Breviblock (Brevibloc)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceEsmololEsmolol
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  • Breviblock
    solution d / infusion 
    Baxter Helskea Limited     United Kingdom
  • Breviblock
    solution in / in 
    Baxter Helskea Limited     United Kingdom
    • Dosage form: & nbspsolution for intravenous administration
    Composition:

    In 1 ml of the drug contains:

    active substance: esmolola hydrochloride 10 mg;

    Excipients: sodium chloride 5.9 mg, sodium acetate trihydrate 2.8 mg, glacial acid 0.546 mg, hydrochloric acid to pH 5.0, sodium hydroxide to pH 5.0, water for injection up to 1 ml.

    Description:

    Transparent solution from colorless to light yellow color.

    Pharmacotherapeutic group:Beta1-blocker selective
    ATX: & nbsp

    C.07.A.B   Selective beta-blockers

    C.07.A.09   Esmolol

    Pharmacodynamics:

    Esmolol is a cardioselective blocker of beta1-adrenergic receptors, which has a rapid onset of action, a very short duration of action, in therapeutic doses that does not have its own sympathomimetic and membrane-stabilizing activity; has antianginal, antihypertensive and antiarrhythmic effect. Reduces catecholamine-stimulated formation of cyclic adenosine monophosphate from adenosine triphosphate, reduces the intracellular current of calcium ions, reduces the heart rate (heart rate), slows conduction, reduces myocardial contractility.Antiarrhythmic effect is determined by depression; impulses in antegrade and, to a lesser extent, in retrograde directions through the atrioventricular node and along additional paths.

    The action begins from the moment of administration, the full therapeutic effect develops 2 min after the administration and ends after 10-20 min after the infusion has stopped.

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

    Esmolol, as well as other beta-blockers, has a negative foreign, chrono, batmo- and dromotropic effect.

    In patients older than 65 years, there was no difference in hemodynamic effects compared with younger patients.

    Pharmacokinetics:

    The half-life of esmolol after intravenous administration is about 9 minutes. Esmolol metabolized by erythrocyte esterases to an acid metabolite ASL-8123, which has a weak (less than 0.1% of esmolol) beta-adrenergic blocking activity.The half-life of the acid metabolite by the kidneys is about 3.7 hours, while chronic renal failure increases by 10 times.

    Less than 2% of esmolol is excreted by the kidneys unchanged.

    Esmolol binds to blood plasma proteins by 55% (for the acid metabolite, this figure is only 10%).

    Indications:

    Supraventricular tachycardias, including atrial fibrillation and atrial flutter, in the perioperative and post-operative period or in any other situations where short-term control of the ventricular rate is required with a short-acting drug.

    Tachycardia and hypertension in the perioperative period.

    Sinus tachycardia is of an uncompensated nature.

    Contraindications:

    - Hypersensitivity to the components of the drug;

    - pronounced bradycardia (heart rate less than 50 beats per minute);

    - syndrome of weakness of the sinus node;

    - atrioventricular blockade of II and III degree;

    - cardiogenic shock;

    - severe arterial hypotension;

    - acute heart failure;

    - pulmonary hypertension;

    - pheochromocytoma without simultaneous use of alpha-blockers;

    - age to 18 years;

    - simultaneous intravenous administration of blockers of "slow" calcium channels (verapamil, diltiazem).

    Carefully:

    - Atrioventricular block of the 1st degree;

    - bronchial asthma, chronic obstructive pulmonary disease;

    - violations of peripheral circulation (Raynaud's syndrome, "intermittent" lameness);

    - chronic heart failure;

    - impaired renal function;

    - hyperkalemia;

    - thyrotoxicosis;

    - psoriasis;

    - myasthenia gravis;

    - angina of Prinzmetal;

    - hypovolemia;

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

    - elderly age;

    - pregnancy;

    - diabetes;

    - Secondary arterial hypertension (due to vasoconstriction, during or after surgery, against hypothermia).

    Pregnancy and lactation:

    Data on the use of the drug in pregnant women and during breastfeeding are absent. Before use, evaluate the potential risk to the fetus and benefit the mother. The use of the drug during pregnancy is possible if the benefit to the mother exceeds the potential risk to the fetus or child.

