Atenolol Nikomed

General characteristics. Structure:

Active agent of an atenolol of 50 or 100 mg, and also excipients: propylene glycol, talc, gelatin, methylhydroxypropyl-cellulose 15 Wednesday (Е 464), sodium lauryl sulfate, magnesium stearate, starch corn, heavy carbonate of magnesium. Dyes: titanium dioxide (E171).

Description
Tablets, coated, 50 mg: white color, with a biconvex surface, a kapsulovidny form, with risky for a break and with AB 55 overprint on one party.
Tablets, coated, 100 mg: white color, with a biconvex surface, a kapsulovidny form, with risky for a break and with AB 57 overprint on one party.

Pharmacological properties:

Pharmacodynamics. Has anti-anginal, anti-hypertensive and antiarrhytmic effect. Has no membrane stabilizing and internal sympathomimetic activity. Reduces stimulated catecholamines formation of tsAMF from ATP. In the first 24 hours after oral administration against the background of decrease in cordial emission reactive increase in the general peripheric resistance of vessels which expressiveness within 1 - 3 days gradually decreases is noted.
The hypotensive effect is connected with reduction of cordial emission, decrease of the activity a renin-angiotenzinovoy of system, sensitivity of baroreceptors and influence on the central nervous system. Hypotensive action is shown as decrease in the systolic, and diastolic arterial pressure (AP), reduction shock and ми nutny volumes. In average therapeutic doses does not exert impact on a tone of peripheral arteries. The hypotensive effect proceeds 24 h, at regular use is stabilized by second week of treatment.
The anti-anginal effect is defined by decrease in need of a myocardium for oxygen as a result of reduction of heart rate (lengthening of a diastole and improvement of perfusion of a myocardium) and contractility, and also decrease in sensitivity of a myocardium to impact of sympathetic stimulation. Urezhayet the heart rate (HR) at rest and at an exercise stress. Due to increase in end diastolic pressure in a left ventricle and increases in stretching of muscle fibers of ventricles can increase oxygen requirement, especially at patients with chronic heart failure.
Antiarrhytmic action is shown by suppression of sinus tachycardia and is connected with elimination of aritmogenny sympathetic influences on the carrying-out system of heart, reduction of speed of spread of activation through a sinuatrial node and lengthening of the refractory period. Carrying out impulses in antegrade oppresses and. to a lesser extent in retrograde the directions through AV (atrioventricular) node and on additional ways of carrying out.
The negative chronotropic effect is shown in 1 h after reception, reaches a maximum later 2-4 h, proceeds to 24 h.
Reduces automatism of a sinus node, urezhat ChSS, conductivity slows down AV, reduces contractility of a myocardium, reduces the need of a myocardium for oxygen. Reduces excitability of a myocardium.
At use in average therapeutic doses exerts less expressed impact on smooth muscles of bronchial tubes and peripheral arteries, than non-selective beta adrenoblockers.

Pharmacokinetics. Absorption from digestive tract - bystry, incomplete (50-60%). bioavailability of-40-50%. time of achievement of the maximum concentration in a blood plasma - 2-4 h Badly gets through a gematoentsefalicheky barrier, passes in insignificant quantities through a placental barrier and in breast milk. Communication with proteins of a blood plasma - 6-16%. Practically it is not metabolized in a liver. An elimination half-life - 6-9 h (increases at patients of advanced age). It is removed by kidneys by glomerular filtering (85-100% in not changed look). The renal failure is followed by lengthening of an elimination half-life and cumulation: at clearance of creatinine it is lower than 35 ml/min. / 1,73 of sq.m an elimination half-life makes 16-27 h, at clearance of creatinine it is lower than 15 ml/min. / 1,73 of sq.m - more than 27 h (reduction of doses is necessary). It is removed during a hemodialysis.

Indications to use:

• arterial hypertension;
• prevention of attacks of stenocardia (except for Printsmetal's stenocardia);
• disturbances of a cordial rhythm: sinus tachycardia, prevention of supraventricular tachyarrhythmias.

