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

Excipients: cellulose microcrystalline 76 mg and 151 mg, corn starch 67 mg and 133 mg, silicon dioxide colloid 2 mg and 4 mg, sodium carboxymethyl starch 10 mg and 20 mg, magnesium stearate 3 mg and 6 mg, talc 3 mg and 6 mg, purified water up to 210 mg and up to 419 mg.

Composition of the film shell: hypromellose 4 mg and 8 mg, titanium dioxide 1 mg and 2 mg, propylene glycol 0.25 mg and 0.5 mg, talc 0.15 mg and 0.3 mg.

Description:

For a dosage of 50 mg - even on both sides round biconvex, rounded from white to almost white, coated with a film membrane;

For a dosage of 100 mg - even on both sides oblong white to almost white tablets coated with a film shell.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B.03 Atenolol

Pharmacodynamics:

Cardioselective beta-blocker, does not possess membrane-stabilizing and internal sympathomimetic activity (SMA). Has antihypertensive, anti-anginal and antiarrhythmic effect. Blocking low-dose (less than 100 mg / day) beta 1-adrenoreceptors of the heart, reduces the stimulated catecholamines formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces intracellular calcium current, has a negative chrono-, dromo-, batmo- and inotropic effect (tends heart rate (heart rate), inhibits conduction and excitability, reduces myocardial contractility).

The total peripheral vascular resistance (OPSS) at the beginning of beta-blockers (in the first 24 hours after oral administration) increases (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 original one to three days later, and with a prolonged appointment decreases.

The hypotensive effect is associated with a decrease in the minute volume of blood (IOC), a decrease in the activity of the renin-angiotensin-aldosterone system (is more important for patients with initial hypersecretion of renin), sensitivity of the aortic artery baroreceptors (there is no increase in their activity in response to a decrease in blood pressure )) and influence on the central nervous system (CNS). The hypotensive effect is manifested by a decrease in both systolic and diastolic blood pressure, a decrease in the shock volume of the blood (CR) and IOC. In average therapeutic doses, it has no effect on the tone of peripheral arteries. The hypotensive effect lasts 24 hours, with regular admission 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 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 under physical exertion. By increasing the end diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for oxygen, especially in patients with chronic heart failure (CHF).

Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of the sinus and ectopic pacemaker and slowing of the atrioventricular (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.

Increases the survival rate of patients who underwent myocardial infarction (reduces the incidence of ventricular arrhythmia and angina attacks).

In contrast, non-selective beta-blockers when used in therapeutic doses medium has a less pronounced effect on organs containing beta 2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchial and uterine) and carbohydrate metabolism; severity of atherogenic differs from the action of propranolol. 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 (GIT) - fast, incomplete (50-60%), bioavailability - 40-50%, solubility in fats is very low. Time to reach the maximum concentration (TCmah) in blood plasma - 2-4 hours. Badly penetrates the blood-brain barrier (BBB), 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 (T1 / 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 T1 / 2 prolongation and cumulation (dose reduction is necessary): for creatinine clearance (CK) less than 35 ml / min / 1.73 m² T1 / 2 is 16-27 hours, with CC below 15 ml / min - more than 27 hours, with anuria lengthened to 144 hours. It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

- prevention of angina attacks, except Prinzmetal angina pectoris;

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

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, AV blockade of HI degree, pronounced bradycardia (heart rate less than 40 bpm), sinus node weakness syndrome, sinoatrial block, acute heart failure or decompensated heart failure, cardiomegaly without signs of CHF, angina Prinzmetal, arterial hypotension (in case of infarction myocardium, systolic blood pressure less than 100 mmHg), pheochromocytoma (without simultaneous use of alpha-blockers), lactation period, simultaneous administration of monoamine oxidase inhibitors (MAO), age to 18 years (efficacy and safety not installed).

Carefully:

Diabetes mellitus type 1 and 2, metabolic acidosis, hypoglycemia, allergic reactions in history, chronic obstructive pulmonary disease (COPD); bronchial asthma;emphysema, CHF (compensated), obliterating peripheral vascular diseases ("intermittent" lameness, Raynaud's syndrome); pheochromocytoma, hepatic insufficiency, chronic renal failure (CRF), myasthenia gravis, thyrotoxicosis, depression (including in anamnesis), psoriasis, pheochromocytoma (with simultaneous use with alpha-blockers), pregnancy, advanced age.

Pregnancy and lactation:

In pregnancy, the drug should be used only in cases where the benefit to the mother exceeds the potential risk to the fetus. Atenolol excreted in breast milk, therefore during the period of breastfeeding the use of the drug 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 the drug once a day. To achieve a stable antihypertensive effect, 1-2 weeks of admission is required. If the hypotensive effect is not enough, the dose is increased to 100 mg in one session. 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 1 week, the dose is increased to 100 mg per day. Older patients and concomitant chronic renal failure need correction of the dosing regimen. In the presence of chronic renal failure, dose adjustment is performed depending on the KK score. With SC more than 35 ml / min / 1.73 m² significant cumulation of the drug does not occur.

In chronic renal failure, the following doses are recommended:

KK 15-35 ml / min / 1.73 m² - 50 mg once a day or 100 mg every other day;

QC less than 15 ml / min / 1.73 m² - 50 mg every other day or 100 mg once every 4 days. Patients who are on hemodialysis, the drug is prescribed at 25 or 50 mg / day immediately after each dialysis session, which must be done in a stationary setting, since there may be a marked decrease in blood pressure.

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.

Side effects:

From the side of the central nervous system: asthenia, weakness, dizziness, headache, drowsiness or insomnia, nightmarish dreams, depression, anxiety, confusion or short-term memory loss, hallucinations, decreased concentration, decreased reaction speed, 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, dry and painful eyes, conjunctivitis.

From the side of the cardiovascular system: bradycardia, sensation heart beat, impaired conduction 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: dryness of the oral mucosa, 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 type 2 diabetes), hypoglycemia (in patients receiving insulin), hypothyroidism.

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 "liver" enzymes, hyperbilirubinemia.

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

Other: pain in the back, arthralgia, decreased 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 reduction of blood pressure, syncope, arrhythmia, ventricular extrasystole, AV blockade II-III degree, development or aggravation of CHF, cyanosis of the nails 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 (epinephrine) or the setting of a temporary pacemaker; with ventricular extrasystole - lidocaine (preparations IA class do not apply); with a pronounced decrease in blood pressure, the patient is transferred to 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-adrenomimetiki. Dialysis is possible.

Interaction:

Allergens used for immunotherapy, or allergen extracts for the administration of skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving atenolol.

Iodine-containing radiopaque agents for intravenous (iv) administration increase the risk of anaphylactic reactions.

Phenytoin for IV administration, drugs for inhalation anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

When used simultaneously with insulin and oral hypoglycemic agents atenolol masks the symptoms of developing hypoglycemia.

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

The hypotensive effect weakens non-steroidal anti-inflammatory drugs (sodium ion delay and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (sodium retention).

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 heart failure, bradycardia, AV blockade and cardiac arrest.

Diuretics, clonidine, sympatholytics, hydralazine, blockers of "slow" calcium channels and other antihypertensives can lead to excessive decrease in 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 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 receiving atenolol, should include monitoring of heart rate and blood pressure (at the beginning of treatment - every day, then once in 3-4 months), the concentration of blood glucose in patients with type 1 and type 2 diabetes (1 every 4-5 months). In elderly patients it is recommended to monitor 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 50 beats per minute.

Approximately in 20% of patients with angina pectoris beta-blockers 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 that violate subendocardial blood flow. In "smokers" the effectiveness of beta-blockers is lower. Patients who use contact lenses should take into account that a reduction in tear fluid production is possible against the background of treatment.

With thyrotoxicosis atenolol can mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, as 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 abolition of atenolol.

It is possible to increase the severity of the allergic reaction and the lack of effect from the usual doses of epinephrine (adrenaline) against the background of a weighed allergic anamnesis.

A few days before the general anesthesia with chloroform or ether Diethyl is necessary to stop taking the drug. If the patient has accepted

the drug before the operation, it should choose the medicines for general anesthesia with minimal negative inotropic action.

Reciprocal activation of the vagus nerve can be eliminated by intravenous injection 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 drugs should be under constant medical supervision to detect a marked decrease in blood pressure or bradycardia.

The drug can be given to patients with bronchospastic diseases in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but it is necessary to take minimal effective doses and monitor patients for possible development of bronchospasm.

In the case of an increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg) 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% every 3-4 days).

It is necessary to cancel the drug before examining the blood and urine content of catecholamines, normetanephrine and vanillylmandelic acid, antiserum antibody titer (for 1 -2 days).

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

During the treatment period, care must be taken when driving vehicles and taking other potentially dangerous speciesactivities that require increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets, film-coated 50 mg and 100 mg.

Packaging:For 30 tablets in a container of polypropylene, together with a glued instruction for use or 10 tablets in an AL / PVC blister. 3 blisters together with instructions for use in a cardboard bundle.

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 expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008843/10

Date of registration:30.08.2010

Expiration Date:Unlimited

The owner of the registration certificate:Agio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd. India

Manufacturer: & nbsp

AGIO PHARMACEUTICALS, Ltd. India

Representation: & nbspAgio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd.

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Atenolol-Agio (Atenolol-Agio)