SotaHEXAL

Pharmacological properties of the drug Sotahexal

SotaHexal is a non-selective β-adrenergic receptor blocker that acts on β1- and β2-adrenergic receptors. It has a pronounced antiarrhythmic effect, the mechanism of which is to increase the duration of the action potential and the absolute refractory period in all parts of the conduction system of the heart (Class III antiarrhythmic drugs). Reduces heart rate and myocardial contractility, slows AV conduction, and reduces the absolute refractory period. By blocking β2-adrenergic receptors, it increases the tone of smooth muscles of the bronchi and blood vessels. After oral administration, 75–90% of sotalol hydrochloride is absorbed from the gastrointestinal tract. Due to the lack of effect of the first phase, absolute bioavailability is 75–90%. The time to reach maximum concentration in blood plasma is 2–3 hours. The volume of distribution is 1.6–2.4 l/kg. Sotalol does not bind to plasma proteins and is not metabolized in the body. Up to 90% of the dose taken is excreted unchanged by the kidneys, the rest is excreted in feces. Renal clearance is 120 ml/min and corresponds to the total clearance of the body. The half-life is 10–20 hours. If renal function is impaired, the elimination of sotalol may increase to 42 hours, which requires a reduction in the dose of the drug.

Indications for use of the drug Sotahexal

Supraventricular tachyarrhythmias accompanied by clinical symptoms (including atrioventricular, nodal, paroxysmal tachycardias in WPW syndrome or paroxysmal atrial fibrillation arrhythmias); maintaining normal sinus rhythm after stopping atrial fibrillation or flutter; severe ventricular heart rhythm disturbances, which are accompanied by severe clinical symptoms (tachyarrhythmias) and their prevention with proven effectiveness; arrhythmias caused by excess circulation of catecholamines or increased sensitivity to catecholamines.

Use of the drug Sotahexal

Dose adjustment of SotaHexal in cases of ventricular arrhythmia should be carried out under the constant supervision of a cardiologist; it can be carried out with appropriate equipment in the cardiac emergency room and continuous monitoring. During treatment, screening tests should be carried out at regular intervals (for example, standard or long-term ECG). If individual ECG parameters are changed, therapy must be carefully analyzed, for example, in cases of QRS QT interval by more than 25% , a 50% increase in PQ QT by more than 500 ms , an increase in the number of attacks or severity of arrhythmia. Treatment of tachyarrhythmias The recommended starting dose of SotaHexal is 40 mg 2 times a day. Subsequently, the drug is prescribed in a daily dose of 160–320 mg, divided into 3 doses. If necessary, the dose of the drug can be increased to 160 mg 3 times a day. Severe ventricular heart rhythm disturbances with severe tachyarrhythmia The initial dose of SotaHexal is 80 mg 2 times a day. If necessary, the daily dose can be increased to 80 mg 3 times a day or up to 160 mg 2 times a day. In case of insufficient effectiveness in the treatment of arrhythmia that threatens the patient's life, the daily dose of SotaHexal can be increased to 480 mg, divided into 2 doses. In these cases, the dose should be increased only if the potential benefit outweighs the potential risk of severe adverse reactions (especially proarrhythmic effects). Atrial fibrillation The initial dose of SotaHexal is 80 mg 2 times a day. If necessary, the daily dose can be increased to 80 mg 3 times a day. In cases of paroxysmal atrial fibrillation, this dose should not be exceeded. If in patients with chronic atrial fibrillation the effectiveness of treatment is insufficient, the dose of sotalol hydrochloride can be increased to a maximum of 160 mg 2 times a day. The dose can only be increased at minimum two to three day intervals. Recommended doses for renal failure In severe renal failure, the use of sotalol hydrochloride is recommended only with regular monitoring of the ECG and the concentration of the drug in the blood serum. If creatinine clearance decreases to 10–30 mol/min (serum creatinine 2–5 mg/dL), a dose reduction of 50% is recommended. If the value of this indicator is less than 190 ml/min (serum creatinine ≤5 mg/dl), then a dose reduction by 1/4 is recommended. SotaHexal tablets should be swallowed without chewing, with a sufficient amount of liquid (for example, a glass of water) before meals. When adjusting the dose in patients after myocardial infarction or with severe cardiac pathology, particularly careful monitoring (for example, using monitoring) should be established. During treatment, appropriate testing should be carried out at regular intervals. In patients with coronary artery disease and/or arrhythmia, as well as after prolonged use of the drug, treatment should be discontinued gradually, since abrupt withdrawal may lead to a worsening of the clinical picture of the disease. The duration of treatment is determined depending on the clinical course of the disease and the patient’s condition.

Contraindications to the use of the drug Sotahexal

Chronic heart failure stage IIB–III; acute myocardial infarction; shock; arterial hypotension; AV block II and III degrees; sinoatrial block; sick sinus syndrome; bradycardia (heart rate less than 50 beats/min); prolongation of the QT ; obliterating vascular diseases; obstructive airway diseases; metabolic acidosis; swelling of the larynx; severe allergic rhinitis; untreated pheochromocytoma; hypokalemia and hypomagnesemia; hypersensitivity to the drug and sulfonamides; a rare hereditary form of galactose intolerance, lactase deficiency or glucose-galactose malabsorption. For patients treated with sotalol (except for intensive drug treatment), intravenous administration of calcium antagonists such as verapamil or diltiazem or other antiarrhythmic drugs (such as disopyramide) is contraindicated.

Precautionary measures

Constant monitoring of heart rate, blood pressure, and ECG is required. Prescribed with caution in diabetes mellitus, pheochromocytoma, renal failure, in old age, psoriasis (including a history, including family), allergic reactions, as well as against the background of desensitizing therapy, diet, in the II–III trimester of pregnancy ( only for strict indications, stop taking 48–72 hours before birth). Alcohol intake should be avoided. Simultaneous intravenous administration of calcium channel blockers (verapamil, diltiazem) should be avoided. Use with caution while working for vehicle drivers and people whose profession involves increased concentration.

If the drug is discontinued, the dose should be reduced gradually.

Side effects of the drug Sotahexal

cardiovascular system: chest pain, undesirable decrease in blood pressure, increased symptoms of heart failure, bradycardia, tachycardia, ECG changes, impaired atrioventricular conduction, syncope or presyncope, edema; very rarely - increased frequency of angina attacks and impaired peripheral perfusion; proarrhythmic effects are possible - in the form of changes or intensification of arrhythmia (can lead to significant impairment of cardiac activity); arrhythmogenic effects (especially often noted in patients with life-threatening arrhythmia and impaired left ventricular function); ventricular tachyarrhythmia (sotalol hydrochloride prolongs the QT ); Gastrointestinal tract: taste disturbance, abdominal pain, nausea, vomiting, diarrhea, dyspepsia, xerostomia. Metabolic disorders: hypoglycemia; increase in total cholesterol and triglycerides, decrease in cholesterol in the HDL fraction. Nervous system: anxiety, confusion, sudden changes in mood, hallucinations, frequent dreams, depression, vertigo, headache, sleep disturbance, fever, feeling tired, paresthesia and cold sensations in the extremities. Hypersensitivity reactions: erythema, itching, exanthema; very rarely - alopecia, psoriasis-like exanthema or increased severity of psoriasis symptoms; anaphylactic reactions. Respiratory system: dyspnea; rarely - allergic bronchitis with fibrosis, temporary hearing loss. Visual organs: dysopia; rarely - conjunctivitis, keratoconjunctivitis, decreased severity of tear secretion. Musculoskeletal system: muscle spasm or myasthenia gravis.

Side effects

From the nervous system and sensory organs: dizziness, headache, feeling of fatigue, sleep disturbance, confusion, paresthesia, depression. Inflammation of the cornea and conjunctiva (should be taken into account when wearing contact lenses), blurred vision (extremely rare), decreased tear production.

From the cardiovascular system and blood (hematopoiesis, hemostasis): heart failure, bradycardia, AV block, angina pectoris (in rare cases), hypotension.

From the respiratory system: bronchospasm.

From the gastrointestinal tract: nausea, diarrhea, constipation, dry mouth.

Metabolism: hypoglycemia (more often in patients with diabetes mellitus or with strict adherence to a diet).

From the genitourinary system: decreased potency.

From the musculoskeletal system: a feeling of coldness in the extremities, muscle weakness or cramps.

From the skin: skin rash, itching (rare); redness, psoriasiform dermatosis, alopecia.

Special instructions for the use of the drug Sotahexal

Treatment with sotalol is carried out under the control of heart rate, blood pressure, and ECG. Constant medical monitoring of patients is necessary in the following cases:

in case of renal failure (it is necessary to monitor the concentrations of creatinine and sotalol hydrochloride in the blood serum at certain intervals);
in diabetes mellitus with significant fluctuations in blood glucose levels, while the symptoms of hypoglycemia can be masked (it is necessary to monitor the concentration of glucose in the blood);
while following strict diets;
with hyperthyroidism (in this case, adrenergic symptoms can be masked);
in case of peripheral perfusion disorders;
for pheochromocytoma (the drug can be used only after blockade of α-adrenergic receptors).

During the period of use of sotalol, patients who have suffered a myocardial infarction or patients with impaired myocardial contractility should be under the supervision of a cardiologist. When discontinuing the drug, the dose is reduced gradually; Particular care is taken when stopping treatment in patients with coronary artery disease and cardiac arrhythmias, as well as after prolonged use of the drug. The question of discontinuing or changing the dosage regimen of the drug in patients with life-threatening cardiac arrhythmias can only be decided by a doctor. Sotalol may increase sensitivity to allergens and increase the severity of anaphylactic reactions, which must be taken into account when treating patients with a history of severe hypersensitivity reactions and those on desensitization therapy. Severe proarrhythmia (sustained ventricular tachycardia, ventricular flutter/fibrillation), predominantly dose-dependent, is noted mainly at the beginning of therapy, as well as with increasing doses of the drug. In cases of severe diarrhea or concomitant use of drugs that cause loss of magnesium and/or potassium, it is necessary to monitor the electrolyte balance and acid-base balance. Since sotalol hydrochloride is found in urine, photometric determination of metanephrine may result in overestimated values. In patients who have taken sotalol, as well as with suspected pheochromocytoma, determination of metanephrine in urine should be carried out using the HPLC method with solid phase extraction. When treating elderly patients, it is necessary to take into account possible renal failure and make appropriate dose adjustments. Pregnancy and breastfeeding Since there is no experience with the use of sotalol during pregnancy, the drug can be prescribed during this period only with an accurate diagnosis and absolute indications for its use. It must be taken into account that sotalol hydrochloride crosses the placenta and reaches pharmacologically active concentrations in fetal tissues, as a result of which the fetus or infant may develop undesirable effects such as bradycardia, hypotension and hypoglycemia. For this reason, therapy should be interrupted 48–72 hours before the expected date of delivery. After birth, the child must be closely monitored for some time (beta receptor blockade may develop). Breastfeeding should be stopped during treatment with the drug. Effect on the ability to drive vehicles and other mechanisms The drug can change the body's reaction rate, which affects the ability to drive vehicles and other mechanisms, especially at the beginning of treatment.

Abrupt withdrawal of the drug After discontinuation of beta-blockers, patients experience increased sensitivity to catecholamines. Isolated cases of exacerbation of angina pectoris, the occurrence of arrhythmia, and, in some cases, the development of myocardial infarction after abrupt cessation of therapy have been reported. In this regard, if it is necessary to abruptly discontinue long-term therapy with Sotahexal, careful monitoring of the patient is recommended, especially with coronary heart disease. If possible, the dose should be reduced gradually over one or two weeks. If necessary, it is recommended to start replacement therapy. Abrupt cessation of drug use can provoke “hidden” coronary insufficiency, as well as the development of arterial hypertension. Proarrhythmia The most dangerous adverse reaction when using antiarrhythmic drugs is the exacerbation of existing arrhythmias or the provocation of new ones. Drugs that prolong the QT interval may cause torsade de pointes (TdP). The occurrence of such arrhythmias is associated with a prolongation of the QT interval, a decrease in heart rate, a decrease in serum potassium and magnesium, with high plasma concentrations of sotalol, as well as the simultaneous use of other drugs that prolong the QT interval. In women, these complications occur more often. The frequency of polymorphic ventricular tachycardia of the “pirouette” type is dose-dependent. This adverse reaction usually occurs early after the start of therapy or when the dose is increased, and stops spontaneously in most patients. At the same time, dose titration reduces the risk of proarrhythmia. Although in most cases polymorphic ventricular tachycardia of the torsade de pointes type is self-limiting and its symptoms coincide with other adverse reactions (for example, syncope), it can also develop into ventricular fibrillation. In clinical studies of patients with refractory ventricular tachycardia/ventricular fibrillation (VT/VF), the incidence of severe proarrhythmias (torsade de pointes or new-onset refractory VT/VF) was <2% at doses up to 320 mg. At higher doses, the incidence more than doubles. Other risk factors for torsade de pointes include significant prolongation of the QT interval with cardiomegaly or congestive heart failure. Patients with sustained ventricular tachycardia and congestive heart failure have the highest risk of serious proarrhythmias (7%). After previously administered antiarrhythmic therapy, the drug Sotahexal can be prescribed only under the condition of careful medical supervision and not earlier than after 2-3 half-lives of the previously prescribed antiarrhythmic drug. Proarrhythmic complications can occur not only at the start of therapy, but also with each dose increase. Starting therapy with 80 mg with a gradual increase can reduce the risk of developing proarrhythmia. The drug Sotahexal should be used with extreme caution when the QT interval lasts more than 480 msec, or the dose of the drug must be reduced; therapy should be discontinued when the QT interval exceeds 550 msec. Due to the risk of proarrhythmogenic effects, the use of the drug in patients with less severe (non-life-threatening) ventricular arrhythmias is not recommended, even if these rhythm disturbances are accompanied by symptoms that are unpleasant for the patient. The drug Sotagekal should not be used to treat ventricular extrasystole. Electrolyte disturbances Sotahexal should not be used in patients with uncorrected hypokalemia or hypomagnesemia, because Possible prolongation of the QT interval, as well as an increase in the risk of polymorphic ventricular tachycardia of the “pirouette” type. Particular attention should be paid to water-electrolyte balance and acid-base balance in patients with prolonged diarrhea or in patients taking drugs that reduce the level of potassium and magnesium in the blood plasma (diuretics). Congestive Heart Failure Beta-adrenergic receptor blockade may further reduce myocardial contractility and cause progression of heart failure symptoms. Therapy with Sotahexal should be started with caution and with a low dose in patients with impaired contractility of the left ventricular myocardium, controlled by therapy with ACE inhibitors, diuretics, cardiac glycosides, etc. Myocardial infarction Positive benefit/risk ratio of the use of sotalol in patients after a myocardial infarction with impaired left ventricular function has not been proven. Careful patient monitoring and dose titration are critical during initiation and continuation of therapy. Sotalol should not be used in patients with a left ventricular ejection fraction <40% without serious ventricular arrhythmias. ECG changes Excessive prolongation of the QT interval, more than 550 ms, may be a sign of drug toxicity. Sinus bradycardia was observed quite often in clinical studies in patients suffering from arrhythmia and taking sotalol. Bradycardia increases the risk of developing polymorphic ventricular tachycardia of the “pirouette” type. Sinus rhythm pauses, arrest, and sinus node dysfunction occurred in less than 1% of patients. The prevalence of second or third degree atrioventricular (AV) block is approximately 1%. Anaphylactoid reactions In patients using beta-blockers with a history of anaphylactic reactions to various allergens, more serious allergic reactions may occur upon repeated contact with the antigen. Such patients may not respond to the usual doses of epinephrine used to treat an allergic reaction. Anesthesia By analogy with other beta-blockers, Sotahexal should be used with caution in patients planning surgical treatment, as well as in combination with anesthetics that reduce myocardial contractility, such as cyclopropane or trichloroethylene. Diabetes mellitus Sotahexal should be used with caution in patients with diabetes mellitus or with a history of episodes of spontaneous hypoglycemia, since the use of beta-blockers may mask signs of the onset of acute hypoglycemia, for example, tachycardia. Thyrotoxicosis The use of beta-blockers may mask some clinical signs of hyperthyroidism (for example, tachycardia). Patients at risk of developing thyrotoxicosis require special attention due to the risk of increased symptoms of hyperthyroidism, up to the development of thyrotoxic crisis, against the background of cessation of the beta-blocking effect upon abrupt discontinuation of the drug. Impaired renal function Since sotalol is primarily eliminated by the kidneys, dosage adjustment is required in patients with impaired renal function. Serum creatinine and/or sotalol hydrochloride levels should be checked regularly. Impaired liver function Since the drug Sotahexal does not undergo first-pass metabolism, the clearance of the drug in patients with impaired liver function does not change. Psoriasis Beta blockers can initiate the development of psoriasis in some cases, aggravate symptoms or contribute to the appearance of psoriasiform exanthema. Beta blockers may accelerate the development of heart failure in patients with alcoholism. Use of the drug by athletes The use of the drug Sotahexal may cause positive results in doping tests. Elderly Elderly patients should use Sotahexal with caution. Effect on laboratory parameters The presence of sotalol in urine may lead to a false increase in the concentration of metanephrine in urine according to photometric methods. In patients with suspected pheochromocytoma, as well as in those taking sotalol, urine screening should be performed using HPLC (high performance liquid chromatography) with solid phase extraction. Other Use of the drug Sotahexal off-label is a potential health risk. Patients who use contact lenses should take into account that during sotalol therapy there may be a decrease in the production of tear fluid.

Drug interactions Sotahexal

Concomitant use with calcium antagonists (verapamil or diltiazem), other antiarrhythmic drugs (disopyramide), as well as beta-adrenergic receptor blockers, calcium ion antagonists (such as nifedipine) can lead to a significant decrease in blood pressure and heart rate. The intravenous administration of calcium ion antagonists such as verapamil or diltiazem, as well as other antiarrhythmic drugs (disopyramide), is contraindicated, with the exception of intensive care. Combination therapy with class I antiarrhythmic drugs (especially quinidine-like drugs) or other class III antiarrhythmic drugs can cause intense prolongation of the Q-T on the ECG and at the same time increase the risk of ventricular arrhythmia. Concomitant use with drugs that cause intense prolongation of QT on the ECG (tricyclic and tetracyclic antidepressants (imipramine, maprotiline), antihistamines (astemizole, terfenadine), quinolone antibiotics (for example, sparfloxacin), macrolide antibiotics (erythromycin), probucol, haloperidol and gelofantrine), leads to an increased risk of proarrhythmic effects (“flutter-flickering”). When used simultaneously with norepinephrine or MAO inhibitors, as well as after discontinuation of clonidine, blood pressure may increase sharply. When using SotaHexal simultaneously with β2-adrenergic receptor agonists, such as salbutamol, terbutaline and isoprenaline, it may be necessary to increase the dose of the latter. Concomitant use with tricyclic antidepressants, barbiturates, phenothiazines, narcotics, as well as antihypertensive drugs, diuretics and vasodilators can lead to a sharp decrease in blood pressure. The negative chronotropic and dromotropic effects of sotalol may be enhanced by concomitant administration of reserpine, clonidine, alpha-methyldopa, ganfacine and cardiac glycosides. The neuromuscular blockade caused by tubocurarine can be increased by β-adrenergic receptor blockade. Concomitant use with insulin or oral antibiotics, especially during strenuous exercise, may induce hypoglycemia and mask its symptoms. The risk of arrhythmia increases with the simultaneous administration of potassium-sparing diuretics (furosemide, hydrochlorothiazide) or other drugs, the use of which causes a loss of potassium or magnesium.

Interaction

When used together with antiarrhythmics IA (especially quinidine type) and class III, the risk of developing ventricular arrhythmias and prolongation of the QT interval increases; with tricyclic antidepressants, barbiturates, phenothiazines, calcium antagonists and narcotic, antihypertensive, diuretic and vasodilating agents - dangerous hypotension and weakness of the sinus node; with norepinephrine or MAO blockers - hypertension; with reserpine, clonidine, alpha-methyldopa, guanfacine and cardiac glycosides - bradycardia or AV block; with potassium-removing diuretics - arrhythmia caused by hypokalemia. Enhances the hypoglycemic effect of insulin and oral hypoglycemic agents.

Overdose of the drug Sotahexal, symptoms and treatment

symptoms: loss of consciousness, dilated pupils, convulsions, severe bradycardia up to asystole, severe arterial hypotension, bronchospasm, decompensated heart failure, as well as atypical ventricular tachycardia (flutter - fibrillation) and symptoms of cardiovascular shock. Treatment: symptomatic. In addition to the general determination of the primary elimination of a substance, in conditions of intensive treatment it is necessary to monitor vital parameters and, if necessary, make appropriate adjustments. Atropine 1–2 mg is administered intravenously as an infusion (bolus); beta-sympathomimetics depending on body weight and effect: dopamine, dobutamine, isoprenaline, orciprenaline and epinephrine; The use of glucagon is effective: initially 1–10 mg IV, then 2.0–2.5 mg/hour as a continuous infusion. Refractory bradycardia should be treated with a temporary pacemaker.