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

Excipients: corn starch, methyl parahydroxybenzoate, propyl parahydroxybenzoate, magnesium stearate, carboxymethyl starch sodium, silicon dioxide colloid.

Description:Tablets of white color, flat-cylindrical, with a facet and a risk.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B.03 Atenolol

Pharmacodynamics:

Has antianginal, antihypertensive and antiarrhythmic effect.Does not possess membrane stabilizing and internal sympathomimetic activity. Reduces the catecholamine-stimulated formation of cAMP from ATP.

AT the first 24 h 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 gradually decreases 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 (BP), a decrease in the impact and minute volumes. In average therapeutic doses does not affect the tone of peripheral arteries. The hypotensive effect lasts 24 hours, with regular use stabilized by the end of the second week 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 stimulation.It reduces the heart rate (HR) at rest and during physical activity. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles can increase the need for oxygen, especially in patients with chronic heart failure.

The antiarrhythmic effect is manifested by the suppression of sinus tachycardia and is associated with the elimination of arrhythmogenic sympathetic effects on the cardiac conduction system, a decrease in the rate of propagation of excitation through the sinoatrial node, and an elongation of the refractory period. Oppresses impulses in antegrade and in lesser extent in the retrograde direction through AV (atrioventricular) node and on additional ways of carrying out. Negative chronotropic effect is manifested after 1 hour after administration, reaches a maximum after 2-4 hours, lasts up to 24 hours.

Reduces the automaticity of the sinus node, lowers heart rate, slows down AV-conductivity, reduces myocardial contractility, reduces the need for myocardium in oxygen. Reduces the excitability of the myocardium.

When used in average therapeutic doses, it has a less pronounced effect on the smoothmusculature of the bronchi and peripheral arteries than non-selective beta-blockers.

Pharmacokinetics:

Absorption from the gastrointestinal tract is fast, incomplete (50-60%), bioavailability is 40-50%, the time to reach the maximum concentration in the blood plasma is 2-4 hours. It penetrates poorly through 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. 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 ml / min / 1.73 m² the half-life is 16-27 hours, with creatinine clearance below 15 ml / min / 1.73 m² - more than 27 hours (a dose reduction is necessary). It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

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

- cardiac arrhythmias: sinus tachycardia, prevention of supraventricular tachyarrhythmias, ventricular extrasystole.

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, atrioventricular (AV) blockade II - III st, pronounced bradycardia (heart rate less than 45-50 bpm), sinus node weakness syndrome, sinouauric blockade, acute or chronic heart failure (in the decompensation stage), cardiomegaly without symptoms of heart failure, angina prinzmetala, arterial hypotension (in the case of use in myocardial infarction, systolic blood pressure less than 100 mm Hg), simultaneous administration of monoamine oxidase inhibitors (MAO), age to 18 years (efficacy and safety not established).

Carefully:

Diabetes mellitus, metabolic acidosis, hypoglycemia, allergic reactions in the anamnesis, chronic obstructive pulmonary disease (including emphysema of the lungs), AV blockade of the 1st degree, chronic heart failure (compensated), obliterating peripheral vascular diseases (intermittent claudication, Raynaud's syndrome), pheochromocytoma, hepatic insufficiency, chronic renal failure, myasthenia gravis, hyperthyroidism, depression (including history), psoriasis , elderly 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 excreted in breast milk, therefore during breast-feeding it is contraindicated.

Dosing and Administration:

Inside before eating, not liquid, squeezed, a small amount of liquid.

Arterial hypertension:

treatment is started with 50 mg of Atenolol 1 time per day. To achieve a stable hypotensive effect, 1 to 2 weeks of admission is required. If the hypotensive effect is insufficient, the dose is increased to 100 mg in one 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. 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 (the 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
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 on hemodialysis, Atenolol prescribe 25 or 50 mg / day immediately after each dialysis, which must be done in a steady state, since 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).

An increase in the daily dose of more than 100 mg is not recommended, since the therapeutic effect is not increased, and the likelihood of side effects increases.

Side effects:

The cardiovascular system: development (aggravation) of symptoms of chronic heart failure (swelling of the ankles, stop, shortness of breath), violation of atrioventricular conduction, arrhythmias, bradycardia, marked decrease in blood pressure, orthostatic hypotension, palpitations.

Central nervous system: dizziness,decreased ability to concentrate attention, decreased reaction speed, drowsiness or insomnia, depression, hallucinations, fatigue, headache, weakness, nightmarish dreams, anxiety, confusion or short-term memory loss, paresthesia in the extremities (in patients with "intermittent" lameness and Raynaud's syndrome), muscle weakness, convulsions.

Fhomework-intestinal tract: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation, taste change.

