Sotahexal, pills 80mg, 20pcs

Composition

Active ingredient: sotalol hydrochloride 80 mg;

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

Pharmacological action

Beta 1 -, beta 2-adrenoblocker. Sotalol is a non-selective blocker of β1 -, β2-adrenergic receptors, which does not have its own sympathomimetic and membrane-stabilizing activity. 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 amount of stress on the heart.

The antiarrhythmic properties of sotalol are associated with both beta-adrenergic blockade and prolongation of the myocardial action potential. The main effect of sotalol is to increase the duration of effective refractory periods in the atrial, ventricular and additional pathways of impulse conduction.

Pharmacokinetics

Suction

Oral bioavailability is almost complete (more than 90%). Cmax in blood plasma is reached in 2.5-4 hours after oral use. 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 blood plasma is proportional to the dose taken.

Distribution

Distribution occurs in the plasma, as well as in peripheral organs and tissues. Css is reached within 2-3 days. Sotalol does not bind to plasma proteins.

Poorly penetrates the BBB, and its concentration in the cerebrospinal fluid is only 10% of the concentration in the blood plasma.

Metabolism

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

Deduction

The main route of elimination from the body is excretion 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 hours.

Pharmacokinetics in special clinical cases

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

Symptomatic and chronic cardiac arrhythmias:

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

Contraindications

• chronic heart failure IIB-III stages;
• cardiogenic shock;
• AV-block II and III degree,
• sinoatrial block;
• sick sinus syndrome node;
• bradycardia (heart rate less than 50 beats/min);
• congenital or acquired long QT syndrome;
• arterial hypotension (systolic BP less than 90 mm Hg. St. )
• occlusive vascular disease;
• asthma or COPD;
• metabolic acidosis;
• pheochromocytoma without co-use of alpha-blockers;
• acute myocardial infarction;
• renal failure (CC less than 10 ml/min);
• General anesthesia causes suppression of myocardial function (e. g., cyclopropane, or trichloroethylene);
• tachycardia type “pirouette”;
• a severe allergic rhinitis;
• simultaneous reception of MAO inhibitors;
• lactation;
• age to 18 years (efficacy and safety not established);
• hypersensitivity to sotalol, the sulfonamides and to other components of the drug.

Should be observed caution when prescribing Sotahexal is used in patients with recent myocardial infarction, diabetes mellitus, psoriasis, impaired renal function, grade I AV block, impaired water and electrolyte balance (hypomagnesemia, hypokalemia), thyrotoxicosis, depression (including in the anamnesis), prolongation of the QT interval, and elderly patients.

Use with extreme caution when indicated in the anamnesis for allergic reactions, as well as against the background of desensitizing therapy, because sotalol suppresses sensitivity to allergens.

Side effects

Nervous system and sensory disorders: dizziness, headache, fatigue, sleep disorders, confusion, paresthesia, depression. Inflammation of the cornea and conjunctiva (should be considered when wearing contact lenses), visual impairment (extremely rare), reduced tear production.

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

From the respiratory system: bronchospasm.

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

From the side of metabolism: hypoglycemia (more often in patients with diabetes mellitus or with strict adherence to a diet).

From the genitourinary system: reduced potency.

From the musculoskeletal system: a feeling of cold in the extremities, muscle weakness or convulsions.

From the skin: skin rash, itching (rarely); redness, psoriasis-like dermatosis, alopecia.

Interaction

With simultaneous use of slow calcium channel blockers such as verapamil and diltiazem, a decrease in blood pressure may occur as a result of impaired contractility. Intravenous use of these drugs with sotalol should be avoided (except in cases of emergency medicine). Combined use of Class Ia antiarrhythmics (especially quinidine-type ones: disopyramide, quinidine, procainamide) or Class III antiarrhythmics (for example, amiodarone) may cause marked prolongation of the QT interval. Drugs that increase the duration of the QT interval should be used with caution with drugs that prolong the QT interval, such as Class I antiarrhythmics, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, as well as some quinolone antibiotics. With simultaneous use of nifedipine and other 1,4-dihydropyridine derivatives, a decrease in blood pressure may occur. Concomitant use of norepinephrine or MAO inhibitors, as well as abrupt withdrawal of clonidine, may cause hypertension. In this case, clonidine withdrawal should be carried out gradually and only a few days after the end of Sotahexal use. Tricyclic antidepressants, barbiturates, phenothiazines, opioids and antihypertensives, diuretics and vasodilators can cause a sharp decrease in blood pressure. The use of drugs for inhalation anesthesia, including tubocurarin against the background of taking Sotahexal increases the risk of myocardial function suppression and the development of arterial hypotension. Concomitant use of Sotahexal with reserpine, clonidine, alpha-methyldopa, guanfacine, and cardiac glycosides may cause severe bradycardia and slow down the conduction of excitation in the heart. Beta-blockers may potentiate withdrawal hypertension after clonidine is discontinued, so beta-blockers should be discontinued gradually, several days before the gradual discontinuation of clonidine. The use of insulin or other oral hypoglycemic agents, especially during exercise, can lead to increased hypoglycemia and the manifestation of its symptoms (increased sweating, rapid pulse, tremor). In case of diabetes mellitus, it is necessary to adjust the doses of insulin and / or hypoglycemic drugs. Potassium-withdrawing diuretics (for example, furosemide, hydrochlorothiazide) can trigger the occurrence of arrhythmia caused by hypokalemia. Concomitant use with Sotahexal may require the use of higher doses of beta-adrenomimetics, such as salbutamol, terbutaline, and isoprenaline.

How to take, course of use and dosage

Sotahexal is taken orally, before meals, without chewing, with a sufficient amount of liquid,80-120 mg/day. in 2-3 doses. With insufficient effectiveness — up to 160-240-320 mg / day in 2-3 doses. In severe arrhythmias — up to 480 mg / day in 2-3 doses. Increasing the dose should be carried out at intervals of 2-3 days.

Overdose

Symptoms: decreased blood pressure, bradycardia, bronchospasm, hypoglycemia, loss of consciousness, generalized convulsive seizures, ventricular tachycardia; in severe cases-symptoms of cardiogenic shock, asystole. Treatment: gastric lavage, hemodialysis, use of activated charcoal. Symptomatic therapy: atropine-1-2 times intravenous jet; glucagon-first as a short intravenous infusion at a dose of 0.2 mg/kg of body weight, then-at a dose of 0.5 mg/kg of body weight intravenous infusion for 12 hours.

Special instructions

Caution should be exercised when prescribing Sotahexal to patients: — with a history of diabetes mellitus with pronounced fluctuations in blood glucose levels, as well as with strict diets;- with pheochromocytoma (simultaneous use of alpha-blockers is necessary);— if you have a history or family history of psoriasis;- with impaired renal function— – the elderly. Treatment with the drug is carried out under the control of heart rate, blood pressure, ECG. With a marked decrease in blood pressure or a decrease in heart rate, the daily dose should be reduced. Patients with impaired renal function need to adjust the dosage regimen.Discontinuation of Sotahexal should be made under the supervision of the attending physician and gradually (especially after prolonged use). Sotahexal 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. It is necessary to monitor the electrolyte balance and acid-base state in patients with severe or prolonged diarrhea and in patients receiving medications that cause a decrease in the content of magnesium and/or potassium in the body. With thyrotoxicosis, sotalol 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. Caution should be exercised when prescribing beta-blockers to patients receiving hypoglycemic agents, since hypoglycemia may develop during prolonged breaks in food intake, and its symptoms, such as tachycardia or tremor, may be masked by the action of the drug.

Form of production

Tablets

Storage conditions

In a dark place, at a temperature not exceeding 25 °C.

Expiration date

Shelf life: 5 years.

Active ingredient

Sotalol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets