Instructions for use ATENOLOL NYCOMED (ATENOLOL NYCOMED)
Monitoring of patients taking Atenolol Nycomed should include monitoring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), blood glucose levels in patients with diabetes (once every 4-5 months). In elderly patients, it is recommended to monitor kidney function (once every 4-5 months).
The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.
For thyrotoxicosis, Atenolol Nycomed can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal concentrations.
In patients with coronary artery disease, abrupt withdrawal of beta-blockers may cause an increase in the frequency or severity of anginal attacks, therefore, discontinuation of Atenolol Nycomed in patients with coronary artery disease must be carried out gradually.
Compared to non-selective beta-blockers, cardioselective beta-blockers have less effect on pulmonary function, however, for obstructive airway diseases, Atenolol Nycomed is prescribed only in case of absolute indications. If it is necessary to prescribe them, in some cases the use of beta2-adrenergic agonists can be recommended.
Patients with bronchospastic diseases can be prescribed cardioselective adrenergic blockers in case of intolerance and/or ineffectiveness of other antihypertensive drugs, but the dosage should be strictly monitored. An overdose is dangerous due to the development of bronchospasm.
Particular attention is necessary in cases where surgical intervention under anesthesia is required in patients taking Atenolol Nycomed. The drug should be stopped 48 hours before the intervention. As an anesthetic, you should choose a drug with as little negative inotropic effect as possible.
When using Atenolol Nycomed and clonidine simultaneously, Atenolol Nycomed should be stopped a few days before clonidine in order to avoid withdrawal symptoms of the latter.
It is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from usual doses of epinephrine against the background of a burdened allergic history.
Medicines that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a pronounced decrease in blood pressure or bradycardia.
In case of increasing bradycardia (less than 50 beats/min), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction in elderly patients, it is necessary to reduce dose or stop treatment.
It is recommended to discontinue therapy if depression caused by taking beta-blockers develops.
If intravenous administration of verapamil is necessary, this should be done at least 48 hours after taking Atenolol Nycomed.
When using Atenolol Nycomed, it is possible to reduce the production of tear fluid, which is important in patients who use contact lenses. Treatment should not be abruptly interrupted due to the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose over 2 weeks or more (reduce the dose by 25% in 3-4 days).
Should be discontinued before testing the content of catecholamines, normetanephrine and vanillylmandelic acid in the blood and urine; antinuclear antibody titers.
Beta blockers are less effective in smokers.
Atenolol nycomed 100 mg 30 pcs. film-coated tablets
pharmachologic effect
Cardioselective beta1-blocker, does not have membrane stabilizing and internal sympathomimetic activity.
It has antihypertensive, antianginal and antiarrhythmic effects. By blocking beta1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, bathmo- and inotropic effect (reduces heart rate), inhibits conductivity and excitability, reduces myocardial contractility). The total peripheral vascular resistance at the beginning of the use of beta-blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of beta2-adrenergic receptors), which after 1-3 days returns to the original level, and with prolonged use destination is reduced.
The antihypertensive effect is associated with a decrease in minute volume of blood flow, a decrease in the activity of the renin-angiotensin-aldosterone system (of greater importance for patients with initial hypersecretion of renin), the sensitivity of the baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease in blood pressure and an effect on the central nervous system .
The antihypertensive effect is manifested by a decrease in both systolic and diastolic blood pressure, a decrease in stroke and minute volume of blood circulation. In average therapeutic doses it has no effect on the tone of peripheral arteries. The antihypertensive effect lasts 24 hours, and with regular use it stabilizes by the end of 2 weeks of treatment.
The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in the sensitivity of the myocardium to the effects of sympathetic stimulation. Reduces heart rate at rest and during physical activity. By increasing end-diastolic pressure in the left ventricle and increasing the stretch of ventricular muscle fibers, it can increase oxygen demand, especially in patients with chronic heart failure.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown of atrioventricular conduction. Inhibition of impulse conduction is observed predominantly in the antegrade and to a lesser extent in the retrograde directions through the atrioventricular (AV) node and along additional pathways.
Practically does not weaken the bronchodilating effect of isoprenaline.
