Composition, form of production and packaging
CorvitolВ® 50
Tablets of white color, round, flat-cylindrical, with a facet and one-sided risk.
1 tab.
metoprolol tartrate 50 mg
Excipients: lactose monohydrate - 110.5 mg, povidone K30 - 3.5 mg, croscarmellose sodium - 8 mg, magnesium stearate - 2 mg, talc - 2.5 mg, silicon dioxide colloid - 1 mg.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
CorvitolВ® 100
Tablets of white color, round, flat-cylindrical, with a facet and one-sided risk.
1 tab.
metoprolol tartrate 100 mg
Excipients: lactose monohydrate - 221 mg, magnesium stearate - 4 mg, povidone K30 - 7 mg, croscarmellose sodium - 16 mg, silicon dioxide colloid - 2 mg, talc - 5 mg.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2008.
PHARMACHOLOGIC EFFECT
Cardioselective beta- 1- adrenoblocker without internal sympathomimetic activity and membrane-stabilizing properties. It has antihypertensive, anti-anginal and antiarrhythmic effects.
Blocking in low doses? 1- adrenoreceptors of the heart, reduces catecholamine-stimulated cAMP formation from ATP, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect (reduces heart rate, inhibits conduction and excitability, reduces myocardial contractility).
OPSS at the beginning of beta-blockers (in the first 24 hours after ingestion) increases (as a result of the reciprocal increase in the activity of ОІ-adrenoreceptors and elimination of stimulation of ОІ2-adrenoreceptors), which returns to the initial one in 1-3 days, decreases.
Antihypertensive effect is due to a decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin system (important in patients with initial hypersecretion of renin) and CNS, restoration of the sensitivity of the aortic baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and, in as a result, a decrease in peripheral sympathetic influences. Reduces elevated blood pressure at rest, with physical stress and stress.
The hypotensive effect develops rapidly (systolic blood pressure decreases after 15 minutes, maximum after 2 hours) and lasts for 6 hours, diastolic blood pressure changes more slowly (stable decrease is observed after several weeks of regular intake).
The anti-angiogenic effect is determined by the decrease in myocardial oxygen demand as a result of a decrease in heart rate (diastolic elongation and improvement of myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to sympathetic innervation. Reduces the number and severity of angina attacks and increases the tolerance of exercise.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing of AV conduction (mainly in the antegrade and, to a lesser extent, retrograde directions through AV-node and by additional ways .For supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional diseases Heart anias and hyperthyroidism slows heart rate or even can lead to recovery of sinus rhythm.
Prevents the development of migraine.
When used in average therapeutic doses, in contrast to non-selective beta-blockers, has a less pronounced effect on organs containing? 2- adrenoreceptors (pancreas, skeletal muscles, smooth musculature of peripheral arteries, bronchi and uterus) and carbohydrate metabolism. When used in large doses (more than 100 mg / day) has a blocking effect on both subtypes of? -adrenoceptors.
PHARMACOKINETICS
Suction
After taking the drug metoprolol quickly and almost completely (about 95%) is absorbed from the digestive tract. Cmax in blood plasma is reached after about 1-2 hours. Due to intensive metabolism during "first passage" through the liver, bioavailability is about 50% at the first intake and increases to 70% with repeated application. Food intake increases bioavailability by 20-40%.
Distribution
The binding with plasma proteins is 10%, V d is 5.5 l / kg.
It penetrates the GEB and the placental barrier. Isolated with breast milk in small amounts.
Metabolism
It is almost completely metabolized in the liver. Two of the three major metabolites have a beta-adrenergic blocking action. In the metabolism of metoprolol, CYP2D6 participates.
Excretion
T 1/2 is an average of 3.5 hours (from 1 hour to 9 hours). It is excreted in the urine, 5% - unchanged.
Pharmacokinetics in special clinical cases
Disturbance of liver function slows the metabolism of metoprolol, with cirrhosis of the liver, the bioavailability of metoprolol increases.
Metoprolol is not excreted in hemodialysis.
INDICATIONS
- arterial hypertension (as a monotherapy or in combination with other antihypertensive drugs), incl. hyperkinetic type;
- tachycardia;
- IHD: myocardial infarction (secondary prevention), prevention of angina attacks;
- heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystole);
- prevention of migraine attacks.
DOSING MODE
When hypertension is prescribed for 100 mg 1 time / day or 50 mg 2 times / day. If necessary, the dose can be increased to 100 mg 2 times / day. The maximum daily dose is 200 mg.
With angina pectoris also prescribed for 100 mg 1 time / day or 50 mg 2 times / day. If necessary, the dose can be increased to 100 mg 2 times / day.
In functional disorders of cardiac activity, accompanied by tachycardia, the initial dose is 50-100 mg / day in 1-2 divided doses. If necessary, the dose may be increased to 200 mg / day in 2 divided doses.
For the prevention of migraine attacks, appoint 100 mg 1 time / day or 50 mg 2 times / day. When the therapeutic effect is achieved, the dose is reduced (under the supervision of the doctor).
In elderly patients with violations of kidney function , as well as the need for hemodialysis do not change the dose.
