Atenolol

ATENOLOL-ASTRAFARM tablets 50 mg, tablets 100 mg

Instruction manual

For medical use of the drug

Atenolol-Astrapharm

(atenolol-astrapharm)

Structure:

Active substance: atenolol;

1 tablet contains atenolol 50 mg or 100 mg;

Excipients:

for tablets of 50 mg: lactose, monohydrate; magnesium stearate; corn starch;

for 100 mg tablets: lactose, monohydrate; magnesium stearate; potato starch.

Dosage form.

Tablets.

Basic physicochemical properties: tablets of white or almost white color, round in shape with a biconvex surface and a risk on one side.

Pharmacotherapeutic group.

Selective β-adrenergic receptor blockers. Code ATX C07A B03.

Pharmacological properties.

Pharmacodynamics

Cardioselective β-adrenoreceptor blocker. It has an antianginal, antihypertensive and antiarrhythmic effect. It has no internal sympathomimetic and membrane-stabilizing activity. It reduces the automatism of the sinus node, slows atrioventricular conduction, reduces myocardial contractility and its oxygen demand. It has a negative chrono-, dromo-, batmo- and isotropic effect.

Pharmacokinetics

After oral administration, 50-60% of atenolol is absorbed in the digestive tract. The maximum concentration in blood plasma (2 μg / ml) is observed after 2–4 hours. The elimination half-life makes 6–7 hours. Less than 5% of atenolol binds to blood proteins. Atenolol is a hydrophilic agent that penetrates poorly through the blood-brain and placental barrier and passes into breast milk. Atenolol is slightly metabolized (less than 10%) in the liver. Most of atenolol (85%) is excreted in the urine in an unchanged state.

The elimination half-life in patients with renal failure may be longer. It is removed during hemodialysis.

Clinical characteristics.

Indications.

• Hypertension treatment.

• Treatment and prevention of angina attacks (chronic stable and unstable angina, especially in the case of combination with tachycardia and hypertension).
• Heart rhythm disturbance (arrhythmia, sinus tachycardia, prevention of supraventricular tachycardia, paroxysmal supraventricular tachycardia, atrial fibrillation and flutter; ventricular (ventricular arrhythmias), including those caused by increased physical exertion, the use of gastric urinary tract therapy and
• Myocardial infarction (treatment and prevention to reduce mortality and reduce the risk of re-infarction).

Contraindications

• Hypersensitivity to atenolol or to other β-adrenergic receptors, or to any components of the drug; acute heart failure; cardiogenic shock; atrioventricular block of the II and III degrees; weak sinus syndrome; sinoatrial block; sinus bradycardia (heart rate less than 45 per minute); arterial hypotension (systolic pressure less than 90 mm Hg. Art.); bronchial asthma; metabolic acidosis; late stages of peripheral circulation disturbance; concomitant use of MAO inhibitors (with the exception of MAO-B inhibitors); untreated pheochromocytoma; renal failure; childhood.

Interaction with other drugs and other types of interactions.

With the simultaneous use of atenolol and:

- antidiabetic agents for oral use, such as insulin, may enhance or prolong their action. In this case, the symptoms of hypoglycemia (especially tachycardia and tremor) may mask or disappear. In this regard, it is necessary to carry out regular monitoring of blood sugar;

- tricyclic antidepressants, barbiturates, phenothiazides, nitroglycerin, diuretics, vasodilators and other antihypertensive agents (e.g. prazosin) may increase the antihypertensive effect;

- calcium channel blockers (such as nifedipine), in addition to enhancing the hypotensive effect, heart failure may develop;

- calcium channel blockers with a negative isotropic effect (such as verapamil, diltiazem), their action may be enhanced, especially in patients with impaired ventricular function and / or atrioventricular conduction, which increase the risk of hypotension and bradycardia. If intravenous administration of verapamil is necessary, this should be done no less than 48 hours after the withdrawal of atenolol;

- cardiac glycosides, reserpine, α-methyldopa, guanfacini and clonidine, a significant slowdown in heart rate may occur;

- indomethacin may decrease the antihypertensive effect of atenolol;

- narcotic drugs and antiseptics enhances the antihypertensive effect. In this case, the additive, negative isotropic effect of both agents is manifested;

- peripheral muscle relaxants (for example, suxamethonium, tubocurarine) may increase neuromuscular blockade, therefore, before an operation accompanied by anesthesia, the anesthesiologist should be informed that the patient is taking the drug Atenolol-Astrafarm;

- aminophylline and theophylline may inhibit therapeutic effects;

- lidocaine may reduce its excretion and increase the risk of toxic effects of lidocaine;

- sympathomimetic drugs, for example, adrenaline, can help reduce the effect of β-blockers.

