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

Excipients: corn starch, crospovidone (polyplasdone XL or kollidone CL), magnesium carbonate heavy (MC 350), magnesium stearate, talc, microcrystalline cellulose.

Description:

Tablets are white or almost white, flat-cylindrical with a facet and a risk. Allowed a slight marbling.

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. Has antihypertensive, anti-anginal and antiarrhythmic effect.Blocking in low doses beta 1-adrenoreceptors of the heart, reduces the stimulated catecholamines the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo-, and inotropic effect (reduces heart rate (heart rate), inhibits conduction and excitability, reduces myocardial contractility).

The total peripheral vascular resistance at the beginning of beta-blockers (in the first 24 hours after oral administration) increases (as a result of the reciprocal increase in the activity of alpha-adrenoreceptors and removal of stimulation of beta2-adrenoreceptors), which returns to baseline after 1-3 days, long-term use is reduced.

The hypotensive effect is associated with a decrease in the minute volume of the blood, a decrease in the activity of the renin-angiotensin-aldosterone system (is of greater importance for patients with initial hypersecretion of renin), sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure (BP) influence on the central nervous system.The hypotensive effect is manifested by a decrease in both systolic and diastolic blood pressure, a decrease in the impact and minute volumes of blood. 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 the second week of treatment.

The antianginal effect is mediated by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (diastolic elongation and improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to sympathetic innervation. Atenolol urezhaet heart rate at rest and with physical exertion. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles can increase the need for oxygen, especially in patients with chronic heart failure.

Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing of atrioventricular conduction.Oppression of impulses is noted mainly in antegrade and to a lesser extent - in the retrograde direction through the atrioventricular node and along additional paths.

Increases the survival rate of patients who underwent myocardial infarction (reduces the incidence of ventricular arrhythmia and angina attacks).

Virtually does not weaken the bronchodilating effect of isoprenaline. In contrast to nonselective 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 used in large doses (more than 100 mg / day) has a blocking effect on both subtypes of beta adrenoreceptors.

Negative chronotropic effect occurs after 1 hour after administration, reaches a maximum after 2-4 hours and lasts up to 24 hours.

Pharmacokinetics:

Absorption of atenolol from the gastrointestinal tract - fast, incomplete (50-60%), bioavailability - 40-50%, solubility in fats is very low. The time to reach the maximum concentration is 2-4 hours. It penetrates badly through the blood-brain barrier, passes through the placental barrier and into breast milk. The connection with plasma proteins is 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 (a decrease in doses is necessary): when the creatinine clearance is less than 35 ml / min / 1.73 m2, the elimination half-life is 16-27 h; with SC below 15 ml / min. - more than 27 hours, with anuria - lengthened to 144 hours. It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

- prevention of angina attacks, except for Prinzmetal angina pectoris;

- cardiac arrhythmias: sinus tachycardia, prevention of supraventricular tachyarrhythmias, ventricular extrasystole.

Contraindications:

- Hypersensitivity to the drug,

- cardiogenic shock,

- atrioventricular block II-III degree,

- pronounced bradycardia (heart rate less than 40 / min),

- syndrome of weakness of the sinus node,

- Sinoatrial blockade,

- acute heart failure or decompensated chronic heart failure,

- cardiomegaly without signs of chronic heart failure,

- Prinzmetal angina,

- arterial hypotension (in case of use with myocardial infarction, systolic blood pressure less than 100 mm Hg),

- the period of lactation,

- simultaneous administration of monoamine oxidase inhibitors (MAO),

- age under 18 years (efficiency and safety not established).

Carefully:

Carefully is used for type 1 and type 2 diabetes, metabolic acidosis, hypoglycemia; allergic reactions in the anamnesis, chronic obstructive pulmonary disease (including bronchial asthma, pulmonary emphysema); with chronic heart failure (compensated), obliterating diseases of peripheral vessels ("intermittent" lameness, Raynaud's syndrome); with pheochromocytoma, hepatic insufficiency, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including in history), psoriasis, pregnancy; in elderly patients.

Pregnancy and lactation:

In pregnancy atenolol should be prescribed only in cases where the benefit to the mother exceeds the potential risk to the fetus. Atenolol excreted in breast milk, therefore during the period of breastfeeding the use of the drug is contraindicated.

Dosing and Administration:

Assign inside, before meals, do not chew, drink a small amount of liquid. The initial dose is 25-50 mg / day; if necessary, increase the dose after 1 week at 50 mg and then, if necessary, up to 200 mg, the average dose - 100 mg / day. The maximum daily dose is 200 mg. Dose reduction in the event of planned cancellation is carried out gradually, by 1/4 dose every 3-4 days.

Arterial hypertension

Treatment is started with 50 mg of the drug Atenolol 1 time per day. To achieve a stable antihypertensive effect, 1-2 weeks of admission is required. If the hypotensive effect is insufficient, the dose is increased to 100 mg per dose.

Angina pectoris

The initial dose is 50 mg per day. If the optimum therapeutic effect is not achieved within a week, the dose is increased to 100 mg per day. Older patients and patients with impaired renal excretory function need a correction of the dosing regimen.In the presence of renal insufficiency, dose adjustment according to QC. In patients with renal insufficiency with CC values above 35 ml / min / 1.73 m² (normal values are 100-150 ml / min / 1.73 m²) significant cumulation of the drug Atenolol not happening.