For violations of liver function, the dose of the drug should be reduced depending on the clinical condition.
The drug is taken after a meal. Tablets can be divided in half, swallowed without chewing, squeezed with a small amount of liquid.
When taking 1 time / day Corvitol should be taken in the morning, with a double intake - in the morning and in the evening. Course of treatment Corvitol is not limited in time and depends on the features of the course of the disease.
SIDE EFFECT
From the side of the central nervous system: fatigue, weakness, headache, dizziness, slowing of the speed of mental and motor reactions, 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, asthenic syndrome, muscle weakness.
From the senses: rarely - reduced vision, reduced secretion of tear fluid, dry and painful eyes, conjunctivitis, tinnitus, rhinitis.
On the part of the cardiovascular system: sinus bradycardia, palpitations, marked decrease in blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness); rarely - decreased myocardial contractility, temporary worsening of symptoms of chronic heart failure (swelling, edema of the feet and / or lower legs, dyspnea), arrhythmias, manifestation of angiospasm (increased peripheral circulatory disturbance, lower extremities cooling, Raynaud's syndrome), myocardial conduction disturbance, cardialgia .
On the part of the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, taste change, increased activity of hepatic enzymes;extremely rarely - hyperbilirubinemia.
Dermatological reactions: exacerbation of psoriasis, psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.
On the part of the respiratory system: nasal congestion, difficulty exhaling (bronchospasm in high doses - loss of selectivity and / or in predisposed patients), dyspnea.
On the part of the endocrine system: hypoglycemia (in patients receiving insulin); rarely - hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypothyroid status.
From the hemopoietic system: rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.
Allergic reactions: urticaria, skin itching, rash.
Other: pain in the back or joints; in isolated cases - a slight increase in body weight, a decrease in libido and / or potency.
CONTRAINDICATIONS
- cardiogenic shock;
- AV blockade II and III degree;
- Sinoatrial blockade;
- SSSU;
- pronounced bradycardia (heart rate <50 bpm);
severe violations of peripheral circulation;
- heart failure in the stage of decompensation;
- Prinzmetal angina;
- arterial hypotension (in case of use in secondary prevention of myocardial infarction - systolic blood pressure <100 mm Hg);
- Acute myocardial infarction (heart rate <45 bpm, PQ interval more than 0.25 s, systolic blood pressure <100 mmHg);
- simultaneous administration of MAO inhibitors or simultaneous iv injection of verapamil;
- lactation period;
- children and adolescents under 18 years of age (efficacy and safety not established);
- Hypersensitivity to metoprolol, other components of the drug and other beta-blockers.
Caution should be given to the drug when diabetes mellitus, metabolic acidosis, bronchial asthma, COPD (emphysema, chronic obstructive bronchitis), obliterating peripheral vascular diseases (intermittent claudication, Reynaud's syndrome), chronic hepatic and / or renal insufficiency, myasthenia gravis, pheochromocytoma, AV blockade of I degree, thyrotoxicosis , depression (including in the anamnesis), psoriasis, in pregnancy, as well as elderly patients.
PREGNANCY AND LACTATION
In pregnancy, Corvitol is prescribed according to strict indications, taking into account the benefit / risk ratio (due to fetal bradycardia, arterial hypotension, hypoglycemia). At the same time, careful monitoring is carried out, especially for fetal development. Strict monitoring of newborns is necessary within 48-72 hours after delivery.
Influence of metoprolol on the newborn has not been studied, therefore women who take Corvitol during lactation should stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug for chronic kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug in chronic liver failure.
SPECIAL INSTRUCTIONS
During the period of taking Corvitol, you should regularly monitor heart rate and blood pressure, blood glucose in patients with diabetes mellitus (1 every 4-5 months). If necessary, for patients with diabetes mellitus, a dose of insulin or hypoglycemic drugs prescribed inside, should be selected individually.
It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at heart rate <50 bpm.
When taking a dose above 200 mg / day reduces cardioselectivity.
With heart failure, treatment with Corvitol begins only after the compensation stage has been reached.
It is possible to increase the severity of reactions of hypersensitivity (against a background of a burdened allergic anamnesis) and the absence of the effect of the administration of usual doses of epinephrine (epinephrine).
Against the background of taking Corvitol, symptoms of impaired peripheral arterial circulation may worsen.
Cancellation of the drug is carried out gradually, reducing the dose for 10 days. With a sharp cessation of treatment, withdrawal can occur (increased angina attacks, increased blood pressure). Particular attention should be paid to patients with angina when removing the drug.
With angina pectoris, the selected dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load - no more than 110 beats / min.
Patients who use contact lenses should take into account that against the background of treatment with beta-adrenoblockers, tear production can be reduced.
Metoprolol may mask certain clinical manifestations of thyrotoxicosis (eg, tachycardia). Sharp abolition of Corvitol in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.
With diabetes, taking Corvitol can mask tachycardia caused by hypoglycemia. Unlike nonselective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.
If necessary, the appointment of patients with bronchial asthma as a concomitant therapy using beta 2 -adrenostimulants; with pheochromocytoma - alpha-adrenoblockers.
