Atenolol

General characteristics. Structure:

Active ingredient: атенолол 100 mg

Pharmacological properties:

Cardioselective beta1-adrenoblocker without internal sympathomimetic activity. Renders anti-hypertensive, anti-anginal, and antiarrhytmic action.

Reduces the stimulating influence on heart of a sympathetic innervation and the catecholamines circulating in blood. Possesses negative hrono-, dromo-, batmo-and inotropic action: reduces ChSS, conductivity and excitability oppresses, reduces contractility of a myocardium. OPSS at the beginning of use of beta adrenoblockers (in the first 24 h after oral administration) increases (as a result of reciprocal increase of activity? - adrenoceptors and elimination of stimulation? 2 adrenoceptors), in 1-3 days are returned to initial, and at prolonged use decrease.

The hypotensive effect is connected with reduction of minute volume of blood, decrease of the activity a system renin-angiotenzinovoy (has bigger value for patients with initial hypersecretion of a renin), sensitivity of baroreceptors of an aortic arch (there is no strengthening of their activity in response to decrease in the ABP) and influence on TsNS; it is shown by decrease in both the systolic, and diastolic ABP, reduction of a stroke output and minute volume. In average therapeutic doses does not exert impact on a tone of peripheral arteries.

The anti-anginal effect is defined by decrease in need of a myocardium for oxygen as a result of reduction of ChSS (lengthening of a diastole and improvement of perfusion of a myocardium) and contractility, and also decrease in sensitivity of a myocardium to influence of a sympathetic innervation. Reduction of ChSS happens 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.

The antiarrhytmic effect is caused by elimination of aritmogenny factors (tachycardia, a superactivity of a sympathetic nervous system, the increased maintenance of tsAMF, arterial hypertension), reduction of speed of spontaneous excitement of sinus and ectopic pacemakers and delay of AV of conductivity. Oppression of carrying out impulses is noted preferential in antegrade and to a lesser extent in retrograde the directions through an AV node and on additional ways.

Unlike non-selective beta adrenoblockers, at use in average therapeutic doses exerts less expressed impact on the bodies containing? 2 adrenoceptors (a pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchial tubes and a uterus), and on carbohydrate metabolism; expressiveness of atherogenous action does not differ from effect of propranolol. Other and dromotropic action is to a lesser extent expressed negative batmo-, hrono-. At use in high doses (more than 100 mg/) causes blockade of both subtypes? - adrenoceptors.

Hypotensive action continues 24 h, at regular reception 2 weeks of treatment are stabilized by the end. Negative chronotropic effect is shown in 1 h after reception, reaches a maximum later 2-4 h and continues to 24 h.

 

Pharmacokinetics. After intake absorption makes of a GIT 50-60%, bioavailability - 40-50%. Practically it is not metabolized in an organism. Badly gets through GEB. Linkng with proteins of plasma - 6-16%.

T1/2 makes 6-9 h. It is removed mainly by kidneys in not changed look. Renal failures are followed mainly by increase in T1/2 and cumulation: at KK less than 35 ml/min. of T1/2 make 16-27 h, at KK less than 15 ml/min. - more than 27 h, at an anury is extended to 144 h. It is removed during a hemodialysis.

At patients of advanced age of T1/2 increases.

Indications to use:

Arterial hypertension, hypertensive crisis, prolapse of the mitral valve, hyperkinetic cardial syndrome of functional genesis, neurocirculatory dystonia on hypertensive type.

Treatment: Ischemic heart disease, stenocardia (tension, rest and unstable).

Treatment and prevention: a myocardial infarction (an acute phase at stable indicators of a hemodynamics, secondary prevention).

Arrhythmias (including at the general anesthesia, an inborn syndrome of the extended QT interval, a myocardial infarction without symptoms of chronic heart failure, a thyrotoxicosis), sinus tachycardia, Bouveret's atrial disease, supraventricular and ventricular premature ventricular contraction, supraventricular and ventricular tachycardia, a ciliary tachyarrhythmia, an atrial flutter.

Essential and senile tremor, agitation and tremor at an abstinence syndrome.

As a part of complex therapy: a hypertrophic obturatsionny cardiomyopathy, a pheochromocytoma (only together with alpha adrenoblockers), a thyrotoxicosis; migraine (prevention).

Route of administration and doses:

Establish individually. The usual dose for adults - inside, in an initiation of treatment makes 25-50 mg of 1 times/days If necessary a dose gradually increase. At a renal failure to patients with KK of 15-35 ml/min. - on 50 mg/days; at KK less than 15 ml/min. - on 50 mg every other day.

Maximum dose: the adult at intake - 200 mg / in 1 or 2 receptions.

