Sotalol pills 160mg, 20pcs

Composition

Composition for one tablet of 160 mg:

Active ingredient:

sotalol hydrochloride – 160,00 mg.

Auxiliary substances:

lactose monohydrate (milk sugar) – 157.30 mg,

corn starch-30.40 mg,

sodium carboxymethyl starch-15.20 mg,

povidone-K 25-1 1.40 mg,

magnesium stearate-3.80 mg,

colloidal silicon dioxide-1.90 mg

Pharmacological action

Pharmacotherapy group: Beta-adrenoblocker Non-selective ATX code: C07AAFarmacodynamics: 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 actions.

Sotalol does not have its own sympathomimetic and membrane-stabilizing activity.

Like other beta-blockers, sotalol suppresses the secretion of renin, and this effect is pronounced both at rest and during exercise.

The beta-adrenoblocking effect of sotalol 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.

Pharmacokinetics:

Absorption rate

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 40 to 640 mg/day, the concentration of sotalol in blood plasma is proportional to the dose taken.

The pharmacokinetics of the D-and L-enantiomers of sotalol are almost identical.

Distribution

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. Poorly penetrates the blood-brain barrier and its concentration in the cerebrospinal fluid is only 10% of the concentration in the blood plasma.

Metabolism

Sotalol is not metabolized.

Deduction

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.

The half-life of sotalol is 10-20 hours.

Special patient groups

Patients with impaired renal function should use 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

Pregnancy

No adequate controlled trials have been conducted in pregnant women. In animal studies, the use of sotalol did not cause teratogenic or other damaging effects on the fetus.

The use of the drug Sotalol during pregnancy, especially in the first trimester, is possible only for vital indications when the benefit of the use for the mother exceeds the possible risk of adverse events in the fetus/child.

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, premature birth, and the birth of an immature fetus. In addition, adverse events (in particular hypoglycemia and bradycardia) may occur in the fetus and 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. It is necessary to carefully monitor the condition of newborns within 48-72 hours after delivery.

Breast-feeding period

Sotalol penetrates into breast milk and reaches effective concentrations there. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Contraindications

– Hypersensitivity to sotalol other components of the drug and to other derivative of sulfonamide;

signs of the syndrome of weakness of the sinus node, including sinoauricular (sinoatrial) blockade except the existence of a functioning artificial pacemaker of the heart;

– the atrioventricular (AV) blockade II and III degree;

– congenital or acquired long QT syndrome or the use of drugs that may prolong the QT interval (see section “Interaction with other medicines”);

– fusiform bidirectional ventricular tachycardia (polymorphic ventricular tachycardia type “pirouette”) or the use of drugs associated with the violation (see section “Interaction with other medicines”);

– symptomatic sinus bradycardia (heart rate less than 50 beats/min);

– uncontrolled congestive heart failure (CHF) CHF including the right ventricle due to pulmonary hypertension;

– cardiogenic shock;

– General anesthesia causes suppression of the myocardial function;

– arterial hypotension (systolic blood pressure (BP) less than 90 mm Hg. St. ) except due to arrhythmias;

severe peripheral circulatory disorders including Raynaud’s syndrome;

– bronchial asthma or chronic obstructive pulmonary disease (COPD) in history;

metabolic acidosis;

renal insufficiency (creatinine clearance < 10 ml/min);

– pheochromocytoma (without the simultaneous use of alpha – blockers);

– the period of breastfeeding;

– age under 18 years (effectiveness and safety not established);

– lactose intolerance lactase deficiency syndrome glucose-galactose malabsorption.

With caution:

Caution should be exercised when using Sotalol in patients who have recently had a myocardial infarction (not earlier than 2 weeks after a myocardial infarction) diabetes mellitus psoriasis impaired renal function (creatinine clearance more than 10 ml/min) atrioventricular (AV) blockade of the first degree chronic heart failure with violations of the water-electrolyte balance: hypomagnesemia hypokalemia; with prolongation of the QT interval in the elderly during surgical interventions allergic reactions in the anamnesis (possibly increased sensitivity to allergens increased severity of hypertension and decreased therapeutic response to epinephrine) as well as against the background of desensitizing therapy for obliterating peripheral vascular diseases and bronchospasm (in the anamnesis).

