Atenolol, 25 mg 30 pcs

It has antianginal, antihypertensive and antiarrhythmic effects. It does not have membrane stabilizing and intrinsic sympathomimetic activity. Reduces catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces intracellular calcium ion current. During the first 24 h after oral administration against the background of decreased cardiac output, there is a reactive increase in total peripheral vascular resistance, which during 1-3 days gradually returns to the baseline, and then gradually decreases. Antihypertensive effect is associated with reduction of the blood minute volume, decrease of renin-angiotensin-aldosterone system activity, baroreceptor sensitivity and influence on the central nervous system. Antihypertensive effect is manifested by both reduction of systolic and diastolic blood pressure (BP), reduction of stroke and minute blood volume. In medium therapeutic doses, it has no effect on peripheral arterial tone. The antihypertensive effect lasts for 24 hours and with regular use is stabilized by the end of the second week of treatment. The antianginal effect is determined by a decrease in myocardial oxygen demand due to a decrease in heart rate (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as by a decrease in myocardial sensitivity to sympathetic stimulation. It reduces heart rate (HR) at rest and during exercise. By increasing left ventricular end-diastolic pressure and increasing ventricular muscle fiber stretch may increase oxygen demand, especially in patients with chronic heart failure. Antiarrhythmic action is manifested by suppression of sinus tachycardia and is associated with the elimination of arrhythmogenic sympathetic effects on the cardiac conduction system, reducing the rate of spread of excitation through the sinoatrial node and lengthening the refractory period. It suppresses conduction of impulses in antegrade and, to a lesser extent, in retrograde direction through AV (atrioventricular) node and along additional conduction pathways. The negative chronotropic effect appears 1 hour after intake, reaches its maximum after 2-4 hours and lasts up to 24 hours. It reduces the automatism of the sinus node, slows heart rate, slows AV conduction, reduces myocardial contractility, reduces myocardial oxygen demand. It reduces myocardial excitability. When used in medium therapeutic doses, it has less pronounced effect on bronchial smooth muscle and peripheral arteries than non-selective beta-adrenoblockers. It increases survival of patients who have had myocardial infarction (reduces the incidence of ventricular arrhythmias and angina attacks). Practically does not weaken the bronchodilator effect of isoprenaline. Unlike non-selective beta-adrenoblockers, when administered in medium therapeutic doses, it has less pronounced effect on the organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism. To a lesser extent, it has negative butmo-, chrono-, ino- and dromotropic effects. When used in high doses (more than 100 mg/day) has a blocking effect on both beta-adrenoreceptor subtypes.

Indications

Arterial hypertension; prevention of angina attacks (except for Prinzmetal angina); cardiac rhythm disorders: sinus tachycardia, prevention of supraventricular tachyarrhythmia, ventricular extrasystoles.

Active ingredient

Composition

Active ingredient: atenolol – 25.0 mg

How to take, the dosage

It is established individually. The usual dose for adults is oral, at the beginning of treatment is 25-50 mg once a day. If necessary, the dose is gradually increased. In patients with impaired renal function in patients with CKD 15-35 ml/min – 50 mg/day; in patients with CKD less than 15 ml/min – 50 mg every other day.

Maximum dose: Adults when taken orally – 200 mg/day in 1 or 2 doses.

Interaction

The antihypertensive effect increases with concomitant use of diuretics.

Concomitant use of agents for inhalation anesthesia increases the risk of increased cardiodepressant effect and development of arterial hypotension.

There have been reports of bradycardia and arterial hypotension when concomitant use of alcuronium chloride.

In concomitant use of verapamil the negative inotropic effect is increased, bradycardia, bradyarrhythmia, significant conduction disorders develop; cases of postural hypotension, dizziness, left ventricular failure, lethargy have been described. Atenolol does not significantly change pharmacokinetic parameters under the influence of verapamil, although there has been described a case of increasing AUC of atenolol.

The concomitant use of disopyramide increases Css, decreases disopyramide clearance, and may impair conduction.

Concomitant use of dipyridamole has described a case of bradycardia and then asystole (when performing an ECG test with dipyridamole in a patient receiving atenolol).

In concomitant use of indomethacin, naproxen and other NSAIDs may decrease the antihypertensive effect of atenolol to some degree due to the interference (under NSAID influence) with renal synthesis and release into bloodstream of prostaglandins PGA and PGE which have strong vasodilatory effect on peripheral arterioles.

The simultaneous use of insulin may increase BP.

Concomitant use of clonidine may cause additive hypotensive effect, sedation, dry mouth.

Concomitant use of caffeine may decrease the effectiveness of atenolol.

A case of increased cardiodepressant effect has been described with concomitant use of nizatidine.

In concomitant use of nifedipine there have been reports of significant arterial hypotension and heart failure, which may be due to increased suppressive effects of nifedipine on the myocardium.

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

Concomitant use of prenylamine may increase the QT interval.

The simultaneous use of chlorthalidone increases the antihypertensive effect.

Special Instructions

Caution should be used with diabetes mellitus, COPD (including Bronchial asthma, pulmonary emphysema), metabolic acidosis, hypoglycemia; allergic reactions in anamnesis, chronic heart failure (compensated), peripheral artery obliterating diseases (intermittent claudication, Raynaud’s syndrome), pheochromocytoma, liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including anamnesis), psoriasis, pregnancy and elderly.

The use of this drug in patients with chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including anamnesis), psoriasis, pregnancy, elderly patients, pediatrics (effectiveness and safety have not been determined).

The use of atenolol may decrease tear fluid production, which is important for patients who use contact lenses.

The withdrawal of atenolol after a prolonged course of treatment should be done gradually under a physician’s supervision.

If combined use of atenolol and clonidine is discontinued, treatment with clonidine continues for several more days after atenolol withdrawal, otherwise severe arterial hypertension may occur.

If patients receiving atenololol require inhalation anesthesia, atenololol should be discontinued or anesthesia product with minimal negative inotropic effects should be selected a few days before the anesthesia is performed.

Influence on driving and operating ability

In patients whose activities require increased concentration, outpatient use of atenolol should be decided only after evaluation of the individual response.

Contraindications

AV-blockade of II and III degree, sinoatrial block, CCSU, bradycardia, (heart rate less than 40 beats/min), arterial hypotension (in case of myocardial infarction, systolic BP less than 100 mm Hg.), cardiogenic shock, chronic heart failure stage IIB-III, acute heart failure, Prinzmetal angina, lactation, concomitant use of MAO inhibitors, hypersensitivity to atenololol.

Side effects

Cardiovascular system disorders:in some cases – bradycardia, arterial hypotension, AV conduction disorders, the appearance of symptoms of heart failure.

Digestive system disorders:In the beginning of therapy, nausea, constipation, diarrhea, dry mouth may occur.

Nervous system disorders:At the beginning of therapy, fatigue, dizziness, depression, mild headache, sleep disturbances, cold sensation and paresthesias in the extremities, decreased patient responsiveness, decreased tear fluid secretion, conjunctivitis may occur.

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

In the respiratory system:in predisposed patients – the appearance of symptoms of bronchial obstruction.

Allergic reactions:cutaneous itching.

Others:increased sweating, redness of the skin.

Overdose

Symptoms:explicit bradycardia, AV blockade of II-III degree, increasing symptoms of heart failure, excessive BP decrease, difficulty breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystoles, cyanosis of finger or palm nails, seizures.

Treatment:Gastric lavage and administration of adsorptive drugs; if bronchospasm occurs, inhalation or intravenous administration of the beta2-adrenomimetic salbutamol is indicated. In AV conduction disorders, bradycardia – intravenous injection of 1-2 mg of atropine, epinephrine or placement of a temporary pacemaker; in ventricular extrasystole – lidocaine (Class 1A drugs are not used); if BP decreases – the patient should be in Trendelenburg position. If there are no signs of pulmonary edema – IV plasma exchange solutions, if ineffective – injection of epinephrine, dopamine, dobutamine; in chronic heart failure – cardiac glycosides, diuretics, glucagon; in convulsions – IV diazepam. Dialysis is possible.

Similarities