Description
Latin name
METOPROLOL-AKRI
Release form
Tablets.
Pharmacological action
Pharmaceutical group: selective beta-1 blocker.
Pharmaceutical action: Metoprolol is a cardioselective beta-adrenergic blocker that does not have internal sympathomimetic activity and membrane-stabilizing properties. It has hypotensive, antianginal and antiarrhythmic effects. Blocking beta1-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP stimulated by catecholamines 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).
The total peripheral 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 beta2-adrenergic receptor stimulation), which returns to the initial one after 1-3 days, and when prolonged use is reduced.
The antihypertensive effect is due to a reflex decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin-aldosterone system (more important in patients with initial hypersecretion of renin) and the central nervous system, and restoration of the sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces elevated blood pressure 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 (lengthening 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 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 AV conduction (mainly in the antegrade and, to a lesser extent, in retrograde directions) through the AV node and along additional paths.
With supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional heart diseases and hyperthyroidism, reduces heart rate, or may even lead to a restoration of sinus rhythm.
Prevents the development of migraines. When used in medium therapeutic doses, unlike non-selective beta-blockers, it has a less pronounced effect on organs containing beta2-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. ) has a blocking effect on both subtypes of beta-adrenergic receptors.
Pharmacokinetics: Absorption after oral administration is complete (95%). Cmax in blood plasma is achieved 1-2 hours after ingestion. T1 / 2 averages 3.5 hours (ranging from 1 to 9 hours). It is subjected to intensive presystemic metabolism, bioavailability is 50% at the first dose and increases to 70% with repeated use. Eating increases bioavailability by 20-40%. The bioavailability of metoprolol increases with cirrhosis.
Communication with plasma proteins – 10%. Penetrates through the blood-brain and placental barriers. It penetrates into breast milk in small quantities.
Metabolized in the liver, 2 metabolites have beta-adrenergic blocking activity. The isoenzyme of CYP2D6 takes part in the metabolism of the drug. About 5% is excreted unchanged by the kidneys.
Treatment of patients with impaired renal function does not require dose adjustment. Impaired liver function slows down the metabolism of the drug, and in cases of insufficiency of liver function, the dose of the drug should be reduced. Not removed by hemodialysis.
Indications
– arterial hypertension (as monotherapy or in combination with other antihypertensive agents)
– coronary heart disease: myocardial infarction (secondary prevention – complex therapy), prevention of angina attacks
– heart rhythm disturbances (supraventricular tachycardia ventricular extrasystole)
– hyperthyroidism (complex therapy)
– prevention of migraine attacks.
Use during pregnancy and lactation
During pregnancy, it is prescribed taking into account the ratio of the benefits to the mother and the risk to the fetus (due to the development of the fetus bradycardia, arterial hypotension, hypoglycemia).
At the same time, they closely monitor, especially the development of the fetus. It is necessary to monitor newborns within 48-72 hours after delivery.
The effect of metoprolol on a newborn, while breastfeeding has not been studied, therefore, women taking Metoprolol-Acre should stop breast-feeding.
Special instructions
Monitoring patients receiving Bidop should include a measurement of heart rate and blood pressure (at the beginning, lay down
Due to the lack of sufficient clinical data, the drug is not recommended for use in children.
Effect 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 dangerous activities that require increased concentration of attention and speed of psychomotor reactions. In the future, the determination of dose safety is carried out individually.
Composition
1 tablet: – metoprolol 100 mg
Excipients:
lactose,
potato starch,
silicon dioxide colloidal,
magnesium stearate,
povidone,
sodium starch glycolate.
Dosage and administration
Tablets are taken orally during or immediately after a meal, do not chew, drink a small amount of liquid.
Arterial hypertension: The initial daily dose is 50-100 mg in 1-2 doses (morning and evening). With an insufficient therapeutic effect, the daily dose can be gradually increased to 100-200 mg and / or additional prescription of other antihypertensive agents. 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).
Hyperthyroidism: 50 mg 2 times a day (morning and evening).
