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

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 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 blood vessels, the severity of which decreases gradually over a period of 1-3 days.

The hypotensive effect is associated with a decrease in cardiac output, a decrease in the activity of the renin-angiotensin system, the sensitivity of the baroreceptors, and effects on the central nervous system. The hypotensive effect is manifested by a decrease in systolic and diastolic arterial pressure, a decrease in the impact and minute volumes. In average therapeutic doses, it has no effect on the tone of peripheral arteries. The hypotensive effect lasts 24 hours, with regular admission stabilized by the end of 2 weeks 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 innervation. It reduces the heart rate at rest and during physical activity. By increasing the tension of the ventricular muscle fibers and the final diastolic pressure in the left ventricle, it can increase the demand for myocardium in 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 influences on the conduction system of the heart, inhibition of heterogeneous automatism, a decrease in the rate of propagation of excitation through the sinouauricular node, and an extension 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 by additional paths.

Reduces the automaticity of the sinus node, reduces the number of heartbeats (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.

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

Pharmacokinetics:

Absorption from the gastrointestinal tract is fast, incomplete (50%), bioavailability is 40-50%, the time to reach the maximum concentration in the blood plasma after ingestion is 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 an elongation of the half-life and cumulation: when the creatinine clearance is less than 35 mg / min / 1.73 m²the half-life is 16 to 27 hours, with creatinine clearance below 15 mg / 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);

- violation of the heart rhythm: 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 40-50 beats / min), sinus node weakness syndrome, sinouauric blockade, acute or chronic heart failure (in decompensation stage), cardiomegaly without signs of heart failure, angina prinzmetala, arterial hypotension (in case of use with myocardial infarction, systolic blood pressure (BP) less than 100 mm Hg), lactation period, simultaneous administration of monoamine oxidase (MAO) inhibitors, age to 18 years (efficacy and safety not in vivo Gödel).

Carefully:Diabetes mellitus, metabolic acidosis, hypoglycemia; allergic reactions in the anamnesis, chronic obstructive pulmonary disease (including emphysema of the lungs); AV blockade of I degree, chronic heart failure, obliterating diseases of peripheral vessels, ("intermittent" lameness, Raynaud's syndrome); pheochromocytoma, chronic renal failure, hepatic insufficiency, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, pregnancy, elderly age.

Pregnancy and lactation:

Pregnant women should be prescribed Atenolol Only in cases where the benefit to the mother exceeds the potential risk to the fetus. Atenolol is excreted in breast milk, therefore during the period of feeding it should be taken only in exceptional cases with great caution.

Dosing and Administration:

Assign inside, before eating, without chewing and washing down with a small amount of liquid.

Arterial hypertension: treatment is started with taking 50 mg of Atenolol 1 time per day. To achieve a stable hypotensive effect, 1 to 2 weeks of admission is required. If the hypotensive effect is insufficient, the dose is increased to 100 mg per 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. Sometimes it is possible to increase the dose to 200 mg once a 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 failure 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 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).

Increasing the daily dose of more than 100 mg is not recommended, because The therapeutic effect does not increase, and the likelihood of side effects increases.

Side effects:The cardiovascular system: development (aggravation) of symptoms of chronic heart failure (swelling of the ankles, stop, shortness of breath), violation of atrioventricular conduction, arrhythmias, bradycardia, marked decrease in blood pressure, orthostatic hypotension, palpitations.

Central nervous system: dizziness, sleep disturbance, decreased ability to concentrate, slow reaction, drowsiness, depression, hallucinations, 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.

Gastrointestinal tract: dry mouth, taste change, nausea, vomiting, diarrhea, constipation.

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

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

Endocrine system: gynecomastia, decreased potency, decreased libido, hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status.

Metabolic reactions: hyperlipidemia.

Skin reactions: urticaria, dermatitis, itching, photosensitivity, increased sweating, skin hyperemia, exacerbation of psoriasis, reversible alopecia.

Sense organs: impaired vision, dryness and soreness of the eyes, a decrease in the secretion of tear fluid, conjunctivitis.