Side effects

According to the World Health Organization, 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 of anxiety sleep disturbance (drowsiness or insomnia) mood changes depression state of depression.

Nervous system disorders:  often – headache dizziness light hallucinations asthenia paresthesia in the extremities syncopal state; frequency unknown-tremor.

Visual disturbances:  often-visual disturbances; very rarely-reduced lacrimation; frequency unknown-inflammation of the cornea and conjunctiva (should be considered when wearing contact lenses).

Hearing disorders and labyrinth disorders:  often – hearing loss.

Cardiac disorders:  often – bradycardia palpitation heart rhythm disturbance shortness of breath chest pain AV block increased symptoms of heart failure proarrhythmia polymorphic ventricular tachycardia of the “pirouette” type; frequency unknown-increased angina attacks.

Vascular disorders:  often-decreased blood pressure peripheral edema; frequency unknown-syncope cold extremities Raynaud’s disease short-term exacerbation of intermittent claudication.

Respiratory, thoracic and mediastinal disorders: infrequently-bronchospasm (especially in case of violation of pulmonary ventilation).

Disorders of the gastrointestinal tract: often-changes in taste dyspepsia (nausea vomiting) diarrhea constipation dryness of the oral mucosa abdominal pain flatulence.

Skin and subcutaneous tissue disorders: frequency unknown-skin rash pruritus skin redness psoriasis dermatosis alopecia urticaria.

Musculoskeletal and connective tissue disorders: often-muscle weakness and cramps.

Genital and breast disorders: often-a decrease in potency.

General disorders and disorders at the injection site: often – increased fatigue asthenia fever.

Laboratory and instrumental data: the frequency is unknown – an increase in the titer of antinuclear antibodies may be observed with excessive results in the photometric analysis of urine for methanephrine (O-methyladrenaline).

Metabolic and nutritional disorders: frequency unknown-hypoglycemia (most likely in patients with diabetes mellitus or with strict adherence to a diet).

Interaction

Antiarrhythmic drugs

Concomitant use of sotalol with Class IA antiarrhythmics (disopyramide quinidine procainamide) and Class III antiarrhythmics (for example, amiodarone dronedarone) may cause prolongation of the QT interval.

The use of sotalol does not significantly affect the concentration of digoxin in the blood serum. Arrhythmogenic effects were more common in patients taking sotalol and digoxin concomitantly; however, this may be due to chronic heart failure, which is a risk factor for arrhythmogenic effects in patients receiving digoxin.

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 polymorphic ventricular tachycardia of the “pirouette” type.

Drugs that increase the duration of the QT interval

Sotalol should be used with extreme caution simultaneously with drugs that prolong the QT interval such as Class I antiarrhythmics phenothiazine derivatives tricyclic antidepressants H 1-antihistamines (terfenadine and astemizole) as well as some quinolone antibiotics.

Drugs that reduce the concentration of catecholamines

Concomitant use of depot-depleting catecholamine drugs (e. g. 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-adrenomimetics

When co-administered with sotalol, higher doses of beta-2-adrenomimetics such as salbutamol terbutaline and isoprenaline may be required.

Norepinephrine and MAO inhibitors

Concomitant use of norepinephrine (norepinephrine) or MAO inhibitors may cause hypertension.

Clonidine

Beta-blockers may potentiate arterial hypertension withdrawal after discontinuation of clonidine. Therefore, beta-blockers should be discontinued gradually several days before clonidine is discontinued. Discontinuation of clonidine should also be carried out gradually and only a few days after the end of sotalol use.

Floctafenin

In the case of shock or hypotension caused by floctafenin, beta-blockers cause a decrease in compensatory cardiovascular reactions.

Tricyclic antidepressants barbiturates phenothiazine derivatives narcotic and antihypertensive drugs diuretics and vasodilators

When used concomitantly with sotalol, they can cause a sharp decrease in blood pressure.

