Atenolol

Chemical name

4-[2-Гидрокси-3-[(1-метилэ тил)амино]пропокси]бе��золацетамид (and in the form of monogidrohlorida)

Gross

C14-H22-N2-O3

Characteristics

Crystalline powder. Rat in the water (26.5 mg / ml, with a temperature of 37 ^ C) well, in 1M hydrochloric acid (300 mg / ml, with a temperature of 25 ^ C) and the bad-in chloroform (3 mg / ml, with a temperature of 25 ^ C).

Of drugs

The drugs-gipotenzivne, antianginalnoe, antiaritmicescoe. Yes blocks beta_1-adrainoretseptora has no мембраностабилизирую щей and internal simpatomimeticescoy activity. Stops central sympathetic impulsaciu weakens the sensitivity of peripheral tissues to kateholaminam, ingibiruet renin secretion. Urejaet HR at rest and with physical activity. Hronotropony negative effect manifests itself after one hour reaches its maximum after 2-4 hours until 24 pm Decreases cordial release, and Sad Dad, reducyruet ortostaticescuu tachycardia. Antihypertensive effect goes on 24 hours off with the regular admission by the end of two weeks. Decreases occurred need of oxygen, but by increasing tension muscle fibers and ventricular end-diastolic pressure in the left jeludocke could increase oxygen request especially in patients with chronic heart failure. Suppress automaticity sinusnogo unit lengthens refrakterny time slowing down for AV node. Increases survival of patients after myocardial infarction (reduced frequency jeludockovh arrhythmias and strokes). Slight decreases life in the lung function, little weakens bronhodilatirtee Izoproterenola.posle the intake of rats about 50% in older people, a slightly higher. C_max is 2-4 h, tying with the plasma protein-6-16%. Poor permeates through GEB passes through the placental barrier, and in breast milk. There is metabolized in the liver, kidneys displayed by clubockova filtering (85%). T_1/2, 6-7 p increases in patients older. Violation of the kidney by elongation and T_1/2 cumulation : if Cl creatinine below 35 mg/min/1 .73 m ^ 2 T_1/2 is 16-27 hrs, in the Cl creatinine less than 15 ml / min, more than 27 hours (to reduce doses). Prolonged use by wakuolizaciei cancer duodenal ulcer from the dogs (15 mg / kg / day) and the development of degenerative processes in miocarde male rats (300 mg / kg / day). In experiments on rats (18 months) and mice (24 months) in the dose of 300 mg / kg / day has no cancer-causing. At doses of 500 and 1500 mg / kg / day (rats) increased the frequency of benign brain tumors layer napochechnikov, adenoma front of pituitary, fibroadenoma breast (female), �арафолликулярно-клет очной carcinoma of the thyroid gland (male). The cytogenetic test (in vivo) and the Ames test revealed no mutagenic properties. The male and female rats dose 100 times greater than MRDC, adverse effect on fertility do not have. The dose of 50 mg / kg / day increased the frequency of rezorbtion embryo / fetus in rats.

Indications

Arterial hypertension, stenocardia, acute myocardial infarction (with stable hemodynamics indicators), tachycardia : sinusova, predserdnaya, ventricular, paroxizmalnaya et al. Arrythmia, fibrillation and began predserdy, giperkineticeski cardialny syndrome, mitral prolapse valve neirocirkulatornaya distonia for gipertonicescomu type; Integrated therapy gipertroficescoy cardiomyopathy, feohromotsytoma, tireotoxicoza, essencialnogo tremora; Migraine (prevention).

Restrictions on the use of

Diabetes mellitus, hypoglycaemia, chronic obstructive lung diseases (emphysema, bronchial asthma), violations of the liver and / or kidneys, male, depression, psoriasis, feohromotsytoma, metabolic acidosis, pregnancy, child (efficiency and security is not defined), and old age.

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, sinusova aetiology (HR less than 50 u. / min), sinoatrialnaya blockade syndrome weakness sinusnogo hub, AV blockade II extent Arterial gipotenzia (Sad less than 90 mm Hg), acute or chronic cardiac insufficiency of the decompensation, cardiogenny shock the peripheral blood, breast-feeding.

Side-Effects

From the nervous system and sensory organs : increased fatigue, weakness, dizziness, headache, drowsiness or insomnia, nightmares, depression, concern sputannosti consciousness or temporary memory loss, hallucinations, relaxation reactivity, paresthesia, convulsions; impaired vision, reducing secretions and saliva slezna fluid Kongunguit.so the circulatory system and blood (blood, gemostaz) : aetiology, rapid heartbeat, the cardiac conductance, AV blockade keep weakening sokratimosti infarction, cardiac failure, gipotenzia, sinkope, the phenomenon Reynaud, vasculit, pain in the chest, B19, Agranulozitoz.so part of the intestine : dryness in the mouth, nausea, vomiting, stomachache, diarrhea, constipation, Violations of the Pecheni.so the respiratory system : dizziness, and laringo- �ронхоспазм.Аллергиче ские reactions : itching, rash, erythema, urticaria, and psoriazopodobne dystrophic changes Koji.prochie : obratimaya alopecia, rash, cooling limbs, male, easing drive, impotence, Peyroni disease, changing enzyme activity, the level of cium, the syndrome, gipotireoidne state hypoglycaemia.

Patient interaction

Antiarrhythmic anaesthetic and the increase cardiodepressivne effects (increased risk of bradikardii, adults, hypotension, congestive heart failure). Reserpine, alfa-metildopa, clonidine, guanfation, heart glycosides potenziruut negative chrono, and dromo- batmotropony effect, insulin and other antidiabetics means-gipoglikemia. NPVS, estrogena, simpatomimetiki, xantina weaken gipotenzivny effects films, the better-simpatolitiki, nitroglycerin, apressin etc. gipotenzivee preparations antatsida-down induction. Zimetidin slowing metabolism. Prolong the antidepoliarizuth miorelaksantov, antikoagulyazionny kumarinov effect. Three / tetratziklicescie antidepressants, neiroleptiki, sedatives, hypnotics, and the alcohol potenziruut oppression CNS. Incompatible with MAO inhibitors.

Overdosing

Symptoms : aetiology, AV blockade degree III, heart failure, breathing problems, gipotenzia, bronhospazm, Gipoglikemia.lechenie : washing stomach, and the appointment of absorbent; symptomatic therapy : atropine, izoprenalin, jortziprenalin, heart or cures glukagon, dioretiki, vazopressornye funds (dopamine, or dobutamin norapinefrin) beta-adrainomimetiki selective, glucose (in / in), the installation of artificial driver rhythm. Perhaps dialysis.

Precautions

Treatment is carried out at regular doctor control. Before starting therapy should be compensated for heart disease. During treatment requires monitoring HR, AD blood glucose (possible correction dose protivodiabeticakih drugs), and control over the appearance of the symptoms of heart Nedostaternsti.s use caution during the the drivers of vehicles and people skills relate to the high concentration of attention. At the time of therapy is recommended that the admission Alkoghola.u patients with diabetes and giperfunkciei thyroid gland may mask tachycardia, gipoglikemiei caused or thyrotoxicosis. In feohromotsytome should simultaneously apply alfa-adrainolitiki. Perhaps greater extent reaction гиперчувствительност и and the lack of economies of the usual doses of epinephrine with aggravated allergologicaki Anamneza.v Where the sick elderly growing bradikardii (less than 1950 u. / min), hypotension (Sad below 100 mm Hg), AV blockade bronchospasm, which jeludockovh arrhythmias, heavy human liver and kidneys, it is necessary to reduce the dose or stop treatment. Termination therapy should be gradual, reducing the dose within 10 to 14 days. Patients with the disease should undergo a period of the drug be monitored carefully. Atenolol should be abolished for 48 h prior to the intervention, using general anesthesia (chloroform or ether), or select anestetik with the least negative effect inotrope.

Dosing and Administration

Inside, the food is not liquid and squeezed few liquid. The mode set individually. In hypertension, 25-50 mg once, by 100-200 mg 1-2 times a day. For details, tahisistoliceskih human heartbeat rhythm is 50 mg once a day; if necessary and good endurance dose can be increased during the week of 100-200 mg / sut. In acute myocardial infarct with stable haemodynamic performance through 12h-second 50 mg; hereinafter referred to as 50 mg twice a day for 6-9 days (under the control of AD ECG, the level of glucose). The functional disorders of the cardiovascular system, 25 mg once a day. If any of the kidneys, depending on Cl creatinine : Cl with 15-35 ml / min-50 mg / day (or 100 mg every other day) less than 15 ml / min, 50 mg every other day (or 100 mg every 4 days); patients in gemodialise, 25-50 mg / day immediately after the dialysis. Older patients initial single dose of 25 mg (can be increased under the control of AD HR).

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