    If treatment is considered appropriate, continuous monitoring of uteroplacental blood flow should be carried out, since beta-blockers can reduce blood supply to the placenta.

    It was reported that the use of the drug in the second and third trimesters of pregnancy or during labor and delivery caused bradycardia of the fetus, which continued after the infusion of the drug was stopped. If pregnant women receive treatment immediately before delivery, the beta-adrenoblocking effect may persist in the newborn for several days after birth and may lead to clinically significant bradycardia, respiratory depression, hypoglycemia, and hypotension. Reduced compensatory cardiovascular reactions and, heart failure may require admission to intensive care, therapy and neonatal care.

    It is not known whether the drug is excreted in breast milk, so if it is necessary to use the drug during lactation, breastfeeding should be interrupted.

    Dosing and Administration:

    Only for intravenous administration!

    Only for short-term use!

    Do not add additional ingredients to the bottle!

    HDo not use it in case of discoloration or precipitation! HDispose of used remnants!

    Avoid contact with alkalis!

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

    The dose of the drug should be selected on an individual basis, based on the clinical response. Doses should be titrated, guided by the ventricular rhythm and, if necessary, arterial pressure (BP).

    BREWBLOCK should be administered with caution to 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 μg / kg / min. To control ventricular rhythm, maintenance infusion doses above 200 mcg / kg / min are not recommended; doses of more than 200 μg / kg / min provide a slight decrease in heart rate, while the frequency of adverse reactions increases. However, higher doses (250-300 μg / kg / min) may be required to adequately monitor blood pressure. The safety of doses above 300 μg / kg / min has not been studied. The dose of the drug with supraventricular tachyarrhythmia should be selected individually by titration, in which each step includes a loading dose followed by a maintenance dose.

    Scheme of initiation and treatment

    Administration of a loading dose of 500 μg / kg / min for 1 min, then administering a maintenance dose of 50 μg / kg / min for 4 minutes *.

    If the result is positive:

    Administration of a maintenance dose of 50 μg / kg / min.

    If the result is negative for 5 min:

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

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

    If the result is positive:

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

    If the result is negative for 5 min:

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

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

    If the result is positive:

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

    If the result is negative:

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

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

    * If the desired target heart rate is reached, but the blood pressure is lowered, STOP introduction of a loading dose and reduce the rate with a sustained administration from 50 μg / kg / min to 25 μg / kg / min or lower. If necessary, the time interval between the titration steps can be increased from 5 to 10 minutes,

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

    After reaching the necessary heart rate and stable clinical state in patients with supraventricular tachycardia, it is possible to make the transition to other antiarrhythmic drugs, for example, verapamil, propranolol or metoprolol, digoxin or quinidine.

    The recommended procedure for such a transition is described below, but the attending physician should be guided by instructions on the use of alternative medications.

    Alternative drug

    Dose

    Propranolol hydrochloride

    10-20 mg every 4 to 6 hours inside

    Digoxin

    0,125-0,5 mg every 6 hours inside or intravenously

    Verapamil

    80 mg every 6 hours

    Quinidine

    200 mg every 2 hours

    The dose of the drug should be reduced as follows:

    1. Within the first hour after the first dose of the alternative drug, reduce the rate of administration of BREWBLOK in 2 times.

    2. After the second dose of the alternative drug, it is necessary to monitor the patient's CC and, if a satisfactory heart rate is maintained during the first hour, BREVIBLOCK should be discontinued.

    The administration of the drug for more than 24 hours was not evaluated. The administration of a drug lasting more than 24 hours should be performed with caution.