In elderly patients, with impaired renal function, as well as with the need for hemodialysis, the dose is not changed. In case of impaired liver function, the dose of Metoprolol-Acre should be reduced depending on the clinical condition.
Side effects
From the central 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 exacerbation of symptoms of chronic heart failure (edema, swelling of the feet and / or lower legs, shortness of breath), arrhythmias, manifestation of angiospasm (increased peripheral disturbance blood circulation, cooling of the lower extremities, Raynaud’s syndrome), impaired myocardial conduction.
From the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, 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 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 insulin-dependent diabetes mellitus).
Laboratory indicators: rarely – thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes, very rarely – 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 Interactions
Concomitant use with MAO inhibitors is not recommended 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. The simultaneous iv administration of verapamil can cause cardiac arrest. The concomitant use of nifedipine leads to a significant decrease in blood pressure.
Inhalation anesthetics (derivatives of hydrocarbons) increase the risk of inhibition of myocardial function and the development of arterial hypotension.
Beta-adrenergic agonists, theophylline, cocaine, estrogens (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (sodium retention and blocking prostaglandin synthesis by the kidneys) weaken the hypotensive effect.
There is an increase in the inhibitory effect on the central nervous system – with ethanol, the summation of the cardiodepressive effect – with anesthetics, an increased risk of peripheral circulation 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 symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).
When combined with antihypertensive drugs, diuretics, a sharp decrease in blood pressure can develop with nitroglycerin or slow calcium channel blockers (special care is necessary when combined with prazosin), an increase in the severity of a decrease in heart rate and inhibition of atrioventricular conduction – with metoprolol with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, reserpine clonidine, guanfacine, general anesthesia and cardiac glycosides. If metoprolol and clonidine are taken at the same time, then when metoprolol is canceled, clonidine is canceled after a few days (due to the risk of withdrawal syndrome).
Inducers of microsomal liver enzymes (rifampicin, barbiturates) lead to an increase in the metabolism of metoprolol, to a decrease in its concentration in blood plasma and a decrease in the effect. Inhibitors (cimetidine, oral contraceptives, phenothiazines) – increase the concentration of metoprolol in plasma.
Allergens used for immunotherapy or allergen extracts for skin tests when used together with metoprolol increase the risk of systemic allergic reactions or anaphylaxis iodine-containing radiopaque substances for iv administration increase the risk of anaphylactic reactions. Reduces xanthine clearance (except for diphillin), especially with the initially increased clearance of theophylline under the influence of smoking. It reduces the clearance of lidocaine, increases the concentration of lidocaine in blood plasma.
Strengthens and prolongs the action of antidepolarizing muscle relaxants, lengthens the anticoagulant effect of coumarins.
When combined with ethanol, the risk of a marked decrease in blood pressure increases.
Overdose
Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, pronounced decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, fainting, with acute overdose – cardiogenic shock, loss of consciousness, coma heart), cardialgia.
The first signs of overdose appear 20 min-2 hours after taking the drug.
Treatment: gastric lavage and absorption absorption symptomatic therapy: in case of pronounced decrease in blood pressure – the patient should be in Trendelenburg in case of excessive decrease in blood pressure, bradycardia and heart failure – in / in, with intervals of 2-5 min. adrenomimetics – to achieve the desired effect or in / in 0. 5-2 mg atropine sulfate. In the absence of a positive effect – dopamine, dobutamine or norepinephrine (norepinephrine).
As a follow-up, it is possible to administer 1-10 mg of glucagon, install a transvenous intracardiac pacemaker. At bronchospasm it is necessary to enter in / in beta2-adrenomimetics. Metoprolol is poorly excreted by hemodialysis.
Storage Conditions
In a dry, dark place at a temperature not exceeding 25 ° C. Keep out of reach of children.
Shelf life
4 years.
Deystvuyushtee substance
Metoprolol
Prescription conditions
pharmacy Prescription
dosage form
tablets
Possible Product Names
Metoprolol Retard-Akrikhin tablets 100 mg 30 pcs.
Akrihin HFK AO, Russia
