Atenolol of TB. 0,05 No. 30

General characteristics. Structure:

Active ingredient: атенолол. Chemical: 4-[2-Gidroksi-3-[1 methylethyl) amine] propoks] - бензолацетатамид.

Pharmacological properties:

Cardioselective beta1-adrenoblocker, does not possess membrane stabilizing and internal SMA. Has hypotensive, anti-anginal and antiarrhytmic effect. Blocking heart beta1-adrenoceptors in low doses, reduces stimulated catecholamines formation of tsAMF from ATP, reduces intracellular current of Ca2+, renders negative hrono-, dromo-, batmo-and inotropic action (urezhat 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 of alpha adrenoceptors and elimination of stimulation of beta2-receptors) which in 1-3 days is returned to initial, and at long appointment – decreases. The hypotensive effect is connected with reduction of cordial emission, decrease of the activity a system renin-angiotenzinovoy (has bigger value at 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. Hypotensive action is shown as decrease in the systolic, and diastolic ABP, reduction of shock and minute volumes. In average therapeutic doses has no effect on a tone of peripheral arteries. The hypotensive effect proceeds 24 h, at regular reception is stabilized by the end of 2 weeks of treatment. 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. Urezhayet ChSS at rest and at an exercise stress. Due to increase in a tension of muscle fibers of ventricles and end diastolic pressure in a left ventricle can raise an oxygen request, 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 carrying out. Oppression of carrying out an impulse is noted preferential in antegrade and, to a lesser extent, in retrograde the directions through an AV node and on additional ways. Increases survival of the patients who had a myocardial infarction (reduces the frequency of development of ventricular arrhythmias and attacks of stenocardia). Practically does not weaken bronkhodilatiruyushchy action of Isoproterenolum. At use in average therapeutic doses, unlike non-selective beta adrenoblockers, exerts less expressed impact on the bodies containing beta2-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. To a lesser extent causes negative batmo-, hrono-, other, and dromotropic effect. At use in high doses (more than 100 mg/days) renders the blocking effect on both subtypes of beta adrenoceptors. 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 a GIT - bystry, incomplete (50 - 60%), bioavailability - 40-50%, solubility in fats very low. TCmax - 2-4 h Badly gets through GEB, passes through a placental barrier and in breast milk. Communication with proteins of plasma - 6-16%. Practically it is not metabolized in a liver. T1/2 is 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 T1/2 and cumulation: at KK it is lower than 35 mg/min. / 1.73 of sq.m, T1/2 makes 16-27 h, at KK it is lower than 15 ml/min. - more than 27 h, at an anury is extended to 144 h (reduction of doses is necessary). It is removed during a hemodialysis.

Indications to use:

Treatment: An ischemic heart disease, stenocardia (tension, rest and unstable), arterial hypertension, hypertensive crisis, a prolapse of the mitral valve, a hyperkinetic cardial syndrome of functional genesis, neurocirculatory dystonia on hypertensive type, an essential and senile tremor, agitation and a tremor at an abstinence syndrome. Treatment and prevention: a myocardial infarction (an acute phase at stable indicators of a hemodynamics, secondary prevention); disturbances of a rhythm (including at the general anesthesia, an inborn syndrome of the extended QT interval, a myocardial infarction without symptoms of heart failure, a thyrotoxicosis), sinus tachycardia, Bouveret's atrial disease, supraventricular and ventricular premature ventricular contraction, supraventricular and ventricular tachycardia, a ciliary tachyarrhythmia, trembling and atrial fibrillation. As a part of complex therapy: IGSS, a pheochromocytoma (only together with alpha adrenoblockers), a thyrotoxicosis; migraine (prevention).

