Buy Breblock ampoules 10 mg/ml, 10 ml, 5 pcs

Esmolol

Brand Baxter

In stock 1674 Items

Available since: 2019-09-19

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Clinical Pharmacology

Breviblock - cardioselective beta-blocker without SMA and membrane stabilizing activity; It has antianginal, hypotensive and antiarrhythmic effects. The hypotensive effect is due to a decrease in catecholamine-stimulated cAMP formation from ATP, intracellular current Ca2 +, a decrease in heart rate and a decrease in myocardial contractility. The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening diastole and improving myocardial perfusion) and a decrease in contractility. By increasing the end-diastolic pressure in the LV and increasing the stretching of the muscle fibers of the ventricles can increase the need for oxygen, especially in patients with CHF. The antiarrhythmic effect is determined by the inhibition of conducting impulses in the antegrade and to a lesser extent retrograde directions through the AV node and along additional paths. The action comes from the moment of administration, the full therapeutic effect develops 2 minutes after the administration and ends 10-20 minutes after the cessation of the infusion.

Indications

Sinus and supraventricular tachycardia, supraventricular tachyarrhythmia (atrial fibrillation, atrial flutter), arterial hypertension, including during and after operations.

Composition

1 ml. contains:

Active substance: esmolol hydrochloride 10 mg.

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Dosage and Administration

Brevibloc injected into / in, IV drip. The dose is established by the introduction of a series of loading and maintenance doses. In case of arrhythmias, initially using a dosing device, a loading dose is administered within 1 min - 500 μg / kg, then at a rate of 50 μg / kg / min over the next 4 minutes; when the desired effect is achieved, a maintenance dose of 25 mcg / kg / min. Interruptions are possible from 5 to 10 minutes between repeated administration. If the effect is not sufficiently pronounced, by the end of 5 minutes, the loading dose should be repeated, then, within 4 minutes, 100 μg / kg / min should be injected (for repeated attempts, this dose can be increased to 150 and then 200 μg / kg / min). When the desired degree of HR reduction is achieved, the following can be used to stabilize the patient's condition: propranolol - 10-20 mg every 4-6 hours orally, verapamil - 80 mg every 8 hours, digoxin - 0.125-0.5 mg every 6 hours orally or iv. also quinidine - 200 mg every 2 h inside. While taking the first dose of one of these drugs for 1 hour, the dose of esmolol can be reduced by 50%. In the case of a patient’s stable condition after taking the first or the second dose of an alternative drug, the infusion can be stopped. During operating anesthesia - IV a bolus, 80 mcg for 15-30 s, then infusion at a rate of 150-300 mcg / min. Arterial hypertension or arrhythmia during or after surgery - IV, 250-500 mg / kg for 1 min (loading dose), then IV drip for 4 minutes - 50 mg / kg / min (maintenance dose). In the absence of effect, re-administered, up to 4 times (loading and maintenance dose, increasing each subsequent maintenance dose by 50 mcg / kg). The maximum maintenance dose for adults is 200 mcg / kg / min. Children with supraventricular arrhythmias - IV drip, 50 mcg / kg / min, followed by increasing the dose (if necessary) every 10 minutes to 300 mcg / kg / min.

Adverse reactions

From the nervous system and sense organs: rarely - a feeling of tiredness, drowsiness, confusion, headache, dizziness, speech and / or vision disorders, agitation.

Since the cardiovascular system and blood (hematopoiesis, hemostasis): rarely - hypotension, signs of peripheral ischemia, bradycardia, palpitations, thrombophlebitis.

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

Contraindications

Hypersensitivity, bradycardia (HR less than 45 / min), AV block II-III., Arterial hypotension (systolic blood pressure below 90 mm Hg, diastolic blood pressure below 50 mm Hg), cardiogenic shock, acute CH, SSS, SA blockade, bleeding, hypovolemia, lactation period. With caution. Bronchial asthma, COPD (emphysema, chronic obstructive bronchitis), CHF, chronic renal failure, secondary hypertension (due to vasoconstriction, during or after surgery, against the background of hypothermia), diabetes, pregnancy, old age.

Drug interactions

Breviblok is incompatible in one syringe with other drugs (including with 5% sodium bicarbonate solution). Increases the concentration of digoxin in the plasma. Morphine, suksametoniy and indirect anticoagulants increase the concentration of esmolol in the blood. Increases the duration of the neuromuscular blockade caused by suxametonium 1.5 times. Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving esmolol. Iodine-containing radiopaque drugs for iv administration increase the risk of anaphylactic reactions. Phenytoin with the on / in the introduction, drugs for inhalation general anesthesia (derivatives of hydrocarbons) increase the severity of the cardiodepressive action and the likelihood of a decrease in blood pressure. Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).Reduces clearance of lidocaine and xanthines (except for difillina) and increases their concentration in plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking. The antihypertensive effect is weakened by NSAIDs (delayed Na + and blockade of Pg synthesis by the kidneys), GCS and estrogens (delayed Na +). Cardiac glycosides, methyldopa, reserpine and guanfacine, BMCC (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV blockade, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics, hydralazine and other hypotensive drugs can lead to an excessive decrease in blood pressure. Lengthens the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Three - and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs increase the central nervous system depression. The simultaneous use with MAO inhibitors due to a significant increase in the hypotensive effect is not recommended; the treatment gap between taking MAO inhibitors and esmolol should be at least 14 days. Unhydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

Pregnancy and Lactation

Safety of use in pregnant women has not been studied. Due to the lack of data on the possibility of Breviblock penetration into breast milk, it is not recommended to use it during breastfeeding.

Special instructions

During the period of treatment it is necessary to carry out careful and continuous monitoring of the ECG, blood pressure, heart rate. The prepared solution is stored for no more than 24 hours at room temperature; freezing of the solution is not allowed. Not recommended for insertion of a butterfly needle. Experience with children is limited. In the experiment, when prescribed in doses exceeding the maximum support for humans 8 times (rabbits) and 30 times (rats), it has a toxic effect on the mother's body, increases the frequency of resorption and fetal mortality. It is necessary to consider the possibility of masking signs of hypoglycemia (tachycardia, increased blood pressure) in patients with diabetes. Against the background of an allergic anamnesis, a more severe manifestation of allergic reactions and the lack of a therapeutic effect from the usual doses of epinephrine are possible. At concentrations greater than 10 mg / ml, tissue irritation is possible; If a local reaction occurs during the infusion, the administration should be stopped and the site of injection should be changed.

Overdosage

Symptoms: hypotension, bradycardia, bronchospasm.

Treatment: in bradycardia - IV the introduction of atropine sulfate or isoproterenol, or glucagon; with arterial hypotension - IV the introduction of fluid and vasoconstrictor agents (epinephrine, norepinephrine, dopamine or dobutamine), with bronchospasm - isoproterenol or xanthine derivative.