Included in the formulation
АТХ:C.07.A.B Selective beta-blockers
C.07.A.09 Esmolol
Pharmacodynamics:Selective β1-adrenoblocker, which does not have internal sympathomimetic activity. It has anti-hypersensitivity, antiarrhythmic, anti-anginal action. In therapeutic doses does not affect the tone of peripheral arteries.
It has a negative foreign, chrono, dromo-, butmotropic effect for 24 hours. Eliminates the effect of arrhythmogenic factors on the heart. Antianginal action is due to a decrease in myocardial oxygen demand.
Pharmacokinetics:After intravenous administration, the maximum concentration is achieved within 5 minutes. The therapeutic effect is achieved 2 minutes after the start of the infusion and lasts for 15-20 minutes after its completion.
Poorly penetrates the blood-brain barrier, penetrates the placenta. When hemodialysis is removed from the blood plasma.
The elimination half-life is 9 minutes.
Partially metabolized in the liver, eliminated by the kidneys in the form of a metabolite.
Indications:Arterial hypertension, sinus tachycardia, supraventricular tachycardia and tachyarrhythmia (including atrial fibrillation and flutter, including during and after surgery), myocardial infarction, unstable angina, thyrotoxic crisis, pheochromocytoma (in combination with α-adrenoblockers).
IV.E00-E07.E05.5 Thyroid crisis or coma
IX.I10-I15.I10 Essential [primary] hypertension
IX.I20-I25.I20.0 Unstable angina
IX.I20-I25.I21 Acute myocardial infarction
IX.I30-I52.I47.1 Nadzheludochkovaya tachycardia
IX.I30-I52.I48 Atrial fibrillation and flutter
Contraindications:Hypersensitivity, sinus bradycardia (less than 45 beats per minute), cardiogenic shock, atrioventricular blockade II-III degree, severe heart failure, sinus node weakness syndrome, sinoatrial block, arterial hypotension (systolic blood pressure below 90 mm Hg. Art. diastolic blood pressure below 50 mm Hg. ), bleeding, hypovolemia.
Carefully:Bronchial asthma, emphysema, chronic obstructive bronchitis, congestive heart failure, diabetes mellitus, impaired renal function; secondary hypertension due to vasoconstriction on the background of hypothermia, during or after operations.
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.
Dosing and Administration:Intravenously at 500 mcg / kg for 1 min, then at 50 mcg / kg for 4 min.Maintenance dose: 25 mcg / kg per min. If there is insufficient efficiency, a repeated dose of 500 μg / kg is introduced, then 100 μg / kg for 4 min. Admissible dose increase up to 150 mcg / kg per min, and then up to 200 mcg / kg per min.
During anesthesia, IV bolus 80 mg is given intravenously for 30 seconds, then as an infusion at a rate of 150-300 μg / kg per min.
Side effects:Central nervous system: dizziness, insomnia, asthenia.
Respiratory system: shortness of breath, rarely - bronchospasm.
The cardiovascular system: bradycardia, atrioventricular blockage, cold extremities.
Blood System: neutropenia, thrombocytopenia.
Sense organs: "dry eye syndrome", transient visual impairment.
Gastrointestinal tract: dyspepsia, diarrhea, or constipation.
Reproductive system: lowering the potency.
Leather: hyperhidrosis.
Allergic reactions.
Overdose:Symptoms: severe bradycardia, arterial hypotension, heart failure, bronchospasm, cardiac arrest is possible.
Treatment: giving the patient a Trendelenburg position, oxygen therapy, intravenous the introduction of fluid (if there is no pulmonary edema); symptomatic therapy: with bradycardia - administration of atropine sulfate, isoproterenol or dobutamine (possibly using epinephrine or conducting transvenous pacing); with heart failure - intravenous the appointment of cardiac glycosides and / or diuretics; with hypotension vasoconstrictors (epinephrine, norepinephrine, dopamine, dobutamine) under control HELL; ventricular extrasystoles are stopped intravenous administration of lidocaine or phenytoin, bronchospasm - beta2-adrenomimetics. maybe intravenous the appointment of glucagon to eliminate bradycardia or hypotension.
Interaction:Potentiates the effect of lidocaine in systemic application.
Strengthens the negative dromo-, ino-, chromotropic effects of amiodarone, anesthetics, antiarrhythmics, diltiazem, verapamil.
Cimetidine increases the bioavailability of esmolol.
Incompatible in one syringe with other means, including with a 5% sodium bicarbonate solution.
Special instructions:When using esmolol, careful and constant medical monitoring and monitoring are necessary ECG, HELL, heart rate and other indicators.
For general anesthesia, patients receiving esmolol, should be used with minimal inotropic action.
It is necessary to stop taking the drug 48 hours prior to surgery.