Description
Release form
Pills in white or white with a grayish or creamy tint, light marbling is allowed.
Pharmacological action
It has antianginal, antihypertensive and antiarrhythmic effects. It does not have membrane stabilizing and internal sympathomimetic activity.
Reduces catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces intracellular Ca2 + current. In the first 24 hours after oral administration, against the background of a decrease in cardiac output, there is a reactive increase in the total peripheral vascular resistance, which gradually returns to the original within 1-3 days, and then gradually decreases.
The antihypertensive effect is associated with a decrease in minute blood volume, a decrease in the activity of the renin-angiotensin system, the sensitivity of baroreceptors and the effect on the central nervous system. The antihypertensive effect is manifested as a decrease in systolic and diastolic blood pressure (BP), a decrease in stroke and minute blood volumes.
At 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 improved myocardial perfusion) and contractility, as well as a decrease in the sensitivity of the myocardium to the effects of sympathetic stimulation. Truncates heart rate (HR) at rest and during exercise.
By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for oxygen, especially in patients with chronic heart failure.
Antiarrhythmic effect is manifested by suppression of sinus tachycardia and is associated with the elimination of arrhythmogenic sympathetic influences on the cardiac conduction system, a decrease in the rate of propagation of excitation through the sinoatrial node and lengthening of the refractory period. It inhibits the conduction of impulses in the antegrade and to a lesser extent in retrograde directions through the AV (atrioventricular) node and along additional conduction paths.
A negative chronotropic effect appears 1 hour after administration, reaches its maximum after 2-4 hours, lasts up to 24 hours.
Decreases the automatism of the sinus node, harnesses heart rate, slows AV conduction, reduces myocardial contractility, and reduces myocardial oxygen demand. Reduces myocardial excitability.
When used in medium therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.
Increases the survival of patients after myocardial infarction (reduces the incidence of ventricular arrhythmias and angina attacks).
Practically does not weaken the bronchodilating effect of isoproterenol.
In contrast to non-selective beta-blockers, when administered in medium therapeutic doses, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of the peripheral arteries, bronchi and uterus), and on carbohydrate metabolism, the severity of the atherogenic effect does not differ from the action of propranolol. To a lesser extent, it has a negative batmo-, chrono-, foreign- 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.
Pharmacokinetics
Absorption from the gastrointestinal tract – fast, incomplete (50-60%), bioavailability – 40-50%, TCmax blood – 2-4 hours. It penetrates poorly through the blood-brain barrier, passes in small amounts through the placental barrier and into breast milk. Communication with blood plasma proteins – 6-16%. Virtually not metabolized in the liver. T1 / 2 – 6-9 hours (increases in elderly patients).
It is excreted by the kidneys by glomerular filtration (85-100% unchanged). Impaired renal function is accompanied by an extension of T1 / 2 and cumulation: with a CK below 35 ml / min / 1.73 m2, T1 / 2 is 16-27 hours, with a CK below 15 ml / min / 1.73 m2 – more than 27 hours (dose reduction is necessary). It is excreted during hemodialysis.
Indications
– arterial hypertension
– prevention of angina attacks (except for Prinzmetal angina)
– heart rhythm disturbances: sinus tachycardia, prevention of supraventricular tachyarrhythmia, ventricular extrasystole.
Pregnancy and lactation
Atenolol crosses the placental barrier and is found in cord blood. Studies on the use of atenolol in the first trimester have not been conducted and, therefore, the possibility of a damaging effect on the fetus cannot be ruled out.
For the treatment of hypertension in the third trimester of pregnancy, the drug is used under close medical supervision. The use of atenolol during pregnancy can be a cause of impaired fetal growth.
Assign atenolol to pregnant women or women planning a pregnancy should only be in cases where the benefit to the mother outweighs the potential risk to the fetus, especially in the first and second trimester of pregnancy, since beta-blockers reduce the level of placental perfusion, which can lead to fetal death or his immaturity and premature birth.
In addition, side effects such as hypoglycemia and bradycardia can occur in both the fetus and the newborn.
