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

gelatin (for a dosage of 50 mg - 2.1 mg, for a dosage of 100 mg - 4.2 mg), sodium lauryl sulfate (for a dosage of 50 mg - 3.3 mg, for a dosage of 100 mg - 6.7 mg), magnesium stearate for dosage of 50 mg to 5.0 mg, for a dosage of 100 mg to 10.0 mg), corn starch (for a dosage of 50 mg to 60.0 mg, for a dosage of 100 mg to 120.0 mg), magnesium carbonate (for dosage 50 mg - 87.5 mg, for the dosage of 100 mg - 175.0 mg).

Shell: propylene glycol (for dosage of 50 mg - about 0.4 mg, for a dosage of 100 mg - about 0.8 mg), titanium dioxide (for a dosage of 50 mg - about 0.8 mg, for a dosage of 100 mg - about 1.7 mg ), talc (for dosage of 50 mg - about 0.8 mg, for dosage of 100 mg - about 1.7 mg), hypromellose (for a dosage of 50 mg - about 2.1 mg, for a dosage of 100 mg - about 4.2 mg ).

Description:

Film coated tablets 50 mg: biconvex, capsular tablets of white color, film-coated, with a risk for fracture and embossing of AB 55.

Film coated tablets 100 mg: biconvex, capsular tablets of white color, film-coated, with a risk for fracture and embossing of AB 57.

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. It has antihypertensive, anti-anginal and antiarrhythmic effects. Blocking in low doses beta1-adrenoreceptors of the heart, reduces catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions, has a negative chrono-,dromo-, batmo- and inotropic action (urezhaet 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.

The antihypertensive 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 (BP) and the influence on the central nervous system.The antihypertensive effect is manifested by a decrease in both systolic and diastolic blood pressure, a decrease in the stroke and minute volume of blood circulation. ednih therapeutic doses has no effect on the tone of the peripheral arteries.Antihypertensive 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 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 at rest and under physical exertion. Due to the increased end-diastolic pressure in the left ventricle and increased stretching of ventricular muscle fibers may increase the need for oxygen, especially in patients with chronic heart failure.

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 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 (AV) node and by additional paths.

Virtually does not weaken the bronchodilating effect of isoprenaline.

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 after 1 hour after administration, reaches a maximum after 2-4 hours, lasts up to 24 hours.

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast, incomplete (45-60%), bioavailability - 40-50%, time to reach the maximum concentration in the blood plasma - 2-4 hours. It penetrates poorly through the blood-brain barrier, passes in small amounts through the placental barrier and into breast milk. The association with plasma proteins is relatively low and is less than 5%.

It is not metabolized in the liver.The half-life of blood plasma is 6-8 hours (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): with creatinine clearance (CC) below 35 ml / min / 1.73 m² the half-life is 16-27 hours, with QC below 15 ml / min - more than 27 hours, with anuria prolonged to 144 hours. It is excreted during hemodialysis.

Indications:

- Arterial hypertension;

- prevention of attacks of stable angina (with the exception of Prinzmetal angina pectoris);

- cardiac rhythm disturbances: sinus tachycardia, prevention of supraventricular tachyarrhythmias, prevention of supraventricular tachyarrhythmias.

Contraindications:

- Hypersensitivity to the drug;

- shock (including cardiogenic and hypovolemic);

- AV blockade II-III degree;

- acute heart failure or decompensated chronic heart failure;

- pronounced bradycardia (heart rate less than 40 beats per minute);

- syndrome of weakness of the sinus node;

- sinoatrial (SA) blockade;

- Cardiomegaly without signs of chronic heart failure;

- angina of Prinzmetal;

- marked hypotension (in the case of myocardial infarction, systolic blood pressure less than 100 mm Hg);

- simultaneous administration of monoamine oxidase inhibitors (MAO);

- lactation period,

- age under 18 years (effectiveness and safety not established);

- pheochromocytoma, with the exception of concomitant therapy with alpha-blockers.

Carefully:

Diabetes mellitus type 1 and 2, metabolic acidosis, hypoglycemia, allergic reactions in history, chronic obstructive pulmonary disease, bronchial asthma, emphysema, AV blockade of I degree, chronic cardiac failure (compensated), obliterating peripheral vascular disease ( "intermittent" claudication, Raynaud syndrome), pheochromocytoma (while the use of alpha blockers), hepatic failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including history) , psoriasis, pregnancy, elderly age.

Pregnancy and lactation:Pregnant women should be prescribed Atenolol Nycomed only in cases where the benefit to the mother exceeds the potential risk to the fetus. Atenolol is excreted in breast milk, so during lactation, if you need to use the drug Atenolol Nycomed, you must stop breastfeeding.

Dosing and Administration:

Assign inside before eating, without chewing, squeezed a small amount of liquid.

Arterial hypertension. Treatment begins with 50 mg of Atenolol Nycomed 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 dose is not recommended, since it is not accompanied by an increase in hypotensive 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 excretory function need a correction of the dosing regimen. In the presence of renal failure recommend correcting the dose depending on the QC. In patients with renal insufficiency with CC values above 35 ml / min / 1.73 m² (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)	Half-life (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

For patients on hemodialysis, Atenolol Nycomed is prescribed 25 or 50 mg / day immediately after each dialysis, which must be done in a hospital setting, 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). 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:

Very frequent (> 1/10); frequent (> 1/100, <1/10); infrequent (> 1/1000, <1/100); rare (> 1/10 000, <1/1 000); very rare (<1/10 000).

