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

Composition:One tablet contains active substance atenolol 50 mg (0.05 g) or 100 mg (0.1 g), and Excipients: corn starch, calcium phosphate, microcrystalline cellulose, calcium stearate, magnesium stearate, primogel.

Description:Tablets are white or white with a weak grayish or creamy hue of color, flat-cylindrical shape. A slight "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 Ca ²⁺. 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 (diastolic elongation and improvement of myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to 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 in 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, almost does not weaken the bronchodilating effect of isoproterenol.

In therapeutic concentrations does not affect beta2-adrenoreceptors, in contrast to non-selective beta-blockers has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries and on 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.

Reduces the automatism of the sinus node, reduces the heart rate, slows down AV conductivity, reduces myocardial contractility, reduces the need for myocardium in oxygen. Reduces the excitability of the myocardium.

When used in moderate therapeutic doses, it has a less pronounced effect on the smooth musculature of the bronchi and peripheral arteries than non-selective beta-blockers.

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (50%), bioavailability - 40-50%, time to reach the maximum concentration in blood plasma -2-4 hours. It penetrates poorly through the blood-brain barrier, passes in small amounts through the placental barrier and in 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 / 1.73 m² -more than 27 hours (reduction of doses 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; acute myocardial infarction with stable hemodynamic parameters.

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, atrioventricular block II-III Article, bradycardia, sick sinus syndrome, sinus block, acute or chronic heart failure (decompensated), cardiomegaly without signs of heart failure, Prinzmetal angina, hypotension (in the case of myocardial infarction, systolic blood pressure less than 100 mm Hg. v.), lactation period, simultaneous reception of MAO inhibitors, under the age of 18 years (effectiveness and safety have defined).

Carefully:Diabetes mellitus, metabolic acidosis, hypoglycemia, allergic reactions in the history, chronic obstructive pulmonary disease (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 is excreted in breast milk, therefore 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 within a week the optimal therapeutic effect is achieved, increase the dose to 100 mg per day. 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 every 4 days

Patients on hemodialysis, Atenolol appoint 50 mg / day immediately after each dialysis, which must be done in a steady state, 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).

In acute myocardial infarction with stable parameters - after 12 hours - 50 mg twice a day or 100 mg once a day for 6-9 days or until discharge from the hospital (under the control of blood pressure, electrocardiograms, blood glucose levels).

Side effects:

The cardiovascular system: the appearance of symptoms of heart failure, violation of atrioventricular conduction, arrhythmias, bradycardia, marked decrease in blood pressure, orthostatic hypotension, palpitations.

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: thrombocyte purpura, anemia (aplastic), thrombosis.

Endocrine system: gynecomastia, decreased potency, decreased libido, hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status.

Metabolic reactions: hyperlipidemia.

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

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: back pain, arthralgia, withdrawal syndrome (increased angina attacks, increased blood pressure).

Overdose:

Symptoms: bradycardia, AV blockade of the IH degree, an increase in symptoms of heart failure, a marked decrease in blood pressure, bronchospasm, hypoglycemia, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the fingernails or palms, convulsions.

Treatment: gastric lavage and administration of adsorptive agents; 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 drugs 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 drugs (neuroleptics), ethanol, sedative and hypnotic LS increase the CNS depression.

Special instructions:

Monitoring of patients receiving atenolol, should include monitoring of heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), blood glucose in diabetic patients (1 every 4-5 months).In elderly patients it is recommended to follow the function of the kidneys (once every 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 / min.

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 ischemic heart disease (CHD), the abrupt withdrawal of beta-blockers can cause an increase in the frequency or severity of anginal attacks, so the cessation of atenolol in patients with IHD should be gradual. Particular attention also requires the selection of doses in patients with cardiac decompensation. Compared with non-selective beta-blockers, cardioselective beta-blockers have less effect on lung function,nevertheless, in obstructive airway diseases atenolol appoint 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 under anesthesia is required in patients taking atenolol. 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 and clonidine, the use of atenolol is stopped a few 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 the usual doses of epinephrine against the background of a burdened 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 constant observation of the doctor for the diagnosis of arterial hypotension or bradycardia.

In the case of an increased bradycardia (less than 50 / min), 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. Cancellation 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 0.05 g and 0.1 g.

Packaging:

For 30 tablets in cans of polymer type BP.

10 tablets per contour cell pack.

Each jar, 1 or 2 contour squares with instruction for use is placed in a bundle.

Storage conditions:

List B. In dry sheltered from light, out of reach of children, at a temperature of no higher than 25 ° C.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003868 / 01

Date of registration:22.07.2009 / 18.11.2011

Expiration Date:Unlimited

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)