Metoprolol-Teva pills 100mg, 30pcs

Composition

1 tablet contains:

metoprolol tartrate 100 mg.

Auxiliary substances:

microcrystalline cellulose,

corn starch,

sodium croscarmelose,

copovidone,

colloidal anhydrous silicon dioxide,

magnesium stearate.

Pharmacological action

METOPROLOL-RATIOPHARM is a selective beta-blocker, acts mainly on the beta-1-adrenergic receptors of the heart (“cardioselective beta-blocker”) without internal sympathomimetic activity and with a weakly expressed membrane-stabilizing effect.

It has antianginal, antihypertensive and antiarrhythmic effects.

Blocking the beta-1-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular flow of calcium ions, has a negative chrono -, dromo -, batmo-and inotropic effect (reduces heart rate (HR), inhibits conduction and excitability, reduces myocardial contractility).

Total peripheral vascular resistance at the beginning of beta-blockers use (in the first 24 hours after oral use) increases (as a result of a reciprocal increase in alpha-adrenergic activity and elimination of beta-1 – adrenergic stimulation), which returns to its original value after 1-3 days, and decreases with prolonged use.

The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin system (of great importance in patients with initial hypersecretion of renin) and the central nervous system, restoration of the sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces high blood pressure (BP) at rest, during physical exertion and stress.

The hypotensive effect develops quickly (systolic blood pressure decreases in 15 minutes, maximum – in 2 hours) and lasts for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular intake.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases exercise tolerance.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in atrioventricular conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular (AV) node) and along additional pathways.

With supraventricular tachycardia, atrial fibrillation, sinus tachycardia, with functional heart diseases and hyperthyroidism, it reduces the heart rate or can even lead to the restoration of sinus rhythm. Prevents the development of migraines.

When used in medium therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on the organs containing beta-1-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of the peripheral arteries of the bronchi and uterus) and on carbohydrate metabolism. When used in large doses (more than 100 mg / day), it has a blocking effect on both subtypes of beta-adrenergic receptors.

Indications

• Arterial hypertension, including hyperkinetic type.
• Tachycardia.
• Coronary heart disease: myocardial infarction; prevention of angina attacks; supraventricular tachycardia; ventricular extrasystole.

Use during pregnancy and lactation

During pregnancy (especially in the first 3 months), the drug should be used only for strict indications, taking into account careful weighing of the benefit/risk ratio, since until now there is insufficient experience of its use during pregnancy, especially in the early stages of pregnancy.

If pregnant women have taken metoprolol, then due to the possibility of bradycardia, hypotension and hyperglycemia in the newborn, treatment is stopped 48-72 hours before the onset of labor. If this is not possible, then the newborn should be under particularly close supervision for 48-72 hours after delivery.

The effect of metoprolol on the newborn during breast-feeding has not been studied, so women taking the drug should stop breast-feeding.

Contraindications

• Hypersensitivity to metoprolol or other components of the drug, other beta-blockers.
• Heart failure in the stage of decompensation.
• Cardiogenic shock.
• Sinus node weakness syndrome, Prinzmetal angina pectoris.
• Grade II and III atrioventricular block.
• Sinoatrial blockade.
• Bradycardia (heart rate before treatment is less than 50 beats per minute).
• Arterial hypotension (if used for secondary myocardial prophylaxis, systolic blood pressure less than 100 mmHg).
• Metabolic acidosis.
• Late stages and severe peripheral circulatory disorders.
• Simultaneous use of MAO inhibitors.
• Lactation period.
• Age up to 18 years (efficacy and safety have not been established).
• Intravenous use of slow calcium channel blockers such as verapamil and diltiazem, or other antiarrhythmics (for example, disopyramide) is contraindicated during treatment with the drug. The exception is patients who are in intensive care units.

With extreme caution:

• Grade I atrioventricular block.
• Diabetes mellitus with strong fluctuations in blood sugar levels (the possibility of a severe hypoglycemic condition).
• Abstinence from eating during a religious fast and heavy physical activity (severe hypoglycemic conditions may occur).
• Pheochromocytoma.
• Chronic renal and/or hepatic insufficiency (when prescribing metoprolol to this category of patients, constant monitoring of the dynamics of the functional state of the liver and/or kidneys is necessary).
• Acute myocardial infarction (heart rate less than 45 beats / min, PQ interval more than 0.25 sec, systolic blood pressure less than 100 mm Hg).
• Manifest psoriasis or a personal or family history of psoriasis.
• Patients with peripheral circulatory disorders, including Raynaud’s syndrome.
• Patients undergoing desensitizing therapy or with a history of severe allergic reactions.
• Bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis).
• Thyrotoxicosis.
• Depression (including a history of depression).
• Pregnancy.
• Advanced age.

