Sotalol Canon, tablets 160 mg 20 pcs

Pharmacotherapeutic group:

Nonselective beta-adrenoblocker

ATC code: C07AA07

Pharmacological properties

Pharmacodynamics

Sotalol is a non-selective beta-adrenergic receptor blocker that acts on both beta1- and beta2-receptors and has no sympathomimetic activity (SMA) or membrane-stabilizing activity (MSA) of its own. Like other beta-adrenoblockers, sotalol suppresses renin secretion, and this effect is pronounced both at rest and during exercise.

The beta-adrenoblocking effect of the drug causes a decrease in heart rate (negative chronotropic effect) and a limited decrease in heart force (negative inotropic effect). These changes in cardiac function reduce myocardial oxygen demand and cardiac workload.

The antiarrhythmic properties of sotalol are associated with both the ability to block beta-adrenergic receptors and the ability to prolong myocardial action potential. The main effect of sotalol is to increase the duration of effective refractory periods in atrial, ventricular and accessory pulse conduction pathways. On electrocardiograms taken in standard leads, properties corresponding to Class II and III antiarrhythmic agents may be reflected in the form of prolongation of PR, QT and QTc intervals (QT with correction for heart rate) with no appreciable changes in QRS complex duration.

Pharmacodynamics

The bioavailability with oral administration is almost complete (more than 90%). The maximum plasma concentration is reached 2.5-4 hours after oral administration, and the equilibrium concentration is within 2-3 days. Absorption of the drug is reduced by approximately 20% when eating compared to an empty stomach. In the dose range of 40 to 640 mg/day, the plasma concentration of Sotalol is proportional to the dose taken.

Distribution occurs in the plasma and in peripheral organs and tissues, with a half-life of 10-20 hours. Sotalol does not bind with blood plasma proteins and is not metabolized. Pharmacokinetics of d- and 1-enantiomers of sotalol is almost the same. Sotalol poorly penetrates the blood-brain barrier, and its concentration in cerebrospinal fluid is only 10% of that in blood plasma.

The main route of excretion 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 age, although impaired renal function in elderly patients reduces the excretion rate, which leads to increased accumulation of the drug in the body.

Indications

prevention of paroxysmal atrial tachycardia, paroxysmal atrial fibrillation, paroxysmal atrioventricular reentrant tachycardia of the “re-enter” type, paroxysmal atrioventricular reentrant tachycardia based on additional conduction pathways and paroxysmal supraventricular tachycardia after surgery, Wolff-Parkinson-White syndrome;
maintaining normal sinus rhythm after relief of atrial fibrillation or atrial flutter;
treatment of symptomatic unstable ventricular tachyarrhythmias and symptomatic premature ventricular contractions;
treatment of arrhythmias caused by increased levels of catecholamines circulating in the blood or increased sensitivity to catecholamines

Pharmacological effect

Pharmacotherapeutic group:

non-selective beta blocker

ATX code: C07AA07

Pharmacological properties

Pharmacodynamics

Sotalol is a non-selective beta-adrenergic receptor blocker that acts on both beta1 and beta2 receptors and has no intrinsic sympathomimetic activity (SMA) or membrane stabilizing activity (MSA). Like other beta-blockers, sotalol suppresses renin secretion, and this effect is pronounced both at rest and during exercise.

The beta-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 cardiac workload.

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. On an electrocardiogram taken in standard leads, properties corresponding to class II and III antiarrhythmic drugs may be reflected in the form of prolongation of the PR, QT and QTc intervals (QT corrected for heart rate) in the absence of noticeable changes in the duration of the QRS complex.

Pharmacodynamics

Bioavailability after oral administration is almost complete (more than 90%). The maximum concentration in blood plasma is achieved 2.5-4 hours after oral administration, and the equilibrium concentration is within 2-3 days. Absorption of the drug is reduced by approximately 20% when taken with food compared to when taken on an empty stomach. In the dose range from 40 to 640 mg/day, the concentration of sotalol in the blood plasma is proportional to the dose taken.

