Sotalol pills 80mg, 20pcs

Composition

Composition per tablet: Active ingredient:  Sotalol hydrochloride 80.0 mgm Auxiliary substances: Lactose monohydrate 97.0 mg, Microcrystalline cellulose 120.0 mg, Colloidal silicon dioxide 1.5 mg, Magnesium stearate 1.5 mg

Pharmacological action

Pharmacotherapy group: antiarrhythmic agent

ATX Code: C07AA

Pharmacodynamics :

Sotalol is an antiarrhythmic agent of Class II and III according to the Vaughan-Williams classification, which has the properties of a non-selective beta-blocker. It is a racemic mixture consisting of D-and L-stereoisomers of sotalol. Both isomers have Class III antiarrhythmic effects, while the L-stereoisomer is responsible for almost all beta-blocking properties. Like other beta-blockers, sotalol suppresses the secretion of renin, and this effect is pronounced both at rest and during exercise. The beta-blocking effect of the drug Causes a decrease in heart rate (HR) (negative chronotropic effect) and a limited decrease in the strength of heart contractions (negative inotropic effect). These changes in cardiac activity reduce the need for oxygen in the myocardium and the amount of load on the heart. The antiarrhythmic properties of sotalol are associated with both the ability to block beta-adrenergic receptors and the ability to prolong the action potential of the myocardium. The main effect of sotalol is to increase the duration of effective refractory periods in the atrial ventricular and additional pathways of pulse conduction. On an electrocardiogram taken in standard leads: properties corresponding to Class II and III can be reflected in the form of prolongation of the PR QT and QTc intervals (QT with heart rate correction) in the absence of noticeable changes in the duration of the QRS complex. Pharmacokinetics: Oral bioavailability is 90% -100%. The maximum concentration in blood plasma is reached in 25-4 hours after oral use and the equilibrium concentration is within 2-3 days (i. e. after taking 5-6 doses when taken 2 times a day). The absorption of sotalol decreases by approximately 20% when taken simultaneously with food compared to fasting. In the dose range from 160 to 640 mg/day, the concentration of sotalol in the blood plasma is proportional to the dose taken. Distribution occurs in the blood plasma as well as in peripheral organs and tissues with a half life of 10-20 hours Sotalol does not bind to plasma proteins and is not metabolized. The pharmacokinetics of the D-and L-enantiomers of sotalol are almost identical. Poorly penetrates the blood-brain barrier and its concentration in the cerebrospinal fluid is only 10% of the concentration in the blood plasma. The main route of elimination from the body is excretion through the kidneys. From 80% to 90% of the administered dose is excreted unchanged by the kidneys and the rest-through the intestines. Patients with impaired renal function should be prescribed smaller doses of the drug. Pharmacokinetics do not change significantly with the patient’s age although impaired renal function in elderly patients reduces the rate of elimination which leads to increased accumulation of sotalol in the body.

Indications

Ventricular arrhythmia:

• prevention of relapses of life-threatening ventricular tachyarrhythmia;
• treatment of symptomatic unstable ventricular tachyarrhythmia.

Supraventricular arrhythmia:

• prevention of paroxysmal atrial tachycardia paroxysmal atrial fibrillation paroxysmal atrioventricular nodal reciprocal tachycardia of the “re-entry” type paroxysmal atrioventricular reciprocal tachycardia involving additional pathways and paroxysmal supraventricular tachycardia after surgery;
• maintenance of normal sinus rhythm after fibrillation conversion atrial fibrillation or atrial flutter.

Use during pregnancy and lactation

No adequate controlled trials have been conducted in pregnant women. Sotalol passes through the placenta and is found in the amniotic fluid. Beta-blockers reduce placental blood flow, which can lead to intrauterine fetal death. In addition, adverse events (in particular hypoglycemia and bradycardia) may occur in the fetus and in the newborn. In the case of therapy during pregnancy, the drug should be discontinued 48-72 hours before the expected date of delivery due to the possibility of developing bradycardia, arterial hypotension, hypokalemia and respiratory depression in newborns. There is an increased risk of heart and lung complications in newborns in the postpartum period. The use of sotalol during pregnancy is possible only if the benefit to the mother exceeds the potential risk to the fetus. It is necessary to carefully monitor the condition of newborns within 48-72 hours after delivery. Sotalol penetrates into breast milk and reaches effective concentrations there. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