In contrast to non-selective beta-blockers, when prescribed in average therapeutic doses, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus), and on carbohydrate metabolism; the severity of the atherogenic effect does not differ from the effect of propranolol. To a lesser extent it has a negative bathmo-, chrono-, ino- and dromotropic effect. When used in large doses (more than 100 mg/day), it has a blocking effect on both subtypes of beta-adrenergic receptors.
The negative chronotropic effect appears 1 hour after administration, reaches a maximum after 2-4 hours, and lasts up to 24 hours.
Composition and release form Atenolol nycomed 100 mg 30 pcs. film-coated tablets
Tablets - 1 tablet:
- Active substance: atenolol 100 mg.
- Excipients: gelatin - 4.2 mg, sodium lauryl sulfate - 6.6 mg, magnesium stearate - 10 mg, corn starch - 120 mg, magnesium carbonate - 175 mg.
- Shell composition: propylene glycol - about 800 mcg, titanium dioxide - about 1.7 mg, talc - about 1.7 mg, hypromellose E15 - about 4.2 mg.
30 pcs. - plastic bottles.
Description of the dosage form
White film-coated tablets, capsule-shaped, biconvex, with a break mark and embossed “AB57”.
Directions for use and doses
Prescribed orally before meals, without chewing, with a small amount of liquid.
Arterial hypertension. Treatment begins with 50 mg of Atenolol Nycomed 1 time per day. To achieve a stable hypotensive effect, 1-2 weeks of administration are required. If the hypotensive effect is insufficient, the dose is increased to 100 mg in one dose. Further increase in dose is not recommended, since it is not accompanied by an increase in the hypotensive effect.
Angina pectoris. The initial dose is 50 mg per day. If the optimal therapeutic effect is not achieved within a week, increase the dose to 100 mg per day. Sometimes it is possible to increase the dose to 200 mg once a day. Elderly patients and patients with impaired renal excretory function require adjustment of the dosage regimen. In the presence of renal failure, dose adjustment is recommended depending on QC. In patients with renal failure with CC values above 35 ml/min/1.73 m2 (normal values are 100-150 ml/min/1.73 m2), significant accumulation of atenolol does not occur.
The following maximum doses are recommended for patients with renal failure:
| Creatinine clearance (ml/min/1.73 m2) | Half-life (h) | Maximum dose |
| 15-35 | 16-27 | 50 mg per day 100 mg every other day |
| less than 15 | more than 27 | 50 mg every other day 100 mg once every four days |
For patients undergoing hemodialysis, Atenolol Nycomed is prescribed 25 or 50 mg/day immediately after each dialysis, which must be carried out in a hospital setting, since a decrease in blood pressure may occur. In elderly patients, the initial single dose is 25 mg (can be increased under the control of blood pressure and heart rate). Increasing the daily dose above 100 mg is not recommended, because the therapeutic effect is not enhanced, and the likelihood of side effects increases.
Pharmacokinetics
After oral administration, absorption from the gastrointestinal tract is 50-60%, bioavailability is 40-50%. Practically not metabolized in the body. Poorly penetrates the BBB. Plasma protein binding - 6-16%.
T1/2 is 6-9 hours. It is excreted mainly by the kidneys unchanged. Impaired renal function is accompanied mainly by an increase in T1/2 and cumulation: with CC less than 35 ml/min, T1/2 is 16-27 hours, with CC less than 15 ml/min - more than 27 hours, with anuria it extends to 144 hours. It is excreted during hemodialysis.
In elderly patients, T1/2 increases.
Indications for use Atenolol nycomed 100 mg 30 pcs. film-coated tablets
- Arterial hypertension;
- prevention of attacks of stable angina (with the exception of Prinzmetal's angina);
- heart rhythm disturbances: sinus tachycardia, prevention of supraventricular tachyarrhythmias, prevention of supraventricular tachyarrhythmias.
Contraindications
- Shock (including cardiogenic and hypovolemic);
- AV block II-III degree;
- acute heart failure or decompensated chronic heart failure;
- severe bradycardia (heart rate less than 40 beats per minute);
- sick sinus syndrome;
- sinoatrial (SA) block;
- cardiomegaly without signs of chronic heart failure;
- Prinzmetal's angina;
- severe arterial hypotension (if used for myocardial infarction, systolic blood pressure less than 100 mm Hg);
- simultaneous use of monoamine oxidase inhibitors (MAO);
- lactation period,
- age under 18 years (efficacy and safety have not been established);
- pheochromocytoma, with the exception of concomitant therapy with alpha-blockers;
- hypersensitivity to the drug.
