Atenolol tablets 50mg, No. 30

Arterial hypertension, hypertensive crisis, mitral valve prolapse, hyperkinetic cardiac syndrome of functional genesis, neurocirculatory dystonia of the hypertensive type.

Treatment: ischemic heart disease, angina pectoris (tension, rest and unstable).

Treatment and prevention: myocardial infarction (acute phase with stable hemodynamic parameters, secondary prevention).

Arrhythmias (including with general anesthesia, congenital long QT syndrome, myocardial infarction without signs of chronic heart failure, thyrotoxicosis), sinus tachycardia, paroxysmal atrial tachycardia, supraventricular and ventricular extrasystole and supraventricular tachycardia ...

Essential and senile tremors, agitation and tremors in withdrawal symptoms.

As part of complex therapy: hypertrophic obstructive cardiomyopathy, pheochromocytoma (only together with alpha-blockers), thyrotoxicosis; migraine (prevention).

Set individually. The usual dose for adults - by mouth, at the beginning of treatment is 25-50 mg 1 time / day. If necessary, the dose is gradually increased. In case of impaired renal function in patients with CC 15-35 ml / min - 50 mg / day; with CC less than 15 ml / min - 50 mg every other day.

Maximum dose: for adults when taken orally - 200 mg / day in 1 or 2 doses.

One tablet contains

active substance - atenolol, 50 mg

AV block II and III degree, sinoatrial blockade, SSSU, bradycardia, (heart rate less than 40 beats / min), arterial hypotension (if used for myocardial infarction, systolic blood pressure less than 100 mm Hg), cardiogenic shock, chronic heart failure stage IIB-III, acute heart failure, Prinzmetal's angina, lactation period, concomitant use of MAO inhibitors, hypersensitivity to atenolol.

pharmachologic effect

Cardioselective beta1-blocker without intrinsic sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects.

Reduces the stimulating effect on the heart of sympathetic innervation and catecholamines circulating in the blood. It has a negative chrono-, dromo-, batmo- and inotropic effect: it reduces heart rate, inhibits conductivity and excitability, and reduces myocardial contractility. OPSS at the beginning of the use of beta-blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in the activity of? -Adrenergic receptors and elimination of stimulation of? 2-adrenergic receptors), after 1-3 days it returns to the initial one, and decreases with prolonged use.

The hypotensive effect is associated with a decrease in the minute blood volume, a decrease in the activity of the renin-angiotensin system (it is of greater importance for patients with initial hypersecretion of renin), the sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and the effect on the central nervous system; is manifested by a decrease in both systolic and diastolic blood pressure, a decrease in stroke volume and minute volume. In medium therapeutic doses, it does not affect the tone of the peripheral arteries.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening of diastole and an improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. The decrease in heart rate occurs at rest and during exercise. By increasing the end-diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, oxygen demand can increase, especially in patients with chronic heart failure.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in AV conduction. Suppression of impulse conduction is observed mainly in the antegrade and to a lesser extent in the retrograde directions through the AV node and along additional pathways.

Unlike nonselective beta-blockers, when used in moderate therapeutic doses, it has a less pronounced effect on organs containing ?2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus), and on carbohydrate metabolism; the severity of atherogenic action does not differ from the action of propranolol. To a lesser extent, negative batmo-, chrono-, ino- and dromotropic effects are expressed. When used in high doses (more than 100 mg / day), it causes blockade of both subtypes of ?-adrenergic receptors.

The antihypertensive effect lasts 24 hours, with regular use it stabilizes by the end of 2 weeks of treatment. The negative chronotropic effect is manifested 1 hour after ingestion, reaches a maximum after 2-4 hours and lasts up to 24 hours.

Pharmacokinetics

After oral administration, absorption from the gastrointestinal tract is 50-60%, bioavailability is 40-50%. Virtually not metabolized in the body. Poorly penetrates the BBB. Plasma protein binding - 6-16%.

T1 / 2 is 6-9 hours. It is excreted mainly by the kidneys unchanged. Renal dysfunction is accompanied mainly by an increase in T1 / 2 and cumulation: with CC less than 35 ml / min T1 / 2 is 16-27 hours, with CC less than 15 ml / min - more than 27 hours, with anuria it is extended to 144 hours. during hemodialysis.

In elderly patients, T1 / 2 increases.

Indications of the active substances of the drug Atenolol

Arterial hypertension, hypertensive crisis, mitral valve prolapse, hyperkinetic cardiac syndrome of functional genesis, neurocirculatory dystonia of the hypertensive type.

Treatment: ischemic heart disease, angina pectoris (tension, rest and unstable).

Treatment and prevention: myocardial infarction (acute phase with stable hemodynamic parameters, secondary prevention).

Arrhythmias (including with general anesthesia, congenital long QT syndrome, myocardial infarction without signs of chronic heart failure, thyrotoxicosis), sinus tachycardia, paroxysmal atrial tachycardia, supraventricular and ventricular extrasystole and supraventricular tachycardia ...

Essential and senile tremors, agitation and tremors in withdrawal symptoms.

As part of complex therapy: hypertrophic obstructive cardiomyopathy, pheochromocytoma (only together with alpha-blockers), thyrotoxicosis; migraine (prevention).