Route of administration and doses:

Inside, before meal, without chewing and washing down with a small amount of liquid. An initial dose - 25-50 mg/days; if necessary the dose is raised in 1 week on 50 mg and further if necessary to 200 mg, an average dose - 100 mg/days. At an ischemic heart disease, takhisistolichesky disturbances of a cordial rhythm - 50 mg of 1 times a day. At an acute myocardial infarction with stable hemodynamic indicators - in 12 h - repeatedly 50 mg; further - on 50 mg 2 times a day within 6-9 days (under control of the ABP, an ECG, concentration of glucose). At a hyperkinetic cardial syndrome appoint 25 mg/days. At KK of 10-30 ml/min. appoint 100 mg every other day or 50 mg/days; at KK less than 10 ml/min. - 50 mg every other day, or 100 mg of 1 times in 4 days, or against the background of a hemodialysis on 50 mg after each dialysis. Elderly patients have an initial single dose - 25 mg (it can be increased under control of the ABP, ChSS). Appointment more than 1 time a day is not reasonable as атенолол works during 24 h. Increase in a daily dose over 100 mg is not recommended since the therapeutic effect amplifies, and the probability of development of side effects increases. The maximum daily dose makes 200 mg. The dose decline in case of the planned cancellation is made gradually, on 1/4 doses by each 3-4 days.

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 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/min. Approximately at 20% of patients with stenocardia beta adrenoblockers are not effective. The main reasons - heavy coronary atherosclerosis with a low threshold of ischemia (ChSS less than 100/mines) and the increased final diastolic pressure of a left ventricle breaking a subendocardial blood stream. At smokers efficiency of beta adrenoblockers is lower. The patients using contact lenses have to consider that against the background of treatment reduction of products of the lacrimal liquid is possible. At a thyrotoxicosis атенолол can disguise certain clinical signs of a hyperthyroidism (for example, tachycardia). Sharp cancellation at patients with a thyrotoxicosis is contraindicated as it is capable to strengthen symptomatology. At a diabetes mellitus can disguise the tachycardia caused by a hypoglycemia. Unlike non-selective beta adrenoblockers practically does not strengthen the hypoglycemia caused by insulin and recovery of concentration of glucose of blood to normal level does not detain. At a concomitant use of a clonidine its reception can be stopped only in several days after cancellation of an atenolol. Strengthening of expressiveness of reaction of hypersensitivity and lack of effect of usual doses of Epinephrinum against the background of the burdened allergological anamnesis is possible. For several days before carrying out the general anesthesia chloroform or ether it is necessary to stop administration of drug. If the patient accepted drug before operation, it should pick up drug with the minimum negative inotropic effect. Reciprocal activation of a vagus nerve can be eliminated in/in administration of atropine (1-2 mg). 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. Patients with bronkhospastichesky diseases can appoint cardioselective adrenoblockers in case of intolerance and/or inefficiency of other hypotensive drugs, but at the same time it is necessary to watch a dosage strictly. The overdose is dangerous by development of a bronchospasm. In case of emergence in patients of advanced age of the accruing bradycardia (less than 50/mines), arterial hypotension (systolic the ABP is lower than 100 mm hg), AV of blockade, 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. It is impossible to interrupt sharply treatment from - for dangers 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). Use at pregnancy and a lactation is possible if the advantage for mother exceeds risk of development of side effects in a fruit and the child. During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. For the period of treatment to exclude ethanol reception. It is necessary to cancel before a research of content in blood and urine of catecholamines, a normetanefrin and vanililmindalny acid; credits of antinuclear antibodies. At smokers efficiency of beta adrenoblockers is lower.

Side effects:

From a nervous system: increased fatigue, weakness, dizziness, a headache, drowsiness or sleeplessness, nightmares, a depression, concern, confusion of consciousness or short-term loss of memory, a hallucination, easing of ability to concentration of attention, reduction in the rate of reaction, paresthesia in extremities (at patients with the "alternating" lameness and Reynaud's syndrome), muscular weakness, spasms. From sense bodys: vision disorder, reduction of secretion of the lacrimal liquid, dryness and morbidity of eyes, conjunctivitis. From CCC: bradycardia, heartbeat, disturbance of conductivity of a myocardium, AV blockade (up to a cardiac standstill), arrhythmias, easing of contractility of a myocardium, development (aggravation) of heart failure (puffiness of anklebones, feet; asthma), orthostatic hypotension, manifestations of a vasomotor spasm (cold snap of the lower extremities, Reynaud's syndrome), vasculitis, stethalgia. From the alimentary system: dryness of a mouth, nausea, vomiting, abdominal pain, diarrhea, lock, taste changes. From respiratory system: a nose congestion, difficulty of breath at appointment in high doses (selectivity loss) and/or at predisposed patients - laringo-and a bronchospasm. From endocrine system: a hyperglycemia (at patients with an insulinonezavisimy diabetes mellitus), a hypoglycemia (at the patients receiving insulin), a hypothyroid state. Allergic reactions: itch, rash, urticaria. From integuments: sweating strengthening, dermahemia, aggravation of symptoms of psoriasis, proriazopodobny skin rashes, reversible allopecia. Laboratory indicators: thrombocytopenia (unusual bleedings and hemorrhages), agranulocytosis, leukopenia, increase in activity of "hepatic" enzymes, hyperbilirubinemia. Influence on a fruit: pre-natal growth inhibition, hypoglycemia, bradycardia. Others: dorsodynia, arthralgia, weakening of a libido, decrease in a potentiality, 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:

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 hypotension. Amiodaronum increases risk of development of bradycardia and oppression of AV of conductivity. Changes efficiency of insulin and peroral hypoglycemic means, masks symptoms of the developing hypoglycemia (tachycardia, increase in the ABP). Increases concentration of lidocaine in plasma (reduces its clearance). Hypotensive effect NPVP (a delay of sodium and blocking of synthesis of Pg kidneys) weaken, estrogen (a sodium delay). BMKK (verapamil, diltiazem), cardiac glycosides and antiarrhytmic means increase risk of development or aggravation of AV of blockade and development of heart failure. Simultaneous in/in administration of verapamil and diltiazem can provoke a cardiac standstill; nifedipine – can lead to considerable decrease in the ABP. Phenytoinum at in introduction, means for the general anesthesia increases expressiveness of cardiodepressive action. Diuretics, a clonidine, sympatholytics, гидралазин, etc. can lead antihypertensives to excessive hypotension. Methyldopum, Reserpinum and гуанфацин increase risk of development of bradycardia and arterial hypotension. Cimetidinum increases concentration in plasma (slows down metabolism). Iodinated radiopaque substances for in/in introductions increase risk of development of anaphylactic reactions. Reduces clearance of xanthines (except Diphyllinum), especially at patients with initially increased clearance of theophylline under the influence of smoking. Prolongs action of not depolarizing muscle relaxants, anti-coagulative effect of coumarins. Rub - and tetracyclic antidepressants, neuroleptics, sedative, hypnagogues and ethanol strengthen oppression of TsNS. 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.

Contraindications:

Hypersensitivity, cardiogenic shock, AV blockade of the II-III St, bradycardia about ChSS less than 40/mines, SSSU, SA blockade, 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. With care - a diabetes mellitus, a metabolic acidosis, a hypoglycemia; allergic reactions in the anamnesis, HOBL (including bronchial asthma, emphysema of lungs); the chronic heart failure (compensated), obliterating diseases of peripheral vessels (the "alternating" lameness, Reynaud's syndrome); pheochromocytoma, liver failure, HPN, myasthenia, thyrotoxicosis, depression (including in the anamnesis), psoriasis, pregnancy, advanced age, children's age (efficiency and safety are not defined).

Overdose:

Symptoms: the expressed heavy bradycardia, dizziness, excessive decrease in the ABP, a faint, arrhythmia, ventricular premature ventricular contraction, AV blockade of the II-III St, heart failure, cyanosis of nails of fingers or palms, spasms, breath difficulty, a bronchospasm.

Treatment: a gastric lavage and purpose of the adsorbing means; at disturbance of AV of conductivity - 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 arterial hypotension - 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 heart failure – cardiac glycosides, diuretics, a glucagon; at spasms - in/in diazepam; at a bronchospasm - it is inhalation or parenterally - beta адреностимуляторы. Carrying out dialysis is possible.

Issue conditions:

According to the recipe

Packaging:

In packaging of 30 tablets on 50 mg of an atenolol in everyone.