Special instructions
Control of patients taking atenolol, should include monitoring of heart rate and blood pressure (at the beginning of treatment – daily, then 1 time in 3-4 months), blood glucose in patients with diabetes mellitus (1 time in 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months).
The patient should be trained in the method of calculating heart rate and instructed on the need for a doctorNo consultation at heart rate less than 50 bpm. With thyrotoxicosis, atenolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can enhance symptoms. With diabetes, 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 heart disease (CHD), abrupt cancellation of beta-blockers can cause an increase in the frequency or severity of anginal attacks, so stop taking atenolol in patients with coronary artery disease gradually.
Compared to non-selective beta-blockers, cardioselective beta-blockers have a lesser effect on lung function, however, with obstructive respiratory diseases, atenolol is prescribed only in case of absolute indications. If necessary, their appointment in some cases, we can recommend the use of beta2-adrenergic agonists.
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 for the development of bronchospasm.
Particular attention is needed when surgery is required under general anesthesia in patients taking atenolol. Taking the drug should be stopped 48 hours before the intervention. As an anesthetic, you should choose a drug with a possibly minimal negative inotropic effect.
With the simultaneous use of atenolol and clonidine, atenolol is stopped several days earlier than clonidine in order to avoid the symptom of withdrawal of the latter. It is possible to increase the severity of the hypersensitivity reaction and the lack of effect of the usual doses of epinephrine against the background of a burdened allergic history.
Medicines that reduce catecholamine stores (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 the case of elderly patients with increasing bradycardia (less than 50 bpm), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunctions, it is necessary to reduce the dose or stop treatment.
It is recommended that therapy be discontinued in the event of development of depression caused by beta-blockers.
If intravenous administration of verapamil is necessary, this should be done at least 48 hours after taking atenolol.
When using atenolol, a decrease in tear fluid production is possible, which is important for patients using contact lenses.
Do not abruptly interrupt treatment because of the danger 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).
Should be abolished before testing the blood and urine levels of catecholamines, normetanephrine, and vanillyl mandelic acid titers of antinuclear chitel. Smokers have lower beta blockers. 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. Atenolol is excreted in breast milk, so if the drug is indicated during lactation, it is better to temporarily stop breastfeeding.
Influence on the ability to drive vehicles and control mechanisms
During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Composition
1 tab.
ascorbic acid 1200 mg
Excipients:
Sodium bicarbonate
Sodium carbonate
Citric acid
Sucrose
Orange flavor
Riboflavin sodium phosphate
Sodium saccharinate
Macrogol 6000
Sodium benzoate srdl6 prd6prd6 prd6prd6prd1 prd6prd6 prd6prd6 prd6prd1 prdfp 30 srdlp prd6 prd6prd6pfrd 30 prd6p
atenolol 100 mg
Dosage and administration
Assign inside before meals, without chewing, with a small amount of liquid.
Arterial hypertension. Treatment begins with 50 mg of atenolol once a day. To achieve a stable hypotensive effect, 1-2 weeks of administration is required. With insufficient severity of the hypotensive effect, the dose is increased to 100 mg in one dose. A further increase in dose is not recommended, since it is not accompanied by an increase in the clinical effect.
With coronary heart disease, tachysystolic cardiac arrhythmias – 50 mg 1 time per day.
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.
Elderly patients and patients with impaired renal excretory function need a dosage adjustment.
In the presence of renal failure, a dose adjustment is recommended depending on creatinine clearance. In patients with renal failure with creatinine clearance 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.
Side effects of
Cardiovascular system: the development (worsening) of symptoms of chronic heart failure (ankle swelling, stop shortness of breath), impaired atrioventricular conduction, arrhythmias, bradycardia, marked decrease in blood pressure, palpitations, weakening of orthotic arteriostasis (myocardiasis, myocardiosis cooling of the lower extremities, Raynaud’s syndrome), vasculitis, chest pain.
CNS: dizziness, decreased ability to concentrate, decreased reaction rate, drowsiness or insomnia, depression, hallucinations, fatigue, headache, weakness, nightmares, anxiety, confusion or short-term memory loss, paresthesia in the limbs (in patients with intermittent claudication and Raynaud’s syndrome), muscle weakness, cramps.
