Sotahexal tablets 80 mg No. 20

Side effects

From the nervous system and sensory organs: dizziness, headache, feeling of fatigue, sleep disturbance, confusion, paresthesia, depression. Inflammation of the cornea and conjunctiva (should be taken into account when wearing contact lenses), blurred vision (extremely rare), decreased tear production.

From the cardiovascular system and blood (hematopoiesis, hemostasis): heart failure, bradycardia, AV block, angina pectoris (in rare cases), hypotension.

From the respiratory system: bronchospasm.

From the gastrointestinal tract: nausea, diarrhea, constipation, dry mouth.

Metabolism: hypoglycemia (more often in patients with diabetes mellitus or with strict adherence to a diet).

From the genitourinary system: decreased potency.

From the musculoskeletal system: a feeling of coldness in the extremities, muscle weakness or cramps.

From the skin: skin rash, itching (rare); redness, psoriasiform dermatosis, alopecia.

Contraindications to the use of the drug Sotahexal

Chronic heart failure stage IIB–III; acute myocardial infarction; shock; arterial hypotension; AV block II and III degrees; sinoatrial block; sick sinus syndrome; bradycardia (heart rate less than 50 beats/min); prolongation of the QT ; obliterating vascular diseases; obstructive airway diseases; metabolic acidosis; swelling of the larynx; severe allergic rhinitis; untreated pheochromocytoma; hypokalemia and hypomagnesemia; hypersensitivity to the drug and sulfonamides; a rare hereditary form of galactose intolerance, lactase deficiency or glucose-galactose malabsorption. For patients treated with sotalol (except for intensive drug treatment), intravenous administration of calcium antagonists such as verapamil or diltiazem or other antiarrhythmic drugs (such as disopyramide) is contraindicated.

Interaction

When used together with antiarrhythmics IA (especially quinidine type) and class III, the risk of developing ventricular arrhythmias and prolongation of the QT interval increases; with tricyclic antidepressants, barbiturates, phenothiazines, calcium antagonists and narcotic, antihypertensive, diuretic and vasodilating agents - dangerous hypotension and weakness of the sinus node; with norepinephrine or MAO blockers - hypertension; with reserpine, clonidine, alpha-methyldopa, guanfacine and cardiac glycosides - bradycardia or AV block; with potassium-removing diuretics - arrhythmia caused by hypokalemia. Enhances the hypoglycemic effect of insulin and oral hypoglycemic agents.

Indications for use of the drug Sotahexal

Supraventricular tachyarrhythmias accompanied by clinical symptoms (including atrioventricular, nodal, paroxysmal tachycardias in WPW syndrome or paroxysmal atrial fibrillation arrhythmias); maintaining normal sinus rhythm after stopping atrial fibrillation or flutter; severe ventricular heart rhythm disturbances, which are accompanied by severe clinical symptoms (tachyarrhythmias) and their prevention with proven effectiveness; arrhythmias caused by excess circulation of catecholamines or increased sensitivity to catecholamines.

Overdose

Symptoms: arterial hypotension, bradycardia, loss of consciousness, generalized convulsive seizures, ventricular tachycardia; in severe cases - symptoms of cardiogenic shock, asystole.

Treatment: administration of atropine - 1-2 times IV bolus, glucagon - first - short-term IV infusion at a dose of 0.2 mg/kg body weight, then at a dose of 0.5 mg/kg body weight for 12 hours dopamine, dobutamine, isoprenaline or adrenaline - depending on body weight and therapeutic effect.

Eliminated by hemodialysis.

