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

Excipients: corn starch - 103.510 mg or 207.020 mg, medical gelatin - 0.486 mg or 0.972 mg, magnesium stearate - 5.182 mg or 10.364 mg, magnesium carbonate - 40.822 mg or 81.644 mg.

Description:Tablets are white or white with a creamy hue of a flat-cylindrical shape with a bevel (for a dosage of 50 mg) and with a facet and a risk (for a dosage of 100 mg). Allowed a slight marbling.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B.03 Atenolol

Pharmacodynamics:

Has antianginal, hypotensive and antiarrhythmic action.Does not possess membrane stabilizing and internal sympathomimetic activity. Reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular current of Ca ²+. In the first 24 hours after oral administration against the background of a decrease in cardiac output, there is a reactive increase in the total peripheral resistance of blood vessels, the severity of which decreases gradually over the course of 1-3 days.

The hypotensive effect is associated with a decrease in cardiac output, a decrease in the activity of the renin-angiotensin system, sensitivity of the baroreceptors, and effects on the central nervous system. Hypotensive effect is manifested by a decrease in systolic and diastolic blood pressure, decrease in shock and minute volumes. In average therapeutic doses, it has no effect on the tone of peripheral arteries. Hypotensive affect continues for 24 hours, with regular admission 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 at rest and during physical activity. By increasing the tension of the ventricular muscle fibers and the end diastolic pressure in the left ventricle, it can increase the myocardial oxygen demand, especially in patients with chronic heart failure.

Antiarrhythmic effect is manifested by suppression of sinus tachycardia and is associated with elimination of arrhythmogenic sympathetic influences on the conduction system of the heart, inhibition of heterogeneous automatism, decrease in the rate of propagation of excitation through the sinouauricular node, and prolongation of the refractory period. Oppresses impulses in antegrade and, to a lesser extent, retrograde directions through AV (atrioventricular) node and along additional pathways.

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

Slightly reduces the vital capacity of the lungs, almost does not weaken the bronchodilating effect of isoproterenol. In therapeutic concentrations does not affect the beta2-addressoreceptors,in contrast to nonselective beta-blockers, has a less pronounced effect on the smooth musculature of the bronchi and peripheral arteries and on lipid metabolism. When taking more than 100 mg per day may have a beta2-adrenergic blocking effect.

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

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (50%), solubility in fats is very poor, bioavailability is 40-50%, time to reach the maximum concentration in the blood plasma after ingestion is 2-4 hours.

Poorly penetrates the blood-brain barrier, passes in small amounts through the placental barrier and into breast milk. Connection with blood plasma proteins - 6-16%.

It is not metabolized in the liver. 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 prolonged half-life and cumulation: when creatinine clearance is less than 35 ml / min / 1.73 m², the half-life is 16-27 hours, with creatinine clearance below 15 ml / min - more than 27 hours (dose reduction is necessary). It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

- prevention of angina attacks: with the exception of Prinzmetal angina pectoris;

- violation of the heart rhythm: sinus tachycardia, prevention of supraventricular tachyarrhythmias; ventricular extrasystole, ventricular tachycardia.

Contraindications:

Hypersensitivity to the components of the drug, cardiogenic shock, atrioventricular block II-III st., severe bradycardia, sinus node weakness syndrome, sinoauric blockade, acute or chronic heart failure (decompensated stage), cardiomegaly without symptoms of heart failure, angina prinzmetal, arterial hypotension (in case of myocardial infarction, systolic blood pressure less than 100 mm Hg. ), pheochromocytoma (without simultaneous use of alpha-adrenoblockers), severe peripheral circulatory disorders, metabolic acidosis, severe forms of bronchial asthma and xr chronic obstructive pulmonary disease, lactation period, simultaneous administration of MAO inhibitors, age to 18 years (efficacy and safety not are defined).

Carefully:

Diabetes mellitus, hypoglycemia; allergic reactions in history, chronic obstructive pulmonary disease, emphysema, bronchospasm in history, atrioventricular blockade of degree 1, chronic heart failure, peripheral circulation disorders ("intermittent" lameness, Raynaud's syndrome); pheochromocytoma (with simultaneous use of alpha-blockers), chronic renal failure, hepatic insufficiency, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, surgical interventions, pregnancy, advanced age.