Side effect

From the side of the cardiovascular system: in some cases - bradycardia, arterial hypotension, abnormalities of AV conduction, the appearance of symptoms of heart failure.

From the digestive system: at the beginning of therapy, nausea, constipation, diarrhea, dry mouth are possible.

From the nervous system: at the beginning of therapy, fatigue, dizziness, depression, mild headache, sleep disturbances, a feeling of cold and paresthesia in the extremities, a decrease in the patient's reactivity are possible.

From the side of the organ of vision: a decrease in the secretion of lacrimal fluid, conjunctivitis.

From the endocrine system: decreased potency, hypoglycemic conditions in patients with diabetes mellitus.

From the respiratory system: in predisposed patients - the appearance of symptoms of bronchial obstruction.

Allergic reactions: itchy skin.

Others: increased sweating, skin redness.

Contraindications for use

AV block II and III degree, sinoatrial blockade, SSSU, bradycardia, (heart rate less than 40 beats / min), arterial hypotension (if used for myocardial infarction, systolic blood pressure less than 100 mm Hg), cardiogenic shock, chronic heart failure stage IIB-III, acute heart failure, Prinzmetal's angina, lactation period, concomitant use of MAO inhibitors, hypersensitivity to atenolol.

Application during pregnancy and lactation

Atenolol crosses the placental barrier, therefore, use during pregnancy is possible only if the intended benefit to the mother outweighs the possible risk to the fetus.

Atenolol is excreted in breast milk, therefore, if necessary, use during lactation is recommended to stop breastfeeding.

Application for violations of liver function

Use with caution in liver failure.

Application for impaired renal function

It should be used with caution in chronic renal failure. In case of impaired renal function in patients with CC 15-35 ml / min - 50 mg / day; with CC less than 15 ml / min - 50 mg every other day.

Application in children

It should be used with caution in pediatrics (efficacy and safety have not been determined).

Use in elderly patients

Use with caution in elderly patients.

special instructions

Use with caution in diabetes mellitus, COPD (including bronchial asthma, pulmonary emphysema), metabolic acidosis, hypoglycemia; history of allergic reactions, chronic heart failure (compensated), obliterating diseases of peripheral arteries (intermittent claudication, Raynaud's syndrome), pheochromocytoma, liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including a history of), psoriasis during pregnancy, in elderly patients, in pediatrics (efficacy and safety have not been determined).

With the use of atenolol, it is possible to reduce the production of tear fluid, which is important for patients using contact lenses.

Cancellation of atenolol after a long course of treatment should be carried out gradually under the supervision of a physician.

When the combined use of atenolol and clonidine is discontinued, clonidine treatment is continued for several more days after the abolition of atenolol, otherwise severe arterial hypertension may occur.

If it is necessary to carry out inhalation anesthesia in patients receiving atenolol, several days before anesthesia, it is necessary to stop taking atenolol or choose an anesthesia drug with a minimal negative inotropic effect.

Influence on the ability to drive vehicles and use mechanisms

In patients whose activities require increased concentration of attention, the question of the outpatient use of atenolol should be resolved only after evaluating the individual response.

Drug interactions

With the simultaneous use of diuretics, the antihypertensive effect is enhanced.

With the simultaneous use of drugs for inhalation anesthesia, the risk of increased cardiodepressive action and the development of arterial hypotension increases.

There are reports of the development of bradycardia and arterial hypotension with the simultaneous use of alcuronium chloride.

With the simultaneous use of verapamil, the negative inotropic effect increases, bradycardia, bradyarrhythmia, pronounced conduction disturbances develop; Cases of postural hypotension, dizziness, left ventricular failure, lethargy are described. Under the influence of verapamil, the pharmacokinetic parameters of atenolol do not change significantly, although a case of an increase in the AUC of atenolol has been described.

With the simultaneous use of disopyramide, Css increases, the clearance of disopyramide decreases, and conduction disturbance is possible.

With the simultaneous use of dipyridamole, a case of the development of bradycardia and then asystole (when conducting an ECG test with dipyridamole in a patient receiving atenolol) is described.

With the simultaneous use of indomethacin, naproxen and other NSAIDs, a decrease in the antihypertensive effect of atenolol is possible, which is to a certain extent due to a violation (under the influence of NSAIDs) of synthesis in the kidneys and the release of prostaglandins PGA and PGE into the bloodstream, which have a strong vasodilating effect on peripheral arterioles.

With the simultaneous use of insulin, an increase in blood pressure is possible.

With the simultaneous use of clonidine, an additive hypotensive effect, sedative effect, dry mouth are possible.

With the simultaneous use of caffeine, a decrease in the effectiveness of atenolol is possible.

With the simultaneous use of nizatidine, a case of increased cardiodepressive action has been described.

With the simultaneous use of nifedipine, cases of severe arterial hypotension and heart failure have been described, which may be due to an increase in the inhibitory effect of nifedipine on the myocardium.

With the simultaneous use of orlistat, the antihypertensive effect of atenolol decreases, which can lead to a significant increase in blood pressure, the development of a hypertensive crisis.

With the simultaneous use of prenylamine, an increase in the QT interval is possible.

With the simultaneous use of chlorthalidone, the antihypertensive effect is enhanced.