Betalok - instructions for use, dose, side effects, contraindications

In patients with myocardial infarction, intravenous metoprolol reduces chest pain and reduces the risk of flicker and atrial flutter. Intravenous administration of metoprolol with the first symptoms (within 24 hours after the onset of the first symptoms) reduces the risk of myocardial infarction.Early treatment with metoprolol leads to an improvement in the future prognosis of myocardial infarction.

A decrease in heart rate (HR) is achieved with paroxysmal tachycardia and atrial fibrillation (flutter).

Metoprolol - β₁-adrenoceptor blocking β₁-receptors at doses significantly lower than the doses required to block β₂receptors. Metoprolol has an insignificant membrane-stabilizing effect and does not show activity of a partial agonist. Metoprolol reduces or inhibits the agonistic effect that catecholamines, produced by nervous and physical stresses, have on cardiac activity. It means that metoprolol has the ability to inhibit the increase in the heart rate, the ability to prevent an increase in heart rate, a minute volume and increased myocardial contractility, as well as an increase in blood pressure (BP) caused by a sharp release of catecholamines.

Patients with symptoms of obstructive pulmonary disease, if necessary, can be prescribed metoprolol in combination with β₂- adrenomimetics.When combined with β₂-adrenomimetikami Betalok®, in therapeutic doses, to a lesser extent affects the induced β₂-adrenomimetics bronchodilation, than non-selective β-adrenoblockers.

Metoprolol, to a lesser degree than non-selective β-blockers, affects insulin production and carbohydrate metabolism. The effect of Betaloc® on the response of the cardiovascular system to hypoglycemia is much less pronounced compared to non-selective β-blockers.

Improvement of the quality of life in the treatment with Betaloc® was observed in patients after myocardial infarction.

Pharmacokinetics:

Metoprolol undergoes oxidative metabolism in the liver with the formation of three major metabolites, none of which has a clinically significant β-blocking effect.

About 5% of the dose is excreted unchanged in the urine.

The average half-life of metoprolol from plasma is about 3-5 hours.

Indications:

- Nadzheludochkovaya tachycardia;

- prevention and treatment of myocardial ischemia, tachycardia and pain in case of myocardial infarction or suspected of it.

Contraindications:

Atrioventricular blockade of II and III degree, heart failure in decompensation stage, permanent or intermittent therapy with inotropic agents acting as beta-adrenomimetics, clinically significant sinus bradycardia, sinus node weakness syndrome (except for patients with a constant rhythm driver), cardiogenic shock, severe disorders peripheral blood circulation, including with the threat of gangrene, arterial hypotension.

Betalok® is contraindicated in patients with suspected acute myocardial infarction at a heart rate of less than 45 beats per minute, interval PQ more than 0.24 seconds or systolic blood pressure less than 100 mm Hg.

Known hypersensitivity to metoprolol and its components or to other β-blockers.

In the treatment of supraventricular tachycardia in patients with systolic blood pressure less than 110 mm Hg.

Patients receiving β-adrenoblockers are contraindicated intravenous administration of blockers of "slow" calcium channels such as verapamil.

Age to 18 years (effectiveness and safety not established).

Carefully:

Atrioventricular blockade of the 1st degree, stenocardia of Prinzmetal, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis, bronchial asthma), diabetes mellitus, severe renal failure.

Pregnancy and lactation:

Pregnancy

Like most drugs, Betaloc® should not be given during pregnancy and during breastfeeding, except when the expected benefit to the mother exceeds the potential risk to the fetus. β-adrenoblockers reduce placental blood flow, which can lead to a delay in intrauterine development, intrauterine fetal death, spontaneous miscarriage and premature birth. When using Betaloc® during pregnancy, appropriate monitoring of the patient and fetus is recommended. Like other antihypertensives, β-blockers can cause side effects, for example, bradycardia in the fetus, newborns, or breastfed babies, and therefore should be especially careful in the appointment of β-adrenoblockers in the last trimester of pregnancy and immediately before childbirth .

