SOTAGEKSAL

Active material: Sotalol
When ATH: C07AA07
CCF: Beta₁-, beta₂-adrenoblokator
ICD-10 codes (testimony): I45.6, I47.1, I47.2, i48, I49.4
When CSF: 01.01.01.01
Manufacturer: Hexal AG (Germany)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills white or nearly white, round, on the one hand engraved convex “SOT”; on the other side – risk, chamfered surface of the tablet to the risk.

Excipients: lactose monohydrate, corn starch, giproloza, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Pills white or nearly white, round, lenticular, with Valium on one party and chasing “SOT” another.

Excipients: lactose monohydrate, corn starch, giproloza, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Pharmacological action

Beta₁-, beta₂-adrenoblokator. Sotalol is a non-selective β Blocker₁-, b₂-adrenoreceptorov, does not have its own membranostabilizirujushhej and sympathomimetic activity. Like other beta-adrenoblokatoram, sotalol suppresses the secretion of Renin, and this effect is pronounced as at rest, and under load. Beta-adrenoblokirtee the drug reduces HEART RATE (hronotroponoe negative effect) and a limited reduction in the strength of heart contractions (negative inotropic action). These changes of cardiac function reduces the need heart of oxygen and the amount of load on the heart.

Antiarrhythmic properties of sotalola are associated with both the β-adrenoceptor blockade, and prolongation of the action potential of myocardium. The main effect of sotalola is to increase the duration of effective refractory periods in predserdnykh, Ventricular and additional ways of spending pulse.

Pharmacokinetics

Absorption

Bioavailability when administered is almost complete (more 90%). C_max plasma levels achieved after 2.5-4 hours after ingestion. Inflammatory drugs is reduced by approximately 20% When food intake compared with the reception of prandial. In the dosing interval 40 to 640 mg/day sotalola concentration in the blood plasma is proportional to the dose taken.

Distribution

Allocation occurs in a plasma, as well as in the peripheral organs and tissues. C_ss reached within 2-3 days. Sotalol is not associated with blood plasma proteins.

Poor penetrate the BBB, with his concentration in the spinal fluid is only 10% concentration in blood plasma.

Metabolism

Not metabolizmu. Pharmacokinetics (d)- and l-enantiomers of sotalola is almost the same.

Deduction

The main way of removal from the body through the kidneys is. From 80 to 90% imposed dose excreted unchanged in urine, and the remainder from faeces. T_1/2 is 10-20 no.

Pharmacokinetics in special clinical situations

Patients with compromised renal function should appoint smaller doses of the drug.

Pharmacokinetics with age changes slightly, Although the kidney function in elderly patients reduces the speed selection, that leads to increased accumulation of the drug in the body.

Testimony

Symptomatic and chronic cardiac arrhythmias:

-ventricular tachycardia, incl. supraventrikuliarnaya tachycardia syndrome Wolf-Parkinson-White syndrome;

-Ventricular arrythmia;

is a paroxysmal form predserdy.

Dosage regimen

The drug is taken orally for 1-2 hour before meals, without chewing, drinking plenty of fluids.

Simultaneous eating (especially milk and milk products) reduces inflammatory drugs.

Dose picked individually, depending on the severity of the disease and the patient response to treatment.

The initial dose is 80 mg / day. In the absence of symptoms of therapeutic effect dose can be gradually increased to 240-320 mg / day, razdelennoy of 2-3 admission. Most patients therapeutic effect was achieved on total daily dose 160-320 mg, razdelennoy of 2 admission.

When life-threatening severe arrhythmia may increase doses up to 480 mg, divided by 2 or 3 individual admission. However, these doses may be granted only in cases, When the potential benefit outweighs the risk of side effects, especially proaritmogennogo actions.

In patients with impaired renal function There is a risk of cumulation, so they must control QC and HR (not below 50 u. / min). Since sotalol is secreted from the body mainly through the kidneys, and since its half-life is increased in the presence of renal failure, dosage should be reduced in the level of serum creatinine more than 120 micromole/l according to the following guidelines:

At severe renal insufficiency It is necessary to conduct regular monitoring of the ECG and the level of drug concentration in the serum.

