Atenolol-Acry - instructions for use, dose, side effects, contraindications

Composition:One tablet contains the active substance atenolol 50 mg or 100 mg, as well as auxiliary substances: corn starch, magnesium hydroxycarbonate, povidone, gelatin medical, magnesium stearate, sodium starch glycolate.

Description:

Tablets are flat-cylindrical, with a facet and a risk, white or white with a greyish or creamy shade of color. Light marble is allowed.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B.03 Atenolol

Pharmacodynamics:

Has antianginal, antihypertensive and antiarrhythmic effect. Does not possess membrane stabilizing and internal sympathomimetic activity. Reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular current of calcium ions. In the first 24 hours after oral administration, against a background of a decrease in cardiac output, there is a reactive increase in the total peripheral resistance of blood vessels, the severity of which decreases gradually over the course of 1-3 days.

The hypotensive effect is associated with a decrease in cardiac output, a decrease in the activity of the renin-angiotensin system, the sensitivity of the baroreceptors, and effects on the central nervous system. The hypotensive effect is manifested as a decrease in systolic and diastolic blood pressure, a decrease in the impact and minute volumes. In average therapeutic doses does not affect the tone of peripheral arteries. The hypotensive effect lasts 24 hours, with regular use stabilized by the second week of treatment.

The antianginal effect is determined by the reduction in myocardial oxygen demand as a result of a decrease in the heart rate (diastole lengthening and improvement perfusion of the myocardium) and contractility, as well as a decrease in the sensitivity of the myocardium to the effects of sympathetic stimulation. It reduces the heart rate at rest and during physical activity. By increasing the tension of the ventricular muscle fibers and the end diastolic pressure in the left ventricle, it can increase the need for oxygen, especially in patients with chronic heart failure.

The antiarrhythmic effect is manifested by the suppression of sinus tachycardia and is associated with the elimination of arrhythmogenic sympathetic effects on the cardiac conduction system, a decrease in the rate of propagation of excitation through the sinoatrial node, and an elongation of the refractory period. Oppresses impulses in antegrade and, to a lesser extent, retrograde directions through AV (atrioventricular) node and on additional ways of carrying out.

Increases the survival rate of patients who underwent myocardial infarction (reduces the incidence of ventricular arrhythmia and angina attacks).Slightly reduces the vital capacity of the lungs, practically does not relieve the bronchodilating effect of isoproterenol.

At therapeutic concentrations, has no effect on beta2-adrenergic receptors, unlike nonselective beta-blockers has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries and lipid metabolism. When taking more than 100 mg per day may have a beta2-adrenergic blocking effect.

Negative chronotropic effect is manifested after 1 hour after administration, reaches a maximum after 2-4 hours, lasts up to 24 hours.

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (50%), bioavailability - 40-50%, solubility in fats is very low. Time to reach the maximum concentration in blood plasma is 2-4 hours. It penetrates badly through the blood-brain barrier, passes in small amounts through the placental barrier and into breast milk. Connection with blood plasma proteins - 6-16%.

It is not metabolized in the liver. The half-life is 6-9 hours (it increases in elderly patients). It is excreted by the kidneys by glomerular filtration (85-100% unchanged).Impaired renal function is accompanied by an elongation of the half-life and cumulation: when the creatinine clearance is less than 35 ml / min / 1.73 m² the half-life is 16-27 hours, with creatinine clearance below 15 ml / min - more than 27 hours (dose adjustment is necessary). It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

- prevention of angina attacks (except Prinzmetal angina pectoris);

- disorders of the heart rhythm: sinus tachycardia, prevention of supraventricular tachyarrhythmias, ventricular extrasystole, ventricular tachycardia;

- acute myocardial infarction with stable hemodynamic parameters.

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, atrioventricular block II-III (in the stage of decompensation), cardiomegaly without symptoms of heart failure, angina of Prinzmetal, arterial hypotension (in case of use with myocardial infarction, systolic blood pressure (BP), heart failure, less than 100 mm Hg), lactation period, simultaneous administration of MAO inhibitors, age to 18 years (efficacy and safety not determined).

Carefully:Diabetes mellitus, metabolic acidosis, hypoglycemia, allergic reactions in history, chronic obstructive pulmonary diseases (including emphysema of the lungs), AV blockade of the 1st degree, chronic heart failure (compensated), obliterating peripheral vascular diseases (intermittent claudication, Raynaud's syndrome), pheochromocytoma, hepatic insufficiency, chronic renal failure, myasthenia gravis, hyperthyroidism, depression (including history), psoriasis , pregnancy, advanced age.

Pregnancy and lactation:Pregnant women should be prescribed atenolol Only in those cases where the benefit to the mother exceeds the potential risk to the fetus. Atenolol excreted in breast milk, so during the period of feeding it should be taken only in exceptional cases and with great care.

Dosing and Administration:

Assign inside before eating, without chewing, squeezed a small amount of liquid.

Arterial hypertension. Treatment begins with 50 mg of atenolol 1 time per day. To achieve a stable hypotensive effect, 1 -2 weeks of admission is required. If the hypotensive effect is insufficient, the dose is increased to 100 mg in one dose.Further increase in the dose is not recommended, since it is not accompanied by an increase in the clinical effect.

Angina pectoris. The initial dose is 50 mg per day. If the optimum therapeutic effect is not achieved within a week, the dose to 100 mg per day is increased. Sometimes it is possible to increase the dose to 200 mg once a day. Older patients and patients with impaired renal excretory function need a correction of the dosing regimen. In the presence of renal failure, dose adjustment is recommended depending on the creatinine clearance. In patients with renal insufficiency with values of creatinine clearance above 35 ml / min / 1.73 m² (normal values are 100-150 ml / min / 1.73 m²) significant cumulation of atenolol does not occur.

The following maximum doses are recommended for patients with renal insufficiency:

Creatinine clearance (ml / min / 1.73 m²)	The half-life of atenolol (h)	The maximum dose
15-35	16-27	50 mg per day or 100
		mg every other day
less than 15	more than 27	50 mg every other day or
		100 mg once every 4 days

For patients on hemodialysis, Atenolol-Acri® is given at a dose of 50 mg / day immediately after each dialysis, which must be performed under steady-state conditions, since there may be a decrease in blood pressure.

In elderly patients, the initial single dose is 25 mg (can be increased under the control of blood pressure, heart rate (heart rate)).

Acute myocardial infarction with stable hemodynamic parameters. After 12 hours - 100 mg once a day or 50 mg twice a day for 6-9 days (under the control of blood pressure, ECG, blood glucose level).

Side effects:

The cardiovascular system: the appearance of symptoms of heart failure, violation of atrioventricular conduction, arrhythmias, bradycardia, pronounced lowering of blood pressure, orthostatic hypotension, palpitations, thrombosis.

Central nervous system: dizziness, decreased ability to concentrate, drowsiness, depression, hallucinations, lethargy, fatigue, headache, weakness, insomnia, nightmares, anxiety, confusion or short-term memory loss, paresthesia in the extremities (in patients with "intermittent" lameness and Raynaud's syndrome), muscle weakness, convulsions.

Gastrointestinal tract: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation, taste change.

Respiratory system: dyspnea, bronchospasm, apnea, nasal congestion.

Hematologic reactions: thrombocytopenic purpura, anemia (aplastic). Endocrine system: gynecomastia, decreased potency, decreased libido, hyperglycemia patients with non-insulin-dependent diabetes mellitus).

Metabolic reactions: hyperlipidemia, hypoglycemia.

Skin reactions: urticaria, dermatitis, itching, photosensitivity, increased sweating, skin hyperemia, exacerbation of psoriasis.

Sense organs: impaired vision, decreased secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis.

Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Laboratory indicators: agranulocytosis, leukopenia, increased activity of "hepatic" enzymes, bilirubin level.

Other: pain in the back and chest, arthralgia, vasculitis, withdrawal syndrome (increased angina attacks, increased blood pressure).

Overdose:

Symptoms, bradycardia, AV blockade II-III degree, the increase in symptoms of heart failure, a marked decrease in blood pressure, bronchospasm, hypoglycemia, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the fingernails or fingers, convulsions.

Treatment: gastric lavage and the appointment of absorbents; when bronchospasm occurs, inhalation or intravenous administration of beta2-adrenomimetic salbutamol is indicated; in violation of AV conduction, bradycardia - intravenous injection of 1-2 mg of atropine, epinephrine or the setting of a temporary pacemaker; with ventricular extrasystole - lidocaine (preparations IA class do not apply); with a decrease in blood pressure - the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema - intravenous plasmasubstitutional solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; with heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam. Dialysis is possible.

Interaction:

With the simultaneous use of atenolol with insulin, antidiabetic drugs - their hypoglycemic effect is enhanced.

When combined with antihypertensive agents of different groups or nitrates, hypotensive effect is enhanced. The simultaneous use of atenolol and verapamil (or diltiazem) can cause a mutual enhancement of cardiodepressive action.

The hypotensive effect is weakened by estrogens (sodium retention) and non-steroidal anti-inflammatory drugs.

With the simultaneous use of atenolol and cardiac glycosides, the risk of bradycardia and violation of atrioventricular conduction increases.

