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

Excipients: corn starch, magnesium hydroxycarbonate, silicon dioxide colloid (aerosil), microcrystalline cellulose, sodium lauryl sulfate, giprolose (hydroxypropylcellulose), talc, calcium stearate.

Description:

Tablets are white or white with a creamy shade of color, flat-cylindrical, with a bevel for dosing 50 mg, with a facet and a risk for a dosage of 100 mg, slight marbling is allowed.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B.03 Atenolol

Pharmacodynamics:

Cardioselective beta1-adrenoblocker has antianginal, antihypertensive and anti-arrhythmic effects. Does not possess membrane stabilizing and internal sympathomimetic activity. Blocking in low doses beta1-adrenoreceptors of the heart, reduces catecholamine-stimulated formation of cyclic adenosine monophosphate from adenine triphosphate, reduces the intracellular current of calcium ions. In the first 24 hours after ingestion 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 gradually decreases over the course of 1-3 days and returns to the initial, and with a prolonged appointment 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.In average therapeutic doses does not affect the tone of peripheral arteries. The hypotensive effect persists for 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 end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of 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 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.

Virtually does not weaken the bronchodilating effect of isoprenaline.

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%, the solubility in fats is very low, the time to reach the maximum concentration in the 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 (a decrease in doses is necessary): 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, with anuria lengthened to 144 hours. It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

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

- cardiac arrhythmias: sinus tachycardia, prevention of supraventricular tachyarrhythmias, ventricular extrasystole.

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, AV blockade II-III degree, pronounced bradycardia (heart rate less than 45-50 beats per minute), sinus node weakness syndrome, sinouauric blockade acute or chronic heart failure in decompensation stage, cardiomegaly without signs of heart failure, angina Prinzmetal,arterial hypotension (if systolic blood pressure is less than 100 mm Hg in case of myocardial infarction), lactation period, simultaneous administration of monoamine oxidase inhibitors (MAO), age to 18 years (efficacy and safety not established).

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:

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.

Atenolol is excreted in breast milk, so if the use of the drug is necessary, breastfeeding should be discontinued.

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, 1-2 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. 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 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 enhanced,and the likelihood of side effects increases.

Dose reduction in the event of planned cancellation is carried out gradually, by 1/4 dose every 3-4 days.

Side effects:

The cardiovascular system: development (aggravation) of symptoms of chronic heart failure (swelling of the ankles, stop, shortness of breath), violation AV conductivity, AV blockade (up to cardiac arrest), arrhythmias, bradycardia, marked decrease in blood pressure, palpitations, weakening of myocardial contractility, orthostatic hypotension, manifestations of angiospasm (cooling of the lower limbs, 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, 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.

Allergic reactions: itching, rash, hives.

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

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

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

Laboratory indicators: agranulocytosis, leukopenia, increased activity "hepatic" enzymes, hyperbilirubinemia, thrombocyte singing (unusual bleeding and hemorrhage).

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

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

Overdose:

Symptoms: pronounced bradycardia, AV blockade II-III degree, increased symptoms of heart failure, excessive reduction in blood pressure, difficulty breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the 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 - 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; atenolol masks the symptoms of developing hypoglycemia. 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 of atenolol weakens estrogens (due to delayed sodium) 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. Atenolol reduces the clearance of xanthines and increases their concentration in the plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

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

The simultaneous use of atenolol with lidocaine, can reduce its elimination and increase the risk of toxic effects of lidocaine.

The use of atenolol together with phenothiazine derivatives, contributes to increasing 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.

It is not recommended simultaneous use of atenolol with MAO inhibitors due to a significant increase in antihypertensive effect, a break in 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 with simultaneous use with atenolol increase the risk of severe systemic allergic reactions or anaphylaxis.

Means for inhalation anesthesia (derivatives of hydrocarbons) when used with atenolol increase the risk of oppression of myocardial function and the development of hypertension.

Amiodarone when used with atenolol increases the risk of bradycardia and oppression AV conductivity.

Cimetidine when used with atenolol increases the concentration of the latter in blood plasma (inhibits metabolism).

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

Atenolol prolongs the action of nondepolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotics (antipsychotics), antipsychotics ethanol, sedatives and hypnotics when used with atenolol increase the inhibition of the central nervous system.

Unhydrated ergot alkaloids when used with atenolol increase the risk of disordersperipheral circulation.

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 (I every 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). Severe cancellation of Atenolol in patients with thyrotoxicosis is contraindicated, since it can enhance symptoms. In diabetes mellitus can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers Atenolol practically does not increase insulin-induced hypoglycemia and does not delay the recovery of glucose in the blood to normal concentration.

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 stopping the intake Atenolol and in patients with IHD it is necessary to carry 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. 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 surgery. As an anesthetic, the drug should be chosen as possibly minimally negative inotropic action.

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 an increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of the liver and kidneys 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.

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).

It should be abolished before the study of blood and urine levels of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies 1-2 days before the test.

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 and 100 mg.

Packaging:

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

3 or 5 contour packs together with instructions for use are placed in a pack of cardboard.

Storage conditions:

List B. Store 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 expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N002154 / 01

Date of registration:22.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)