Distribution occurs in the 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 1-enantiomers of sotalol are almost the same. Sotalol penetrates the blood-brain barrier poorly, 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 lower doses of the drug. With age, pharmacokinetics change slightly, although impaired renal function in elderly patients reduces the rate of excretion, which leads to increased accumulation of the drug in the body.

Special instructions

Treatment with Sotalol Canon is carried out under the control of heart rate (HR), blood pressure, and ECG. If the drug is discontinued, the dose should be reduced gradually. Treatment should not be abruptly interrupted due to the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually.

In case of thyrotoxicosis, the drug Sotalol Canon can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase the symptoms of the disease.

When prescribing Sotalol Canon to patients with pheochromocytoma, alpha-blockers should be prescribed simultaneously.
When prescribing beta-blockers to patients receiving hypoglycemic drugs, caution should be exercised, since hypoglycemia may develop during prolonged breaks in food intake. Moreover, its symptoms such as tachycardia or tremor will be masked due to the action of the drug.

The drug Sotalol Canon should not be used in patients with hypokalemia or hypomagnesemia until the existing disorders are corrected. These conditions may increase the degree of QT prolongation and increase the likelihood of torsade de pointes (TdP). Electrolyte balance and acid-base status should be especially carefully monitored in patients with severe or prolonged diarrhea and in patients receiving drugs that cause a decrease in magnesium and/or potassium in the body.

The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats per minute; In smokers, the effectiveness of beta-blockers is lower; patients using contact lenses should take into account that during treatment the production of tear fluid may decrease; it is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from usual doses of epinephrine against the background of a burdened allergic history; in case of increasing bradycardia (less than 50 beats/min), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction in elderly patients, it is necessary to reduce the dose or stop treatment; it is recommended to discontinue therapy if depression caused by taking beta-blockers develops; Avoid ethanol intake during treatment; should be discontinued before testing blood and urine levels of catecholamines, normetanephrine and vanillyl mandelic acid, and antinuclear antibody titers.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, headaches and a feeling of fatigue may occur, so care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Sotalol

Composition

1 tablet contains:

active substance:

sotalol hydrochloride – 160 mg

excipients:

calcium hydrogen phosphate dihydrate – 118 mg,

colloidal silicon dioxide (Aerosil) – 1 mg,

croscarmellose sodium – 12 mg,

mannitol – 56.8 mg,

povidone – 8.6 mg,

magnesium stearate – 3.6 mg.

Contraindications

Hypersensitivity to sotalol or other components of the drug and sulfonamide derivatives;
Decompensated chronic heart failure;
Cardiogenic shock;
Atrioventricular block II and III degrees;
Sinoatrial block;
Sick sinus syndrome;
Tachycardia of the “pirouette” type;
Severe bradycardia (heart rate less than 50 beats/min.)
Congenital or acquired syndromes characterized by prolongation of the QT interval;
Bronchial asthma or chronic obstructive pulmonary disease (COPD);
Pheochromocytoma without simultaneous administration of alpha-blockers;
Renal failure (creatinine clearance less than 10 ml/min);
General anesthesia that causes suppression of myocardial function (for example, cyclopropane or trichlorethylene);
Arterial hypotension (systolic blood pressure less than 90 mm Hg);
Concomitant use of monoamine oxidase inhibitors (MAO);
Lactation period;
Severe peripheral circulatory disorders, including Raynaud’s syndrome;
Metabolic acidosis;
Age up to 18 years (efficacy and safety have not been established).

With caution
Caution should be exercised when prescribing the drug to patients who have recently suffered a myocardial infarction, with diabetes mellitus, psoriasis, as well as patients with impaired renal function, with atrioventricular block of the first degree, with water-electrolyte imbalance: hypomagnesemia, hypokalemia, thyrotoxicosis; depression (including a history), pheochromocytoma (when taken simultaneously with alpha-blockers), a burdened allergic history, old age.

Side Effects

Sotalol is usually well tolerated. Side effects are transient and in rare cases require interruption or cessation of treatment.

