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

Other Ingredients: Povidone K25 - 5.00 mg or 10.00 mg, sodium lauryl sulfate - 1.50 mg or 3.00 mg, corn starch - 30.25 mg or 60.50 mg, pregelatinized starch (corn starch 1500) - 30.25 mg or 60.50 mg, lactose monohydrate 30.90 mg or 61.80 mg, silicon dioxide colloidal anhydrous 1.50 mg or 3.00 mg, magnesium stearate 0.60 mg or 1.20 mg. The total weight of the tablet is 150.00 mg or 300.00 mg.

Description:

Round biconvex tablets of white color with a risk on one side and labeling "C24" (50 mg dosage) and "C25" (100 mg dosage).

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B.03 Atenolol

Pharmacodynamics:

Cardioselective beta 1-adrenoblocker does not possess membrane-stabilizing and internal sympathomimetic activity. Has antihypertensive, anti-anginal and antiarrhythmic effect. Blocking at low doses beta1-adrenoreceptors of the heart, reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic action (tends heart rate (heart rate), inhibits conduction and excitability, reduces myocardial contractility).

The total peripheral vascular resistance at the beginning of beta-blockers (in the first 24 hours after ingestion) 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 initial one after 1-3 days, and after prolonged the appointment is reduced.

Hypotensive effect is associated with a decrease in minute volume of blood flow, decreased activity of the renin-angiotensin-aldosterone system (higher for patients with initial hypersecretion renin) baroreceptor sensitivity of the aortic arch (not going to increase their activity in response to a decrease in blood pressure) and the effect on the central nervous system . The hypotensive effect is manifested by a decrease in both systolic and diastolic arterial pressure, a decrease in the specific volume of blood flow and the minute volume of blood flow. 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.

Antianginal effect determined by the reduction of myocardial oxygen demand by decreasing the heart rate (diastole elongation and improving myocardial perfusion) and contractility and decreased sensitivity to the effects of myocardial sympathetic innervation. It reduces the heart rate at rest and under physical exertion. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers Ventricles can increase the need for oxygen, especially in patients with chronic heart failure.

Antiarrhythmic effect is caused by 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 sinus and ectopic pacemakers and slowing of atrioventricular conduction. Oppression of impulses is noted predominantly in the antegrade and to a lesser extent in the retrograde direction through the atrioventricular node and along additional pathways. Increases the survival rate of patients who underwent myocardial infarction (reduces the incidence of ventricular arrhythmia and angina attacks).

Virtually does not weaken the bronchodilating effect of isoproterenol.

In contrast to nonselective beta-blockers, when administered at moderate therapeutic doses, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus), and carbohydrate metabolism; the severity of atherogenic action does not differ from that of propranolol.To a lesser extent, it 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 is manifested 1 hour after admission, reaches a maximum after 2-4 hours and lasts up to 24 hours.

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (50-60%), bioavailability - 40-50%, solubility in fats is very low. The time to reach the maximum concentration - 2-4 hours. Poorly penetrates the blood-brain barrier, passes 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 (a decrease in doses is necessary): when creatinine clearance is less than 35 ml / min / 1.73 m2, the elimination half-life is 16-27 hours, with QC 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 for Prinzmetal angina pectoris)

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

Contraindications:

Hypersensitivity to the drug, cardiogenic shock, atrioventricular block II-III degree, pronounced bradycardia (heart rate less than 40 beats / min.), sinus node weakness syndrome, sinoatrial block, acute heart failure or decompensated chronic heart failure, cardiomegaly without symptoms of chronic heart failure, angina prinzmetala, arterial hypotension (in case of use in infarction myocardium, systolic blood pressure (BP) less than 100 mm Hg), lactation period, simultaneous administration of monoamine oxidase inhibitors (MAO), age to 18 years (efficacy and b Safety not established).

Carefully:

Diabetes mellitus, metabolic acidosis, hypoglycemia, allergic reactions in history, chronic obstructive pulmonary disease (including bronchial asthma, emphysema), chronic heart failure (compensated),obliterating diseases of peripheral vessels ("intermittent" lameness, Raynaud's syndrome); pheochromocytoma, hepatic insufficiency, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including in the anamnesis), psoriasis, pregnancy, advanced age.

Pregnancy and lactation:

When pregnancy should be prescribed Atenolol Stada® only in cases where the benefit to the mother exceeds the potential risk to the fetus. Atenolol Stada® is excreted in breast milk, therefore, during the period of breastfeeding the use of the drug is contraindicated.

Dosing and Administration:

Inside before meals, do not chew, drink a small amount of liquid.

Arterial hypertension

Treatment is started with 50 mg of the drug Atenolol Stada® once a 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 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 optimal effect is not achieved within a week, increase the dose to 100 mg per 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 US. In patients with renal insufficiency, the values of CS are above 35 ml / min / 1.73 m² (the normal values are 100-150 ml / min / 1.73 m²) significant cumulation of the drug Atenolol Stada® 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
		100 mg every other day
less than 15	more than 27	50 mg every other day
		100 mg once every four days

Patients on hemodialysis, Atenolol Stada® is prescribed at 25 or 50 mg / day immediately after each dialysis session, which should be done in a hospital setting, since a drop in blood pressure may occur.

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

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 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, palpitations, violation conduction of the myocardium, atrioventricular blockade (up to cardiac arrest), arrhythmias, weakening of myocardial contractility, development of chronic heart failure, 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 insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status.

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 depression of blood pressure, syncope, arrhythmia, ventricular extrasystole, atrioventricular block II-III degree, chronic heart failure, cyanosis of the fingernails or palms, convulsions, difficulty breathing, bronchospasm.

Treatment: gastric lavage and administration of absorbent drugs; with violation of atrioventricular conduction and / or bradycardia - intravenous injection of 1-2 mg of atropine, epinephrine (epinephrine) or setting up 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 chronic heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam; with bronhospazme - inhalation or parenteral - beta-adrenostimulyatory. Dialysis is possible.

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 agents 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 cardio-depressive 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 (except diphylline) 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, atrioventricular 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 inhibition 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 atenololShould include monitoring of heart rate and blood pressure (at the beginning of treatment - daily, then 1 every 3-4 months), the content of blood glucose in patients with diabetes mellitus (1 every 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 50 beats per minute.

Approximately 20% of patients with angina 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, which violate the 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 should stop taking the drug. If the patient has taken the drug before the operation, he should choose medicines for general anesthesia with a minimally 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 drugs should be under constant medical supervision to detect a marked decrease in blood pressure or bradycardia.

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

In the case of elderly patients with increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mmHg), atrioventricular blockade, bronchospasm, ventricular arrhythmias,severe violations of the liver and kidneys need 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.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets of 50 mg and 100 mg.

Packaging:

10 tablets per blister of aluminum foil and polyvinyl chloride film.

2, 3, 5 or 10 blisters together with instructions for medical use of the drug are placed in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.Do not use the drug after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015683 / 01

Date of registration:17.03.2009

Expiration Date:Unlimited

Date of cancellation:2017-08-25

The owner of the registration certificate:SHTADA Artznajmittel AGSHTADA Artznajmittel AG Germany

Manufacturer: & nbsp

ALLPHAMED PHARBIL ARZNEIMITTEL, GmbH Germany

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp08.10.2017

Illustrated instructions

Instructions

Atenolol SHTADA® (Atenolol STADA®)