Sotalol Sandoz of the tab. of 80 mg No. 50

Pharmacological properties

Pharmacodynamics. sotalol sandoz — a non-selective blocker of β-adrenoceptors which works on β1 — and β2-адренорецепторы. has the significant antiarrhytmic action which mechanism consists in increase in duration of action potential and the refractory period on all sites of the carrying-out system of heart (iii a class of antiarrhytmic drugs). reduces chss and contractility of a myocardium, reduces automatism of sinus node, slows down av-conductivity. blocking β2-адренорецепторы, raises a tone of unstriated muscles of bronchial tubes, vessels.

Pharmacokinetics. After oral administration of 75-90% of a sotalol of a hydrochloride it is absorbed in a digestive tract. Owing to lack of effect of primary hepatic passing the bioavailability is 75–90%. Time of achievement of the C _max in blood plasma — 2–3 h. Distribution volume — 1.6-2.4 l/kg. Sotalol does not contact proteins of blood plasma. 75–90% of the accepted dose are removed by kidneys in not changed look, the rest — with a stake. The renal clearance is 120 ml/min. of T _½ — 10–20 h. In a renal failure it increases to 42 h that demands a medicament dose decline. Drug is removed at a hemodialysis.

Indication

Heavy symptomatic ventricular disturbances of a warm rhythm.

Symptomatic supraventricular arrhythmias as tachycardia demanding treatment:

• prevention of chronic fibrillation of auricles after cardiostimulation by a direct current;
• prevention of paroxysmal fibrillation of auricles.

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Use

At treatment by antiarrhytmic means of ventricular arrhythmias, life-threatening to begin therapy and also it is necessary to raise doses in the conditions of a hospital in the presence of the equipment for monitoring and assessment of variability of a warm rhythm.

during treatment needs to conduct control researches with regular intervals (for example by means of the standard ECG at an interval of 1 month or long the ECG each 3 months and in case of need — the ECG at loading).

Therapy should be reconsidered if separate parameters worsen, for example, duration of QRS increases or Q–T interval for more than 25% is extended, P–Q interval for more than 50% is extended or the frequency and weight of arrhythmias increases.

Heavy symptomatic ventricular disturbances of a warm rhythm. An initial dose — 80 mg of the medicament Sotalol Sandoz 2 times a day. If the efficiency of therapy is insufficient, it is possible to raise a dose to 80 mg of a sotalol of a hydrochloride 3 times a day or to 160 mg of a sotalol of a hydrochloride 2 times a day.

in case of insufficient efficiency at treatment of arrhythmias, life-threatening the patient, the daily dose of a sotalol of a hydrochloride can be increased up to 480 mg and is distributed on 2–3 receptions.

Purpose of such dose demands assessment of a ratio of potential advantage and risk of emergence of heavy side reactions (especially pro-arrhythmic effects).

Dose is recommended to be raised with an interval of not less than 2-3 days.

Fibrillation of auricles. The initial dose of a sotalol of a hydrochloride makes 80 mg 2 times a day. In case of insufficient efficiency it is possible to raise a daily dose to 80 mg 3 times a day. This dose should be exceeded in case of paroxysmal fibrillation of auricles.

in case of insufficient efficiency to patients with a chronic form of fibrillation of auricles can increase a dose to the maximum 160 mg 2 times a day.

Dose is recommended to be raised with an interval of not less than 2-3 days.

Recommended doses in a renal failure. As there is a risk of accumulation of a sotalol against the background of repeated reception at patients with renal failures, such patients should korrigirovat a dose depending on clearance of creatinine, considering ChSS (not lower than 50 ud. / mines) and clinical performance.

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In a heavy renal failure recommends use of a sotalol of a hydrochloride only at regular control of the ECG and concentration of medicament in blood plasma.

If clearance of creatinine of 60 ml/min., are appointed by the recommended doses; at clearance of creatinine of 30-60 ml/min. the dose decline for 50% is recommended; at clearance of 10-30 ml/min. apply ¼ recommended doses; at clearance of creatinine of 10 ml/min. medicament is not used.

Patients of advanced age. For treatment of patients of advanced age it is necessary to consider possible renal failures.

Route of administration. A pill should be taken without chewing, washing down with enough liquid (for example 1 glass of water), to food. The medicament should not be taken at meal time as at the same time absorption of a sotalol of a hydrochloride in a digestive tract can be reduced (in particular, it concerns some milk and dairy products).

use Duration. Duration of treatment is determined by the doctor.

to the Patients who had a myocardial infarction or with heavy disturbances of warm activity constant careful medical control is necessary for

during dose adjustment of antiarrhytmic means.

Sick with an ischemic heart disease and/or arrhythmia or after prolonged use therapy by medicament should be stopped gradually as sudden cancellation can lead to deterioration in a clinical state.

Contraindication

Hypersensitivity to a sotalol, streptocides or other components of drug.

Heart failure of the IV degree on NYHA, acute and chronic heart failure of the II-III degree (in a decompensation stage), an acute myocardial infarction, blockade of the II-III degree (if the patient has no functioning pacemaker), ventricular tachycardia like torsade de pointes, sinuatrial blockade, a sick sinus syndrome, symptomatic sinus bradycardia (50 ud. / mines), heavy dysfunction of sinus node, the congenital or acquired syndrome the extended interval Q–T, heavy or uncontrollable chronic heart failure, Printsmetal's stenocardia, cardiogenic shock, a renal failure (clearance of creatinine of 10 ml/min.), a hypopotassemia, a hypomagnesiemia, arterial hypotension, the significant disturbances of peripheric circulation, OH and chronic obstructive diseases of lungs, a laryngeal edema, allergic rhinitis, a metabolic acidosis, not treated pheochromocytoma, diabetes, a cardiomegaly (without symptoms of heart failure), the occlusal diseases of peripheral vessels (complicated by gangrene, the alternating lameness or pain at rest), Reynaud's syndrome, anesthesia medicaments which cause a myocardium depression, simultaneous use of MAO-A inhibitors, floktafeniny.

introduction of antagonists of calcium of type of verapamil and diltiazem or other antiarrhytmic medicaments is contraindicated to

For patients who are treated sotaloly (except for intensive medicament treatment).

Side effects

Frequency of undesirable reactions is classified by

under the following scheme: very often (≥1/10), it is frequent (≥1/100, 1/10), infrequently (≥1/1000, 1/100), is rare (≥1/10,000, 1/1000), is very rare (1/10,000), frequency is unknown (it is impossible to estimate due to the lack of data).

from the immune system: sotalol can increase sensitivity to allergens and weight of anaphylactic reactions.

Metabolic disturbances and disturbances from food: a hypoglycemia (signs of decrease in sugar in blood (in particular tachycardia) can mask against the background of therapy by drug). Patients who adhere to long starvation, sick diabetes and with a spontaneous hypoglycemia in the anamnesis need to consider it. Hyperglycemia, hypothyroid state. Increase in the general in XC and TG, reduction of XC, LPVP.

from mentality: often — uneasiness, confusion of consciousness, change of mood, a hallucination, hyperexcitability, a depression; seldom — sleep disorders.

from nervous system: often — dizziness, drowsiness, a headache, a dyssomnia, paresthesias, cryesthesia in extremities, fatigue, weakness, spasms, a tremor.

from an organ of sight: often — a disorder of vision; infrequently — conjunctivitis; very seldom — a keratoconjunctivitis, reduction of secretion of plaintive liquid (especially when using contact lenses), dryness and eye pain, inflammation of a cornea and conjunctiva, a photophobia.

from an organ of hearing: often — a hearing disorder.

from a cardiovascular system: often — a stethalgia, orthostatic hypotension, strengthening of symptoms of heart failure (hypostasis of anklebones, feet, an asthma), bradycardia, heartbeat, changes on the ECG, disturbance of conductivity of a myocardium, AV blockade, a syncopal or presinkopalny state, pro-arrhythmic effects (changes of a rhythm or strengthening of arrhythmia, can lead to considerable disturbance of warm activity with possible cardiac arrest), weakening of sokratitelny function of a myocardium, manifestation of a vasomotor spasm (strengthening of disturbances of peripheric circulation, cold sense in extremities, the alternating lameness, Reynaud's syndrome). Aritmogenny effects are more often observed at patients with heavy, life-threatening arrhythmias and dysfunction of a left ventricle; very seldom — increase in quantity of attacks of stenocardia and disturbance of peripheral perfusion. Considering what sotalol extends Q–T time, at its use the ventricular tachyarrhythmia (including torsade de pointes), especially in overdose cases can be observed.

