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Metoprolol-Ratiopharm tablets 100 mg No. 30

Compound

1 tablet contains: metoprolol tartrate 100 mg.
Excipients: microcrystalline cellulose, corn starch, croscarmellose sodium, copovidone, colloidal anhydrous silica, magnesium stearate.

Pharmacokinetics

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

It has antianginal, hypotensive and antiarrhythmic effects.

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

The total peripheral vascular resistance at the beginning of the use of beta-adrenergic blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of beta 1-adrenergic receptors), which after 1-3 days returns to the original level, and when long-term use - decreases.

The hypotensive 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 baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease in blood pressure) and ultimately, 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 after 15 minutes, maximum after 2 hours) and lasts for 6 hours, diastolic blood pressure changes more slowly: a stable 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 (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in the sensitivity of the myocardium 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 of atrioventricular conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through atrioventricular (AV) node) and along additional pathways.

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

When used in average therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on 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 for use

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

Contraindications

Hypersensitivity to metoprolol or other components of the drug, other beta-blockers.
Heart failure in the stage of decompensation.
Cardiogenic shock.
Sick sinus syndrome, Prinzmetal's angina.
Atrioventricular block II and III degrees.
Sinoatrial block.
Bradycardia (heart rate before treatment is less than 50 beats per minute).
Arterial hypotension (if used for secondary myocardial prevention, systolic blood pressure less than 100 mm Hg).
Metabolic acidosis.
Late stages and severe peripheral circulatory disorders.
Concomitant use of MAO inhibitors.
Lactation period.
Age up to 18 years (efficacy and safety have not been established).
During treatment with the drug, intravenous administration of slow calcium channel blockers such as verapamil and diltiazem, or other antiarrhythmics (for example, disopyramide) is contraindicated. The exception is for patients in intensive care units.

With extreme caution:

First degree atrioventricular block.
Diabetes mellitus with severe fluctuations in blood sugar levels (possibility of severe hypoglycemic conditions).
Abstinence from eating during religious fasting and heavy physical activity (severe hypoglycemic conditions may occur).
Pheochromocytoma.
Chronic renal and/or liver failure (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 seconds, systolic blood pressure less than 100 mm Hg).
Manifest psoriasis or personal or family history of psoriasis.
Patients with peripheral circulatory disorders, including Raynaud's syndrome.
Patients on desensitizing therapy or with a history of severe allergic reactions.
Bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis).
Thyrotoxicosis.
Depression (including history).
Pregnancy.
Elderly age.

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

Directions for use and doses

The tablets are taken orally with a small amount of liquid, without chewing, with food 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 disease. If it is necessary to discontinue treatment, the dose is reduced gradually (for at least 10 days) under the supervision of a physician.

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

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

Storage conditions

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

Best before date

5 years.

special instructions

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

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

The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

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

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

The drug is discontinued gradually, reducing the dose over 10 days. If treatment is abruptly stopped, withdrawal syndrome may occur (increased angina attacks, increased blood pressure). When discontinuing the drug, special attention should be paid to patients with angina pectoris.

For exertional angina, the selected dose of the drug should ensure the heart rate at rest within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min.

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

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

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

If necessary, beta 2-adrenergic stimulants are used as concomitant therapy for patients with bronchial asthma, and alpha-blockers 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); discontinuation of the drug is not recommended.

Drugs that reduce catecholamine reserves (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure and bradycardia.

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

During treatment with metoprolol, you should wear appropriate clothing, because the drug may cause skin allergies to sunlight.

In elderly patients, it is recommended to monitor liver function. 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 dysfunction , 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 hazardous activities that require increased concentration and speed of psychomotor reactions, and avoid taking ethanol.

Conditions for dispensing from pharmacies

Available with prescription

Side effects

From the nervous system: increased fatigue, weakness, headache, slower 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 loss, muscle weakness.

