Atenolol-Belupo pills coated 50mg N30
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Active ingredients
Atenolol
Release form
Pills
Composition
Atenolol 50 mg adjuvants: microcrystalline cellulose, lactose monohydrate, povidone, maize starch, talc, colloidal silicon dioxide, croscarmellose sodium, magnesium stearate.
Pharmacological effect
It has antianginal, antihypertensive and antiarrhythmic effects. Does not possess membrane stabilizing and internal sympathomimetic activity. Reduces catecholamine-stimulated formation of cAMP from ATP. During the first 24 hours after oral administration, a decrease in cardiac output leads to a reactive increase in the total peripheral vascular resistance, the severity of which gradually decreases within 1-3 days. The hypotensive effect is associated with a decrease in cardiac output and a decrease in renin activity -angiotensin system, sensitivity of baroreceptors and effects on the central nervous system. The hypotensive effect is manifested in both a decrease in systolic and diastolic blood pressure, a decrease in stroke and minute volumes. In moderate therapeutic doses, it does not affect the tone of the peripheral arteries. The antihypertensive effect lasts 24 hours, with regular use it stabilizes by the end of the second week of treatment. The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening diastole and improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic stimulation. Trimming heart rate at rest and during exercise. By increasing the end-diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles can increase the need for oxygen, especially in patients with chronic heart failure. The antiarrhythmic effect manifests itself in suppressing sinus tachycardia and is associated with the elimination of arrhythmogenic sympathetic effects on the cardiac conduction system, a decrease in speed the spread of excitation through the sinoatrial node and lengthening of the refractory period.Inhibits conduction of impulses in antegrade and to a lesser extent - in retrograde directions through the AV node and along additional pathways. The negative chronotropic effect appears 1 hour after administration, reaches a maximum after 2-4 hours, lasts up to 24 hours. Reduces the automatism of the sinus node , slows heart rate, slows AV conductivity, reduces myocardial contractility, reduces myocardial oxygen demand. Reduces the excitability of the myocardium. When used in moderate therapeutic doses it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.
Pharmacokinetics
Absorption from the gastrointestinal tract is fast, incomplete (50-60%). Bioavailability - 40-50%. The time to reach Cmax in the blood plasma is 2-4 hours. It penetrates the BBB poorly, passes in small quantities through the placental barrier and into breast milk. Communication with plasma proteins - 6-16%. Practically not metabolized in the liver. T1 / 2 - 6-9 h (increased in elderly patients). Excreted by the kidneys by glomerular filtration (85-100% - unchanged). Violation of the kidney function is accompanied by T1 / 2 lengthening and cumulation: with QC below 35 ml / min / 1.73 m2 T1 / 2 is 16-27 h, with QC below 15 ml / min / 1.73 m2 - more than 27 hours (reduction of doses is necessary). Excreted during hemodialysis.
Indications
- arterial hypertension; - prevention of angina attacks (with the exception of Prinzmetal stenocardia); - cardiac arrhythmias: sinus tachycardia, prevention of supraventricular tachyarrhythmias, ventricular extrasystole; - acute myocardial infarction with stable hemodynamic parameters.
Contraindications
- hypersensitivity to the drug; - cardiogenic shock; - AV block II and III degree; - severe bradycardia (heart rate less than 45-50 beats / min); - SSS; - sinoauricular block; - acute or chronic heart failure (in decompensation stages); - cardiomegaly without signs of heart failure; - Prinzmetal stenocardia; - arterial hypotension (in case of use for myocardial infarction, systolic blood pressure less than 100 mm Hg); - lactation period; - simultaneous administration of MAO inhibitors; - age 18 years old (efficiency and safety not fixed ovleny) .With caution: diabetes; metabolic acidosis; hypoglycemia; a history of allergic reactions; chronic obstructive pulmonary disease (includingemphysema); AV block I degree; chronic heart failure (compensated); peripheral vascular obliterans (intermittent claudication, Raynaud's syndrome); pheochromocytoma; liver failure; chronic renal failure; myasthenia gravis; thyrotoxicosis; depression (including in the anamnesis); psoriasis; pregnancy; elderly age.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
Pregnant women should be prescribed atenolol only in cases where the benefit to the mother outweighs the potential risk to the fetus. If it is necessary to use atenolol during lactation, it is necessary to decide whether to stop breastfeeding (atenolol is excreted in breast milk).
