Sotageksal

General characteristics. Structure:

Active agents: 80 or 160 mg of a sotalol of a hydrochloride.

Excipients: lactoses monohydrate, starch corn, hypro rod, carboxymethylstarch of sodium, silicon dioxide colloid, magnesium stearate.

Pharmacological properties:

Sotalol represents a non-selective blocker β adrenergic receptors, acting both on β1, and on β2 receptors and not having own sympathomimetic activity (SMA) and membrane stabilizing activity (MSA). It is similar to others a beta to adrenoblockers, соталол suppresses secretion of a renin, and this effect has the expressed character as at rest, and at loading.
β adrenoceptor blocking effect of drug causes decrease in heart rate (negative chronotropic effect) and limited decrease in force of cordial reductions (negative inotropic effect). These changes of function of heart reduce the need of a myocardium for oxygen and volume of load of heart.
Antiarrhytmic properties of a sotalol are connected as with ability to blockade a beta of adrenergic receptors, and with ability to prolongation of action potential of a myocardium. The main effect of a sotalol consists in increase in duration of the effective refractory periods in atrial, ventricular and additional ways of carrying out an impulse.

Pharmacokinetics. Bioavailability at intake is almost full (more than 90%). The maximum concentration in a blood plasma is reached in 2,5 4 hours after intake, and equilibrium concentration within 2 3 days. Absorption of drug decreases approximately by 20% at meal in comparison with reception on an empty stomach. In a dose interval from 40 to 640 mg/day concentration of a sotalol in a blood plasma is proportional to the accepted dose. Distribution happens in plasma, and also in peripheral bodies and fabrics, and the elimination half-life makes 10 20 hours.
Sotalol does not contact proteins of a blood plasma and is not exposed to metabolism. The pharmacokinetics of d-and l of enantiomer of a sotalol is almost identical.
Badly gets through a blood-brain barrier, and its concentration in cerebrospinal fluid makes only 10% of concentration in a blood plasma.
The main way of removal from an organism is renal elimination. From 80 to 90% of the entered dose are allocated in not changed view with urine, and other part with a stake.
Patients with an impaired renal function should appoint smaller doses of drug. With age the pharmacokinetics changes slightly though the renal failure at elderly patients reduces allocation speed that leads to the increased accumulation of drug in an organism.

Indications to use:

Symptomatic and chronic disturbances of a cordial rhythm:

- ventricular tachycardia, including supraventricular tachycardia at Wolf's syndrome – Parkinson Whyte;
- ventricular premature ventricular contraction;
- paroxysmal form of atrial fibrillation.

Route of administration and doses:

Drug is accepted inside in 1-2 hours prior to food, without chewing, washing down with enough liquid.
The concomitant use of food (especially milk and dairy products) reduces drug absorption.
The dose of drug is selected individually depending on disease severity and reaction of the patient to treatment.
The initial dose makes 80 mg (1 tablet of Sotageksal) a day. At insufficiency of expressiveness of therapeutic effect the dose can be gradually increased to 240-320 mg a day, divided into 2-3 receptions. At most of patients the therapeutic effect is reached on the general daily dose of 160-320 mg divided into 2 receptions.
At life-threatening heavy arrhythmias increase in a dose as much as possible to 6 tablets of Sotageksal (480 mg of a sotalol) divided into 2 or 3 separate receptions is possible. However it is only possible to appoint such doses when the potential advantage outweighs risk of development of side effects, especially proaritmogenny action.
Patients with a renal failure have a risk of development of cumulation therefore they need to control the size of clearance of creatinine and heart rate (not lower than 50 beats per minute).
As соталол it is allocated from an organism mainly through kidneys, and the period of its semi-removal increases in the presence of a renal failure, a dosage of drug it is necessary to reduce at blood serum creatinine level more than 120 µmol/l according to the following recommendations:

Blood serum creatinine		The recommended dose
µmol/l	mg/dl
<120	<1,2	Usual dose
120-200	1,20 - <2,3	3/4 usual doses
200-300	2,3 - <3,4	1/2 usual doses
300-500	3,4 - <5,7	1/4 usual doses

At a heavy renal failure it is necessary to carry out regular control of an ECG and level of concentration of drug in blood serum.
Duration of therapy is defined by the attending physician.
If you forgot to take a pill in time, the following time it is not necessary to accept additional amount of drug, it is necessary to accept only the appointed Sotageksal's number.

