Description
Latin name
Sotalol Canon
Sotalol Canon Tablet Release Form.
packaging 10 pcs – blister packs (2) – packs of cardboard.
Pharmacological action
Beta1-, beta2-blocker. Sotalol is a non-selective -Adrenoreceptor blocker that acts on both 1- and 2 receptors without its own sympathomimetic and membrane-stabilizing activity.
Like other beta-blockers, sotalol inhibits the secretion of renin, and this effect is pronounced both at rest and during exercise. The beta-adrenergic blocking effect of the drug causes a decrease in heart rate (negative chronotropic effect) and a limited decrease in heart rate (negative inotropic effect). These changes in heart function reduce myocardial oxygen demand and heart load.
The antiarrhythmic properties of sotalol are associated with both blockade of -adrenoreceptors and the ability to prolong the myocardial action potential. 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. On an ECG taken in standard leads, properties corresponding to class II and III of antiarrhythmic drugs can be reflected in the form of lengthening of PR intervals, QT and QTc (QT with heart rate correction) in the absence of noticeable changes in the duration of the QRS complex.
Pharmacokinetics
Absorption
Oral bioavailability is almost complete (over 90%). Cmax in blood plasma is reached 2.5-4 hours after ingestion. The absorption of the drug is reduced by approximately 20% with food compared with fasting. In the range of doses from 40 to 640 mg / day, the concentration of sotalol in the blood plasma is proportional to the dose taken.
Distribution of
Does not bind to plasma proteins. It is distributed in plasma, as well as in peripheral organs and tissues. Css is reached within 2-3 days. It penetrates poorly through the BBB, and the concentration in the cerebrospinal fluid is only 10% of the concentration in the blood plasma.
Metabolism
Not metabolized. The pharmacokinetics of the d- and l-enantiomers of sotalol is almost the same.
Excretion
The main route of excretion from the body is through the kidneys. From 80 to 90% of the administered dose is excreted unchanged by the kidneys, and the rest through the intestines. T1 / 2 is 10-20 hours.
Pharmacokinetics in special patient groups
Patients with impaired renal function should be prescribed lower doses of the drug.
With age, the pharmacokinetics do not change significantly, although impaired renal function in elderly patients reduces the elimination rate, which leads to an increased accumulation of the drug in the body.
Indications
prophylaxis of paroxysmal atrial tachycardia, paroxysmal atrioventricular recurrent tachycardia of the re-enter type, paroxysmal atrioventricular recurrent tachycardia based on additional pathways and Wolf-Parkinson-White Syndrome
maintaining a normal sinus rhythm after stopping atrial fibrillation or atrial flutter
treatment of symptomatic unstable ventricular tachyarrhythmias and symptomatic premature ventricular contractions
treatment of high blood levels caused by high or low blood pressure.
Contraindications
decompensated chronic heart failure
cardiogenic shock
AV block II and III degree
sinoatrial blockade
SSSU
acquired tachycardia type pirouette srdlrdp minor bronchial asthma or COPD
pheochromocytoma without the simultaneous administration of alpha-blockers
renal failure (CC less than 10 ml / min)
general anesthesia using medication tv, causing suppression of myocardial function (e.g. cyclopropane or trichlorethylene)
arterial hypotension (systolic blood pressure less than 90 mmHg)
severe peripheral circulatory disorders, including Raynaud’s syndrome
metabolic acidosis
simultaneous use of MAO inhibitors
lactation period
age up to 18 years (efficacy and safety not established)
hypersensitivity to sotalol or other components of the drug and sulfonamide derivatives.
With caution, the drug should be prescribed to patients who have recently had myocardial infarction, with diabetes mellitus, psoriasis, patients with impaired renal function, with AV blockade of the first degree, impaired water-electrolyte balance (hypomagnesemia, hypokalemia), thyrotoxicosis, depression (i.e. hours in the anamnesis), pheochromocytoma (with concomitant use with alpha-blockers), aggravated allergic history, elderly patients.
Use during pregnancy and lactation
Use of the drug Sotalol Canon during pregnancy, especially in the first 3 months, is possible only for vital indications after a careful assessment of the ratio of all risk factors.
In the case of therapy during pregnancy, the drug should be discontinued 48-72 hours before the expected date of delivery due to the possibility of developing bradycardia, arterial hypotension, hypokalemia and respiratory depression in newborns.
Sotalol passes into breast milk and reaches effective concentrations there. If necessary, the appointment of the drug during lactation, breastfeeding should be discontinued.
Composition
1 tablet contains:
Active ingredient:
sotalol hydrochloride – 160 mg
Excipients:
calcium hydrogen phosphate dihydrate – 118 mg,
silicon dioxide colloidal (Aerosil) – 1 mg,
croscarmellose sodium – 12 mg,
mannitol – 56.8 mg,
povidone – 8.6 mg,
magnesium stearate – 3.6 mg .
Dosage and administration
The drug is taken orally 1-2 hours before a meal.
At the beginning of treatment, it is recommended to prescribe 160 mg / day in 2 divided doses (after about 12 hours). This dose can be increased if necessary after an appropriate clinical assessment of the patient’s condition to 240 or 320 mg / day. In most patients, the therapeutic response is achieved with the use of the drug in a total daily dose of 160-320 mg, divided into 2 doses.
Some patients with life-threatening refractory ventricular arrhythmia may require up to 480-640 mg / day, however, such doses can only be prescribed in cases where the potential benefit outweighs the risk of side effects, especially proarrhythmogenic effects.
In patients with cardiomyopathy, chronic heart failure, with angina pectoris, arterial hypertension, conditions after myocardial infarction, it is recommended to begin treatment in a hospital. The initial dose is 160 mg / day in 1 or 2 doses. After a week, the dose can be increased if necessary by 80 mg / day (1 tab. 80 mg or 1/2 tab. 160 mg) at weekly intervals. The rate of dose increase depends on the tolerability of the drug to patients, which, in particular, is assessed by the degree of bradycardia induced and the clinical response. Due to the relatively long T1 / 2 in most patients, sotalol is effective when taken 1 time / day. Dose interval: 160-320 mg / day.
Patients with impaired renal function
Since sotalol is excreted mainly in the urine, T1 / 2 increases in the presence of renal failure, the dose should be reduced at a serum creatinine level of more than 120 μmol / L in accordance with the following recommendations: serum creatinine
Recommended dose
µmol / l mg / dl
less than 120 Typical dose
120-200 1.20-3 / 4 normal dose
200-300 2.3-1 / 2 normal dose
300-500 3. 4-1 / 4 of the usual dose of
Side effects
Sotalol is usually well tolerated. Side effects are transient and in rare cases require interruption or discontinuation of treatment.
From the side of the nervous system: dizziness, headache, sleep disturbance (drowsiness or insomnia), depression, paresthesia in the extremities, anxiety, emotional lability, depression, tremor.
From the side of the organ of vision: visual impairment.
On the part of the hearing organ: hearing impairment.
From the cardiovascular system: bradycardia, chest pain, shortness of breath, ECG changes, palpitations, arterial hypotension, arrhythmogenic effect, heart failure, peripheral edema, fainting.
From the digestive system: nausea, vomiting, dyspepsia, diarrhea, abdominal pain, flatulence, violation of taste sensations.
From the genitals and mammary gland: decreased potency.
From the musculoskeletal system: cramps.
Allergic reactions: urticaria, skin rash.
Common disorders: fever, feeling tired, asthenia.
On the part of laboratory and instrumental data: overestimated results may be observed with the photometric analysis of urine for methanephrine (O-methyladrenaline).
If pheochromocytoma is suspected, the urine of patients should be examined using high performance liquid chromatography with solid phase extraction.
Drug Interaction
Concurrent administration of sotalol with class IA antiarrhythmic agents (disopyramide, quinidine, procainamide) and class III drugs (eg, amiodarone) may cause QT prolongation.
The use of potassium-lowering diuretics can lead to hypokalemia or hypomagnesemia, which increases the likelihood of pirouette arrhythmias.
Sotalol should be used with extreme caution in combination with other QT-prolonging agents such as class I antiarrhythmic agents, phenothiazines, tricyclic antidepressants, terfenadine and astemizole, as well as some quinolone antibiotics.
Concurrent use of beta blockers and slow calcium channel blockers can lead to arterial hypotension, bradycardia, conductivity disorders, and heart failure. The use of beta-blockers in combination with blockers of slow calcium channels that suppress myocardial function (eg, verapamil and diltiazem) should be avoided due to the additive effect of these agents on AV conductance and ventricular function.
Concomitant use of catecholamine depleting agents (eg, reserpine and guanitidine), together with beta-blockers, leads to an excessive decrease in the sympathetic nervous system tone at rest. Patients should be closely monitored for possible signs of decreased blood pressure and / or severe bradycardia, which may result in fainting.
Hyperglycaemia may develop with concomitant administration with insulin and hypoglycemic agents. In this case, it is necessary to adjust the dose of hypoglycemic agents. Sotalol may mask the symptoms of hypoglycemia.
When administered concurrently with sotalol, it may be necessary to administer beta2-adrenomimetics, such as salbutamol, terbutalin, and isoprenaline, at higher doses.
The use of sotalol does not have a noticeable effect on the concentration of digoxin in the serum. Arrhythmogenic activity was observed more frequently in patients receiving sotalol concomitantly with digoxin, however, this may be associated with chronic heart failure, which is a risk factor for arrhythmogenic action in patients receiving digoxin.
Beta-blockers can potentiate arterial hypertension of withdrawal after discontinuation of clonidine. Therefore, beta-blockers should be discontinued gradually, several days before the gradual discontinuation of clonidine.
Beta-blockers cause a decrease in compensatory cardiovascular responses in the event of shock or hypotension due to floctafenin.
The use of inhalation anesthesia, including tubocurarin, against the background of taking sotalol increases the risk of myocardial function suppression and the development of arterial hypotension.
Potassium concentration should be monitored when used with amphotericin B and GKS.
Co-administration with laxatives is not recommended.
Overdose
Symptoms: bradycardia, chronic heart failure, exacerbation of chronic heart failure, excessive reduction of blood pressure, bronchospasm, hypoglycemia.
Treatment: gastric lavage, administration of activated charcoal for disorders of AV-conductivity is injected into / in 1-2 mg of atropine, with low efficiency set a temporary pacemaker with bronchospasm – inhalation or parenteral beta-adrenomimetic in reducing blood pressure is effective epinephrine.
Storage conditions
The drug should be stored out of the reach of children, in a dry, dark place at a temperature of no higher than 25 ° C.
Expiration
2 years.
Active substance
Sotalol
Pharmacy terms
Prescription
Canonfarma, Russia