In all these cases, the attending physician should carefully weigh the benefit / risk ratio when prescribing the drug.

Side effects

Nervous system disorders:  increased fatigue, weakness, headache, slowing of the speed of mental and motor reactions; rarely – paresthesia in the extremities (in patients with intermittent claudication and Raynaud’s syndrome), depression, anxiety, decreased attention, drowsiness, insomnia, nightmares, confusion or short-term memory impairment, muscle weakness.

From the side of the senses:  rarely-decreased vision, decreased secretion of tear fluid, dry and painful eyes, conjunctivitis, tinnitus.

From the cardiovascular system:  sinus bradycardia, palpitations, decreased blood pressure, orthostatic hypotension, dizziness, sometimes loss of consciousness); rarely-decreased myocardial contractility, temporary aggravation of symptoms of chronic heart failure (edema, swelling of the feet and/or lower legs, shortness of breath), arrhythmias, angiospasm (increased peripheral circulatory disorders, cold of the lower extremities, Raynaud’s syndrome), impaired myocardial conduction, cardialgia.

From the digestive system:  nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, liver dysfunction, taste changes.

From the side of the skin:  urticaria, pruritus, rash, psoriasis exacerbation, psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.

Respiratory system disorders:  nasal congestion, difficulty exhaling (bronchospasm when administered in high doses – loss of selectivity and/or in predisposed patients), shortness of breath.

From the endocrine system:  hypoglycemia (in patients receiving insulin), rarely: hyperglycemia (in patients with diabetes mellitus), hypothyroidism.

Laboratory parameters:  rarely-thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes; extremely rarely-hyperbilirubinemia.

Effect on the fetus:  possible intrauterine growth retardation, hypoglycemia, bradycardia.

Other services:  pain in the back or joints, like all beta-blockers, in isolated cases can cause a slight increase in body weight, a decrease in libido and / or potency.

Interaction

Concomitant use with monoamine oxidase (MAO) inhibitors is not recommended due to a significant increase in the hypotensive effect. The treatment interval between taking MAO inhibitors and metoprolol should be at least 14 days.

Simultaneous intravenous use of verapamil may cause cardiac arrest.Simultaneous use of nifedipine leads to a significant decrease in blood pressure.

Inhaled anaesthetic agents (hydrocarbon derivatives) increase the risk of myocardial function depression and hypotension.

Beta-adrenostimulants, theophylline, cocaine, estrogens (sodium retention), Indometacin and other nonsteroidal anti-inflammatory drugs (sodium retention and blocking prostaglandin synthesis by the kidneys) weaken the hypotensive effect.

There is an increase in the depressive effect on the central nervous system – with ethanol ; summation of the cardiodepressive effect – with anesthesia; an increase in the risk of peripheral circulatory disorders – with ergot alkaloids.

When taken together with oral hypoglycemic agents, their effect may decrease; with insulin, it may increase the risk of hypoglycemia, increase its severity and lengthening, masking some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

When combined with antihypertensive agents, diuretics, nitroglycerin or slow calcium channel blockers, a sharp decrease in blood pressure may develop (special caution is necessary when combined with prazosin); an increase in the severity of heart rate reduction and atrioventricular conduction depression when using metoprolol with verapamil, diltiazem, antiarrhythmic agents (amiodarone), reserpine, clonidine, guanfacine, general anesthesia and cardiac glycosides.

Inducers of microsomal liver enzymes (rifampicin, barbiturates) lead to an increase in metoprolol metabolism, a decrease in the concentration of metoprolol in blood plasma and a decrease in the effect.

Inhibitors (cimetidine, oral contraceptives, phenothiazines) – increase the concentration in blood plasma.

Allergens used for immunotherapy or allergen extracts for skin tests when combined with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine-containing radiopaque substances for intravenous use increase the risk of anaphylactic reactions.

Reduces the clearance of xanthine (except diphylline), especially in patients with initially increased clearance of theophylline under the influence of smoking. Reduces the clearance of lidocaine, increases the concentration of lidocaine in blood plasma. Enhances and prolongs the action of antidepolarizing muscle relaxants; prolongs the anticoagulant effect of coumarins.

When combined with ethanol, the risk of a pronounced decrease in blood pressure increases.

