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

Active substance:
atenolol	25 mg	50 mg	100 mg
Excipients:
potato starch	26.85 mg	53.7 mg	107.4 mg
crospovidone	8.125 mg	16.25 mg	32.5 mg
povidone	5.0 mg	10.0 mg	20.0 mg
microcrystalline cellulose	8.175 mg	16.35 mg	32.7 mg
silicon dioxide colloid (aerosil)	1.075 mg	2.15 mg	4.3 mg
magnesium stearate	1.625 mg	3.25 mg	6.5 mg
polysorbate (Tween 80)	0.05 mg	0.01 mg	0.2 mg
stearic acid	4.1 mg	8.2 mg	16.4 mg
Uncoated tablet weight	80 mg	160 mg	320 mg
Excipients for the shell:
Opadrai II (series 85 F)
polyvinyl alcohol	1.28 mg
macrogol	0.664 mg
talc	0.474 mg
titanium dioxide	0.8 mg
Opadrai II (series 85F)
polyvinyl alcohol		2.56 mg
macrogol		1.293 mg
talc		0.947 mg
titanium dioxide		1.458 mg
Aluminum lacquer based on quinoline yellow dye		0.141 mg
aluminum lacquer based on indigo carmine		0.001 mg
Opadrai II (series 85F)
polyvinyl alcohol			5.12 mg
macrogol			2.586 mg
talc			1.894 mg
titanium dioxide			1.197 mg
Aluminum lacquer based on the dye of the charming red			1.769 mg
Aluminum lacquer based on the sunset yellow dye			0.234 mg
Weight of coated tablets	83.2 mg	166.4 mg	332.8 mg

Description:

Tablets, film-coated 25 mg:

white or almost white, round, biconvex tablets. On the cross-section, two layers are visible, the inner layer is white or almost white.

Tablets, film-coated 50 mg:

yellow, round, biconvex tablets. On the cross-section, two layers are visible, the inner layer is white or almost white.

Tablets, film-coated 100 mg:

red, round, biconcave tablets, with a risk. On the cross-section, two layers are visible, the inner layer is white or almost white.

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 cAMP from ATP, reduces the intracellular current of Ca2 +, has a negative chrono-, dromo-, batmo- and inotropic action (reduces the 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) is increased 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, and with 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 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 and influence on the central nervous system.The antihypertensive effect is manifested by a decrease in both systolic and diastolic arterial pressure, a decrease in the shock volume of blood and minute blood volume. has an effect on the tone of the peripheral arteries.The antihypertensive effect 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 at rest and during physical activity. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle ventricular fibers may 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 content), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing 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. Reduces the incidence of ventricular arrhythmias and angina episodes in patients who underwent myocardial infarction. Virtually does not weaken the bronchodilating effect of isoproterenol. In contrast to non-selective beta-blockers, when administered at medium, 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. 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 after 1 hour after administration, reaches 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, the maximum concentration of the drug in the blood plasma (TS_m_Oh) 2-4 hours. Poor penetration 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. 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 (reduction of doses is necessary): when creatinine clearance is less than 35 ml / min / 1.73 m 2 T_1/2 is 16-27 hours, with creatinine clearance below 15 ml / min - more than 27 hours, with anuria - is extended to 144 hours. It is output during the procedure of hemodialysis.

Indications:

Arterial hypertension, prevention of attacks of stable angina (with the exception of Prinzmetal angina), cardiac rhythm disturbances: sinus tachycardia, prevention of supraventricular tachyarrhythmias, ventricular extrasystole.

Contraindications:

Hypersensitivity to the components of the drug, cardiogenic shock, AV blockade II-III degree, pronounced bradycardia with a heart rate less than 40 / min, sinus node weakness syndrome, sinoatrial block, acute and chronic heart failure in the stage of decompensation, cardiomegaly without signs of chronic heart failure, stenocardia Prinzmetal, arterial hypotension (in case of use with myocardial infarction, systolic blood pressure less than 100 mmHg), pheochromocytoma (without simultaneous use of alpha-blockers), breastfeeding period, age 18 years (efficacy safety not established), simultaneous reception of monoamine oxidase inhibitors.

Carefully:Type I diabetes mellitus, metabolic acidosis, hypoglycaemia; weighed allergic anamnesis, chronic obstructive pulmonary disease, bronchial asthma, emphysema; chronic heart failure, obliterating peripheral vascular diseases ("intermittent" lameness, Raynaud's syndrome); pheochromocytoma with simultaneous use of alpha-adrenoblockers, liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis,depression (including in the anamnesis), psoriasis, pregnancy, advanced age, AV blockade of the 1st degree.

Pregnancy and lactation:

Application of the drug Atenolol during pregnancy and breastfeeding is contraindicated. The use of the drug is possible if the expected benefit for the mother exceeds the potential risk to the fetus.

Atenolol excreted in breast milk, so if you need the drug Atenolol during breastfeeding, breastfeeding should be cancel.

Dosing and Administration:

Inside, before reception, food, without liquid and squeezed a small amount of liquid.

Arterial hypertension. The initial dose is 25-50 mg once a day. To achieve a stable hypotensive effect, it takes 1-2 weeks for the drug to be taken. If necessary, increase the dose to 100 mg in one dose.

Angina pectoris. The initial dose is 50 mg once a day. If the optimum therapeutic effect is not achieved within a week, the dose to 100 mg per day is increased.

