A CARDIOLOGICAL GROUP
Active material: Metoprolol
When ATH: C07AB02
CCF: Beta1-adrenoblokator
ICD-10 codes (testimony): G43, I10, i20, I21, I47.1, I49.4
When CSF: 01.01.01.02
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Pills white or nearly white, round, lenticular, with Phillips dividing line and double bevel on one side and engraving “(E) 435” – on the other side, without smell.
1 tab. | |
metoprolol tartrate | 25 mg |
Excipients: microcrystalline cellulose, sodium carboxymethyl, Colloidal anhydrous silica, povidone, magnesium stearate.
30 PC. – jars of dark glass (1) – packs cardboard.
60 PC. – jars of dark glass (1) – packs cardboard.
Pills white or nearly white, round, lenticular, with Valium on one party and chasing “(E) 434” – on the other side, without smell.
1 tab. | |
metoprolol tartrate | 50 mg |
Excipients: microcrystalline cellulose, sodium carboxymethyl, Colloidal anhydrous silica, povidone, magnesium stearate.
30 PC. – jars of dark glass (1) – packs cardboard.
60 PC. – jars of dark glass (1) – packs cardboard.
Pills white or nearly white, round, lenticular, with Valium on one party and chasing “(E) 432” – on the other side, without smell.
1 tab. | |
metoprolol tartrate | 100 mg |
Excipients: microcrystalline cellulose, sodium carboxymethyl, Colloidal anhydrous silica, povidone, magnesium stearate.
30 PC. – jars of dark glass (1) – packs cardboard.
60 PC. – jars of dark glass (1) – packs cardboard.
Pharmacological action
Kardioselektivnyj β-adrenoceptor Blocker, without internal sympathomimetic and membranostabilizirujushhej activity. Provides antihypertensive, antianginalnoe and antiaritmicescoe action.
Blocking in low doses β1-adrenergic receptors of the heart, reduces the formation of catecholamines stimulated cAMP from ATP, reduces intracellular current Ca2+, It has a negative chrono, dromo-, ʙatmo- and inotropic effect (slows heart rate, oppressing conductivity and anxiety, reduces myocardial contractility).
PR at the beginning of the drug (first 24 hours after oral administration) increases, through 1-3 day use returned to the original level, upon further application – decreases.
Antihypertensive activity due to a decrease in cardiac output and synthesis of Renin, inhibition of the Renin-angiotensin system and central nervous system, restoring sensitivity of aortic arch baroreceptors (not going to enhance their activity in response to the decline of HELL) and in the end reduced peripheral sympathetic influences. Reduces increased ad alone, the physical tension and stress.
HELL is reduced through 15 m, maximally – through 2 no; the action lasts for 6 no. There has been a steady decline after a few weeks of regular admission.
Antianginalny effect is determined by the reduction in myocardial oxygen demand as a result of a decrease in HEART RATE (the lengthening of the diastolic pressure and myocardial perfusion improvement) and contractility, as well as the decrease in myocardial sensitivity to the effects of the sympathetic innervation. Reduces the frequency and severity of angina attacks and increases portability physical loads.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of sympathetic nervous system, increase of cyclic AMP, arterial hypertension), decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing AV-conduction (mainly in the antegrade and, less, in retrograde direction through the AV-node) and on additional routes.
With supraventricular tachycardia, atrial fibrillation, Sinus tachycardia with functional heart disease and hyperthyroidism HEART RATE slows and may even lead to the restoration of sinus rhythm.
Prevents migraine.
When long-term admission to reduces cholesterol in the blood.
When used in therapeutic doses, medium has less pronounced impact on, содержащие b2-adrenoreceptory (pancreas, skeletal muscle, smooth muscle peripheral arteries, bronchi, uterus) and carbohydrate metabolism.
When used in high doses (more 100 mg / day) It exerts a blocking effect on both subtypes of β-adrenoceptor.
