Breviblock, 10 mg/ml 10 ml 5 pcs

Esmolol is a cardioselective beta1-adrenoreceptor blocker with rapid onset of action, very short duration of action, in therapeutic doses having no sympathomimetic and membrane stabilizing activity of its own; it has antianginal, antihypertensive and antiarrhythmic effects.

Decreases catecholamine-stimulated formation of cyclic adenosine monophosphate from adenosine triphosphate, reduces intracellular calcium ion current, decreases heart rate (HR), slows conduction, reduces myocardial contractility.

The antiarrhythmic effect is determined by inhibition; conduction of impulses in antegrade and, to a lesser extent, in retrograde direction through the atrioventricular node and along accessory pathways.

The action occurs from the moment of infusion, the full therapeutic effect develops 2 min after infusion and ends 10-20 min after cessation of the infusion.

Esmololol by its chemical nature belongs to the class of phenoxypropanolamine beta-adrenoblockers. It has an enzymatically labile ester link, as a result of which it is rapidly metabolized and has a short plasma elimination half-life.

Esmolol, like other beta-adrenoblockers, has negative in-, chrono-, batmo- and dromotropic effects.

There were no differences in hemodynamic effects in patients older than 65 years compared to younger patients.

Indications

Active ingredient

Composition

1 ml of the drug contains:

the active ingredient:

esmolol hydrochloride 10 mg;

excipients:

sodium chloride 5.9 mg,

sodium acetate trihydrate 2.8 mg,

ice-cold acetic acid 0.546 mg,

How to take, the dosage

For intravenous administration only!

For short-term use only!

Do not add any additional ingredients to the bottle!

Do not use if there is any discoloration or sludge formation! Any unused residue must be discarded.

Please 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 on an individual basis based on clinical response. Doses should be titrated based on ventricular rhythm and, if necessary, blood pressure (BP).

BREVIBLOK should be administered with caution in patients with impaired renal function (see “Special Precautions”).

Supraventricular tachycardias, including atrial fibrillation and atrial flutter

The effective dose of the drug for treatment of supraventricular tachyarrhythmias is 50-200 µg/kg/min. For control of ventricular rhythm, maintenance infusion doses greater than 200 µg/kg/min are not recommended; doses greater than 200 µg/kg/min provide little reduction in HR, with an increased incidence of adverse reactions. However, higher doses (250-300 mcg/kg/min) may be required for adequate BP control.

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

The treatment initiation and administration regimen

The administration of a loading dose of 500 µg/kg/min for I min, followed by a maintenance dose of 50 µg/kg/min for 4 min*.

If positive:

The administration of a maintenance dose of 50 µg/kg/min.

In case of a negative result within 5 min:

Repeat administration with a dose of 500 µg/kg/min for 1 min.

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

If positive:

Inject a maintenance dose of 100 µg/kg/min.

In case of a negative result within 5 min:

Repeat administration with a dose of 500 µg/kg/min for 1 min.

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

If positive:

Inject a maintenance dose of 150 µg/kg/min.

In case of a negative result:

Repeat administration with a dose of 500 µg/kg/min for I min.

Increase maintenance dose to 200 µg/kg/min and leave at that level.

* If the desired endpoint HR is achieved but the BP is decreasing, PREVENT the loading dose and reduce the maintenance dose rate from 50 µg/kg/min to 25 µg/kg/min or lower. If necessary, the time interval between titration steps can be increased from 5 to 10 min,

Note: There is no evidence that maintenance doses above 200 µg/kg/min result in greater therapeutic effect. The safety of doses above 300 µg/kg/min has not been studied.

The recommended order for this transition is described below, but the treating physician should be guided by the instructions for use of the alternative medications.

Alternative medication

Dose

Propranololol hydrochloride

10-20 mg every 4 to 6 hours orally

Interaction

Enhances the concentration of digoxin in the blood, increases the hypotensive effect of inhaled anesthetic agents, prolongs the myorelaxant effect of succinylcholine (1.5 times).

Morphine and warfarin increase blood concentrations.

Special Instructions

With caution, Brevibloc is prescribed in patients with bronchospastic disorders, diabetes mellitus, renal dysfunction.

Injection at concentrations greater than 10 mg/ml should be avoided because of possible skin necrosis. Continue infusion for more than 24 hours with caution (insufficient study experience).

Possible use 48 hours after withdrawal of verapamil and reserpine.

The use of butterfly needles is not recommended. Incompatible in the same syringe with 5% sodium bicarbonate solution.

Contraindications

– marked bradycardia (heart rate less than 50 bpm);

– sinus node weakness syndrome;

– atrioventricular block of degree II and III;

– cardiogenic shock;

– severe arterial hypotension;

p> – acute heart failure;

– pulmonary hypertension;

– pheochromocytoma without concomitant use of alpha-adrenoblockers;

– age less than 18 years;

– concomitant intravenous administration of “slow” calcium channel blockers (verapamil, diltiazem).

– Grade I atrioventricular block;

– bronchial asthma, chronic obstructive pulmonary disease;

– peripheral circulatory disorders (Raynaud’s syndrome, “intermittent” claudication);

– chronic heart failure;

– impaired renal function;

– hyperkalemia;

– thyrotoxicosis;

– psoriasis;

– myasthenia gravis;

– Prinzmetal angina;

– hypovolemia;

– pheochromocytoma (when alpha-adrenoblockers are used concomitantly);

– older age;

– pregnancy;

– diabetes mellitus;

– secondary arterial hypertension (due to vasoconstriction, during or after surgery, against a background of hypothermia).

Side effects

Nervous system and sensory organs: rarely – feeling of fatigue, drowsiness, confusion, headache, dizziness, speech and/or vision disorders, agitation.

Cardiovascular system and blood (hematopoiesis, hemostasis): rarely – hypotension, signs of peripheral ischemia, bradycardia, palpitations, thrombophlebitis.

Others: Rarely: chills, fever, dyspnea, bronchospasm, constipation, urinary retention, burning, induration or infiltration of the skin around the site of drug administration (in extravasation).

Overdose

Symptoms:hypotension, bradycardia, bronchospasm.

Treatment: for bradycardia, IV administration of atropine sulfate or isoproterenol or glucagon; for arterial hypotension, IV administration of fluids and vasoconstrictors (epinephrine, noradrenaline, dopamine or dobutamine); for bronchospasm, isoproterenol or xanthine derivative.

Pregnancy use

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

In the absence of data on the possibility of Breviblock penetration into the mother’s milk, it is not recommended to use while breastfeeding.