Sotalol - instructions for use, dose, side effects, contraindications

Active substanceSotalolSotalol

Similar drugsTo uncover

SOTAHEXAL

pills inwards

HEXAL AG Germany

Sotalex®

pills inwards

Bristol-Myers Squibb France

Sotalol

pills inwards

TECHNOLOGY OF DRUGS, LTD. Russia

Sotalol

pills inwards

ATOLL, LLC Russia

Sotalol Canon

pills inwards

CANONFARMA PRODUCTION, CJSC Russia

Dosage form: & nbsppills

Composition:

Composition per one tablet: dosage:

Active substance: 80 mg 160 mg

Sotalol hydrochloride 80.0 160.0 mg

Excipients:

Lactose Monohydrate 97.0 mg 194.0 mg

Microcrystalline cellulose 120.0 mg 240.0 mg

Silica colloidal dioxide 1.5 mg 3.0 mg

Magnesium stearate 1.5 mg 3.0 mg

Description:Round biconvex tablets of white color.

Pharmacotherapeutic group:antiarrhythmic drug

ATX: & nbsp

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

C.07.A.A.07 Sotalol

Pharmacodynamics:

Sotalol is an antiarrhythmic drug of Class II and III according to the Vogan-Williams classification, which possesses the properties of a non-selective beta-blocker. It is a racemic mixture consisting of D- and L-stereoisomers of sotalol. Both isomers have class III antiarrhythmic effects, while the L-stereoisomer is practically

for all beta-adrenoblocking properties.

Like other beta-blockers, sotalol suppresses the secretion of renin, and this effect has a pronounced character both at rest and during exercise. Beta-adrenoblokiruyuschee effect of the drug Causes a decrease in heart rate (heart rate) (negative chronotropic action) and a limited decrease in the force of the heartbeats (negative inotropic effect). These changes in cardiac activity reduce the need for myocardium in oxygen and the volume of the heart load. Antiarrhythmic properties of sotalol are associated with both the ability to blockade of 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: properties corresponding to Class II and III can be reflected in the form of lengthening PR, QT and QTc intervals (QT with correction for heart rate) in the absence of noticeable changes in the duration of the QRS complex.

Pharmacokinetics:

Bioavailability with oral administration is 90% -100%.The maximum concentration in the blood plasma is achieved after 2.5-4 h after ingestion, and the equilibrium concentration within 2-3 days (ie after taking 5-6 doses when taken 2 times a day). Absorption of sotalol is reduced by approximately 20% with simultaneous intake with food compared with fasting. In the dose range from 160 to 640 mg / day, the concentration of sotalol in the blood plasma is proportional to the dose taken. Distribution occurs in the blood plasma, as well as in peripheral organs and tissues, 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 L-enantiomers of sotalol are almost identical. 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 dose administered is excreted unchanged by the kidneys, and the rest is through the intestine.

Patients with impaired renal function should be given smaller doses of the drug. As the patient ages, the pharmacokinetics change slightly, although impaired renal function in elderly patients reduces the rate of excretion,which leads to an increased accumulation of sotalol in the body.

Indications:

Ventricular arrhythmia:

prevention of recurrence of life-threatening ventricular tachyarrhythmia;

treatment of symptomatic unstable ventricular tachyarrhythmia.

Nadzheludochkovaya arrhythmia:

prevention of paroxysmal atrial tachycardia, paroxysmal atrial fibrillation, paroxysmal atrial-ventricular nodal reciprocating tachycardia of the "re-entry" type, paroxysmal atrial-ventricular reciprocal tachycardia involving additional pathways and paroxysmal supraventricular tachycardia after surgical intervention;

maintenance of normal sinus rhythm after conversion of atrial fibrillation or atrial flutter.

Contraindications:

Mental disturbance: feelings of anxiety, sleep disturbances (drowsiness or insomnia), mood changes, depression, depression;

Hypersensitivity to sotalol, other derivatives of sulfonamide and to other components of the drug;

Heart failure in the stage of decompensation;

Cardiogenic shock;

Atrioventricular (AV) block of II or III degree;

Sinoatrial block;

Syndrome of weakness of the sinus node;

Pronounced bradycardia (heart rate less than 50 beats per minute);

Angina of princemetal;

Congenital or acquired long QT interval syndrome;

Hypokalemia;

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

Severe violations of peripheral circulation, including Raynaud's syndrome;

Bronchial asthma or chronic obstructive pulmonary disease (COPD);

Metabolic acidosis;

Pheochromocytoma without simultaneous administration of alpha-blockers; Cardiomegaly (no signs of heart failure);

Acute myocardial infarction in the first 2 weeks after myocardial infarction and with a decrease in the left ventricular ejection fraction (less than 40%);

General anesthesia that causes suppression of myocardial function (eg, cyclopropane or trichlorethylene);

Ventricular tachycardia of the "pirouette" type;

Severe allergic rhinitis;

Simultaneous administration of monoamine oxidase inhibitors (MAO), simultaneous intravenous administration of blockers of "slow" calcium channels like verapamil (see section "Interaction with other drugs"),

Age under 18 years (efficiency and safety not established);

Lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome.