Duration of therapy is determined by the attending physician.

In that case, If the patient had forgotten to take the pill, next time should not take additional medication, It is necessary to adopt only the assigned number Sotageksala.

Side effect

Cardio-vascular system: bradycardia, breathlessness, chest pain, heartbeat, AV блокада, increased symptoms of heart failure, heartbeat, swelling, fainting, aritmogennoe action, decrease in blood pressure; rarely – increasing angina attacks.

From the digestive system: nausea, vomiting, diarrhea, constipation, dry mouth, abdominal pain, flatulence.

CNS: headache, dizziness, fatigue, state of depression, anxiety, mood changes, tremor, asthenia, sleep disorders (drowsiness or insomnia), depression, paresthesias in extremities.

From the senses: visual impairment, inflammation of the cornea and conjunctiva (to consider when wearing contact lenses), decrease in lacrimation, hearing disorder, sense of taste.

On the part of the endocrine system: gipoglikemiâ (most likely in patients with diabetes mellitus, or with strict dieting).

The respiratory system: bronchospasm (especially if there is a violation of pulmonary ventilation).

With the genitourinary system: reduced potency.

Dermatological reactions: skin rash, itch, redness, psoriazoformny Dermatosis, alopecia, hives.

Laboratory findings: elevated results when using photometric analysis of urine metanephrine (About-metiladrenalin).

Other: cold extremities, muscular weakness, convulsions, fever.

Contraindications

-chronic heart failure IIB-III stage;

- Cardiogenic shock;

— AV-blockade II or III degrees;

- Sinoatrialynaya blockade;

sick sinus syndrome;

- Vыrazhennaya bradycardia (HR less 50 u. / min);

is congenital or acquired long QT syndrome;

- Hypotension (systolic blood pressure less than 90 mmHg.);

— obliterating diseases of blood vessels;

-bronchial asthma or COPD;

- Metabolic acidosis;

-pheochromocytoma without simultaneous appointment Alfa-adrenoblokatorov;

- Acute myocardial infarction;

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

-General anesthesia, causing inhibition of myocardial function (eg, R22 or trichloroethylene);

-tachycardia type “pirouette”;

-severe allergic rhinitis;

- Simultaneous MAO inhibitors;

- Lactation;

- Up to 18 years (efficacy and safety have not been established);

-hypersensitivity to sotalolu, sulfonamidam to other components of the drug.

Observe caution in the appointment Sotageksala patients, recently suffered myocardial infarction, for patients with diabetes, psoriaze, impaired renal function, AV-blockade I degree, If there is a violation vodno-elektrolitnogo balance (gipomagniemiya, kaliopenia), thyrotoxicosis, depression (incl. and in history), When extending the QT interval, elderly patients.

FROM caution used for guidance in history on allergic reactions, as well as on the background of spending desensibilizirujushhej therapy, tk. sotalol suppresses the sensitivity to allergens.

Pregnancy and lactation

Reception Sotageksala during pregnancy, especially, first 3 of the month, only available by vital conditions and with careful correlation of all risk factors.

In the case of therapy during pregnancy, admission drug should be lifted for 48-72 hours before the expected date of childbirth because of the opportunities for the development of bradycardia, hypotension, hypokalemia and depressed respiration in newborns.

Sotalol passes into breast milk and reaches effective concentrations there. If necessary, the appointment of the drug in breastfeeding, breastfeeding must stop.

Cautions

Caution must be exercised in the appointment Sotageksala patients:

— a history of diabetes mellitus with marked fluctuations in blood glucose levels, as well as subject to strict diets;

— feohromotsytome (should the simultaneous appointment of Alfa-adrenoblokatorov);

— with a history or family history of psoriasis;

— in violation of the kidney;

-seniors.

