Metoprolol retard-Akrikhin 25 mg long-acting tablets 30
Women's clothing size
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active substance: metoprolol tartrate in terms of 100 % substance - 25 mg;
excipients: lactose monohydrate, silicon dioxide colloidal, potato starch, povidone, sodium carboxymethyl starch, magnesium stearate.
Metoprolol refers to cardioselective blockers of beta-adrenergic receptors, which does not have internal sympathomimetic activity and membrane-stabilizing properties. It has a hypotensive, antianginal and antiarrhythmic effect. Blocking in low doses beta1-adrenergic receptors of the heart, reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular flow of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic action (reduces the heart rate (heart rate), inhibits conductivity and excitability, reduces myocardial contractility).
The total peripheral resistance at the beginning of the use of beta-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 beta2-adrenergic receptors), which after 1-3 days returns to the original, and with prolonged use - decreases.
The hypotensive effect is due to a reflex decrease in cardiac output and synthesis of renin, inhibition of the activity of the renin-angiotensin-apdosterone system (of greater 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, as a result, a decrease in peripheral sympathetic influences. Reduces high blood pressure pressure (BP) 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 stable decrease is observed after several weeks of regular intake.
The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of heart rate reduction (lengthening of diastole and improvement of 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 tolerance to physical activity.
The 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 the sinus and ectopic pacemakers and deceleration of atrioventricular (AV) conduction (predominantly in the antegrade and, to a lesser extent, in the retrograde direction) through the AV node and along additional pathways.
With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart disease and hyperthyroidism, it reduces heart rate, or can even lead to the restoration of sinus rhythm.
Prevents the development of migraine. When used in medium therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of 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 beta-adrenergic receptors.
Absorption when ingested is complete (95%). Maximum concentration in the blood plasma is achieved 1-2 hours after ingestion. The average half-life is 3.5 hours (ranging from 1 to 9 hours). Undergoes intensive presystemic metabolism, bioavailability is 50% at the first dose and increases to 70% with repeated use. Food intake increases bioavailability by 20-40%.
The bioavailability of metoprolol increases with cirrhosis of the liver. The connection with blood plasma proteins is 10%. It penetrates 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 CYP2D6 takes part in the metabolism of the drug. About 5% is excreted unchanged by the kidneys. Treatment of patients with reduced renal function does not require dose adjustment. Impaired liver function slows down the metabolism of the drug, and in cases of liver failure, the dose of the drug should be reduced. Not removed during hemodialysis.
Indications for use
- arterial hypertension (as monotherapy or in combination with other antihypertensive drugs);
- ischemic 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.
- hypersensitivity to metoprolol or other components of the drug, other beta-blockers;
- cardiogenic shock;
- atrioventricular blockade (AV) ii-III degree;
- syndrome of weakness of the sinus node;
- pronounced bradycardia;
- chronic cardiac insufficiency in the stage of decompensation;
- Prinzmetal's angina;
- arterial hypotension (in the case of use in the secondary prevention of myocardial infarction - systolic blood pressure less than 100 mm Hg. st., heart rate less than 45 beats / min);
- lactation period (see "Pregnancy and lactation");
- simultaneous administration of monoamine oxidase inhibitors (MAO) or simultaneous intravenous administration of verapamil (see "Interaction with other drugs");
- age up to 18 years (efficacy and safety have not been established);
- lactose intolerance, lactase deficiency or Glucose-galactose malabsorption.
Dosage and Administration
Tablets are taken orally during or immediately after a meal, do not chew, wash down with a small amount of liquid. Arterial hypertension. The initial daily dose is 50-100 mg in 1-2 reception (morning and evening). With insufficient therapeutic effect, the daily dose can be gradually increased to 100-200 mg and / or additional administration of other antihypertensive drugs. 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).
Hyperthyroidism. 50 mg 2 times a day (morning and evening).
In elderly patients, with impaired renal function, as well as if necessary, hemodialysis, the dose is not changed. In case of impaired liver function, the dose of the drug should be reduced depending on the clinical condition.
From the central nervous system: increased fatigue, weakness, headache, slowing down the speed of mental and motor reactions. Rarely - paresthesia in limbs (in patients with "intermittent" claudication and Raynaud's syndrome), depression, anxiety, decreased attention, drowsiness, insomnia, "nightmarish" dreams, confusion or short-term memory impairment, muscle weakness.
From the senses: rarely - decreased vision, decreased secretion of tear fluid, dry and painful eyes, conjunctivitis, tinnitus.
From the cardiovascular system: sinus bradycardia, palpitations, lowering blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness). Rarely - a decrease in myocardial contractility, a temporary aggravation of the symptoms of chronic heart failure (edema, swelling of the feet and / or lower legs, shortness of breath), arrhythmias, angiospasm (increased peripheral circulatory disorders, cooling of the lower extremities, Raynaud's syndrome), impaired myocardial conduction.
From the digestive system: nausea, vomiting, pain in the abdomen, dry mouth, diarrhea, constipation, 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 insulin-dependent diabetes mellitus).
Laboratory indicators: rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of "hepatic" enzymes, extremely rarely - Hyperbilirubinemia.
Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia are possible.
Other: pain in the back or joints, as and all beta-blockers in isolated cases can cause a slight increase in body weight, a decrease in libido and / or potency.
Keep out of reach of children.
- Dosage form
- long-acting tablets
- 25 mg
- Number of tablets
- INN Russian