by 5 to 8 minutes. 6. This product will reduce the efficacy of adrenaline. 7. When used in combination with verapamil in patients with poor heart function, this product will cause cardiac arrest.

Keep away from light and store in sealed container.

0.1g

18 months

Harbin Medisan Pharmaceutical Co., Ltd.

• Founded in:

  1996-06-21

• Address:

  Beijing Road, Limin Development Zone, Harbin

• Tax NO.:

  91230100607168790X

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  316.35755 million yuan

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