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

Excipients: corn starch - 0.111 g, magnesium hydroxycarbonate (magnesium carbonate basic) - 0.175 g, magnesium stearate (magnesium stearic acid water) - 0.010 g, gelatin (gelatin food) - 0.004 g.

Description:Tablets white or white with a creamy shade of color, flat-cylindrical shape with a facet and a risk. Light marble is allowed.

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- adrenergic receptors of the heart, stimulated by catecholamines reduces the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces intracellular calcium ion current has a negative chronotropic, dromo-, BATM and inotropic effects (heart rate slows, inhibits conductivity and excitability, reduces myocardial contractility).

Total peripheral resistance vessels in the early use of beta-blockers (for the first 24 hours after oral administration) is increased (as a result of reciprocal increase in the activity of alpha-adrenoceptor stimulation and removal of beta2-adrenoceptor), which is 1-3 days returns to the original, and prolonged the appointment is reduced.

Antihypertensive effect is associated with a decrease in the minute volume of blood circulation, 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. Antihypertensive effect is manifested by a decrease in both systolic and diastolic arterial pressure, a decrease in the shock volume of blood and the minute volume of blood circulation. 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 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 end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers, the ventricles of the heart can increase the need for myocardium in 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, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and slowing of atrioventricular conduction. The suppression of impulses is noted mainly in the antegrade and to a lesser extent in the retrograde direction through the atrioventricular node and along additional paths.

Virtually does not weaken the bronchodilating effect of isoprenaline.

Atenolol, in contrast to non-selective beta-blockers, when administered at moderate therapeutic doses, has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus), and carbohydrate metabolism; to a lesser extent than non-selective beta-blockers, 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 from the gastrointestinal tract - fast, incomplete (50%), bioavailability - 40-50%, time to reach the maximum concentration in blood plasma - 2-4 hours. It penetrates badly through the blood-brain barrier, passes through the placental barrier and into breast milk. Connection with proteins in blood plasma - 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: when the creatinine clearance is less than 35 mg / min / 1.73 m², the half-life is 16-27 hours, with creatinine clearance below 15 mg / min. - more than 27 hours (reduction of doses is necessary). It is displayed during the procedure of hemodialysis.

Indications:

- Arterial hypertension;

- prevention of attacks of stable angina, with the exception of Prinzmetal angina pectoris;

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

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, atrioventricular block II-III st, pronounced bradycardia with heart rate less than 50 beats per minute, sinus node weakness syndrome, sinouauric blockade, acute and chronic heart failure in decompensation stage, cardiomegaly without symptoms of heart failure, angina prinzmetal, severe arterial hypotension (in case of use in myocardial infarction , systolic blood pressure less than 100 mm Hg), pheochromocytoma (without simultaneous use of alpha-blockers), simultaneous administration of monoamine inhibitors oxidases, severe peripheral circulatory disorders, severe forms of bronchial asthma and chronic obstructive pulmonary disease, age under 18 years (efficacy and safety not established).

Carefully:

Diabetes mellitus, metabolic acidosis, hypoglycemia; weighed allergic anamnesis, chronic obstructive pulmonary disease, bronchial asthma, emphysema; chronic heart failure, violation of peripheral circulation ("intermittent" lameness,Raynaud's syndrome); severe arterial hypotension, pheochromocytoma (with simultaneous use of alpha-adrenoblockers), liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, atrioventricular blockade of the 1st degree, bronchospasm in the anamnesis, elderly age.

Pregnancy and lactation:

Atenolol penetrates the placental barrier, is found in the blood of the umbilical cord. Pregnant women should be prescribed atenolol Only in those cases where the benefit to the mother exceeds the potential risk to the fetus. Atenolol excreted in breast milk, so the drug is not recommended during breastfeeding.

Dosing and Administration:

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

Doses of the drug and the duration of treatment are established by the attending physician individually, depending on the therapeutic effect and tolerability. Do not change the dosage and stop treatment with atenolol without advice from your doctor. Abrupt cancellation of the drug can cause ischemia of the heart with exacerbation of angina or hypertension or provoke myocardial infarction. Given this, the drug should be withdrawn be strictly controlled by the attending physician and gradually.

