Metoprolol Akrihin Tablets 50mg N30
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Active ingredients
Metoprolol
Release form
Pills
Composition
Metoprolol 50 mg. Excipients: lactose monohydrate, colloidal silicon dioxide, potato starch, povidone, sodium carboxymethyl starch, magnesium stearate.
Pharmacological effect
Metoprolol is a cardioselective blocker of beta-adrenergic receptors that does not have intrinsic sympathomimetic activity and membrane-stabilizing properties. It has antihypertensive, antianginal and antiarrhythmic effects. By blocking beta1-adrenoreceptors of the heart in low doses, it reduces catecholamine-stimulated cAMP formation from ATP, reduces the intracellular current of calcium ions, has a negative chrono, dromo, batmoid and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility). The total peripheral resistance at the beginning of beta-blockers (within the first 24 hours after ingestion) increases (as a result of a reciprocal increase in alpha-adrenoreceptor activity and the removal of beta2-adrenoreceptor stimulation), which returns to baseline after 1-3 days, and application - decreases. The hypotensive effect is due to a reflex decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin-aldosterone system (is more important in patients with initial renin hypersecretion) and the central nervous system, the restoration of the sensitivity of baroreceptors of the aortic arch (their activity does not increase in response to reduction blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces increased blood pressure at rest, with physical exertion and stress. The hypotensive effect develops quickly (systolic blood pressure decreases after 15 minutes, maximum after 2 hours) and lasts 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.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, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing AV conduction (mainly in the antegrade and, to a lesser extent, in retrograde ) through the AV node and along additional paths. When supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional heart disease and hyperthyroidism, 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 beta2-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 beta-adrenoreceptors.
Pharmacokinetics
Absorption when taken full (95%). Cmax in blood plasma is achieved within 1-2 hours after ingestion. T1 / 2 averages 3.5 hours (ranging from 1 to 9 hours). Subjected to intensive presystemic metabolism, bioavailability is 50% at the first dose and increases to 70% when reapplied. Eating increases bioavailability by 20-40%. Bioavailability of metoprolol increases with liver cirrhosis. Communication with plasma proteins - 10%. It penetrates the hematoencephalic and placental barriers. Penetrates into breast milk in small quantities. Metabolized in the liver, 2 metabolites have beta-adrenoceptor blocking activity. CYP2D6 isoenzyme is involved in the metabolism of the drug. About 5% is excreted unchanged by the kidneys. Treatment of patients with reduced kidney function does not require dose adjustment of the drug. Impaired liver function slows down the metabolism of the drug, and in cases of insufficiency of the liver, the dose of the drug should be reduced. Not removed during hemodialysis.
Indications
- arterial hypertension (as monotherapy or in combination with other antihypertensive drugs); - Ischemic heart disease: myocardial infarction (secondary prophylaxis - complex therapy), prophylaxis of attacks of stenocardia; - disturbances of a heart rhythm (supraventricular tachycardia; ventricular premature beats); - hyperthyroidism (complex therapy); - prevention of migraine attacks.
Contraindications
- cardiogenic shock; - atrioventricular block (AV) II-III degree; - sinoatrial (SA) blockade; - sick sinus syndrome; - severe bradycardia; - chronic heart failure in the stage of decompensation; - Prinzmetal angina; - arterial hypotension (in the case of use in the secondary prevention of myocardial infarction - systolic blood pressure less than 100 mm Hg. Art. Heart rate less than 45 beats / min); - lactation period; - simultaneous administration of MAO inhibitors or simultaneous intravenous administration of verapamil; - age up to 18 years (efficacy and safety have not been established); - lactose intolerance, lactase deficiency or glucose-galactose malabsorption. - hypersensitivity to metoprolol or other components of the drug, other beta-blockers; With care: diabetes, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis), obliterating diseases of peripheral vessels ("intermittent" claudication, Raynaud's syndrome), chronic hepatic and / or kidney failure, myasthenia, pheochromocytoma (with the simultaneous use of alpha-blockers), AV block I degree, thyrotoxicosis, depression (including history), psoriasis, pregnancy, old age.