    Tachycardia and hypertension in the perioperative period

    In the treatment of tachycardia and (or) arterial hypertension in the perioperative period, the following dosing regimens should be used:

    a) With intraoperative treatment - with general anesthesia, when the control of the ventricular rhythm is required, administer a bolus loading dose of 80 mg for 15-30 seconds, followed by infusion at a dose of 150 μg / kg / min. Titrate the rate of administration if necessary to 300 μg / kg / min.

    b) After leaving the general anesthesia infusion at a rate of 500 μg / kg / min for 4 minutes, followed by infusion of 300 μg / kg / min.

    at) In the postoperative period, when time permits for titrating the dose, give a loading dose of 500 μg / kg / min for 1 minute before each titration step to ensure a rapid onset of action of the drug. The titration steps are 50, 100, 150, 200, 250 and 300 μg / kg / min for 4 minutes each with a stop when the desired therapeutic effect is achieved.

    Additional information on doses: when therapeutic effect is achieved or blood pressure is lowered, the introduction of the loading dose should be stopped and the infusion rate reduced to 12.5-25 μg / kg / min.In addition, if necessary, increase the time interval between the titration steps from 5 to 10 min.

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

    Side effects:

    Undesirable reactions recorded during clinical trials

    The adverse reactions presented in this section have been identified in clinical trials of the drug during the treatment of supraventricular tachycardia / tachyarrhythmia, as well as during the perioperative period.

    The frequency of adverse reactions to the drug was assessed using the following scale: very frequent (≥ 1/10), frequent (≥ 1/100 - <1/10), infrequent (≥ 1/1000 - <1/100), rare (≥ 1/10 000 - <1/1000) and very rare (<1/10 000).

    System-Organ Class

    Preferred term MedRA

    Frequency

    Infringements from

    metabolism and nutrition

    Anorexia

    Infrequent

    Hyperkalemia

    --*

    Disorders of the psyche

    Depression

    Infrequent

    Pathological thinking

    Infrequent

    Anxiety

    Infrequent

    Irritability

    Infrequent

    Infringements from

    nervous system

    Confused Consciousness

    Frequent

    Headache

    Frequent

    Dizziness

    Frequent

    Drowsiness

    Frequent

    Excitation

    Frequent

    Convulsions

    Infrequent

    Paresthesia

    Infrequent

    Fatigability

    Infrequent

    Speech disorder

    Infrequent

    Infringements from

    organ of vision

    Visual impairment

    Infrequent

    Infringements from

    hearts

    Heart failure

    Infrequent

    Increased pulmonary artery pressure

    Infrequent

    Bradycardia

    Infrequent

    Ventricular extrasystoles

    Infrequent

    Accelerated idioventricular rhythm

    --*

    Nodal rhythm

    Infrequent

    Atrioventricular block

    --*

    Chest pain

    Infrequent

    Angina pectoris

    Infrequent

    Vascular disorders

    Arterial hypotension

    Very Frequent

    Asymptomatic arterial hypotension

    Very Frequent

    Arterial hypotension with clinical manifestations

    Frequent

    Peripheral ischemia

    Infrequent

    Pallor

    Infrequent

    "Tides"

    Infrequent

    Dispnoe

    Frequent

    Infringements from

    respiratory system,

    organs of the chest and

    the mediastinum

    Bronchospasm

    Infrequent

    Wheezing

    Infrequent

    Abnormal respiratory noises, including

    number of wheezing

    Infrequent

    Nasal congestion

    Infrequent

    Infringements from

    gastrointestinal

    tract

    Nausea

    Frequent

    Vomiting

    Infrequent

    Dyspepsia

    Infrequent

    Discomfort and abdominal pain

    Infrequent

    Constipation

    Infrequent

    Dryness of the oral mucosa

    Infrequent

    Disturbance of taste perception

    --*

    Violations from the musculoskeletal and

    connective tissue

    Musculoskeletal pain (pain in the scapular region)

    Infrequent

    Ridge chondrite

    --*

    Disorders from the kidneys and urinary tract

    Retention of urine

    Infrequent

    General disorders and

    violations in place

    introduction of

    Increased sweating

    Frequent

    Reactions at the injection site (total) 3

    Frequent

    Phlebitis and thrombophlebitis at the site of administration

    --*

    Sealing at the injection site

    Frequent

    Inflammation at the site of administration

    Frequent

    Burning at the injection site

    Infrequent

    Ecchymosis at the site of administration

    Infrequent

    Edema at the site of administration

    Infrequent

    Erythema at the site of administration

    Infrequent

    Pain at the injection site

    Infrequent

    Asthenia

    Infrequent

    Chills

    Infrequent

    Fever

    Infrequent

    Note:

    1 Includes an increased incidence of ventricular extrasystole and twin ventricular extrasystoles.

    2 Based on reports of hypotension in eight placebo-controlled perioperative studies, hypotension was less common in patients who received the drug during the perioperative period than patients who received the drug during treatment with supraventricular tachycardia / tachyarrhythmia.Moreover, in these eight studies, the proportion (or frequency) of hypotension in patients receiving the drug and general anesthesia was the same as the proportion (or frequency) of hypotension in patients receiving placebo and general anesthesia.

    3 See necrosis and blistering at the injection site in the section "Undesirable reactions in the postmarketing period", and also see the "Special instructions" section.

    * - Data for frequency estimation is not enough.

    Undesirable reactions in the postmarketing period

    In addition to undesirable reactions recorded in clinical trials, the following undesirable reactions were recorded during post-marketing use.

    Disorders from the metabolism and nutrition: metabolic acidosis.

    Heart Disease: cardiac arrest, pulmonary edema, coronary artery spasm.

    Disturbances from the skin and subcutaneous tissues: angioedema, urticaria.

    Disturbances from the musculoskeletal connective tissue: muscle weakness (see also sections "Special instructions" and "Interaction with other drugs").

    General disorders and disorders at the site of administration: necrosis at the site of injection, vesicles at the infusion site, blistering (see also reactions at the site of administration described in "Undesirable reactions recorded during clinical trials" and "Special instructions").

    If any of the side effects indicated in the manual are aggravated or you notice any other side effects not listed in the instructions, inform the doctor.

    Overdose:

    Symptoms

    From the cardiovascular system: possible pronounced bradycardia, atrioventricular blockade (I, II and III degrees), nodal rhythm, slowing of intraventricular conduction, decreased myocardial contractility, severe arterial hypotension, acute heart failure (including cardiogenic shock), cardiac arrest, electromechanical dissociation.

    From the central nervous system possible respiratory depression, seizures, sleep and mood disorders, fatigue, inhibition, coma.

    Also possible bronchospasm, mesenteric ischemia, peripheral cyanosis, hyperkalemia and hypoglycemia:

    Overdose can lead to the development of life-threatening conditions and death.

    Treatment

    The first step in case of symptoms of an overdose should be to stop the injection.

    When bradycardia intravenous administration of atropine is indicated. Catecholamines that increase heart rate may be indicated, and / or an artificial pacemaker may be required. When heart failure intravenous diuretics and / or cardiac glycosides are indicated. In shock, developed due to inadequate contractility of the myocardium, intravenous injection of the drug with a positive inotropic effect, for example, dopamine, dobutamine, isoprenaline or amrinone is indicated. When symptomatic arterial hypotension should consider the possibility of intravenous injection of plasma-substituting solutions and / or vasopressor agents such as dopamine or norepinephrine. When bronchospasm intravenously injected beta2-adrenomimetics and / or theophylline derivatives.

    In cases of overdose, continuous monitoring of the patient is required.

    Interaction:

    The drug is not compatible with a 5% solution of sodium bicarbonate because of limited stability and with furosemide - due to precipitation.

    Pharmacokinetic interactions

    With simultaneous introduction digoxin and the drug BREVIBLOCK there was an increase in the concentration in the blood of digoxin by about 10-20%. The pharmacokinetics of the drug did not change.

    With simultaneous intravenous administration of morphine and BREVIBLOCK, there was no change in the concentration of morphine in the blood plasma, while the equilibrium concentration of esmolol in the blood increased by an average of 46%, while the other pharmacokinetic parameters remained unchanged.

