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 re-enter tachycardia, paroxysmal atrioventricular re-entry tachycardia based on additional conduction pathways and paroxysmal supraventricular tachycardia after surgical intervention, Wolf-Parkinson-White syndrome;maintenance of normal sinus rhythm after arrest of atrial fibrillation or atrial flutter;
• treatment of symptomatic unstable ventricular tachyarrhythmias and symptomatic premature ventricular contractions;
• treatment of arrhythmias due to elevated levels of catecholamines circulating in the blood or hypersensitivity to catecholamines

Active ingredient

Sotalol

Composition

1 tablet contains:

the active ingredient:

sotalol hydrochloride – 160 mg

excipients:

calcium hydrophosphate 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.

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How to take, the dosage

The drug is taken orally 1-2 hours before meals.

At the beginning of treatment, it is recommended to take 160 mg per day in two doses (approximately 12 hours later). This dose can be increased if necessary after appropriate clinical evaluation of the patient to 240 or 320 mg daily. In most patients, therapeutic response is achieved on a total daily dose of 160 to 320 mg divided into two doses. Some patients with life-threatening refractory ventricular arrhythmias may require up to 480 to 640 mg of the drug daily; however, such doses should only be prescribed when the potential benefit outweighs the increased risk of side effects, especially proarrhythmogenic effects.

In patients with cardiomyopathy, chronic heart failure, angina pectoris, arterial hypertension, and conditions after myocardial infarction, it is recommended to start treatment in a hospital setting. The initial dose is 160 mg per day in one or two doses. After a week, the dose can be increased, if necessary, by 80 mg/day (1 tablet of 80 mg or ½ tablet of 160 mg) at weekly intervals. The rate of dose increase depends on the patient’s tolerability of the drug, which is assessed, in particular, by the degree of induced bradycardia and clinical response. Due to relatively long half-life in most patients, sotalol is effective when taken once a day. Dose interval: 160 to 320 mg/day.

Interaction

Antirhythmic agents. Concomitant administration of Sotalol with antiarrhythmic drugs of class IA (disopyramide, quinidine, procainamide) and class III drugs (e.g., amiodarone) may cause prolongation of the QT interval.

Diuretics that reduce potassium content. Use of this type of diuretics may lead to hypokalemia or hypomagnesemia, which increases the likelihood of pirouette-type arrhythmias.

Drugs that increase QT interval duration. Sotalol should be used with extreme caution in combination with other QT interval prolonging agents, such as class I antiarrhythmic agents, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, and some quinolone antibiotics.

Slow calcium channel blockers. Concomitant use of beta-adrenoblockers and “slow” calcium channel blockers may lead to hypotension, bradycardia, conduction disorders and heart failure. The use of beta-adrenoblockers in combination with “slow” calcium channel blockers that suppress myocardial function (e.g., 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. Concomitant use of catecholamine depot depleting agents (e.g., reserpine and guanitidine) together with beta-adrenoblockers leads to an excessive reduction in the tone of the sympathetic nervous system at rest. Patients should be closely monitored because of possible signs of decreased BP and/or marked bradycardia, which may lead to fainting.

Insulin and oral hypoglycemic agents. Hyperglycemia may develop, in which case the dose of hypoglycemic agents should be adjusted. Sotalol may mask the symptoms of hypoglycemia.

Beta2-adrenomimetics. Concomitant use with sotalol may require higher doses of beta2-adrenomimetics such as salbutamol, terbutaline, and isoprenaline.

Digoxin. Sotalol administration has no detectable effect on digoxin serum concentrations. 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-adrenoblockers may potentiate arterial withdrawal hypertension following discontinuation of clonidine; therefore, beta-adrenoblockers should be withdrawn gradually, several days before clonidine is phased out.

Floktafenin. In case of shock or arterial hypotension caused by floktafenin, beta-adrenoblockers cause a decrease in compensatory cardiovascular responses.

Tubocurarine. The use of agents for inhalation anesthesia, including tubocurarine, with sotalol increases the risk of inhibition of myocardial function and development of arterial hypotension.

Amphotericin B and glucocorticosteroids. Potassium levels should be monitored during concomitant use.

Laxatives. Concomitant use with laxatives is not recommended.

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Special Instructions

Treatment with Sotalol Canon is carried out under control of heart rate (HR), BP, ECG. In case of drug withdrawal, the dose should be reduced gradually. Treatment should not be abruptly interrupted because of the risk of severe arrhythmias and myocardial infarction. Withdrawal should be done gradually.

In thyrotoxicosis, Sotalol Canon may mask certain clinical signs of thyrotoxicosis (e.g., tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it may worsen the symptoms of the disease.

When prescribing Sotalol Canon in patients with pheochromocytoma, alpha-adrenoblockers should be prescribed simultaneously.
Caution should be exercised when prescribing beta-adrenoblockers in patients receiving hypoglycemic drugs because hypoglycemia may develop during prolonged pauses in food intake. And its symptoms, such as tachycardia or tremor, will be masked by the action of the drug.

The drug Sotalol Canon should not be used in patients with hypokalemia or hypomagnesemia until the disorders have been corrected. These conditions may increase the degree of QT interval prolongation and increase the probability of pirouette arrhythmia. Electrolyte balance and acid-base status should be monitored particularly carefully in patients with severe or prolonged diarrhea and in patients receiving agents causing decrease of magnesium and/or potassium in the body.

The patient should be instructed on how to calculate heart rate and the need for medical consultation if the heart rate is less than 50 bpm; the effectiveness of beta-adrenoblockers is lower in smokers; patients who wear contact lenses should be aware that tear production may decrease with treatment; the hypersensitivity reactions may become more pronounced and the lack of effect from the usual doses of epinephrine against a history of poor allergy; in elderly patients with increasing bradycardia (less than 50 bpm), hypotension (systolic BP below 100 mmHg), atrioventric hemophilia (BP less than 50 mmHg, atrialoventric hemophilia) and hypotension in the age group. atrioventricular block, bronchospasm, ventricular arrhythmias, severe hepatic and renal dysfunction, the dose should be reduced or treatment should be stopped; it is recommended to stop therapy if depression occurs due to taking beta-adrenoblockers; during treatment, ethanol administration should be excluded; catecholamines, normetanephrine and vanillylmindalic acid, antinuclear antibodies titers should be cancelled before testing in blood and urine.

Impact on driving and operating machinery

Hypnotic headache and fatigue may occur during treatment, therefore caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

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Contraindications

• High sensitivity to sotalol or other drug components and sulfonamide derivatives;
• Decompensated chronic heart failure;
• Cardiogenic shock;
• Atrioventricular block of II and III degree;

Syno-atrial block;

Sinus sinus block syndrome.Atrioventricular block of degree II and III;

• Sinoatrial block;
• Sinus node weakness syndrome;
• Pirouette tachycardia;
• Veep bradycardia (heart rate less than 50 bpm.)
• 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-adrenoblockers;
• Renal insufficiency (creatinine clearance less than 10 ml/min);
• General anesthesia that causes suppression of myocardial function (e.g., cyclopropane or trichloroethylene);
• Arterial hypotension (systolic BP less than 90 mm Hg Hg.);
• Simultaneous use of monoamine oxidase inhibitors (MAOIs);
• Period of lactation;
• Metabolic acidosis;
• Age under 18 years of age (efficacy and safety not established).

Cautions
Cautions should be taken when prescribing the drug in patients who have recently had a myocardial infarction, in diabetes mellitus, psoriasis, as well as in patients with impaired renal function, in atrioventricular block of degree I, in violation of the water-electrolyte balance: hypomagnesemia, hypokalemia, thyrotoxicosis; depression (including anamnesis), pheochromocytoma (when simultaneously taken with alpha-adrenoblockers), aggravated allergic history, old age.

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Side effects

Sotalol is usually well tolerated. Side effects are transient and rarely require interruption or discontinuation of treatment.

Nervous system disorders:
Feeling of fatigue, asthenia, dizziness, headache, sleep disturbances (drowsiness or insomnia), depressed states, paresthesias in the extremities, anxiety, emotional lability, depression, tremor.

Visual disturbances:
Visual disturbances.

Hearing organ disorders and labyrinth disorders:
Hearing disorders.

Heart disorders:
Bradycardia, chest pain, dyspnea, electrocardiogram (ECG) changes, palpitations, arterial hypotension, arrhythmogenic effects, heart failure.

Vascular disorders:
Peripheral edema, syncope.

Gastrointestinal tract disorders:
Nausea, vomiting, dyspepsia, diarrhea, abdominal pain, flatulence. Disturbance of taste.

Skin and subcutaneous tissue disorders:
Urticaria, skin rash.

Musculoskeletal and connective tissue disorders:
Seizures.

Regenerative tract and mammary gland disorders:
Decreased potency.

General disorders:
Fever.

Laboratory and instrumental findings:
Excessive results may be seen in photometric urinalysis for methanephrine (O-methyladrenaline). If pheochromocytoma is suspected, the urine of patients should be examined using high-performance liquid chromatography with solid-phase extraction.

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Overdose

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

Treatment: gastric lavage, prescription of activated charcoal, in atrioventricular conduction disorders administer IV 1-2 mg atropine, in case of low effectiveness a temporary pacemaker is installed; in bronchospasm inhaled or parenterally beta-adrenomimetic; in blood pressure decrease epinephrine is effective; hemodialysis.

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Similarities

Sotagexal, Sotalol, Sotalol Canon