Breastfeeding period

The amount of metoprolol released into breast milk and the β-adrenergic blocking effect in a breastfed infant (when metoprolol is taken by the mother at therapeutic doses) are minor.

Dosing and Administration:

Nadzheludochkovaya tachycardia

Begin the administration with 5 mg (5 ml) of Betaloc® at a rate of 1-2 mg / min. You can repeat the introduction with a 5-minute interval to achieve a therapeutic effect. Usually the total dose is 10-15 mg (10-15 ml). The recommended maximum dose for intravenous administration is 20 mg (20 ml).

Prophylaxis and treatment of myocardial ischemia, tachycardia and pain with or suspected of myocardial infarction

Intravenous 5 mg (5 ml) of the drug. You can repeat the introduction with a 2 minute interval, the maximum dose is 15 mg (15 ml). 15 minutes after the last injection, metoprolol for oral administration at a dose of 50 mg (Betaloc®) every 6 hours for 48 hours.

Impaired renal function

There is no need to adjust the dose in patients with impaired renal function.

Impaired liver function

Usually, due to the low degree of association with plasma proteins, dose adjustment is not required.However, with a severe violation of liver function (in patients with portocaval anastomosis), a dose reduction may be required.

Elderly age

There is no need to adjust the dose in elderly patients.

Children

Experience with Betaloc® in children is limited.

Side effects:

Betaloc® is well tolerated by patients, and the side effects are mostly light and reversible.

As a result of clinical studies or with the use of the drug Betalok® (metoprolol tartrate), the following undesirable side effects have been described in clinical practice. In many cases, the cause-and-effect relationship with treatment with Betaloc® was not established.

To assess the frequency of cases, the following criteria were applied: very often (> 10%), often (1-9.9%), infrequently (0.1-0.9%), rarely (0.01-0.09%) and very rarely (<0.01%).

From the side of the cardiovascular system

Often: bradycardia, postural disorders (very rarely accompanied by fainting), a feeling of coldness of the limbs, a feeling of palpitations.

Infrequent: temporary increase in symptoms of heart failure, cardiogenic shock in patients with acute myocardial infarction, atrioventricular blockade of degree I, edema, pain in the heart.

Rarely: other conduction disorders, arrhythmias.

Very rarely: gangrene in patients with previous severe impairment of peripheral circulation.

From the central nervous system

Very often: increased fatigue.

Often: dizziness, headache.

Infrequently: paresthesia, seizures, exacerbation of depression, decreased concentration, drowsiness or insomnia, nightmares.

Rarely: increased excitability, anxiety.

Very rarely: amnesia / memory disorders, depressed state, hallucinations.

From the digestive system

Often: nausea, abdominal pain, diarrhea, constipation.

Infrequently: vomiting.

Rarely: dry mucous membrane oral cavity, liver dysfunction.

Very rarely: hepatitis.

From the skin and subcutaneous tissues

Infrequent: rash (in the form of urticaria), increased sweating.

Rarely: alopecia.

Very rarely: photosensitization, exacerbation of psoriasis.

From the respiratory system

Often: dyspnoea with exercise.

Infrequent: bronchospasm in patients with bronchial asthma.

Rarely: rhinitis.

From the sense organs

Rarely: visual disturbances, dryness and / or eye irritation, conjunctivitis.

Very rarely: ringing in the ears, a violation of taste.

From the side of metabolism

Infrequent: weight gain.

From the musculoskeletal system

Very rarely: arthralgia.

From the side of the blood

Very rarely: thrombocytopenia.

Other

Rarely: impotence / sexual dysfunction.

Overdose:

Symptoms

In case of an overdose, a marked decrease in blood pressure, acute heart failure, bradycardia, bradyarrhythmia, intracardiac conduction disorder and bronchospasm may be noted.

Treatment

Treatment should be carried out in a medical institution that has the equipment and conditions for maintaining vital activity and monitoring the patient's condition.

With bradycardia and conduction disorders apply atropine and adrenomimetics, if necessary, install an artificial pacemaker.

At the expressed depression of arterial pressure, an acute cardiac insufficiency and shock should be given to therapy aimed at increasing the volume of circulating blood plasma; use glucagon in the form of injection (then, if necessary, enter glucagon in the form of intravenous infusion); intravenously administer adrenomimetics (such as dobutamine) together with α₁-adrenomimetics in case of symptoms of vasodilation. It is also possible intravenous administration of drugs containing calcium ions.

For cupping bronchospasm, bronchodilators should be used.

Interaction:

It is necessary to avoid the co-administration of Begahalk with the following preparations:

Derivatives of barbituric acid: barbiturates (the study was conducted with phenobarbital) slightly increase metabolism of metoprolol, due to the induction of enzymes.

Propaphenon: when administering propafenone to four patients treated with metoprolol, an increase in plasma concentrations of metoprolol was observed in 2-5 times, while two patients had side effects typical of metoprolol. This interaction was confirmed during the study on 8 volunteers. Probably, the interaction is due to the inhibition of propafenone, like quinidine, metoprolol metabolism through the cytochrome system P4502D6. Taking into account the fact that propafenone has the properties of β-blocker, the joint appointment of metoprolol and propafenone is not advisable.

Verapamil: a combination of β-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and β-adrenoblockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function.

The combination of Betaloc® with the following drugs may require dose adjustment:

Class I antiarrhythmic drugs: Antiarrhythmics of Class I and β-adrenoceptors can lead to a summation of a negative inotropic effect, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function. Also, this combination should be avoided in patients with sinus node weakness syndrome and atrioventricular conduction disorder. The interaction is described by the example of disopyramide.

Amiodarone: The combined use of amiodarone and metoprolol can lead to severe sinus bradycardia.Taking into account the extremely long half-life of amiodarone (50 days), possible interaction should be considered after a long time after amiodarone withdrawal.

Diltiazem: Diltiazem and βadrenoblockers mutually enhance the inhibitory effect on atrioventricular conduction and sinus node function. In the combination of metoprolol with diltiazem, cases of severe bradycardia were noted.

Non-steroidal anti-inflammatory drugs (NSAIDs): NSAIDs weaken the antihypertensive effect βadrenoblockers. This interaction is most documented for indomethacin. There was no marked interaction for sulindac. In the studies with diclofenac, the described reaction was not noted.

Diphenhydramine: Diphenhydramine reduces the clearance of metoprolol to a-hydroxymethoprolol 2.5 times. At the same time there is an increase in the effect of metoprolol.

Epinephrine (adrenaline): There were reported 10 cases of severe arterial hypertension and bradycardia in patients taking non-selective β-blockers (including pindolol and propranolol) and received epinephrine (adrenalin). Interaction is noted in the group of healthy volunteers.It is assumed that similar reactions may occur and the application of epinephrine with local anesthetic together with a random contact with the bloodstream. It is assumed that this risk is much lower with the use of cardioselective β-adrenoblockers.

Phenylpropanolamine: Phenylpropanolamine (norephedrine) in a single dose of 50 mg can cause an increase in diastolic blood pressure to pathological values in healthy volunteers. Propranolol mainly prevents the increase in blood pressure, caused by phenylpropanolamine. but β-adrenoceptors can cause reactions of paradoxical arterial hypertension in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported against phenylpropanolamine.

Quinidine: Quinidine inhibits the metabolism of metoprolol in a particular group of patients with rapid hydroxylation (in Sweden about 90% of the population), mainly causing a significant increase in plasma concentrations of metoprolol and an increase in β-blockade. It is believed that this interaction is characteristic of other β-adrenoblockers in the metabolism of which cytochrome participates P4502D6.

Clonidine: Hypertensive reactions with abrupt cancellation of clonidine can be enhanced by joint admission of β-blockers. When combined, in the case of the withdrawal of clonidine, discontinuation of the adrenoblockers should be started several days before the withdrawal of clonidine.

Rifampicin: Rifampicin can enhance the metabolism of metoprolol, decreasing the plasma concentration of metoprolol.

The concentration of metoprolol in the blood plasma can be increased when combined with cimetidine, hydralazine, selective serotonin reuptake inhibitors, such as paroxetine, fluoxetine and sertraline.

Patients simultaneously taking metoprolol and other β-blockers (eye drops) or monoamine oxidase (MAO) inhibitors should be closely monitored.

Against the background of taking β-blockers, inhalational anesthetics increase the cardiodepressive effect.

On the background of admission βadrenoblockers patients who receive oral hypoglycemic agents may require a dose adjustment of the latter.

Cardiac glycosides when combined with β-adrenoblockers can increase the time of atrioventricular conduction and causebradycardia.

Special instructions:

Patients taking β-adrenoblockers, do not enter intravenously blockers of "slow" calcium channels such as verapamil.

Patients with bronchial asthma or chronic obstructive pulmonary disease should be prescribed concomitant therapy β₂- adrenomimetics. When need to increase the dose of β₂- adrenomimetics.

When applying β₁- adrenoblockers, the risk of their effect on carbohydrate metabolism or the possibility of masking the symptoms of hypoglycemia is significantly less than with the use of nonselective β-blockers.

In patients with chronic heart failure in the stage of decompensation, it is necessary to achieve a compensation stage both before and during treatment with the drug.

Patients with angina prinzmetal not recommended nonselective β-blockers.

Very rarely, patients with impaired atrioventricular conduction may experience deterioration (a possible outcome is an atrioventricular block). If bradycardia develops against the background of treatment, the dose of Betaloc® should be reduced.

Metoprolol may increase the violation peripheral arterial blood circulation, mainly due to lower blood pressure.

Caution should be exercised when prescribing the drug to patients with severe renal failure, metabolic acidosis, co-administration with cardiac glycosides.

In patients taking beta-adrenoblockers, anaphylactic shock occurs in a more severe form.

Patients with pheochromocytoma concomitantly with Betaloc® should be given alpha-blockers.

In the case of surgery, you should inform surgeon / anesthesiologist that the patient is taking a β-blocker. It is not recommended to cancel therapy with beta-adrenoblocker before the operation. In patients with risk factors for cardiovascular disease, high doses of metoprolol should be avoided, without prior titration of the dose in surgical interventions (with the exception of heart surgery), because of the risk of bradycardia, arterial hypotension and stroke, including fatal outcome .

In case the systolic blood pressure is less than 100 mm Hg. Betaloc® should be administered intravenously only if special precautions are taken due to the risk of developingmore pronounced reduction blood pressure (for example, in patients with arrhythmias).

When treating patients with myocardial infarction or suspected of it, it is necessary to evaluate the basic parameters of hemodynamics after each injection of the drug at a dose of 5 mg (see section "Method of administration and dose").

Do not prescribe a second dose - the second or third at a heart rate of less than 40 beats / min, the interval PQ more than 0.26 seconds. and systolic blood pressure less than 90 mm Hg. st., as well as with increased dyspnea or the appearance of cold sweat.

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

Evaluation of the effect of Betaloc® on intravenous administration on the ability to drive vehicles and other mechanisms has not been studied.

Form release / dosage:

Solution for intravenous administration, 1 mg / ml.

Packaging:

5 ml per ampoule of colorless boron-silicate glass with a notch. 5 ampoules in a plastic holder in a cardboard box with instructions for use.

On an ampoule above a notch the colored point is put, put by a paint; above the dot are two colored rings.

Storage conditions:

In the dark place at a temperature below 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001402/07

Date of registration:06.07.2007

Expiration Date:Unlimited

The owner of the registration certificate:AstraZeneca ABAstraZeneca AB Sweden

Manufacturer: & nbsp

ASTRAZENECA, AB Sweden

Representation: & nbspAstraZeneca Pharmaceuticals Ltd.AstraZeneca Pharmaceuticals Ltd.

Information update date: & nbsp24.01.2017

Illustrated instructions

Instructions

Betaloc® (Betaloc®)