Dosage and administration
Inside. Appoint inside before food, without chewing, washing down with a small amount of liquid. Arterial hypertension: treatment is begun with 50 mg of Atenolol Belupo 1 time / day. To achieve a stable hypotensive effect requires 1-2 weeks of admission. With insufficient severity of the hypotensive effect, the dose is increased to 100 mg in a single dose. A further increase in the dose is not recommended, since it is not accompanied by an increase in the clinical effect. Stenocardia: the initial dose is 50 mg / day. If the optimal therapeutic effect is not achieved within a week, increase the dose to 100 mg / day. In the presence of renal insufficiency, a dose adjustment is recommended depending on creatinine clearance (CK).In patients with renal failure with QA values above 35 ml / min / 1.73 m2 (normal values are 100-150 ml / min / 1.73 m2), there is no significant cumulation of Atenolol Belupo. Atenolol Belupo is prescribed 50 mg / patient undergoing hemodialysis. immediately after each session of dialysis, which should be carried out in stationary conditions, as there may be a decrease in blood pressure. For elderly patients, the initial single dose is 25 mg (can be increased under the control of blood pressure, heart rate). Acute myocardial infarction with stable hemodynamic and indicators - 100 mg 1 time / day or 50 mg 2 times / day for 6–9 days or until discharge from the hospital (controlled by blood pressure, ECG, blood glucose level). Increasing the daily dose of more than 100 mg is not recommended, because the therapeutic effect is not enhanced, and the likelihood of side effects increases.
Side effects
From the side of the cardiovascular system: development (aggravation) of symptoms of chronic heart failure (swelling of ankles, feet; shortness of breath), impaired atrioventricular conduction, arrhythmia, bradycardia, marked reduction in blood pressure, orthostatic hypotension, palpitations, impaired myocardial conduction, alleviation of myocardial myocardial infarction, myocardial contractility, myocardial contractility, myocardial contraction angiospasm (cooling of the lower limbs, Raynaud's syndrome), vasculitis, chest pain. For the central nervous system and peripheral nervous system: dizziness, decreased ability to concentrate and attention, slow reaction, drowsiness or insomnia, depression, hallucinations, fatigue, headache, weakness, nightmares, anxiety, confusion or short-term memory loss, paresthesias in the extremities (in patients with intermittent claudication and Raynaud's syndrome), muscular weakness, convulsions. From the digestive system: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation, change in taste. From the respiratory system: dyspnea, bronchospasm, apnea, nasal congestion. Hematologist ical reactions: platelet purpura, anemia (aplastic), thrombosis. From the endocrine system: gynecomastia, reduced potency, decreased libido, hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin),hypothyroid state. Metabolic reactions: hyperlipidemia. Skin reactions: urticaria, dermatitis, pruritus, photosensitivity, increased sweating, skin hyperemia, exacerbation of the course of psoriasis, reversible alopecia. Sensory organs: blurred vision, reduced tearing fluid, dryness and illness, and. Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia. From the laboratory parameters: agranulocytosis, leukopenia, increased activity of liver enzymes, hyperbilirubinemia, tro mbocytopenia (unusual bleeding and hemorrhage). Others: back pain, arthralgia, withdrawal syndrome (increased angina attacks, increased blood pressure). The frequency of side effects increases with increasing dose of the drug.
Overdose
Symptoms: severe bradycardia, stage II-III AV blockade, increase in heart failure symptoms, excessive blood pressure reduction, difficulty in breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the fingernails or palms of the fingernails or palms, cramps. Treatment: gastric lavage and prescription adsorbing drugs; in the event of bronchospasm, inhalation or intravenous administration of beta2-adrenomimetica salbutamol is indicated. In violation of AV-conduction, bradycardia - in / in the introduction of 1-2 mg of atropine, epinephrine or staging a temporary pacemaker; with ventricular extrasystole - lidocaine (class 1A drugs are not used); with a decrease in blood pressure, the patient should be in the Trendelenburg position. If there are no signs of pulmonary edema - in / in plasma-substituting solutions, with the ineffectiveness - the introduction of epinephrine, dopamine, dobutamine; in chronic heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam. Dialysis is possible.
Interaction with other drugs
With simultaneous use of atenolol with insulin, oral hypoglycemic drugs, their hypoglycemic effect is enhanced. When used in combination with antihypertensive drugs of different groups or nitrates, the hypotensive effect is enhanced. The simultaneous use of atenolol and verapamil (or diltiazem) can cause mutual enhancement of the cardiodepressive action. The hypotensive effect weakens estrogens (sodium retention), NSAIDs, GCS. With the simultaneous use of atenolol and cardiac glycosides, the risk of developing bradycardia and impaired AV conduction increases. with reserpine,Methyldopa, clonidine, verapamil may cause severe bradycardia. Simultaneous IV injection of verapamil and diltiazem may cause cardiac arrest; nifedipine can lead to a significant decrease in blood pressure. When co-administered with atenolol and ergotamine derivatives, xanthine is less effective. When you stop the combined use of atenolol and clonidine, clonidine is continued for several days after the withdrawal of atenolol. Simultaneous use of lidocaine can reduce its elimination and increase the risk of toxic action of lidocaine. The use together with derivatives of phenothiazine helps to increase the concentration of each of the drugs in serum. enithoin with the on / in the introduction, drugs for general anesthesia (hydrocarbon derivatives) increase the severity of the cardiac depressive effect and the likelihood of lowering blood pressure. When used together with aminophylline and theophylline, mutual suppression of therapeutic effects is not recommended. Simultaneous use of MAO inhibitors is not recommended due to a significant increase in the hypotensive effect , a break in treatment between taking MAO inhibitors and atenolol should be at least 14 days. Allergens used for the immunothera Pii, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis. Means for inhalation anesthesia (hydrocarbon derivatives) increase the risk of inhibition of myocardial function and development of arterial hypertension. Amiodarone increases the risk of developing bradycardia and inhibition of AV conduction. Cimetidine increases plasma concentration (inhibits metabolism). Iodine-containing radiopaque drugs for intravenous injections increase risk of anaphylactic reactions. Extends the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Tri-and tetracyclic antidepressants s, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs enhance inhibition TsNS.Pri simultaneous use of insulin and oral hypoglycemic agents masks symptoms developing gipoglikemii.Negidrirovannye ergot alkaloids to increase the risk of development of peripheral krovobrascheniya.
special instructions
Monitoring patients receiving Atenolol Belupo should include monitoring of heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), blood glucose in diabetic patients (1 time in 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months). Patients should be trained in how to calculate heart rate and instruct on the need for medical consultation with heart rate less than 50 beats / min. During thyrotoxicosis, atenolol can mask certain clinical signs of thyrotoxicosis (for example , tachycardia). Sharp cancellation in patients with thyrotoxicosis is contraindicated, as it can strengthen the symptoms. In case of diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-adrenergic blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal concentration. In patients with CHD, abrupt withdrawal of beta-adrenergic blockers may cause an increase in the frequency or severity of angina attacks, so stopping atenolol in patients CHD should be carried out gradually. Compared with non-selective beta-blockers, cardio-selective beta-blockers have less effect on the function lungs, however, with obstructive respiratory diseases Atenolol Belupo is prescribed only in case of absolute indications. If necessary, use of beta2-adrenomimetics can be recommended in some cases. Patients with bronchospastic diseases can be prescribed cardio-selective adrenergic blockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but it should strictly follow the dosage. Overdose is dangerous for the development of bronchospasm. Special attention is needed in cases where surgical intervention is required under anesthesia in patients taking atenolol. The drug should be stopped 48 hours before the intervention. As an anesthetic, a drug with possibly minimal negative inotropic effects should be chosen. When atenolol and clonidine are used simultaneously, atenolol is stopped for several days before clonidine in order to avoid the symptom of the latter being canceled. allergic history. Drugs that reduce the supply of catecholamines (eg, reserpine),can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect pronounced reduction in blood pressure or bradycardia. In case of elderly patients, bradycardia is growing (less than 50 beats / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction, reduce the dose or stop treatment. It is recommended to stop If you need intravenous verapamil, this should be done no less than 48 hours after taking atenolol. When using atenolol, a reduction in the production of tear fluid is possible, which is important in patients using contact lenses. abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks. and more (reduce the dose by 25% in 3-4 days). It should be abolished before the study content in the blood and urine of catecholamines, normetanephrine and vanillyl almond acid; titers of antinuclear antibodies. In smokers, the effectiveness of beta-blockers is lower. The effect on the ability to drive vehicles and control mechanisms. During the period of treatment, it is necessary to refrain from practicing potentially dangerous activities that require increased concentration and psychomotor speed.