In patients taking both Atenolol-Astrafarm and clonidine, the latter can be canceled only a few days after discontinuation of treatment with the drug.

Features of the application.

In the treatment with atenolol, calcium channel blockers such as verapamil and diltiazem or other antiarrhythmic drugs (for example, disopyramide) should not be administered intravenously.

The exception is patients who are being treated in intensive care units.

In all these cases, the doctor must carefully weigh the benefit / risk ratio by prescribing the drug Atenolol-Astrafarm.

If thrombocytopenic or non-thrombocytopenic purpura occurred in patients treated with other β-blockers, it is necessary to bear in mind the possibility of this side effect in the treatment of atenolol.

It should be remembered that while taking atenolol in extremely rare cases, manifestation of latent diabetes mellitus or worsening of the condition of patients with diabetes mellitus is possible. Violations of lipid metabolism are sometimes observed: at a level of total cholesterol that remains normal, the level of high density lipoproteins decreases and the level of triglycerides in blood plasma rises.

Do not change the dosage or stop treatment with atenolol without consulting a doctor. With a sudden withdrawal of the drug, a withdrawal syndrome may develop. Therefore, drug withdrawal and dose reduction should occur slowly and gradually.

With special care and only under strict medical supervision, it is necessary to prescribe Atenolol-Astrapharm:

• with atrioventricular block I degree;
• with diabetes with fluctuations in blood sugar (due to the possibility of a severe hypoglycemic condition;
• in case of prolonged hunger strike and severe physical exertion (severe hypoglycemic conditions may occur);
• with pheochromocytoma (without α₁-adrenoreceptors);
• in case of impaired liver and / or kidney function (the appointment of atenolol in this category of patients requires constant monitoring of the dynamics of the functional state of the liver and / or kidneys);
• in the presence of psoriasis or psoriasis in a personal or family history;
• patients with impaired peripheral circulation, including Raynauds syndrome;
• patients undergoing desensitizing therapy or with a history of severe allergic reactions;
• with thyrotoxicosis, atenolol can mask the clinical signs of hyperthyroidism.

β-blockers are not recommended for use with vasospastic angina (Prinzmetal angina).

Atenolol-Astrafarm should be used with caution in patients with myasthenia gravis.

If it is necessary to carry out surgical interventions, it is recommended to discontinue therapy with Atenolol-Astrafarm 24 hours before the surgical intervention or choose an anesthetic with minimal negative inotropic effect.

With thyrotoxicosis, atenolol can mask the symptoms of hypoglycemia, in particular tachycardia.

For elderly patients, treatment is recommended to start with the lowest doses (the dose can be increased under the control of blood pressure and heart rate).

In case of manifestation in these patients of severe bradycardia, arterial hypotension, rhythm disturbance, conduction or other complications, it is necessary to reduce the dose of atenolol or to cancel it.

The drug contains lactose, so it should not be prescribed to patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.

Use during pregnancy or lactation.

Atenolol crosses the placental barrier.

During pregnancy (especially in the first trimester), the drug Atenolol-Astrafarm is used only when the expected benefit to the mother outweighs the potential risk to the fetus, since there is still no sufficient experience of its use by pregnant women, especially in the early stages. If women took atenolol, then due to the possibility of a child having bradycardia, hypoglycemia and respiratory depression, treatment should be stopped at least 24–48 hours before delivery. If this is not possible, then the infant should be closely monitored for 24–48 hours after birth.

Atenolol passes into breast milk, so you should stop breast-feeding during treatment with the drug.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

At the beginning of treatment, with an increase in dosing and the development of adverse reactions, the reaction rate may decrease, so you should refrain from driving vehicles and working with precise mechanisms.

Dosage and administration.

The tablets are swallowed without chewing and washed down with a small amount of liquid, before meals, preferably at the same time.

The doctor sets the dose of the drug and the duration of treatment individually, depending on the therapeutic effect obtained.

