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ATENOLOL
Release form
Tablets
For children
Not used
For pregnant women
Not recommended
For nursing mothers
Not recommended
For drivers
Not recommended
Storage temperature
to 25 °C
INSTRUCTION
storage
active substance: atenolol; 1 tablet contains atenolol 50 mg (0.05 g); excipients: potato starch, calcium stearate, magnesium carbonate, microcrystalline cellulose, povidone.
Medicinal form
Tablets. The main physicochemical properties: tablets are white or white with a grayish tint, with a flat surface and beveled edges.
Pharmacotherapeutic group
Selective blockers of β-adrenoceptors. ATX code C07A B03.
Pharmacological properties
Pharmacodynamics. Atenolol belongs to the group of cardioselective β1-adrenoblockers. The drug has antianginal, hypotensive and antiarrhythmic effects. Reduces sinus node automatism, heart rate (HR), slows down atrioventricular conduction, reduces myocardial contractility and its need for oxygen. When used in medium therapeutic doses, it does not cause side effects (bronchospasm, heart failure, etc.) typical of non-selective β-blockers. Pharmacokinetics. After ingestion, approximately 50% is absorbed internally (food does not affect bioavailability), slightly more in the elderly. It is slowly absorbed in the digestive tract. The maximum concentration of the drug in blood serum is observed after 2–4 hours. Binding to blood plasma proteins is insignificant (6–16%). Does not penetrate the blood-brain barrier, passes the placental barrier. 85% is excreted by the kidneys, secreted by the mammary glands. The half-life after oral administration is 6–9 hours; in patients with renal failure, this period may be longer. To a small extent (less than 10%) is subject to biotransformation in the liver.
Indication
- Treatment of arterial hypertension; - treatment and prevention of angina attacks (chronic stable and unstable angina, especially when combined with tachycardia and arterial hypertension); - heart rhythm disorders (arrhythmia, sinus tachycardia, prevention of supraventricular tachycardia, paroxysmal supraventricular tachycardia, atrial fibrillation and flutter; ventricular (ventricular) arrhythmias, including those caused by increased physical activity, taking sympathomimetic agents; prevention of ventricular tachycardia and ventricular fibrillation); - myocardial infarction (treatment and prevention to reduce mortality and reduce the risk of repeated infarction).
Contraindication
- Hypersensitivity to the components of the medicinal product or to other β-blockers; - acute heart failure; - cardiogenic shock; - atrioventricular block II and III degrees; − sinus node weakness syndrome; − sinoatrial blockade; − sinus bradycardia (heart rate less than 45 beats per minute); - arterial hypotension (systolic pressure less than 90 mm Hg); - bronchial asthma; - metabolic acidosis; - severe disorders of peripheral blood circulation; - simultaneous use of monoamine oxidase (MAO) inhibitors (with the exception of MAO-B inhibitors); − untreated pheochromocytoma; - kidney failure.
Interaction with other medicinal products and other forms of interaction
With the simultaneous use of atenolol and: - antidiabetic agents for oral use, such as insulin, their effect may be enhanced or prolonged. At the same time, symptoms of hypoglycemia (especially tachycardia and tremor) may be masked or disappear. In this regard, it is necessary to carry out regular control of blood sugar; - tricyclic antidepressants, barbiturates, phenothiazides, nitroglycerin, diuretics, vasodilators and other antihypertensive agents (for example, prazosin) may increase the hypotensive effect; - calcium channel blockers (nifedipine), in addition to increasing the hypotensive effect, heart failure may develop; - calcium channel blockers with a negative inotropic effect (verapamil, diltiazem) may increase their effect, especially in patients with impaired ventricular function and/or atrioventricular conduction, which increases the risk of arterial hypotension and bradycardia. If intravenous verapamil is necessary, it should be done at least 48 hours after withdrawal of atenolol; - cardiac glycosides, reserpine, α-methyldopa, guanfacine and clonidine may cause significant slowing of the heart rate; - indomethacin may reduce the antihypertensive effect of atenolol; - the antihypertensive effect of narcotics and antiseptics is enhanced. At the same time, the additive, negative isotropic effect of both means is manifested; - peripheral muscle relaxants (for example, suxamethonium, tubocurarine) may increase the neuromuscular blockade, therefore, before the operation, which is accompanied by anesthesia, the anesthesiologist should be informed that the patient is taking atenolol; - euphylline and theophylline may have mutual inhibition of therapeutic effects; - lidocaine may reduce its elimination and increase the risk of toxic effects of lidocaine; - sympathomimetic agents (adrenaline) may decrease the effect of β-blockers; - nitrates, peripheral vasodilators, MAO inhibitors increase their hypotensive effect; - propafenone enhances the effect of atenolol, which is part of the drug; - drugs containing potassium, the effect of the latter is weakened; - drugs that suppress the central nervous system, the sedative effect increases; - the narcotic effect of narcotic analgesics increases, dangerous retardation occurs; - anticholinesterase agents, angiotensin-converting enzyme inhibitors (captopril, enalapril, lisinopril), the level of potassium in the blood increases. For patients who take atenolol and clonidine at the same time, the latter can be canceled only a few days after stopping treatment with atenolol. Atenolol enhances the antihypertensive effect of prazosin, their combination leads to a greater decrease in blood pressure than when taking only one drug. Intravenous calcium channel blockers such as verapamil and diltiazem or other antiarrhythmic agents (eg, disopyramide) should not be used during treatment with atenolol.
Features of use
If thrombocytopenic or non-thrombocytopenic purpura has been observed in patients treated with other β-blockers, it is necessary to keep in mind the possibility of this side effect occurring during treatment with atenolol. It should be remembered that during the reception of atenolol in extremely rare cases the manifestation of latent diabetes mellitus or worsening of the condition of patients with existing diabetes mellitus is possible. Sometimes there are disorders of lipid metabolism: with a level of total cholesterol that remains normal, the level of high-density lipoproteins decreases and the level of triglycerides in the blood plasma increases. Do not change the dosage or stop treatment with atenolol without consulting a doctor. Patients with coronary heart disease/hypertension may develop a withdrawal syndrome upon sudden withdrawal of the drug: increase in the frequency or severity of anginal attacks, increase in blood pressure, therefore withdrawal of the drug and reduction of the dose should occur slowly and gradually, within 10–14 days. In the event that the pulse rate drops below 50-55 beats per minute at rest and patients develop symptoms related to bradycardia, the dose should be reduced. Atenolol can increase both sensitivity to allergens and the severity of anaphylactic reactions. Such patients may be resistant to the usual doses of adrenaline (epinephrine) used to treat allergic reactions. Since atenolol is excreted by the kidneys, the dose should be reduced in patients with creatinine clearance below 35 ml/min/1.73 m2. Atenolol should be used with extreme caution and only under strict medical supervision: - with atrioventricular blockade of the 1st degree; - in case of diabetes with fluctuating blood sugar levels (in connection with the possibility of a severe hypoglycemic state); - in the case of prolonged fasting and heavy physical exertion (severe hypoglycemic states may occur); - with pheochromocytoma (with prior appointment of α1-adrenoceptor blockers); - with liver and/or kidney function disorders (when prescribing atenolol to this category of patients, constant monitoring of the dynamics of the functional state of the liver and/or kidneys is required); - with existing psoriasis or psoriasis in a personal or family history; - patients with impaired peripheral blood circulation, including Raynaud's syndrome; - patients who are undergoing desensitization therapy or have a history of severe allergic reactions; - with thrombocytopenic/non-thrombocytopenic purpura in the anamnesis; - with hyperthyroidism (the drug can mask tachycardia); - patients with myasthenia gravis. In thyrotoxicosis, atenolol can mask clinical signs of hyperthyroidism, hypoglycemia (especially tachycardia and tremor). β-blockers are not recommended for vasospastic angina (Prinzmetal's angina). If surgical interventions are necessary, it is recommended to stop atenolol therapy 24 hours before surgery or choose an anesthetic agent with a minimal negative inotropic effect. During treatment with atenolol, changes in the results of some laboratory tests are possible: an increase in the level of lipoproteins, cholesterol and potassium in the blood serum, the level of catecholamines and the products of their metabolism in the urine and blood. Although the relationship between atenolol and depression has not been fully established, the drug should be used with caution in such patients. For elderly patients, it is recommended to start treatment with reduced doses, especially in case of impaired kidney function (the dose can be increased under the control of blood pressure and heart rate). If severe bradycardia, hypotension, rhythm disturbances, conduction or other complications are detected in such patients, it is necessary to reduce the dose of atenolol or cancel it. If it is necessary to prescribe the drug to patients with broncho-obstructive syndrome, simultaneous use of β2-adrenomimetics is possible. Alcohol consumption should be excluded during treatment with atenolol. In all of these cases, the physician must carefully weigh the benefit/risk ratio when prescribing atenolol. Use during pregnancy or breastfeeding. Atenolol penetrates through the placental barrier and into breast milk. During pregnancy (especially in the 1st trimester), atenolol can be used only in exceptional cases, after carefully weighing the benefit/risk ratio, since there is still no sufficient experience of its use in pregnant women, especially in the early stages. If women took atenolol, treatment should be stopped at least 24-48 hours before delivery due to the possibility of bradycardia, hypoglycemia and respiratory depression in the child. If this is not possible, the infant should be under special close observation for 24 to 48 hours after birth. Atenolol is excreted in breast milk, so breastfeeding should be stopped