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

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 catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic action (urezhaet heart rate (heart rate), inhibits conduction and excitability, reduces myocardial contractility). The total peripheral resistance of the vessels at the beginning of beta-blockers (in the first 24 hours after ingestion) increases (as a result of the reciprocal increase in the activity of alpha-adrenergic receptors and elimination of stimulation of beta2-adrenoreceptors), which returns to the initial one after 1-3 days, the appointment is reduced. Antihypertensive action associated with a decrease in cardiac output (IOC), the decrease in activity of the renin-angiotensin-aldosterone system (higher for patients with initial hypersecretion renin) baroreceptor sensitivity of the aortic arch (not going to increase their activity in response to a decrease in blood pressure (BP ) and influence on the central nervous system (CNS).Antihypertensive effect is manifested by a decrease in both systolic and diastolic blood pressure, a decrease in the shock volume of blood and IOC.

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 decrease in myocardial oxygen demand as a result of a decrease in 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 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 of the heart can increase the demand for myocardium in oxygen, especially in patients with chronic heart failure (CHF). 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 (AV) carrying out. The suppression of impulses is noted predominantly in the antegrade and, to a lesser extent, retrograde direction through AV node and by additional paths. Practically not weakens the bronchodilating effect of isoprenaline. In contrast to nonselective beta-blockers, when administered at medium therapeutic doses, it has a less pronounced effect on organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus), and carbohydrate metabolism. To a lesser extent, negative batmono-, chrono-, ino- and dromotropic action. When used in large doses (more than 100 mg / day) has a blocking effect on both subtypes of beta adrenoreceptors. Negative chronotropic effect is manifested 1 hour after admission, reaches a maximum after 2-4 hours and lasts up to 24 hours.

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (50-60%), bioavailability - 40-50%, solubility in fats is very low. Time to reach the maximum concentration (TCmah) in the blood plasma after ingestion - 2-4 hours.Poorly penetrates the blood-encephalic barrier, passes through the placental barrier and into breast milk. Connection with blood plasma proteins - 6-16%.

It is not metabolized in the liver. Half-life (T_1/2) - 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 lengthening T_1/2 and cumulation: with clearance of creatinine (CC) below 35 ml / min / 1.73 m² the half-life is 16-27 hours, with QC below 15 ml / min / 1.73 m² - more than 27 hours (reduction of doses is necessary), with anuria prolonged to 144 hours. It is displayed during the procedure of hemodialysis.

Indications:

- Arterial hypertension;

- prevention of attacks of stable angina (except Prinzmetal angina pectoris);

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

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, AV blockade of II-III degree, expressed bradycardia with heart rate less than 50 beats per minute, sinus node weakness syndrome, sinoatrial block, acute and chronic heart failure in the stage of decompensation, cardiomegaly without signs of CHF, angina Prinzmetal,arterial hypotension (in case of use with myocardial infarction, systolic blood pressure less than 100 mm Hg), simultaneous administration of monoamine oxidase (MAO) inhibitors, pheochromocytoma (without simultaneous use of alpha-blockers), age to 18 years (efficacy and safety not established), lactation period.

Carefully:

Diabetes mellitus, metabolic acidosis, hypoglycemia; weighed allergic anamnesis; chronic obstructive pulmonary disease, bronchial asthma, emphysema; CHF, obliterating diseases of peripheral vessels ("intermittent" lameness, Raynaud's syndrome); atrioventricular blockade of the 1st degree; pheochromocytoma (with simultaneous use of alpha-blockers), liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including in history), psoriasis, pregnancy, advanced age.

Pregnancy and lactation:

In pregnancy atenolol should be used 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:

Inside, before eating, without chewing and washing down with a small amount of liquid, treatment starts with a dose of 50 mg once a day.

When arterial hypertension treatment is started with 50 mg once a day. To achieve a stable antihypertensive effect, it takes 1-2 weeks to take. If the antihypertensive effect is insufficient, the dose is increased to 100 mg (2 tablets) in one dose. Further increase in the dose is not recommended, since it is not accompanied by an increase in the clinical effect.

For prevention of attacks of stable angina the initial dose is 50 mg per day. If within a week the optimal therapeutic effect is not achieved, increase the dose to 100 mg per day. Older patients and patients with impaired renal function need to adjust the dosage regimen. In the presence of renal failure, dose adjustment is recommended depending on the creatinine clearance. In patients with renal insufficiency with values of creatinine clearance above 35 ml / min / 1.73 m² (normal values are 100-150 ml / min / 1.73 m²) significant cumulation does not occur.

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

Creatinine clearance (ml / min / 1.73 m²)	The half-life of Atenolol (h)	The maximum dose
15-35	16-27	50 mg per day or 100 mg every other day
less than 15	more than 27	50 mg every other day or 100 mg every 4 days

Patients who are on hemodialysis are prescribed 50 mg / day immediately after each hemodialysis session, which must be done in a hospital setting, since there may be a decrease in blood pressure.

When heart rhythm disturbance treatment is started with 50 mg once a day. After establishing control over the violation of the rhythm of the heart pass to a maintenance dose of 50-100 mg per day.

The maximum daily dose is 100 mg. Dose reduction in the event of planned cancellation is gradual, reduce the dose by 25% every 3-4 days.

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 speed, paresthesia in the extremities (in patients with "intermittent "lameness and Raynaud's syndrome), convulsions.

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

From the cardiovascular system: bradycardia, palpitation, conduction disturbance of the myocardium, AV blockade (up to cardiac arrest), arrhythmias, weakening of myocardial contractility, development (aggravation) of chronic heart failure, orthostatic hypotension, manifestations of angiospasm (cooling of the lower extremities, Raynaud's syndrome), vasculitis, chest pain.

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

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 with type 1 diabetes), hypothyroid status (decreased thyroid function).

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

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

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

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

Other: pain in the back, arthralgia, weakening of libido, myasthenia gravis, gynecomastia, 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, AV blockade of the I-III degree, CHF, cyanosis of the fingernails or palms of the hands, convulsions, difficulty breathing, bronchospasm.

Treatment: gastric lavage and administration of adsorptive drugs; in violation of AV conduction and / or bradycardia - intravenous injection of 1-2 mg of 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 - the patient should be in the Trendelenburg position. If there are no signs of pulmonary edema - intravenous plasmo-replacing solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; at CHF - cardiac glycosides, diuretics; with convulsions - intravenous 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 increase 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 a simultaneous appointment with insulin and hypoglycemic medications for oral administration, the hypoglycemic effect of the latter is enhanced.

Reduces the 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 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 (BCC) (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or aggravating the course of chronic heart failure, bradycardia, AV blockade and cardiac arrest.

Diuretics, clonidine, sympatholytics, hydralazine, BCCC and other antihypertensive drugs may lead to excessive blood pressure lowering. 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 CNS depression.

It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive action, a break in the 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 - every day, then once in 3-4 months), the concentration of glucose in the blood in patients with diabetes (1 time in 4-5 months). In elderly patients it is recommended to monitor the kidney function (1 time in 4-5 months).

It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at heart rate less than 50 beats per minute.

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 beats / 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 a reduction in tear fluid production is possible against the background of treatment.

When using Atenolol in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (unless an effective alpha-adrenoblockade is previously achieved).

With thyrotoxicosis Atenolol can mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.

With diabetes mellitus Atenolol can mask tachycardia caused by hypoglycemia. In contrast to nonselective beta-blockers, it does not substantially increase insulin-induced hypoglycemia and does not delay the recovery of glucose in the blood to normal concentrations.

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 withdrawal of the latter. 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.

A few days before the general anesthesia should stop taking the drug. If the patient has taken the drug before surgery, he should choose a drug 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 the supply of catecholamines (for example, reserpine), can enhance the action of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a marked decrease in blood pressure or bradycardia.

If intravenous verapamil is needed, it should be done at least 48 hours after taking Atenolol.

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

In the case of elderly patients with an increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mmHg) AV blockade, bronchospasm, ventricular arrhythmias, severe impairment of liver and kidney function, it is necessary to reduce the dose or stop treatment.

In patients with coronary heart disease (CHD), the abrupt cancellation of beta-blockers can cause an increase in the frequency or severity of anginal attacks, so stopping the use of Atenolol in patients with IHD should be gradual.

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). It should be abolished before the study of blood and urine levels of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies 1-2 days before the test.

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

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

Form release / dosage:

Tablets of 50 mg.

Packaging:For 10 tablets in a contour mesh package, for 3 or 5 contour squares, along with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Store in inaccessible to children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-001422

Date of registration:29.07.2011

Expiration Date:Unlimited

The owner of the registration certificate:FARMPROJECT, CJSC FARMPROJECT, CJSC Russia

Manufacturer: & nbsp

FARMPROJECT, CJSC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)