    Pharmacodynamic and other interactions

    Simultaneous use of the drug with other antihypertensive drugs, drugs that depress myocardial contractility, or inhibit the function of the sinus node, or conduct electrical impulses in the myocardium, can enhance the effect of the drug on blood pressure, myocardial contractility and impulses in the myocardium. Pharmacodynamic interactions with such drugs can lead, for example, to severe arterial hypotension, heart failure, severe bradycardia, sinus pause, sinoauric block, atrioventricular block and / or cardiac arrest. In addition, the use of certain drugs against the background of beta-adrenergic blockade can lead to an increase in the syndrome of "withdrawal".In this regard, the drug should be used with caution and only after a thorough individual risk assessment and expected benefit in patients receiving drugs that can cause these types of pharmacodynamic interactions, including but not limited to the following drugs: alfuzosin, doxazosin and other alpha-blockers; amifostine; amiodarone; anticholinesterase drugs; antipsychotic drugs; apomorphine; baclofen; verapamil, diltiazem and other blockers of "slow" calcium channels that inhibit cardiac activity (with joint use of the drug and verapamil in patients with decreased myocardial function, cases of cardiac arrest with a fatal outcome are noted); cardiac glycosides; disopyramide, lidocaine, phenytoin, flecainide; inhalation anesthetics; levodopa; monoamine oxidase inhibitors; mefloquine; opiates, opioids, including fentanyl; barbiturates of short action; tricyclic antidepressants (for example, imipramine, amitriptyline); clonidine, guanfacine, moxonidine. Beta-adrenoblockers increase the risk of recurrent arterial hypertension with the abolition of clonidine,guanfacin and moxonidine. Therefore, it is first necessary to cancel the beta-blocker, and the withdrawal should be gradual.

    When beta-blockers are used, patients at risk of anaphylactic reactions may respond more actively to exposure allergen (random, diagnostic or therapeutic). Patients who use beta-blockers may not be immune to the usual doses of epinephrine used to treat anaphylactic reactions.

    Beta-adrenoblockers, including BREVIBLOCK, caused muscle weakness. Therefore, beta-blockers can theoretically reduce the effectiveness anticholinesterase agents when treating muscle weakness.

    Simultaneous use of beta-blockers and hypoglycemic agents for ingestion or insulin can enhance the hypoglycemic effect of the latter. Beta-adrenoblockers may mask tachycardia that occurs with hypoglycemia, although other manifestations, such as dizziness and increased sweating, may occur.

    Reserpine and other drugs that deplete catecholamine stocks may have an additive effect when combined with beta-blockers.Therefore patients who, together with the BREVIBLOCK preparation, are simultaneously administered catecholamine inhibitors, should be carefully monitored for signs of arterial hypotension or severe bradycardia, which can lead to dizziness, fainting, or orthostatic hypotension.

    Simultaneous use of beta-blockers with derivatives of ergot alkaloids can lead to severe peripheral vasoconstriction and arterial hypertension. Possible weakening effects glucagon, associated with increased blood glucose levels.

    Nonsteroidal anti-inflammatory drugs can cause a decrease in the antihypertensive effect of beta-blockers.

    Because of the risk of reducing heart contractility against a background of high systemic vascular resistance, BREWBLOCK should not be used to control tachycardia in patients receiving drugs that have vasoconstrictive and positive inotropic effects, including: epinephrine, norepinephrine, dopamine.

    The effect of the drug may decrease with simultaneous use with sympathomimetic drugs, having activity of beta-adrenergic agonists.The doses of each drug may need to be adjusted based on the patient's response, or alternative therapeutic agents may be considered. The drug increases the duration of the induced succinylcholine neuromuscular blockade.

    When used simultaneously with sulfinpyrazone, the antihypertensive effects of beta-blockers may be reduced.

    Special instructions:

    During the treatment it is necessary to carry out a thorough and constant monitoring of the electrocardiogram, blood pressure, heart rate.

    Influence on blood pressure, heart rate, rhythm and contractility of the heart

    - Undesirable reactions to beta-blockers, including BREVIBLOCK, from the heart and blood vessels can be severe, especially in patients with hemodynamic disorders and patients taking drugs that increase the risk of cardiovascular reactions (see section "Interaction with other drugs"). . Severe reactions may include unconsciousness, cardiogenic shock, cardiac arrest, which can lead to death. BREWBLOCK, in the absence of contraindications (see the section "Contraindications"), should be used with caution and only after a thorough individual assessment of the risks and expected benefits in patients with hemodynamic disorders and patients,which simultaneously receive drugs that increase the risk of conduction disorders and myocardial contractility.