Treatment out under the supervision of HR, FROM, ECG. Expression reduction of hell or urezhenii HR, the daily dose should be reduced.

Patients with impaired renal function requires correction mode.

Cancellation of admission Sotageksala should be done under the supervision of a physician and gradually (especially after long-term use).

Sotageksal should not be used in patients with gipokaliemiei or gipomagniemiej to the correction of existing violations. These conditions can increase the degree of elongation QT interval and increase the likelihood of arrhythmias type “pirouette”. Requires control of electrolyte balance and acid-base status in patients with severe or prolonged diarrhea and patients, receiving medicines, causing reduction of magnesium and potassium in the body and/or.

When may mask certain sotalol tireotoxicose clinical signs of hyperthyroidism (eg, taxikardiju). Sudden removal of tiretoksikozom patients is contraindicated, Since the ability to strengthen the symptoms of the disease.

When you assign a beta-adrenoblokatorov patients, receiving hypoglycemic agents, Caution should be exercised, because during prolonged breaks in food intake can develop hypoglycemia, and its symptoms, How tachycardia or tremor, can be masked due to the action of the drug.

Overdose

Symptoms: decrease in blood pressure, bradycardia, bronchospasm, gipoglikemiâ, loss of consciousness, generalized convulsive seizures, ventricular tachycardia; in severe cases – symptoms of cardiogennogo shock, asistolija.

Treatment: gastric lavage, hemodialysis, appointment of activated carbon. Symptomatic therapy: atropyn – 1-2 times in/in struino; glucagon – first as brief in/in infusion dose 0.2 mg / kg body weight, then – dose 0.5 mg/kg body weight in/in cefuroxim during 12 no.

Drug Interactions

While admission slow calcium channels blocker Verapamil and diltiazem type may reduce the magnitude of HELL as a result of the deterioration of contractility. Should be avoided in/with the introduction of these drugs against the backdrop of sotalola (except in cases of emergency medicine).

The combined use of antiarrhythmics class I A (especially hinidinovogo type: disopyramide, quinidine, prokaynamyd) or class III (eg, Amiodarone) can cause pronounced elongation QT interval. Preparations, increase the QT interval duration, should be used with caution with drugs, prolonging the QT interval, such, as class I antiarrhythmics, fenotiazinы, tricyclic antidepressants, and terfenadin astemizol, as well as some antibiotics hinolonovogo series.

While receiving nifedipine and other derivative digidropiridina-1.4 may reduce the magnitude of HELL.

The simultaneous appointment of norepinephrine or MAO inhibitors, as well as the sudden removal of clonidine may cause arterial hypertension. In this case, the abolition of the clonidine should be gradually and only a few days after the reception of Sotageksala.

Tricyclic antidepressants, barbiturates, fenotiazinы, opioid and antihypertensives, diuretics and vasodilators may cause a sharp decline ad.

The use of means of inhalation narcosis, incl. tubokurarina against the backdrop of the admission Sotageksala increases the risk of oppression of myocardial function and development of arterial hypotension.

If you are applying to Sotageksala with rezerpinom, clonidine, Alpha metildopoj, guanfacinom and cardiac glycosides may develop bradycardia and a slowdown of the institution at the heart of.

Beta-adrenoblokatora may potenzirovti arterial hypertension screening cancellation, After receiving clonidine, Therefore, beta-adrenoblokatora should be lifted gradually, a few days before the phasing out of clonidine.

Appointment of insulin or other oral gipoglikemicakih funds, especially, during physical exercise, can exacerbate hypoglycemia and its symptoms (increased sweating, rapid pulse, tremor). Diabetes need a correction doses of insulin and/or hypoglycemic drugs.

Kaliivforodaschie diuretics (eg, furosemid, gidroxlorotiazid) can provoke the appearance of arrhythmia, caused by gipokaliemiei.

Together with the application Sotageksalom, you may need to use higher doses of beta-adrainomimetikov, such as salbutamol, terbutaline and isoprenaline.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 5 years.