Use during pregnancy and lactation
During pregnancy, prescribed taking into account the ratio of benefits to the mother and the risk to the fetus (due to the development of fetal bradycardia, hypotension, hypoglycemia). At the same time conduct careful monitoring, especially for the development of the fetus. It is necessary to monitor the newborn within 48-72 h after delivery. The effect of metoprolol on a newborn while breastfeeding has not been studied, so women who take Metoprolol-Akrikhin should stop breastfeeding.
Dosage and administration
Tablets are taken orally during or immediately after a meal, not chewed, washed down with a small amount of liquid. Arterial hypertension. The initial daily dose is 50-100 mg in 1-2 doses (morning and evening). With insufficient therapeutic effect, the daily dose can be gradually increased to 100-200 mg and / or the additional prescription of other antihypertensive agents. The maximum daily dose of 200 mg. Angina, arrhythmias, prevention of migraine attacks 100-200 mg per day in two doses (in the morning and evening). Secondary prevention of myocardial infarction 200 mg per day in two doses (morning and evening). Hyperthyroidism On 50 mg 2 times a day (in the morning and in the evening). In elderly patients, with impaired renal function, and if necessary for hemodialysis, the dose is not changed. 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: fatigue, weakness, headache, slowing down the speed of mental and motor reactions; rarely, paresthesia in the limbs (in patients with intermittent claudication and Raynaud's syndrome), depression, anxiety, loss of attention, drowsiness, insomnia, nightmarish dreams, confusion or short-term memory impairment, muscle weakness. From the senses: rarely - reduced vision, reduced secretion of tear fluid, dry and sore eyes, conjunctivitis, tinnitus. Since the cardiovascular system: sinus bradycardia, palpitations, lowering blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness); rarely, a decrease in myocardial contractility, temporary worsening of symptoms of chronic heart failure (edema, swelling of the feet and / or lower legs, shortness of breath), arrhythmias, angiospasm (increased disturbance of the peripheral circulation, cooling of the lower extremities, Raynaud's syndrome), myocardial conduction. On the part of the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, change in taste. On the part of the skin: 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 in exhalation (bronchospasm when administered in high doses - loss of selectivity and / or in susceptible patients), shortness of breath.On the part of the endocrine system: hypoglycemia (in patients receiving insulin); rarely, hyperglycemia (in patients with insulin-dependent diabetes mellitus). Laboratory indicators: rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes, extremely rare - hyperbilirubinemia. Effect on the fetus: possible intrauterine growth retardation, hypoglycemia, bradycardia. Others: pain in the back or joints, as well as all beta-blockers in individual cases, can cause a slight increase in body weight, decrease in libido and / or potency.