With the simultaneous administration of atenolol with reserpine, methyldopa, clonidine, verapamil, a pronounced bradycardia may occur.

Simultaneous intravenous administration of verapamil and diltiazem can provoke cardiac arrest; nifedipine can lead to a significant decrease in blood pressure.

With the simultaneous use of atenolol with derivatives of ergotamine, xanthine, its effectiveness is reduced.

When the combined use of atenolol and clonidine is discontinued, clonidine treatment continues for a few more days after atenolol is discontinued.

Simultaneous use with lidocaine may reduce its elimination and increase the risk of toxic effects of lidocaine.

The use together with phenothiazine derivatives, promotes an increase in the concentration of each of the drugs in the blood serum.

Phenytoin with IV introduction, funds for general anesthesia increase the severity of cardiosupressive action.

When combined with euphyllin and theophylline, mutual suppression of therapeutic effects is possible.

It is not recommended simultaneous use with MAO inhibitors.

Allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis. Means for inhalation anesthesia (derivatives of hydrocarbons) increase the risk of oppression of myocardial function and the development of hypertension.

Amiodarone increases the risk of bradycardia and oppression AV conductivity.

Cimetidine increases the concentration in the blood plasma (inhibits metabolism).

Iodine-containing radiopaque agents for intravenous administration increase the risk of anaphylactic reactions.

Prolongs the effect of nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic, sedative and hypnotic drugs increase the inhibition of the central nervous system.

Special instructions:

Monitoring of patients receiving atenolol, should include monitoring of heart rate and blood pressure (at the beginning of treatment - daily, then 1 time in 3-4 months), blood glucose in diabetic patients (1 time in 4-5 months).In elderly patients it is recommended to monitor the kidney function (1 time in 4-5 months).

You should teach the patient how to calculate heart rate and instruct you about the need for medical consultation at a heart rate of less than 50 beats per minute.

With thyrotoxicosis atenolol can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms. In diabetes mellitus can mask tachycardia caused by hypoglycemia. In contrast to nonselective beta-blockers, it does not substantially increase insulin-induced hypoglycemia and does not delay the recovery of glucose in the blood to normal levels.

In patients with coronary heart disease (CHD), abrupt cancellation of beta-blockers can cause an increase in the frequency or severity of anginal attacks, so the discontinuation of Atenolol-ACRI in patients with IHD should be gradual.

Particular attention also requires the selection of doses in patients with cardiac decompensation. In comparison with non-selective beta-blockers,cardioselective beta-blockers have less effect on lung function, however, in obstructive airways diseases, Atenolol-ACRI is prescribed only in the case of absolute indications. If necessary, in some cases, the use of beta2-adrenomimetics can be recommended.

Patients with bronchospastic diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but strict monitoring of dosage should be carried out. Overdosing is dangerous by the development of bronchospasm.

Particular attention is needed in cases where surgical intervention is required under anesthesia in patients taking Atenolol-ACRI. The drug should be discontinued 48 hours before the intervention. As an anesthetic, the drug should be chosen with the possible minimum negative inotropic effect.

With the simultaneous use of Atenolol-ACRI and clonidine, the use of Atenolol-ACRI is discontinued for several days before clonidine in order to avoid the symptom of withdrawal of the latter.

It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from conventional dosesepinephrine against a background of a weighed allergic anamnesis.

Drugs that reduce catecholamine stocks (for example, reserpine), can enhance the action of beta-blockers, so patients who take such combinations of drugs, should be under the constant supervision of the doctor for the diagnosis of arterial hypotension or bradycardia.

In the case of an increased bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg) in elderly patients, AV blockade, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction reduce the dose or stop treatment.

It is recommended to stop therapy with the development of depression caused by the use of beta-blockers.

If intravenous verapamil is needed, this should be done at least 48 hours after taking atenolol.

When using atenolol, tear production can be reduced, which is important in patients using contact lenses.

Do not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction.Abolition is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days).

It should be abolished before the study of blood and urine levels of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies.

In smokers, the effectiveness of beta-blockers is lower.

Effect on the ability to drive transp. cf. and fur:During the treatment period it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 50 and 100 mg.

Packaging:For 10 or 14 tablets in a planar cell package. For 2, 3 or 5 contour squares with instructions for use are placed in a cardboard box.

Storage conditions:

List B. In a dry, protected from light and inaccessible to children at a temperature of no higher than 25 ° C.

Shelf life:

2 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003306 / 01

Date of registration:03.03.2009

Expiration Date:Unlimited

Date of cancellation:2016-10-03

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Information update date: & nbsp08.10.2017

Illustrated instructions

Instructions

Atenolol-Acry® (Atenolol-Akri®)