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Active ingredients
Metoprolol
Release form
Pills
Composition
Metoprolol tartrate 100 mg; excipients: lactose, povidone, talc, magnesium stearate, microcrystalline cellulose, rice starch.
Pharmacological effect
A cardioselective beta1-adrenoblocker with no internal sympathomimetic activity and membrane stabilizing properties. It has antihypertensive, antianginal, antiarrhythmic effects .; By blocking β1-adrenoreceptors of the heart in low doses, it reduces catecholamine-stimulated cAMP formation from ATP, reduces the intracellular current of Ca2 +, has a negative chrono-dromo, batmoy and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility) .; OPS at the beginning of beta-blockers (in the first 24 hours after oral administration) increases (as a result of the reciprocal increase in β-adrenoreceptor activity and the removal of β2-adrenoreceptor stimulation), which returns to baseline after 1-3 days, and decreases with long-term administration ; Acute antihypertensive effect is due to a decrease in cardiac output, a stable antihypertensive effect develops within 2-3 weeks and is due to a decrease in renin synthesis and accumulation of plasma renin, inhibition of the activity of the renin-angiotensin system (important for patients with initial renin hypersecretion) and CNS, recovery of sensitivity aortic arch baroreceptors (their activity does not increase in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces increased blood pressure at rest, with physical exertion and stress .; Blood pressure decreases after 15 minutes, maximum after 2 hours and the decrease continues for 6 hours, diastolic blood pressure changes more slowly: a steady decrease is observed after several weeks of regular use; The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening diastole and an improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. It reduces the number and severity of angina attacks and increases exercise tolerance .; Antiarrhythmic effect due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of cAMP, arterial hypertension),a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown of atrioventricular conductivity (mainly in the antegrade and, to a lesser extent, in retrograde directions through the AV node) and along additional paths .; When supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional heart disease and hyperthyroidism, the drug slows heart rate or may even lead to the restoration of sinus rhythm. Prevents migraine development .; When used in moderate therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing β2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of the peripheral arteries, bronchi and uterus) and on carbohydrate metabolism. When used in large doses (more than 100 mg / day) has a blocking effect on both subtypes of β-adrenoreceptors.
Pharmacokinetics
Absorption; After ingestion is rapidly and almost completely (95%) absorbed from the gastrointestinal tract. Cmax of metoprolol in plasma is achieved within 1-2 hours after ingestion. Bioavailability is 50% at the first dose and increases to 70% with repeated use. Eating increases bioavailability by 20-40%.; Distribution; Plasma protein binding averages 10%; It penetrates the BBB and placental barrier. It is excreted in breast milk in small quantities .; Metabolism; Biotransformed in the liver. Metabolites do not possess pharmacological activity .; Withdrawal; T1 / 2 averages 3.5 hours (from 1 to 9 hours). About 5% of the drug is excreted unchanged by the kidneys. Not removed during hemodialysis .; Pharmacokinetics in special clinical situations; Metoprolol increases bioavailability with liver cirrhosis. Impaired liver function slows down the metabolism of the drug.
Indications
- arterial hypertension (including hyperkinetic type) as monotherapy or in combination with other antihypertensive drugs; - IHD: myocardial infarction (secondary prophylaxis - complex therapy), prophylaxis of angina attacks; - disturbances of a heart rhythm (supraventricular tachycardia, ventricular premature beats); - hyperthyroidism (complex therapy); - prevention of migraine attacks.
Contraindications
- cardiogenic shock; - AV block II or III degree; - sinoatrial block; - SSSU; - severe bradycardia; - chronic heart failure in the decompensation phase; - Prinzmetal angina; - arterial hypotension (in the case of use in the secondary prevention of myocardial infarction - systolic blood pressure less than 100 mm Hg, heart rate less than 45 beats / min); - lactation period; - simultaneous use with MAO inhibitors; - simultaneous i / v verapamil; - age up to 18 years; - hypersensitivity to metoprolol or other components of the drug, other beta-blockers .; Precautions should be prescribed for diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis), peripheral vascular disease obliterans (intermittent claudication, Raynaud's syndrome), chronic hepatic and / or renal failure, myasthenia, pheochromocytoma, AV-blockade I degree, thyrotoxicosis, depression (including history), psoriasis, pregnancy, as well as elderly patients.
Use during pregnancy and lactation
In pregnancy, Metocard should be used only when the intended benefit to the mother outweighs the potential risk to the fetus .; Metoprolol penetrates the placental barrier. If necessary, the use of the drug during pregnancy due to the possible development of newborn bradycardia, hypotension, hypoglycemia, it is necessary to ensure careful monitoring of the development of the fetus. After delivery, it is necessary to ensure strict monitoring of the condition of the newborn within 48-72 hours; Metoprolol is excreted in breast milk. The effect of metoprolol on a newborn has not been studied, so if you need to use Metocardia during lactation, breastfeeding should be stopped.