Carefully:

Care should be taken when prescribing the drug Sotalol patients with recent myocardial infarction (no earlier than 2 weeks after myocardial infarction), diabetes mellitus, psoriasis, renal dysfunction, grade I atrioventricular block, chronic heart failure, water-electrolyte imbalance: hypomagnesemia, hypokalemia; at

hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hyperthyroidism, hypertension, hypertension, hypertension, hypertension, hypertension; background of carrying out desensitizing therapy, with obliterating diseases of peripheral vessels, with bronchospasm (in anamnesis).

Pregnancy and lactation:

Adequate controlled studies in pregnant women have not been conducted. Sotalol penetrates the placenta and is found in the amniotic fluid. Beta-adrenoblockers reduce placental blood flow, which can lead to fetal death in utero. In addition, undesirable phenomena (in particular,

hypoglycemia and bradycardia) may occur in the fetus and in the newborn.

In the case of therapy during pregnancy, the drug should be withdrawn 48-72 hours before the expected delivery due to the possibility of bradycardia, arterial hypotension, hypokalemia and respiratory depression in newborns. There is an increased risk of complications from the heart and lungs in newborns in the postpartum period.

The use of sotalol during pregnancy is possible only if the benefit to the mother exceeds the potential risk to the fetus. A careful monitoring of the condition of newborns is necessary within 48-72 hours after childbirth.

Sotalol penetrates into breast milk and reaches effective concentrations there. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, for 1-2 hours before eating, without chewing, squeezed with enough liquid.The dose of the drug is selected individually depending on the severity of the disease, evaluation of the electrocardiogram (ECG), kidney function, interaction with other medications taken and the patient's response to treatment.

The initial dose is 80 mg 2 times a day (approximately at an interval of 12 hours). If the therapeutic effect is inadequate, after a corresponding clinical evaluation of the patient's condition, 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 daily dose of 160-320 mg, divided into 2 doses.

In life-threatening severe arrhythmias, a dose increase of up to 480 mg, divided into 2 or 3 separate doses, is possible. However, such doses can be prescribed only in cases where the potential benefit exceeds the risk of side effects, especially pro-arrhythmogenic action.

In connection with the presence of the effect of antiarrhythmics in the third class of the drug, the possibility of increasing the QT interval should be monitored and, if necessary, individual dosing should be performed.

In patients with cardiomyopathy or chronic heart failure (CHF),with angina pectoris, arterial hypertension, after a previous myocardial infarction, it is recommended to start therapy in a hospital. The initial dose is 160 mg / day in 1 or 2 doses. After a week, the dose can be increased by 80 mg / day with weekly intervals if necessary. 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 the therapeutic response to the therapy. Due to the relatively long half-life in most patients, the drug Sotalol is effective when taken 1 time per day. Dose interval: 160-320 mg / day.

Use in patients with impaired renal function

In patients with impaired renal function, there is a risk of cumulation, so they need to monitor the amount of creatinine clearance (CC) and heart rate (at least 50 beats per minute).

Because the sotalol is excreted mainly by the kidneys and its half-life increases, it is necessary to change the dosage regimen (the time between doses of the drug) when the SC is less than 60 ml / min, according to the table below:

Creatinine clearance, ml / min	Dosing interval
>60	12h
30-59	24 h
10-29	36-48 h
< 10	Individual
	picking

Dosage of the drug in case of impaired renal function should be reduced with a serum CC concentration of more than 120 μmol / l in accordance with the following recommendations:

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

The duration of therapy is determined by the doctor.

In the event that you forgot to take a pill on time, the next time you should not double the dose, you only need to take the prescribed amount of the drug Sotalol.

Side effects:

According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: often (> 1/100, <1/10), infrequently (> 1/1000, <1/100), rarely (> 1 / 10000, <1/1000) and very rarely (<1/10000), including individual messages; frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

Mental disturbances: often: feelings of anxiety, sleep disturbances (drowsiness or insomnia), mood changes, depression, depression.