    - When using the drug, there was an arterial hypotension, including severe hypotension. Arterial hypotension depends on the dose (see sections "Method of administration and dose" and "Side effect"). Careful monitoring of patients should be carried out, especially in the case of low blood pressure, before treatment begins. In the case of a sharp decrease in blood pressure should reduce the dose of the drug or stop its introduction. Arterial hypotension, as a rule, passes within 30 minutes after discontinuation of the drug administration. In some cases, additional treatment may be required.

    - When the drug was used, bradycardia, including severe bradycardia, and cardiac arrest were observed. The drug should be used with extreme caution in patients with low heart rate before treatment and only when it is believed that the potential benefit exceeds the risk. The drug is contraindicated in patients with existing severe sinus bradycardia (see section "Contraindications"). In the case of severe bradycardia, the dose should be reduced or discontinued.In some cases, additional treatment may be required.

    - Beta-adrenoblockade reduces myocardial contractility and can provoke or aggravate heart failure. At the first sign or symptom of clinically significant oppression of myocardial activity, the dose of the drug should be reduced or discontinued. In some cases, additional treatment may be required. Care should be taken when using the drug in patients with impaired myocardial contractility (the drug is contraindicated in patients with severe heart failure or cardiogenic shock - see the section "Contraindications"). Beta-adrenoblockers affect the function of the sinus node, as well as sinus-atrial and atrioventricular conduction, and can lead to the development of a syndrome of weakness of the sinus node, sinoatrial and atrioventricular blockade, including complete blockade, which can lead to cardiac arrest. This effect is most typical for patients with already existing dysfunction of the sinus node and conduction disorders (the drug is contraindicated in patients with atrioventricular blockade of II or III degree and in patients with sinus node weakness syndrome - see the section Contraindications).The drug should be used with caution in patients with other cardiac conduction disorders, including atrioventricular blockade of the I degree.

    Use with caution in patients with pheochromocytoma and only with the simultaneous use of alpha-adrenoreceptor blockers (see the section "Contraindications").

    BREWBLOCK should not be used as an agent for the treatment of hypertension in patients whose elevated blood pressure is due mainly to vasoconstriction on the background of hypothermia.

    Patients with impaired reactivity of the respiratory tract, for example, patients with bronchial asthma, should not receive beta-blockers. BREWBLOCK, due to its relative beta-1-selectivity and titruvosti, can be used with caution in patients with impaired reactivity of the respiratory tract. However, since beta-1 selectivity is not absolute, accurate dosing of the drug is required to achieve the lowest possible effective dose. In the case of bronchospasm or worsening of the existing bronchospasm, infusion should be stopped immediately; if the condition allows, it is possible to prescribe beta2-adrenomimetics.

    The drug should be used with caution. the patients who are prone to or prone to hypoglycemia, as well as in patients with diabetes mellitus, who receive insulin or hypoglycemic agents for oral administration.

    - Beta-adrenoblockers may mask tachycardia that occurs with hypoglycemia, although other manifestations, such as dizziness and increased sweating, may occur.

    - The concomitant use of beta-blockers and hypoglycemic agents may exacerbate the hypoglycemic effect of the latter (see also the section "Interaction with other drugs").

    When using the drug BREVIBLOCK observed reaction at the site of administration. They included signs and symptoms of irritation and inflammation at the injection site (see section "Side effect").

    Because of the risk of reducing heart contractility against a background of high systemic vascular resistance, the drug should not be used to control tachycardia in patients receiving drugs that have vasoconstrictive and positive inotropic effects, including epinephrine, norepinephrine, dopamine.

    Beta-blockers can increase the number and duration of angina attacks in patients with angina prinzmetal due to unimpeded alpha-adrenoreceptor mediated spasm of the coronary arteries. For these patients, non-selective beta-blockers should not be used, and selective beta-1-blockers should be used only with special precautions.

    In patients with hypovolemia The drug can weaken reflex tachycardia and increase the risk of hypotension. In this regard, in such patients the drug should be used with special precautions.