From the senses: rarely - decreased vision, decreased secretion of tear fluid, dry and sore 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 worsening of symptoms of chronic heart failure (edema, swelling of the feet and/or lower legs, shortness of breath ), arrhythmias, manifestation of vasospasm (increased peripheral circulatory disorders, coldness 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, change in taste.

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

From the respiratory system: nasal congestion, difficulty exhaling (bronchospasm when prescribed 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), hypothyroidism.

Laboratory indicators: 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: back or joint pain, like all beta-blockers, in isolated cases can cause a slight increase in body weight, decreased libido and/or potency.

Use during pregnancy and breastfeeding

During pregnancy (especially in the first 3 months), the drug should be used only according to strict indications, taking into account careful weighing of the benefit/risk ratio, because To date, there is no sufficient experience with its use during pregnancy, especially in the early stages of pregnancy.

If pregnant women took metoprolol, then due to the possibility of bradycardia, arterial hypotension and hyperglycemia in the newborn, treatment is stopped 48-72 hours before birth. If this is not possible, the newborn should be monitored especially closely for 48-72 hours after birth.

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

Interaction

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

Simultaneous intravenous administration of verapamil can provoke cardiac arrest. The simultaneous administration of nifedipine leads to a significant decrease in blood pressure.

Inhalation anesthetics (hydrocarbon derivatives) increase the risk of suppression of myocardial function and the development of arterial hypotension.

Beta-agonists, theophylline, cocaine, estrogens (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (sodium retention and blocking renal prostaglandin synthesis) weaken the hypotensive effect.

There is an increased inhibitory effect on the central nervous system with ethanol, a summation of the cardiodepressive effect with anesthesia, and an increased risk of peripheral circulatory disorders with ergot alkaloids.

When taken together with oral hypoglycemic agents, their effect may be reduced; when taken with insulin, the risk of developing hypoglycemia may increase, its severity may increase and prolong, masking some 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 required when combined with prazosin), an increase in the severity of the decrease in heart rate and inhibition of atrioventricular conduction when using metoprolol with verapamil, diltiazem, antiarrhythmic drugs (amiodarone) , reserpine, clonidine, guanfacine, general anesthesia and cardiac glycosides.

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

Inhibitors (cimetidine, oral contraceptives, phenothiazines) - increase plasma concentrations.

Allergens used for immunotherapy or allergen extracts for skin testing when used together with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine-containing radiocontrast agents for intravenous administration increase the risk of anaphylactic reactions.

Reduces the clearance of xanthine (except for 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 the blood plasma. Strengthens and prolongs the effect of antidepolarizing muscle relaxants, prolongs the anticoagulant effect of coumarins.

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

Overdose

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, fainting, in case of 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 20 minutes - 2 hours after taking the drug. Treatment: gastric lavage and administration of adsorbents, symptomatic therapy: if there is a pronounced decrease in blood pressure, the patient should be in the Trendelenburg position; in case of an excessive decrease in blood pressure, bradycardia and heart failure, in /in, at intervals of 2-5 minutes, bata-adrenergic stimulants - until the desired effect is achieved, or intravenously 0.5-2 mg of atropine sulfate. If there is no positive effect, dopamine, dobutamine or norepinephrine (norepinephrine). As subsequent measures, it is possible to prescribe 1-10 mg of glucagon and install a transvenous intracardial pacemaker. For bronchospasm, beta 1-adrenergic receptor stimulants should be administered intravenously. For convulsions - slow intravenous administration of diazepam. Hemodialysis is not effective.

Application

Trimetazidine-ratiopharm is taken orally, 1 tablet (20 mg) 3 times a day with meals, with a glass of water. The duration of treatment is determined depending on the severity and course of the disease.

Patients with kidney failure

In patients with moderate renal impairment (creatinine clearance - 30-60 ml/min), the recommended dose of trimetazidine is 1 tablet (20 mg) 2 times a day, morning and evening with meals.

Elderly patients

Elderly patients are more sensitive to the effects of trimetazidine due to age-related decline in renal function. For patients with moderate renal impairment (creatinine clearance - 30-60 ml/min), the recommended dose of trimetazidine is 1 tablet (20 mg) 2 times a day, morning and evening with meals.

For elderly patients, the dose must be titrated carefully.

Side effects

Adverse reactions that have been identified as side effects that may be associated with the use of trimetazidine are listed below.

From the nervous system: headache, dizziness, symptoms of parkinsonism (tremor, akinesia, muscle hypertonicity, gait instability, restless legs syndrome and other movement disorders related to the above, which usually disappear after discontinuation of treatment), sleep disturbance (insomnia, drowsiness ).

From the cardiovascular system: palpitation, extrasystole, tachycardia, arterial hypotension, orthostatic hypotension, which may be associated with malaise, dizziness or falling, in particular in patients using antihypertensive drugs, facial flushing.

From the gastrointestinal tract: pain in the epigastric region, diarrhea, dyspepsia, nausea and vomiting, constipation.

From the skin and subcutaneous tissue: rash, itching, urticaria, acute generalized exanthematous pustular rash, angioedema.

General disorders: asthenia.

From the blood and lymph system: agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

Hepatobiliary disorders: hepatitis.

Pharmacological properties

Pharmacodynamics.
Mechanism of action. By preserving energy metabolism in cells exposed to hypoxia or ischemia, trimetazidine prevents a decrease in intracellular ATP levels, thereby ensuring the proper functioning of ion pumps and transmembrane sodium-potassium flux while maintaining cellular homeostasis.

Trimetazidine inhibits fatty acid β-oxidation by blocking long-chain 3 ketoacyl-CoA thiolase (3-CAT), which increases glucose oxidation. In cells under ischemic conditions, the process of obtaining energy through the oxidation of glucose requires less oxygen compared to the process of obtaining energy through the β-oxidation of fatty acids. Strengthening the process of glucose oxidation optimizes energy processes in cells and, accordingly, maintains sufficient energy metabolism under ischemic conditions.

The drug also helps maintain the level of ATP and AMP in brain cells, supports the functional activity of hepatocyte mitochondria, and also prevents the adverse effects of free radicals by reducing the intensity of lipid peroxidation and increasing the potential of the antioxidant defense system.

Pharmacodynamic effects. In patients with coronary artery disease, trimetazidine acts as a metabolic agent, maintaining intracellular levels of high-energy phosphates in the myocardium. The effects are achieved without accompanying hemodynamic changes.

In otorhinolaryngological practice, Trimetazidine-ratiopharm improves the tolerability of vestibular tests, increases hearing acuity, reduces the intensity of tinnitus, effectively reduces the degree, duration and frequency of dizziness attacks in Meniere's disease and dizziness of vascular origin. In case of perceptual deafness, it provides an increase in the range of perception in decibels and improves hearing.

In patients with chorioretinal vascular disorders, the drug helps restore the functional activity of the retina, which is manifested by normalization of electroretinogram parameters, improves visual acuity and expands the visual field, which is associated with favorable anatomical changes. This leads to a weakening of the functional symptoms of retinal pathology, especially in age-related macular degeneration.

Pharmacokinetics. Trimetazidine-ratiopharm is completely and quickly absorbed from the digestive tract. Cmax in blood plasma is achieved in less than 2 hours and is 55 ng/ml after a single dose of 20 mg. Biostool content - more than 85%. A stable concentration is established approximately 24–36 hours after repeated doses and remains so throughout the entire treatment period. Approximately 16% is protein bound in vitro. Well distributed in tissues. The volume of distribution is 4.8 l/kg.

It is excreted primarily by the kidneys, 51% unchanged. T½ is almost 6 hours in healthy people and 12 hours in people over 65 years of age.

Food intake does not affect the pharmacokinetics of the drug.