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

Active substanceEsatenololEsatenolol

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Estecor

pills inwards

AKTAVIS GROUP, AO Iceland

Dosage form: & nbsppills

Composition:

1 tablet of 12.5 mg contains:

active substance: S(-) Atenolol 12.5 mg;

Excipients: cellulose microcrystalline 100.5 mg, pregelatinized starch 15 mg, silicon dioxide colloid 1 mg, carboxymethyl starch sodium (sodium starch glycolate) 9 mg, magnesium stearate 2 mg.

1 tablet of 25 mg contains:

active substance: S(-) Atenolol 25 mg;

Excipients: cellulose microcrystalline 85.5 mg, pregelatinized starch 15 mg, silicon dioxide colloid 3 mg, carboxymethyl starch sodium (sodium starch glycolate) 9 mg, magnesium stearate 2.5 mg.

1 tablet of 50 mg contains:

active substance: S(-) Atenolol 50 mg;

Excipients: cellulose microcrystalline 110.7 mg, pregelatinized starch 90 mg, silicon dioxide colloid 2.5 mg, carboxymethyl starch sodium (sodium starch glycolate) 10 mg, magnesium stearate 2.5 mg, sodium lauryl sulfate 2.5 mg, starch 1.5 mg, dye sunlight sunset yellow 0.3 mg.

Description:

Tablets 12.5 mg - round biconvex tablets of white color with bevelled edge even on both sides.

Tablets 25 mg - round biconvex tablets of white color with bevelled edges with a risk on one side.

50 mg tablets - Round tablets of light orange color with a risk on one side.

Pharmacotherapeutic group:beta1-blocker selective

ATX: & nbsp

C.07.A.B Selective beta-blockers

C.07.A.B.03 Atenolol

Pharmacodynamics:

Atenolol is a racemic mixture of two optical forms of isomers R(+) and S(-), the ratio of which in racemic Atenolol is 1: 1. S(-) Atenolol chirally purified form of Atenolol.

S(-) Atenolol - cardioselective β₁-adrenergic blocker. Act S(-) Atenolol on the endocrine system and metabolism consists in a decrease in the activity of the renin-angiogenesic system and the concentration of free fatty acids in the blood plasma. S(-) Atenolol highly hydrophilic, unlike others β- adrenoblokatorov, showing lipophilic properties. The ego can cause a low proportion of side effects from the central nervous system (CNS). In addition, selective β-adrug blocker S(-) Atenolol to a lesser extent causes the prolongation of the action of insulin, which is the cause of hypoglycemia, in contrast to nonselective β -blockers.

S(-) Atenolol reduces heart rate (heart rate) and reduces myocardial contractility, which allows to reduce the occurrence of symptoms of angina pectoris.

The results of clinical studies have shown that only S(-) enantiomer is capable of blocking β-receptor, a R(+) enantiomer does not exhibit blocking activity against receptors. It follows that the dose S(-) Atenolol (25 mg) is halved compared to racemic Atenolol (50 mg).

A comparative study of racemic Atenolol, S(-) Atenolol and R(+) Atenolol showed that racemic Atenolol and S(-) Atenolol equally reduce systolic and diastolic arterial pressure (BP) and heart rate, while R(+) Atenolol did not make any changes to these parameters.

The hemodynamic effect of racemic Atenolol (100 mg) is similar in intensity S(-) Atenolol in a dose less than twice (50 mg), while RThe isomer does not cause any changes in the indices at a dosage of 50 mg.

Affinity S(-) Atenolol to β₁-adrenoceptors is clearly higher than that of R(+) Atenolol. It was also proved that only S(-) Atenolol responsible for the negative chrono- and inotropic effects, and RThe isomer does not affect these parameters.

Pharmacokinetics:

S(-) Atenolol is well absorbed after ingestion, is metabolized by "primary passage" through the liver.Since the preparation is hydrophilic, the absorption is incomplete, but rapid, when administered. The value of the maximum concentration in blood plasma (FROM_mOh) - 781.81 mg / ml, which reaches its value after 3 hours (TC_mOh). Area under the curve AUC₀_-_t- 4513.88 ng * h / ml. The value of the area under the curve AUC_0-∞ - 5243.86 ng * h / ml. The half-life (T_1/2) - 4.02 parts.

Indications:

Arterial hypertension, prevention of angina attacks (with the exception of Prinzmetal angina), heart rhythm disturbances.

Contraindications:

Hypersensitivity to S(-) Atenolol or racemic atenolol, cardiogenic shock, atrioventricular (AV) blockade II-III st, pronounced bradycardia (heart rate less than 40 beats / min), sinus node weakness syndrome, sinoatrial block, acute heart failure (CH) or chronic heart failure (CHF) in the decompensation stage, cardiomegaly without symptoms of CHF, angina Prinzmetal, arterial hypotension (in case of myocardial infarction, systolic blood pressure less than 100 mm Hg), various violations of peripheral arterial blood flow, simultaneous administration of monoamine oxidase (MAO) inhibitors, pregnancy and lactation.

Carefully:

Diabetes mellitus, metabolic acidosis, hypoglycemia; allergic reactions in the anamnesis, chronic obstructive pulmonary disease (including bronchial asthma, emphysema); CHF (compensated), obliterating peripheral vascular diseases ("intermittent" lameness, Raynaud's syndrome); pheochromocytoma, hepatic insufficiency, chronic renal insufficiency, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis, pregnancy, advanced age, age under 18 years (efficacy and safety not determined).

