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Active ingredients
Sotalol
Release form
Pills
Composition
Active ingredient: Sotalol hydrochloride Concentration of active ingredient (mg): 160
Pharmacological effect
Beta1-, beta2-adrenergic blocker. Sotalol is a non-selective blocker of β1-, β2-adrenoreceptors, which does not have its own sympathomimetic and membrane-stabilizing activity. Like other beta-blockers, sotalol inhibits renin secretion, and this effect is pronounced both at rest and during exercise. Beta-adrenoceptor 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 volume of the load on the heart. The antiarrhythmic properties of sotalol are associated with both the blockade of β-adrenoreceptors and the prolongation of the action potential 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 conducting an impulse.
Pharmacokinetics
AbsorptionBioavailability when administered orally is almost complete (more than 90%). Cmax in plasma is reached 2.5-4 hours after ingestion. The absorption of the drug is reduced by approximately 20% when eating compared with fasting. In the dose range from 40 to 640 mg / day, the concentration of sotalol in the 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. It penetrates badly through BBB, and its concentration in the cerebrospinal fluid is only 10% of the concentration in the blood plasma. Metabolism Does not undergo metabolism. The pharmacokinetics of the d- and l-enantiomers of sotalol are almost the same. InjectionThe main way of excretion 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 is excreted. T1 / 2 is 10-20 hours. Pharmacokinetics in special clinical situations Patients with impaired renal function should be given lower doses of the drug. Pharmacokinetics change slightly with age, although renal impairment in elderly patients decreases the excretion rate, which leads to an increased accumulation of the drug in the body.
Indications
Supraventricular tachyarrhythmia: nodal tachycardia, WPW tachycardia, paroxysmal atrial fibrillation; ventricular tachycardia, ventricular premature beats.
Contraindications
Hypersensitivity (including sulfonamides), chronic heart failure stage IIb-III, shock, AV blockade II-III degree, sinoatrial blockade, sick sinus syndrome, bradycardia, prolongation of the QT interval, hypokalemia, hypotension, severe peripheral circulatory disorders , obstructive diseases of the respiratory tract (including bronchial asthma), metabolic acidosis, laryngeal edema, myasthenia gravis, severe allergic rhinitis.
Precautionary measures
Caution should be exercised in appointing Sotahexal to patients who have recently suffered a myocardial infarction, in diabetes mellitus, psoriasis, renal dysfunction, AV degree I-blockade, in violation of the water-electrolyte balance (hypomagnesaemia, hypokalemia), thyrotoxicosis, depression ( and history), with prolongation of the QT interval, elderly patients. With extreme caution is used with instructions in the history of allergic reactions, as well as during desensitization therapy, because Sotalol inhibits sensitivity to allergens.
Use during pregnancy and lactation
Reception of Sotahexal during pregnancy, especially in the first 3 months, is possible only according to vital indications and with a careful ratio of all risk factors. In the case of therapy during pregnancy, the drug should be discontinued 48-72 hours before the expected due date of childbirth bradycardia, hypotension, hypokalemia and respiratory depression in newborns. Sotalol penetrates into breast milk and reaches effective concentrations there. If necessary, the appointment of the drug during lactation, breastfeeding should be stopped.
Dosage and administration
Sotahexal accept inside, before food, without chewing, washing down with enough liquid, on 80-120 mg / days. in 2-3 doses. With a lack of effectiveness - up to 160-240-320 mg / day. in 2-3 doses. With severe arrhythmias - up to 480 mg / day. in 2-3 doses. Increasing the dose should be carried out at intervals of 2-3 days.
Side effects
From the nervous system and sensory organs: dizziness, headache, fatigue, sleep disturbance, confusion, paresthesia, depression. Inflammation of the cornea and conjunctiva (should be considered when wearing contact lenses), blurred vision (extremely rare), decreased tearing. From the cardiovascular system and blood (hematopoiesis, hemostasis): heart failure, bradycardia, AV blockade, angina (in rare cases ), hypotension. For the respiratory system: bronchospasm. For the digestive tract: nausea, diarrhea, constipation, dry mouth. For metabolism: hypoglycemia (often in diabetic patients or with strict diet). howl system: reduction potentsii.So the musculoskeletal system: the feeling of a cold snap in the extremities, muscle weakness or sudorogi.So the skin: skin rash, pruritus (uncommon); redness, psoriasis dermatosis, alopecia.
Overdose
Symptoms: decreased blood pressure, bradycardia, bronchospasm, hypoglycemia, loss of consciousness, generalized seizures, ventricular tachycardia; in severe cases, symptoms of cardiogenic shock, asystole. Treatment: gastric lavage, hemodialysis, the appointment of activated carbon. Symptomatic therapy: atropine - 1-2 times w / w jet; glucagon - first as 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 in infusion for 12 hours.
Interaction with other drugs
At the same time taking blockers of slow calcium channels such as verapamil and diltiazem, a decrease in blood pressure is possible as a result of worsening contractility. It should be avoided in / in the introduction of these drugs with the use of sotalol (except for emergency medicine). The combined use of class IA antiarrhythmic drugs (especially of the quinidine type: disopyramide, quinidine, procainamide) or class III (eg, amiodarone) can cause a pronounced lengthening of the interval QT. 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 antiarrhythmic drugs, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, as well as some quinolone antibiotics. When used simultaneously with nifedipine and other derivatives 1 , 4-dihydropyridine may decrease the value of blood pressure. Simultaneous administration of norepinephrine or MAO inhibitors, as well as abrupt withdrawal of clonidine can cause arterial hypertension.In this case, the withdrawal of clonidine should be carried out gradually and only a few days after the end of Sotahexal administration. Tricyclic antidepressants, barbiturates, phenothiazines, opioid and antihypertensive drugs, diuretics, and vasodilators can cause a sharp decrease in blood pressure. Use of agents for inhalation anesthesia, including. tubocurarine while taking Sotahexal increases the risk of inhibition of myocardial function and development of arterial hypotension. With simultaneous use of Sotahexal with reserpine, clonidine, alpha methyldopa, guanfacine and cardiac glycosides, it is possible to develop pronounced bradycardia and slow the onset of arousal in the heart. cancellation, after discontinuation of clonidine, therefore, beta-blockers should be abolished gradually, a few days before eniya receiving klonidina.Naznachenie insulin or other oral hypoglycemic agents, especially during exertion, can lead to increased expression of hypoglycemia and its symptoms (sweating, increased heart rate, tremor). In diabetes mellitus, dosage adjustment of insulin and / or hypoglycemic drugs is necessary. Calcic diuretics (for example, furosemide, hydrochlorothiazide) can cause the occurrence of arrhythmia caused by hypokalemia. and isoprenaline.
special instructions
Caution should be exercised in the appointment of Sotahexal patients: with diabetes in history with severe fluctuations in blood glucose levels, as well as with strict diet; with pheochromocytoma (simultaneous administration of alpha-blockers is necessary); in the presence of a history or a family history of psoriasis; in violation of renal function; elderly. The drug treatment is carried out under the control of heart rate, blood pressure, ECG. With a pronounced decrease in blood pressure or a decrease in heart rate, the daily dose should be reduced. Patients with impaired renal function require correction of the dosing regimen. The withdrawal of Sotahexal should be made under the supervision of a doctor and gradually (especially after long-term use). Cogexal should not be used in patients with hypokalemia or hypomagnesemia before correction of existing violations.These conditions can increase the degree of prolongation of the QT interval and increase the likelihood of arrhythmias such as pirouette. 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 a decrease in magnesium and / or potassium in the body. During thyrotoxicosis, sotalol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt cancellation in patients with tiretoksikozom contraindicated because it can enhance the symptoms of the disease. When prescribing beta-adrenergic blockers in patients receiving hypoglycemic agents, caution should be exercised, because during long breaks in the meal, hypoglycemia may develop, and its symptoms such as tachycardia or tremor may develop may be masked by the action of the drug.