Pharmacodynamics and pharmacokinetics
The drug has antiarrhythmic, antianginal, and hypotensive effects. It has negative dromotropic, chronotropic, inotropic and bathmotropic effects.
The hypotensive effect is achieved by influencing the nervous system, reducing the sensitivity of baroreceptors on the aortic arch, reducing the activity of the renin-angiotensin system , and reducing the IOC.
The drug reduces systolic and diastolic blood pressure, reduces IOC, SV.
The medication does not affect the tone of peripheral arteries in therapeutic doses.
The antianginal effect is ensured by a decrease in the oxygen demand of myocardial cardiomyocytes, which leads to a decrease in heart rate. The drug reduces heart rate at rest and during physical activity.
The antiarrhythmic effect is ensured by the elimination of arrhythmogenic factors (arterial hypertension, increased cAMP content, increased activity of the sympathetic nervous system, tachycardia), slowing down atrioventricular conduction , and reducing the rate of spontaneous excitation of the ectopic and sinus pacemaker.
When taking Atenolol, the survival rate of patients who have suffered a myocardial infarction increases significantly.
The drug does not weaken the bronchodilatory effect of isoproterenol.
Pharmacodynamics: effect on blood pressure
The mechanism of action of the drug Atenolol is based on the ability of the active ingredients of the drug to block β-receptors, suppressing the influence of stress factors on the patient’s internal organs and systems.
Atenolol for high blood pressure is characterized by the presence of the following pharmacological properties:
- slowing heart rate;
- normalization of blood pressure indicators;
- reducing the risk of developing heart rhythm disturbances, potentially life-threatening for the patient.
Atenolol is an effective inhibitor of vasomotor centers, as well as the release of renin from the renal apparatus. It has the ability to powerfully counteract cardiac β-receptors, significantly reducing cardiac output.
Indications for use of Atenolol
What are the pills for?
The medicine is prescribed for hypertensive crisis , arterial hypertension, angina pectoris, ischemic heart disease, neurocirculatory dystonia , hyperkinetic cardiac syndrome of functional origin, withdrawal syndrome, tremor, essential tremor, agitation.
The drug is recommended for use for the prevention of rhythm disturbances, myocardial infarction, ventricular extrasystole , sinus tachycardia, atrial flutter, atrial fibrillation, and ventricular tachycardia.
The medication is prescribed for migraine, thyrotoxicosis, pheochromocytoma .
Indications for use of Atenolol Nycomed are similar.
Contraindications
The medicine is not used for severe bradycardia, 2-3 degree atrioventricular block, cardiogenic shock , decompensated form of CHF, acute heart failure, SA blockade, Prinzmetal angina , intolerance to the active component, cardiomegaly, breastfeeding, taking MAO inhibitors.
For pulmonary emphysema, allergies, metabolic acidosis, diabetes mellitus, hypoglycemia, pheochromocytoma, bronchial asthma, thyrotoxicosis, myasthenia gravis, liver failure , pregnancy, psoriasis, depression, children and the elderly, and Raynaud's syndrome, the drug is used with caution.
Side effects
Sense organs: conjunctivitis , visual disturbances, dry eyes, decreased tear production, sore eyes.
Nervous system: depression, insomnia, headaches, dizziness, weakness, asthenia, drowsiness, depression, paresthesia in the extremities , impaired concentration, short-term memory loss, convulsions, myasthenia gravis.
Cardiovascular system: chest pain, vasculitis, coldness of the lower extremities, vasospasm, orthostatic hypotension, CHF, weakened myocardial contractility, arrhythmia, atrioventricular block, palpitations, bradycardia, myocardial conduction disturbances.
Digestive system: changes in taste perception, epigastric pain, nausea, vomiting, dry mouth, stool disorders: constipation , diarrhea.
Respiratory system: bronchospasm, laryngospasm , difficulty breathing, nasal congestion.
Endocrine system: hypothyroid state, hyperglycemia, hypoglycemia.
