Description
Release form
Intravenous solution.
Packing
5 pcs. 5 ml each.
Pharmacological action of
In patients with myocardial infarction, intravenous administration of metoprolol reduces chest pain and reduces the risk of atrial fibrillation and flutter. Intravenous administration of metoprolol at the first symptoms (within 24 hours after the first symptoms appear) reduces the risk of myocardial infarction. The early initiation of metoprolol treatment improves the further prognosis of treatment for myocardial infarction.
Achieved reduction in heart rate (HR) with paroxysmal tachycardia and atrial fibrillation (flutter).
Metoprolol is a 1-blocker that blocks 1 receptors at doses much lower than the doses required to block 2 receptors. Metoprolol has a slight membrane-stabilizing effect and does not show the activity of a partial agonist. Metoprolol reduces or inhibits the agonistic effect that catecholamines, which are formed during nervous and physical stresses, exert on the cardiac activity. This means that metoprolol has the ability to prevent an increase in heart rate, minute volume and increased myocardial contractility, as well as an increase in blood pressure caused by the release of catecholamines. If necessary, patients with symptoms of obstructive pulmonary disease may be prescribed metoprolol in combination with 2-adrenergic agonists. When used together with Betaloc ® 2-adrenomimetics in therapeutic doses, it affects the bronchodilation caused by 2-adrenomimetics to a lesser extent than non-selective -Adrenergic blockers.
Metoprolol to a lesser extent than non-selective -adrenoblocks. affect insulin production and carbohydrate metabolism. The effect of Betaloc ® on the reaction of the cardiovascular system under hypoglycemia is significantly less pronounced compared with non-selective -Adrenergic blockers. Improving the quality of life during treatment with Betaloc was observed in patients after myocardial infarction.
Contraindications
Atrioventricular block II and III degree.
Decompensated heart failure.
Clinically significant sinus bradycardia.
Sick sinus syndrome.
Cardiogenic shock.
Severe peripheral circulatory disorders.
Arterial hypotension.
Patients with acute myocardial infarction with a heart rate of less than 45 beats per minute, PQ interval more than 0.24 seconds or systolic blood pressure less than 100 mm Hg
For serious peripheral vascular disease with the threat of gangrene.
Intravenous administration of ² Ñslow ² Ñ calcium channel blockers such as verapamil is contraindicated in patients receiving -adrenergic blockers.
Age under 18 years (efficacy and safety not established).
Known hypersensitivity to metoprolol and its components or to other -adrenergic blockers.
Precautions: atrioventricular block I degree, Prinzmetal angina, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis, bronchial asthma), diabetes mellitus, severe renal failure.
Use during pregnancy and lactation
Pregnancy: Like most drugs, Betalok ® should not be prescribed during pregnancy and during lactation, unless the expected benefit to the mother outweighs the potential risk to the fetus. Like other antihypertensive drugs, β-blockers can cause side effects, such as bradycardia in the fetus, newborns or breast-fed babies, therefore, one should be especially careful when prescribing -adrenoblockers in the last trimester of pregnancy and immediately before childbirth.
Lactation: the amount of metoprolol that is excreted in breast milk, and – the blocking effect in a breast-fed baby (when the mother takes metoprolol in therapeutic doses), are negligible.
Special instructions
Patients taking -adrenergic blockers should not be given intravenous ² Ñslow ² Ñ calcium channel blockers such as verapamil. To patients suffering from bronchial asthma or obstructive pulmonary disease, concomitant bronchodilation therapy should be prescribed. If necessary, increase the dose of 2-adrenergic agonist. When using 1-blockers, the risk of their effect on carbohydrate metabolism or the possibility of masking hypoglycemia is significantly less than when using non-selective -Adrenergic blockers.
In patients with chronic heart failure in the stage of decompensation, it is necessary to achieve the stage of compensation both before and during treatment with the drug.
Patients with Prinzmetal angina are not recommended to prescribe non-selective -adrenergic blockers.
Very rarely, patients with impaired atrioventricular conduction may worsen (a possible outcome is atrioventricular block). If bradycardia develops during treatment, the dose of Betalock should be reduced. Metoprolol may worsen symptoms of peripheral arterial circulatory disorders due to lower blood pressure. Caution should be exercised when prescribing the drug to patients suffering from severe renal failure, with metabolic acidosis, co-administration with cardiac glycosides. In patients taking -blockers, anaphylactic shock occurs in a more severe form. Patients suffering from pheochromocytoma, in parallel with the drug Betalok, should be prescribed alpha-alrenoblocker. In case of surgery, the anesthetist should be informed that the patient is taking -Adrenoblocker. Do not prescribe a second dose – a second or third with a heart rate of less than 40 beats per minute, PQ interval of more than 0.26 seconds and systolic blood pressure of less than 90 mm Hg
Composition
1 ml of solution contains:
Active substances: metoprolol tartrate for injection – 1 mg.