Pregnancy and lactation:Pregnant women should be prescribed Atenolol Only in cases where the benefit to the mother exceeds the potential risk to the fetus. Atenolol is excreted in breast milk, therefore during the period of feeding it should be taken only in exceptional cases with great caution.

Dosing and Administration:

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

Arterial hypertension. Treatment begins with taking 50 mg of 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.Further increase in the dose is not recommended, since it is not accompanied by an increase in the clinical effect.

Angina pectoris. The initial dose is 50 mg per day. If the optimum therapeutic effect is not achieved within a week, the dose to 100 mg per day is increased. Sometimes it is possible to increase the dose to 200 mg once a day. Older patients and patients with impaired renal excretory function need a correction of the dosing regimen. In the presence of renal failure, dose adjustment is recommended depending on the creatinine clearance. In patients with renal insufficiency at creatinine clearance values above 35 ml / min / 1.73 m² (normal values are 100-150 ml / min / 1.73 m²) significant cumulation of atenolol does not occur. The following maximum doses are recommended for patients with renal insufficiency:

Creatinine clearance ml / min / 1.73 m²	The half-life of Atenolol (h)	The maximum dose
10-30	16-27	50 mg per day or 100 mg every other day
Less than 10	More than 27	50 mg every other day or 100 mg every 4 days

Patients on hemodialysis, Atenolol appoint 50 mg / day immediately after each dialysis, which must be done in a hospital setting, because there may be a decrease in blood pressure.

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.

The maximum daily dose is 200 mg. Dose reduction in case of planned cancellation is performed at 25% dose every 3-4 days.

Side effects:

Occurring side effects are associated with the main pharmacological action of the drug and are expressed as follows:

- the cardiovascular system: development or aggravation of heart failure symptoms, atrioventricular conduction disorder, bradycardia, sinus node weakness syndrome, marked decrease in blood pressure, palpitations, peripheral circulation disorders (coldness of the lower extremities, intermittent claudication, Raynaud's syndrome), orthostatic hypotension;

- central nervous system: dizziness, sleep disturbance, decreased ability to concentrate, drowsiness, depression, hallucinations, headache, insomnia, nightmares, anxiety, confusion or short-term memory loss, weakened reactivity, paresthesia, convulsions;

- gastrointestinal tract: dryness of the oral mucosa, nausea, vomiting, diarrhea, abdominal pain, constipation, intrahepatic cholestasis;

- respiratory system: dyspnoea, bronchospasm;

- from the side of the hemostasis system: thrombocytopenia, leukopenia, agranulocytosis;

- endocrine system: gynecomastia, decreased potency, decreased libido, hyperglycemia (in patients with type 2 diabetes mellitus), hypoglycemia (in patients with type 1 diabetes mellitus and type 2 diabetes mellitus on insulin therapy), hypothyroidism;

- metabolic reactions: hyperlipidemia;

- skin reactions: urticaria, dermatitis, itching, photosensitivity, increased sweating, skin hyperemia, exacerbation of psoriasis, psoriasis-like skin rash, purpura, hypersensitivity reactions, including angioedema;

- Senses: impaired vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis;

- Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia;

- laboratory indicators: an increase in the activity of "hepatic" transaminases, bilirubin concentrations, an increase in the titer of antinuclear antibodies;

- other: withdrawal syndrome (increased angina attacks, increased blood pressure), reversible alopecia, muscle weakness, lethargy, fatigue.

Possible development of adverse events that occur with the use of other beta-blockers - a syndrome accompanied by pain in the throat, laryngospasm and respiratory failure; Mesenteric thrombosis, ischemic colitis, Peyronie's syndrome.

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

Overdose:

Symptoms: bradycardia, atrioventricular block II and III degree, the increase in symptoms of heart failure, a marked decrease in blood pressure, bronchospasm, hypoglycemia, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the fingernails or palms, convulsions.

Treatment: gastric lavage and administration of adsorptive agents; when bronchospasm occurs, inhalation or intravenous administration of beta2-adrenomimetic salbutamol is indicated. In violation of AV conduction, 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 arterial hypotension - the patient should be in Trendelenburg position. If there are no signs of pulmonary edema - intravenous plasmasubstitutional solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; with heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam. Dialysis is possible.

Interaction:

With simultaneous use of Atenolol with insulin, hypoglycemic means for ingestion - their hypoglycemic effect is enhanced.