Skin: reversible alopecia, psoriasis-like skin rashes, increased sweating, exacerbation of psoriasis symptoms, skin hyperemia.
Also noted are back pain, bradycardia , decreased potency, decreased libido, arthralgia, and intrauterine growth retardation.
The severity of side effects directly depends on the dose of the drug.
Atenolol 30 film-coated tablets 50 mg
Registration Certificate Holder
ATOLL (Russia)
Dosage form
Medicine - Atenolol
Description
Film-coated tablets
white or almost white, cylindrical, biconvex; on the fracture, two layers are visible - a white or almost white core and a film shell.
1 tab.
atenolol 50 mg
Excipients
: microcrystalline cellulose 117 mg, sodium carboxymethyl starch 6.4 mg, povidone 3 mg, magnesium stearate 3 mg, potato starch 10 mg, colloidal silicon dioxide 0.6 mg.
Film shell composition:
opadry II 85F48105 White 6 mg, including polyvinyl alcohol 2.814 mg, macrogol-3350 1.416 mg, talc 1.044 mg, titanium dioxide 0.726 mg.
10 pieces. — cellular contour packages (1) — cardboard packs. 10 pieces. — contour cell packaging (2) — cardboard packs. 10 pieces. — cellular contour packages (3) — cardboard packs. 10 pieces. — contour cell packaging (4) — cardboard packs. 10 pieces. — contour cell packaging (5) — cardboard packs. 10 pieces. — contour cell packaging (10) — cardboard packs. 30 pcs. — cellular contour packages (1) — cardboard packs. 30 pcs. — contour cell packaging (2) — cardboard packs. 30 pcs. — cellular contour packages (3) — cardboard packs. 30 pcs. — contour cell packaging (4) — cardboard packs. 30 pcs. — contour cell packaging (5) — cardboard packs. 30 pcs. — contour cell packaging (10) — cardboard packs. 10 pieces. — polymer jars (1) — cardboard packs. 20 pcs. — polymer jars (1) — cardboard packs. 30 pcs. — polymer jars (1) — cardboard packs. 40 pcs. — polymer jars (1) — cardboard packs. 50 pcs. — polymer jars (1) — cardboard packs. 100 pieces. — polymer jars (1) — cardboard packs.
Indications
Arterial hypertension, hypertensive crisis, mitral valve prolapse, hyperkinetic cardiac syndrome of functional origin, neurocirculatory dystonia of the hypertensive type.
Treatment: IHD, angina (stress, rest and unstable).
Treatment and prevention: myocardial infarction (acute phase with stable hemodynamic parameters, secondary prevention).
Arrhythmias (including with general anesthesia, congenital syndrome of the elongated QT interval, myocardial infarction without signs of chronic heart failure, thyrotoxicosis), sinus tachycardia, paroxysmal atrial tachycardia, overlaid and ventricular extrasystole, overflow and ventricular tachycardia, twin Tel tachyarrhythmia, atrial flutter .
Essential and senile tremor, agitation and tremor during withdrawal syndrome.
As part of complex therapy: hypertrophic obstructive cardiomyopathy, pheochromocytoma (only together with alpha-blockers), thyrotoxicosis; migraine (prevention).
Contraindications for use
AV block II and III degrees, sinoatrial block, SSSU, bradycardia (heart rate less than 40 beats/min), arterial hypotension (if used for myocardial infarction, systolic blood pressure less than 100 mm Hg), cardiogenic shock, chronic stage IIB-III heart failure, acute heart failure, Prinzmetal's angina, lactation period, simultaneous use of MAO inhibitors, hypersensitivity to atenolol.
pharmachologic effect
Cardioselective beta1-blocker without intrinsic sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects.
Reduces the stimulating effect on the heart of sympathetic innervation and catecholamines circulating in the blood. It has a negative chrono-, dromo-, batmo- and inotropic effect: it reduces heart rate, inhibits conductivity and excitability, and reduces myocardial contractility. OPSS 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 α-adrenergic receptors and the elimination of stimulation of β2-adrenergic receptors), after 1-3 days it returns to the original level, and with prolonged use it decreases.
The hypotensive effect is associated with a decrease in minute blood volume, a decrease in the activity of the renin-angiotensin 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; manifested by a decrease in both systolic and diastolic blood pressure, a decrease in stroke volume and cardiac output. In average therapeutic doses it has no effect on the tone of peripheral arteries.
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 innervation. A decrease in heart rate occurs 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 AV conduction. Inhibition of impulse conduction is observed predominantly in the antegrade and to a lesser extent in the retrograde directions through the AV node and along additional pathways.
Unlike non-selective beta-blockers, when used in average therapeutic doses, it has a less pronounced effect on organs containing β2-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. The negative bathmo-, chrono-, ino- and dromotropic effects are less pronounced. When used in high doses (more than 100 mg/day), it causes blockade of both subtypes of β-adrenergic receptors.
The hypotensive effect lasts 24 hours, and with regular use it stabilizes by the end of 2 weeks of treatment. The negative chronotropic effect appears 1 hour after administration, reaches a maximum after 2-4 hours and lasts up to 24 hours.
Drug interactions
With simultaneous use of diuretics, the antihypertensive effect is enhanced.
With the simultaneous use of inhalation anesthesia, the risk of increased cardiodepressive effects and the development of arterial hypotension increases.
There are reports of the development of bradycardia and arterial hypotension with simultaneous use of alcuronium chloride.
With simultaneous use of verapamil, the negative inotropic effect increases, bradycardia, bradyarrhythmia, and severe conduction disturbances develop; Cases of postural hypotension, dizziness, left ventricular failure, and lethargy have been described. Under the influence of verapamil, the pharmacokinetic parameters of atenolol do not change significantly, although a case of an increase in the AUC of atenolol has been described.
With simultaneous use of disopyramide, Css increases, disopyramide clearance decreases, and conduction disturbances are possible.
With the simultaneous use of dipyridamole, a case of the development of bradycardia and then asystole has been described (during an ECG test with dipyridamole in a patient receiving atenolol).
With the simultaneous use of indomethacin, naproxen and other NSAIDs, it is possible to reduce the antihypertensive effect of atenolol, which is to a certain extent due to the disruption (under the influence of NSAIDs) of the synthesis in the kidneys and the release into the bloodstream of prostaglandins PGA and PGE, which have a strong vasodilating effect on peripheral arterioles.
With the simultaneous use of insulin, an increase in blood pressure is possible.
With simultaneous use of clonidine, additive hypotensive effects, sedation, and dry mouth are possible.
With simultaneous use of caffeine, the effectiveness of atenolol may be reduced.
With simultaneous use of nizatidine, a case of increased cardiodepressive effect has been described.
With simultaneous use of nifedipine, cases of severe arterial hypotension and heart failure have been described, which may be due to an increased inhibitory effect of nifedipine on the myocardium.
With simultaneous use of orlistat, the antihypertensive effect of atenolol is reduced, which can lead to a significant increase in blood pressure and the development of a hypertensive crisis.
With simultaneous use of prenylamine, an increase in the QT interval is possible.
With simultaneous use of chlorthalidone, the antihypertensive effect is enhanced.
Dosage regimen
Installed individually. The usual dose for adults - orally, at the beginning of treatment is 25-50 mg 1 time / day. If necessary, the dose is gradually increased. In case of impaired renal function, patients with CC 15-35 ml/min - 50 mg/day; with CC less than 15 ml/min - 50 mg every other day.
Maximum dose:
adults when taken orally - 200 mg/day in 1 or 2 doses.
Side effect
From the cardiovascular system:
in some cases - bradycardia, arterial hypotension, AV conduction disturbances, and the appearance of symptoms of heart failure.
From the digestive system:
At the beginning of therapy, nausea, constipation, diarrhea, and dry mouth are possible.
