Atenolol

General characteristics. Structure:

Active ingredient: 50 mg or 100 mg of an atenolol in 1 tablet.

Excipients: magnesium carbonate the main, starch corn, potato starch, magnesium stearate, talc.

Pharmacological properties:

Pharmacodynamics. Atenolol has anti-hypertensive, anti-anginal and antiarrhytmic effect. Atenolol reduces automatism of a sinus node, reduces heart rate at loading and at rest, slows down atrioventricular conductivity, reduces contractility and excitability of a myocardium, cordial emission, the need of a myocardium for oxygen and, thereby, significantly improves cordial activity.

Pharmacokinetics. Atenolol - badly soluble beta-blocker in lipids. After intake drug is quickly soaked up from digestive tract - about 50% of the dose accepted inside. The rest is allocated in not changed view with excrements and a small amount of drug gets through a blood-brain barrier.

Linkng with proteins of plasma is minimum. Atenolol is not metabolized or exposed to an insignificant metabolization in a liver and is brought, mainly, by kidneys.

Indications to use:

Angina of exertion, arterial hypertension; secondary prevention at the patients who had a myocardial infarction.

Route of administration and doses:

Inside before food, without chewing, washing down with a small amount of water.

At gipertenzii:naznachat once 50-100 mg. The stable effect is reached in 1-2 weeks. The further lowering of arterial pressure can be reached by a combination with other means, for example, diuretics.

At stenocardia: an initial dose – 50 mg a day. If the optimum effect is not reached within the first week, it is recommended to appoint a dose of 100 mg a day once or in stages. Further increase in a dose is inexpedient.

At a myocardial infarction with stable hemodynamic indicators: inside, in 10 min. after the last in/in introductions of an atenolol, in a dose of 50 mg, then repeatedly 50 mg in 12 h; further - on 50 mg 2 times a day or on 100 mg once within 6-9 days (under control of arterial pressure, an electrocardiography, content of glucose in blood).

Features of use:

The sudden termination of therapy can lead to an exacerbation of stenocardia, arrhythmias, a myocardial infarction and death. Treatment by beta antagonists reduces cordial emission and can aggravate symptoms of arterial insufficiency at patients with diseases of peripheral or mezenterialny vessels. Beta адренэргическая blockade can "mask" some clinical manifestations of a hyperthyroidism (tachycardia), its sudden cancellation can provoke thyrocardiac crisis.

Because атенолол it is removed by kidneys, at heavy renal failures dose adjustment is necessary. The patient with clearance of creatinine of 15-35 ml/min. appoint in a dose 50 mg a day or 100 mg once every other day, it is lower than 15 ml/min. - 50 mg every other day or to 100 mg there are once each four days. The patient who is on a hemodialysis appoint in 50 mg after each session of dialysis in the conditions of a hospital since the expressed hypotension is possible.

There is no experience of use of an atenolol in children's practice therefore children are not recommended to appoint it.

At surgical intervention it is necessary to observe a 48-hour interval between reception of the last dose of an atenolol and the beginning of anesthesia. It is necessary to be careful at use of ether, cyclopropane, trichloroethylene. The disturbances connected with dominance of a tone of a vagus nerve are adjusted by atropine (1-2 mg in/in).

When drug has to be excluded from the established scheme of treatment, it is recommended to reduce doses gradually for minimizing of risk of an exacerbation of stenocardia or development of a myocardial infarction. It is necessary to reduce doses within about 2 weeks. At this time the patient has to avoid the increased physical activity.

Pregnancy and feeding by a breast. Atenolol gets through a placental barrier, it is found in umbilical cord blood, collects in breast milk. In this regard drug do not appoint pregnant as it can cause a fruit growth inhibition. For the period of treatment it is necessary to stop breastfeeding.

Patients, with allergic reactions of anaphylactic type to any substance, the accepting beta-blockers, can answer with heavier course of allergic reaction to repeated administration of allergen (accidental, diagnostic or medical). Such patients can not react to usual doses of the adrenaline applied to stopping of allergic reaction.

Side effects:

Bradycardia, cold snap of extremities, postural hypotension, onychalgia, dizziness, prostration, fatigue, lethargy, drowsiness, depression, hallucinations, nausea, diarrhea, skin rashes, xerophthalmus.

At patients of advanced age thorax pain, confusion of consciousness are possible a dorsodynia or joints. Seldom the leukopenia, orthostatic hypotension meet (dizziness upon transition to vertical position from situation <lying> or <sitting>).

At use of high doses there can be a decrease in sexual function, unusual fatigue or weakness.

Interaction with other medicines:

Meal does not influence absorption of an atenolol.

Atenolol it is necessary to appoint with care: with antiarrhytmic means of the I class (Disopyramidum, etc.); along with verapamil - the patient with disturbance of atrioventricular conductivity not to appoint, and after cancellation another it is not necessary to administer one drug intravenously during 48 h!

Care is necessary at transfer of the patient from a clonidine on blockers of beta adrenoceptors. At their simultaneous use атенолол it is necessary to cancel some days before gradual cancellation of a clonidine.

Drugs, the exhausting stocks of catecholamines (Reserpinum, etc.), have the additive effect at their co-administration with atenololy. Including drugs for cold and vasoconstrictive drops in a nose, lead the combined use of an atenolol and alpha and adrenergic stimulators to strengthening of hypertensive reaction.

Cyclooxygenase inhibitors, for example, indometacin, can reduce hypotensive effect of an atenolol. Simultaneous use of cardiac glycosides and an atenolol is followed by reduction of atrioventricular conductivity, heart rate, increases risk of development of bradycardia.

Influence on ability to drive the car and to work with other mechanisms. Disturbance of ability of patients is improbable to drive the car or to work with the equipment at drug use. However it is necessary to take the fact that dizziness and fatigue can take place into account.

Contraindications:

Absolute: the congestive heart failure which is not compensated by cardiac glycosides and diuretics; sinus bradycardia, arterial hypotension (systolic arterial pressure of 100 mm Hg and below), sick sinus syndrome, atrioventricular block of II and III degrees, cardiogenic shock; pregnancy.

Relative: bronchial asthma and heavy obstructive respiratory insufficiency, the alternating lameness and Reynaud's syndrome, an insulin-dependent diabetes mellitus, not treated pheochromocytoma.

Overdose:

Symptoms: bradycardia, AV blockade of II and III degrees, heart failure, hypotonia, bronchospasm, hypoglycemia.

Treatment: symptomatic, the expressed bradycardia is stopped atropine (1-2 mg in/in), and if necessary stimulators of beta adrenoceptors (изопреналин - on 25 mkg in/in, slowly) or ortsiprenaliny (0,5 mg in/in, slowly). Use of cardiac glycosides and a glucagon is shown; installation of an artificial pacemaker.

Storage conditions:

In the place protected from light and moisture, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

10 tablets in a blister strip packaging, in packaging No. 10×3 together with a leaf insert.