When combined with hypotensive agents of different groups or nitrates, diuretics, sympatholytics, there is an intensification of the hypotensive effect.

Simultaneous use of Atenolol and verapamil (or diltiazem) can cause a mutual enhancement of cardiodepressive action.

The hypotensive effect is weakened by estrogens (sodium retention).

With the simultaneous use of Atenolol and cardiac glycosides, the risk of bradycardia and atrioventricular conduction disorders increases.

With the simultaneous administration of Atenolol with reserpine, methyldopa, clonidine,verapamil may cause severe bradycardia.

The simultaneous intravenous administration of verapamil and diltiazem is unacceptable. it can provoke heart failure. Simultaneous application with nifedipine may lead to a significant decrease in blood pressure.

With simultaneous use of Atenolol with derivatives of ergotamine, xanthine, non-steroidal anti-inflammatory drugs, its effectiveness decreases.

When the combined use of Atenolol and clonidine is discontinued, clonidine treatment is continued for several days after the withdrawal of Atenolol.

Simultaneous use with lidocaine can reduce its excretion and increase the risk of toxic effects of lidocaine.

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

Phenytoin with an intravenous injection of a general anesthetic enhances severity of cardiodepressive action.

When combined with euphyllin and theophylline, a mutual suppression of therapeutic effects.

It is not recommended simultaneous use with MAO inhibitors. 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.

Means for inhalation anesthesia (derivatives of hydrocarbons) increase the risk of oppression of myocardial function and development of arterial hypotension.

Amiodarone increases the risk of developing bradycardia and suppressing atrioventricular conduction.

Cimetidine increases the concentration in the blood plasma (inhibits metabolism).

Iodine-containing radiopaque substances for intravenous administration increase the risk of anaphylactic reactions.

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

Tri- and tetracyclic antidepressants, antipsychotic, sedative, hypnotics, barbiturates and ethanol increase the CNS depression.

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

Special instructions:

Monitoring 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 mellitus (1 every 4-5 months). In elderly patients it is recommended to follow the function of the kidneys (once every 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 beats per minute.

With thyrotoxicosis Atenolol can mask certain clinical signs of hyperthyroidism (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms. Unlike nonselective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.

In patients with coronary heart disease (CHD), the abrupt withdrawal of beta-blockers can cause an increase in the frequency or severity of anginal attacks, so the termination of Atenolol in patients with IHD is necessary to conduct gradually.

Particular attention also requires the selection of doses in patients with cardiac decompensation.In comparison with non-selective beta-blockers, cardioselective beta-blockers have less effect on lung function, however, in obstructive diseases of respiratory ways Atenolol should be assigned only in the case of absolute indications. If necessary, in some cases, the use of beta2-adrenomimetics can be recommended.

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

Particular attention is needed if surgical intervention under anesthesia is required in patients taking Atenolol. The drug should be discontinued 48 hours before surgery. As an anesthetic, the drug should be chosen with the possible minimum negative inotropic effect.

With simultaneous use of Atenolol and clonidine, the use of Atenolol stop for a few days before clonidine in order to avoid the withdrawal syndrome of the latter.

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

Drugs that reduce catecholamine stocks (for example, reserpine), can strengthen the action of beta-blockers, so patients who take such combinations of drugs should be under constant observation of the doctor for the diagnosis of arterial hypotension or bradycardia.

In the case of severe bradycardia (less than 50 bpm), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of the liver and kidney function in elderly patients, 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.

If necessary, the intravenous administration of verapamil, this should be done at least 48 hours after receiving Atenolol.

With the use of Atenolol may reduce the production of tear fluid, which is important for patients who use contact lenses.

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 is necessary to cancel the drug before examining the blood and urine content of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies.

In smokers, the effectiveness of beta-blockers is lower.

Effect on the ability to drive transp. cf. and fur:During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets of 50 and 100 mg.

Packaging:

10 tablets per contour cell pack. For 20, 30 or 50 tablets in cans of polymeric.

Each jar or 2, 3, 5 contour packs, together with instructions for use, are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children. Keep in original packaging.

Shelf life:2 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001653/07

Date of registration:18.07.2007

Expiration Date:Unlimited

The owner of the registration certificate:PHARMSTANDART-UFIM VITAMIN FACTORY, OJSC PHARMSTANDART-UFIM VITAMIN FACTORY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-UFIM VITAMIN FACTORY, OJSC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)