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

Excipients: magnesium hydroxycarbonate pentahydrate 46.1 mg or 92.2 mg, corn starch 97.7 mg or 195.4 mg, gelatin 1.2 mg or 2.4 mg, magnesium stearate 5 mg or 10 mg.

Description:Tablets of flat-cylindrical form with a facet on both sides (for a dosage of 50 mg) and with a facet on both sides and a risk on one side (for a dosage of 100 mg), from white to white with a creamy shade of color, slight marbling is allowed.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B.03 Atenolol

Pharmacodynamics:

Cardioselective beta1-adrenoblocker does not possess membrane-stabilizing and internal sympathomimetic activity. It has antihypertensive, anti-anginal and antiarrhythmic effects. Blocking in low doses beta1-adrenoreceptors of the heart, reduces the catecholamine-stimulated formation of cyclic adenosine monophosphate from adenosine triphosphate, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic action (reduces the heart rate, inhibits conduction and excitability, reduces contractility myocardium). The total peripheral vascular resistance at the beginning of beta1-blockers (in the first 24 hours after ingestion) increasesas a result of the reciprocal increase in the activity of alpha-adrenergic receptors and elimination of stimulation of beta2-adrenoreceptors), which is returned in 1-3 days to the initial, and with a long-term administration decreases. Antihypertensive effect is associated with a decrease in the minute volume of blood, a decrease in the activity of the renin-angiotensin-aldosterone system (is of great importance for patients with the 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 influence on the central nervous system. Antihypertensive effect is manifested by a decrease in both systolic and diastolic blood pressure (BP), a decrease in the shock and minute blood volume. In average therapeutic doses, it has no effect on the tone of peripheral arteries. Antihypertensive action lasts 24 hours, with regular admission is 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 (HR) at rest and during physical activity. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers, the ventricles can increase the demand for myocardium in oxygen, especially in patients with chronic heart failure.

Antiarrhythmic effect is caused by elimination of arrhythmogenic factors - (tachycardia, increased activity of the sympathetic nervous system, increased content of cyclic adenosine monophosphate, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing of atrioventricular (A) carrying out. The suppression of impulses is noted mainly in the antegrade and, to a lesser extent, retrograde direction through A node and by additional paths. Increases the survival rate of patients who underwent myocardial infarction (reduces the incidence of development ventricular arrhythmias and angina attacks). Virtually does not weaken the bronchodilating effect of isoprenaline.

Unlike non-selective beta-blockers, when administered at moderate therapeutic doses, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus), and carbohydrate metabolism; the severity of atherogenic action does not differ from that of propranolol.To a lesser extent, it has a negative batmo-, chrono-, ino-and dromotropic effect. When applied in high doses (over 100 mg / day) has a blocking effect on both beta-adrenoceptor subtype. The negative chronotropic effect appears after 1 h after oral administration, reaching a maximum after 24 hours and continued to 24 hours.

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (50-60%) bioavailability - 40-50%, fat solubility is very low. Time to reach the maximum concentration in blood plasma - 2 - 4 hours.

Poorly penetrates the blood-brain barrier, passes 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 % in unmodified form). Impaired renal function is accompanied by an elongation of the half-life and cumulation (a reduction in the dose is necessary): with clearance creatinine below 35 ml / min / 1.73 m2 elimination half-life is 16-27 hours, with creatinine clearance below 15 ml / min - more than 27 hours, with anuria lengthened to 144 hours. It is outputted to the hemodialysis input.

Indications:

Arterial hypertension.

Prevention of attacks of stable angina, with the exception of Prinzmetal angina pectoris.

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

Contraindications:Increased sensitivity to the components of the drug and other beta-blockers, cardiogenic shock, atrioventricular block II-III bradycardia with a heart rate of less than 45 beats / min, syndrome of weakness of the sinus node, sinoauric blockade, acute heart failure or decompensated chronic heart failure, cardiomegaly without symptoms of chronic heart failure, angina prinzmetala, arterial hypotension (in case of myocardial infarction, systolic blood pressure less than 100 mm Hg), simultaneous, administration of monoamine oxidase inhibitors (MAO); lactation period, age under 18 years (effectiveness and safety not established); pheochromocytoma without simultaneous use of alpha-blockers, severe peripheral circulatory disorders, severe bronchial asthma, severe liver dysfunction.

Carefully:Diabetes mellitus, metabolic acidosis, hypoglycemia; allergic reactions in history, chronic obstructive pulmonary disease, bronchial asthma, emphysema light; chronic heart failure (compensated), obliterating peripheral vascular diseases ("intermittent" lameness, Raynaud's syndrome); pheochromocytoma with simultaneous use of alpha-adrenoblockers, hepatic insufficiency, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including in history), psoriasis, pregnancy, elderly age.

Pregnancy and lactation:

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

The drug is contraindicated during breastfeeding, so if you need to take the drug, breastfeeding should be discontinued.

Dosing and Administration:

Inside, before eating, without chewing, squeezed a small amount of liquid.

Arterial hypertension: the initial dose is 50 mg once a day. If the antihypertensive effect is insufficient, the dose is raised to 100 mg / day. Further increase in dose is not recommended. it is not accompanied by amplification clinical effect.

Angina pectoris: the initial dose is 50 mg / day. If the optimum therapeutic effect is not achieved within 1 week, the dose is increased to 100 mg / day.

Older patients and concomitant chronic renal insufficiency need a correction of the dosing regimen depending on the creatinine clearance: in the case of creatinine clearance of 15-35 ml / min, 50 mg once a day or 100 mg every other day; when creatinine clearance is less than 15 ml / min - 50 mg every other day or 100 mg once every 4 days. Patients who are on hemodialysis - 25 or 50 mg / day immediately after each session of hemodialysis. To obtain a dose of 25 mg, you must take ½ tablets of 50 mg.

With tachysystolic heart disorders rhythm - 50 mg once a day, if necessary and good tolerability, the dose may be increased within a week to 100-200 mg / day.

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:

Most of the side effects associated with the use of atenolol are weakly expressed and transient.

The most common adverse events are associated mainly with pharmacological action of the drug and are expressed as follows:

From the side of the cardiovascular system: bradycardia, palpitations, atrioventricular block (up to cardiac arrest), arrhythmias, weakening myocardial contractility (conduction of the heart), development (aggravation) chronic heart failure, orthostatic hypotension, manifestations angiospasm (coldness of the lower extremities, Raynaud's syndrome), vasculitis, chest pain.

From the central nervous system: asthenia, weakness, dizziness, headache pain, drowsiness or insomnia, "nightmarish" dreams, depression, anxiety, confusion, consciousness or short-term memory loss, hallucinations, decreased ability to concentrate, decreased reaction speed, paresthesia of limbs (in patients with "intermittent" lameness and Reynaud's syndrome); muscle weakness, convulsions.

From the sense organs: impaired vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis, changes in taste.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, cholestasis, jaundice.

From the respiratory system: nasal congestion, dyspnea, laryngo- and bronchospasm, thrombocytopenic purpura.

From the endocrine system: Hyperglycemia (in patients with type 2 diabetes), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions: skin itching, rash, hives, angioedema.

From the skin: increased sweating, skin hyperemia, exacerbation of psoriasis symptoms, psoriasis-like skin rash, reversible alopecia.

Laboratory indicators: thrombocytopenia, (unusual bleeding and hemorrhages), agranulocytosis, leukopenia, increased activity of "hepatic" transaminases, hyperbilirubinemia, positive test results for antinuclear antibodies.

Other: pain in the back, arthralgia, weakening of libido, decreased potency, syndrome "cancellation" (increased angina attacks, increased blood pressure).

The frequency of side effects increases with an increase in the dose of the drug.

Overdose:

Symptoms: severe bradycardia, dizziness, excessive decrease arterial pressure, fainting, arrhythmia, ventricular extrasystole, AV blockade II-III, degree, aggravation of symptoms chronic heart failure, cyanosis of the fingernails or palms, convulsions, difficulty breathing (loss of selectivity), bronchospasm.

Treatment: gastric lavage and the use of adsorptive drugs; in violation of AV conduction and / or bradycardia - intravenous injection of 1-2 mg, 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 patient must be translated in the Trendelenburg position. If there are no signs of pulmonary edema - intravenous plasmasubstitutional solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; with chronic heart failure cardiac glycosides, diuretics; with convulsions - in / in diazepam; at bronhospazme - beta-adrenostimulyatory (inhalation or parenteral). Hemodialysis is effective.

Interaction:

Allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving Atenolol. Iodine-containing radiopaque funds for in / in the introduction increase the risk of anaphylactic reactions.