Features of use:

It is necessary to be careful at Sotageksal's appointment to patients

- at a diabetes mellitus in the anamnesis with the expressed fluctuations of level of glucose in blood, and also at observance of rigid diets;
- at a pheochromocytoma (co-administration an alpha – adrenoblockers is necessary);
- in the presence in the anamnesis or the family anamnesis of psoriasis;
- at a renal failure;
- advanced age.

Side effects:

Warmly – vascular system:
bradycardia, short wind, retrosternal pain, heartbeat, AV blockade, strengthening of symptoms of heart failure, heartbeat, hypostases, a faint, aritmogenny action, decrease in the ABP, in rare instances – strengthening of attacks of stenocardia.

Zheludochno – an intestinal path:
nausea, vomiting, diarrhea, lock, dryness in a mouth, an abdominal pain, a meteorism.

Central nervous system:
the headache, dizziness, increased fatigue, condition of depression, feeling of alarm, change of mood, tremor, adynamy, sleep disorder are possible: drowsiness or sleeplessness, a depression, paresthesias in extremities.

From sense bodys:
Vision disorders, inflammation of a cornea and conjunctiva (it is necessary to consider when carrying contact lenses), reduction of a slezootdeleniye, hearing disorder, flavoring feelings.

Metabolism:
Hypoglycemia (it is the most probable at patients with a diabetes mellitus, or at strict observance of diets).

Laboratory indicators:
The overestimated results results can be observed in the fotometichesky analysis of urine on метанефрин (O-metiladrenalin).

Respiratory system:
Bronchospasm (especially at disturbance of lung ventilation).

Urinogenital system:
Decrease in a potentiality.

Integuments:
Skin rash, itch, reddening, psoriazoformny dermatosis, alopecia, small tortoiseshell.

Others:
Cold snap of extremities, muscular weakness, spasms, fever.

Interaction with other medicines:

At a concomitant use of blockers of "slow" calcium channels like verapamil and diltiazem decrease in size ABP as a result of deterioration in contractility is possible.
It is necessary to avoid intravenous administration of these drugs against the background of use of a sotalol (except for cases of urgent medicine).
The combined use of antiarrhytmic means of the class IA (especially hinidinovy type: Disopyramidum, quinidine, procaineamide), or a class III (for example, Amiodaronum) can cause the expressed lengthening of an interval of QT.
The drugs increasing QT interval duration: it is necessary to apply with care with drugs. QT extending an interval, such as antiarrhytmic means of the I class, fenotiazina, tricyclic antidepressants, терфенадин and астемизол, and also some antibiotics of a hinolonovy row.
At a concomitant use of nifedipine and other derivative 1,4 dihydropyridines decrease in size ABP is possible.
Co-administration of noradrenaline or MAO inhibitors, and also sharp cancellation of a clonidine can cause arterial hypertension. In this case cancellation of a clonidine should be carried out gradually and only in several days after the end of reception of Sotageksal.
Tricyclic antidepressants, barbiturates, fenotiazina, narcotic and anti-hypertensive means, diuretics and vazodilatator can cause sharp decrease in the ABP.
Use of means for an inhalation anesthesia, including tubocurarine against the background of Sotageksal's reception increases risk of oppression of function of a myocardium and development of arterial hypotension.
At simultaneous use of Sotageksal with Reserpinum, a clonidine, alpha метилдопой, guanfatsiny and cardiac glycosides development of the expressed bradycardia and delay of carrying out excitement in heart is possible.
Beta adrenoblockers can exponentiate arterial hypertension of cancellation, after the termination of reception of a clonidine; therefore beta adrenoblockers should be cancelled gradually, some days before the gradual termination of reception of a clonidine.
Purpose of insulin or other peroral hypoglycemic means, in particular, at an exercise stress, can lead to strengthening of a hypoglycemia and manifestation of its symptoms (the increased perspiration, the speeded-up pulse, a tremor). At a diabetes mellitus correction of doses of insulin, and/or gipoglikemiziruyushchy drugs is necessary.
Kaliyvyvodyashchy diuretics (e.g., furosemide, a hydrochlorothiazide) can provoke developing of the arrhythmia caused by a hypopotassemia.
Stimulators of beta2-receptors. At simultaneous use with Sotageksal use of higher doses of beta-agonists, such as salbutamol, тербуталин and изопреналин can be required.

Contraindications:

- Hypersensitivity to a sotalol, sulfonamides and to other components of drug;
- Chronic heart failure of the II B – the III stage;
- Cardiogenic shock;
- Atrioventricular block of II or III degrees;
- Sinuatrial blockade
- Sick sinus syndrome;
- The expressed bradycardia (heart rate less than 50 уд. / min.);
- The inborn or acquired syndrome of the extended QT interval;
- Arterial hypotension (the systolic arterial pressure (AP) is less than 90 mm hg);
- Obliterating diseases of vessels;
- Bronchial asthma or chronic obstructive pulmonary disease (COPD);
- Metabolic acidosis;
- A pheochromocytoma without co-administration of alpha adrenoblockers;
- Acute myocardial infarction;
- Renal failure (clearance of creatinine less than 10 ml/min.)
- The general anesthesia causing suppression of function of a myocardium (for example, cyclopropane or trichloroethylene)
- Tachycardia like "pirouette"
- Heavy allergic rhinitis
- Concomitant use of inhibitors of a monoaminooxidase (MAO)
- Lactation period
- Age up to 18 years (efficiency and safety are not established).

It is necessary to be careful at Sotageksal's appointment to the patients who recently had a myocardial infarction at a diabetes mellitus, psoriasis, a renal failure, an atrioventricular block of the I degree, at disturbance of water and electrolytic balance: hypomagnesiemia, hypopotassemia; at a thyrotoxicosis, a depression (including in the anamnesis), when lengthening an interval of QT, at advanced age.
With extra care apply at instructions in the anamnesis on allergic reactions, and also against the background of performing the desensibilizing therapy since соталол suppresses sensitivity to allergens.
Pregnancy and period of feeding by a breast
Sotageksal's reception during pregnancy, especially, in the first 3 months. it is possible only according to zhiznennovazhny indications and at a careful ratio of all risk factors.
In case of performing therapy at pregnancy, administration of drug should be cancelled in 48 - 72 hours prior to the estimated term of childbirth because of a possibility of development of bradycardia, arterial hypotension, a hypopotassemia and respiratory depression at newborns.
Sotalol gets into breast milk and reaches effective concentration there. In need of purpose of drug during feeding by a breast, breastfeeding needs to be stopped.

Overdose:

Symptoms:
Decrease in the ABP, bradycardia, bronchospasm, hypoglycemia, loss of consciousness, generalized convulsive attacks, ventricular tachycardia; in hard cases – symptoms of cardiogenic shock, an asystolia.
Treatment:
Gastric lavage, hemodialysis, purpose of absorbent carbon. Symptomatic therapy: atropine – 1 – 2 time intravenously struyno; a glucagon – at first in the form of short intravenous infusion in a dose of 0,2 mg/kg of body weight, then in a dose of 0,5 mg/kg of body weight intravenously infusion within 12 hours.

Storage conditions:

At a temperature not above 25 °C!
To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Tablets on 80 or 160 mg.
On 10 tablets in the blister from polyvinylchloride and aluminum foil.
On 1, 2, 3, 5 or 10 blisters in a cardboard pack with the application instruction.