Sotaleks - instructions for use, doses, side effects, contraindications

Active substanceSotalolSotalol

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SOTAHEXAL

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Bristol-Myers Squibb France

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TECHNOLOGY OF DRUGS, LTD. Russia

Sotalol

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ATOLL, LLC Russia

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CANONFARMA PRODUCTION, CJSC Russia

Dosage form: & nbsppills

Composition:

Each tablet contains:

Active ingredient: 160 mg of sotalol hydrochloride.

Excipients: lactose monohydrate, stearic acid, magnesium stearate, corn starch, silicon dioxide colloidal anhydrous, microcrystalline cellulose.

Description:

Round biconvex tablets of white color with a risk on one side and engraving "160" on the other.

Pharmacotherapeutic group:beta-blocker

ATX: & nbsp

C.07.A.A Non-selective beta-blockers

C.07.A.A.07 Sotalol

Pharmacodynamics:

Sotalol is a non-selective blocker of 3-adrenergic receptors that acts on both β1 and β2 receptors and does not have its own sympathomimetic activity (CMA) and membrane-stabilizing activity (MCA) .As with other beta-adrenoblockers, sotalol suppresses the secretion of renin, and this effect has a pronounced character both at rest and during exercise.

The β-adrenoblocking effect of the drug causes a decrease in the heart rate (negative chronotropic action) and a limited decrease in the force of the heart contractions (negative inotropic action). These heart function changes reduce myocardial oxygen demand and heart burden volume.

Antiarrhythmic properties of sotalol are associated with both the ability to blockade beta-adrenergic receptors, and with the ability to prolong the potential of the action of the myocardium. The main effect of sotalol is to increase the duration of effective refractory periods in the atrial, ventricular and additional ways of carrying out the pulse. On an electrocardiogram recorded in standard leads: the properties corresponding to Class II and III can be reflected in the form of prolongation of the intervals PR, QT and QTc (QT with correction for heart rate) in the absence of noticeable changes in the duration of the QRS complex.

Pharmacokinetics:

Bioavailability for oral administration is almost complete (more than 90%). The maximum concentration in the blood plasma is achieved after 2.5-4 hours after ingestion, and the equilibrium concentration within 2-3 days.Absorption of the drug is reduced by approximately 20% when eating 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 the central compartment (plasma), as well as in the peripheral compartment, with a half-life of 10-20 hours.

Sotalol does not bind to blood plasma proteins and is not metabolized. The pharmacokinetics of the d- and 1-enantiomers of sotalol are almost identical.

Sotalol poorly penetrates the blood-brain barrier, and its concentration in the cerebrospinal fluid is only 10% of the concentration in the blood plasma. The main way to remove from the body is the secretion through the kidneys. From 80 to 90% of the administered dose is excreted unchanged in the urine, and the rest with feces. Patients with impaired renal function should be given smaller doses of the drug. With age, the pharmacokinetics changes insignificantly, although renal dysfunction in elderly patients reduces the rate of excretion, which leads to increased accumulation of the drug in the body.

Indications:

paroxysmal atrial tachycardia, paroxysmal atrial fibrillation, paroxysmal atrioventricular recurrent tachycardia of the "re-enter" type, paroxysmal atrioventricular recurrent tachycardia on the basis of additional routes and paroxysmal supraventricular tachycardia after surgery, Wolff-Parkinson-White syndrome;

maintenance of a normal sinus rhythm after arresting atrial fibrillation or atrial flutter;

treatment of symptomatic unstable ventricular tachyarrhythmias and symptomatic premature contractions of the ventricle;

treatment of arrhythmias caused by elevated levels of catecholamines circulating in the blood or increased sensitivity to catecholamines.

Contraindications:

- Hypersensitivity to sotalol or other components of the drug and sulfonamides;

- Chronic heart failure IIB - III stage;

- Cardiogenic shock;

- Atrioventricular blockade of II and III degree;

- Sinoatrial block;

- Syndrome of weakness of the sinus node;

- Tachycardia of the "pirouette" type;

- Symptomatic sinus bradycardia (heart rate less than 50 beats / min.)

- Congenital or acquired syndromes characterized by lengthening of the QT interval;

- Bronchial asthma or chronic obstructive pulmonary disease (COPD);

- Pheochromocytoma without simultaneous administration of a-adrenoblockers;

- Renal failure (creatinine clearance less than 10 ml / min);

- General anesthesia, which causes suppression of myocardial function (for example, cyclopropane or trichlorethylene);

- Arterial hypotension (systolic blood pressure less than 90 mm Hg);

- Simultaneous administration of monoamine oxidase inhibitors (MAO);

- Lactation period;

- Age to 18 years (effectiveness and safety not established).

Carefully:

Caution should be used when prescribing the drug to patients who have recently undergone myocardial infarction with diabetes, psoriasis, as well as patients with impaired renal function, in case of atrioventricular blockade of the first degree, in violation of water-electrolyte balance: hypomagnesemia, hypokalemia, thyrotoxicosis; depression (including in the anamnesis), lengthening of QT interval, elderly age.

Pregnancy and lactation:

The drug should be used during pregnancy only if there are vital indications.

Dosing and Administration:

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

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

In patients with cardiomyopathy or chronic heart failure with angina, hypertension, conditions after myocardial infarction, it is recommended to begin treatment in a hospital. The initial dose is 160 mg per day in one or two doses. After a week, the dose can be increased as necessary to 80 mg / day ('L tablets 160 mg) at weekly intervals.The rate of dose increase depends on the tolerance of the drug to patients, which, in particular, is assessed by the degree of induced bradycardia and clinical response. Due to the relatively long half-life in most patients, SOTALEX® is effective once a day. Dose interval: 160 - 320 mg / day.

Use in patients with impaired renal function

Because the sotalol is excreted from the body mainly in the urine, and the half-life period increases with renal insufficiency, the dosage of the drug should be reduced with a serum creatinine level of more than 120 μmol / l in accordance with the following recommendations:

Serum Blood Creatinine		Recommended dose
μmol / l	mg / dL
less than 120	less than 1,2	Usual Dose
120-200	1,20 - less than 2,3	3/4 of the usual dose
200-300	2,3 - less than 3,4	1/2 of the usual dose
300-500	3,4 - less than 5,7	1/4 of the usual dose

Side effects:

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

From the cardiovascular system: bradycardia, dyspnea, retrosternal pain, palpitations, edema, decreased blood pressure, arrhythmogenic effect, fainting, heart failure.

From the skin: urticaria, skin rash.

From the gastrointestinal tract: nausea, vomiting, indigestion, diarrhea,

abdominal pain, flatulence.

From the side of the central nervous system: a feeling of fatigue, asthenia, dizziness, headache, sleep disturbances: drowsiness or insomnia, depression, paresthesia in the extremities, feelings of anxiety, mood changes, tremors.

From the genitourinary system: sexual dysfunction.

From the musculoskeletal system: convulsions.

From the senses: visual impairment, taste sensations, hearing impairment. Laboratory indicators: There may be overestimated results with

photometric analysis of urine for metanephrine (O-methyl adrenaline). If pheochromocytoma is suspected, patients should be examined using high performance liquid chromatography with solid phase extraction.

Other: fever.

Overdose:

Symptoms: bradycardia, chronic heart failure, decreased blood pressure,

bronchospasm, hypoglycemia.

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

Interaction:

Antiarrhythmic drugs. Simultaneous administration of sotalol with antiarrhythmic agents of the IA class (disopyramide, quinidine, procainamide) and drugs of the third class (for example, amiodarone) can cause an extension of the QT interval.

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

Drugs that increase the duration of the QT interval. SOTALOL® should be used with extreme caution in combination with other QT prolonging agents such as Class I antiarrhythmics, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, as well as some antibiotics of the quinolone series.

Blockers of "slow" calcium channels. Simultaneous administration of beta-adrenoblockers and blockers of "slow" calcium channels can lead to arterial hypotension, bradycardia, conduction disorders and heart failure.It should avoid the use of beta-blockers in combination with blockers of "slow" calcium channels that suppress myocardial function (for example, verapamil and diltiazem), in connection with the additive effect of these agents on atrioventricular conduction and the function of the ventricle.

Drugs that lower the level of catecholamines. Simultaneous use of funds depleting depots of catecholamines (for example, reserpine and guanitidine), together with beta-adrenoblokatorami leads to excessive suppression of the tone of the sympathetic nervous system at rest. Patients should be carefully monitored because of possible signs of lowering blood pressure and / or severe bradycardia, which can lead to fainting.

Insulin and oral hypoglycemic agents. Hyperglycemia may develop, in this case it is necessary to adjust the dose of hypoglycemic agents. SOTALEX® can mask symptoms of hypoglycemia.

Stimulants of p 2 -receptors. When used simultaneously with the drug SOTALEX®, higher doses (3-agonists, such as salbutamol, terbutaline and isoprenaline.

Digoxin.The intake of sotalol does not cause a significant effect on the concentration of digoxin in serum. The arrhythmogenic effect was 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 effect in patients receiving digoxin.

Clonidine. Beta-adrenoblockers can potentiate the arterial hypertension of withdrawal, after stopping the use of clonidine; so beta-blockers should be canceled gradually, a few days before the gradual discontinuation of clonidine.

Special instructions:

Treatment with the drug SOTALEK® is carried out under the control of heart rate, blood pressure, ECG. In case of cancellation, the dose should be reduced gradually.

Do not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually.

With thyrotoxicosis sotalol can mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, since it can strengthen the symptoms of the disease.

When prescribing the drug SOTALEX® patients with pheochromocytoma should simultaneously be prescribed a-adrenoblockers.

When prescribing beta-blockers, patients receiving hypoglycemic drugs should be careful, because during prolonged interruptions in eating can develop hypoglycemia. And such her symptoms, like tachycardia or tremor, will be masked by the action of the drug.

SOTALEX® should not be used in patients with hypokalemia or hypomagnesemia before correction of existing disorders. These conditions can increase the degree of prolongation of the QT interval and increase the likelihood of arrhythmia of the "pirouette" type. It is necessary to closely monitor the electrolyte balance and acid-base state in patients with severe or prolonged diarrhea and in patients receiving drugs that cause a decrease in the content of magnesium and / or potassium in the body.

Form release / dosage:

Tablets of 160 mg.

For 10 tablets per blister, PVC / A1 foil. 3 blisters with instructions for use in a cardboard box.

Packaging:

For 10 tablets per blister, PVC / A1 foil. 3 blisters with instructions for use in a cardboard box.

Storage conditions:

At a temperature of 15 to 25 ° C.

KEEP OUT OF THE REACH OF CHILDREN!

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N011672 / 01

Date of registration:29.12.2006

The owner of the registration certificate:Bristol-Myers SquibbBristol-Myers Squibb France

Manufacturer: & nbsp

BRISTOL-MYERS SQUIBB France

Information update date: & nbsp18.08.2015

Illustrated instructions

Instructions

Sotalex® (Sotalex® )