From the side of the nervous system: often: headache, dizziness, light hallucinations, asthenia, paresthesia in the extremities,syncopal condition; frequency is unknown: increased fatigue, tremor.

From the senses: often: visual impairment, hearing impairment, changing taste sensations; Very rarely: a decrease in tearing; frequency unknown: inflammation of the cornea and conjunctiva (should be borne in mind when wearing contact lenses). From the cardiovascular system: often: bradycardia, palpitations, heart rhythm disturbance, shortness of breath, chest pain, AV blockade, increased heart failure symptoms, proarrhythmia, pirouette type arrhythmia, decreased blood pressure, swelling; frequency unknown: syncope, increased angina attacks, cold extremities, Raynaud's disease, short-term exacerbation of intermittent claudication.

From the side of the system of the thorax and mediastinum: infrequently: bronchospasm (especially in case of pulmonary ventilation impairment).

On the part of the digestive system: often: dyspepsia (nausea, vomiting), diarrhea, constipation, dryness of the oral mucosa, abdominal pain, flatulence.

From the side of the rut and subcutaneous tissues: frequency is unknown: skin rash, itching,

redness, psoriasis dermatosis, alopecia, urticaria.

From the musculoskeletal and connective tissue: often: muscle weakness, convulsions.

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: education

antinuclear antibodies, hypoglycemia (most likely in patients with diabetes mellitus, or with strict adherence to diets), there may be overestimated results in the photometric analysis of urine for metanephrine.

Overdose:

Symptoms: decreased blood pressure, bradycardia, bronchospasm, hypoglycemia, loss of consciousness, generalized convulsive seizures, prolongation of the QT interval, ventricular tachycardia (including pirouette type); in severe cases - the symptoms of cardiogenic shock, asystole, sometimes with a fatal outcome.

Treatment: gastric lavage, hemodialysis, the use of activated charcoal. Symptomatic therapy:

Bradycardia: atropine - 1 -2 times intravenously struino; glucagon - first in the form of a brief intravenous infusion at a dose of 0.2 mg / kg body weight, then at a dose of 0.5 mg / kg body weight intravenously, infusion for 12 hours.

Atrioventricular block of 2-3 degrees: a temporary

an artificial pacemaker.

Severe BP reduction: effective epinephrine.

Bronchospasm: amophillin or sympathomimetics of beta-2-adrenoreceptors (inhalation). Tachycardia as pirouette: cardioversion, setting up a temporary artificial pacemaker (if necessary), epinephrine and / or magnesium sulfate.

Interaction:

Antiarrhythmic drugs. Simultaneous use of sotalol with antiarrhythmic agents of the IA class (disopyramide, quinidine, procainamide) and III class (for example, amiodarone) can cause a pronounced extension of the QT interval. Digoxin. The use of sotalol has no significant effect on the concentration of digoxin in serum. The arrhythmogenic effect developed more often in patients using simultaneously sotalol and digoxin (risk of developing bradycardia).

Blockers of "slow" calcium channels (BCCI). Simultaneous administration of beta-blockers and BCCC can lead to arterial hypotension, bradycardia, conduction disorders and heart failure. It should avoid simultaneous use of beta-blockers with BCCC, suppressing the function of the myocardium (for example,

verapamil and diltiazem), due to the additive effect of these agents on AV conduction and ventricular function.

Avoid intravenous administration of these drugs against the background of the use of sotalol (except for cases of emergency medicine).

Potassium-withdrawing diuretics (for example, furosemide, hydrochlorothiazide). 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. Use with caution with drugs that extend the QT interval, such as Class I antiarrhythmics, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, as well as some antibiotics of the quinolone series.

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

Insulin or hypoglycemic agents for oral administration.Hyperglycemia may develop, in this case, correction of doses of hypoglycemic agents is necessary. Sotalol can mask the symptoms of hypoglycemia.

Beta2-adrenomimechgics. When used simultaneously with sotalol, higher doses of beta2-adrenomimetics may be required, such as salbutamol, terbutaline and isoprenaline.

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

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

The use of funds for inhalation anesthesia, including tubocurarine on the background of sotalol, increases the risk of oppression of myocardial function and development of arterial

hypotension.

Isozymes of the cytochrome P450 system. It is not expected to interact with drugs that are metabolized by cytochrome P450 isoenzymes.