If it is necessary to perform a surgical procedure, it is necessary to warn the anesthesiologist about the therapy (choice of a means for general anesthesia with minimal negative inotropic action), drug discontinuation is not recommended.
Drugs that reduce the reserves of catecholamines (for example, reserpine), can enhance the action of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision for the detection of excessive lowering of blood pressure and bradycardia.
In elderly patients, it is recommended to regularly monitor liver function.
Correction of the dosing regimen (sometimes abolition of the drug) is required only in the case of an elderly patient with an increasing bradycardia (less than 50 beats / min), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe liver function disorders.
Patients with severe renal failure are advised to monitor kidney function.
It is necessary to carry out special monitoring of the condition of patients with depression taking Corvitol; In the case of development of depression caused by the use of beta-blockers, it is recommended to stop therapy.
During treatment, Corvitol should wear appropriate clothing, since the drug may cause photosensitivity.
With concurrent administration of Corvitol and clonidine, clonidine may be withdrawn only a few days after discontinuation of treatment with Corvitol.
Use in Pediatrics
Because of the lack of sufficient clinical data, Corvitol is not recommended for use in children.
Impact on the ability to drive vehicles and manage mechanisms
During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: severe severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, syncope; when acute overdose - cardiogenic shock, loss of consciousness, coma, AV-blockade (until the development of complete transverse blockade and cardiac arrest), cardialgia.
The first signs of an overdose appear after 20 minutes - 2 hours after taking the drug.
Treatment : gastric lavage, the appointment of absorbents, the conduct of symptomatic therapy - with a marked decrease in blood pressure the patient should be in the Trendelenburg position, in the case excessive reduction in blood pressure, bradycardia and heart failure - intravenous administration (with an interval of 2-5 minutes) of beta-adrenostimulants to achieve the desired effect or intravenous injection of 0.5-2 mg of atropine sulfate. In the absence of a positive effect - the introduction of dopamine, dobutamine or norepinephrine (norepinephrine). In the future, it is possible to prescribe 1-10 mg glucagon, the setting of a transvenous intracardiac electrostimulator. When bronhospazme should be introduced iv / beta-adrenostimulyatory. With the development of seizures, a slow IV dose of diazepam is recommended. Hemodialysis is not effective.
DRUG INTERACTION
It is not recommended simultaneous use of Corvitol with MAO inhibitors due to a significant increase in antihypertensive effect. The interval between taking MAO inhibitors and metoprolol should be at least 14 days.
In / in the introduction of verapamil against the background of taking Corvitol can provoke a cardiac arrest.
Simultaneous use of Corvitol with nifedipine leads to a significant decrease in blood pressure.
Means for inhalation anesthesia (derivatives of hydrocarbons) with simultaneous application with Corvitol increase the risk of oppression of myocardial function and development of arterial hypotension.
Beta-adrenostimulators, theophylline, cocaine, estrogen (sodium retention), indomethacin and other NSAIDs (sodium retention and blockage of prostaglandin synthesis by the kidneys) weaken the hypotensive effect of Corvitol.
With the simultaneous administration of Corvitol with ethanol, there is an increase in the inhibitory effect on the central nervous system and the risk of a marked decrease in blood pressure increases.
With simultaneous reception of Corvitol with funds for anesthesia, there is a summation of the cardiodepressive effect.
With the simultaneous administration of Corvitol with ergot alkaloids, an increased risk of peripheral circulatory disorders is observed.
With the joint administration of Corvitol with oral hypoglycemic agents, their effect may be reduced; with insulin - increased risk of hypoglycemia, increased its severity and lengthening, masking of some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).
When the combination of Corvitol 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.
Decrease in heart rate and AV suppression can be observed with Corvitol with verapamil, diltiazem, antiarrhythmics (amiodarone), reserpine, alpha-methyldopa, clonidine, guanfacin, general anesthetic agents and cardiac glycosides.
If metoprolol and clonidine are taken concomitantly, when metoprolol is withdrawn, clonidine is withdrawn after a few days (due to the risk of withdrawal syndrome).
Inductors of microsomal liver enzymes (rifampicin, barbiturates), while the use Korvitolom lead to increased metabolism of metoprolol, to decrease the concentration of metoprolol in the blood plasma and reduced its effect.
Inhibitors of microsomal liver enzymes (cimetidine, oral contraceptives, phenothiazines) increase the concentration of metoprolol in the blood plasma.
The allergens used for immunotherapy, or allergen extracts for skin tests when used together with Korvitolom, increase the risk of systemic allergic reactions or anaphylaxis.
Iodinated X-ray contrast agents for in / in or combined with Korvitolom increase the risk of anaphylactic reactions.
Metoprolol reduces the clearance of xanthine (except dyphylline), especially with the initially increased clearance of theophylline under the influence of smoking.
Metoprolol reduces lidocaine clearance, increasing the concentration of lidocaine in the blood plasma.
Korvitol while applying enhances and prolongs the effect antidepolyarizuyuschih relaxants.
Korvitol lengthens while applying the anticoagulant effect of coumarins.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 3 years.