How to take, course of use and dosage

Tablets are taken orally with a small amount of liquid, without chewing, with a meal or immediately after a meal. Tablets can be divided. The course of treatment is not limited in time and depends on the characteristics of the course of the disease. If it is necessary to cancel treatment, the dose is reduced gradually (at least for 10 days). under the supervision of a doctor.

Arterial hypertension-the initial daily dose is 50-100 mg in 1-2 doses (morning and evening). If the therapeutic effect is insufficient, the daily dose can be gradually increased to 100-200 mg. The maximum daily dose is 200 mg.

Angina pectoris, arrhythmias, prevention of migraine attacks – 100-200 mg per day in two doses (morning and evening).

Secondary prevention of myocardial infarction-200 mg per day in two doses (morning and evening).

Functional disorders of cardiac activity, accompanied by tachycardia-100 mg per day in two doses (morning and evening).

When the therapeutic effect is achieved, the dose is reduced (under the supervision of a doctor). Elderly patients are recommended to start treatment with 50 mg / day.

Overdose

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, syncope, acute overdose – cardiogenic shock, loss of consciousness, coma, atrioventricular block (up to the development of complete transverse block and cardiac arrest), cardialgia. The first signs of overdose appear in 20 minutes-2 hours after taking the drug. Treatment: gastric lavage and use of adsorbents; symptomatic therapy: with a pronounced decrease in blood pressure, the patient should be in the Trendelenburg position; in case of excessive decrease in blood pressure, bradycardia and heart failure-IV, at intervals of 2-5 minutes, bata-adrenostimulants-until the desired effect is achieved or iv 0.5-2 mg of atropine sulfate. In the absence of a positive effect – dopamine, dobutamine or norepinephrine (norepinephrine). As a follow-up, it is possible to prescribe 1-10 mg of glucagon, setting up a transvenous intracardial electrostimulator. In case of bronchospasm, intravenous beta-1-adrenergic stimulants should be administered. For convulsions-slow intravenous use of diazepam. Hemodialysis is not effective.

Special instructions

Monitoring of patients taking beta-blockers includes regular monitoring of heart rate and blood pressure, blood glucose in patients with diabetes mellitus (1 time in 4-5 months).

If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents prescribed by mouth should be selected individually.

The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

When taking a dose higher than 200 mg per day, cardioselectivity decreases.

In heart failure, treatment with metoprolol begins only after reaching the compensation stage. It is possible to increase the severity of hypersensitivity reactions (against the background of a burdened allergic history) and the lack of effect from the introduction of conventional doses of epinephrine (epinephrine). It may increase the symptoms of peripheral arterial circulation disorders.

Discontinuation of the drug is carried out gradually, reducing the dose over 10 days. If treatment is abruptly discontinued, a “withdrawal” syndrome may occur (increased angina attacks, increased blood pressure). Special attention should be paid to patients with angina pectoris when discontinuing the drug.

With angina pectoris, the selected dose of the drug should provide a resting heart rate in the range of 55-60 beats / min, with a load of no more than 110 beats / min.

Patients who use contact lenses should take into account that against the background of treatment with beta-blockers, tear fluid production may decrease.

Metoprolol may mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase symptoms.

In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels.

If necessary, beta-2-adrenostimulants are used as concomitant therapy for patients with bronchial asthma; alpha-adrenoblockers are used for pheochromocytoma.

If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being performed (choosing a general anesthesia agent with minimal negative inotropic effect), and discontinuing the drug is not recommended.

Drugs that reduce the supply of catecholamines (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be constantly monitored by a doctor for excessive lowering of blood pressure and bradycardia.

Special monitoring should be carried out for patients with depressive disorders taking metoprolol; in case of depression caused by taking beta-blockers, it is recommended to stop therapy.

During treatment with metoprolol, appropriate clothing should be worn, as the drug may cause skin allergies to sunlight.

In elderly patients, monitoring of liver function is recommended. Correction of the dosage regimen is required only if elderly patients develop increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver function disorders, and sometimes it is necessary to stop treatment.

Due to the lack of sufficient clinical data, the drug is not recommended for use in children.

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, and to exclude the use of ethanol.

Form of production

Pills.

Storage conditions

Store at a temperature not exceeding 30°C. Keep out of reach of children.

Shelf

life is 5 years.

Active ingredient

Metoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, for pregnant women as prescribed by a doctor

Indications

Angina, Myocardial Infarction, Arrhythmia, Migraine, Hypertension