Heavy proaritmogenny effects (constant ventricular tachycardia or blinking ventricles/fibrillation or torsade de pointes) depend on a dose and arise mainly at the beginning of therapy and at increase in a dose.

from a respiratory system: often — rhinitis, the complicated breath, a bronchospasm, a laryngospasm; infrequently — dispnoe, can arise at patients with obstructive disturbances of lungs; very seldom — an allergic bronchitis with fibrosis.

from a GIT: often — disturbance of taste, an abdominal pain, nausea, vomiting, diarrhea, dyspepsia, a meteorism, xerostomia; seldom — a constipation, dryness in a mouth, anorexia, an abnormal liver function (urine of dark color, yellowness of scleras or skin, a cholestasia).

from skin: often — an erythema, skin rash, a small tortoiseshell, an itching, a dieback, the strengthened sweating, a dermahemia; seldom — an alopecia; very seldom — a psoriazopodobny dieback, emergence/progressing of symptoms of psoriasis.

from a musculoskeletal system: muscular spasm or myasthenia, dorsodynias, arthralgias, muscle pains.

from a reproductive system: disturbances of sexual function.

General disturbances: often — fever, fatigue, cyanosis of extremities, an asthenia, a withdrawal.

Laboratory indicators: thrombocytopenia, agranulocytosis, leukopenia, formation of antinuclear antibodies, change of activity of enzymes, bilirubin level.

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Special instructions

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needs careful medical observation in the following cases:

• renal failure (dose decline); carrying out regular monitoring of renal function, including creatinine definition is necessary and also it is necessary to control concentration of a sotalol in blood plasma;
• patients with diabetes with considerable fluctuations of level of glucose in blood (at the same time symptoms of a hypoglycemia can be disguised); it is necessary to carry out monitoring of concentration of glucose to blood and to inform patients that the main symptom of a hypoglycemia during treatment sotaloly is the increased sweating;
• long starvation;
• hyperthyroidism; adrenergic symptoms can be disguised; at treatment of patients with suspicion of a thyrotoxicosis it is necessary to avoid the fast termination of reception of a sotalol as aggravation of symptoms of a hyperthyroidism, in particular thyrocardiac crisis is possible;
• peripheral disturbances of perfusion, such as Reynaud's syndrome and the alternating lameness; complaints can arise in an initiation of treatment;
• patients with a pheochromocytoma; the sotalol a hydrochloride can be applied only after preliminary blockade of α-adrenoceptors;
• patients with the atopic anamnesis, anaphylactic reactions in the anamnesis and the patients receiving the desensibilizing therapy (perhaps heavier course of anaphylactic reactions and insensitivity to usual doses of epinephrine at their treatment);
• patients with vasospastic stenocardia (Printsmetal's stenocardia), a myasthenia gravis, a depression (including in the anamnesis);
• in the presence of states and/or administration of medicaments promoting lengthening of an interval of Q-T;
• patients who recently had a myocardial infarction (the increased risk of aritmogenny action);
• patients with a syndrome of dysfunction of sinus node which is associated with symptomatic arrhythmias (the sotalola a hydrochloride can cause sinus bradycardia, sinus pauses or a stop of sinus node);
• patients with stagnant heart failure;
• patients with psoriasis (strengthening of symptoms of psoriasis).

Sotalol's

hydrochloride can increase weight of the available arrhythmias or cause new. Pro-arrhythmic effects can be various: from increase in frequency of premature reductions of ventricles and to development of heavier ventricular tachycardia, ventricular fibrillation or piruetny tachycardia. Risk factors which increase the probability of developing of piruetny tachycardia is the dose, presence of steady ventricular tachycardia, a floor (at women the frequency of emergence is higher), excessive increase in duration of an interval of Q-T _c , a cardiomegaly or chronic heart failure.