Dosage and administration
The drug is taken orally at the same time with a meal or immediately after a meal. Tablets can be divided in half, but not chewed, and drink down with a liquid .; With hypertension, the initial dose is 50-100 mg / day in 1-2 doses. If necessary, the daily dose is gradually increased to 100-200 mg. In the absence of a satisfactory therapeutic effect, Metocard may be administered in combination with other antihypertensive agents.The maximum daily dose is 200 mg. For angina pectoris, arrhythmias, prevention of migraine attacks, 100-200 mg / day are prescribed in 2 divided doses (morning and evening) .; In the secondary prevention of myocardial infarction prescribed in a dose of 200 mg / day in 2 divided doses (morning and evening) .; When functional disorders of cardiac activity, accompanied by tachycardia, the drug is prescribed at a dose of 100 mg / day in 2 doses (morning and evening) .; Elderly patients, with impaired renal function, as well as with the need for hemodialysis do not require dose adjustment of the drug .; In case of abnormal liver function, the dose should be reduced depending on the clinical condition.
Side effects
On the part of the central nervous system and peripheral nervous system: fatigue, weakness, headache, slowing down the speed of mental and motor reactions; rarely - paresthesias in the limbs (in patients with intermittent claudication and Raynaud's syndrome), depression, anxiety, loss of attention, drowsiness, insomnia, nightmares, confusion or short-term memory impairment, muscle weakness .; On the part of the senses: rarely - reduced vision, reduced secretion of tear fluid, dry and sore eyes, conjunctivitis, tinnitus .; Since the cardiovascular system: sinus bradycardia, palpitations, lower blood pressure, orthostatic hypotension, dizziness, and sometimes - loss of consciousness; rarely, reduced myocardial contractility, temporary worsening of symptoms of chronic heart failure (edema, swelling of feet and / or lower legs, shortness of breath), arrhythmias, angiospasm (increased disturbance of peripheral circulation, cooling of the lower extremities, Raynaud's syndrome), myocardial conduction disorder .; On the part of the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, change in taste, abnormal liver function, increased activity of liver enzymes; extremely rare - hyperbilirubinemia .; Dermatological reactions: urticaria, pruritus, rash, exacerbation of psoriasis, psoriasis-like skin reactions, skin flushing, exanthema, photodermatosis, increased sweating, reversible alopecia .; On the part of the respiratory system: nasal congestion,difficulty of exhalation (bronchospasm when administered in high doses - loss of selectivity and / or in predisposed patients), shortness of breath .; On the part of the endocrine system: hyperglycemia in patients with insulin-dependent diabetes mellitus, hypothyroidism .; On the part of the hemopoietic system: rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia .; Effect on the fetus: possible intrauterine growth retardation, hypoglycemia, bradycardia .; Other: pain in the back or joints; in rare cases - a slight increase in body weight, decreased libido and / or potency .; Side effects depend on the individual sensitivity of the patient. Usually they are minor and disappear after drug withdrawal.
Overdose
Symptoms: severe severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked reduction in blood pressure, arrhythmia, ventricular extassistoliya, bronchospasm, fainting, in acute overdose - cardiogenic shock, loss of consciousness, coma, AV-blockade and cardiac arrest), cardialgia. The first signs of overdose appear within 20 min-2 h after taking the drug .; Treatment: gastric lavage and the appointment of adsorbing agents, symptomatic therapy: with a marked decrease in blood pressure, the patient should be in the Trendelenburg position; in case of excessive decrease in blood pressure, bradycardia and heart failure - in / in the introduction (with an interval of 2-5 minutes) beta-adrenostimulyatorov to achieve the desired effect or in / in the introduction of 0.5-2 mg atropine sulfate. In the absence of a positive effect, administration of dopamine, dobutamine or norepinephrine (norepinephrine). As a follow-up, perhaps, the appointment of 1-10 mg of glucagon, staging transvenous intracardial electrostimulator. When bronchospasm should be introduced into / in stimulators β2-adrenergic receptors .; Metoprolol is poorly excreted by hemodialysis.