Respiratory system: dyspnea, bronchospasm, apnea, nasal congestion.

Hematologic reactions: thrombocytopenic purpura, anemia (aplastic), thrombosis.

Endocrine system: gynecomastia, decreased potency, decreased libido, hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status.

Metabolic reactions: hyperlipidemia.

Skin reactions: urticaria, dermatitis, itchy skin, photosensitivity, increased sweating, skin hyperemia, exacerbation of psoriasis, reversible alopecia.

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

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

Laboratory indicators: agranulocytosis, leukopenia, increased activity of "hepatic" enzymes, hyperbilirubinemia.

Other: back pain, arthralgia, 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: pronounced bradycardia, AV blockade II - III degree, increased symptoms of heart failure, excessive reduction in blood pressure, difficulty breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the fingernails or palms, convulsions.

Treatment: gastric lavage and administration of absorbent drugs; when bronchospasm occurs, inhalation or intravenous (iv) injection of beta 2-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 of Class 1A 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; with chronic heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam. Dialysis is possible.

Interaction:

With the simultaneous use of atenolol with insulin, oral hypoglycemic drugs - their hypoglycemic effect is enhanced. When combined with antihypertensive agents of different groups or nitrates, hypotensive effect is enhanced. The 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), non-steroidal anti-inflammatory drugs and glucocorticosteroids.

With the simultaneous use of atenolol and cardiac glycosides, the risk of bradycardia and violation of atrioventricular conduction increases.

With the simultaneous administration of atenolol with reserpine, methyldopa, clonidine, verapamil, a pronounced bradycardia may occur.

The use of atenolol with simultaneous intravenous administration of verapamil or diltiazem increases the risk of developing or worsening heart failure, bradycardia, AV blockade and cardiac arrest. Nifedipine can lead to a significant decrease in blood pressure. With the simultaneous use of atenolol with derivatives of ergotamine, xanthine, its effectiveness is reduced.

When the combined use of atenolol and clonidine is discontinued, clonidine treatment continues for a few more days after atenolol is discontinued.

Simultaneous use with lidocaine may reduce its elimination 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, drugs for inhalation anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

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

It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive effect, a break in treatment between the intake of 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.

Amiodarone increases the risk of bradycardia and oppression AV conductivity. Cimetidine increases the concentration in the blood plasma (inhibits metabolism). Iodine-containing radiocontrast drugs for IV administration increase the risk of anaphylactic reactions.

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.

Special instructions:

Control of patients receiving Atenolol, should include monitoring of heart rate and blood pressure (at the beginning of treatment - every day, then every 3 to 4 months),the content of blood glucose in patients with diabetes mellitus (1 every 4 to 5 months). In elderly patients it is recommended to follow the function of the kidneys (once every 4 to 5 months).

It is necessary to teach the patient how to calculate heart rate and instruct 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 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.

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 the use of Atenolol in patients with IHD should be gradual.

In comparison with nonselective beta-blockers, cardioselective beta-blockers have less effect on lung function, however,in obstructive airway diseases atenolol appoint 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 case of intolerance and / or ineffectiveness of other antihypertensive drugs, but strict monitoring of dosage should be carried out. Overdosing is dangerous by the development of bronchospasm.

Particular attention is needed in cases where surgical intervention is required under general anesthesia in patients taking Atenolol. The drug should be discontinued 48 hours before the intervention. 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 withdrawal syndrome of the latter.

Patients with a burdened allergological anamnesis when taking beta1-adrenoblockers have an increased risk of developing anaphylactoid reactions,which may occur in a more severe form and the use of conventional doses of epinephrine may be ineffective.

Drugs that reduce catecholamine stores (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 detection of a marked decrease in blood pressure or bradycardia.

In the case of elderly patients increasing bradycardia (. Less than 50 beats / minute), hypotension (systolic blood pressure below 100 mm Hg; Art.), Atrioventricular block, bronchospasm, ventricular arrhythmia, serious liver and kidney functions 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.

When applying Atenolol may reduce the production of tear fluid, which has a value in patients using 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. and more (reduce the dose by 25% in 3 to 4 days).

It is necessary to cancel the use of the drug before the study of 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 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 25 mg, 50 mg, 100 mg.

Packaging:

For 10, 14 or 20 tablets in a contour mesh box made of a polyvinylchloride film and aluminum foil.

l, 2, 3, 4, 5, 7 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N014941 / 01

Date of registration:13.10.2009

Expiration Date:Unlimited

The owner of the registration certificate:M. J. Biofarm Pvt. Ltd.M. J. Biofarm Pvt. Ltd. India

Manufacturer: & nbsp

M.J. BIOPHARM, Pvt. Ltd. India

Representation: & nbspM.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group M.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group India

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)