Pharmacokinetics
Absorption
Quickly and completely (95%) absorbed from the gastrointestinal tract. Cmax plasma achieved through 1.5-2 hours after ingestion. Bioavailability is 50%. During the treatment the bioavailability increases to 70%. Food increases the bioavailability of the 20-40%.
Distribution
Vd is 5.6 l / kg. The binding to plasma proteins – 12%. Penetrates the GEB and placental barrier. Is the breast milk in small quantities.
Metabolism
Metoprolol biotransformiroetsa in the liver. Metabolites not possess pharmacological activity.
Deduction
T1/2 averages 3.5-7 no. Metoprolol is almost completely excreted in the urine for 72 no. About 5% the dose is excreted unchanged in.
Pharmacokinetics in special clinical situations
When expressed violations of the liver bioavailability and T1/2 Metoprolol is increased, which may require correction dose.
If any of the kidneys (T)1/2 systemic clearance and metoprolol did not significantly change.
Testimony
- Arterial hypertension (in monotherapy or in combination with other antigipertenzivei drugs), incl. Hyperkinetic type;
- CHD (secondary prevention of myocardial infarction, prevention of angina attacks);
- Heart rhythm disturbances (supraventricular arrhythmias, ventricular premature beats);
- Hyperthyroidism (in the complex therapy);
-Prevention of migraine attacks.
Dosage regimen
At hypertension administered in a daily dose of 50-100 mg / day 1 or 2 admission (in the morning and in the evening). The lack of therapeutic effect of gradual increase in daily doses up to 100-200 mg.
At angina, najeludockovh aritmiah, to Prevention of migraines administered at a dose of 100-200 mg / day 2 admission (in the morning and in the evening).
To secondary prevention of myocardial infarction appoint in the average daily dose 200 mg 2 admission (in the morning and in the evening).
At functional disorders of cardiac activity, accompanied by tachycardia, administered in a daily dose of 100 mg 2 admission (in the morning and in the evening).
In elderly patients, patients with impaired renal function, as well as, if necessary, of the kidney changes in dosage is not required.
In Patients with severe hepatic impairment the drug should be used in smaller doses, in view of the slow metabolism of metoprolol.
The tablets should be taken inside during or immediately after a meal. Tablets can be split in half, but don't chew.
Side effect
From the central and peripheral nervous system: fatigue, weakness, headache, slowing of mental and motor responses; rarely – paresthesias in extremities, depression, anxiety, decreased ability to concentrate, drowsiness, insomnia, nightmares, confusion or short-term memory, asthenic syndrome, muscular weakness.
From the senses: rarely – reduced vision, reduced secreta slezna fluid, kseroftalm, conjunctivitis, noise in ears.
Cardio-vascular system: sinusovaya bradycardia, heartbeat, decrease in blood pressure, orthostatic hypotension; rarely – reducing sokratimosti attack, a temporary exacerbation of symptoms of chronic heart failure, Arrhythmia, increased violations of peripheral blood circulation (coldness of the lower extremities, Raynaud's syndrome), conduction disturbances infarction; in a few cases – AV блокада, kardialgija.
From the digestive system: nausea, vomiting, stomach ache, diarrhea, constipation, dry mouth, change in taste; increase in liver transaminases; rarely – giperʙiliruʙinemija.
Dermatological reactions: hives, itching, rash, exacerbation of psoriasis, psoriasiform skin changes, dermahemia, rash, photodermatoses, increased sweating, obratimaya alopecia.
The respiratory system: nasal congestion, difficulty exhaling (bronchospasm in the appointment of high doses or predisposed patients), breathlessness.
On the part of the endocrine system: gipoglikemiâ (patients, receiving insulin); rarely – giperglikemiâ.
From the hematopoietic system: thrombocytopenia, agranulocytosis, leukopenia.
Other: back pain or joint pain, a slight increase in body mass index, decreased libido and / or potency.