Dosing and Administration:

Inside, before eating, without chewing and washing down with a small amount of liquid.

Arterial hypertension. Treatment begins with 12.5 mg Estecor 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 25 or 50 mg once a day. Further increase in the dose is not recommended, since it is not accompanied by an increase in the clinical effect.

Heart rhythm disturbances and prevention of angina attacks. The initial dose is 12.5 mg per day.If the optimal therapeutic effect is not achieved within a week, the dose is increased to 25 or 50 mg per day.

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

In elderly patients the initial single dose is 12.5 mg (can be increased under the control of blood pressure, heart rate).

An increase in the daily dose of more than 50 mg is not recommended, as the therapeutic effect is not increased, and the likelihood of side effects increases.

Patients on hemodialysis, Estecor is prescribed but 25 mg / day immediately after each dialysis, which must be performed under steady-state conditions, since there may be a decrease in blood pressure.

Side effects:

From the nervous system: asthenia, weakness, dizziness, headache, drowsiness or insomnia, nightmarish dreams, depression, anxiety, confusion, or short-term memory loss, hallucinations, decreased concentration, decreased reaction rate, paresthesia in the extremities (in patients with "intermittent "lameness and Raynaud's syndrome), myasthenia gravis, convulsions.

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

From the cardiovascular system: bradycardia, palpitation, conduction disturbance of the myocardium, AV blockade (up to cardiac arrest), arrhythmias, weakening of myocardial contractility, development (aggravation) of CHF, orthostatic hypotension, manifestations of angiospasm (cooling of the lower extremities, Raynaud's syndrome), vasculitis, chest pain.

From the digestive system: dry mouth, nausea, vomiting, abdominal pain, constipation or diarrhea, changes in taste.

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

From the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), a hypothyroid condition.

Allergic reactions: itching, rash, hives.

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

Laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of "hepatic" enzymes, hyperbilirubinemia.

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

Other: pain in the back, arthralgia, weakening of libido, decreased potency, 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: severe bradycardia, dizziness, excessive decrease in blood pressure, syncope, arrhythmia, ventricular extrasystole, AV blockade II-III st, CHF, cyanosis of the fingernails or palms, 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; with CHF - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam; with bronhospazme - inhalation or parenteral - beta-adrenostimulyatory. It is possible to conduct hemodialysis or hemoperfusion.

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 radiocontrast drugs (LS) for intravenous administration increase the risk of anaphylactic reactions.

Phenytoin with intravenous administration of drugs for inhalation of general anesthesia (derivatives of hydrocarbons) increases the severity of cardiodepressive action and the likelihood of lowering blood pressure.

When administered concomitantly with insulin and oral hypoglycemic drugs, it masks the symptoms of developing hypoglycemia.

Reduces the clearance of lidocaine and xanthines (except diprofilina) and increases their concentration in blood plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

Hypotensive effect weakens non-steroidal anti-inflammatory drugs (delay Na+ and synthesis blockade Pg kidneys), glucocorticosteroids and estrogens (delay Na+).

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

Diuretics, clonidine, sympatholytics, hydralazine, BCCI and other antihypertensive drugs can lead to excessive blood pressure lowering.

Lengthens the effect of nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics increase the depression of the central nervous system.

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.

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.

Special instructions:

Control of patients taking Estecor 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 (once every 4-5 months).

In elderly patients it is recommended to follow the function of the kidneys (once every 4-5 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.

Approximately 20% of patients with angina pectoris β-adrenoconvertors 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 (LV LV), which breaks 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 Estekor can mask certain clinical signs of thyrotoxicosis (for example, 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 admission may be terminated only a few days after the abolition of Estecor.

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 with chloroform or ether should stop taking the drug. If the patient has taken the drug before the operation, he should choose a medicine for general anesthesia with a minimum negative inotropic effect. Reciprocal activation n.vagus can be eliminated in / in the administration of atropine (1-2 mg).

Drugs that reduce catecholamine stores (for example, reserpine), can enhance the action of beta-blockers, so patients who take such combinations of funds should be under constant medical supervision to detect a marked decrease in blood pressure or bradycardia.

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

In the case of an increased bradycardia (less than 50 beats per minute), 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. 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 should be abolished before the study of blood and urine levels of catecholamines, normetanephrine and vanillylmandelic acid; titers of antinuclear antibodies.

It is necessary to regulate the dose of the drug for kidney diseases.

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

During the treatment period, care must be taken when driving a motor vehicle and doing other activities.potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, 12.5 mg, 25 mg and 50 mg.

Packaging:

For 14 tablets in strips of aluminum foil.

2 strips together with instructions for use in a cardboard box.

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 expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005120/08

Date of registration:LSR-005120/08

The owner of the registration certificate:AKTAVIS GROUP, AO AKTAVIS GROUP, AO Iceland

Manufacturer: & nbsp

EMCURE PHARMACEUTICALS Ltd India

Representation: & nbspAktavis, Open Company Aktavis, Open Company

Information update date: & nbsp01.10.2015

Illustrated instructions

Instructions

Estecor (Estecor)