With tachysystolic heart rhythm disorders - 50 mg once a day.

The following maximum doses are recommended for patients with renal insufficiency:

Creatinine clearance (ml / min / 1,73 m²)	Half-life (h)	The maximum dose
15-35	16-27	50 mg per day 100 mg every other day
less than 15	more than 27	50 mg every other day 100 mg once every four days

Patients on hemodialysis, atenolol prescribe 25 or 50 mg / day immediately after each dialysis session, which must be done in a steady state, as there may be a drop in blood pressure.

In elderly patients, the initial single dose is 25 mg (can be increased under the control of blood pressure and heart rate).

An increase in the daily dose of more than 100 mg is not recommended, since the therapeutic effect is not increased, and the likelihood of side effects increases.

Side effects:

From the nervous system: asthenia, weakness, dizziness, headache, drowsiness or insomnia, nightmarish dreams, depression, anxiety, confusion, or short-term memory loss, hallucinations, decreased concentration, decreased reaction rate, paresthesia in the extremities (in patients with "intermittent "lameness and Raynaud's syndrome), myasthenia gravis, convulsions.

From the sense organs: impaired vision, decreased secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis.

From the side of the cardiovascular system: bradycardia, palpitations, impaired myocardial conductivity, atrioventricular blockade (up to cardiac arrest), arrhythmias, weakened myocardial contractility, development of chronic heart failure, orthostatic hypotension, manifestations of angiospasm (cooling of the lower extremities, Raynaud's syndrome), vasculitis, pain in the breasts.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, changes in taste.

From the respiratory system: nasal congestion,difficulty breathing when given in high doses (loss of selectivity) and / or in predisposed patients - laryngo- and bronchospasm.

From the endocrine system: hyperglycemia (in patients with type 2 diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status.

Allergic reactions: itching, rash, hives.

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

From the laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of "hepatic" enzymes, hyperbilirubinemia.

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

Other: pain in the back, arthralgia, weakening of libido, decreased potency, withdrawal syndrome (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 in blood pressure, syncope, fibrillation, arrhythmia, ventricular extrasystole, atrioventricular block II-III degree, chronic heart failure, cyanosis of the nails or palms, convulsions, difficulty breathing, bronchospasm.

Treatment: gastric lavage and administration of absorbent drugs; with violation of atrioventricular conduction and / or bradycardia - intravenous injection of 1-2 mg of atropine, epinephrine (epinephrine) or the setting of a temporary pacemaker; with ventricular extrasystole - lidocaine (preparations IA class do not apply); with a decrease in blood pressure - the patient should be in the Trendelenburg position. If there are no signs of pulmonary edema - intravenously plasma-substituting solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; with chronic heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - intravenously diazepam; with bronhospazme - inhalation or parenteral - beta-adrenostimulyatory. Dialysis is possible.

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 drugs for intravenous administration increases the risk of anaphylactic reactions.

Phenytoin with intravenous administration, drugs for inhalation of general anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

With simultaneous administration with insulin and oral hypoglycemic drugs atenolol masks the symptoms of developing hypoglycemia.

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

The hypotensive effect of atenolol weakens non-steroidal anti-inflammatory drugs (sodium ion delay and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (sodium ion delay).

Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of "slow" calcium: channels (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs with simultaneous use with atenolol increase the risk of developing or exacerbating the cardiacinsufficiency, bradycardia, atrioventricular blockade and cardiac arrest.

Diuretics, clonidine, sympatholytics, hydralazine, blockers of "slow" calcium channels and other antihypertensive drugs with simultaneous use with atenolol can lead to excessive reduction in blood pressure.

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

Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase the inhibition of the central nervous system.

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.

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

Special instructions:

Control of patients receiving 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 diabetic patients (1 time in 4-5 months).In elderly patients it is recommended to monitor the kidney function (1 time in 4-5 months).

You should teach the patient how to calculate heart rate and instruct you about the need for medical consultation at a heart rate of less than 50 / min.

Approximately in 20% of patients with angina pectoris beta-adrenoblockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 / min) and an increased end-diastolic volume of the left ventricle, which breaks the subendocardial blood flow. In "smokers" the effectiveness of beta-blockers 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, atenolol practically does not increase insulin-induced hypoglycemia and does not delay the recovery of glucose in the blood to normal concentration.

With simultaneous application with clonidine, its administration can be stopped only a few days after the atenolol withdrawal.

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

A few days before the general anesthesia with chloroform or ether, it is necessary to stop taking atenolol. If the patient has taken the drug before the operation, he should choose a medicine for general anesthesia with a minimum negative inotropic effect.

Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).

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 observation of the doctor for the detection of a marked decrease in blood pressure or bradycardia.

The drug can be prescribed to patients with bronchospastic diseases in the case of intolerance and / or ineffectiveness of other antihypertensive drugs, but it should be strictly monitored for dosage.Overdosing is dangerous by the development of bronchospasm.

In the case of an increased bradycardia (less than 50 / min), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of the 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.

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

Atenolol should be withdrawn before examining the blood and urine levels of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies (for 1 -2 days).

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets of 50 mg.

Packaging:

For 10 or 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

According to 1, 2, 3 contour cell packs of 10 tablets or 1, 2 contour cell packs of 30 tablets with instructions for use are placed in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark 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 N002774 / 01

Date of registration:10.09.2008 / 29.12.2009

Expiration Date:Unlimited

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)