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

Description:Tablets from white to white with a creamy shade of color, round, flat-cylindrical shape with a facet and a risk. Allowed a slight marbling.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B.03 Atenolol

Pharmacodynamics:

Has antianginal, hypotensive and antiarrhythmic action. 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, 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-aldosterone system, the sensitivity of the aortic arch baroreceptors and the influence on the central nervous system. Hypotensive effect is manifested as a decrease in systolic and diastolic blood pressure, a decrease in the impact and minute volume of blood. In average therapeutic doses does not affect the tone of peripheral arteries.

The hypotensive effect lasts 24 hours, with regular use stabilizes 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 final diastolic pressure in the left ventricle of the heart and increasing the tension of the ventricular muscle fibers atenolol can increase the need for myocardium in oxygen, especially in patients with chronic heart failure.

Antiarrhythmic effect is manifested in the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, arterial hypertension), a decrease in the rate of excitation through the sinoatrial node, and an elongation of the refractory period. Inhibits impulses in antegrade and, to a lesser extent, in retrograde directions through atrioventricular (AV) node and on additional ways of carrying out.

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 non-selective beta-blockers when administered at average therapeutic doses atenolol has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus), and carbohydrate metabolism. When used in large doses (more than 100 mg / day) has a blocking effect on both subtypes of beta adrenoreceptors.

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

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (50%), 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 in breast milk. Connection with blood plasma proteins - 6-16%.It is not metabolized in the liver. The half-life period 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 displayed during the procedure of hemodialysis.

Indications:

Arterial hypertension.

Prevention of angina attacks (except for Prinzmetal angina).

Heart rhythm disturbances: sinus tachycardia, prevention of supraventricular tachyarrhythmias, ventricular extrasystole.

Contraindications:

Hypersensitivity to atenolol or other components of the drug, cardiogenic shock, - atrioventricular block II-III st, pronounced 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,Prinzmetal angina, arterial hypotension (in case of use with myocardial infarction, systolic blood pressure less than 100 mm Hg), breastfeeding period, simultaneous administration of monoamine oxidase (MAO) inhibitors, age under 18 years (efficacy and safety not established).

Carefully:

Diabetes mellitus, metabolic acidosis, hypoglycemia, weighed down allergic anamnesis, chronic obstructive pulmonary disease, emphysema, bronchial asthma, AV blockade of I degree, chronic heart failure (compensated), obliterating diseases of peripheral vessels ("intermittent" lameness, Raynaud's syndrome), pheochromocytoma (with the simultaneous use of alpha-adrenoblockers), severe disturbances of peripheral blood circulation, hepatic insufficiency, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, pregnancy, elderly age.

Pregnancy and lactation:

The use of the drug is possible only in cases where the benefit to the mother exceeds the potential risk to the fetus,

Atenolol excreted in breast milk, so if you need to use the drug during breastfeeding, breastfeeding should be discarded.

Dosing and Administration:

Inside before eating, not liquid, squeezed a small amount of liquid.

The maximum daily dose is 100 mg.

Arterial hypertension. Treatment begins with 50 mg of atenolol 1 time per day. To achieve a stable hypotensive effect, it takes 1-2 weeks to take. 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.

Violation of the heart rate. When tachistystolic heart rhythm disorders are prescribed 50 mg per day.

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 values of creatinine clearance above 35 ml / min / 1.73 m²(normal values are 100-15 0 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 hospital setting, since there may be a decrease in blood pressure.

In elderly patients, the initial single dose is 25 mg (1/2 tablet 50 mg). The dose can be increased under the control of blood pressure and heart rate.

Side effects:

From the cardiovascular system: the appearance (aggravation) of symptoms of chronic heart failure (swelling of the ankles, feet), palpitations, violation of atrioventricular conduction, arrhythmias, bradycardia, pronounced lowering of arterial pressure, orthostatic hypotension, manifestations of angiospasm (coldness of the lower extremities, Raynaud's syndrome)vasculitis, pain in the chest.

From the 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 patients with "intermittent" lameness and Raynaud's syndrome), muscle weakness, convulsions.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, diarrhea, abdominal pain, constipation, taste change, intrahepatic cholestasis, ischemic colitis.

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

From the hematopoiesis: thrombocytic purpura, anemia (aplastic), thrombosis, mesenteric thrombosis.

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

From the side of metabolism: hyperlipidemia.

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

From the 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" transaminases, the concentration of bilirubin, an increase in the titer of antinuclear antibodies.

Other: pain in the back, arthralgia, withdrawal syndrome (increased angina attacks, increased blood pressure), Peyronie's syndrome, a syndrome accompanied by pain in the throat.

If any of the side effects listed in the manual are aggravated, or you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

Symptoms: pronounced bradycardia, AV blockade II-III degree, the increase in symptoms of chronic 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 the appointment of absorbents; 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 - intravenously plasma-substituting solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine. With hypoglycemia - the introduction of a solution of dextrose (glucose); with heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - intravenously 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, 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), non-steroidal anti-inflammatory drugs and 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.

Application together with phenothiazine derivatives, contributes to the increase concentration of each of the drugs in the blood serum ..

Phenytoin with intravenous administration, means 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 for 14 days and after. Allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis.

The 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 developing anaphylacticreactions.

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

Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase the inhibition of the central nervous system.

With simultaneous use with disopyramide, the steady-state concentration in the blood increases (C_ss) and the clearance of disopyramide decreases, conduction disruption is possible.

The simultaneous use of quinidine and atenolol can lead to orthostatic hypotension.

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

Special instructions:

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

It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at heart rate less than 50 beats per minute.

With thyrotoxicosis atenolol can mask certain clinical signs of thyrotoxicosis (for example, 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.

In patients with coronary heart disease, abrupt cancellation of beta-blockers can cause an increase in the frequency or severity of anginal attacks, so stopping the use of atenolol in patients with ischemic heart disease should be done gradually.

Particular attention also requires the selection of doses in patients with chronic heart failure. 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. Reception of the drug Atenolol 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 stocks (for example, reserpine), can enhance the action of beta-blockers, so patients who take such combinations of drugs should be under constant medical supervision for the diagnosis of arterial hypotension or bradycardia.

In the case of elderly patients with increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mmHg) AV 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, it 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 two weeks or more (reduce the dose by, 25 % in 3-4 days).

It is necessary to cancel the drug Atenolol 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 period of treatment, it is recommended to refrain from driving vehicles, servicing moving mechanisms and practicing other potentially dangerous activities requiring increased 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 printed lacquered.

For 3, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002610

Date of registration:22.03.2012

Expiration Date:Unlimited

The owner of the registration certificate:KIROVSKAYA PHARMACEUTICAL COMPANY, LTD. KIROVSKAYA PHARMACEUTICAL COMPANY, LTD. Russia

Manufacturer: & nbsp

KIROVSKAYA PHARMACEUTICAL COMPANY, LTD. Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)