Older patients and patients with impaired renal excretory function need a correction of the dosing regimen.

In patients with renal failure, dose adjustment is recommended depending on the creatinine clearance. In patients with renal failure with creatinine clearance values above 35 ml / min / 1.73 m² (normal values are 100-150 ml / min / 1.73 m²) significant cumulation does not occur. -

With the clearance of creatinine 15-35 ml / min, 100 mg every other day or 50 mg / day is prescribed; when creatinine clearance is less than 15 ml / min - 50 mg every other day, or 100 mg once every 4 days. Against the background of hemodialysis of 50 mg after each dialysis (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 and heart rate).

To prevent attacks of angina pectoris - 100 mg once a day, with tachysystolic heart rhythm disorders - 50 mg once a day.

Appointment of the drug more than 1 time per day is not appropriate, because atenolol is active for 24 hours. The maximum daily dose is 100 mg. 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.

Dose reduction in the event of planned cancellation is gradual.

Side effects:

From the central nervous system: asthenia, weakness, dizziness, headache, drowsiness or insomnia / "nightmarish" dreams, depression, anxiety, confusion, or short-term lossmemory, hallucinations, decrease ability to concentrate, reduce speed reaction, 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, increased heart rate, impaired conduction 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 limbs, 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.

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

Co the endocrine system: Hyperglycemia (in patients with diabetes mellitus 2 type), hypoglycemia (in patients with type 1 diabetes mellitus), can mask the symptoms of hyperthyroidism.

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

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

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

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

Other: pain in the back, arthralgia, myasthenia gravis, weakening of libido, decreased potency, gynecomastia, withdrawal syndrome (increased angina attacks, increased blood pressure).

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

If any of the side effects listed in the manual are aggravated; or you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: severe bradycardia, dizziness, excessive depression of arterial pressure, syncope, arrhythmia, ventricular extrasystole, AV blockade II-III st., exacerbation of symptoms of chronic heart failure, cyanosis of the fingernails or palms of the hands, convulsions, difficulty breathing, bronchospasm.

Treatment: gastric lavage and administration of absorbent 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 plasmasubstitutional solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; in chronic heart failure - cardiac glycosides / diuretics; with convulsions - in / in; diazepam;with bronhospazme - inhalation or parenteral - beta-adrenostimulyatory. Dialysis is possible.

Interaction:

Allergens used for immunotherapy, or extracts, allergens for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving atenolol. Iodine-containing radiocontrast drugs for IV administration increase the risk of anaphylactic reactions.

Phenytoin with IV introduction, medicines 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 hypoglycemic agents for oral administration, masks the symptoms of developing hypoglycemia.

Reduces the clearance of lidocaine and xanthines and increases their concentration in the plasma, especially 1 in patients with initially elevated clearance of theophylline under the influence of smoking. Hypotensive effect weakens non-steroidal anti-inflammatory drugs (delay Na⁺ and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (delay Na⁺).

Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of "slow calcium" channels (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or exacerbating the course of heart failure, bradycardia, AV blockade and cardiac arrest.

Diuretics, clonidine, sympatholytics, hydralazine, slow calcium channel blockers and other antihypertensive drugs can lead to excessive lowering of blood pressure.

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 monoamine oxidase inhibitors and due to a significant increase in antihypertensive effect, a break in treatment between taking monoamine oxidase inhibitors and atenolol should be at least 14 days.

Unhydrated ergot alkaloids increase the risk development of peripheral circulatory disorders.

Special instructions:

Control of patients taking the drug Atenolol, should include monitoring the heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 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).

The patient should be taught how to calculate the heart rate and instructed about the need for medical advice at a heart rate of 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 per minute) and an increased end-diastolic volume of the left ventricle, which violate 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.

In thyrotoxicosis, the drug Atenolol can mask certain clinical signs of thyrotoxicosis (eg, tachycardia).Sharp abolition in patients with thyrotoxicosis is contraindicated, since, it is able to strengthen, symptomatology. In diabetes mellitus can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, the drug Atenolol practically does not increase insulin-induced hypoglycemia and does not delay the recovery of glucose in the blood to normal concentration.

With simultaneous admission with clonidine, his admission can be stopped only a few days after the drug was discontinued Atenolol.

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 Atenolol. If the patient has taken the drug Atenolol before surgical intervention, he should choose medicines for general anesthesia with minimal negative inotropic action.

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-adrenoblockers, so patients who take such combination of medicines, should be under the constant supervision of the doctor, for the purpose of revealing the expressed decrease in arterial pressure or bradycardia.

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

If older bradycardia (less than 50 / min) appears in the elderly, arterial hypotension (systolic arterial ₍pressure below 100 mm Hg) AV blockade, bronchospasm, ventricular arrhythmias, severe disorders the function of the liver and kidneys need to reduce the dose or stop treatment.

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).

Patients with ischemic heart disease should drug withdrawal period Atenolol be under close supervision.

With the development of depression caused by admission beta-blockers, drug therapy Atenolol should be discontinued.

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

The risk of paradoxical arterial hypertension is possible when used in patients with pheochromocytoma without simultaneous use of alpha-blockers.

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

During the treatment period, care must be taken when driving vehicles, servicing moving mechanisms, and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Film coated tablets, 25 mg, 50 mg and 100 mg.

Packaging:

By 7, 10, 15, 20 or 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 1, 2, 3, 4, 5 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

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:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000673

Date of registration:28.07.2011

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)