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

Excipients (core): cellulose microcrystalline - 58.5 mg, sodium carboxymethyl starch 3.2 mg, povidone (polyvinylpyrrolidone) 1.5 mg, magnesium stearate 1.5 mg, potato starch 5.0 mg, silicon dioxide colloid 0.3 mg.

Auxiliary substances (shell): Opadrai II 85F48105 white - 3.0 mg, incl. polyvinyl alcohol - 1,407 mg, macrogol-3350 - 0,708 mg, talc - 0,522 mg, titanium dioxide - 0,363 mg.

Active substance: atenolol 50.0 mg.

Excipients (core): cellulose microcrystalline - 117.0 mg, sodium carboxymethyl starch - 6.4 mg, povidone (polyvinylpyrrolidone) 3.0 mg, magnesium stearate 3.0 mg, potato starch 10.0 mg, silicon dioxide colloid 0.6 mg .

Auxiliary substances (shell): Opadrai II 85F48105 white - 6.0 mg, incl. polyvinyl alcohol - 2,814 mg, macrogol-3350 - 1,416 mg, talc - 1,044 mg, titanium dioxide - 0,726 mg.

Active substance: atenolol 100.0 mg.

Excipients (core): cellulose microcrystalline - 234.0 mg, sodium carboxymethyl starch - 12.8 mg, povidone (polyvinylpyrrolidone) - 6.0 mg, magnesium stearate - 6.0 mg, potato starch - 20.0 mg, silicon dioxide colloid - 1.20 mg.

Auxiliary substances (shell): Opadrai II 85F48105 white - 12.0 mg, incl. polyvinyl alcohol - 5,628 mg, macrogol-3350 - 2,832 mg, talc - 2,088 mg, titanium dioxide - 1,452 mg.

Description:

Cylindrical, biconvex tablets, covered with a film shell of white or almost white color, on the fracture are visible two layers - a core of white or almost white color and a film shell.

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 ingestion against the 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 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 impact and minute volume of blood.

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. Slim heart rate contractions (HR) at rest and under physical exertion. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers, the ventricles 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 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 arrhythmias and angina attacks).

Virtually does not weaken the bronchodilating effect of isoprenaline.

In contrast to nonselective beta-blockers, when administered at medium therapeutic doses, it has a less pronounced effect on organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus), and carbohydrate metabolism. 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 through the 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 components, cardiogenic shock, atrioventricular (AV) blockade of II-III st.(Without artificial cardiac pacemaker), bradycardia (heart rate less than 60 bpm. / Min.), Sick sinus syndrome, sinoatrial block, acute or chronic heart failure decompensation, cardiomegaly without signs of heart failure, Prinzmetal angina, hypotension ( in the case of myocardial infarction, systolic blood pressure less than 100 mm Hg) during breastfeeding, simultaneous inhibitors of monoamine oxidase (MAO), age 18 years (efficacy and safety Reparata is not installed). Severe asthma and chronic obstructive pulmonary disease (COPD) in history, pheochromocytoma (without simultaneous application of α-blockers), severe peripheral circulatory disorders.

Carefully:

Diabetes mellitus (may mask the symptoms of hypoglycemia), hypoglycemia, metabolic acidosis, conducting desensitizing therapy, chronic obstructive pulmonary disease, bronchospasm (in history) AV blockade of I degree, chronic heart failure (compensated), violations of peripheral circulation,pheochromocytoma (with simultaneous use of alpha-blockers), hepatic insufficiency, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, advanced age, pregnancy, surgical intervention.

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 was not 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.

Atenolol is secreted into breast milk, so if during breast-feeding the drug is necessary, breastfeeding is recommended to be canceled.

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 requires 1 -2 weeks of admission. If the antihypertensive effect is insufficient, the dose is increased to 100 mg in one dose. A further increase in the dose is not recommended, since it is not accompanied by an increase in the therapeutic 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.

Elderly patients and patients with impaired renal excretory function need to adjust the dosage 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 m (normal values are 100-150 ml / min / 1.73 m) significant accumulation 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 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, as the therapeutic effect is not increased, and the likelihood of side effects increases.

Side effects:

From the cardiovascular system: development (aggravation) of symptoms chronic heart failure (swelling of the ankles, stop, dyspnea), violation of atrioventricular conduction,arrhythmia, bradycardia, marked decrease in blood pressure, palpitations, decreased myocardial contractility, orthostatic hypotension, manifestations of angiospasm (cooling of the lower extremities, Raynaud's syndrome), vasculitis, chest pain, sinus node weakness syndrome.

From the central nervous system: dizziness, decreased ability to concentrate attention, 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.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, a taste disorder.

From the respiratory system: dyspnea, bronchospasm, apnea, nasal congestion.

From the side of the hemostasis system: thrombocyte purpura, anemia (aplastic), thrombosis.

On the part of the reproductive system: decreased potency, decreased libido, Peyronie's disease.

From the side of metabolism: hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients with type 1 diabetes), hypothyroid status.

From the skin: urticaria, dermatitis, itchy skin, photosensitivity, increased sweating, skin hyperemia, exacerbation of psoriasis, reversible alopecia.

From the sense organ: visual impairment, a decrease in the 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 the IH degree, an increase in symptoms of heart failure, a marked decrease in blood pressure, difficulty breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the fingernails or palms, convulsions, hypoglycemia.

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 marked decrease in blood pressure - the patient should be in the Trendelenburg position. If there are no signs of pulmonary edema - intravenously plasma-substituting solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; with chronic heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - intravenously diazepam. Dialysis is possible. In hypoglycemia, intravenous dextrose (glucose) can be indicated.

Interaction:

With the simultaneous use of atenolol with insulin, hypoglycemic agents for oral administration - their hypoglycemic effect is enhanced.

When used simultaneously with antihypertensive 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 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 intravenous administration, medicines for general anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

When used simultaneously 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 - every day, then once every 3-4 months), the concentration of blood glucose in patients with diabetes mellitus (1 time in 4-5 months.). In elderly patients it is recommended to monitor the kidney function (1 time in 4-5 months).

It is necessary to teach the patient how to calculate the heart rate and instruct him about the need for medical consultation at a heart rate of less than 60 beats per minute.

With thyrotoxicosis atenolol can mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, as it can strengthen symptoms.In diabetes mellitus can mask tachycardia caused by hypoglycemia. Unlike nonselective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.

Have patients with ischemic heart disease (CHD) abrupt withdrawal of beta-adrenoblockers can cause an increase in the frequency or severity of angio attacks, so the cessation of the use of atenolol in patients with IHD should be carried out gradually.

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. Overdose is dangerous development 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 surgery. 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 earlier than 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 (adrenaline) against the background of a weighed allergic 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 medical supervision to detect a marked decrease in blood pressure or bradycardia.

In the case of elderly patients with increasing bradycardia (less than 60 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm,ventricular arrhythmias, severe impairment 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 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. and more (reduce the dose by 25% in 3-4 days).

Atenolol should be withdrawn before examining the 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, film-coated at 25 mg, 50 mg, 100 mg.

Packaging:

For 10, 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50 or 100 tablets in cans of polymeric for medicines. One jar or 1, 2, 3, 4, 5 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package (bundle).

Storage conditions:

In 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:LP-002294

Date of registration:05.11.2013

Expiration Date:05.11.2018

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp28.09.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)