during treatment with the drug. The ability to influence the speed of reaction when driving vehicles or other mechanisms. During the treatment period, the patient should refrain from driving vehicles or working with complex mechanisms, given that during treatment with atenolol such side reactions from the nervous system as dizziness, headache, confusion, hallucinations, depressive disorders are possible. especially in case of impaired kidney function (the dose can be increased under the control of blood pressure and heart rate). If severe bradycardia, hypotension, rhythm disturbances, conduction or other complications are detected in such patients, it is necessary to reduce the dose of atenolol or cancel it. If it is necessary to prescribe the drug to patients with broncho-obstructive syndrome, simultaneous use of β2-adrenomimetics is possible. Alcohol consumption should be excluded during treatment with atenolol. In all of these cases, the physician must carefully weigh the benefit/risk ratio when prescribing atenolol. Use during pregnancy or breastfeeding. Atenolol penetrates through the placental barrier and into breast milk. During pregnancy (especially in the 1st trimester), atenolol can be used only in exceptional cases, after carefully weighing the benefit/risk ratio, since there is still no sufficient experience of its use in pregnant women, especially in the early stages. If women took atenolol, treatment should be stopped at least 24-48 hours before delivery due to the possibility of bradycardia, hypoglycemia and respiratory depression in the child. If this is not possible, the infant should be under special close observation for 24 to 48 hours after birth. Atenolol is excreted in breast milk, so breastfeeding should be stopped during treatment with the drug. The ability to influence the speed of reaction when driving vehicles or other mechanisms. During the treatment period, the patient should refrain from driving vehicles or working with complex mechanisms, taking into account that during treatment with atenolol such adverse reactions from the nervous system as dizziness, headache, confusion, hallucinations, depressive disorders are possible. especially in case of impaired kidney function (the dose can be increased under the control of blood pressure and heart rate). If severe bradycardia, hypotension, rhythm disturbances, conduction or other complications are detected in such patients, it is necessary to reduce the dose of atenolol or cancel it. If it is necessary to prescribe the drug to patients with broncho-obstructive syndrome, simultaneous use of β2-adrenomimetics is possible. Alcohol consumption should be excluded during treatment with atenolol. In all of these cases, the physician must carefully weigh the benefit/risk ratio when prescribing atenolol. Use during pregnancy or breastfeeding. Atenolol penetrates through the placental barrier and into breast milk. During pregnancy (especially in the 1st trimester), atenolol can be used only in exceptional cases, after carefully weighing the benefit/risk ratio, since there is still no sufficient experience of its use in pregnant women, especially in the early stages. If women took atenolol, treatment should be stopped at least 24-48 hours before delivery due to the possibility of bradycardia, hypoglycemia and respiratory depression in the child. If this is not possible, the infant should be under special close observation for 24 to 48 hours after delivery. Atenolol is excreted in breast milk, so breastfeeding should be stopped during treatment with the drug. The ability to influence the speed of reaction when driving vehicles or other mechanisms. During the treatment period, the patient should refrain from driving vehicles or working with complex mechanisms, given that during treatment with atenolol such side reactions from the nervous system as dizziness, headache, confusion, hallucinations, depressive disorders are possible. therefore, during treatment with the drug, breastfeeding should be stopped. The ability to influence the speed of reaction when driving vehicles or other mechanisms. During the treatment period, the patient should refrain from driving vehicles or working with complex mechanisms, taking into account that during treatment with atenolol such adverse reactions from the nervous system as dizziness, headache, confusion, hallucinations, depressive disorders are possible. therefore, during treatment with the drug, breastfeeding should be stopped. The ability to influence the speed of reaction when driving vehicles or other mechanisms. During the treatment period, the patient should refrain from driving vehicles or working with complex mechanisms, given that during treatment with atenolol such side reactions from the nervous system as dizziness, headache, confusion, hallucinations, depressive disorders are possible.