Use of the drug Sotahexal

Dose adjustment of SotaHexal in cases of ventricular arrhythmia should be carried out under the constant supervision of a cardiologist; it can be carried out with appropriate equipment in the cardiac emergency room and continuous monitoring. During treatment, screening tests should be carried out at regular intervals (for example, standard or long-term ECG). If individual ECG parameters are changed, therapy must be carefully analyzed, for example, in cases of QRS QT interval by more than 25% , a 50% increase in PQ QT by more than 500 ms , an increase in the number of attacks or severity of arrhythmia. Treatment of tachyarrhythmias The recommended starting dose of SotaHexal is 40 mg 2 times a day. Subsequently, the drug is prescribed in a daily dose of 160–320 mg, divided into 3 doses. If necessary, the dose of the drug can be increased to 160 mg 3 times a day. Severe ventricular heart rhythm disturbances with severe tachyarrhythmia The initial dose of SotaHexal is 80 mg 2 times a day. If necessary, the daily dose can be increased to 80 mg 3 times a day or up to 160 mg 2 times a day. In case of insufficient effectiveness in the treatment of arrhythmia that threatens the patient's life, the daily dose of SotaHexal can be increased to 480 mg, divided into 2 doses. In these cases, the dose should be increased only if the potential benefit outweighs the potential risk of severe adverse reactions (especially proarrhythmic effects). Atrial fibrillation The initial dose of SotaHexal is 80 mg 2 times a day. If necessary, the daily dose can be increased to 80 mg 3 times a day. In cases of paroxysmal atrial fibrillation, this dose should not be exceeded. If in patients with chronic atrial fibrillation the effectiveness of treatment is insufficient, the dose of sotalol hydrochloride can be increased to a maximum of 160 mg 2 times a day. The dose can only be increased at minimum two to three day intervals. Recommended doses for renal failure In severe renal failure, the use of sotalol hydrochloride is recommended only with regular monitoring of the ECG and the concentration of the drug in the blood serum. If creatinine clearance decreases to 10–30 mol/min (serum creatinine 2–5 mg/dL), a dose reduction of 50% is recommended. If the value of this indicator is less than 190 ml/min (serum creatinine ≤5 mg/dl), then a dose reduction by 1/4 is recommended. SotaHexal tablets should be swallowed without chewing, with a sufficient amount of liquid (for example, a glass of water) before meals. When adjusting the dose in patients after myocardial infarction or with severe cardiac pathology, particularly careful monitoring (for example, using monitoring) should be established. During treatment, appropriate testing should be carried out at regular intervals. In patients with coronary artery disease and/or arrhythmia, as well as after prolonged use of the drug, treatment should be discontinued gradually, since abrupt withdrawal may lead to a worsening of the clinical picture of the disease. The duration of treatment is determined depending on the clinical course of the disease and the patient’s condition.

Precautionary measures

Constant monitoring of heart rate, blood pressure, and ECG is required. Prescribed with caution in diabetes mellitus, pheochromocytoma, renal failure, in old age, psoriasis (including a history, including family), allergic reactions, as well as against the background of desensitizing therapy, diet, in the II–III trimester of pregnancy ( only for strict indications, stop taking 48–72 hours before birth). Alcohol intake should be avoided. Simultaneous intravenous administration of calcium channel blockers (verapamil, diltiazem) should be avoided. Use with caution while working for vehicle drivers and people whose profession involves increased concentration.

If the drug is discontinued, the dose should be reduced gradually.

Pharmacological properties of the drug Sotahexal

SotaHexal is a non-selective β-adrenergic receptor blocker that acts on β1- and β2-adrenergic receptors. It has a pronounced antiarrhythmic effect, the mechanism of which is to increase the duration of the action potential and the absolute refractory period in all parts of the conduction system of the heart (Class III antiarrhythmic drugs). Reduces heart rate and myocardial contractility, slows AV conduction, and reduces the absolute refractory period. By blocking β2-adrenergic receptors, it increases the tone of smooth muscles of the bronchi and blood vessels. After oral administration, 75–90% of sotalol hydrochloride is absorbed from the gastrointestinal tract. Due to the lack of effect of the first phase, absolute bioavailability is 75–90%. The time to reach maximum concentration in blood plasma is 2–3 hours. The volume of distribution is 1.6–2.4 l/kg. Sotalol does not bind to plasma proteins and is not metabolized in the body. Up to 90% of the dose taken is excreted unchanged by the kidneys, the rest is excreted in feces. Renal clearance is 120 ml/min and corresponds to the total clearance of the body. The half-life is 10–20 hours. If renal function is impaired, the elimination of sotalol may increase to 42 hours, which requires a reduction in the dose of the drug.

Sotahexal tablets 80 mg No. 20

Compound

Active substance: sotalol hydrochloride 80 mg.
Excipients: lactose monohydrate, corn starch, hyprolose, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate.

Pharmacokinetics

When taken orally, sotalol is absorbed from the gastrointestinal tract, Cmax in plasma is reached after 2-3 hours. Vd is 2 l/kg. T1/2 - about 15 hours. Excreted mainly by the kidneys.