From the nervous system:
at the beginning of therapy, fatigue, dizziness, depression, mild headache, sleep disturbances, a feeling of cold and paresthesia in the extremities, and a decrease in the patient’s reactivity are possible.
From the side of the organ of vision:
decreased secretion of tear fluid, conjunctivitis.
From the endocrine system:
decreased potency, hypoglycemic conditions in patients with diabetes.
From the respiratory system:
in predisposed patients - the appearance of symptoms of bronchial obstruction.
Allergic reactions:
skin itching.
Other:
increased sweating, redness of the skin.
special instructions
Use with caution in diabetes mellitus, COPD (including bronchial asthma, emphysema), metabolic acidosis, hypoglycemia; history of allergic reactions, chronic heart failure (compensated), obliterating diseases of the peripheral arteries (intermittent claudication, Raynaud's syndrome), pheochromocytoma, liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including a history), psoriasis, during pregnancy, in elderly patients, in pediatrics (efficacy and safety have not been determined).
When using atenolol, it is possible to reduce the production of tear fluid, which is important for patients who use contact lenses.
Atenolol should be withdrawn gradually after a long course of treatment under medical supervision.
When stopping the combined use of atenolol and clonidine, treatment with clonidine is continued for several more days after atenolol is discontinued, otherwise severe arterial hypertension may occur.
If inhalation anesthesia is necessary in patients receiving atenolol, a few days before anesthesia it is necessary to stop taking atenolol or select an anesthetic agent with minimal negative inotropic effect.
Effect on the ability to drive vehicles and operate machinery.
In patients whose activities require increased concentration, the issue of outpatient use of atenolol should be decided only after assessing the individual reaction.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - With caution. Restrictions when breastfeeding - Contraindicated.
Atenolol penetrates the placental barrier, so use during pregnancy is possible only if the expected benefit to the mother outweighs the possible risk to the fetus.
Atenolol is excreted in breast milk, so if it is necessary to use it during lactation, it is recommended to stop breastfeeding.
Use for renal impairment
Restrictions for impaired renal function - With caution.
Use with caution in chronic renal failure. In case of impaired renal function, patients with CC 15-35 ml/min - 50 mg/day; with CC less than 15 ml/min - 50 mg every other day.
Use for liver dysfunction
Restrictions for liver dysfunction - With caution.
Should be used with caution in case of liver failure.
Use in elderly patients
Restrictions for elderly patients - Use with caution.
Should be used with caution in elderly patients.
Use in children
Restrictions for children - With caution.
It should be used with caution in pediatrics (efficacy and safety have not been determined).
Instructions for use of Atenolol (Method and dosage)
The tablets are taken orally, washed down with liquid, and do not chew.
The initial dosage is 25-50 mg per day, after a week, if necessary, the amount of the drug is increased by 50 mg, the average daily dosage is 100 mg.
For tachysystolic disorders and for ischemic heart disease, Atenolol is prescribed once a day, 50 mg.
Acute myocardial infarction with stable hemodynamic parameters: intravenous infusions, then take a 50 mg tablet after 10 minutes, repeat after 12 hours.
For cardiac hyperkinetic syndrome, 25 mg per day is indicated.
The drug is effective for 24 hours; the drug is not used more than once a day. It is not recommended to prescribe more than 200 mg per day. The medication is withdrawn gradually, every 3 days - ¼ dose.
Instructions for use of Atenolol Nycomed are similar.
Composition, release form and manufacturer
The drug Atenolol is presented on the pharmaceutical market in an easy-to-use tablet form. The manufacturer of this medication is Croatian.
The tablets contain:
- Atenolol is the main active ingredient of the drug.
- Auxiliary ingredients (magnesium stearate, starch, silicon dioxide, lactose monohydrate).
At the pharmacy you can purchase the medicine Atenolol in the following dosages of the main active ingredient:
- 25 mg;
- 50 mg;
- 100 mg.
The drug is sold in packages of 20, 50 or 100 tablets.
Atenolol is a drug used in the treatment of hypertension
Overdose
Manifested by bronchospasm , cyanosis of the nail plates, convulsions , difficulty breathing, arrhythmia, fainting, drop in blood pressure, dizziness, severe bradycardia.
Emergency gastric lavage is required.
In case of atrioventricular conduction disturbance or bradycardia, atropine, epinephrine is administered intravenously, or a temporary pacemaker is installed.
If there is a sharp drop in blood pressure, the patient is placed in the Trendelenburg position .
In the absence of signs of pulmonary edema, plasma-substituting solutions are administered intravenously; in case of ineffectiveness, dobutamine , epinephrine, and dopamine are administered.
For convulsive syndrome, intravenous infusion of diazepam is indicated. Dialysis is effective.
Interaction
In patients taking Atenolol, allergen extracts for skin testing, as well as allergens for immunotherapy, significantly increase the risk of developing severe systemic allergic reactions, anaphylaxis. The risk of anaphylactic reactions increases with intravenous administration of radiocontrast agents.
A fall in blood pressure and cardiodepressive effects have been observed with intravenous infusion of phenytoin, as well as with the use of drugs for inhaled general anesthesia. The drug can mask the signs of developing hypoglycemia with the simultaneous use of oral hypoglycemic agents and insulin.
Atenolol reduces the clearance of xanthines and lidocaine . Estrogens, glucocorticosteroids, NSAIDs, BMCC, guanfacine, reserpine, methyldopa , cardiac glycosides, amiodarone, Diltiazem , Verapamil and many antiarrhythmic medications increase the likelihood of developing atrioventricular block, bradycardia, cardiac arrest, and worsening heart failure.
Hydralazine, sympatholytics, clonidine, diuretics, antihypertensive drugs, BMCC can significantly reduce blood pressure.
Atenolol prolongs the duration of action of coumarins, non-depolarizing muscle relaxants. Neuroleptics, sedatives, hypnotics, ethanol, tetracyclic and tricyclic antidepressants increase the inhibitory effect on the central nervous system.
The simultaneous administration of MAO inhibitors is unacceptable due to the risk of hypotension. Impaired peripheral circulation is observed when using medications with non-hydrogenated ergot alkaloids.
Interaction with other drugs and alcohol
It is not recommended to combine Atenolol tablets with barbiturates and diuretics, since these drugs increase the effect of the drug on blood pressure.
The combination of Atenolol with calcium antagonists can cause a hypotensive crisis and heart failure.
The use of these tablets with hypoglycemic drugs enhances the effect of Atenolol, which can provoke possible adverse reactions.
The combination with adrenaline and norepinephrine leads to a sharp increase in blood pressure.
Combination with anti-inflammatory drugs weakens the effect of Atenolol tablets and its ability to influence blood pressure.
The drug Atenolol is not compatible with alcohol! The simultaneous use of tablets with alcoholic drinks leads to a decrease in the ability to concentrate and reaction speed.
Atenolol is incompatible with alcohol
special instructions
Taking the drug should be accompanied by regular measurement of blood pressure, pulse, and sugar levels in people with diabetes .
Elderly patients are advised to periodically monitor the condition of the renal system. The doctor needs to instruct the patient and teach him how to measure heart rate correctly. In 20% of patients with angina, adrenergic blockers do not provide the desired effect due to severe coronary atherosclerosis with a low ischemic threshold and impaired subendocardial blood flow .
In patients with nicotine addiction, the effectiveness of Atenolol is significantly lower than in patients who do not smoke. During therapy, there may be a decrease in the production of tear fluid, which should be warned about in patients who wear contact lenses.
The drug may mask the clinical picture of thyrotoxicosis (tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is unacceptable due to the risk of increasing the severity of the symptoms of the disease. Atenolol is able to mask tachycardia during hypoglycemia. The medication is discontinued several days before the planned general anesthesia with ether or chloroform. Otherwise, the patient is selected a drug for general anesthesia, which has minimal inotropic effects.
