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

ExcipientsLactose, corn starch, sodium starch glycolate, sodium lauryl sulfate, San-sen yellow dye, isopropyl alcohol, polyvinylpyrrolidone, silicon dioxide colloid, purified talc, magma stearate, hydroxypropyl methylcellulose, polyethylene glycol, titanium dioxide, purified water.

For a dosage of 50 mg:

Active substance: atenolol 50 mg

Excipientslactose, corn starch, silicon colloidal dioxide, isopropyl alcohol, sodium lauryl sulfate, povidone, purified water, soluble dye San-sen yellow, purified talc, magnesium stearate, hydroxypropyl methylcellulose, titanium dioxide, methylene chloride, light liquid paraffin, polyethylene glycol .

Description:

Orange colored tablets, film-coated, round, biconvex, with a dividing risk on one side. On the cross-section, a thin layer of the shell and the core from light orange to orange.

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 stimulation of catecholamines formation of cAMP and ATP, reduces the intracellular current of sodium ions. During the first 24 hours after oral administration, with a reduction 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 barocereptors, and effects on the central nervous system. The hypotensive effect is manifested by 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 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 tension of the ventricular muscle fibers and the final diastolic pressure in the left ventricle, it can increase the demand for myocardium in oxygen, especially in patients with chronic insufficiency.The antiarrhythmic effect is manifested by suppression of sinus tachycardia and is associated with the elimination of arrhythmogenic sympathetic influences on the conduction system of the heart, inhibition of heterogeneous automatism, a decrease in the rate of propagation of excitation through the sinouauricular node, and an extension of the refractory period. Oppresses the impulses in antegrade and, to a lesser extent, in retrograde directions through the atrioventricular node and along additional paths.

Increases the survival rate of patients who underwent myocardial infarction (reduces the incidence of ventricular arrhythmias and 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 beta-2 adrenergic receptors, in contrast to non-selective beta-adrenoblockers 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, it can have a beta-2-adrenergic blocking effect.

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

Pharmacokinetics:

After ingestion, the drug is rapidly absorbed from the gastrointestinal tract - approximately 50% of the dose taken internally. The solubility in fats is poor, the bioavailability is 40-50%, the 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. Relationship with plasma proteins is 6-16%.

It is not metabolized in the liver. Half-life of 6-9 hours (increases in elderly patients). They are excreted by the kidneys by glomerular filtration (85-100% unchanged). Function violation kidney is accompanied by an elongation of the half-life and cumulation: when 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 / 1.73 m² - more than 27 hours (reduction of doses is necessary). It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

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

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

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, atrioventricular blockade of grade II or III, severe bradycardia, sinus node weakness syndrome, sinoauric blockade, acute or chronic heart failure (decompensated), cardiomegaly without symptoms of heart failure, angina prinzmetala, arterial hypotension (in case of use in myocardial infarction, systolic blood pressure less than 100 mm Hg), bronchial asthma, lactation period, simultaneous administration of monoamine oxidase inhibitors s (MAO), under 18 years of age (efficacy and safety not established).

Carefully:

With care - diabetes mellitus, metabolic acidosis, hypoglycemia, allergic reactions in history, chronic obstructive pulmonary disease (including emphysema of the lungs), AV blockade of 1 degree, chronic heart failure (compensated), obliterating diseases of peripheral vessels ("intermittent" lameness, Raynaud's syndrome), pheochromocytoma, chronic renal failure, hepatic insufficiency, myasthenia gravis, thyrotoxicosis, depression (incl.in anamnesis), psoriasis, pregnancy, 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, so 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, drink with a small amount of liquid.

Arterial hypertension:

Treatment is started 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 function need to adjust the dose depending on the creatinine clearance. In patients with renal insufficiency with values of creatinine clearance above 35 ml / min / 1.73 m³ (the normal value is 100-150 ml / min / 1.73 m³) 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)	Concentration of serum creatinine (mmol / l)	The dose of atenolol
15-35	300-600	50 mg per day
less than 15	more than 600	50 mg every other day or
		100 mg once every 4 days

Patients on hemodialysis, atenolol appoint 50 mg / day immediately after each dialysis in a hospital under careful medical supervision, since there is a risk of developing arterial hypotension.