Lymphotericin B, glucose and mineralocorticosteroids (for systemic use), some laxatives may cause hypokalemia.It is necessary to control the potassium content with simultaneous application with sotalol.

Special instructions:

Treatment with drug Sotalol spend under the control of heart rate, a BP, an electrocardiogram.

The initiation of sotalol therapy or a change in dosage should be accompanied by an appropriate medical examination including ECG monitoring with QT interval evaluation, monitoring kidney function, measuring the electrolyte content, and concomitant therapy.

In case of withdrawal of the drug Sotalol the dose should be reduced gradually, especially in patients with coronary heart disease, after a recent myocardial infarction, hypertension. Do not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually.

It is necessary to teach the patient how to calculate heart rate and instruct the patient about the need to consult a doctor at a heart rate of less than 50 beats per minute.

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

In the appointment of sotalol, patients with pheochromocytoma should be concomitantly assigned alpha-blockers.

Should be appointed sotalol with caution to patients:

at a diabetes with the expressed fluctuations of concentration of a glucose in a blood, and also at observance of a strict diet;

with pheochromocytoma (simultaneous administration of alpha - adrenoblockers is necessary);

if there is a history or family history of psoriasis;

if the kidney function is impaired;

the elderly.

Care must be taken when using sotalol in patients with CHF: beta-adrenoblockade can further reduce myocardial contractility and provoke worsening of symptoms of CHF. It should be used with caution at the beginning of therapy in

patients with left ventricular dysfunction. With standard treatment (enzyme angiotenzinprevragtsayuschego inhibitors, diuretics, cardiac glycosides, etc.) Must be assigned a lower initial dose and then select a dose given clinical situation.

Sotalol can be used after previous antiarrhythmic therapy, only under the condition of careful monitoring and at least 2-3 half-lives of the anti-arrhythmic agent used earlier (see.section "Interaction with other drugs"), are used with extreme caution in case of anamnesis for allergic reactions, as well as against desensitizing therapy. sotalol suppresses sensitivity to allergens.

Sotalol 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. These disorders must be corrected before starting the use of the drug Sotalol.

It is necessary to control the water-electrolyte balance and acid-base state in patients with severe or prolonged diarrhea and in patients receiving medicines that cause a decrease in magnesium and / or potassium in the body. When prescribing beta-blockers, patients receiving hypoglycemic agents should be careful, because during prolonged interruptions in eating, hypoglycemia may develop, and symptoms such as tachycardia or tremor can be masked by the action of sotalol.

In smokers, the effectiveness of beta-blockers is lower.

Patients who use contact lenses should take into account that the tear fluid production can be reduced against the background of therapy.

If elderly patients develop an increasing bradycardia (less than 50 minutes per minute), arterial hypotension (systolic blood pressure less than 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmia, severe liver and kidney function, it is necessary to reduce the dose of the drug or stop therapy.

It is recommended to stop therapy with the development of depression caused by the use of beta-blockers.

Beta-adrenoblockers can aggravate the course of psoriasis.

Like other beta-blockers, sotalol should be used with caution in patients who underwent surgery.

For the duration of therapy, alcohol intake should be avoided.

It is necessary to cancel the drug before determining in the blood and urine catecholamines, normetanefrin and vanillylmandelic acid; titers of antinuclear antibodies.

Effect on the ability to drive transp. cf. and fur:

Care must be taken when driving vehicles and engaging in other potentially hazardous activities,requiring increased concentration and speed of psychomotor reactions (risk of developing headaches and increased fatigue).

Form release / dosage:

Tablets of 80 mg and 160 mg.

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 30 tablets in a jar (bottle) polymer for medicines or a jar (bottle) for medicines made of plastic.

Free space in the jar (bottle) is filled with cotton absorbent medical cotton.

Each jar (vial) or 3 contour mesh packages together with the instruction for use is placed in a pack of cardboard box.

Packaging:

Tablets of 80 mg and 160 mg.

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 30 tablets in a jar (bottle) polymer for medicines or a jar (bottle) for medicines made of plastic.

Free space in the jar (bottle) is filled with cotton absorbent medical cotton.

Each jar (vial) or 3 contour mesh packages together with the instruction for use is placed in a pack of cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002768

Date of registration:17.12.2014

The owner of the registration certificate:TECHNOLOGY OF DRUGS, LTD. TECHNOLOGY OF DRUGS, LTD. Russia

Manufacturer: & nbsp

TECHNOLOGY OF DRUGS, LTD. Russia

Information update date: & nbsp18.08.2015

Illustrated instructions

Instructions

Sotalol (Sotalol)