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

Tablets 25 mg: wheat starch 60,50 mg, lactose monohydrate 46,00 mg, microcrystalline cellulose 24,00 mg, carboxymethyl starch sodium (sodium starch glycolate) 12,00 mg, copovidone 5.00 mg, talc 5.00 mg, magnesium stearate 1.50 mg, silicon dioxide colloid 1.00 mg, Opaprai white OY-B-28920 (lecithin (soybean) - 2,000% by weight, polyvinyl alcohol 45.520% by weight, talc 20,000% by weight, titanium dioxide 32,000% by weight, xanthan rubber 0.480% by weight) - 5.00 mg;

Tablets 50 mg: wheat starch 74,50 mg, lactose monohydrate 80,00 mg, microcrystalline cellulose 15,00 mg, carboxymethyl starch sodium (sodium starch glycolate) 20,00 mg, copovidone 10.00 mg, talc 7.00 mg, magnesium stearate 2.50 mg, silicon dioxide colloid 1.00 mg, Opadrai yellow OY-GM-22920 (hypromellose 2910 15 cP 31.250% by weight, polydextrose 31.250% by weight, titanium dioxide 30.500% by weight, macrogol 4000 - 6.250% by weight, iron oxide yellow 0.750% by weight) - 7.00 mg.

Description:

Tablets 25 mg: round tablets of biconvex form, film-coated, white.

Tablets 50 mg: round tablets of biconvex form, film-coated, yellow.

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 catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions. In the first 24 hours after oral administration, with a decrease in cardiac output, there is a reactive increase in the total peripheral resistance of the vessels,which within 1-3 days gradually returns to the original and then gradually decreases. The antihypertensive effect is associated with a decrease in the minute volume of blood, a decrease in the activity of the renin-angiotensin-aldosterone system, the sensitivity of the baroreceptors and the influence on the central nervous system. Antihypertensive effect is manifested as a decrease in systolic and diastolic blood pressure (BP), a decrease in the shock and minute blood volume.

In average therapeutic doses does not affect the tone of peripheral arteries. Antihypertensive effect lasts 24 hours, with regular use stabilized by the end of 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 (HR) at rest and during physical activity. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibersVentricles 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 the impulses in the antegrade and, to a lesser extent, in the retrograde direction through the atrioventricular (AV) node and on additional ways of carrying out.

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

Reduces the automaticity of the sinus node, lowers 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.

Increases the survival rate of patients,who underwent myocardial infarction (reduces the incidence of ventricular arrhythmia and angina attacks).

Virtually does not weaken the bronchodilating effect of isoproterenol.

In contrast, non-selective beta-blockers when used in therapeutic doses medium has a less pronounced effect on organs containing beta 2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchial and uterine) and carbohydrate metabolism; the severity of atherogenic action does not differ from that of propranolol. To a lesser extent, it has a negative batmo-, chrono-, ino-and dromotropic effect. When used in large doses (more than 100 mg / day) has a blocking effect on both subtypes of beta adrenoreceptors.

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (50-60%), bioavailability - 40-50%, time to reach the maximum concentration in the blood plasma - 2-4 hours. It penetrates poorly 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 prolongation of the half-life and cumulation: when 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 tachyarrhythmia, ventricular extrasystole.

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, atrioventricular (AV) blockade II-III , severe bradycardia (heart rate less than 40 beats per minute), sinus node weakness syndrome, sinoauric blockade, acute or chronic heart failure in decompensation stage, cardiomegaly without symptoms of heart failure, angina prinzmetala, arterial hypotension (in case of use in infarction myocardium,systolic blood pressure less than 100 mm Hg), simultaneous administration of monoamine oxidase inhibitors (MAO), age to 18 years (efficacy and safety of the drug not established), patients with celiac disease (the preparation contains wheat starch); lactose intolerance, galactosemia or the syndrome of impaired glucose / galactose absorption (contains lactose monohydrate).

Carefully:

Diabetes mellitus, metabolic acidosis, hypoglycemia, allergic reactions in the anamnesis, 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 , elderly age, pregnancy.

Pregnancy and lactation:

Atenolol penetrates the placental barrier and is found in the umbilical cord blood. Studies on the use of atenolol in the first trimester have not been conducted and, therefore, the possibility of damaging effects on the fetus can not be ruled out.For the treatment of arterial Hypertension in the third trimester of pregnancy, the drug is used under close medical supervision. The use of atenolol during pregnancy can be a cause of impaired fetal growth. Assign atenolol pregnant or planning to become pregnant women should only be in cases where the benefit to the mother outweighs the potential risk to the fetus, especially in the first and second trimester of pregnancy, a hook as beta-blockers reduce the level of placental perfusion, which may result in fetal death or immaturity and premature birth. In addition, such side effects as hypoglycemia and bradycardia can be observed in both the fetus and the newborn.

Atenolol excreted in breast milk, so during the period of taking the drug should stop breastfeeding.

