Description
Latin name
Metoprolol
Release form
Tablets.
Packaging
In a blister pack of 10 tablets. There are 3 blisters in the package.
Pharmacological action of
Metoprolol is a cardioselective -adrenoreceptor blocker that does not have internal sympathomimetic activity and membrane-stabilizing properties. It has hypotensive, antianginal and antiarrhythmic effects.
Blocking low-level -adrenoreceptors of the heart, reduces catecholamine-stimulated cAMP production from ATP, reduces the intracellular Ca2 + current, has a negative chrono-, dromo-, batmo- and inotropic effect (reduces heart rate, inhibits conduction and excitability, reduces myocardial contractility )
The total peripheral resistance at the beginning of the use of -adrenergic blockers (in the first 24 hours after oral administration) – increases (as a result of a reciprocal increase in the activity of -adrenoreceptors and the elimination of stimulation of -adrenoreceptors), which returns to the initial one after 1-3 days, and when long-term appointment – is reduced.
Acute antihypertensive effect due to a decrease in cardiac output, sinus tachycardia with functional heart diseases and hyperthyroidism, reduces the heart rate, or can even lead to the 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 β-adrenergic receptors (pancreas, skeletal muscle, smooth muscles of the peripheral arteries, 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 -Adrenoreceptors.
PHARMACOKINETICS
Metoprolol is rapidly and almost completely (95%) absorbed in the digestive tract. Cmax in blood plasma is achieved 1-2 hours after ingestion. T1 / 2 averages 3.5 hours (ranging from 1 hour to 9 hours).degrees, in 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, breast-feeding should be discontinued.
Composition
1 tablet contains: metoprolol tartrate 50 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 the
From the nervous system: increased fatigue, weakness, headache, slowing of the speed of mental and motor reactions rarely – paresthesia in the limbs (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, the 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, a change in taste.
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.
Effect on the fetus: intrauterine growth retardation is possible, hypoglycemia, bradycardia.
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-blockers, theophylline, cocaine, estrogens (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (sodium retardation 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: expressed severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, fainting, with acute overdose, flushing, complete transverse blockage and cardiac arrest), cardialgia. 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 min, bath adrenostimulators – until reaching 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 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
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pharmacies Prescription
dosage form
dosage form
tablets
Merkle GmbH, Germany