    Abolition of BREVIBLOCK

    Since the "cancellation" syndrome can not be ruled out, as for all beta-blockers, care should be taken with a sharp discontinuation of the administration of the drug to patients with ischemic heart disease. In a clinical electrophysiological study, the increase in the heart rate 30 minutes after discontinuation was moderate, but significantly higher than the original heart rate. Beta-blockers also increase the risk of recurrent hypertension when withdrawn; clonidine, guanfacin and moxonidine (see Table 1).section "Interaction with other drugs").

    In patients with impaired peripheral circulation (including Raynaud's disease or syndrome and peripheral vascular occlusive disease), the drug should be used with caution, since beta-blockers can enhance violations of peripheral circulation.

    The drug should be administered with caution patients with impaired renal function. Acid metabolite of the drug is excreted by the kidneys mainly unchanged. His excretion is significantly reduced in patients with kidney disease. In patients with terminal stage of renal failure, his half-life increased by 10 times, and the level in blood plasma increased significantly.

    Hyperkalemia

    The use of beta-blockers, including BREVIBLOCK, was accompanied by an increase in potassium in the blood plasma and hyperkalemia. The risk increases if patients have such factors as renal failure. It has been reported that intravenous administration of beta-blockers causes potentially life-threatening hyperkalemia in patients on hemodialysis.

    Use in patients with metabolic acidosis

    It has been reported that beta-blockers, including BREVIBLOCK, cause or contribute to the development of hyperkalemic renal tubular acidosis. In addition, acidosis can usually be accompanied by reduced myocardial contractility. The drug should be used with caution in patients with previous metabolic acidosis.

    Use in patients with thyrotoxicosis

    Beta-adrenergic blockade may mask some clinical signs of hyperthyroidism (eg, tachycardia). A sharp cessation of beta-adrenergic blockade can provoke a thyrotoxic crisis. In this regard, patients should be closely monitored for the development of thyrotoxicosis when beta-blockers are discontinued.

    Use in patients with an increased risk of developing severe hypersensitivity reactions

    When using beta-blockers, patients with an increased risk of developing anaphylactic reactions may respond more actively to the effects of an allergen (accidental, diagnostic or therapeutic). Patients who use beta-blockers may not be immune to the usual doses of epinephrine used to treat anaphylactic or anaphylactoid reactions (cf.(see also the section "Interaction with other drugs").

    Use in patients with psoriasis in an anamnesis

    When beta-blockers were used, there was an exacerbation of psoriasis or the appearance of psoriasis or psoriaticformations. In patients with psoriasis, a history of beta-blockers should be prescribed only after a thorough analysis of the expected benefits and risks.

    Use in patients with muscle weakness

    Beta-adrenoblockers, including BREVIBLOCK, caused muscle weakness. The drug should be used with caution in patients with muscle weakness.

    Application in the elderly

    Elderly patients should be administered with caution. Generally, dose selection for an elderly patient should be carried out with caution, usually starting from a low dose range, taking into account the greater frequency of reduced renal or cardiac function, concomitant diseases, or other medications.

    Use in patients with hepatic impairment

    Since the drug is metabolized by erythrocyte esterases, no special precautions are required in patients with hepatic impairment.

    Effect on the ability to drive transp. cf.and fur:

    Some of the undesirable effects that occur after the use of the drug, such as dizziness or drowsiness, can affect a patient's ability to drive vehicles and work with mechanisms. Patients should not drive vehicles or operate machinery until such effects disappear.

    Form release / dosage:Solution for intravenous administration, 10 mg / ml.
    Packaging:

    For 10 ml of the drug in bottles of dark glass. The bottle is sealed with a rubber stopper under an aluminum run-off and covered with a plastic cover.

    5 bottles per cardboard box together with instructions for use.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:For hospitals
    Registration number:П N016165 / 02
    Date of registration:18.02.2010 / 18.05.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:Baxter Helskea LimitedBaxter Helskea Limited United Kingdom
    Manufacturer: & nbsp
    Representation: & nbspBaxter Baxter USA
    Information update date: & nbsp23.02.2017
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