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. The maximum daily dose is 100 mg, as the dose increase is not accompanied by an increase in the therapeutic 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 or 100 mg 1 groove in 4 days

Patients on hemodialysis, atenolol appoint 50 mg / day immediately after each procedure for hemodialysis in hospital, since it is possible to reduce blood pressure.

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

You can apply atenolol in another dosage form - 50 mg tablets with a risk.

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

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: development or aggravation of symptoms of chronic heart failure, atrioventricular conduction disorder, bradycardia, marked decrease in blood pressure, chest pain, palpitations, arrhythmias, orthostatic reactions, atrioventricular block;

- central nervous system: asthenia, dizziness, sleep disturbance, decreased concentration, drowsiness, depression, hallucinations, lethargy, fatigue, headache, weakness, insomnia, nightmarish dreams, anxiety, confusion or short-term memory loss, weakened reactivity, parasthesia in the extremities (in patients with "intermittent" lameness and Raynaud's syndrome), muscle weakness, convulsions;

- gastrointestinal tract: dryness of the oral mucosa, 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, hypoglycemia (in patients with type 1 diabetes mellitus), hyperglycemia (in patients with type 2 diabetes), hypothyroid status (abnormalities in the body due to a decline in the production of thyroid hormones);

- skin reactions: urticaria, dermatitis, pruritus, photosensitivity reactions, reversible alopecia, skin hyperemia, psoriasis-like skin rashes, angioedema;

- Senses: impaired vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis, changes in taste, nasal congestion;

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

- laboratory indicators: agranulocytosis, leukopenia, increased activity "hepatic" enzymes, hyperbilirubinemia, positive test results for antinuclear antibodies;

- other: withdrawal syndrome (increased angina attacks, increased blood pressure), back pain, arthralgia, cholestasis, jaundice, increased sweating, angiospasm, vasculitis, exacerbation of psoriasis.

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 if you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

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

Treatment: gastric lavage and the appointment of enterosorbents. In violation of atrioventricular 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 - intravenously plasma-substituting solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; in chronic heart failure - cardiac glycosides, diuretics; at. convulsions - intravenously diazepam, with bronchospasm - beta-adrenostimulators (inhalation or parenteral). Hemodialysis is effective.

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 developing anaphylactic reactions. Phenytoin when administered intravenously, 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 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 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 (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or exacerbating the course of chronic heart failure, bradycardia, atrioventricular blockade and cardiac arrest. Diuretics, clonidine, sympatholytics, hydralazine, blockers of "slow" calcium channels 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, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase the inhibition of the central nervous system.

It is not recommended simultaneous use with monoamine oxidase inhibitors due to a significant increase in antihypertensive action, a break in treatment between taking monoamine oxidase inhibitors and atenolol should be at least 14 days. Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

Special instructions:

Control of patients taking Atenolol-UBF should include monitoring heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), blood glucose concentration in patients with diabetes mellitus (1 every 4-5 month). 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 / min) and an increase in the end-diastolic volume of the left ventricle that disrupts 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.

In thyrotoxicosis, Atenolol-UBF 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 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 administration of clonidine, his reception may be discontinued only a few days after the withdrawal of Atenolol-UBF.

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 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 Atenolol-UBF, so patients taking such combinations of drugs should be under constant medical supervision to detect a marked decrease in blood pressure or bradycardia.

Atenolol-UBF can be prescribed to patients with bronchospastic diseases 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.

In the case of an increasing bradycardia (less than 50 beats / min), arterial hypotension (systolic blood pressure below 100 mmHg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of the liver and kidneys 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 taking Atenolol-UBF.

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 canceled Atenolol-UBF before the study of blood and urine levels of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies 1-2 days before the test.

The risk of paradoxical arterial hypertension when using Atenolol-UBF in patients with pheochromocytoma is not possible without the 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 and occupying otherspotentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets of 100 mg.

Packaging:

10 tablets per contour cell packaging made of polyvinylchloride film and foil of aluminum printed lacquered or paper packaging with polymer coating.

By 10, 20, 30, 40, 50, 60 tablets in cans of polymeric.

Each bank or 1, 2, 3, 5, 6 contour squares with instructions for use are placed in a cardboard package.

Storage conditions:

In dry, dark 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 expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002527 / 01

Date of registration:27.10.2008 / 17.04.2012

Expiration Date:Unlimited

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp08.10.2017

Illustrated instructions

Instructions

Atenolol-UBF (Atenolol-UBF)