Atenolol - Akri®

General characteristics. Structure:

Active ingredient: 50 mg or 100 mg of an atenolol.

Excipients: starch corn, magnesium hydroxycarbonate, povidone, gelatin medical, magnesium stearate, sodium starch glycollate.

Drug which has anti-anginal, anti-hypertensive and antiarrhytmic effect.

Pharmacological properties:

Pharmacodynamics. Has no membrane stabilizing and internal sympathomimetic activity. Reduces stiyomulirovanny catecholamines formation of tsAMF from ATP, reduces intracellular current of calcium ions. In the first 24 h after oral administration against the background of decrease in cordial emission reactive increase in the general peripheric resistance of vessels which vyrazhenyonost within 1-3 days gradually decreases is noted.

The hypotensive effect is connected with reduction of cordial emission, decrease in an aktivnoyosta a renin-angiotenzinovoy of system, sensitivity of baroreceptors and influence on a tsenyotralny nervous system. Hypotensive action is shown as decrease in sistolicheyosky, and diastolic arterial pressure, reduction of shock and minute volumes. In average therapeutic doses does not exert impact on a tone of peripheral aryoteriya. The hypotensive effect proceeds 24 h, at regular use стабилизирует­ся 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 a vozyodeystviye of sympathetic stimulation. Urezhayet heart rate at rest and at an exercise stress. Due to increase in a tension of muscle fibers of ventricles and konechyony diastolic pressure in a left ventricle 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, umensheyoniy speeds of spread of activation through a sinuatrial node and lengthening of the refyorakterny period. Carrying out impulses in antegrade and, to a lesser extent, in retrograde the directions through AV (atrioventricular) node and on additional ways of carrying out oppresses.

Increases survival of the patients who had a myocardial infarction (reduces the frequency of development of ventricular arrhythmias and attacks of stenocardia). Slightly reduces the zhizyonenny capacity of lungs, practically does not weaken bronkhodilyatiruyushchy action of Isoproterenolum.

In therapeutic concentration does not influence _{beta2-adrenoceptors}, unlike non-selective beta adrenoblockers exerts less expressed impact on a smooth musyokulatura of bronchial tubes and peripheral arteries and on lipidic exchange. At reception more than 100 mg a day can have _{beta2-adrenoceptor blocking} effect.

The negative chronotropic effect is shown in 1 h after reception, reaches a maximum later 2-4 h, proceeds to 24 h.

Pharmacokinetics. Absorption from digestive tract - bystry, incomplete (50%), bioavailability - 40-50%, solubility in fats very low. Time of achievement of the maximum concentration in a blood plasma - 2-4 h Badly gets through a gemato-entsefalicheky barrier, passes in neznayochitelny quantities through a placental barrier and in breast milk. Communication with proteins of a plazyoma of blood - 6-16%.

Practically it is not metabolized in a liver. An elimination half-life - 6-9 h (it uvelichivayotsya 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} the period to a floor-vshedeniya makes 16-27 h, at clearance of creatinine it is lower than 15 ml/min. - more than 27 h (a neobkhoyodima correction of doses). 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, ventricular ektrasistoliya, ventricular tachycardia;

- an acute myocardial infarction with stable hemodynamic indicators.

Route of administration and doses:

Appoint inside before food, without chewing, washing down with a small amount of liquid.

Arterial hypertension. Treatment is begun with 50 mg of an atenolol of 1 times a day. The dosyotizheniye of stable hypotensive effect requires 1-2 weeks of reception. At nedostatochyony expressiveness of hypotensive effect the dose is raised to 100 mg in one step. Dalneyyoshy increase in a dose is not recommended as it is not followed by strengthening клиническо­го effect.

Stenocardia. The initial dose makes 50 mg a day. If within a week the optimum therapeutic effect is not 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 a dozirovayoniya is necessary for patients of advanced age and bolyyony 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. / 1,73 ^{the sq.m} (normal values make 100-150 ml/mip/1.73 ^sq.m) znayochitelny cumulation of an atenolol does not occur.

The following maximum doses for patients from a renal nedostatochnoyostyyu are recommended:

Clearance of creatinine (ml/min. / 1,73 sq.m)	Elimination half-life of an atenolol (h)		Maximum dose
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

The patient who is on a hemodialysis, Atenolol - ^{Akri®naznachayut} on 50 mg/days to a srayoz 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, the heart rate (HR)).

Acute myocardial infarction with stable indicators of a gemodinamicheskgsha. In 12 hours - 100 mg of 1 times a day or on 50 mg 2 times a day within 6-9 days (under control of the ABP, an ECG, glucose level in blood).