From the side of the cardiovascular system

Often: bradycardia, coldness of the lower limbs, hypotension.

Rarely: the development or aggravation of chronic heart failure, AV blockade, arrhythmias, syncope, peripheral edema, chest pain, conduction disorders of the heart,Orthostatic hypotension and syncope, Raynaud's syndrome.

From the central nervous system

Often: asthenia, muscle weakness.

Infrequent: sleep disturbances (drowsiness or insomnia).

Rarely: "nightmarish" dreams, hallucinations, psychoses, depression, confusion or short-term memory loss, anxiety, dizziness, headache, paresthesia of the extremities (in patients with intermittent claudication and Raynaud's syndrome), convulsions, changes in taste.

Very rarely: myasthenia gravis.

From the sense organs

Visual impairment, a decrease in the secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis.

From the endocrine system

Infrequently: can mark symptoms of hyperthyroidism. Hypoglycemia (in patients receiving insulin) or hyperglycemia (in patients with type 2 diabetes mellitus).

From the respiratory system

Rarely: bronchospasm, wheezing, dyspnoea in predisposed patients and / or when taken in high doses (loss of selectivity), nasal congestion.

From the digestive system

Often: nausea, vomiting. Abdominal pain, constipation, or diarrhea.

Rarely: dryness of the oral mucosa, cholestasis.

Laboratory indications

Infrequently: increased activity of "liver" transaminases.

Rarely: thrombocytopenia, agranulocytosis, leukopenia, hyperbilirubinemia.

Very rarely: positive test results for antinuclear antibodies.

From the skin

Rarely: skin rash, reversible alopecia, purpura, exacerbation of psoriasis and skin itching.

Very rarely: a lupus-like syndrome. Psoriasis-like skin rash, hypersensitivity reactions, including angioedema and urticaria.

Other:

Rarely: decreased potency.

Very rarely: decreased libido.

Overdose:

Symptoms: pronounced bradycardia, dizziness, marked decrease in blood pressure, syncope, arrhythmia, ventricular extrasystole, AV blockade II-III degree, chronic heart failure, cyanosis of the nails or palms, convulsions, difficulty breathing, bronchospasm.

Treatment: if violated 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); at expressed reduction 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. Hemodialysis is possible.

Interaction:

With the simultaneous use of atenolol with insulin, hypoglycemic agents for oral administration - the hypoglycemic effect of the latter is enhanced. When combined with hypotensive agents of different groups or nitrates, hypotensive effect is enhanced. The simultaneous use of atenolol and verapamil (or diltiazem) can cause a mutual increase in the effect of these drugs.

The antihypertensive effect is weakened by estrogens (sodium retention) and non-steroidal anti-inflammatory drugs, glucocorticosteroids.

With the simultaneous use of atenolol and cardiac glycosides, the risk of developing bradycardia and violation AV conductivity.

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

Simultaneous intravenous administration of verapamil and diltiazem can provoke 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, medicines for general anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

When combined with euphyllin 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 taking 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.

Means for inhalation anesthesia (derivatives of hydrocarbons) increase the risk of oppression of myocardial function and the development of hypertension.

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

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.

Special instructions:

Control of patients taking Atenolol Nycomed should include monitoring heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), blood glucose concentration 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).

You should teach the patient how to calculate heart rate and instruct you about the need for medical consultation at a heart rate of less than 50 beats per minute.

In thyrotoxicosis, Atenolol Nycomed can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Drastic withdrawal of the drug is contraindicated because it can enhance symptoms. In diabetes mellitus can mask tachycardia caused by hypoglycemia. Unlike non-selective 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), abrupt cancellation of beta-blockers can cause an increase in the frequency or severity of angina attacks, therefore, stopping the use of Atenolol Nycomed in patients with IHD should be gradual. Reduce the dose for two weeks or more.

Compared with non-selective beta-blockers, cardioselective beta-blockers have less effect on lung function, however,at obstructive diseases of respiratory ways Atenolol Nycomed is used only in 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 Nycomed. 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 the drug Atenolol Nycomed and clonidine, the drug Atenolol Nycomed is stopped several days earlier than clonidine in order to avoid the withdrawal syndrome.

It is possible to increase the severity of the reaction of hypersensitivity and the lack of effect from the usual doses of epinephrine against the background of a burdened allergological anamnesis.

Drugs that reduce catecholamine stores (for example, reserpine), can enhance the action of beta-adrenoblockers, so patients who take such combination of medicines, should be under the constant supervision of the doctor for the purpose of revealing the expressed depression of a BP or a bradycardia.

In the case of an increased bradycardia (less than 40 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.

If intravenous verapamil is needed, this should be done at least 48 hours after taking the drug Atenolola Nycomed.

When using the drug Atenolola Nycomed, it is possible to reduce the production of tear fluid, which is important 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 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 (for 1-2 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, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Film coated tablets 50 mg and 100 mg.

Packaging:

For 30 tablets in a plastic bottle sealed with a screw cap, under which a gasket with a tear-off ring is installed, which provides control of the first opening.

One bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:5 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011912 / 01

Date of registration:30.03.2011 / 30.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:Takeda Pharma A / STakeda Pharma A / S Denmark

Manufacturer: & nbsp

TAKEDA, GmbH Germany

Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.

Information update date: & nbsp08.10.2017

Illustrated instructions

Instructions

Atenolol Nycomed (Atenolol Nycomed)