If in the course of therapy duration of an interval of Q-T _c exceeds 500 ms — the care at use is necessary and if exceeds 550 ms — the dose decline or the termination of administration of medicament is required. Pro-arrhythmic effects are more often observed in the first 7 days after the beginning of therapy or at increase in a dose. For reduction of risk of pro-arrhythmia it is recommended to begin treatment in a dose of 80 mg 2 times a day, and then to gradually titrate doses with simultaneous control of efficiency (programmable electrocardiostimulation or monitoring of the ECG on Holtera) and safety (duration of an interval of Q-T, ChSS and level of electrolytes of blood plasma).

In the cases of heavy diarrhea or competitive administration of medicines causing loss of magnesium and/or potassium needs to exercise control of electrolytic balance and acid-base equilibrium.

not to apply sotalol at patients with a hypopotassemia or a hypomagnesiemia before correction of an imbalance because of the probability of risks lengthening of an interval of Q-T and development of ventricular tachycardia like torsade de pointes.

Monitoring of the patients accepting Sotalol Sandoz has to include observation of ChSS, the ABP, the ECG, glucose content in blood at patients with diabetes. At patients of advanced age it is necessary to control indicators of function of kidneys. Patients with a renal failure need correction of the mode of dosing.

patients who had a myocardial infarction or at which ventricular function worsened have a risk of exacerbation of arrhythmia (pro-arrhythmia).

Before prescribing of medicament needs to cancel other antiarrhytmic means — the break in treatment has to make not less than 2-3 T _½ last.

At end of a course of treatment reception of a sotalol of a hydrochloride needs to be stopped gradually, reducing a dose during 2 weeks and more, under observation of the doctor. Frequency of administration of medicament cannot be changed. It is impossible to stop suddenly treatment — possibly development of heavy arrhythmias and a myocardial infarction.

At treatment of patients of advanced age needs to consider possible presence of the accompanying pathology, in particular a renal failure and hypersensitivity to drug, even on condition of usual dosing.

Patients using contact lenses have to consider

that at treatment the reduction of products of plaintive liquid is possible.

Thanks to blockade of β-adrenoceptors sotalol the sensitivity to allergens and weight of anaphylactic reactions that needs to be considered at treatment of patients with heavy reactions of hypersensitivity (including in the anamnesis) and those which are on the desensibilizing therapy can raise

.

In case of need surgical intervention needs to report

to the anesthesiologist about reception of a sotalol, some days before operation it is necessary to stop reception of a sotalol or to pick up anesthetic with the minimum negative inotropic effect.

In rare instances medicament can cause psoriasis, increase in expressiveness of its symptoms or to lead to a psoriazopodobny dieback.

Sotalol should be applied with care at AV blockade of the I degree owing to negative impact on conductivity.

Use of a sotalol is contraindicated to

in heavy allergic rhinitis in connection with strengthening of obstruction of airways.

Owing to presence of a sotalol of a hydrochloride at urine can give photometric definition of a metanefrin to obtaining the overestimated values.

should carry out by

At patients with suspicion on a pheochromocytoma which receive a sotalol a hydrochloride the analysis of urine by means of highly effective liquid chromatography with solid-phase extraction.

Drug contains lactose therefore patients should not appoint it with rare hereditary forms of intolerance of a galactose, deficiency of lactase or a syndrome of glyukozo-galaktozny malabsorption.

Use of a sotalol of a hydrochloride can result

in positive takes of doping tests.

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to Patients with the complicated breath appoint medicament on condition of careful assessment of a ratio of advantage and risk.

during treatment should not take alcohol in connection with a likelihood of developing orthostatic hypotension.

Use during pregnancy or feeding by a breast. As there is no sufficient experience of use of a sotalol of a hydrochloride during pregnancy, it is only possible to appoint medicament when the expected advantage for mother exceeds potential risk for a fruit.

Sotalol's

hydrochloride gets through a placenta and reaches pharmacological effective concentration in fruit fabrics therefore at a fruit or the newborn it is possible to expect emergence of such side reactions as bradycardia, arterial hypotension and a hypoglycemia. For this reason the therapy needs to be interrupted for 48–72 h before expected date of childbirth. After the birth for babies for some time it is necessary to establish careful observation (possibly development of blockade of β-adrenoceptors).

