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

Composition:One tablet of 50 mg or 100 mg active substance atenolol, and Excipients: magnesium carbonate basic, corn starch or potato or sodium starch glycollate, gelatin medical, magnesium stearic acid, microcrystalline cellulose, polyvinylpyrrolidone, lactose.

Description:

Tablets are white or white with a creamy shade of color, flat-cylindrical with a bevel. Presence of marble is admissible.

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 Ca²⁺. 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, the sensitivity of the baroreceptors, and effects on the central nervous system. The hypotensive effect is manifested as a decrease in systolic and diastolic blood pressure, a decrease in the impact and minute volumes. 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 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 (diastole lengthening and improvement of myocardial perfusion) and contractility,as well as a decrease in the sensitivity of the myocardium to the effects of sympathetic innervation. It reduces the heart rate at rest and during physical activity. By increasing the tension of the ventricular muscle fibers and the final diastolic pressure in the left ventricle, it can raise the 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 sinoaricular node, and lengthening of the refractory period. Oppresses impulses in antegrade and, to a lesser extent, retrograde directions through AV node and by additional paths.

Increases the survival rate of patients who have had myocardial infarction (lowers the frequency of ventricular arrhythmias and angina attacks). Slightly reduces the vital function of the lungs, almost does not weaken the bronchodilating effect of isoproterenol.

In therapeutic concentrations does not affect beta2-adrenoreceptors,in contrast to nonselective beta-blockers, has a less pronounced effect on the smooth muscles 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%), bioavailability - 40-50%, time to reach the maximum concentration in the plasma - 2-4 hours. It penetrates badly through the blood-brain barrier, passes through the placental barrier and into breast milk. Permeability through the blood-brain barrier and the placental barrier is low. 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 mg / min / 1.73 m², half-life is 16-27 hours, with creatinine clearance below 15 mg / min - more than 27 hours (a reduction in doses is necessary). It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

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

- disorders of the heart rhythm: sinus tachycardia, prevention supraventricular tachyarrhythmias.

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, atrioventricular block II-III Stroke, severe bradycardia, sinus node weakness syndrome, sinoauric blockade, acute or chronic heart failure (in decompensation stage), cardiomegaly without symptoms of heart failure, Prinzmetal angina, low blood pressure (in case of myocardial infarction, systolic blood pressure less than 100 mm Hg .st.), lactation period, simultaneous administration of monoamine oxidase inhibitors, age to 18 years.

Carefully:

Diabetes mellitus, metabolic acidosis, hypoglycemia; allergic reactions in history, chronic obstructive pulmonary diseases (incl. bronchial asthma, emphysema); chronic heart failure, obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); pheochromocytoma, hepatic insufficiency,chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including in the anamnesis), psoriasis, pregnancy, advanced age.

Pregnancy and lactation:

Pregnant women should be prescribed Atenolol Only in those 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, do not chew, squeezed a small amount of liquid.

Arterial hypertension. Treatment begins with 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 with values of creatinine clearance 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

Patients on hemodialysis, atenolol appoint 50 mg / day immediately after each dialysis, 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, heart rate).

Side effects:

The most common side effects are related to the main pharmacological action of the drug and are expressed as follows:

the cardiovascular system: the appearance of cardiac symptoms insufficiency, violation of atrioventricular conduction, bradycardia, marked decrease in blood pressure, sensation of cold and paresthesia in the limbs;

central nervous system: dizziness, sleep disturbance, decreased ability to concentrate, drowsiness, depression, hallucinations, lethargy, fatigue, headache;

gastrointestinal tract: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation;

respiratory system: dyspnea, bronchospasm, apnea;

hematological reactions: thrombocytic purpura, anemia (aplastic), thrombosis;

endocrine system: gynecomastia, decreased potency, decreased libido;

metabolic reactions: hyperlipidemia, hypoglycemia;

skin reactions: urticaria, dermatitis, itching, photosensitivity.

sensory organs: impaired vision, reduced lacrimal fluid secretion, dry and painful eyes, conjunctivitis, vasculitis, chest pain;

influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia;

Other: Peyronie's disease, 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: bradycardia, atrioventricular block II and III degree, an increase in the symptoms of heart failure, a marked decrease in blood pressure, bronchospasm, hypoglycemia.

Treatment: In severe bradycardia intravenous injection of 1 ml of a 0.1% solution of atropine sulfate is indicated. When AV blockade of II and III degree is possible the appointment of isoprenaline in tablets (5 mg under the tongue with a repetition in 2-4 hours) or intravenous drip or slow jet injection of the solution at a dose of 0, 5-1 mg. When bronchospasm occurs, inhalation or intravenous administration of beta2-adrenomimetic salbutamol is indicated.

Interaction:

With the simultaneous use of Atenolol with insulin, antidiabetic drugs - their hypoglycemic effect is enhanced.

When combined with antihypertensive agents of different groups or nitrates, diuretics, sympatholytics, the hypotensive effect intensifies. Simultaneous use of Atenolol and verapamil (or diltiazem) can cause a mutual enhancement of cardiodepressive action.

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, a pronounced bradycardia may occur.

Simultaneous intravenous administration of verapamil and diltiazem can provoke cardiac arrest; nifedipine - can lead to a significant decrease in blood pressure.

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

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, promotes an increase in the concentration of each of the drugs in the blood serum.

Phenytoin with IV introduction, means for general anesthesia increases the severity of cardiodepressive action.

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

It is not recommended simultaneous use with MAO inhibitors.

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 bradycardia and oppression AV conductivity.

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, anticoagulant effect of coumarins.

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

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 every 3-4 months), 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).

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.

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 non-selective 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), abrupt cancellation of beta-blockers can cause an increase in the frequency or severity of antianginal seizures, so it is necessary to gradually stop atenolol in patients with IHD.

Particular attention also requires the selection of doses in patients with cardiac decompensation. Compared with non-selective beta-blockers, cardioselective beta-blockers have less effect on lung function, however, in obstructive airway diseases Atenolol should be assigned only in the case of absolute indications. If it is necessary to prescribe them, in some cases, it may be recommended to use beta 2-adrenomimetics.

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 in cases where 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 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 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 enhance 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 an increased bradycardia (less than 50 / min), arterial hypotension (systolic blood pressure below 100 mm Hg) in elderly patients, AV blockade, bronchospasm, ventricular arrhythmias, severe impairment of 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.

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. Cancellation 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 content in the blood and urine 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 mg and 100 mg.

Packaging:For 14 or 10 tablets in a planar cell pack. For 30 or 50 tablets in a jar, bottlee polymeric. Bank, vial, 1, 3 or 5 contour cell packs at pack of cardboard.

Storage conditions:

List B. Store in a dry place inaccessible to children and protected from light.

At a temperature not exceeding 25 C.

Shelf life:

2 years. Do not use the product after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002550 / 01

Date of registration:03.10.2008

Expiration Date:Unlimited

The owner of the registration certificate:PRANAFARM, LLC PRANAFARM, LLC Russia

Manufacturer: & nbsp

PRANAFARM, LLC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)