Sotalol tabs 160mg #20

Sotalol user manual

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Sotalol is an antiarrhythmic agent, a non-selective beta-blocker.

Release form and composition

Sotalol is available in the form of tablets: biconvex, round, white [10 pcs. in a contour acheikova packing, 30 pcs. in a polymer / plastic jar (bottle); 3 packages or 1 can (bottle) in a cardboard box].
1 tablet contains:
    active substance: sotalol hydrochloride - 80 or 160 mg;
    additional components: microcrystalline cellulose, lactose monohydrate, magnesium stearate, colloidal silicon dioxide.

Pharmacodynamics

Sotalol is a class II and III antiarrhythmic drug according to the Vaughan-Williams classification, exhibiting the properties of a non-selective beta-blocker. The substance is a racemic mixture containing the D- and L-stereoisomers of sotalol. Both isomers are characterized by class III antiarrhythmic effects, however, the L-stereoisomer is responsible for virtually all beta-blocking properties.
As well as other beta-blockers, the drug actively inhibits renin secretion during exercise and at rest.
The beta-blocking effect of sotalol leads to a decrease in heart rate (HR), demonstrating a negative chronotropic effect, and causes a limited decrease in cardiac muscle contractions (negative inotropic effect). These changes in cardiac activity provide a decrease in myocardial oxygen demand, reduce the load on the heart. The antiarrhythmic effect of sotalol is due to the creation of a blockade of beta-adrenergic receptors, as well as prolongation of the action potential of myocardial cells.
The main property of the substance is its ability to increase the duration of effective refractory periods in the ventricular, atrial and additional pathways of impulse conduction. On the electrocardiogram (ECG), taken in standard leads, properties corresponding to the II and III class of antiarrhythmic drugs can be reflected in the form of prolongation of the PR, QT and QTc intervals (QT with heart rate correction) against the background of the absence of significant changes in the duration of the QRS complex.

Pharmacokinetics

After oral administration, the maximum concentration of sotalol in the blood plasma is observed after 2.5-4 hours, and the equilibrium concentration is observed within approximately 2-3 days (after using 5-6 doses). The bioavailability of the substance is 90-100%, simultaneous intake with food reduces its absorption by about 20%.
When using daily doses from 160 to 640 mg, the plasma concentration of sotalol in the blood is proportional to the dose taken. The agent is distributed in plasma, in peripheral organs and tissues, the half-life (T½) can vary from 10 to 20 hours.
The pharmacokinetic parameters of the D- and L-enantiomers of a substance are almost the same. The drug does not undergo biotransformation and does not bind to blood plasma proteins. Poorly passes through the blood-brain barrier (BBB), the level of its content in the cerebrospinal fluid is only 10% of the plasma level. The drug is excreted from the body mainly through the kidneys, unchanged - about 80-90% of the dose taken, the rest is excreted in the feces.

Indications for use

    ventricular arrhythmia: life-threatening ventricular tachyarrhythmia (to prevent recurrence), symptomatic unstable ventricular tachyarrhythmia (therapy);
    supraventricular arrhythmia: paroxysmal atrial fibrillation, paroxysmal atrial tachycardia, paroxysmal atrioventricular nodal reciprocal tachycardia of the re-entry type, paroxysmal atrioventricular reciprocal tachycardia involving additional surgical pathways, paroxysmal arrhythmias, );
    atrial fibrillation or atrial flutter (to maintain normal sinus rhythm after arresting these arrhythmias).

Contraindications

Absolute:
    sinoatrial blockade;
    atrioventricular (AV) block II – III degree;
    heart failure in the phase of decompensation;
    cardiogenic shock;
    sick sinus syndrome (SSS);
    Prinzmetal's angina;
    congenital / acquired long QT syndrome;
    severe bradycardia (with a heart rate below 50 beats / min);
    hypokalemia;
    severe peripheral circulatory disorders (including Raynaud's syndrome);
    arterial hypotension [systolic blood pressure (BP) below 90 mm Hg. Art.];
    pirouette-type ventricular tachycardia;
    cardiomegaly (without signs of heart failure);
    a period of 14 days after acute myocardial infarction against the background of a decrease in the left ventricular ejection fraction (below 40%);
    pheochromocytoma (without the concomitant use of alpha-blockers);
    metabolic acidosis;
    severe allergic rhinitis;
    chronic obstructive pulmonary disease (COPD) or bronchial asthma;
    general anesthesia leading to suppression of myocardial function (including trichlorethylene or cyclopropane);
    mental disorders: depression, anxiety, drowsiness / insomnia, depression, mood changes;
    age under 18;
    a combination with monoamine oxidase (MAO) inhibitors, with intravenous (iv) administration of slow calcium channel blockers that suppress myocardial function (for example, verapamil, diltiazem - due to an additive effect on ventricular function and AV conduction);
    syndrome of glucose-galactose malabsorption, lactase deficiency and lactose intolerance;
    lactation period;
    hypersensitivity to any of the constituents of the drug and other sulfonamide derivatives.
Relative (taking Sotalol is required with extreme caution):
    AV block I degree;
    a period within 14 days after suffering a myocardial infarction;
    lengthening of the QT interval;
    diabetes;
    impaired renal function;
    chronic heart failure (CHF) (due to a possible additional decrease in myocardial contractility and aggravation of CHF symptoms);
    disturbances in water and electrolyte balance (hypokalemia / hypomagnesemia);
    depression (including history);
    thyrotoxicosis (Sotalol is able to mask such clinical signs of thyrotoxicosis as tachycardia);
    history of allergic reactions, as well as concomitant desensitizing treatment (due to a possible increase in sensitivity to allergens, aggravation of arterial hypertension and a decrease in the therapeutic response to epinephrine);
    elderly age;
    surgical interventions;
    obliterating lesions of peripheral vessels;
    bronchospasm (history);
    psoriasis (due to the possible aggravation of the course of this disease).

Instructions for the use: method and dosage

Sotalol is taken orally 1-2 hours before meals, without breaking or chewing, with a sufficient amount of water. The dose of the drug is set individually, taking into account the severity of the disease, ECG, kidney function, patient's response to therapy and interactions with other concomitant drugs.
At the beginning of the course, it is recommended to take the agent 80 mg 2 times a day with an approximate interval of 12 hours. In case of insufficient severity of the therapeutic effect, depending on the patient's condition, a gradual increase in the daily dose to 240-320 mg, divided into 2-3 doses, is possible. The majority of patients manage to achieve a therapeutic response when using Sotalol in a total daily dose of 160-320 mg taken in 2 divided doses.
Against the background of the development of severe arrhythmias of a life-threatening nature, it is possible to increase the dose to a maximum of 480 mg per day, divided into 2-3 doses. The appointment of maximum doses is allowed only in cases where the potential benefit of therapy significantly outweighs the threat of developing adverse reactions, especially proarrhythmogenic effects.
Sotalol has the effect of class III antiarrhythmics, as a result of which it is required to control the possibility of increasing the QT interval and, if necessary, to select doses individually.
In the presence of CHF, cardiomyopathy, arterial hypertension, angina pectoris, as well as in conditions after myocardial infarction, therapy should be started in a hospital setting. Patients in these risk groups are recommended to start treatment with a daily dose of 160 mg in 1 or 2 divided doses. 7 days after the start of the course, if necessary, it is possible to gradually increase the daily dose by 80 mg at weekly intervals. The dose is increased at a rate depending on the tolerability of the drug, assessing the latter by the clinical response and the degree of induced bradycardia.
In most patients, as a result of a relatively long T½ sotalol, the drug is effective when taken 1 time per day. The dose interval is 160-320 mg per day.
In patients with functional impairment of the kidneys, there is a possibility of cumulation development, as a result of which they need to control the heart rate (at least 50 beats / min) and creatinine clearance (CC). Since sotalol is excreted mostly by the kidneys, when their activity is impaired, the T½ of the substance increases, therefore, with a CC of less than 60 ml / min, it is necessary to adjust the period between taking the drug in accordance with this table:
    CC> 60 - 12 hours;
    CC 30–59 - 24 hours;
    CC 10-29 - 36-48 hours;
    CC <10 - individual selection.
The dose of the drug should be reduced when the level of CC in the blood serum is over 120 μmol / l according to the following recommendations:
    CC <120 μmol / l (CC <1.2 mg / dl) - usual dose;
    CC 120-200 μmol / L (CC 1.2-2.3 mg / dL) - ¾ of the usual dose;
    CC 200-300 μmol / l (CC 2.3-3.4 mg / dl) - ½ the usual dose;
    CC 300-500 μmol / L (CC 3.4-5.7 mg / dL) - ¼ of the usual dose.
The duration of treatment is established by the attending physician. If one of the doses was missed, the next time the dose should not be doubled, the drug is taken as usual in the recommended amount.

Side effects

    organs of the chest and mediastinum: infrequently - bronchospasm (mainly in violation of pulmonary ventilation);
    nervous system: often - dizziness, headache, paresthesia in the extremities, light hallucinations, syncope, asthenia; with an unknown frequency - tremor, increased fatigue;
    mental disorders: often - drowsiness / insomnia, anxiety, mood changes, depression, depression;
    cardiovascular system: often - chest pain, palpitations, AV-blockade, bradycardia, shortness of breath, heart rhythm disturbances, proarrhythmia, increased symptoms of heart failure, decreased blood pressure, arrhythmia like "pirouette", edema; with an unknown frequency - cold extremities, increased angina attacks, fainting, short-term exacerbation of intermittent claudication, Raynaud's disease;
    sense organs: often - hearing impairment, change in taste, visual impairment; extremely rare - a decrease in lacrimation; with an unknown frequency - inflammation of the conjunctiva and cornea (should be considered when wearing contact lenses);
    digestive system: often - abdominal pain, dyspepsia (in the form of nausea, vomiting), constipation, diarrhea, flatulence, dryness of the oral mucosa;
    musculoskeletal and connective tissue: often - cramps, muscle weakness;
    skin and subcutaneous tissues: with an unknown frequency - psoriasiform dermatosis, itching, skin rash, redness, urticaria, alopecia;
    general disorders: often - fever, asthenia, fatigue;
    genitourinary system: often - decreased potency;
    laboratory and instrumental data: with an unknown frequency - the appearance of antinuclear antibodies, hypoglycemia (most often in the presence of diabetes mellitus or with strict adherence to diets), overestimated indicators in photometric analysis of urine for metanephrine.

Overdose

Symptoms of an overdose of Sotalol include: bronchospasm, decreased blood pressure, hypoglycemia, bradycardia, generalized seizures, loss of consciousness, ventricular tachycardia (including the "pirouette" type), lengthening of the QT interval. In case of severe overdose, symptoms of cardiogenic shock, asystole, sometimes fatal, may appear.
In this condition, it is recommended to carry out gastric lavage, intake of activated charcoal, hemodialysis, symptomatic therapy. If bradycardia occurs, intravenous jet injection of atropine is prescribed (1-2 times); intravenous rapid infusion of glucagon at a dose of 0.2 mg / kg, and then in the form of a long intravenous infusion (within 12 hours) at a dose of 0.5 mg / kg.
With a pronounced decrease in blood pressure, epinephrine is administered, with the development of bronchospasm, the use of aminophylline or inhalation of beta2-adrenoreceptor sympathomimetics is recommended. In case of atrioventricular block of 2-3 degrees and tachycardia of the "pirouette" type, it is possible to install an external temporary pacemaker. Also, with pirouette tachycardia, cardioversion is performed, epinephrine and / or magnesium sulfate is administered.

Special instructions

Sotalol therapy is carried out under the control of blood pressure, heart rate, ECG. At the beginning of the course of treatment or when adjusting the dose, an appropriate medical examination should be carried out, which includes monitoring of renal function, electrolyte content, ECG monitoring (with an assessment of the QT interval).
When the drug is discontinued, the dose must be reduced gradually, since an abrupt interruption of therapy can lead to the development of myocardial infarction and severe arrhythmias.
The patient should be aware that he needs to see a doctor if the heart rate is less than 50 beats / min.
Abrupt discontinuation of the drug in the presence of thyrotoxicosis may increase its symptoms, as a result of which it is recommended to slowly reduce the dose of Sotalol before the end of treatment.
Patients with pheochromocytoma should take the drug in combination with alpha-blockers.
In case of left ventricular dysfunction at the beginning of the course, the agent should be used with caution. Against the background of standard treatment (cardiac glycosides, diuretics, angiotensin-converting enzyme inhibitors, etc.), the drug should be taken at a lower initial dose, and then the dose should be adjusted depending on the clinical situation.
In the presence of hypokalemia / hypomagnesemia, the degree of prolongation of the QT interval and the risk of arrhythmias of the "pirouette" type may increase. Before taking Sotalol, it is necessary to correct these violations of the water-electrolyte balance.
In the case of concomitant treatment with drugs that lead to a decrease in the level of magnesium and / or potassium, or in the presence of severe / prolonged diarrhea, it is necessary to monitor the water-electrolyte balance and acid-base state.
The action of beta-blockers in smokers is reduced.
If in elderly patients during therapy arterial hypotension appears (systolic blood pressure less than 100 mm Hg), increasing bradycardia (below 50 beats / min), ventricular arrhythmia, AV blockade, bronchospasm, severe functional disorders of the kidneys and liver, it is necessary reduce the dose of Sotalol or stop taking it.
During the period of treatment, it is required to stop drinking alcohol.
Before establishing the level of normetanephrine, catecholamines, vanillyl mandelic acid in the blood and urine, as well as the presence of antinuclear antibody titers in the blood serum, the drug should be discontinued.

Influence on the ability to drive vehicles and complex mechanisms

Since during therapy there is a possibility of increased fatigue and headache, patients who drive vehicles and other complex mechanisms should be careful.

Application during pregnancy and lactation

According to the instructions, Sotalol passes through the placenta and is detected in the amniotic fluid. Beta-blockers weaken placental blood flow, which can cause intrauterine fetal death. If drug therapy is required during pregnancy, it should be discontinued 48–72 hours before the expected date of delivery due to the possible development of hypokalemia, respiratory depression, arterial hypotension and bradycardia in the newborn. In the postpartum period, these newborns are more likely to develop complications from the heart and lungs.
The use of Sotalol during pregnancy is permissible only after a thorough assessment of the ratio of all possible risk factors. The condition of newborns within 48–72 hours after delivery should be under close medical supervision.
Since it is known that the drug penetrates into breast milk, while reaching effective concentrations, if it is necessary to take it during lactation, breastfeeding should be discontinued.

Childhood use

The drug is contraindicated in children and adolescents under 18 years of age, since the safety profile of Sotalol in this age group of patients has not been studied.

With impaired renal function

In the presence of functional disorders of the kidneys, it is necessary to reduce the dose of Sotalol.

Use in the elderly

The pharmacokinetics of sotalol in elderly patients changes insignificantly, but with existing impaired renal function, it is possible to reduce the rate of its excretion and, as a result, to increase its accumulation in the body. Elderly patients should use Sotalol with caution.

Drug interactions

    class IA and III antiarrhythmics (procainamide, quinidine, disopyramide and amiodarone): a pronounced prolongation of the QT interval is possible; Sotalol can be used only after the completion of antiarrhythmic therapy, under strict control, not earlier than after 2-3 T½ of the previously used antiarrhythmic agent;
    digoxin: the threat of bradycardia is aggravated (there is no noticeable change in the level of digoxin in the blood serum);
    potassium-excreting diuretics (including hydrochlorothiazide, furosemide): hypokalemia or hypomagnesemia may develop, increasing the likelihood of pirouette-type arrhythmias;
    antidiabetic oral agents, insulin: the likelihood of hyperglycemia increases, which may require a dose adjustment of antidiabetic drugs (Sotalol is able to mask the signs of hypoglycemia);
    blockers of slow calcium channels: the risk of developing bradycardia, arterial hypotension, heart failure, conduction disturbances increases;
    tricyclic antidepressants, class I antiarrhythmics, astemizole, terfenadine, phenothiazines, some quinolone antibiotics: prolongation of the QT interval is possible (caution should be exercised with this combination);
    beta2-adrenergic agonists (isoprenaline, terbutaline, salbutamol): it may be necessary to increase the doses of these drugs;
    agents that deplete the depot of catecholamines (guanethidine, reserpine): the threat of a decrease in blood pressure and / or the occurrence of severe bradycardia is aggravated, which can cause fainting (due to excessive suppression of the tone of the sympathetic nervous system at rest);
    vasodilators, diuretics, antihypertensive and narcotic drugs, phenothiazines, barbiturates, tricyclic antidepressants: the risk of a sharp decrease in blood pressure increases;
    clonidine (with abrupt withdrawal), norepinephrine, MAO inhibitors: the likelihood of arterial hypertension increases (clonidine therapy should be gradually discontinued a few days after the end of Sotalol);
    amphotericin B, gluco- and mineralocorticosteroids (in case of systemic use), certain laxatives: hypokalemia may appear (potassium levels should be monitored);
    means for inhalation anesthesia (including tubocurarine): the risk of suppression of myocardial function and the occurrence of arterial hypotension increases;
    isozymes of the cytochrome P450 system: no interaction was observed.

Terms and conditions of storage

Store in a place protected from light, out of reach of children, at temperatures up to 25 ° C.
Shelf life is 2 years.

Reviews

There are very few reviews of Sotalol, and almost all of them testify to its effectiveness in the treatment of arrhythmias. Patients who have taken the drug also indicate that it must be used strictly following the recommendations and only as directed by a doctor.
The disadvantages of the drug include addiction and weakening of the effect with prolonged use, as well as the possible development of side effects.

Terms of sell

You can buy Sotalol without a prescription.