Route of administration and doses:

Appoint inside before food, without chewing, washing down with a small amount of liquid.
Arterial hypertension. Treatment begin with 50 mg Atenolola Nikomed 1 time a day. Achievement of stable hypotensive effect requires 1 - 2 weeks of reception. At insufficient expressiveness of hypotensive effect the dose is raised to 100 mg in one step. Further increase in a dose is not recommended as it is not followed by strengthening of clinical effect.
Stenocardia. The initial dose makes 50 mg a day. If within a week the optimum therapeutic effect is reached, increase a dose to 100 mg a day. Increase in a dose up to 200 mg is sometimes possible once a day. Correction of the mode of dosing is necessary for patients of advanced age and patients with disturbances of secretory function of kidneys. In the presence of a renal failure recommend dose adjustment depending on clearance of creatinine. Patients with a renal failure at values of clearance of creatinine have higher than 35 ml/min. / 1,73m2 (normal values make 100-150 ml/min. / 1,73 sq.m) considerable cumulation of an atenolol does not occur.
The following maximum doses for patients with a renal failure are recommended:

Clearance of creatinine     Elimination half-life    Maximum dose
(ml/min. / 1.73 sq.m)          atenolol (h)
15-35                           16-27                              50 mg a day or 100 mg every other day
less than 15                      more than 27                         50 mg every other day or 100 mg of 1 times in 4 days

To the patient, the being pas a hemodialysis, Atenolol Nikomed appoint 50 mg/days right after carrying out each dialysis that needs to be carried out in stationary conditions as decrease in the ABP can take place.
Elderly patients have an initial single dose - 25 mg (it can be increased under control of the ABP, ChSS).

Features of use:

Control of the patients accepting Atenolol Nikomed has to include observation of ChSS and the ABP (in an initiation of treatment - daily, then 1 time in 3-4 months), the content of glucose of blood at patients with a diabetes mellitus (1 time in 4-5 months). At elderly patients it is recommended to monitor function of kidneys (1 times in 4-5 months).
It is necessary to train the patient in a technique of calculation of ChSS and to instruct about need of medical consultation at ChSS less than 50 уд. / min.
At a thyrotoxicosis Atenolol Nikomed can mask certain clinical signs of a thyrotoxicosis (for example, tachycardia). Sharp cancellation at patients with a thyrotoxicosis is contraindicated as it is capable to strengthen symptomatology. At a diabetes mellitus can mask the tachycardia caused by a hypoglycemia. Unlike non-selective beta adrenoblockers practically does not strengthen the hypoglycemia caused by insulin and recovery of content of glucose in blood to normal concentration does not detain.
With the coronary heart disease (CHD) sharp cancellation of beta adrenoblockers can cause increase in frequency or weight of anginal attacks therefore the reception termination Atenolola Nikomed at ischemic heart disease patients needs to be carried out gradually in patients. In comparison with non-selective beta adrenoblockers. cardioselective beta adrenoblockers possess smaller impact on function of lungs, nevertheless, at obstructive respiratory diseases Atenolol Nikomed appoint only in case of absolute indications. In need of their appointment in certain cases it is possible to recommend use of beta2-adrenomimetik.
Patients with bronkhospastichesky diseases can appoint cardioselective adrenoblockers in case of intolerance and/or inefficiency of other hypotensive medicines, but at the same time it is necessary to watch a dosage strictly. The overdose is dangerous by development of a bronchospasm.
The special attention is necessary in cases if surgical intervention under anesthetic is required from the patients accepting Atenolol Nikomed. Administration of drug should be stopped in 48 hours prior to intervention. As anesthetic it is necessary to choose drug with perhaps minimum negative inotropic effect.
At simultaneous use Atenolola Nikomed and a clonidine reception Atenolola Nikomed is stopped for several days before a clonidine for the purpose of avoidance of a symptom of cancellation of the last.
Strengthening of expressiveness of hypersensitivity reaction and lack of effect of usual doses of Epinephrinum against the background of the burdened allergological anamnesis is possible.
The medicines reducing stocks of catecholamines (for example, Reserpinum), can strengthen effect of beta adrenoblockers. therefore the patients accepting such combinations of medicines have to be under constant observation of the doctor regarding identification of the expressed decrease in the ABP or bradycardia.
In case of emergence in patients of advanced age of the accruing bradycardia (less than 50 уд. / mines), arterial hypotension (systolic the ABP is lower than 100 mm hg), an atrioventricular block, a bronchospasm, ventricular arrhythmias, heavy abnormal liver functions and kidneys it is necessary to reduce a dose or to stop treatment.
It is recommended to stop therapy at development of the depression caused by reception by beta adrenoblockers.
In case of need intravenous administration of verapamil it should be done in not less than 48 hours after reception Atenolola Nikomed.
At use Atenolola Nikomed reduction of products of the lacrimal liquid is possible that matters at the patients using contact lenses.
It is impossible to interrupt sharply treatment because of danger of development of heavy arrhythmias and a myocardial infarction. Cancellation is carried out gradually, reducing a dose during 2 weeks and more (lower a dose by 25% in 3-4 days).
It is necessary to cancel before a research of content in blood and urine of catecholamines. normetanefrin and vanililmindalny acid; credits of antinuclear antibodies.
At smokers efficiency of beta adrenoblockers is lower.
Pregnancy and period of feeding by a breast. Pregnant women should appoint атенолол only when the advantage for mother exceeds potential risk for a fruit. Atenolol is allocated with breast milk therefore during feeding it should be accepted only in exceptional cases and carefully.

Side effects:

Cardiovascular system: development (aggravation) of symptoms of chronic heart failure (puffiness of anklebones, feet; asthma), disturbance of atrioventricular conductivity, arrhythmia, bradycardia. the expressed decrease in the ABP, orthostatic hypotension, heartbeat.
Central nervous system: dizziness, decline in the ability to concentration of attention, reduction in the rate of reaction, drowsiness or sleeplessness, a depression, hallucinations, increased fatigue, a headache, weakness, "dreadful" dreams, concern, confusion of consciousness or short-term loss of memory, paresthesia in extremities (at patients with the "alternating" lameness and Reynaud's syndrome), muscular weakness, spasms.
Digestive tract: dryness in a mouth, nausea, vomiting, a diarrhea, abdominal pains, a lock, taste change.
Respiratory system: диспноэ, bronchospasm, apnoea, nose congestion.
Hematologic reactions: platelet purpura, anemia (aplastic), thrombosis;
Endocrine system: a gynecomastia, decrease in a potentiality, decrease in a libido, a hyperglycemia (at patients with a non-insulin-dependent diabetes mellitus), a hypoglycemia (at the patients receiving insulin), a hypothyroid state.
Metabolic reactions: lipidemia.
Skin reactions: urticaria, dermatitis, itch, photosensitivity, sweating strengthening, dermahemia, aggravation of a course of psoriasis, reversible alopecia.
Sense bodys: vision disorder, reduction of secretion of the lacrimal liquid, dryness and morbidity of eyes, conjunctivitis.
Influence on a fruit: pre-natal growth inhibition, hypoglycemia, bradycardia.
Laboratory indicators: agranulocytosis, leukopenia, increase in activity of "hepatic" enzymes, hyperbilirubinemia.
Others: dorsodynia, arthralgia, syndrome of "cancellation" (strengthening of attacks of stenocardia, increase in the ABP).
Frequency of by-effects increases at increase in a dose of drug.

Interaction with other medicines:

At simultaneous use of an atenolol with insulin, peroral hypoglycemic medicines - their gipoglikemiziruyushchy action amplifies. At combined use to anti-hypertensive means of different groups or nitrates there is strengthening of hypotensive action. Simultaneous use of an atenolol and verapamil (or diltiazem) can cause mutual strengthening of cardiodepressive action.
The hypotensive effect is weakened by estrogen (a sodium delay) and non-steroidal anti-inflammatory drugs, glucocorticosteroids.
At simultaneous use of an atenolol and cardiac glycosides the risk of development of bradycardia and disturbance of atrioventricular conductivity increases.
At co-administration of an atenolol with Reserpinum, metildopy, a clonidine, verapamil developing of the expressed bradycardia is possible.
Simultaneous in/in administration of verapamil and diltiazem can provoke a cardiac standstill; nifedipine can lead to considerable decrease in the ABP.
At a concomitant use of an atenolol with derivatives of ergotamine, xanthine, its efficiency decreases.
At the termination of the combined use of an atenolol and a clonidine treatment by a clonidine is continued by some more days after cancellation of an atenolol.
Simultaneous use with lidocaine can reduce its removal and increase risk of toxic effect of lidocaine.
Use together with derivatives of a fenotiazin. promotes increase in concentration of each of drugs in blood serum.
Phenytoinum at in introduction, medicines for the general anesthesia (derivatives of hydrocarbons) increase expressiveness of cardiodepressive action and probability of decrease in the ABP.
At combined use with an Euphyllinum and theophylline, perhaps mutual suppression of therapeutic effects.
Simultaneous use with MAO inhibitors owing to considerable strengthening of hypotensive action is not recommended, having rummaged in treatment between reception of MAO inhibitors and an atenolola has to make not less than 14 days.
The allergens used for an immunotherapy or extracts of allergens for skin tests increase risk of emergence of heavy system allergic reactions or an anaphylaxis.
Means for an inhalation anesthesia (derivatives of hydrocarbons) increase risk of oppression of function of a myocardium and development of arterial hypertension. Amiodaronum increases risk of development of bradycardia and oppression of AV of conductivity. Cimetidinum increases concentration in a blood plasma (slows down metabolism). Iodinated X-ray contrast HP for in/in introductions increase risk of development of anaphylactic reactions.
Extends action of not depolarizing muscle relaxants and anticoagulating effect of coumarins.
Rub - and tetracyclic antidepressants, antipsychotic HP (neuroleptics), ethanol, sedative and somnolent medicines strengthen oppression of TsNS.

Contraindications:

Hypersensitivity to drug, cardiogenic shock, atrioventricular (AV) blockade of the II-III Art. the expressed bradycardia (ChSS less than 45-50 уд.мин.), a sick sinus syndrome, a sinoauricular block, acute or chronic heart failure (in a decompensation stage), a cardiomegaly without symptoms of heart failure, Printsmetal's stenocardia, arterial hypotension (in case of use at a myocardial infarction, systolic the ABP less than 100 mm hg), the lactation period, a concomitant use of MAO inhibitors. age up to 18 years (efficiency and safety are not established).

With care: a diabetes mellitus, a metabolic acidosis, a hypoglycemia, allergic reactions in the anamnesis, a chronic obstructive pulmonary disease (including emphysema of lungs). AV the blockade of the I degree, chronic heart failure (compensated), obliterating diseases of peripheral vessels (the "alternating" lameness, Reynaud's syndrome), a pheochromocytoma, a liver failure, a chronic renal failure, a myasthenia, a thyrotoxicosis, a depression (including in the anamnesis), psoriasis, pregnancy, advanced age.

Overdose:

Symptoms: the expressed bradycardia, AV blockade of the II-III degree, increase of symptoms of heart failure, excessive decrease in the ABP, breath difficulty, a bronchospasm, dizziness, a syncope, arrhythmia, ventricular premature ventricular contraction, cyanosis of nails of fingers or palms, spasms.
Treatment: a gastric lavage and purpose of the adsorbing medicines; at emergence of a bronchospasm inhalation or intravenous administration of a beta2-adrenomimetik of salbutamol is shown. At disturbance of AV of conductivity, bradycardia - in/in introduction of 1-2 mg of atropine, Epinephrinum or statement of a temporary pacemaker; at ventricular premature ventricular contraction - lidocaine (the drugs IA of a class are not used); at decrease in the ABP - the patient has to be in the provision of Trendelenburga. If there are no fluid lungs signs - in/in plasma substituting solutions, at inefficiency - introduction of Epinephrinum, dopamine, Dobutaminum; at chronic heart failure - cardiac glycosides, diuretics, a glucagon; at spasms - in/in diazepam. Carrying out dialysis is possible.

Storage conditions:

In dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C. Period of validity of 5 years. Not to use after the date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, on 50 and 100 mg.
On 30 tablets in the plastic bottle corked by the screw-on cover under which the laying with a ring for a separation providing control of the first opening is built in.
Part of the label is attached to a bottle by a special adhesive tape which allows to raise the label. The application instruction is made in the form of the developing leaf placed under a mobile part of the label, the edge of the instruction is fixed to a bottle.