Interaction with other drugs
Not recommended simultaneous use with MAO inhibitors due to a significant increase in the hypotensive effect. The interval between taking MAO and metoprolol inhibitors should be at least 14 days. Simultaneous i / v verapamil may cause cardiac arrest.The simultaneous appointment of nifedipine leads to a significant decrease in blood pressure .; Against the background of simultaneous use with Metocardia, agents for general inhalation anesthesia (hydrocarbon derivatives) increase the risk of inhibition of myocardial function and the development of arterial hypotension .; Beta-adrenergic stimulants, theophylline, cocaine, etrogens (sodium retention), indomethacin and other NSAIDs (sodium retention and blocking the synthesis of prostaglandin by the kidneys) weaken the hypotensive effect .; There is a strengthening of the inhibitory effect on the central nervous system, while applying with the standard; the sum of the cardiodepressive effect - with the means for general anesthesia; increased risk of peripheral circulatory disorders - with ergot alkaloids .; When taken together with oral hypoglycemic agents, their effect may be reduced; with insulin - increasing the risk of hypoglycemia, increasing its severity and duration, masking some of the symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure) .; When combined with antihypertensive drugs, diuretics, nitroglycerin or slow calcium channel blockers, a sharp decrease in blood pressure may develop (special caution is necessary when combined with prazosin) .; When using Metocarda with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, alpha methyldopa, clonidine, guanfacine, general anesthesia and cardiac glycosides, an increase in the severity of heart rate reduction and suppression of AV conductivity is observed; If metoprolol and clonidine are taken at the same time, then if you cancel metoprolol, clonidine is canceled after a few days (due to the risk of withdrawal syndrome) .; Inducers of liver microsomal enzymes (rifampicin, barbiturates) lead to increased metabolism of metoprolol, to a decrease in the concentration of metoprolol in blood plasma and a decrease in the effect. Inhibitors of microsomal liver enzymes (cimetidine, oral contraceptives, phenothiazines) - increase the concentration of metoprolol in the blood plasma .; Allergens used for immunotherapy or allergen extracts for skin tests when used together with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine radiopaque substances for intravenous infusion - increase the risk of anaphylactic reactions .; Metoprolol with simultaneous use reduces the clearance of xanthine (except diphillin),especially with initially increased clearance of theophylline under the influence of smoking; reduces lidocaine clearance, increases the concentration of lidocaine in the blood plasma .; With the simultaneous use of the method, it strengthens and prolongs the effect of anti-depolarizing muscle relaxants, prolongs the anticoagulant effect of coumarins .; The combined use of Metocard with ethanol increases the risk of a pronounced decrease in blood pressure .; Three - and tetracyclic antidepressants, antipsychotics (neuroleptics), sedatives and hypnotic drugs when used in conjunction with metoprolol, enhance CNS depression.
special instructions
Monitoring patients receiving Metocard includes regular monitoring of heart rate and blood pressure, blood glucose levels in diabetic patients. If necessary, the dose of insulin or oral hypoglycemic drugs for diabetics should be selected individually .; The patient should be trained in the method of counting the heart rate and instructed on the need for medical consultation with a heart rate of less than 50 bpm. At a dose higher than 200 mg / day, cardio selectivity decreases; In heart failure, treatment with metoprolol begins only after reaching the stage of compensation .; It is possible to increase the severity of hypersensitivity reactions (against the background of an aggravated allergic history) and the lack of effect of administering usual doses of epinephrine (adrenaline) .; While taking Metocardia, symptoms of disturbed peripheral arterial blood circulation may intensify .; The abolition of the drug is carried out gradually, reducing the dose within 10 days .; With a sharp cessation of treatment may cause withdrawal (increased angina attacks, increased blood pressure). Particular attention in case of drug withdrawal should be given to patients with angina .; With angina pectoris, the selected dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load of no more than 110 beats / min; Patients using contact lenses should take into account that during treatment with beta-blockers it is possible to reduce the production of tear fluid .; Metoprolol may mask some clinical manifestations of hyperthyroidism (for example, tachycardia). Abrupt cancellation in patients with thyrotoxicosis is contraindicated, since it can enhance symptoms .; In diabetes metocology, Metocardia may mask tachycardia caused by hypoglycemia.Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the recovery of blood glucose concentration to normal levels .; If necessary, the appointment of patients with bronchial asthma as a concomitant therapy using stimulators β2-adrenergic receptors; with pheochromocytoma - alpha-blockers .; If surgical intervention is necessary, the anesthesiologist should be warned about the therapy being conducted (the choice of means for general anesthesia with minimal negative inotropic effect); the drug is not recommended to be canceled .; Drugs that reduce the supply of catecholamines (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect excessive blood pressure and bradycardia .; In elderly patients, it is recommended to regularly monitor liver function. Correction of the dosing regimen is required only if an increasing bradycardia (less than 50 beats / min) appears in the elderly patient, a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, and severe liver function impairment. , it is sometimes necessary to discontinue treatment .; Patients with severe renal insufficiency are advised to monitor their renal function .; Special monitoring should be carried out for patients with depressive disorders who take metoprolol; in the case of the development of depression caused by taking beta-blockers, it is recommended to stop therapy .; Use in pediatrics; Safety and efficacy of the drug in children and adolescents under the age of 18 years have not been established .; Impact on the ability to drive vehicles and control mechanisms; At the beginning of treatment with metoprolol, patients may experience dizziness, fatigue. In this case, they should refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and psychomotor speed. In the future, this issue should be resolved after evaluating the patient's individual response to the therapy being conducted.