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

When used simultaneously with insulin and hypoglycemic agents for oral administration, masks the symptoms of developing hypoglycemia.

Reduces clearance of lidocaine and xanthines and increases their concentration in blood plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

Antihypertensive effects weaken non-steroidal anti-inflammatory drugs (sodium retention and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (sodium retention).

Cardiac glycosides, methyldopa, clonidine, reserpine and guanfacine, blockers of "slow" calcium channels (verapamil, diltiazem), amiodarone intensify the negative chrono-, dromo- and batmotropic effect.

Diuretics, clonidine, sympatholytics, hydralazine, blockers of "slow" calcium channels, etc. antihypertensive drugs can lead to excessive blood pressure lowering.With the simultaneous use of Atenolol and clonidine, the use of Atenolol is stopped for several days before clonidine in order to avoid the symptom of the withdrawal of the latter. Lengthens the effect of nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

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

It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive action, a break in treatment between taking MAO inhibitors and Atenolol should be at least 14 days.

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

Beta-sympathomimetics weaken the antihypertensive effect.

Alpha-adrenoblockers increase the antihypertensive effect of Atenolol.

Antiarrhythmic drugs of the first class intensify cardiodepressive action (the risk of bradycardia, arrhythmia, hypotension, heart failure increases).

Special instructions:

Control of patients receiving Atenolol, should include monitoring the heart rate (heart rate) and blood pressure (at the beginning of treatment - every day, then every 3 to 4 months), the concentration of blood glucose in diabetic patients (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 a heart rate of less than 50 beats per minute.

Approximately 20% of patients with angina pectoris Atenolol Ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min) and an increased end-diastolic volume of the left ventricle, which breaks the subendocardial blood flow. In "smokers" the effectiveness of Atenolol is lower.

Patients who use contact lenses should take into account that, on the background of treatment, tear fluid production can be reduced.

With thyrotoxicosis Atenolol can mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms. In diabetes mellitus can mask tachycardia caused by hypoglycemia.In contrast to non-selective beta-blockers, there is almost no increase in insulin-induced hypoglycemia and does not delay the restoration of glucose concentration in the blood to normal concentration.

It is possible to increase the severity of the allergic reaction and the lack of effect from the usual doses of epinephrine against the background of a burdened allergological anamnesis.

In several days Before conducting a general anesthesia with chloroform or ether, it is necessary to stop taking Atenolol. If the patient has taken the drug before surgery, he should choose the means for general anesthesia with minimum negative inotropic action.

Reciprocal activation of the vagus nerve can be eliminated with / in the introduction atropine (1-2 mg). Means that reduce catecholamine stocks (for example, reserpine), can strengthen the action Atenolola, therefore, patients taking such combinations of funds should be under the constant supervision of a doctor for the detection of a pronounced decrease in blood pressure or bradycardia. Atenolol can be prescribed to patients with bronchospastic diseases in the case of intolerance and / or ineffectiveness of other antihypertensive drugs, but at the same time strictly follow the dosage. Overdosing is dangerous by the development of bronchospasm. Increased bradycardia occurs in elderly patients (less 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Pg.), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe disorders liver function 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 taking Atenolol. Do not abruptly interrupt treatment because of the risk of developing severe arrhythmias and heart attacks myocardium. Abolition is carried out gradually, reducing the dose for 2 weeks or more (reduce a dose of 25% v-4 days). It should be canceled before the study of concentrations in the blood and urine of catecholamines, normetanephrine and vanillylmandelic acid, antinuclear antibody titers for 1-2 days before the study.

Effect on the ability to drive transp. cf. and fur:During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 50 and 100 mg.

Packaging:

For 10 (for a dosage of 100 mg) or 20 (for a dosage of 50 mg) tablets in a contour mesh box made of a polyvinylchloride film and aluminum foil.

For 30 or 50 (for dosage of 50 mg) tablets in cans of polymer material. A bank or 3 contour packs of 10 tablets or 2 contour packs of 20 tablets together with instructions for use are placed in a pack of cardboard for consumer containers.

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:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001152 / 01

Date of registration:19.05.2011

Expiration Date:Unlimited

The owner of the registration certificate:MARBIOFARM, OJSC MARBIOFARM, OJSC Russia

Manufacturer: & nbsp

MARBIOFARM, OJSC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)