Contraindications

Mental disorders: anxiety sleep disorders (drowsiness or insomnia) mood changes depression state of depression;Hypersensitivity to sotalol, other sulfonamide derivatives and other components of the drug;Decompensated heart failure;Cardiogenic shock;Atrioventricular (AV) block II or III degree;Sinoatrial block;Sinus node weakness syndrome;Severe bradycardia (heart rate less than 50 beats/min);Prinzmetal angina pectoris;Congenital or acquired long QT syndrome;Hypokalemia;Hypotension (systolic blood pressure (BP) less than 90 mm Hg);Severe peripheral circulatory disorders including Raynaud’s syndrome;Bronchial asthma or chronic obstructive pulmonary disease (COPD);Metabolic acidosis;Pheochromocytoma without concomitant use of alpha-blockers; Cardiomegaly (without signs of heart failure);Acute myocardial infarction in the presence of acute myocardial infarction. first 2 weeks after a myocardial infarction and with a decrease in the left ventricular ejection fraction (less than 40%);General anesthesia that causes suppression of myocardial function (for example, cyclopropane or trichloroethylene);Ventricular tachycardia of the “pirouette”type;Severe allergic rhinitis;Simultaneous use of monoamine oxidase inhibitors (MAO) simultaneous intravenous use of “slow” calcium channel blockers of the Verapamil type up to 18 years (efficacy and safety). safety not established); lactose intolerance lactase deficiency and glucose-galactose malabsorption syndrome.

With caution:

Caution should be exercised when prescribing Sotalol to patients who have recently had a myocardial infarction (not earlier than 2 weeks after a myocardial infarction) with diabetes mellitus psoriasis impaired renal function atrioventricular block of the first degree chronic heart failure with a violation of the water-electrolyte balance: hypomagnesemia hypokalemia; with thyrotoxicosis depression (including in the anamnesis) with prolongation of the QT interval in the elderly with surgical interventions allergic reactions a history of adverse reactions (possibly increased sensitivity to allergens, increased hypertension, and decreased therapeutic response to epinephrine) as well as against the background of desensitizing therapy for obliterating peripheral vascular diseases with bronchospasm (in the anamnesis).

Side effects

According to the World Health Organization (WHO), adverse events are classified according to their frequency as follows: common (>1/100 ><1/10) uncommon (>1/1000 <1/10) uncommon (><1/100) rare (>1/10000 <1/100) rare (><1/1000) and very rare (Mental disorders: often: feeling anxious sleep disturbance (drowsiness or insomnia) mood changes depression state of depression. Nervous system disorders: common: headache dizziness light hallucinations asthenia paresthesia in the extremities syncopal state; frequency unknown: increased fatigue tremor. Sensory disorders: common: visual disturbances hearing disturbances changes in taste sensations; very rare: decreased lacrimation; frequency unknown: inflammation of the cornea and conjunctiva (should be considered when wearing contact lenses). From the cardiovascular system: often: bradycardia palpitation cardiac arrhythmia dyspnea chest pain AV block increased symptoms of heart failure proarrhythmia pirouette arrhythmia decreased blood pressure edema; frequency unknown: fainting increased angina attacks cold extremities Raynaud’s disease short-term exacerbation of intermittent claudication. From the thoracic and mediastinal system: infrequently: bronchospasm (especially with impaired pulmonary ventilation). From the digestive system: often: dyspepsia (nausea vomiting) diarrhea constipation dryness of the oral mucosa abdominal pain flatulence. From the rut and subcutaneous tissues: frequency unknown: skin rash pruritus redness psoriasis dermatosis alopecia urticaria. Musculoskeletal and connective tissue disorders: common: muscle weakness convulsions. From the genitourinary system: often: reduced potency. General disorders and disorders at the injection site: often: increased fatigue asthenia fever. Laboratory and instrumental data: frequency unknown: formation of antinuclear antibodies hypoglycemia (most likely in patients with diabetes mellitus or with strict adherence to diets) there may be overestimated results in the photometric analysis of urine for metanephrine.

Interaction

Antiarrhythmic drugs.Concomitant use of sotalol with Class IA antiarrhythmics (disopyramide quinidine procainamide) and Class III antiarrhythmics (for example, amiodarone) may cause marked prolongation of the QT interval. Digoxin. The use of sotalol does not significantly affect the concentration of digoxin in the blood serum. Arrhythmogenic effects developed more frequently in patients using both sotalol and digoxin (risk of bradycardia). Slow calcium channel blockers (BMCC’). Concomitant use of beta-blockers and BMCC can lead to hypotension, bradycardia, conduction disturbances, and heart failure. Concomitant use of beta-blockers with BMCC inhibiting myocardial function (for example, verapamil and diltiazem) should be avoided due to the additive effect of these agents on AV conduction and ventricular function. Intravenous use of these drugs should be avoided when sotalol is used (except in cases of emergency medicine). Potassium-withdrawing diuretics (e. g. furosemide hydrochlorothiazide). The use of diuretics of this type can lead to hypokalemia or hypomagnesemia, which increases the likelihood of arrhythmia of the “pirouette”type. Drugs that increase the duration of the QT interval. It should be used with caution with drugs that prolong the QT interval such as Class I antiarrhythmics phenothiazines tricyclic antidepressants terfenadine and astemizole as well as some quinolone antibiotics. Drugs that reduce the level of catecholamines. Concomitant use of depot-depleting catecholamines (for example, reserpine and guanethidine) with beta-blockers leads to excessive suppression of the tone of the sympathetic nervous system at rest. Patients should be carefully monitored for possible signs of a marked decrease in blood pressure and / or severe bradycardia, which may lead to syncope. Insulin or hypoglycemic agents for oral use. Hyperglycemia may develop in this case, it is necessary to adjust the doses of hypoglycemic agents. Sotalol may mask the symptoms of hypoglycemia. Beta-2-adrenomimeptics. When co-administered with sotalol, higher doses of beta-2-adrenomimetics such as salbutamol terbutaline and isoprenaline may be required. Concomitant use of norepinephrine or MAO inhibitors, as well as abrupt withdrawal of clonidine, may cause hypertension. In this case, the elimination of clonidine should be carried out gradually and only a few days after the end of taking sotalol. Tricyclic antidepressants barbiturates phenothiazines narcotic and antihypertensive drugs diuretics and vasodilators can cause a sharp decrease in blood pressure. The use of inhaled anesthetics, including tubocurarin, while taking sotalol increases the risk of myocardial function suppression and hypotension. Cytochrome P 450 isoenzymes. No interaction is expected with drugs that are metabolized by cytochrome P 450 isoenzymes. Lmfotericin B gduco-and mineralocorticosteroids (with systemic use) some laxatives can cause hypokalemia. It is necessary to control the potassium content when used simultaneously with sotalol.

How to take, course of use and dosage

Inside 1-2 hours before meals without chewing with a sufficient amount of liquid. The dose of the drug is selected individually depending on the severity of the disease, assessment of the electrocardiogram (ECG), renal function, interaction with other medications taken and the patient’s response to treatment. The initial dose is 80 mg 2 times a day (approximately at intervals of 12 hours). If the therapeutic effect is not sufficiently pronounced, after an appropriate clinical assessment of the patient’s condition, the dose can be gradually increased to 240-320 mg per day, divided into 2-3 doses. In most patients, the therapeutic effect is achieved with a daily dose of 160-320 mg divided into 2 doses. With life-threatening severe arrhythmias, it is possible to increase the dose to a maximum of 480 mg divided into 2 or 3 separate doses. However, such doses can only be prescribed in cases where the potential benefit outweighs the risk of side effects, especially proarrhythmogenic effects. Due to the presence of the drug effect of class III antiarrhythmics, the possibility of increasing the QT interval should be monitored and, if necessary, individual dose selection should be carried out. In patients with cardiomyopathy or chronic heart failure (CHF), angina pectoris, arterial hypertension after a previous myocardial infarction, it is recommended to start therapy in a hospital setting. The initial dose is 160 mg / day in 1 or 2 divided doses. After a week, the dose can be increased by 80 mg / day at weekly intervals, if necessary. The rate of dose increase depends on the patient’s tolerance to the drug, which is assessed in particular by the degree of induced bradycardia and the therapeutic response to the therapy. Due to the relatively long half-life in most patients, Sotalol is effective when taken once a day. Dose range: 160-320 mg / day. Use in patients with impaired renal function patients with impaired renal function are at risk of accumulation, so they need to monitor the value of creatinine clearance (CC) and heart rate (at least 50 beats/min). Since sotalol is mainly excreted by the kidneys and its half-life increases, the dosage regimen (time between drug doses) should be changed when the creatinine clearance is less than 60 ml / min according to the table below:

The dosage of the drug in case of impaired renal function should be reduced if the concentration of serum creatinine clearance exceeds 120 mmol / l in accordance with the following recommendations:–

The duration of therapy is determined by the doctor. In the event that you forget to take the pill in time, the next time you should not double the dose, you should only take the prescribed amount of Sotalol.

Overdose

Symptoms: decreased blood pressure bradycardia bronchospasm hypoglycemia loss of consciousness generalized convulsive seizures prolongation of the QT interval ventricular tachycardia (including “pirouette” type); in severe cases-symptoms of cardiogenic shock asystole sometimes fatal. Treatment: gastric lavage hemodialysis the use of activated charcoal. Symptomatic therapy:Bradycardia: atropine-1-2 times intravenously; glucagon-first in the form of a short intravenous infusion at a dose of 02 mg/kg of body weight, then at a dose of 05 mg/kg of body weight intravenously infusion for 12 hours Atrioventricular block of 2-3 degrees: a temporary artificial pacemaker is possible. Marked reduction in blood pressure: epinephrine is effective. Bronchospasm: amiophylline or beta-2-adrenergic sympathomimetics (inhaled). Pirouette-type tachycardia: cardioversion – setting a temporary artificial pacemaker (if necessary) with epinephrine and / or magnesium sulfate.

Special instructions

Treatment with Sotalol is carried out under the control of heart rate and blood pressure ECG. Starting sotalol therapy or changing the dosage should be accompanied by an appropriate medical examination including ECG monitoring with an assessment of the QT interval monitoring of renal function measurement of electrolyte content and concomitant therapy. If Sotalol is discontinued, the dose should be reduced gradually, especially in patients with coronary heart disease after a myocardial infarction or arterial hypertension. Do not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually. The patient should be trained in the method of calculating heart rate and instructed to consult a doctor if the heart rate is less than 50 beats/min. With thyrotoxicosis, sotalol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with giretoxicosis is contraindicated because it can increase the symptoms of the disease. When prescribing sotalol to patients with pheochromocytoma, alpha-blockers should be prescribed simultaneously. Sotalol should be administered with caution to patients:

• with diabetes mellitus with pronounced fluctuations in the concentration of glucose in the blood as well as with a strict diet;
• with pheochromocytoma (simultaneous use of alpha – blockers is necessary);
• with a history or family history of psoriasis;
• with impaired renal function;
• the elderly.

Caution should be exercised when using sotalol in patients with CHF: beta-blockers can further reduce myocardial contractility and provoke worsening of the symptoms of CHF. It should be used with caution at the beginning of therapy in patients with left ventricular dysfunction. With standard therapy (angiotensin-converting enzyme inhibitors, diuretics, cardiac glycosides, etc. ), it is necessary to prescribe a lower initial dose of the drug and then select the dose taking into account the clinical situation. Sotalol can only be used after previous antiarrhythmic therapy if carefully monitored and after at least 2-3 half-lives of the previously used antiarrhythmic agent (see the section “Interaction with other drugs”). Use with extreme caution when indicated in the anamnesis for allergic reactions as well as against the background of desensitizing therapy because sotalol suppresses sensitivity to allergens. Sotalol should not be used in patients with hypokalemia or hypomagnesemia until the existing disorders are corrected. These conditions can increase the degree of prolongation of the QT interval and increase the likelihood of arrhythmia of the “pirouette”type. These violations should be corrected before starting the use of Sotalol. It is necessary to monitor the water-electrolyte balance and acid-base state in patients with severe or prolonged diarrhea and in patients receiving medications that cause a decrease in the content of magnesium and / or potassium in the body. When prescribing beta-blockers to patients receiving hypoglycemic agents, caution should be exercised since hypoglycemia may develop during prolonged breaks in food intake, and its symptoms such as tachycardia or tremor may be masked by the action of sotalol. In smokers, the effectiveness of beta-blockers is lower. Patients who use contact lenses should take into account that during therapy it is possible to reduce the production of tear fluid. In case of increasing bradycardia (less than 50 beats/min)in elderly patients. hypotension (systolic blood pressure less than 100 mm Hg) AV blockage of bronchospasm ventricular arrhythmia severe liver and kidney function disorders should reduce the dose of the drug or discontinue therapy. It is recommended to stop therapy if you develop depression caused by taking beta-blockers. Beta-blockers can worsen the course of psoriasis. Like other beta-blockers, sotalol should be used with caution in patients who have undergone surgery. For the duration of therapy, it is necessary to exclude alcohol intake. The drug should be discontinued before determining the normetanephrine and vanillylmindalic acid catecholamines in the blood and urine; titers of antinuclear antibodies.

Influence on the ability to drive vehicles and mechanisms:

Caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions (risk of developing headaches and fatigue).

Storage conditions

In a dark place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 2 years. Do not use after the expiration date.

Active ingredient

Sotalol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets