Sotagexal, tablets 80 mg 20 pcs

Beta1-, beta2-adrenoblocker. Sotalol is a non-selective blocker of β1-, β2-adrenoreceptors that has no sympathomimetic and membrane-stabilizing activity 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 blockade of β-adrenoreceptors and prolongation of 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.

Pharmacokinetics

Intake

The bioavailability when taken orally is almost complete (more than 90%). Cmax in plasma is reached 2.5-4 hours after oral administration. Absorption is reduced by approximately 20% with food compared to fasting. In the dose range from 40 to 640 mg/day the plasma concentration of Sotalol is proportional to the dose taken.

Distribution

Distribution occurs in plasma and in peripheral organs and tissues. It occurs within 2 to 3 days. Sotalol does not bind to plasma proteins.

It penetrates poorly through the GEB, and its concentration in cerebrospinal fluid is only 10% of that in blood plasma.

Metabolism

It is not metabolized. The pharmacokinetics of the d- and l-enantiomers of sotalol are virtually identical.

Elevation

The primary route of excretion is through the kidneys. From 80 to 90% of the administered dose is excreted unchanged in the urine, and the rest in the feces. T1/2 is 10-20 h.

Pharmacokinetics in special clinical cases

Patients with impaired renal function should be prescribed lower doses of the drug.

The pharmacokinetics do not change much 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

Symptomatic and chronic cardiac rhythm disorders:

• ventricular tachycardia, including. supraventricular tachycardia in Wolff-Parkinson-White syndrome;
• ventricular extrasystole;
• paroxysmal atrial fibrillation.

Active ingredient

Sotalol

Composition

Active ingredient:sotalol hydrochloride 80 mg;

Associates: corn starch; lactose; hydroxypropylcellulose; sodium starch glycolate; silicon dioxide; magnesium stearate

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How to take, the dosage

SotaGEXAL is taken orally before meals, without chewing, with plenty of fluid, 80-120 mg/day in 2-3 doses. If effectiveness is insufficient, up to 160-240-320 mg/day in 2-3 doses. In severe arrhythmias, up to 480 mg/day in 2-3 doses. The dose should be increased at 2-3 day intervals.

Interaction

The simultaneous use of slow calcium channel blockers such as verapamil and diltiazem may decrease BP as a result of impaired contractility. The intravenous administration of these drugs against the background of sotalol use should be avoided (except in cases of emergency medicine).
Combined use of class I A antiarrhythmic agents (especially quinidine type: disopyramide, quinidine, procainamide) or class III (eg, amiodarone) may cause pronounced prolongation of the QT interval. Drugs that prolong the QT interval should be used with caution with drugs that prolong the QT interval, such as antiarrhythmic agents of class I, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, as well as some quinolone antibiotics.
Concomitant administration of nifedipine and other 1,4-dihydropyridine derivatives may decrease BP.
Concomitant administration of noradrenaline or MAO inhibitors, as well as abrupt clonidine withdrawal may cause arterial hypertension. In this case the clonidine should be withdrawn gradually and only several days after the end of Sotagexal.
Tricyclic antidepressants, barbiturates, phenothiazines, opioids and antihypertensive agents, diuretics and vasodilators may cause a sharp decrease in BP.
Simultaneous use of Sotagexal with reserpine, clonidine, alpha-methyldopa, guanfacine and cardiac glycosides may cause marked bradycardia and delayed excitation in the heart.
Beta-adrenoblockers may potentiate arterial withdrawal hypertension after discontinuation of clonidine, so beta-adrenoblockers should be withdrawn gradually, several days before gradual discontinuation of clonidine.
Administration of insulin or other oral hypoglycemic agents, especially during physical activity, may lead to increased hypoglycemia and manifestation of its symptoms (increased sweating, rapid pulse, tremor). In diabetes the doses of insulin and/or hypoglycemic drugs should be corrected.
Potassium-excretory diuretics (e.g., furosemide, hydrochlorothiazide) may provoke arrhythmias caused by hypokalemia.
Concomitant use with Sotagexal may require the use of higher doses of beta-adrenomimetics such as salbutamol, terbutaline and isoprenaline.

Special Instructions

Caution should be exercised when prescribing Sotagexal to patients:
– with a history of diabetes mellitus with marked fluctuations in blood glucose levels, as well as with strict diets;
– In pheochromocytoma (simultaneous administration of alpha-adrenoblockers is required);
– In the history or family history of psoriasis;
– In renal dysfunction;
– The elderly.
The drug is administered under the control of HR, blood pressure and ECG. In case of marked BP lowering or HR decrease the daily dose should be reduced.
Patients with impaired renal function require correction of the dosage regimen.
The Sotaguexal administration should be withdrawn under control of the attending physician and gradually (especially after long-term use).
Sotaguexal should not be used in patients with hypokalemia or hypomagnesemia until the correction of the existing disorders. These conditions may increase the degree of QT interval prolongation and increase the probability of “pirouette” arrhythmia. It is necessary to control electrolyte balance and acid-base status in patients with severe or prolonged diarrhea and in patients receiving drugs that cause reduction of magnesium and/or potassium in the body.
In thyrotoxicosis sotalol may mask certain clinical signs of thyrotoxicosis (such as tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it may exacerbate the symptoms of the disease.
Caution should be exercised when prescribing beta-adrenoblockers to patients receiving hypoglycemic agents because hypoglycemia may develop during prolonged interruptions of food intake, with symptoms such as tachycardia or tremors possibly masked by the drug.

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Contraindications

• chronic heart failure stage IIB-III;
• cardiogenic shock;
• AV-blockade of degree II or III;
• sinoatrial block;
• syndrome of weak sinus node;
• explicit bradycardia (HR less than 50 bpm.
• correlated or acquired long QT interval syndrome;
• arterial hypotension (systolic blood pressure <90 mmHg).);
• obliterative vascular disease;
• bronchial asthma or COPD;
• metabolic acidosis;
• pheochromocytoma without concomitant prescription of alpha-adrenoblockers;
• acute myocardial infarction;
• renal insufficiency (CK less than 10 ml/min);
• common anesthesia causing suppression of myocardial function (such as cyclopropane or trichloroethylene);
• pirouette tachycardia;
• severe allergic rhinitis;
• concurrent use of MAO inhibitors;
• lactation period;
• high sensitivity to sotalol, sulfonamides, and other components of the drug.

Patients who have recently had a myocardial infarction, diabetes, psoriasis, renal dysfunction, AV blockade of degree I, electrolyte balance disorders (hypomagnesemia, hypokalemia), thyrotoxicosis, depression (including in case of history) should be treated with caution when prescribing Sotagexal.

In case of QT interval prolongation, elderly patients.

Particular caution should be exercised if there is evidence of allergic reactions in the past and during desensitization therapy because sotalol suppresses sensitivity to allergens.

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Side effects

Nervous system and sensory organs: dizziness, headache, feeling of fatigue, sleep disturbance, confusion, paresthesia, depression. Corneal and conjunctival inflammation (should be considered when wearing contact lenses), visual impairment (extremely rare), decreased tear production.

Cardiovascular system and blood (hematopoiesis, hemostasis): heart failure, bradycardia, AV blockade, angina pectoris (in rare cases), hypotension.

Respiratory system: bronchospasm.

Gastrointestinal system disorders: nausea, diarrhea, constipation, dry mouth.

Metabolic disorders: hypoglycemia (more often in diabetic patients or when strictly following the diet).

Urinary system disorders: decreased potency.

Musculoskeletal disorders: feeling of coldness in the extremities, muscle weakness or cramps.

Skin disorders: skin rash, itching (rare); redness, psoriasiform dermatosis, alopecia.

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Overdose

Symptoms: BP decrease, bradycardia, bronchospasm, hypoglycemia, loss of consciousness, generalized seizures, ventricular tachycardia; in severe cases – symptoms of cardiogenic shock, asystole.
Treatment: gastric lavage, hemodialysis, administration of activated charcoal. Symptomatic therapy: atropine – 1-2 times by IV stream; glucagon – first as a brief IV infusion at a dose of 0.2 mg/kg body weight, then – at a dose of 0.5 mg/kg body weight by IV infusion for 12 hours.

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Similarities

Sotagexal, Sotalol, Sotalol Canon