Nervous system disorders:
Feeling of fatigue, asthenia, dizziness, headache, sleep disturbance (drowsiness or insomnia), depression, paresthesia in the limbs, anxiety, emotional lability, depression, tremor.

Visual disorders:
Visual impairment.

Hearing and labyrinthine disorders:
Hearing impairment.

Cardiac disorders:
Bradycardia, chest pain, shortness of breath, changes in the electrocardiogram (ECG), palpitations, arterial hypotension, arrhythmogenic effect, heart failure.

Vascular disorders:
Peripheral edema, fainting.

Gastrointestinal disorders:
Nausea, vomiting, dyspepsia, diarrhea, abdominal pain, flatulence. Impaired sense of taste.

Skin and subcutaneous tissue disorders:
Hives, skin rash.

Musculoskeletal and connective tissue disorders:
Cramps.

Disorders of the genital organs and breast:
Decreased potency.

General disorders:
Fever.

Laboratory and instrumental data:
Inflated results may be observed in photometric urine analysis for metanephrine (O-methyladrenaline). If pheochromocytoma is suspected, the urine of patients should be examined using high-performance liquid chromatography with solid-phase extraction.

Interaction

Antiarrhythmic drugs. Concomitant administration of sotalol with class IA antiarrhythmic drugs (disopyramide, quinidine, procainamide) and class III drugs (for example, amiodarone) may cause prolongation of the QT interval.

Diuretics that reduce potassium levels. The use of diuretics of this type may lead to hypokalemia or hypomagnesemia, which increases the likelihood of torsade de pointes (TdP).

Drugs that prolong the QT interval. Sotalol should be used with extreme caution in combination with other drugs that prolong the QT interval, such as class I antiarrhythmics, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, and some quinolone antibiotics.

Blockers of “slow” calcium channels. The simultaneous use of beta-blockers and slow calcium channel blockers can lead to arterial hypotension, bradycardia, conduction disturbances and heart failure. The use of beta-blockers in combination with slow calcium channel blockers that suppress myocardial function (for example, verapamil and diltiazem) should be avoided due to the additive effect of these drugs on atrioventricular conduction and ventricular function.

Drugs that lower catecholamine levels. The simultaneous use of catecholamine depleting agents (for example, reserpine and guanitidine) with beta-blockers leads to an excessive decrease in the tone of the sympathetic nervous system at rest. Patients should be carefully monitored due to possible signs of decreased blood pressure and/or severe bradycardia, which can lead to syncope.

Insulin and hypoglycemic agents for oral administration. Hyperglycemia may develop, in which case it is necessary to adjust the dose of hypoglycemic agents. Sotalol may mask the symptoms of hypoglycemia.

Beta2-adrenergic agonists. When used concomitantly with sotalol, higher doses of beta2-agonists such as salbutamol, terbutaline and isoprenaline may be required.

Digoxin. Taking sotalol does not cause a noticeable effect on the concentration of digoxin in the blood serum. Arrhythmogenic effects were more frequent in patients receiving sotalol concomitantly with digoxin; however, this may be due to chronic heart failure, which is a risk factor for arrhythmogenic effects in patients receiving digoxin.

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

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

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

Amphotericin B and glucocorticosteroids. If used concomitantly, monitor potassium levels.

Laxatives. Concomitant use with laxatives is not recommended.

Overdose

Symptoms: bradycardia, chronic heart failure, exacerbation of chronic heart failure, marked decrease in blood pressure, bronchospasm, hypoglycemia.

Treatment: gastric lavage, administration of activated charcoal; in case of atrioventricular conduction disturbances, 1-2 mg of atropine is administered intravenously; if efficiency is low, a temporary pacemaker is installed; for bronchospasm, inhaled or parenteral beta-agonist; Epinephrine is effective in lowering blood pressure; hemodialysis.

Storage conditions

The drug should be stored out of the reach of children, in a dry, dark place at a temperature not exceeding 25°C.

Shelf life

2 years.

Manufacturer

Kanonpharma production CJSC, Russia