Methods of application
Tablets are swallowed without chewing and with a small amount of liquid before meals, preferably at the same time. The dosage of the drug and the duration of treatment are set by the doctor individually, depending on the obtained therapeutic effect. Myocardial infarction: after intravenous administration, 12 hours after the injection, 50 mg orally and 100 mg after another 12 hours are prescribed. Chronic stable and unstable angina pectoris: 100 mg of atenolol 1 time per day or 50 mg 2 times per day are usually prescribed. Arterial hypertension: treatment, as a rule, begins with the use of 100 mg of the drug 1 time per day. For some patients, 50 mg per day is sufficient. The effect is observed after 2 weeks. In case of ineffectiveness, atenolol is used together with diuretics. Supraventricular (supraventricular) and ventricular (ventricular) arrhythmias: the drug is prescribed 1–2 times a day for 50–100 mg. The maximum daily dose is 200 mg. Doses for patients with significant impairment of kidney function depend on the level of creatinine clearance (CK): with a creatinine clearance of 10–30 ml/min, the dose is reduced by 2 times (50 mg per day or every other day), and with a creatinine clearance of less than 10 ml/min reduced by 4 times compared to usual. Patients on hemodialysis should use 50 mg of the drug after each dialysis. This must be done in a hospital setting, as a significant drop in blood pressure may occur. Children. Do not use the medicine for children.
Overdose
Symptoms: the clinical picture depends on the degree of intoxication and is manifested mainly by disturbances in the cardiovascular and central nervous systems. Overdose can lead to bradycardia, a decrease in blood pressure, heart failure, cardiogenic shock. In severe cases, there is a disturbance of consciousness and/or breathing, bronchospasm, vomiting; extremely rarely – generalized convulsive attacks. Treatment: gastric lavage, taking activated charcoal, in case of overdose or in a condition where there is a threat of a decrease in heart rate and/or blood pressure, treatment with atenolol must be stopped. In intensive care units, vital signs should be carefully monitored and, if necessary, adjusted. If necessary, prescribe: - atropine (0.5–2 mg intravenously as a bolus), epinephrine; – glucagon: initial dose of 1–10 mg intravenously (stream), then – 2–2.5 mg/h as a continuous infusion; – sympathomimetics depending on body weight and effect (dopamine, dobutamine, isoprenaline, oxyprenaline, or adrenaline). If refractoriness to bradycardia therapy is observed, temporary electrocardiostimulation is possible. In case of bronchospasm, prescribe β2-sympathomimetics in the form of an aerosol (if the effect is insufficient, also intravenously) or aminophylline intravenously. With generalized convulsions - slow intravenous administration of diazepam. It is removed by hemodialysis.
Side effects
From the side of the cardiovascular system: arterial hypotension, bradycardia, atrioventricular conduction disturbances (up to cardiac arrest), orthostatic hypotension, the consequence of which can be a syncopal state, intermittent lameness, which is more pronounced in patients with Raynaud's syndrome, the appearance of symptoms of heart failure, feeling coldness and paresthesia in the limbs. In some cases, patients with angina pectoris may have increased attacks. From the nervous system: fatigue, dizziness, sleep disturbances, headache, increased sweating, depressive disorders, night terrors, insomnia, drowsiness, confusion, hallucinations, mood swings, psychosis. On the part of the organs of vision: impaired vision, decreased secretion of lacrimal glands, conjunctivitis, feeling of dryness in the eyes. From the side of the digestive tract: nausea, constipation, diarrhea, dry mouth, dyspepsia, violation of the level of transaminases, intrahepatic cholestasis, hepatotoxicity. From the endocrine system: hypoglycemia (in patients with diabetes). From the genitourinary system: libido and potency disorders, impotence, gynecomastia, difficulty urinating. From the side of the respiratory system: in susceptible patients - the appearance of symptoms of bronchial obstruction, bronchospasm. From the hematopoietic system: purpura, thrombocytopenia, leukopenia. From the side of the immune system: hyperemia of the skin, itching, skin rashes (exacerbation of psoriasis), psoriasis-like skin reactions, exanthema, alopecia, urticaria, increased level of antinuclear antibodies, photosensitization, hypersensitivity reactions (angioedema), lupus syndrome. Others: muscle weakness, withdrawal syndrome: increased frequency or severity of anginal attacks, increased blood pressure.
Expiration date
2 years
Storage conditions
Store in the original packaging at a temperature not higher than 25 ºС. Keep out of the reach of children.
Packaging
10 tablets in a blister; 2 blisters in a cardboard pack.
Leave category
By prescription.
Producer
Monfarm PJSC.
Address
Ukraine, 19161, Cherkasy region, Uman district, village Avramivka, str. Zavodska, 8.