In elderly people 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:

from the cardiovascular system: the appearance of symptoms of heart failure, violation of atrioventricular conduction, bradycardia, marked decrease in blood pressure, palpitations; thrombosis.

from the central nervous system: dizziness, sleep disturbance, decreased ability to concentrate, drowsiness, depression, hallucinations, lethargy, fatigue, headache, weakness, insomnia, nightmares, anxiety, confusion or short-term memory loss, weakened reactivity, paresthesia in the extremities patients with "Intermittent" lameness and Raynaud's syndrome), muscle weakness, convulsions;

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

from the respiratory system: dyspnea, bronchospasm, apnea;

hematological reactions: thrombocyte purpura, anemia (aplastic);

from the endocrine system: gynecomastia, decreased potency, decreased libido; hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status; metabolic reactions: hyperlipidemia;

skin reactions: urticaria, dermatitis, itching, photosensitivity, increased sweating, skin hyperemia, exacerbation of psoriasis;

sensory organs: impaired vision, decreased secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis, vasculitis, pain in the chest;

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

laboratory indicators: agranulocytosis, leukopenia, increased activity of "hepatic" enzymes and bilirubin level;

Other: syndrome of "withdrawal" (increased attacks of angina pectoris, increased blood pressure), reversible alopecia, back pain, arthralgia.

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

Overdose:

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

In case of an overdose, take atenolol should be discontinued and the patient should be under medical supervision.

Treatment: gastric lavage and the appointment of absorbents. When bronchospasm occurs, inhalation or intravenous administration of beta 2-adrenomimetic salbutamol is indicated. In severe bradycardia, 1 ml of a 0.1% solution of atropine sulfate should be administered intravenously. In violation of AV conductivity - epinephrine or setting up a temporary pacemaker, with ventricular extrasystole - lidocaine (preparations IA class do not apply), with arterial hypotension - the patient should be in the Trendelenburg position. If there are no signs of pulmonary edema - intravenous plasmasubstitutional solutions, with ineffectiveness - the introduction of epinephrine, dopamine, dobutamine, with heart failure - cardiac glycosides, with convulsions - in / in diazepam. Dialysis is possible.

Interaction:

With the simultaneous use of atenolol and insulin (or other oral antidiabetics), it is possible to intensify their hypoglycemic effects.

When combined with antihypertensive agents of other groups or nitrates, diuretics, sympatholytic drugs occurs to enhance the hypotensive effect.

Simultaneous use of atenolol and verapamil (or diltiazem) is 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 violation of atrioventricular conduction increases.

With the simultaneous administration of atenolol with reserpine, methyldopa, clonidine, verapamil, a pronounced bradycardia may occur. Patients receiving concomitantly atenolol and clonidine, clonidine cancellation only after a few days after the cessation of treatment with atenolol.

Simultaneous iv injection of verapamil and diltiazem can provoke heart failure, nifedipine - can lead to a significant decrease HELL.

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

When used concomitantly with lidocaine, it 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.

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 developing bradycardia and depresses 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 nonpolarizing 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 1 time in 3-4 months), blood glucose in diabetic patients (1 time in 4-5 months). In elderly patients it is recommended to monitor the kidney function (1 time in 4-5 months).

It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at heart rate less than 50un / 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 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 cessation of atenolol in patients with IHD should be gradual.

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.

Atenolol masks tachycardia, which occurs with hypoglycemia, and may prolong the duration of hypoglycemic reaction to insulin. Caution should be exercised with simultaneous use of atenolol and hypoglycemic drugs in patients with diabetes mellitus. 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, a drug with a possible minimal negative inotropic effect should be chosen.

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 cancellation 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 a background of allergicanamnesis.

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.

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

In the case of elderly patients with severe bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mmHg) 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 intravenous verapamil is needed, this should be done no less than 48 hours after taking atenolol.

With the use of atenolol, tear production can be reduced, which is important for 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 or more (reduce the dose by 25% in 3-4 days).

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:Pills.

Packaging:For 14 tablets per blister, Al / PVC. 2 blisters together with instructions for use in a cardboard box.

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:

3 years.

Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015392 / 01

Date of registration:16.03.2009

Expiration Date:Unlimited

The owner of the registration certificate:Ipka Laboratories Ltd.Ipka Laboratories Ltd. India

Manufacturer: & nbsp

IPCA LABORATORIES, Ltd. India

Representation: & nbspIPKA LABORATORIES LTD. IPKA LABORATORIES LTD. India

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol (Atenolol)