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

Laboratory indicators: agranulocytosis, leukopenia, changes in the activity of "hepatic" enzymes, hyperbilirubinemia.

Other: withdrawal syndrome (increased angina attacks, increased blood pressure), back pain, arthralgia. The frequency of side effects increases with an increase in the dose of the drug.

Overdose:

Symptoms: severe bradycardia, atrioventricular block of II and III degree, increased symptoms of heart failure, marked decrease in blood pressure, bronchospasm, hypoglycemia, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of fingernails or palms, convulsions.

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 administration 1 - 2 mg of atropine, epinephrine or the setting of a temporary pacemaker; with ventricular extrasystole lidocaine (preparations IA class do not apply); with arterial hypotension - 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 heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam. Dialysis is possible.

Interaction:With the simultaneous use of Atenolol with insulin, oral hypoglycemic agents - their hypoglycemic effect is enhanced.

When combined with antihypertensive agents of different groups or nitrates, diuretics, sympatholytes, hypotensive effect is enhanced. 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 atrioventricular conduction disorders 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 simultaneous administration of Atenolol with derivatives of ergotamine, xanthine its effectiveness is reduced.

When the combined use of Atenolol and clonidine is discontinued, clonidine treatment is continued for several days after the withdrawal of Atenolol.

Simultaneous use with lidocaine can reduce its excretion and increase the risk of toxic effects of lidocaine.

The use together with phenothiazine derivatives helps to increase the concentration of each of the drugs in the blood serum.

Phenytoin with IV introduction,medicines for inhalation of general anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of reducing blood pressure.

When combined with eufillinom (aminophylline) and theophylline possible mutual suppression of therapeutic effects.

It is not recommended simultaneous use 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 increase the risk of severe systemic allergic reactions or anaphylaxis.

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 IV administration increase the risk of anaphylactic reactions.

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

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

Special instructions:

Control of patients receiving Atenolol, should include monitoring of heart rate and blood pressure (at the beginning of treatment - every day, then every 3 to 4 months), blood glucose in patients with diabetes mellitus (1 every 4 to 5 months). In elderly patients it is recommended to follow the function of the kidneys (once every 4 to 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 (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, as 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 blood glucose to normal concentrations.

In patients with coronary heart disease (CHD), abrupt withdrawal of beta-blockers may cause an increase in the frequency or severity of anginal attacks, so the termination of Atenolol in patients with IHD should be gradual.

In comparison with nonselective beta-adrenoblockers, cardioselective beta-blockers have less effect on lung function, however, in obstructive airway diseases Atenolol appoint only in the case of absolute indications. If you want to assign them in some cases, you can recommend the use of beta₂-adrenomimetics.

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 if surgical intervention under anesthesia is required 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 for several days before clonidine in order to avoid the withdrawal syndrome 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 medical supervision for the diagnosis of arterial hypotension or bradycardia. In the case of elderly patients with severe bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg) 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 necessary, intravenous verapamil should be done at least 48 hours after taking Atenolol.

With the use of Atenolol may reduce the production of tear fluid, which is important for patients who use 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 2 weeks or more (reduce the dose by 25 % in 3 - 4 days).

It is necessary to cancel the drug before examining the blood and urine content 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 driving motor vehicles and practicing potentially dangerous activities that require an increased concentration and speed of psychomotor reactions.

Form release / dosage:Tablets 50 mg, 100 mg.

Packaging:

For 10 and 15 tablets with a dosage of 50 mg in a loop cell package. For 10 tablets with a dosage of 100 mg per circuit cell pack. 3 contour packs of 10 tablets, 2 contour packs of 15 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007945/08

Date of registration:08.10.2008 / 22.09.2016

Expiration Date:Unlimited

The owner of the registration certificate:TATHIMFARMPREPARATY, JSC TATHIMFARMPREPARATY, JSC Russia

Manufacturer: & nbsp

TATHIMFARMPREPARATY, JSC Russia

Information update date: & nbsp20.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)