With caution: diabetes mellitus type 1 and 2, metabolic acidosis, hypoglycemia, history of allergic reactions, chronic obstructive pulmonary disease, bronchial asthma, emphysema, AV block I degree, chronic heart failure (compensated), obliterating peripheral vascular diseases (“intermittent " lameness, Raynaud's syndrome), pheochromocytoma (with simultaneous use of alpha-blockers), liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including a history), psoriasis, pregnancy, old age.
Application Atenolol nycomed 100 mg 30 pcs. film-coated tablets during pregnancy and breastfeeding
Pregnant women should be prescribed Atenolol Nycomed only in cases where the benefit to the mother outweighs the potential risk to the fetus. Atenolol is excreted in breast milk, therefore, during lactation, if it is necessary to use the drug Atenolol Nycomed, it is necessary to stop breastfeeding.
Use in children
Contraindicated: under 18 years of age (efficacy and safety have not been established).
special instructions
Monitoring of patients taking Atenolol Nycomed should include monitoring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), blood glucose concentration in patients with diabetes (once every 4-5 months). In elderly patients, it is recommended to monitor renal function (once every 4-5 months).
The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.
For thyrotoxicosis, Atenolol Nycomed can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal of the drug is contraindicated as it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal values.
In patients with coronary artery disease, abrupt withdrawal of beta-blockers may cause an increase in the frequency or severity of angina attacks, therefore, discontinuation of Atenolol Nycomed in patients with coronary artery disease must be carried out gradually. Reduce the dose for two weeks or more. Compared to non-selective beta-blockers, cardioselective beta-blockers have less effect on pulmonary function, however, for obstructive airway diseases, Atenolol Nycomed is used only in case of absolute indications. If it is necessary to prescribe them, in some cases the use of beta2-adrenergic agonists can be recommended.
Patients with bronchospastic diseases can be prescribed cardioselective adrenergic blockers in case of intolerance and/or ineffectiveness of other antihypertensive drugs, but the dosage should be strictly monitored. An overdose is dangerous due to the development of bronchospasm.
Particular attention is necessary in cases where surgical intervention under anesthesia is required in patients taking Atenolol Nycomed. The drug should be stopped 48 hours before the intervention. As an anesthetic, you should choose a drug with as little negative inotropic effect as possible.
When using the drug Atenolol Nycomed and clonidine simultaneously, the drug Atenolol Nycomed should be stopped several days before clonidine in order to avoid withdrawal syndrome.
It is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from usual doses of epinephrine against the background of a burdened allergic history.
Medicines that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a pronounced decrease in blood pressure or bradycardia.
In case of increasing bradycardia (less than 40 beats/min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction in elderly patients, it is necessary to reduce the dose or stop treatment.
It is recommended to discontinue therapy if depression caused by taking beta-blockers develops.
If intravenous administration of verapamil is necessary, this should be done at least 48 hours after taking Atenolol Nycomed.
When using the drug Atenolol Nycomed, it is possible to reduce the production of tear fluid, which is important in patients who use contact lenses.
Treatment should not be abruptly interrupted due to the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose over 2 weeks or more (reduce the dose by 25% in 3-4 days).
Should be discontinued before testing the content of catecholamines, normetanephrine and vanillylmandelic acid in the blood and urine; titers of antinuclear antibodies (in 1-2 days).
Beta blockers are less effective in smokers.
Impact on the ability to drive vehicles and perform work requiring increased concentration and speed of psychomotor reactions
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose
Symptoms: severe bradycardia, dizziness, marked decrease in blood pressure, fainting, arrhythmia, ventricular extrasystole, AV block II-III degree, chronic heart failure, cyanosis of the nails or palms, convulsions, difficulty breathing, bronchospasm.
Treatment: in case of impaired AV conduction and/or bradycardia - intravenous administration of 1-2 mg of atropine, epinephrine (adrenaline) or installation of a temporary pacemaker; for ventricular extrasystole - lidocaine (class IA drugs are not used); with a pronounced decrease in blood pressure, the patient should be in the Trendelenburg position. If there are no signs of pulmonary edema - intravenous plasma replacement solutions, if ineffective - administration of epinephrine, dopamine, dobutamine; for chronic heart failure - cardiac glycosides, diuretics, glucagon; for convulsions - intravenous diazepam; for bronchospasm - inhalation or parenteral - beta-agonists. Hemodialysis is possible.
Side effects Atenolol nycomed 100 mg 30 pcs. film-coated tablets
Very common (>1/10); frequent (>1/100, 1/1000, 1/10,000,
From the cardiovascular system: often - bradycardia, coldness of the lower extremities, hypotension; rarely - development or worsening of chronic heart failure, AV block, arrhythmias, fainting, peripheral edema, chest pain, cardiac conduction disturbances, orthostatic hypotension and fainting, Raynaud's syndrome.
From the central nervous system: often - asthenia, muscle weakness; uncommon - sleep disturbances (drowsiness or insomnia); rarely - “nightmare” dreams, hallucinations, psychosis, depression, confusion or short-term memory loss, anxiety, dizziness, headache, paresthesia of the limbs (in patients with intermittent claudication and Raynaud’s syndrome), convulsions, changes in taste; very rarely - myasthenia.
From the senses: blurred vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis.
From the endocrine system: infrequently - may mark symptoms of hyperthyroidism. Hypoglycemia (in patients receiving insulin) or hyperglycemia (in patients with type 2 diabetes mellitus).
From the respiratory system: rarely - bronchospasm, wheezing, shortness of breath in patients predisposed to this and/or when taken in high doses (loss of selectivity), nasal congestion.
From the digestive system: often - nausea, vomiting. stomach pain, constipation, or diarrhea; rarely – dryness of the oral mucosa, cholestasis.
Laboratory indications: infrequently - increased activity of liver transaminases; rarely - thrombocytopenia, agranulocytosis, leukopenia, hyperbilirubinemia; very rarely - positive test results for antinuclear antibodies.
From the skin: rarely - skin rash, reversible alopecia, purpura, exacerbation of psoriasis and itching; very rarely - lupus-like syndrome. Psoriasis-like skin rash, hypersensitivity reactions, including angioedema and urticaria.
Other: rarely - decreased potency; very rarely - decreased libido.
Drug interactions
With the simultaneous use of atenolol with insulin, hypoglycemic agents for oral administration, the hypoglycemic effect of the latter is enhanced. When used together with antihypertensive drugs of different groups or nitrates, the hypotensive effect is enhanced. The simultaneous use of atenolol and verapamil (or diltiazem) may cause mutual enhancement of the effects of these drugs.
The antihypertensive effect is weakened by estrogens (sodium retention) and non-steroidal anti-inflammatory drugs, glucocorticosteroids.
With the simultaneous use of atenolol and cardiac glycosides, the risk of developing bradycardia and AV conduction disorders increases.
When atenolol is prescribed simultaneously with reserpine, methyldopa, clonidine, verapamil, severe bradycardia may occur.
Simultaneous intravenous administration of verapamil and diltiazem can provoke cardiac arrest; nifedipine can lead to a significant decrease in blood pressure. When taking atenolol simultaneously with ergotamine and xanthine derivatives, its effectiveness is reduced.
When stopping the combined use of atenolol and clonidine, treatment with clonidine is continued for several days after discontinuation of atenolol. Concomitant use with lidocaine may reduce its elimination and increase the risk of lidocaine toxicity.
Use together with phenothiazine derivatives helps to increase the concentration of each drug in the blood serum.
Phenytoin, when administered intravenously, and drugs for general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of a decrease in blood pressure.
When used together with aminophylline and theophylline, mutual suppression of therapeutic effects is possible.
Concomitant use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect; the break in treatment between taking MAO inhibitors and atenolol should be at least 14 days.
Allergens used for immunotherapy or allergen extracts used for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis.
Inhalation anesthetics (hydrocarbon derivatives) increase the risk of suppression of myocardial function and the development of arterial hypertension.
Amiodarone increases the risk of bradycardia and AV conduction depression.
Cimetidine increases plasma concentrations (inhibits metabolism).
Iodine-containing radiocontrast agents for intravenous administration increase the risk of anaphylactic reactions.
Prolongs the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.
Tri- and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase CNS depression.