Features of use:

Monitoring of the patients accepting атенолол 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 bolyyony 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 neobkhodimoyost of medical consultation at ChSS less than 50 уд. / min.

At a thyrotoxicosis атенолол can disguise certain clinical priznayok of a thyrotoxicosis (for example, tachycardia). Sharp cancellation at patients with a thyrotoxicosis of a protiyovopokazan as it is capable to strengthen symptomatology. At a diabetes mellitus can zamaskiyorovat the tachycardia caused by a hypoglycemia. Unlike non-selective beta adrenoblockers practically does not strengthen the hypoglycemia caused by insulin and does not zaderyozhivat recovery of content of glucose in blood to normal level.

With the coronary heart disease (CHD) sharp cancellation of beta adrenoblockers can cause increase in frequency or weight of anginal attacks therefore prekrashcheyony reception Atenolol - ^Akri® at ischemic heart disease patients needs to be carried out gradually in patients.

The special attention is also required by selection of doses at patients with a decompensation of cordial activity. In comparison with non-selective beta adrenoblockers, cardioselective beta adrenoblockers possess smaller impact on function of lungs, nevertheless at obstructive respiratory diseases Atenolol - ^Akri® appoint only in case of absolute indications. In need of their appointment in certain cases it is possible to rekoyomendovat use _{of beta2-adrenomimetik}.

Patients with bronkhospastichesky diseases can appoint cardioselective adrenoblockers in case of intolerance and/or inefficiency of other hypotensive prepayorat, 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 - ^Akri®. 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 Atenolol - ^Akri®i of a clonidine reception Atenolol - ^{Akri®prekrashchayut} for several days before a clonidine for the purpose of avoidance of a symptom of cancellation of the last.

Strengthening of expressiveness of reaction of hypersensitivity and lack of an effekyot from usual doses of Epinephrinum against the background of the burdened allergological anamnesis is possible.

The drugs reducing stocks of catecholamines (for example, Reserpinum), can strengthen effect of beta adrenoblockers therefore the patients accepting such combinations of drugs have to be under constant observation of the doctor regarding detection of arterial hypotension 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), AV of blockade, a bronyokhospazm, 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 of beta adrenoblockers.

In case of need intravenous administration of verapamil it should be done not meyony, than in 48 hours after reception of an atenolol.

At use of an atenolol 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 within 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, holes-metanefrina 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. Ateyonolol is allocated with breast milk therefore during feeding it should be accepted only in exceptional cases and carefully.

Influence on ability to drive the car and to work with the equipment. During treatment не­обходимо to refrain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Cardiovascular system: emergence of symptoms of heart failure, disturbance of atrioventricular conductivity, arrhythmia, bradycardia, the expressed decrease in arterialyyony pressure, orthostatic hypotension, heartbeat, thrombosis.

Central nervous system: dizziness, decline in the ability to concentration of a vniyomaniye, drowsiness, a depression, hallucinations, slackness, feeling of fatigue, a headache, a slayobost, sleeplessness, nightmares, concern, confusion of consciousness or short-term loss of memory, paresthesia in extremities (at patients with the "alternating" lameness and sindroyomy Reynaud), muscular weakness, spasms.

Digestive tract: dryness in a mouth, nausea, vomiting, a diarrhea, abdominal pains, a lock, a taste izyomeneniye.

Respiratory system: диспноэ, bronchospasm, apnoea, nose congestion.

Hematologic reactions: Werlhof's disease, anemia (aplastic).

Endocrine system: a gynecomastia, decrease in a potentiality, decrease in a libido, a hyperglycemia (at patients with a non-insulin-dependent diabetes mellitus). Metabolic reactions: lipidemia, hypoglycemia.

Skin reactions: urticaria, dermatitis, itch, photosensitivity, strengthening potootdeleyoniya, dermahemia, aggravation of a course of psoriasis.

Sense bodys: vision disorder, reduction of secretion of the lacrimal liquid, dryness and bolezyonennost of eyes, conjunctivitis.

Influence on a fruit: pre-natal growth inhibition, hypoglycemia, bradycardia.

Laboratory indicators: agranulocytosis, leukopenia, increase in activity of "hepatic" enzymes, bilirubin level.

Others: dorsodynia and breasts, arthralgia, vasculitis, syndrome of "cancellation" (strengthening of attacks of stenocardia, increase in the ABP).

Interaction with other medicines:

At simultaneous use of an atenolol with insulin, antidiabetic means - 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.<