Gastrointestinal tract: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation or diarrhea, taste change.
Respiratory system: dyspnea, bronchospasm, apnea, nasal congestion.
Hematologic reactions: platelet purpura, anemia (aplastic), thrombosis.
Endocrine system: decreased potency, decreased libido, hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state.
Skin reactions: urticaria, dermatitis, pruritus, photosensitivity, increased sweating, flushing of the skin, exacerbation of psoriasis, reversible alopecia.
Sensory organs: impaired vision, decreased secretion of lacrimal fluid, dry and sore eyes, conjunctivitis.
Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia. Laboratory indicators: agranulocytosis, leukopenia, increased activity of liver enzymes, hyperbilirubinemia, thrombocytopenia (unusual bleeding and hemorrhage).
Other: back pain, arthrapgia, withdrawal syndrome (tachycardia, frequent attacks of angina pectoris, increased blood pressure, etc.).
The frequency of adverse events increases with increasing doses of the drug.
Drug interaction
With the simultaneous use of atenolol with insulin, hypoglycemic agents for oral administration, their hypoglycemic effect is enhanced. When combined with antihypertensive agents of different groups or nitrates, an increase in the hypotensive effect occurs. The simultaneous use of atenolol and verapamil (or diltiazem) can cause a mutual increase in cardiodepressive action.
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 atrioventricular conduction disturbance increases.
With the simultaneous administration of atenolol with reserpine, methyldopa, clonidine, verapamil, severe bradycardia may occur.
The simultaneous iv administration of verapamil and diltiazem can cause cardiac arrest, nifedipine can lead to a significant decrease in blood pressure. With the simultaneous administration of atenolol with derivatives of ergotamine, xanthine, its effectiveness decreases.
When the combined use of atenolol and clonidine is discontinued, treatment with clonidine is continued for several more days after the withdrawal of atenolol.
Concomitant use with lidocaine may reduce its excretion and increase the risk of toxic effects of lidocaine.
Use in conjunction with phenothiazine derivatives helps to increase the concentration of each drug in the blood serum.
Phenytoin with iv administration, drugs for general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.
When combined with aminophylline and theophylline, mutual suppression of therapeutic effects is possible.
The simultaneous use with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect, the break in treatment between taking MAO inhibitors and atenolol should be at least 14 days.
Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis.
Inhalation anesthetics (derivatives of hydrocarbons) increase the risk of inhibition of myocardial function and the development of hypertension. Amiodarone increases the risk of developing bradycardia and inhibition of AV conduction. Cimetidine increases the concentration in blood plasma (inhibits metabolism). Iodine-containing radiopaque agents for iv administration increase the risk of anaphylactic reactions.
Extends the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.
Three- and tetracyclic antidepressants, antipsychotics (antipsychotics), ethanol, sedatives and hypnotics increase central nervous system depression.
Non-hydrogenated ergot alkaloids increase the risk of peripheral circulation disorders.
Overdose
Symptoms: severe bradycardia, AV block II-III degree, increase in symptoms of heart failure, excessive decrease in blood pressure, difficulty breathing, bronchospasm, dizziness, fainting, arrhythmia, ventricular extrasystole, cyanosis of the fingernails or palmar.
Treatment: gastric lavage and the appointment of adsorbing drugs when bronchospasm occurs, inhaled or intravenous administration of salbutamol beta2-adrenergic agonist is indicated.
In case of violation of AV conduction, bradycardia – iv administration of 1-2 mg of atropine, epinephrine or staging of 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 – iv plasma-replacing solutions, if ineffective – administration of epinephrine, dopamine, dobutamine in chronic heart failure – cardiac glycosides, diuretics, glucagon in convulsions – iv diazepam. Dialysis is possible.
Storage Conditions
List B. In a dry, dark place at a temperature not exceeding 25 ° C.
Keep out of the reach and sight of children.
Expiration
2 years.
active substance
Atenolol
lekarstvennaja form
tablets
Prescribing
For adults as prescribed by a doctor, Pregnant as prescribed by a doctor
Indications
Indications
hypertension, arrhythmia, angina
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