Description
Latin name
Metoprolol-ratiopharm
Release form
Tablets.
Packaging
In a blister pack of 10 tablets. There are 3 blisters in the package.
Pharmacological action
METOPROLOL-RATIOPHARM is a selective beta-blocker, mainly affects beta-1-adrenergic receptors of the heart (“cardioselective beta-blocker”) without internal sympathomimetic activity and with a weakly expressed membrane-stabilizing effect.
It has antianginal, hypotensive and antiarrhythmic effects.
Blocking beta 1 -adrenoreceptors 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-, batmo- and inotropic effect (reduces heart rate (HR), inhibits conduction and excitability, reduces myocardial contractility).
The total peripheral vascular resistance at the beginning of the use of beta-blockers (in the first 24 hours after ingestion) increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of beta-1-adrenoreceptor stimulation), which returns to the initial one after 1-3 days, and with long-term appointment – 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 aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure ) and, as a result, a decrease in peripheral sympathetic influences. Lowers high blood pressure (BP) at rest, with physical exertion and stress.
The antihypertensive 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: 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 (longer diastole and improved 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.
Antiarrhythmic effect is 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 in atrioventricular conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular (AV) node) and along additional routes.
With supraventricular tachycardia, atrial fibrillation, sinus tachycardia, with functional heart diseases and hyperthyroidism, it reduces heart rate or may even lead to a restoration of sinus rhythm. Prevents the development of migraine.
When used in medium therapeutic doses, unlike non-selective beta-blockers, it has a less pronounced effect on organs containing beta 1 -adrenoreceptors (pancreas, skeletal muscle, 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
– Arterial hypertension (as monotherapy or in combination with other antihypertensive drugs), including hyperkinetic type.
– Tachycardia.
– Coronary heart disease: myocardial infarction (secondary prevention) prevention of angina attacks supraventricular tachycardia ventricular extrasystole.
Contraindications
– Hypersensitivity to metoprolol or other components of the drug, other beta-blockers.
– Decompensated heart failure.
– Cardiogenic shock.
– Syndrome weakness syndrome, Prinzmetal angina.
– Atrioventricular block II and III degree.
– Sinoatrial blockade.
– Bradycardia (heart rate before treatment is less than 50 beats per minute).
– Arterial hypotension (if used in secondary myocardial prophylaxis, systolic blood pressure is less than 100 mm Hg).
– Metabolic Acidosis.
– Late stages and severe peripheral circulatory disorders.
– Concomitant use of MAO inhibitors.
– Lactation.
– Age under 18 years of age (efficacy and safety not established).
– In the treatment of the drug is contraindicated in / in the introduction of such blockers of “slow” calcium channels, as verapamil and diltiazem, or other antiarrhythmics (for example, disopyramids). The exception is patients who are in intensive care units.
With extreme caution:
– Atrioventricular block I degree.
– Diabetes mellitus with strong fluctuations in blood sugar (the possibility of a severe hypoglycemic condition).
– Abstinence from eating during religious fasting and heavy physical exertion (severe hypoglycemic conditions may occur).
– Pheochromocytoma.
– Chronic renal and / or liver failure (with the appointment of metoprolol in 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 psoriasis in a personal or family history.
– Patients with impaired peripheral circulation, including Raynaud’s syndrome.
– Patients, being on desensitizing therapy or with a severe allergic reaction in history.
– Bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis).
– Thyrotoxicosis.
– Depression (including history).
– Pregnancy.
– Old age.
In all these cases, the attending physician must carefully weigh the benefit / risk ratio when prescribing the drug.
Use during pregnancy and lactation
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, as To date, there is no sufficient experience of its use in pregnancy, especially in the early stages of pregnancy.
If pregnant women took metoprolol, then due to the possibility of a newborn having bradycardia, arterial hypotension and hyperglycemia, treatment is stopped 48-72 hours before the onset of labor. If this is not possible, then the newborn should be under especially close supervision for 48-72 hours after birth.
The effect of metoprolol on a newborn, while breastfeeding has not been studied, therefore, women taking the drug should stop breastfeeding.
Composition of
1 tablet contains: Irbesartan 300 mg, Hydrochlorothiazide 125 mg
Excipients: Microcrystalline cellulose, croscarmellose sodium, lactose monohydrate, magnesium stearate, silicon dioxide, ferrous oxide, ferrous red oxide, ferrous red oxide, yellow iron oxide, nitrous oxide, yellow carbonate, nitrous oxide
1 tablet contains: metoprolol tartrate 100 mg.
Excipients: microcrystalline cellulose, corn starch, croscarmellose sodium, copovidone, anhydrous colloidal silicon dioxide, magnesium stearate.
Dosage and administration
Tablets are taken orally with a small amount of liquid, without chewing, with food or immediately after eating. Tablets can be divided. The course of treatment is not limited in time and depends on the characteristics of the course of the disease. If it is necessary to cancel treatment, the dose is reduced gradually (at least within 10 days) under the supervision of a doctor.