Contraindications
- Cardiogenic shock;
— AV-blockade II and III degrees;
- Sinoatrialynaya blockade;
- SSS;
- Vыrazhennaya bradycardia (Heart Rate<50 u. / min);
- Heart failure decompensation;
- Angiospastic angina (Prinzmetal angina);
- Severe hypotension (systolic blood pressure<100 mmHg.);
- Lactation;
- Simultaneous MAO inhibitors;
-simultaneous in/with the introduction of Verapamil;
-hypersensitivity to metoprololu and other ingredients of the drug.
FROM caution should be prescribed for patients with diabetes, metabolic acidosis, asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis), Obliterative diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome), chronic liver failure, chronic renal failure, myasthenia, pheochromocytoma, AV-blockade I degree, thyrotoxicosis, depression (incl. history), psoriaze, pregnancy, as well as children and adolescents under the age of 18 years, elderly patients.
Pregnancy and lactation
Use Jegiloka® Pregnancy may only, when the intended benefits to the mother outweighs the potential risk to the fetus. If necessary, the appointment of the drug during this period should be careful monitoring of the fetus and newborn during 48-72 hours after childbirth, because of possible intrauterine growth retardation, bradycardia, hypotension, respiratory depression, gipoglikemiâ.
Influence of metoprolol on newborn baby during breast-feeding is not known, Therefore, women, host a cardiological group®, should stop breastfeeding.
Cautions
In appointing the drug a cardiological group® should regularly monitor the HR and ad. Patients should be warned, What if HR<50 beats/min a doctor's consultation.
In patients with diabetes mellitus should regularly monitor the level of glucose in the blood and, if necessary, a correction dose of insulin or gipoglikemicakih oral drugs.
Appointment Of Jegiloka® patients with chronic heart failure is possible only after reaching the stage of compensation.
Patients, host a cardiological group®, may increase the severity of hypersensitivity reactions (with aggravated allergic history) and lack of effect from the introduction of conventional doses of epinephrine (adrenaline).
Against the backdrop of Jegiloka® possible aggravation of the symptoms of human peripheral blood circulation.
A cardiological group® should be lifted gradually, consistently reducing the dose for 10 days. In a dramatic treatment may arise syndrome (increasing angina attacks, increased blood pressure). During the period of preparation for patients with angina should be under close medical supervision.
When strokes voltage selected dose should provide heart rate at rest within 55-60 u. / min, under load – no more 110 u. / min.
Patients, use contact lenses, We should take into account, that treatment with beta-adrenoblokatorami may reduce slezna fluid.
Metoprolol may mask some of the clinical manifestations of hyperthyroidism (taxikardiju). Sudden removal in patients with thyrotoxicosis is contraindicated, because the symptoms can increase.
Diabetes mellitus receiving Jegiloka® may mask symptoms gipoglikemii (taxikardiju, Sweating, increased blood pressure).
In the appointment of metoprolol in patients with bronchial asthma must be simultaneous application beta2-adrenomimetikov.
In patients with feohromotsytoma a cardiological group® should be used in conjunction with alpha-adrenergic.
Before carrying out any surgical procedure you must inform the anesthesiologist about the therapy Jegilokom® (selection of drugs for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not required.
In appointing the drug for older patients should regularly monitor liver function. Correction mode is required only in the case of elderly patients increasing bradycardia, significant decrease in blood pressure, AV-blockade, bronchospasm, ventricular arrhythmias, severe violations of the liver. Sometimes it is necessary to discontinue treatment.
Should conduct special monitoring of patients with depressive disorders in anamnesis. In the case of the development of depression a cardiological group® should be abolished.
If you are applying to Jegiloka® with clonidine Jegiloka cancelled® clonidine should be lifted after a few days (with regard to the risk of the syndrome).
Preparations, reducing stocks catecholamines (eg, reserpine) may enhance the action of beta-blockers, so patients, accepting such combination drugs, should be under constant medical supervision to identify excessive loss AD or bradycardia.