Overdose
Symptoms: expressed severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked reduction in blood pressure, arrhythmia, ventricular premature beats, bronchospasm, fainting, in acute overdose - cardiogenic shock, loss of consciousness, coma, atrioventricular block (up to the full development of cross blockade and cardiac arrest), cardialgia. The first signs of overdose appear within 20 min-2 hours after taking the drug. Treatment: gastric lavage and taking adsorbing agents; symptomatic therapy: in case of marked reduction in blood pressure - the patient should be in the Trendelenburg position; in case of excessive reduction of blood pressure, bradycardia and heart failure - in / in, with an interval of 2-5 minutes, beta-adrenomimetics - to achieve the desired effect or in / in 0.5-2 mg of atropine sulfate. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (norepinephrine). As a follow-up, perhaps, the introduction of 1-10 mg of glucagon, the installation of transvenous intracardial electrostimulator. When bronchospasm should be entered into / in beta2-adrenomimetics. 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. A break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days. Simultaneous i / v verapamil may cause cardiac arrest. The simultaneous appointment of nifedipine leads to a significant reduction in blood pressure.Means for inhalation anesthesia (derivatives of hydrocarbons) increase the risk of inhibition of myocardial function and the development of arterial hypotension. Beta adrenomimetics, theophylline, cocaine, estrogens (sodium retention), indomethacin and other nonsteroidal anti-inflammatory drugs (sodium retention and blocking the synthesis of prostaglandin by the kidneys) weaken the hypotensive effect. There is an increase in the inhibitory effect on the central nervous system - with ethanol; the sum of the cardiodepressive effect - with the means for anesthesia; increased risk of peripheral circulatory disorders - with ergot alkaloids. When taken together with hypoglycemic agents for oral administration, it is possible to reduce their effect; with insulin - increasing the risk of hypoglycemia, increasing its severity and lengthening, masking some of the symptoms of hypoglycemia (tachycardia, sweating, high blood pressure). When combined with antihypertensive drugs, diuretics, nitroglycerin, or blockers of “slow” calcium channels, a sharp decrease in blood pressure may develop (special caution is necessary when combined with prazosin); increase in the severity of the contraction of the heart rate and inhibition of atrioventricular conduction - when metoprolol is used with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, methyldopa, clonidine, guanfacine, agents for general anesthesia and cardiac glycosides. If metoprolol and clonidine are taken at the same time, then when you cancel metoprolol, clonidine is canceled after a few days (due to the risk of the “cancellation” syndrome). Inducers of liver microsomal enzymes (rifampicin, barbiturates) lead to an increase in the metabolism of metoprolol, to a decrease in its concentration in the blood plasma and a decrease in the effect. Inhibitors (cimetidine, oral contraceptives, phenothiazines) - increase plasma concentration of metoprolol. Allergens used for immunotherapy or allergen extracts for skin tests when combined with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine radiopaque substances for intravenous administration increase the risk of anaphylactic reactions.Reduces clearance of xanthine (except diphillin), especially with initially increased clearance of theophylline under the influence of smoking. Reduces clearance of lidocaine, increases the concentration of lidocaine in the blood plasma. Strengthens and prolongs the action of anti-depolarizing muscle relaxants; lengthens the anti-ticoagulant effect of coumarins. When combined with ethanol increases the risk of a pronounced decrease in blood pressure.
special instructions
Monitoring patients taking beta-blockers, includes regular monitoring of heart rate and blood pressure, blood glucose in diabetics. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic drugs administered orally should be selected individually. The patient should be trained in the method of counting heart rate and instructed on the need for medical consultation with a heart rate less than 50 beats / min. When receiving a dose of more than 200 mg per day decreases cardioselectivity. 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 from the administration of usual doses of epinephrine (adrenaline). May exacerbate symptoms of peripheral arterial circulation. The abolition of the drug is carried out gradually, reducing the dose within 10 days. With an abrupt cessation of treatment, a “withdrawal” syndrome may occur (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). Sharp cancellation in patients with thyrotoxicosis is contraindicated, as it can strengthen the symptoms. In case of diabetes mellitus, it can mask tachycardia caused by hypoglycemia.Unlike non-selective beta-adrenergic blockers, insulin-induced hypoglycemia practically does not increase and does not delay the restoration of glucose concentration in the blood to normal levels. If necessary, appoint patients with bronchial asthma, beta2-adrenomimetics are used as concomitant therapy; with pheochromocytoma - alpha-blockers. If surgery is necessary, the anesthesiologist should be warned about the therapy being conducted (the choice of anesthetic for general anesthesia with minimal negative inotropic effects), and it is not recommended to stop the drug. Drugs that reduce the supply 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 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 mmHg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver function disorders It is sometimes necessary to discontinue treatment. Patients with severe renal insufficiency are advised to monitor renal function. Special monitoring should be carried out for patients with depressive disorders who take metoprolol; in case of development of depression caused by taking beta-blockers, it is recommended to stop therapy. Due to the lack of sufficient clinical data, the drug is not recommended for use in children. 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, the determination of the safety of the dose is carried out individually.