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

Excipients: corn starch, povidone low molecular weight, lactose (milk sugar), ethanol (ethyl alcohol), magnesium stearate, talc, silicon dioxide colloid, croscarmellose sodium (impellosis).

Description:

Round tablets white or white with a greyish or creamy shade of color with a facet and risk (for tablets with a dosage of 100 mg) or without risks (for tablets with a dosage of 50 mg). 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 catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of Ca²⁺. 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 the vessels, which gradually returns to the initial one within 1-3 days and then gradually decreases. The hypotensive effect is associated with a decrease in the minute volume of blood, a decrease in the activity of the renin-angiotensin system, the sensitivity of the baroreceptors and the influence on the central nervous system. The hypotensive effect is manifested as a decrease in systolic and diastolic blood pressure (BP), a decrease in the impact and minute volumes of blood.

In average therapeutic doses does not affect the tone of peripheral arteries.The hypotensive 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 increased stretching of ventricular muscle fibers 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.

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 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.

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 to nonselective beta-blockers, when administered at moderate therapeutic doses, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus), 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 Badly penetrates 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 / 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, expressed 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 signs of heart failure, angina prinzmetala, arterial hypotension (in case of myocardial infarction, systolic blood pressure less than 100 mmHg), lactation period, simultaneous administration of monoamine oxidase inhibitors (MAO), age to 18 years - efficacy and safety of the drug are not established.

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 treatment of 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 pregnancy, should only be used when the benefit to the mother exceeds the potential risk to the fetus, especially in the first and second trimester of pregnancy, since beta-blockers reduce the level of placental perfusion, which can lead to 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.

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 if during the period of breastfeeding the drug is indicated, it is better to stop breastfeeding for a while.

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.

With ischemic heart disease, tachysystolic heart rhythm disorders - 50 mg once a day.

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 values of creatinine clearance 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	Half-life	The maximum dose
(ml / min / 1.73 m²)	atenolol (h)
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 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 reaction rate, drowsiness or insomnia, depression, hallucinations, fatigue, headache, weakness, "nightmarish" dream, 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 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 non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), 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, excessive decrease in blood pressure, difficulty breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of fingernails or palms, convulsions.

Treatment: gastric lavage and administration of absorbent drugs; when bronchospasm occurs, inhalation or intravenous administration of beta2-adrenomimetic salbutamol is indicated. In violation of AV conduction, bradycardia - in / in introduction 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 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, glucocorticosteroids. 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, 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 effect,a break in treatment between taking 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 oppression 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), 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 (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 recovery of glucose in the blood to normal concentrations.

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 cessation 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 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 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 an increasing bradycardia (less than 50un / min), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of the liver and kidney function in elderly patients, 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.

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. and 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 mg, 100 mg.

Packaging:

10 tablets per contour cell pack.

3 or 5 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002160 / 01

Date of registration:21.05.2009

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)