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. The maximum daily dose of 200 mg.
Angina pectoris, arrhythmias, prevention of migraine attacks – 100-200 mg per day in two divided doses (morning and evening).
Secondary prevention of myocardial infarction – 200 mg per day in two divided doses (morning and evening).
Functional disorders of cardiac activity, accompanied by tachycardia – 100 mg per day in two divided doses (morning and evening).
When the 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.
Side effects of
From the nervous system: fatigue, weakness, headache, slowing down the rate 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 impairment, muscle weakness.
On the part of the sensory organs: rarely – decreased vision, decreased secretion of lacrimal 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 angiospasm (increased impairment of peripheral circulation, cooling of the lower extremities, Raynaud’s syndrome), impaired myocardial conduction, cardialgia.
From the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, impaired liver function, taste change.
From the skin: urticaria, pruritus, rash, exacerbation of psoriasis, psoriasis-like skin reactions, hyperemia of the skin, exanthema, photodermatosis, increased sweating, reversible alopecia.
From the respiratory system: nasal congestion, difficulty breathing out (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 mellitus), hypothyroidism.
Laboratory indicators: rarely – thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes is extremely rare – hyperbilirubinemia.
Influence on the fetus: intrauterine growth retardation, hypoglycemia, and bradycardia are possible.
Other: pain in the back or joints, like all beta-blockers, in rare cases can cause a slight increase in body weight, decreased libido and / or potency.
Drug Interaction
Concomitant use with monoamine oxidase (MAO) inhibitors is not recommended due to a significant increase in antihypertensive activity. The interval between treatment with MAO inhibitors and metoprolol should be at least 14 days.
Simultaneous administration of verapamil may provoke cardiac arrest. Concomitant administration of nifedipine leads to a significant decrease in blood pressure.
Inhalation anesthesia (hydrocarbon derivatives) increases the risk of myocardial function suppression and the development of hypotension.
Beta Adrenostimulants, Theophylline, cocaine, estrogens (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (sodium retention and blocking of prostaglandin synthesis by the kidneys) all attenuate the antihypertensive effect.
There is an increase in the depressant effect on the central nervous system – with ethanol summation of the cardio-depressive effect – with anesthesia drugs, increasing the risk of peripheral circulation disorders – with ergot alkaloids.
When taken together with oral hypoglycemic agents, their effect with insulin may be reduced – increasing the risk of hypoglycemia, increasing its severity and lengthening, masking some symptoms of hypoglycemia (tachycardia, sweating, increasing blood pressure).
When combined with antihypertensives, diuretics, nitroglycerin or blockers of slow calcium channels can develop a sharp decrease in blood pressure (special caution is required when combined with prazosin) increase in the severity of heart rate reduction and inhibition of atrioventricular conduction when using metoprolol with verapamil, diltiaromide, antithromycin, antipyretic general anesthesia and cardiac glycosides.
Inductors of liver microsomal enzymes (rifampicin, barbiturates) lead to increased metoprolol metabolism, decreased plasma metoprolol concentration, and decreased effect.
Inhibitors (cimetidine, oral contraceptives, phenothiazines) – increase blood plasma concentrations.
Allergens used for immunotherapy, or allergen extracts for skin samples when combined with metoprolol increase the risk of systemic allergic reactions or anaphylaxis, iodine-containing X-ray contrast agents for I / O administration increase the risk of anaphylactic reactions.
Reduces the clearance of xanthine (except for dipyllin), especially in patients with initially elevated theophylline clearance under the influence of smoking. Reduces lidocaine clearance, increases plasma concentration of lidocaine. Strengthens and prolongs action of antidepolarizing muscle relaxants prolongs anticoagulant effect of coumarins.
When combined with ethanol, there is an increased risk of a marked decrease in blood pressure.
Overdose
Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, fainting, with acute overdose – cardiogenic shock, loss of consciousness, coma, atrioventricular blockade (up to the development of complete transverse cardiac blockade). The first signs of overdose manifest themselves after 20 minutes – 2 hours after taking the drug.
Treatment: gastric lavage and appointment of adsorbing agents symptomatic therapy: in case of pronounced decrease in blood pressure – the patient should be in the position of Trendelenburg in case of excessive decrease in blood pressure, bradycardia and heart failure – in / in, with an interval of 2-5 minutes, bath adrenostimulators until the desired effect is achieved 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 administration of 1-10 mg of glucagon, the staging of transvenous intracardiac pacemaker. At bronchospasm it is necessary to enter in / in stimulators of beta 1 -adrenoreceptors. In convulsions – slow in / in the introduction of diazepam. Hemodialysis is not effective.
Storage conditions
Store at a temperature not exceeding 30 ° C, in a dry place.
Expiration
5 years.
Deystvuyuschee substances
Metoprolol
dosage form
dosage form
tablets
Merkle GmbH, Germany
