Atenolol Renewal pills 100mg, 30pcs

Composition

1 tablet contains: Active ingredient: atenolol-0.1 gh auxiliary substances: magnesium hydroxycarbonate-0.08 g-0.16 g potato starch-0.059 g-0.118 g gelatin – 0.009 g – 0.018 g Magnesium stearate – 0.001 g-0.002 g stearic acid – 0.001 g-0.002

Pharmacological action

It has antianginal, antihypertensive and antiarrhythmic effects. It has no membrane-stabilizing and internal sympathomimetic activity. Reduces catecholamine-stimulated cAMP formation from ATP.

In the first 24 hours after oral use, against the background of a decrease in cardiac output, a reactive increase in total peripheral vascular resistance is noted, the severity of which gradually decreases over 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 baroreceptors, and an effect on the central nervous system. The hypotensive effect is manifested by both a decrease in systolic and diastolic blood pressure (BP), a decrease in stroke and minute volumes.

In medium therapeutic doses, it does not affect the tone of peripheral arteries. The antihypertensive effect lasts 24 hours, with regular use it stabilizes by the end of the second week of treatment.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic stimulation. Reduces the heart rate (HR) at rest and during exercise.

By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it 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 influences on the cardiac conduction system, a decrease in the rate of propagation of excitation through the sinoatrial node, and an extension of the refractory period.

It inhibits the conduction of impulses in the antegrade and, to a lesser extent, in the retrograde directions through the AV (atrioventricular) node and along additional pathways.

The negative chronotropic effect manifests itself 1 hour after use, reaches a maximum after 2-4 hours, and lasts up to 24 hours.

Reduces the automatism of the sinus node, reduces heart rate, slows AV conduction, reduces myocardial contractility, reduces the need for myocardial oxygen. Reduces the excitability of the myocardium. When used in medium therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.

Pharmacokinetics

Absorption from the gastrointestinal tract is rapid, incomplete (50-60%), bioavailability is 40-50%, and the time to reach the maximum concentration in blood plasma is 2-4 hours. Poorly penetrates the blood-brain barrier, passes in small amounts through the placental barrier and into breast milk. Binding to plasma proteins is 6-16%. It is practically not metabolized in the liver. The elimination half-life is 6-9 hours (increases in elderly patients). It is excreted by the kidneys by glomerular filtration (85-100% unchanged). Impaired renal function is accompanied by prolongation of the elimination half-life and accumulation: with creatinine clearance below 35 ml / min/1.73 m2, the elimination half-life is 16-27 hours, with creatinine clearance below 15 ml / min/1.73 m2-more than 27 hours (dose reduction is necessary). It is removed during hemodialysis.

Indications

-Arterial hypertension;

– prevention of angina attacks (with the exception of Prinzmetal angina)

— – heart rhythm disorders: sinus tachycardia, prevention of supraventricular tachyarrhythmia, ventricular extrasystole.

Contraindications

— Cardiogenic shock;

— the atrioventricular (AV) blockade II-III degree;

— severe bradycardia (heart rate less than 40 beats/min);

— syndrome of weakness of the sinus node;

— sinoauricular blockade;

— acute or chronic heart failure in the stage of decompensation;

— cardiomegaly without signs of heart failure;

— Prinzmetal’s angina;

— arterial hypotension (in case of use in myocardial infarction;

— systolic blood pressure less than 100 mm Hg. St. )

— lactation period;

— simultaneous use of monoamine oxidase inhibitors (MAOIS);

— age under 18 years ( effectiveness and safety of the drug has not been established);

— hypersensitivity to the drug.

With caution:  diabetes mellitus, metabolic acidosis, hypoglycemia, a history of allergic reactions, chronic obstructive pulmonary disease (including emphysema), grade I AV block, chronic heart failure (compensated), obliterating peripheral vascular diseases (intermittent claudication, Raynaud’s syndrome), pheochromocytoma, liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including a history), psoriasis, old age, pregnancy.

Side effects

Cardiovascular system:  development (aggravation) of symptoms of chronic heart failure (swelling of the ankles, feet, shortness of breath), atrioventricular conduction disorders, arrhythmias, bradycardia, marked decrease in blood pressure, palpitation, weakening of myocardial contractility, orthostatic hypotension, manifestations of angiospasm (cold of the lower extremities, Raynaud’s syndrome), vasculitis, chest pain.

Central Nervous System:  dizziness, decreased ability to concentrate, decreased reaction speed, drowsiness or insomnia, depression, hallucinations, increased fatigue, headache, weakness, ” nightmarish “dreams, anxiety, confusion or short-term memory loss, paresthesia in the extremities (in patients with” intermittent ” claudication and Raynaud’s syndrome), muscle weakness, convulsions.

GASTROINTESTINAL TRACT:  dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation or diarrhea, change in taste.

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

Hematological reactions:  platelet purpura, anemia (aplastic), thrombosis.

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

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

Sensory organs:  visual impairment, decreased lacrimal fluid secretion, dry and painful eyes, conjunctivitis.

Effect on the fetus:  intrauterine growth retardation, hypoglycemia, bradycardia. Laboratory parameters: agranulocytosis, leukopenia, increased activity of “liver” enzymes, hyperbilirubinemia, thrombocytopenia (unusual bleeding and hemorrhage).

Other services:  back pain, arthraplasia, withdrawal symptoms (tachycardia, increased angina attacks, increased blood pressure, etc. ).

The frequency of side effects increases with increasing dose of the drug.

Interaction

With simultaneous use of atenolol with insulin, hypoglycemic agents for oral use-their hypoglycemic effect is enhanced. When combined with antihypertensive agents of different groups or nitrates, the hypotensive effect increases. Concomitant use of atenolol and verapamil (or diltiazem) may cause a mutual increase in the cardiodepressive effect.