Use in Pediatrics
The efficacy and safety of Jegiloka® in children and adolescents under the age of 18 years not determined.
Effects on ability to drive vehicles and management mechanisms
Patients, activities that require increased attention, the question of the appointment of the drug on an outpatient basis should be decided only after an assessment of the individual patient's response.
Overdose
Symptoms: vыrazhennaya sinusovaya bradycardia, dizziness, nausea, vomiting, cyanosis, hypotension, arrhythmia, ventricular premature beats, bronchospasm, fainting; in acute overdose – cardiogenic shock, loss of consciousness, coma, AV-blokada until development complete transverse blockade and heart failure, kardialgija.
The first signs of an overdose appear 20 min-2 h after administration.
Treatment: gastric lavage, appointment of adsorbents, simptomaticheskaya therapy: In marked decrease in blood pressure – Trendelenburg position, in the case of acute arterial hypotension, bradycardia and threatening congestive heart failure – I / (intervals 2-5 m) the introduction of beta-adrenostimuljatorov or/introduction 0.5-2 mg of atropine sulfate, in the absence of positive effect – Dopamine, dobutamine or norepinephrine. As a follow-up to the appointment 1-10 mg of glucagon, setting transvenoznogo intrakardialnogo electrostimulator. When bronchospasm – in/in the introduction of beta2-adrenostimuljatorov, with cramps – slow in / diazepam. Metoprolol bad displays using hemodialysis.
Drug Interactions
If you are applying to Jegiloka® with MAO inhibitors may significantly strengthened gipotenzivnogo actions. The interval between receiving MAO inhibitors and Jegiloka® must be at least 14 days.
Simultaneous in/with the introduction of Verapamil can trigger cardiac arrest, the simultaneous appointment nifedipina leads to significant reduction of HELL.
Means for inhalation anesthesia (hydrocarbon derivatives) together with the application Jegilokom® increase the risk of oppression of myocardial contractility, and arterial hypotension development.
Together with the use of beta-adrenostimuljatory, theophylline, cocaine, Estrogens, indomethacin and other NSAIDS reduce gipotenzivny effect Jegiloka®.
If you are applying to Jegiloka® and increasing ethanol oppressive action on the central nervous system.
If you are applying to Jegiloka® with ergot amplified risk of peripheral blood circulation.
If you are applying a cardiological group® increases effect gipoglikemicakih oral drugs and insulin and increases the risk of hypoglycemia.
If you are applying to Jegiloka® with antigipertenzivei means, Diuretics, nitratami, blokatorami calcium channels increases the risk of arterial hypotension.
If you are applying to Jegiloka® with Verapamil, diltiazemom, antiarrhythmic drugs (Amiodarone), reserpine, methyldopa, clonidine, guanfacinom, funds for general anesthesia and cardiac glycosides may experience increased symptoms urezhenija curves and oppression AV conduction.
Inductors of microsomal liver enzymes (rifampicin, barbiturates) accelerate the metabolism of metoprolol, resulting in lower concentration metoprolola plasma and Jegiloka effect reduction®.
Liver microsomal enzymes inhibitors (cimetidine, oral contraceptives, fenotiazinы) increase concentration metoprolola plasma.
Allergens, used for immunotherapy, or allergen extracts for skin samples in a joint application with Jegilokom®, the risk of systemic allergic reactions or anaphylaxis.
Some iodine rentgenocontrast materials for the on/in the introduction together with the application Jegilokom® increase the risk of developing anaphylactic reactions.
A cardiological group® While applying reduces clearance xantinov, especially in patients with initially increased clearance of theophylline under the influence of smoking.
Together with the application Jegilokom® reduced clearance of lidocaine and lidocaine concentrations in plasma.
If you are applying a cardiological group® enhance and prolong the effect nedepoliarizuth miorelaksantov; extends the activity proximity anticoagulants.
When coupled with the use of ethanol increases the risk reduction expressed HELL.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children at temperature from 15 ° to 25 ° C. Shelf life – 5 years.