Tubocurarine

The use of inhaled anesthetics, including tubocurarin, while taking sotalol increases the risk of myocardial function suppression and hypotension.

Cytochrome P 450 isoenzymes

Sotalol is not expected to interact with drugs that are metabolized by cytochrome P450 isoenzymes.

Amphotericin B gluco-and mineralocorticosteroids (with systemic use) some laxatives

Hypokalemia may occur. 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. Simultaneous food intake (especially milk and dairy products) reduces the absorption of the drug.

The dose of the drug is selected individually depending on the severity of the disease ECG assessment of renal function interaction with other medications taken and the patient’s response to treatment.

The initial dose is 80 mg per day (1/2 tablet Sotalol 80 mg 2 times a day with an interval of approximately 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 by applying 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 480-640 mg divided into 2 or 3 separate doses. However, such doses can only be used 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.

Special patient groups

For patients patients with cardiomyopathy or chronic heart failure (CHF), angina pectoris, arterial hypertension after a previous myocardial infarction are 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 developing accumulation, so they should monitor the value of creatinine clearance (CC) and heart rate (at least 60 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:

Creatinine clearance in ml / min	Dosage interval
≥60	12 h
30-59	24 h
10-29	36-48 h

Creatinine clearance for men is calculated by the formula: ((140-age) x weight (kg)) / (72 x serum creatinine concentration (mg / dl)); for women, the result is multiplied by 085. If the laboratory analyzer gives the result of serum creatinine concentration in units of mmol / l, then the result should be divided by 884 (1 mg / dl = 884 mmol/L).

In case of severe renal impairment (creatinine clearance 10-29 ml / min), it is necessary to regularly monitor the ECG and the concentration of the drug in the blood serum.

Use in patients with impaired liver function

No dose adjustment is required.

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 polymorphic ventricular tachycardia of the “pirouette” type); in severe cases-symptoms of cardiogenic shock asystole, sometimes with a fatal outcome.

Treatment: gastric lavage hemodialysis the use of activated charcoal.

Symptomatic therapy:

Bradycardia: atropine-1-2 times intravenously; glucagon-first as a short intravenous infusion at a dose of 02 mg/kg body weight, then at a dose of 05 mg/kg body weight intravenously infusion for 12 hours.

Grade II-III atrioventricular block: a temporary artificial pacemaker can be installed.

Marked reduction in blood pressure: epinephrine (epinephrine) is effective.

Bronchospasm: aminophylline or beta-2-adrenergic sympathomimetics (inhaled).

Polymorphic ventricular tachycardia of the “pirouette” type: cardioversion placement of a temporary artificial pacemaker (if necessary) with epinephrine (epinephrine) and / or magnesium sulfate.

Special instructions

Monitoring the patient’s condition

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.

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 60 beats/min.

In case of increasing bradycardia (less than 60 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.

Drug withdrawal

After the withdrawal of beta-blockers, patients have increased sensitivity to catecholamines. After abrupt discontinuation of therapy, isolated cases of angina exacerbation, arrhythmia and, in some cases, the development of myocardial infarction have been reported. Therefore, if it is necessary to discontinue Sotalol, the dose should be reduced gradually, especially in patients with coronary heart disease after a myocardial infarction with arterial hypertension. Do not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction.

Careful monitoring of the patient is recommended, especially with coronary heart disease. If possible, the dose should be reduced gradually over one or two weeks. If necessary, it is recommended to prescribe replacement therapy. Abrupt discontinuation of the drug can provoke “latent” coronary insufficiency and the development of arterial hypertension.

Proarrhythmogenic effect

The most dangerous side effect of antiarrhythmic drugs is the aggravation of existing arrhythmias or the provocation of new arrhythmias. Drugs that prolong the QT interval can trigger polymorphic ventricular tachycardia of the “pirouette” type. The occurrence of such arrhythmias is associated with prolongation of the QT interval a decrease in heart rate a decrease in serum potassium and magnesium with a high plasma concentration of sotalol as well as the simultaneous use of other drugs that prolong the QT interval. In women, these complications occur more often.