Indications for use

Ventricular arrhythmia:

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

Supraventricular arrhythmia:

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

Contraindications

• Hypersensitivity to sotalol, to other components of the drug and sulfonamides;
• evidence of sick sinus syndrome, including sinoauricular block, unless there is a functioning artificial driver
• heart rate;
• atrioventricular block II and III degrees;
• congenital or acquired long QT interval syndrome or the use of drugs that can prolong the QT interval (see section "Interaction");
• bidirectional fusiform ventricular tachycardia or the use of drugs associated with this disorder (see section "Interaction");
• symptomatic sinus bradycardia (heart rate <45 - 50 beats/min);
• uncontrolled congestive heart failure (CHF), including right ventricular CHF due to pulmonary hypertension;
• cardiogenic shock;
• anesthesia causing suppression of myocardial function;
• arterial hypotension), except in cases caused by arrhythmia;
• Raynaud's phenomenon and severe peripheral circulatory disorders;
• history of bronchial asthma or chronic obstructive pulmonary disease (COPD);
• metabolic acidosis;
• renal failure (creatinine clearance <10 ml/min);
• pheochromocytoma without simultaneous use of alpha-blockers;
• lactation period;
• age under 18 years (efficacy and safety have not been established).

Carefully:

Caution should be exercised when prescribing Sotahexal to patients who have recently suffered a myocardial infarction, with diabetes mellitus, psoriasis, renal dysfunction, first degree atrioventricular block, with water-electrolyte imbalance: hypomagnesemia, hypokalemia; with thyrotoxicosis, depression (including a history), with prolongation of the QT interval, in old age.

Use with extreme caution when there is a history of allergic reactions, as well as against the background of desensitizing therapy, because sotalol suppresses sensitivity to allergens.

Directions for use and doses

The drug is taken orally 1-2 hours before meals, without chewing, with a sufficient amount of liquid.

Simultaneous ingestion of food (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 and the patient’s response to treatment. The initial dose is 80 mg (1 tablet of Sotahexal) per day. If the therapeutic effect is insufficient, 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 at a total daily dose of 160-320 mg, divided into 2 doses.

For some patients with life-threatening refractory ventricular arrhythmia, it is possible to increase the dose to a maximum of 6-8 tablets of Sotahexal (480-640 mg sotalol), divided into 2 or 3 separate doses. However, such doses should only be used in cases where the potential benefit outweighs the risk of side effects, especially proarrhythmogenic effects.

Patients with impaired renal function are at risk of developing cumulation, so they need to monitor creatinine clearance and heart rate (not lower than 50 beats per minute). Since sotalol is excreted primarily by the kidneys and its half-life increases in the presence of renal impairment, the dose of the drug should be reduced according to the following recommendations:

Creatinine clearance for men is calculated using the formula: ((140-age) x weight (kg))/(72 x serum creatinine concentration (mg/dL)); for women, the result obtained is multiplied by 0.85.

If a laboratory analyzer gives a result of serum creatinine concentration in units of µmol/L, then it is necessary to divide the result by 88.4 (1 mg/dL = 88.4 µmol/L).

In case of severe renal dysfunction, it is necessary to regularly monitor the ECG and the concentration of the drug in the blood serum. The duration of therapy is determined by the attending physician.

If you forget to take a pill on time, next time you should not take an additional amount of the drug; you should only take the prescribed dose of Sotahexal.

Storage conditions

At a temperature not higher than 25 °C. Keep out of the reach of children.

Best before date

5 years. Do not use after the expiration date.

special instructions

Discontinuation of the drug
Increased sensitivity to catecholamines is observed in patients after discontinuation of beta-blockers. After abrupt cessation of therapy, isolated cases of exacerbation of angina pectoris, the occurrence of arrhythmia, and, in some cases, the development of myocardial infarction have been reported. Therefore, careful monitoring of the patient is recommended, especially with coronary heart disease, if it is necessary to abruptly discontinue long-term therapy with Sotahexal. If possible, the dose should be reduced gradually over one or two weeks. If necessary, it is recommended to initiate replacement therapy. Abrupt cessation of drug use can provoke “hidden” coronary insufficiency, as well as the development of arterial hypertension.

Proarrhythmia

The most dangerous side effect of antiarrhythmic drugs is the exacerbation of existing arrhythmias or the provocation of new arrhythmias. Drugs that prolong the QT interval can cause torsade de pointes (TdP), or torsade de pointes (TdP).

The occurrence of such arrhythmias is associated with a prolongation of the QT interval, a decrease in heart rate, a decrease in serum potassium and magnesium, with high plasma concentrations of sotalol, as well as the simultaneous use of other drugs that prolong the QT interval. In women, these complications occur more often. Torsade de pointes tachycardia usually occurs early after the start of therapy or when the dose is increased, and stops spontaneously in most patients. At the same time, dose titration reduces the risk of proarrhythmia. Rarely, torsade de pointes tachycardia can progress to ventricular fibrillation.

Other risk factors for torsade de pointes include significant prolongation of the QT interval with cardiomegaly or congestive heart failure.

Patients with sustained ventricular tachycardia and congestive heart failure have the highest risk of serious proarrhythmias (7%). The drug Sotahexal should be used with extreme caution when the QT interval lasts more than 480 msec, or the dose of the drug must be reduced; therapy should be discontinued when the QT interval exceeds 550 msec.

Electrolyte disorders Sotahexal should not be used in patients with uncorrected hypokalemia or hypomagnesemia, because Possible prolongation of the QT interval, as well as an increase in the potential for tachycardia of the “pirouette” type. Particular attention should be paid to the water-electrolyte ratio and acid-base balance in patients with prolonged diarrhea or patients receiving magnesium and/or drugs that remove potassium from the body (diuretics).

Congestive heart failure

Beta-adrenergic receptor blockade may further reduce myocardial contractility and cause progression of heart failure symptoms.

Therapy with Sotahexal should be started with caution and with a low dose in patients with impaired contractility of the left ventricular myocardium, controlled by therapy with ACE inhibitors, diuretics, cardiac glycosides, etc. Myocardial infarction Positive benefit/risk ratio of the use of sotalol in patients after a myocardial infarction with impaired left ventricular function has not been proven. Careful patient monitoring and dose titration are critical during initiation and continuation of therapy. Sotalol should not be used in patients with a left ventricular ejection fraction <40% without serious ventricular arrhythmias.

ECG changes

Excessive prolongation of the QT interval, greater than 550 msec, may be a sign of drug toxicity. Anaphactoid reactions In patients using beta-blockers with a history of anaphylactic reactions to various allergens, more serious allergic reactions may occur upon repeated contact with the antigen. Such patients may not respond to the usual doses of epinephrine used to treat an allergic reaction.

Diabetes

Sotahexal should be used with caution in patients with diabetes mellitus or with a history of episodes of spontaneous hypoglycemia, since the use of beta-blockers may mask signs of the onset of acute hypoglycemia, such as tachycardia.

Thyrotoxicosis

The use of beta blockers may mask some clinical signs of hyperthyroidism (eg, tachycardia). Patients with suspected thyrotoxicosis should be carefully monitored to avoid the development of thyrotoxicosis, including thyroid storm, when the drug is discontinued.

Impaired renal function Since sotalol is primarily eliminated by the kidneys, dosage adjustment is required in patients with impaired renal function.

Psoriasis

The use of beta blockers may worsen the symptoms of psoriasis.

Description

Beta blocker.

Use in children

Contraindicated under 18 years of age (efficacy and safety have not been established).

Pharmacodynamics

Sotalol is a non-selective β-adrenergic receptor blocker that acts on both β1 and β2 receptors and has no intrinsic sympathomimetic activity (SMA) or membrane stabilizing activity (MCA). Like other beta-blockers, sotalol suppresses renin secretion, and this effect is pronounced both at rest and during exercise. The β-adrenergic blocking effect of the drug causes a decrease in heart rate (negative chronotropic effect) and a limited decrease in the force of heart contractions (negative inotropic effect).

These changes in cardiac function reduce myocardial oxygen demand and the amount of workload on the heart.

The antiarrhythmic properties of sotalol are associated both with the ability to block beta-adrenergic receptors and with the ability to prolong the myocardial action potential. The main effect of sotalol is to increase the duration of effective refractory periods in the atrial, ventricular and accessory impulse pathways.

Side effects

According to the World Health Organization (WHO), adverse reactions are classified according to their frequency as follows: very common (>1/10), common (>1/100, <1/10), uncommon (>1/1000, < 1/100), rare (>1/10000, <1/1000) and very rare (<1/10000);
frequency unknown - based on available data, it was not possible to determine the frequency of occurrence. Mental disorders: often: anxiety, sleep disturbances (drowsiness or insomnia), fatigue, mood changes, depression, depression.

From the nervous system: often: headache, dizziness, light hallucinations, asthenia, paresthesia in the extremities, syncope; frequency unknown: increased fatigue, tremor.

From the senses: often: visual impairment, hearing impairment, changes in taste sensations; very rarely: decreased lacrimation; frequency unknown: inflammation of the cornea and conjunctiva (should be taken into account when wearing contact lenses).

From the cardiovascular system: often: bradycardia, palpitations, cardiac arrhythmias, shortness of breath, chest pain, AV block, increased symptoms of heart failure, proarrhythmia, arithmia, decreased blood pressure, edema; frequency unknown: fainting, increased attacks of angina, painful coldness of the extremities, Raynaud's disease, short-term exacerbation of intermittent claudication.

From the respiratory side: urticaria.

Other: cold extremities, muscle weakness, cramps, fever.

System, chest organs and mediastinum: uncommon: bronchospasm (especially in case of impaired pulmonary ventilation).

From the digestive system: often: dyspepsia (nausea, vomiting), diarrhea, constipation, dry oral mucosa, abdominal pain, flatulence.

From the skin and subcutaneous tissues: frequency unknown: skin rash, itching, redness, psoriasiform dermatosis, alopecia, urticaria.

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

From the genitourinary system: often: decreased 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), inflated results may be observed in a photometic analysis of urine for metanephrine (O-methyladrenaline).

Use during pregnancy and breastfeeding

The use of the drug Sotahexal during pregnancy, especially in the first trimester, is possible only for health reasons and with a careful balance of all risk factors.
In animal studies, sotatol did not cause teratogenic or other damaging effects on the fetus. There have been no controlled studies of the use of sotalol in pregnant women. Sotalol penetrates the hematoplacental barrier. Beta-blockers reduce placental blood flow, which can cause intrauterine fetal death, premature birth, and the birth of an immature fetus. In the case of therapy during pregnancy, the use of the drug should be discontinued 48-72 hours before the expected due date due to the possibility of developing hypoglycemia, bradycardia, arterial hypotension, hypokalemia and respiratory depression in newborns. Sotalol passes into breast milk and reaches effective concentrations there. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Interaction

When taking “slow” calcium channel blockers such as verapamil and diltiazem simultaneously, a decrease in blood pressure may occur as a result of worsening contractility.

Intravenous administration of these drugs should be avoided while using sotalol (except in emergency situations).

The combined use of class IA antiarrhythmic drugs (especially the quiniline type: disopyramide, quinidine, procainamide) or class III (for example, amiodarone) can cause a pronounced prolongation of the QT interval. Drugs that prolong the duration of the OT interval: drugs should be used with caution. Those that prolong the QT interval, such as class I antiarrhythmics, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, as well as some quinolone antibiotics.

When taking nifedipine and other 1,4-dihydropyridine derivatives simultaneously, a decrease in blood pressure is possible.

The simultaneous administration of norepinephrine or MAO inhibitors, as well as abrupt withdrawal of clonidine, can cause arterial hypertension. In this case, withdrawal of clonidine should be carried out gradually and only a few days after stopping Sotahexal.

Tricyclic antidepressants, barbiturates, phenothiazines. narcotic and antihypertensive drugs, diuretics and vasodilators can cause a sharp decrease in blood pressure.

The use of inhalation anesthesia, including tubocurarine, while taking Sotahexal increases the risk of suppression of myocardial function and the development of arterial hypotension.

With simultaneous use of Sotahexal with reserpine, clonidine. alpha-methyldopa. guanfacine and cardiac glycosides may develop severe bradycardia and slow down the conduction of excitation in the heart.

Beta blockers may potentiate withdrawal hypertension following discontinuation of clonidine; therefore, beta blockers should be discontinued gradually, several days before tapering off clonidine.

Prescribing insulin or other oral hypoglycemic agents, especially during physical activity, can lead to increased hypoglycemia and the manifestation of its symptoms (excessive sweating, rapid pulse, tremor). For diabetes mellitus, dose adjustment of insulin and/or hypoglycemic drugs is necessary.

Potassium-volatile diuretics G, for example, furosemide. hydrochlorothiazide) can provoke arrhythmia caused by hypokalemia. Beta2 receptor stimulants. When used concomitantly with Sotahexal, higher doses of beta-agonists such as salbutamol, terbutaline and isoprenaline may be required.

Overdose

Symptoms: decreased blood pressure, bradycardia, bronchospasm, hypoglycemia, loss of consciousness, generalized convulsive seizures, prolongation of the QT interval, ventricular tachycardia (including the “feasting” type);
in severe cases - symptoms of cardiogenic shock, asystole, sometimes with death. Treatment: gastric lavage, hemodialysis, use of activated carbon.

Symptomatic therapy. Bradycardia: atropine - 1-2 times intravenously; glucagon - first in the form of a short intravenous infusion at a dose of 0.2 mg/kg body weight, then at a dose of 0.5 mg/kg body weight intravenously infused over 12 hours. Atrioventricular block 2 - 3 degrees: it is possible to install a temporary artificial pacemaker .

Marked decrease in blood pressure: epinephrine is effective. Bronchospasm: aminophylline or beta-2-adrenergic receptor sympathomimetics (inhalation). Torsade de pointes tachycardia: cardioversion, temporary pacemaker (if necessary), epinephrine and/or magnesium sulfate.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, you should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.