Excipients: sodium chloride for injection – 9 mg water for injection – up to 1 ml.
Dosage and administration of
Supraventricular tachycardia: begin administration with 5 mg (5 ml) of Betalok at a rate of 1 2 mg / min. You can repeat the introduction with a 5-minute interval until a therapeutic effect is achieved. Typically, the total dose is 10-15 mg (10-15 ml). The recommended maximum dose for intravenous administration is 20 mg (20 ml).
Prevention and treatment of myocardial ischemia, tachycardia and pain with or suspected myocardial infarction: intravenously 5 mg (5 ml) of the drug. You can repeat the introduction at 2 minute intervals, maximum dose is 15 mg (15 ml). 15 minutes after the last injection, metoprolol is prescribed for oral administration at a dose of 50 mg (Betalok) 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 a low degree of binding to plasma proteins, dose adjustment is not required. However, in severely impaired liver function (in patients with portocaval anastomosis), a dose reduction may be required.
Elderly: there is no need to adjust the dose in elderly patients.
Children: The experience with Betaloc in children is limited.
Side effects
Betal is well tolerated by patients and the side effects are mostly mild and reversible.
As a result of clinical trials or with the use of Betalok (metoprolol tartrate), the following undesirable side effects have been described in clinical practice. In many cases, a causal relationship with Betalok treatment has not been established.
The following criteria were used to assess the incidence of cases: Very often (> 10%).
Often (1-9.9%).
Infrequently (0.1-0.9%).
Rarely (0.01-0.09%).
Very rare (<0.01%). Cardiovascular system: often – bradycardia, postural disorders (very rarely accompanied by fainting), cold extremities, palpitations infrequently – temporary increase in symptoms of heart failure, cardiogenic shock in patients with acute myocardial infarction AV block I degree rarely – other cardiac conduction disorders, arrhythmias very rarely – gangrene in patients with previous severe peripheral circulatory disorders. CNS: very often – increased fatigue often – dizziness, headache rarely – increased nervous irritability, anxiety, impotence / sexual dysfunction infrequently – paresthesia, cramps, depression, decreased attention, drowsiness or insomnia, nightmares very rarely – amnesia / memory impairment depression, hallucinations. GIT: often – nausea, abdominal pain, diarrhea, constipation infrequently – vomiting rarely – dry mouth. Liver: rarely – impaired liver function. Skin: infrequently – rash (in the form of urticaria), excessive sweating rarely – hair loss is very rare – photosensitivity, exacerbation of psoriasis. Respiratory: often – shortness of breath with physical effort infrequently – bronchospasm in patients with bronchial asthma rarely – rhinitis. Sensory organs: rarely – visual impairment, dryness and / or eye irritation, conjunctivitis very rarely – tinnitus, taste disturbances. Metabolism: infrequently – weight gain. From the side of the musculoskeletal system: very rarely – arthralgia. Blood: very rarely – thrombocytopenia. Drug interactions Betaloc ® should not be co-administered with the following drugs: Barbiturate derivatives: barbiturates (tested with phenobarbital) slightly increase metoprolol metabolism due to enzyme induction. Propafenone: when prescribing propafenone to four patients treated with metoprolol, a 2 5-fold increase in the plasma concentration of metoprolol is noted. however, two patients had side effects characteristic of metoprolol. This interaction was confirmed in a study of 8 volunteers. The interaction is probably due to the inhibition by propafenone, like quinidium, of metoprolol metabolism via the cytochrome P4502D6 system. Taking into account the fact that propafenone has the properties of a β-blocker, the combined administration of metoprolol and propafenone does not seem appropriate. 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-blockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function. Combination of Betaloc with the following drugs, which may require dose adjustment: Class I antiarrhythmic drugs: Class I antiarrhythmic drugs and β-blockers can lead to a summation of the negative inotropic effect, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function. A similar combination should also be avoided in patients with sick sinus syndrome and atrioventricular conduction disturbance. The interaction is described by the example of a disopyramid. 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), one should take into account the possible interaction long after the withdrawal of amiodarone. Nonsteroidal anti-inflammatory drugs (NSAIDs): NSAIDs weaken the antihypertensive effect of β-blockers. This interaction is most documented for indomethacin. No described interaction was noted for sulindac. In studies with diclofenac, the described reaction was not observed. Diphenhydramine: Diphenhydramine reduces the clearance of metoprolol to -hydroxymethoprolol by 2.5 times. At the same time, an increase in the action of metoprolol is observed. Epinephrine (adrenaline): 10 cases of severe arterial hypertension and bradycardia have been reported in patients taking non-selective β-blockers (including pindolol and proprapolol) and receiving epinephrine (adrenaline). The interaction was also noted in the group of healthy volunteers. It is assumed that similar reactions can be observed with the use of epinephrine in conjunction with local anesthetics in case of accidental entry into the vascular bed. Supposed that this risk is much lower with cardioselective β-blockers. Phenytropanolamine: Phenylpropanolamine (norephedrine) in a single dose of 50 mg can cause an increase in diastolic blood pressure to pathological values in healthy volunteers. Propranolol basically inhibits the increase in blood pressure caused by phenylpropanolamine. However, β-adrenergic blocking agents can cause reactions of naroloxal arterial hypertension in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported with phenylpropanolamine. Quinidine: Quinidine inhibits metoprolol metabolism in a special group of patients with fast hydroxylation (approximately 90% of the population in Sweden), mainly causing a significant increase in the plasma concentration of metoprolol and an increase in β-blockade. Believe that such an interaction is also characteristic of other β-blockers in the metabolism of which cytochrome P4502D6 is involved. Clonidine: Hypertensive reactions with abrupt cancellation of clonidine may be enhanced with co-administration of -adrenergic blockers. When used jointly, in case of withdrawal of clonidine. discontinuation of β-blockers should begin a few days before the cancellation of clonidine. Rifampicin: Rifampicin may enhance metoprolol metabolism by decreasing the plasma concentration of metoprolol. The concentration of metoprolol in blood plasma may increase when combined with cimegidine, hydratazip, selective serotonin inhibitors such as paroxetine, fluoxetine and sertratin. Patients taking metoprolol and other β-blockers (eye drops) or monoamine oxidase inhibitors (MAOs) at the same time, must be closely monitored. While taking β-blockers, inhaled anesthetics enhance the cardiac depressant effect. Against the background of taking β-blockers, patients receiving oral hypoglycemic agents may need a dose adjustment of the latter. Cardiac glycosides when used together with β-blockers can increase the time of atrioventricular conduction and cause bradycardia. Overdose Toxicity: Metoprolol at a dose of 7.5 g in adults has caused fatal intoxication. A 5-year-old child receiving 100 mg of metoprolol had no signs of intoxication after gastric lavage. Taking 450 mg of metoprolol by a 12-year-old teenager resulted in moderate intoxication. Reception 1, 4 g and 2.5 g of metoprolol in adults caused moderate and severe intoxication, respectively. The intake of 7.5 g by adults resulted in extremely severe intoxication. Symptoms: Symptoms from the cardiovascular system are the most serious symptoms of metoprolol overdose, but sometimes, especially in children and adolescents, CNS symptoms and pulmonary function suppression may prevail. Bradycardia, atrioventricular blockade of I-lII degree, asystole, pronounced decrease in blood pressure, weak peripheral perfusion, heart failure, cardiogenic shock, inhibition of lung function, apnea, increased fatigue, impaired consciousness, loss of consciousness, loss of consciousness, , nausea, vomiting, esophageal spasm, hypoglycemia (especially in children) or hyperglycemia, hypercalcemia, effects on the kidneys, transient myasthenic syndrome. Concomitant use of alcohol, antihypertensive drugs, quinidine or barbiturates may worsen the patient’s condition. The first signs of overdose can be observed 20 min – 2 hours after the administration of the drug. Treatment: appointment of activated charcoal, if necessary gastric lavage. IMPORTANT! Atropine (0.25-0.5 mg / v for adults, 10-20 mcg / kg for children) should be given before gastric lavage (because of the risk of vagus nerve stimulation). If necessary – maintaining the airway (intubation) and adequate ventilation. Blood volume replenishment and glucose infusion. ECG monitoring. Atropine 1.0-2.0 mg I / O, repeat if necessary (especially in the case of vagal symptoms). In the case of (suppression) of myocardial depression, infusional administration of dobutamine or dopamine is indicated. Glucagon of 50-150 μg / kg I / O may be used at 1 minute intervals. In some cases, adrenaline may be an effective addition to therapy. With arrhythmia and enlargement of the ventricular complex (QRS), sodium (chloride or bicarbonate) solutions are infused. Installation of an artificial rhythm driver is possible. In case of cardiac arrest due to overdose, resuscitation may be needed within a few hours. Terbutaline (injectable or by inhalation) can be used to treat bronchospasm. Symptomatic treatment is carried out. Storage Conditions In a dark place at a temperature below 25 ° C. Keep out of the reach and sight of children. Shelf life 5 years. dosage form infusion solution Appointment Appointment Adult on prescription AstraZeneca, Britain