Polymorphic ventricular tachycardia of the “pirouette” type usually occurs early after the start of therapy or with an increase in the dose and stops spontaneously in most patients. At the same time, titration of the dose reduces the risk of proarrhythmia. Other risk factors for polymorphic ventricular tachycardia of the “pirouette” type include significant prolongation of the QT interval in combination with cardiomegaly or chronic heart failure.

Patients with sustained ventricular tachycardia and chronic heart failure have the highest risk of serious arrhythmias (7%).

Sotalol should be used with extreme caution if the QT interval is longer than 480 ms, and it is necessary to reduce the dose of the drug. If the duration of the QT interval exceeds 550 ms, therapy should be discontinued.

Sotalol can only be used after previous antiarrhythmic therapy if carefully monitored and after at least 2-3 half-lives of the previously prescribed antiarrhythmic agent (see the section “Interaction with other drugs”).

ECG changes

Excessive prolongation of the QT interval (more than 550 ms) may be a sign of drug toxicity.

Electrolyte disturbances

Sotalol should not be used in patients with hypokalemia or hypomagnesemia until the existing disorders are corrected. These conditions can lead to prolongation of the QT interval and increase the likelihood of polymorphic ventricular tachycardia of the “pirouette”type. These electrolyte disturbances 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.

Chronic heart failure (CHF)

Beta-adrenergic blockade can further reduce myocardial contractility and provoke worsening of CHF symptoms. Caution should be exercised when using Sotalol in patients with CHF receiving standard therapy (angiotensin-converting enzyme inhibitors, diuretics, cardiac glycosides, etc. ). In patients with left ventricular dysfunction, a lower initial dose of sotalol should be used at the beginning of therapy and then the dose should be selected according to the clinical situation.

Myocardial infarction

A positive ratio of the expected benefit to the possible risk of using sotalol in patients after a previous myocardial infarction with impaired left ventricular function has not been proven. Careful patient monitoring and dose titration are crucial during initiation and continuation of therapy. Sotalol should not be used in patients with left ventricular ejection fraction

Anaphylactoid reactions

When using beta-blockers in patients with a history of anaphylactic reactions to various allergens, more serious allergic reactions may occur when repeated contact with the antigen. Such patients may not respond to the usual doses of epinephrine (epinephrine) used to treat an allergic reaction. Therefore, the drug Sotalol should be used with extreme caution when indicated in the anamnesis of allergic reactions, as well as against the background of desensitizing therapy.

Diabetes mellitus

Sotalol should be used with caution in patients with diabetes mellitus or with a history of spontaneous hypoglycaemia, since the use of beta-blockers may mask the signs of the onset of acute hypoglycaemia (for example, tachycardia).

Thyrotoxicosis

The use of beta-blockers may hide some of the clinical signs of hyperthyroidism (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase the symptoms of the disease. Patients with suspected thyrotoxicosis should be carefully monitored to avoid the development of thyrotoxicosis, including a thyrotoxic crisis, when the drug is discontinued.

Pheochromocytoma

When using sotalol in patients with pheochromocytoma, alpha-blockers should be used simultaneously.

Psoriasis

Beta-blockers can worsen the course of psoriasis.

Smoking

In smokers, the effectiveness of beta-blockers is lower than in non-smokers.

Impaired renal function

Since sotalol is mainly excreted by the kidneys in patients with impaired renal function, dose adjustment is required.

Laboratory tests

The drug should be discontinued before determining the normetanephrine and vanillylmindalic acid catecholamines in the blood and urine; titers of antinuclear antibodies.

Other things

Patients using contact lenses should take into account that sotalol therapy may reduce the production of tear fluid.

It is recommended to stop therapy if you develop depression caused by taking beta-blockers.

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.

Sotalol should be used with caution in elderly patients.

Influence on the ability to drive vehicles and fur. :

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

At a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Sotalol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets