Sotalol Canon pills 160mg, 20pcs

Composition

1 tablet contains:

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

Pharmacological action

Pharmacotherapy group:

non-selective beta-adrenoblocker

ATX code: C 07 AA 07

Pharmacological properties

Pharmacodynamics

Sotalol is a non-selective beta-adrenergic receptor blocker that acts on both beta-1 and beta-2 receptors and does not have its own sympathomimetic activity (SMA) and 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 strength of heart contractions (negative inotropic effect). These changes in heart function reduce the oxygen demand of the myocardium and the 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 impulse conduction. On an electrocardiogram taken in standard leads, properties corresponding to class II and III antiarrhythmic agents can be reflected in the form of prolongation of the PR, QT and QTc intervals (QT with correction for heart rate) in the absence of noticeable changes in the duration of the QRS complex.

Oral bioavailability is almost complete (more than 90%). The maximum concentration in blood plasma is reached 2.5-4 hours after oral use, and the equilibrium concentration is within 2-3 days. The absorption of the drug decreases by approximately 20% with food compared to fasting. 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 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 identical. Sotalol does not penetrate well through the blood-brain barrier, and its concentration in the cerebrospinal fluid is only 10% of the concentration in 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 is excreted through the intestines. Patients with impaired renal function should be prescribed smaller doses of the drug. With age, the 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.

Indications

• prevention of paroxysmal atrial tachycardia, paroxysmal atrial fibrillation, recurrent paroxysmal atrioventricular tachycardia type “re-enter” recurrent paroxysmal atrioventricular tachycardia on the basis of additional ways of carrying out and paroxysmal supraventricular tachycardia after surgical intervention, the syndrome Wolff-Parkinson-white;
• the maintenance of normal sinus rhythm after the relief of atrial fibrillation or atrial flutter;
• treatment is symptomatic unstable ventricular tachyarrhythmias and symptomatic premature ventricular contractions;
• the treatment of arrhythmias due to high content of catecholamines circulating in the blood or increased sensitivity to catecholamines

Contraindications

• Hypersensitivity to sotalol or other components of the drug and sulfonamide derivatives;
• Decompensated chronic heart failure;
• Cardiogenic shock;
• Grade II and III atrioventricular block;
• Sinoatrial blockade;
• Sinus node weakness 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 use of alpha-blockers;
• Renal insufficiency (creatinine clearance less than 10 ml / min);
• General anesthesia that causes suppression of myocardial function (for example, cyclopropane or trichloroethylene);
• Arterial hypotension (systolic blood pressure less than 90 mm Hg);
• Simultaneous use of monoamine oxidase (MAO) inhibitors;
• Lactation period;
• Severe peripheral circulatory disorders, including Raynaud’s syndrome;
• Metabolic acidosis;
• Age up to 18 years (efficacy and safety have not been established).

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

Side effects

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

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

Visual disturbances: Visual impairment.

Hearing disorders and labyrinth disorders: Hearing disorders.

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

Vascular disorders: Peripheral edema, syncope.

Disorders of the gastrointestinal tract: Nausea, vomiting, dyspepsia, diarrhea, abdominal pain, flatulence. Violation of taste sensations.

Skin and subcutaneous tissue disorders: Urticaria, skin rash.

Musculoskeletal and connective tissue disorders: Convulsions.

Genital and breast disorders: Reduced potency.

Common disorders: Fever.

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

Interaction

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

Diuretics that reduce the potassium content. The use of diuretics of this type can lead to hypokalemia or hypomagnesemia, which increases the likelihood of arrhythmia of the “pirouette”type.

Medications that increase the duration of 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, as well as some quinolone antibiotics.

Slow calcium channel blockers. Concomitant use of beta-blockers and slow calcium channel blockers can lead to hypotension, bradycardia, conduction disturbances, and heart failure. The use of beta-blockers in combination with slow calcium channel blockers that inhibit myocardial function (for example, verapamil and diltiazem) should be avoided, due to the additive effect of these agents on atrioventricular conduction and ventricular function.

Drugs that lower the level of catecholamines. Concomitant use of agents that deplete the catecholamine depot (for example, reserpine and guanitidine), together with beta-blockers, leads to an excessive decrease in the tone of the sympathetic nervous system at rest. Patients should be carefully monitored for possible signs of lowering blood pressure and / or severe bradycardia, which may lead to syncope.

Insulin and hypoglycemic agents for oral use. Hyperglycemia may develop, in which case it is necessary to adjust the dose 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.

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 after discontinuation of clonidine; therefore, beta-blockers should be discontinued gradually, several days before gradual discontinuation of clonidine.

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

Tubocurarine. The use of drugs for inhalation anesthesia, including tubocurarin, while taking sotalol increases the risk of myocardial suppression and the development of arterial hypotension.

Amphotericin B and glucocorticosteroids. With simultaneous use, it is necessary to monitor the level of potassium.

Laxatives. Concomitant use with laxatives is not recommended.

How to take, course of use and 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 (after about 12 hours). This dose can be increased, if necessary, to 240 or 320 mg per day after an appropriate clinical assessment of the patient’s condition. In most patients, the therapeutic response is achieved at a total daily dose of 160-320 mg, divided into two doses. Some patients with life-threatening refractory ventricular arrhythmia may require up to 480-640 mg of the drug per day; however, such doses can only be prescribed in cases where the potential benefit outweighs the increased risk of side effects, especially pro-arrhythmogenic effects.

In patients with cardiomyopathy, chronic heart failure, angina pectoris, arterial hypertension, 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 by 80 mg / day if necessary (1 tablet of 80 mg or ½ tablet of 160 mg) at weekly intervals. The rate of dose increase depends on the patient’s tolerance to the drug, which, in particular, is assessed by the degree of induced bradycardia and clinical response. Due to the relatively long half-life in most patients, sotalol is effective when taken once a day. Dose range: 160-320 mg / day.

Overdose

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

Treatment: gastric lavage, the appointment of activated charcoal, with violations of atrioventricular conduction,1-2 mg of atropine is administered intravenously, with low efficiency, a temporary pacemaker is installed; with bronchospasm, inhaled or parenteral beta-adrenomimetic; with a decrease in blood pressure, epinephrine is effective; hemodialysis.

Special instructions

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

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

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

Sotalol Canon 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. Particular attention should be paid to the electrolyte balance and acid-base status 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 trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats / min; smokers have a lower effectiveness of beta-blockers; patients using contact lenses should take into account that during treatment there may be a decrease in tear fluid production; hypersensitivity reactions may increase and the lack of effect from conventional doses of epinephrine against the background of a burdened allergic anamnesis; if elderly patients develop increasing bradycardia (less than 50 beats / min) hypotension (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver and kidney function disorders, the dose should be reduced or treatment should be discontinued; it is recommended to stop therapy if depression develops due to beta-blockers; ethanol should be excluded for the duration of treatment; catecholamines, normetanephrine and vanillylmindal acid, titers should be discontinued before testing in blood and urine. antinuclear antibodies.

Influence on the ability to drive motor vehicles and manage mechanisms

During the treatment period, headache and fatigue may occur, so 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.

Form of production

Tablets are white or almost white in color, round, flat-cylindrical, with a risk.

Storage conditions

The drug should be stored out of the reach of children, dry, protected from light at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Sotalol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets