Breviblock, ampoules 10mg/ml, 10ml, 5pcs

Composition

1 ml of the drug contains:

Active ingredient:  

esmolol hydrochloride 10 mg;

excipients:  

sodium chloride 5.9 mg,

sodium acetate trihydrate 2.8 mg,

glacial acetic acid 0.546 mg,

hydrochloric acid up to pH 5.0,

sodium hydroxide up to pH 5.0,

water for injection up to 1 ml

Pharmacological action

Esmolol is a cardioselective blocker of beta-1-adrenergic receptors, which has a rapid onset of action, a very short duration of action, and in therapeutic doses does not have its own sympathomimetic and membrane-stabilizing activity; it has antianginal, antihypertensive and antiarrhythmic effects.

Reduces the catecholamine-stimulated formation of cyclic adenosine monophosphate from adenosine triphosphate, reduces the intracellular flow of calcium ions, reduces heart rate( HR), slows down conduction, and reduces myocardial contractility.

The antiarrhythmic effect is determined by the inhibition of pulse conduction in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular node and along additional pathways.

The action begins from the moment of use, the full therapeutic effect develops 2 minutes after use and ends 10-20 minutes after the infusion is stopped.

Esmolol by its chemical nature belongs to the class of phenoxypropanolamine beta-blockers. It has an enzymatically labile ester unit, as a result of which it is rapidly metabolized and has a short half-life from blood plasma.

Esmolol, like other beta-blockers, has a negative ino -, chrono -, batmo – and dromotropic effect.

In patients over 65 years of age, there were no differences in hemodynamic effects compared to younger patients.

Indications

• Arterial hypertension,
• hypertensive crises of various etiologies,
• sinus tachycardia,
• supraventricular tachycardia and tachyarrhythmia (including atrial fibrillation and flutter, including during and after surgery);
• thyrotoxic crisis,
• myocardial infarction,
• pheochromocytoma,
• unstable angina.

Use during pregnancy and lactation

The safety of using Breviblock in pregnant women has not been studied.

Due to the lack of data on the possibility of Breviblock penetration into mother’s milk, it is not recommended to use it during lactation.

Contraindications

– Hypersensitivity to the components of the drug;

– severe bradycardia (heart rate less than 50 beats/min);

– syndrome of weakness of the sinus node;

– atrioventricular block II and III degree;

– cardiogenic shock;

– severe arterial hypotension;

acute heart failure;

pulmonary hypertension;

– pheochromocytoma without the simultaneous use of alpha-blockers;

– age under 18 years;

– simultaneous intravenous blocker of “slow” calcium channels (verapamil, diltiazem).

With caution:

– Atrioventricular block I degree;

– bronchial asthma, chronic obstructive pulmonary disease;

– disorders of peripheral blood circulation (Raynaud’s syndrome, “intermittent” claudication);

– chronic heart failure;

– violation of kidney function;

– hyperkalemia;

– tireotoxicose;

– psoriasis;

– myasthenia gravis;

– Prinzmetal’s angina;

– hypovolemia;

– pheochromocytoma (with simultaneous use of alpha-blockers);

old age;

– pregnancy;

– diabetes;

– secondary hypertension (caused by vasoconstriction, during, or after surgery, against the background of hypothermia).

Side effects

Nervous system and sensory disorders: rarely-feeling tired, drowsy, confused, headache, dizziness, speech and/or vision disorders, agitation.

Cardiovascular and blood disorders (hematopoiesis, hemostasis): rarely-hypotension, signs of peripheral ischemia, bradycardia, palpitation, thrombophlebitis.

Other services: rarely-chills, fever, dyspnoea, bronchospasm, constipation, urinary retention, burning, induration or infiltration of the skin around the injection site (with extravasation).

Interaction

Increases the concentration of digoxin in the blood, enhances the hypotensive effect of inhaled anesthetics, prolongs the muscle relaxant effect of succinylcholine (1.5 times).

Morphine and warfarin increase the concentration in the blood.

How to take, course of use and dosage

For intravenous use only!

Only for short-term use!

Do not add any additional ingredients to the bottle!

Do not use in case of discoloration or precipitation! Destroy any unused leftovers!

Avoid contact with alkalis!

The loading dose of 0.5 mg / kg / min for a 70 kg patient is 3.5 ml.

The dose of the drug should be selected individually, based on the clinical response. Doses should be titrated according to ventricular rhythm and, if necessary, blood pressure (BP).

BREVIBLOCK should be administered with caution in patients with impaired renal function (see section “Special instructions”).

Supraventricular tachycardia, including atrial fibrillation and atrial flutter

The effective dose of the drug for the treatment of supraventricular tachyarrhythmia is 50-200 mcg/kg/min. To control ventricular rhythm, maintenance infusion doses above 200 mcg / kg / min are not recommended; doses above 200 mcg/kg / min provide a slight decrease in heart rate, while the frequency of adverse reactions increases. However, higher doses (250-300 mcg/kg/min) may be required for adequate blood pressure control.

The safety of doses above 300 mcg / kg / min has not been studied. The dose of the drug for supraventricular tachyarrhythmia should be selected individually by titration, in which each step includes a loading dose, followed by a maintenance dose.

Scheme of starting and conducting treatment

use of a loading dose of 500 mcg / kg / min for I min, followed by a maintenance dose of 50 mcg / kg / min for 4 min*.

If the result is positive:

use of a maintenance dose of 50 mcg/kg/min.

If the result is negative within 5 minutes:

Repeat the use with a dose of 500 mcg/kg/min for 1 min.

Increase the maintenance dose to 100 mcg/kg/min for the next 4 minutes.

If the result is positive:

use of a maintenance dose of 100 mcg/kg/min.

If the result is negative within 5 minutes:

Repeat the use with a dose of 500 mcg/kg/min for 1 min.

Increase the maintenance dose to 150 mcg/kg/min for the next 4 minutes.

If the result is positive:

use of a maintenance dose of 150 mcg/kg/min.

If the result is negative:

Repeat the use with a dose of 500 mcg / kg / min for I min.

Increase the maintenance dose to 200 mcg/kg/min and leave it at this level.

* If the desired end value of heart rate is reached, but blood pressure decreases, it is necessary to STOP the loading dose and reduce the rate with maintenance use from 50 mcg / kg / min to 25 mcg/kg / min or lower. If necessary, the time interval between titration steps can be increased from 5 to 10 minutes,

Note:  There is no evidence that maintenance doses above 200 mcg / kg / min lead to a greater therapeutic effect. The safety of doses above 300 mcg / kg / min has not been studied.

After achieving the necessary heart rate and stable clinical condition in patients with supraventricular tachycardia, you can switch to other antiarrhythmic drugs, for example, such as verapamil, propranolol or metoprolol, digoxin or quinidine.

The recommended procedure for this transition is described below, but the attending physician should follow the instructions for using alternative medications.

The dose of the drug should be reduced as follows:

1. During the first hour after the first dose of an alternative drug, reduce the rate of use of BREVIBLOCK by 2 times.

2. After the second dose of an alternative drug, it is necessary to monitor H

Drug use for more than 24 hours was not evaluated. use of the drug lasting more than 24 hours should be performed with caution.

Tachycardia and arterial hypertension in the perioperative period

When treating tachycardia and / or arterial hypertension in the perioperative period, the following dosage regimens should be used: :

a) During intraoperative treatment – under general anesthesia, when ventricular rhythm control is required-enter a bolus loading dose of 80 mg for 15-30 seconds, followed by an infusion at a dose of 150 mcg / kg / min. Titrate the rate of use, if necessary, to 300 mcg / kg / min

. b) After coming out of general anesthesia, perform an infusion at a rate of 500 mcg / kg / min for 4 minutes, followed by an infusion of 300 mcg/kg / min

. ) In the postoperative period, when the time for titration of the dose allows, a loading dose of 500 mcg/kg/min is given for 1 min before each titration step to ensure a rapid onset of action of the drug. Titration steps of 50,100,150,200,250 and 300 mcg / kg / min for 4 minutes each with a stop when the required therapeutic effect is achieved.

Additional dose information: if the therapeutic effect is achieved or blood pressure decreases, stop the loading dose and reduce the infusion rate to 12.5-25 mcg / kg / min. In addition, if necessary, increase the time interval between titration steps from 5 to 10 minutes.

The drug should be discontinued if the heart rate or blood pressure rapidly approaches the lower limit of normal or exceeds it, and then resume use without loading doses at a reduced dose after the heart rate or blood pressure returns to a satisfactory level.

Overdose

Symptoms: hypotension, bradycardia, bronchospasm.

Treatment: for bradycardia-intravenous use of atropine sulfate or isoproterenol, or glucagon; for arterial hypotension-intravenous use of fluids and vasoconstrictors (epinephrine, norepinephrine, dopamine or dobutamine), for bronchospasm — isoproterenol or a derivative of xanthine.

Special instructions

With caution, Breviblock is prescribed to patients with bronchospastic diseases, diabetes mellitus, and impaired renal function.

use at concentrations greater than 10 mg / ml should be avoided due to possible skin necrosis. Cautiously continue the infusion for more than 24 hours (study experience is insufficient).

It can be used 48 hours after the withdrawal of verapamil and reserpine.

It is not recommended to use butterfly needles. Incompatible in one syringe with 5% sodium bicarbonate solution.

Form of production

Solution for injection

Storage conditions

At a temperature not exceeding 25 °C (do not freeze)

Shelf life

2 years

Active ingredient

Esmolol

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

Adult Doctor’s prescription