The hypotensive effect is weakened by estrogens (sodium retention) and nonsteroidal anti-inflammatory drugs, glucocorticosteroids. Concomitant use of atenolol and cardiac glycosides increases the risk of developing bradycardia and impaired atrioventricular conduction.

When atenolol is co-administered with reserpine, methyldopa, clonidine, verapamil, severe bradycardia may occur.

Simultaneous intravenous use of verapamil and diltiazem can cause cardiac arrest; nifedipine can lead to a significant decrease in blood pressure. With simultaneous use of atenolol with derivatives of ergotamine, xanthine, its effectiveness decreases.

If the combined use of atenolol and clonidine is discontinued, treatment with clonidine is continued for several days after atenolol is discontinued.

Concomitant use with lidocaine may reduce its excretion and increase the risk of lidocaine toxicity.

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

Phenytoin with intravenous use, drugs for general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure.

When combined with eufillin and theophylline, mutual suppression of therapeutic effects is possible.

Concomitant use with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect, a break in treatment between taking 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.

Inhaled anesthesia products (hydrocarbon derivatives) increase the risk of myocardial function suppression and the development of arterial hypertension.Amiodarone increases the risk of developing bradycardia and inhibition of AV conduction. Cimetidine increases the concentration in the blood plasma (inhibits metabolism). Iodine-containing radiopaque agents for intravenous use increase the risk of anaphylactic reactions.

It prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri-and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives, and sleeping pills increase central nervous system depression.

Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

How to take, course of use and dosage

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

Arterial hypertension. Treatment begins with 50 mg of atenolol once a day. To achieve a stable antihypertensive effect,1-2 weeks of use are required. If the hypotensive effect is not sufficiently pronounced, the dose is increased to 100 mg in one dose. A further increase in the dose is not recommended, as it is not accompanied by an increase in the clinical effect.

For ischemic heart disease, tachysystolic heart rhythm disorders-50 mg 1 time a day.

Angina pectoris. The initial dose is 50 mg per day. If the optimal therapeutic effect is not achieved within a week, increase the dose to 100 mg per day.

Elderly patients and patients with impaired excretory function of the kidneys need to adjust the dosage regimen.

In the presence of renal insufficiency, dose adjustment is recommended depending on creatinine clearance. In patients with renal insufficiency with creatinine clearance values above 35 ml / min/1.73 m2 (normal values are 100-150 ml / min/1.73 m2), significant accumulation of atenolol does not occur.

Overdose

Symptoms: severe bradycardia, grade II-III AV block, increased symptoms of heart failure, excessive decrease in blood pressure, difficulty breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the fingernails or palms, convulsions.

Treatment: gastric lavage and use of adsorbent drugs; if bronchospasm occurs, inhaled or intravenous use of the beta-2-adrenomimetic salbutamol is indicated.

In case of violation of AV conduction, bradycardia-intravenous use of 1-2 mg of atropine, epinephrine or a temporary pacemaker; in case of ventricular extrasystole-lidocaine (Class 1 A drugs are not used); with a decrease in blood pressure-the patient should be in the Trendelenburg position.

If there are no signs of pulmonary edema-intravenous plasma-substituting solutions, if ineffective-use of epinephrine, dopamine, dobutamine; in chronic heart failure-cardiac glycosides, diuretics, glucagon; in convulsions-intravenous diazepam. Dialysis is possible.

Special instructions

Monitoring of patients taking 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 patients with diabetes mellitus (1 time in 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months).

The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min. In thyrotoxicosis, atenolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration 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 discontinuation of atenolol in patients with CHD should be carried out gradually.

Compared to non-selective beta-blockers, cardioselective beta-blockers have a lower impact on lung function, however, in obstructive airway diseases, atenolol is prescribed only in the case of absolute indications. If necessary, their appointment in some cases, you can recommend the use of beta-2-adrenomimetics.

Patients with bronchospastic diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but the dosage should be strictly monitored. Overdose is dangerous for the development of bronchospasm.

Special attention should be paid in cases where surgical intervention is required under anesthesia in patients taking atenolol. The drug should be discontinued 48 hours before the intervention. As an anesthetic, you should choose a drug with the minimum possible negative inotropic effect.

With simultaneous use of atenolol and clonidine, atenolol is stopped several days earlier than clonidine in order to avoid the withdrawal symptom of the latter. It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from conventional doses of epinephrine against the background of a burdened allergic history.

Medications that reduce the supply of catecholamines (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of medications should be constantly monitored by a doctor for a pronounced decrease in blood pressure or bradycardia.

If elderly patients develop increasing bradycardia (less than 50 beats/min), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver and kidney function disorders, the dose should be reduced or treatment should be discontinued.

It is recommended to stop therapy if you develop depression caused by taking beta-blockers.

If intravenous use of verapamil is necessary, this should be done at least 48 hours after taking atenolol.

When using atenolol, it is possible to reduce the production of tear fluid, which is important in patients using contact lenses.

Do not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Withdrawal is carried out gradually, reducing the dose over 2 weeks. and more (reduce the dose by 25% in 3-4 days).

It should be canceled before testing the content of catecholamines, normetanephrine and vanillylmindalic acid in the blood and urine; titers of antinuclear shg antibodies. In smokers, the effectiveness of beta-blockers is lower. Pregnancy and lactation.

Pregnant women should be prescribed atenolol only when the benefit to the mother outweighs the potential risk to the fetus. Atenolol is excreted in breast milk, so if the drug is indicated during lactation, it is better to stop breastfeeding for a while.

Influence on the ability to drive motor vehicles and manage mechanisms

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Active ingredient

Atenolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, for pregnant women as prescribed by a doctor

Indications

Angina, Arrhythmia, Hypertension