Intravenous administration of atropine eliminates reciprocal activation of the vagus nerve. The drug can be prescribed to patients with bronchospastic pathology if other antihypertensive drugs are ineffective or intolerant, subject to strict adherence to the dosage regimen.
If elderly people develop arterial hypotension, increasing bradycardia, ventricular arrhythmia, bronchospasm, severe disorders of the liver and kidneys, the dosage of the drug is reduced or therapy is stopped completely. If depression develops, the drug is replaced. Abrupt withdrawal can cause myocardial infarction, a severe form of arrhythmia. The drug is discontinued by gradually reducing the dosage over two weeks.
Before determining the level of normetanephrine, catecholamines, antinuclear body titers, and vanillylmandelic acid, Atenolol is discontinued. The medication affects the control of vehicles.
Recipe in Latin:
Rp: Atenololi 0.05 D. td N 30 in tab. S. 1 tablet 1 time per day.
Reception features
Doctors strongly advise people with certain health problems to pay attention to the peculiarities of taking Atenolol:
- For psoriasis, taking pills can trigger a relapse of the disease.
- In patients suffering from angina, treatment with Atenolol may lead to an increase in the number of attacks;
- In case of ischemic disease, do not abruptly stop taking the drug. Patients in this category are recommended to smoothly and gradually reduce the daily dose of tablets.
- During therapy with Atenolol, the development of thyrotoxicosis can be missed, since this drug hides the symptoms characteristic of this pathology.
- With diagnosed myasthenia gravis, there is a possibility of deterioration of the patient’s general condition and exacerbation of clinical signs of the disease.
- For hypoglycemia in people with diabetes, the tablets may affect the heart rate.
For depressive conditions and nervous disorders, therapy with Atenolol should be carried out under the supervision and strict supervision of a qualified specialist!
For a number of diseases, taking Atenolol has its own peculiarities; you should consult your doctor
Atenolol's analogs
Level 4 ATC code matches:
Biol
Metocard
Metozok
Nebilet
Nebilong
Betaxolol
Bisogamma
Aritel
Cordinorm
Vasocardin
Corvitol
Bidop
Bisoprolol
Nebivolol
Biprol
Bisoprol
Concor Cor
Lokren
Concor
Niperten
Analogues of Atenolol are the following products: Atenobene , Atenova , Atenol , Tenolol.
Reviews of Atenolol
The drug is effective for hypertension and arrhythmia, and is quite inexpensive. However, side effects are common, such as hallucinations and a decrease in blood sugar. Reviews of Atenolol Nycomed are generally better than those of drugs produced by other manufacturers.
Reviews during pregnancy are generally positive; those who used the medication mostly did not notice any side effects. However, it should be remembered that according to the results of clinical studies, such side effects on the fetus are very possible.
Use during pregnancy and lactation
Atenolol is approved for use during pregnancy, but the patient’s treatment must be under strict medical supervision.
The active ingredients of the drug penetrate the placenta into the fetus. Due to the lack of sufficient information about the effect of Atenolol tablets on the formation of organs and systems of the unborn baby, this medicine is not recommended for use during the first trimester of pregnancy.
During pregnancy, Atenolol is used only if absolutely necessary.
Further therapy is carried out under the supervision of medical specialists. Taking the drug must be stopped no later than 2 days before the expected day of birth. Otherwise, the likelihood of the following unwanted complications in the newborn increases:
- Hypoglycemia;
- Bradycardia;
- Respiratory dysfunction;
- Hypotension (low blood pressure).
Young mothers should be aware that the active ingredients of Atenolol have the ability to pass into breast milk. The use of these blood pressure pills during lactation can negatively affect the baby’s health, causing the following problems:
- Hypoglycemia;
- Bradycardia;
- A sharp decrease in blood pressure.
For this reason, during treatment with Atenolol, it is recommended to temporarily transfer the baby to artificial feeding.
Atenolol price, where to buy
Price Atenolol 25 mg, 30 tablets - 17 rubles.
50 mg, 30 pieces - 21 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
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Pharmacy Dialogue
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PaniPharmacy
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