Myocardial infarction: after intravenous administration, 12 mg after injection are prescribed 50 mg orally and 100 mg after another 12 hours.

Chronic stable and unstable angina: 100 mg of atenolol is usually prescribed 1 time per day or 50 mg, which is taken 2 times.

Arterial hypertension: treatment, as a rule, begins with the use of 100 mg of Atenolol-Astrafarm 1 time per day. Some patients need only 50 mg per day. The effect is observed after 2 weeks. In case of inefficiency, atenolol is used along with diuretics.

Supraventricular (supraventricular) and ventricular (ventricular) arrhythmias: Atenolol-Astrafarm is prescribed 1-2 times a day, 50-100 mg each.

The maximum daily dose is 200 mg.

In patients with significant impaired renal function, the doses of Atenolol-Astrafarm depend on the level of creatinine clearance (CC): with CC 10-30 ml / min, the dose is reduced by 2 times (50 mg per day or every other day), and with CC less than 10 ml / min dose is reduced by 4 times compared with conventional.

Patients on hemodialysis should use 50 mg of the drug after each dialysis.

This must be done in a hospital setting, as a marked decrease in blood pressure can occur.

Children.

The drug is not used in children.

Overdose.

Symptoms: the clinical picture depends on the degree of intoxication and is manifested mainly by a violation of the cardiovascular and central nervous systems.

An overdose can lead to arterial hypotension, bradycardia, heart failure and cardiogenic shock. In severe cases, respiratory disorders, bronchospasm, vomiting, impaired consciousness are observed; extremely rarely - generalized convulsive attacks.

Treatment: 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 is stopped. In intensive care units, careful monitoring of vital parameters should be carried out and, if necessary, corrected.

If necessary, appoint:

• atropine (0.5–2 mg intravenously as a bolus);
• glucagon: the initial dose of 1-10 mg intravenously (stream), then 2-2.5 mg / hour in the form of a long infusion;
• sympathomimetics depending on body weight and effect (dopamine, dobutamine, isoprenaline, oxyprenaline or adrenaline).

If refractory to bradycardia therapy is observed, temporary pacing is possible.

With bronchospasm, β is prescribed₂-sympathomimetics in the form of an aerosol (with an insufficiency of the effect also intravenously) or aminophylline intravenously.

With generalized seizures, slow intravenous administration of diazepam is prescribed.

It is removed by hemodialysis.

Adverse Reactions

On the part of the cardiovascular system: bradycardia, arterial hypotension, impaired atrioventricular conduction (up to cardiac arrest) and manifestations of symptoms of heart failure, a feeling of cold and paresthesia in the limbs. in some cases, in patients with angina pectoris, an increase in seizures cannot be ruled out.

From the nervous system: dizziness, feeling tired, headache, sleep disturbances, nightmares, depressive disorders, hallucinations, psychoses, insomnia or drowsiness, confusion.

From the digestive tract: dyspepsia, diarrhea, nausea, constipation, hepatotoxicity, dry mouth, impaired transamiasis, intrahepatic cholestasis.

From the endocrine system: the development of a hypoglycemic state is possible, especially in patients with diabetes mellitus with hypoglycemic therapy.

On the part of the immune system: itching, redness of the skin, exanthema, photosensitivity, hypersensitivity reactions (angioedema), skin rashes (exacerbation of psoriasis), urticaria rashes, increased levels of antinuclear antibodies.

From the urinary system: in some cases, there were cases of impaired libido and potency, gynecomastia, impotence, and difficulty urinating.

From the respiratory system: in patients prone to possible manifestations of bronchial obstruction; bronchospasm.

From the blood system: purpura, thrombocytopenia.

Other: conjunctivitis or decreased secretion of the lacrimal glands, increased perspiration, blurred vision, muscle weakness, dry eyes, alopecia, psoriasis-like skin reactions.

Shelf life.

3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 ⁰s.

Keep out of the reach of children.

Packaging.

10 tablets in a blister; 2.6, 9 or 10 blisters per box.

Vacation category.

On prescription.

Manufacturer.

Astrafarm LLC, Ukraine.

The location of the manufacturer and the address of the place of his activity.

08132, Kiev region, Kiev-Svyatoshinsky district, city of Cherry, st. Kiev, 6.