Features of use:

With care it is necessary to apply at a diabetes mellitus, HOBL (including bronchial asthma, emphysema of lungs), a metabolic acidosis, a hypoglycemia; allergic reactions in the anamnesis, chronic heart failure (compensated), obliterating diseases of peripheral arteries (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, at pregnancy, at patients of advanced age, in pediatrics (efficiency and safety are not defined).

At use of an atenolol reduction of products of the lacrimal liquid is possible that matters for the patients using contact lenses.

Cancellation of an atenolol after a long course of treatment should be carried out gradually under observation of the doctor.

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, otherwise developing of the expressed arterial hypertension is possible.

In need of carrying out an inhalation anesthesia at the patients receiving атенолол some days before carrying out an anesthesia it is necessary to stop reception of an atenolol or to pick up anesthetic with the minimum negative inotropic effect.

Influence on ability to driving of motor transport and to control of mechanisms

At patients whose activity demands the increased concentration of attention the issue of out-patient use of an atenolol should be resolved only after assessment of individual reaction.

Side effects:

From cardiovascular system: in some cases - bradycardia, arterial hypotension, AV conductivity disturbances, emergence of symptoms of heart failure.

From the alimentary system: at the beginning of therapy nausea, locks, diarrhea, dryness in a mouth are possible.

From TsNS and peripheral nervous system: at the beginning of therapy the fatigue, dizziness, a depression, a slight headache, sleep disorders, a cryesthesia and paresthesias in extremities, decrease in reactionary ability of the patient, reduction of secretion of the lacrimal liquid, conjunctivitis are possible.

From endocrine system: decrease in a potentiality, hypoglycemic states at patients with a diabetes mellitus.

From respiratory system: predisposed patients have an emergence of symptoms of bronchial obstruction.

Allergic reactions: skin itch.

Others: sweating strengthening, erubescence.

Interaction with other medicines:

At simultaneous use of diuretics anti-hypertensive action amplifies.

At simultaneous use of means for an inhalation anesthesia the risk of strengthening of cardiodepressive action and development of arterial hypotension increases.

There are messages on development of bradycardia and arterial hypotension at simultaneous use a chloride alkuroniya.

At simultaneous use of verapamil negative inotropic effect amplifies, bradycardia, a bradyarrhythmia, the expressed conductivity disturbances develops; cases of postural hypotension, dizziness, a left ventricular failure, a lethargy are described. Under the influence of verapamil pharmacokinetic parameters of an atenolol significantly do not change though the case of increase in AUC of an atenolol is described.

At simultaneous use of Disopyramidum Css raises, the clearance of Disopyramidum decreases, conductivity disturbance is possible.

At simultaneous use of Dipiridamolum the case of development of bradycardia and then asystolias (is described when carrying out the ECG test with Dipiridamolum at the patient receiving атенолол).

At simultaneous use of indometacin, Naproxenum and other NPVS reduction of anti-hypertensive action of an atenolol that is to some extent caused by disturbance (under the influence of NPVS) synthesis in kidneys and release in a blood stream of PGA and PGE prostaglandins which render strong vazodilatiruyushchy effect on peripheral arterioles is possible.

At simultaneous use of insulin increase in the ABP is possible.

At simultaneous use of a clonidine the additive hypotensive effect, sedative action, dryness in a mouth is possible.

At simultaneous use of caffeine reduction of efficiency of an atenolol is possible.

At simultaneous use of a nizatidin the case of strengthening of cardiodepressive action is described.

At simultaneous use of nifedipine cases of the expressed arterial hypotension and heart failure are described that can be caused by strengthening of the oppressing influence of nifedipine on a myocardium.

At simultaneous use of an orlistat anti-hypertensive action of an atenolol decreases that can lead to substantial increase of the ABP, development of hypertensive crisis.

At simultaneous use of Prenylaminum increase in an interval of QT is possible.

At simultaneous use of Chlortalidonum anti-hypertensive action amplifies.

Contraindications:

AV blockade of II and III degrees, sinuatrial blockade, SSSU, bradycardia, (ChSS less than 40 уд. / mines), arterial hypotension (in case of use at a myocardial infarction, systolic the ABP less than 100 mm hg), cardiogenic shock, chronic heart failure of IIB-III of a stage, an acute heart failure, Printsmetal's stenocardia, the lactation period, a concomitant use of MAO inhibitors, hypersensitivity to an atenolol.

Use at pregnancy and feeding by a breast
Atenolol gets through a placental barrier therefore use at pregnancy is possible only if the estimated advantage for mother exceeds possible risk for a fruit.

Atenolol is allocated with breast milk therefore in need of use in the period of a lactation it is recommended to stop breastfeeding.

Issue conditions:

According to the recipe

Packaging:

10 pieces - planimetric strip packagings (3) - packs cardboard.
15 pieces - planimetric strip packagings (2) - packs cardboard.