Dosing and Administration:

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

Arterial hypertension. Treatment is started with 50 mg of Atenolol 1 time per day. To achieve a stable antihypertensive effect, 1 to 2 weeks of admission is required.If the antihypertensive 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. 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 creatinine clearance values above 35 ml / min / 1.73 m² (the 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 prescribe at 25 or 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).

An increase in the daily dose of more than 100 mg is not recommended, since the therapeutic effect is not increased, and the likelihood of side effects increases.

Side effects:

The cardiovascular system: development (aggravation) of symptoms of chronic cardiac insufficiency (swelling of the ankles, stop, dyspnea), atrioventricular conduction disorder, arrhythmias, bradycardia, marked decrease in blood pressure, palpitations, weakening of myocardial contractility, orthostatic hypotension, manifestations of angiospasm (coldness of the lower extremities, Raynaud's syndrome), vasculitis, chest pain.

Central nervous system: dizziness, decreased ability to concentrate, decreased response time, drowsiness or insomnia, depression, hallucinations, fatigue, headache, weakness, nightmarish dreams, 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, abdominal pain, constipation or diarrhea, a change in taste.

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

Hematologic reactions: thrombocyte purpura, anemia (aplastic), thrombosis.

Endocrine system: decreased potency, decreased libido, hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients with type 1 diabetes), hypothyroid status.

Skin reactions: urticaria, dermatitis, pruritus, 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 "hepatic" enzymes, hyperbilirubinemia, thrombocytopenia (unusual bleeding and hemorrhage).

Other: pain in the back, arthralgia, withdrawal syndrome (tachycardia, increased attacks of angina, increased blood pressure, etc.).

The frequency of side effects increases with an increase in the dose of the drug.

Overdose:

Symptoms: pronounced bradycardia, AV blockade of II-III degree, increase in symptoms of heart failure, marked decrease in blood pressure, difficulty in breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of fingernails or palms, convulsions.

Treatment: gastric lavage and the use of adsorptive drugs; 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 of Class 1A 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 chronic heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam. Dialysis is possible.

Interaction:

With the simultaneous use of atenolol with insulin, hypoglycemic agents for oral administration - their hypoglycemic effect is enhanced. When combined with hypotensive agents of different groups or nitrates, the antihypertensive effect is enhanced. The simultaneous use of atenolol and verapamil (or diltiazem) can cause a mutual enhancement of cardiodepressive action.

The antihypertensive effect is weakened by estrogens (sodium retention) and non-steroidal anti-inflammatory drugs, glucocorticosteroids. With the simultaneous use of atenolol and cardiac glycosides, the risk of bradycardia and violation of atrioventricular conduction increases.

With the simultaneous use 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.

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, medicines for general anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

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

It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive action, a break in the treatment between the intake of MAO inhibitors and atenolol should be at least 14 days.

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.

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

Tri- and tetracyclic antidepressants, antipsychotics (antipsychotics), antipsychotics ethanol, sedatives and hypnotics increase the inhibition of the central nervous system,

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

Special instructions:

Control 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), the concentration of blood glucose in patients with diabetes (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 (eg, 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 restoration of glucose concentration in the blood to normal values. In patients with coronary heart disease (CHD), the abrupt withdrawal of beta-blockers can cause an increase in the frequency or severity of anginal attacks, so the termination of the use of Atenolol in patients with IHD should be gradual.

In comparison with non-selective beta-blockers, cardioselective beta-blockers have less effect on lung function, however, 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 assigned cardioselective adrenoblockers in case of intolerance and / or inefficiency of other antihypertensive drugs,but you should strictly follow the dosage. Overdosing is dangerous by the development of bronchospasm.

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

With the simultaneous use of Atenolol and clonidine, the use of Atenolol is stopped for several days before clonidine in order to avoid the symptom of the withdrawal of the latter. It is possible to increase the severity of the reaction of hypersensitivity and the lack of effect from the usual doses of epinephrine against the background of a burdened allergological anamnesis.

Drugs that reduce catecholamine stores (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 detection of a marked decrease in blood pressure or bradycardia.

In the case of a growing bradycardia in elderly patients (less than 50 beats per minute)arterial hypotension (systolic blood pressure below 100 mmHg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of liver and kidney function, it is necessary to 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.

At application Atenolola reduction of production of a tear fluid is possible, that is important at 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 canceled before the study of concentrations in the blood and urine 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 hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets coated with a film coat of 25 mg and 50 mg.

Packaging:10 tablets in a blister of PVC / aluminum foil. 3 blisters together with instructions for use in a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N013492 / 01-2001

Date of registration:13.12.2011

Expiration Date:Unlimited

The owner of the registration certificate:AKTAVIS, LTD. AKTAVIS, LTD. Russia

Manufacturer: & nbsp

BALKANPHARMA-DUPNITSA, AD Bulgaria

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)