Sotalol's

hydrochloride gets into breast milk. Feeding by a breast during treatment needs to be stopped.

Children. Drug is not appointed to children.

Ability to influence speed of response at control of vehicles or other mechanisms. During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

not to apply

Interaction

:

• with antiarrhytmic medicaments I of a class (Disopyramidum, quinidine sulfate and procaineamide) and the III class (Amiodaronum) — can potentially increase a myocardium refrakternost. Amiodaronum increases risk of developing of bradycardia and oppression of AV conductivity. In case of simultaneous use of a sotalol with other β-adrenoceptors it is possible to expect additive effects of class II (decrease in the ABP and ChSS);
• with medicines which increase Q–T interval duration (antiarrhytmic medicaments of class I and III, derivatives of a fenotiazin, tricyclic antidepressants, terfenadin, astemizol, erythromycin, lithium drugs).

Three - and tetracyclic antidepressants, neuroleptics, narcotic analgetics, antihistaminic, sedative, sleeping medicines and ethanol strengthen oppression of central nervous system.

Simultaneous use of a sotalol of a hydrochloride with tricyclic antidepressants, barbiturates, fenotiaziny and narcotic analgetics and also antihypertensives, diuretics and vazodilatator can lead to excessive decrease in the ABP.

Means for an inhalation anesthesia (derivatives of hydrocarbons) and muscle relaxants increase risk of oppression of function of a myocardium and development of arterial hypotension.

Allergens which apply to an immunotherapy or extracts of allergens for skin tests increase risk of emergence of heavy system allergic reactions or an anaphylaxis.

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With medicines which exhaust stocks of catecholamines (reserpine, guanetidin) — considerable decrease in a tone of sympathetic nervous system can be observed. At patients it is regularly necessary to control the ABP and ChSS as hypotension, the profound bradycardia, a loss of consciousness are possible.

Negative chronotropic and negative dromotropic effects of a sotalol of a hydrochloride can increase at simultaneous use with reserpine, a clonidine, alpha metildopoy, guanfatsiny and cardiac glycosides.

With digoxin the probability of pro-arrhythmic effects increases, positive inotropic action of glycosides of a foxglove decreases. Both foxglove glycosides, and a sotalola a hydrochloride slow down AV conductivity. If despite adequate therapy the foxglove glycosides, noted reduction of weight of heart failure, reception of a sotalol needs to be stopped.

With antihypertensives (diuretics, sympatholytics, a clonidine, gidralazin) — perhaps excessive decrease in the ABP.

Furosemide, a hydrochlorothiazide and other diuretics removing potassium can provoke development of arrhythmia owing to a hypopotassemia.

At simultaneous use of a sotalol with Amphotericinum V, GKS needs to control potassium level.

Iodinated X-ray contrast substances for in/in introductions increase risk of development of anaphylactic reactions.

Xanthines and sympathomimetics reduce activity of a sotalol.

At simultaneous use with agonists β ₂ - receptors, such as salbutamol, terbutalin and izoprenalin, can arise need of increase in a dose of agonist β ₂ - receptors.

NPVP and estrogen weaken hypotensive effect of a sotalol of a hydrochloride, Sulfasalazinum increases its concentration in blood plasma.

Antagonists of calcium (verapamil and diltiazem), cardiac glycosides and antiarrhytmic means strengthen disturbance of AV conductivity, increase risk of development or increases in AV blockade and heart failure. At combined use with blockers of calcium channels perhaps additive hypotensive influence on the ABP.

Simultaneous use of antagonists of calcium ions of type of nifedipine can lead

to considerable falling of the ABP, strengthening of a sick sinus syndrome.

Norepinephrinum, MAO-B inhibitors and the sudden termination of reception of a clonidine can exponentiate ricochet AG. Reception of a sotalol needs to be stopped some days before gradual cancellation of reception of a clonidine, and having rummaged in treatment by MAO-B inhibitors and sotaloly has to make not less than 14 days.

Sotalol prolongs action of not depolarizing muscle relaxants, anti-coagulative effect of coumarins, increases concentration of lidocaine in blood plasma, increases effect of insulin and reduces effect of oral hypoglycemic means (correction of doses of antidiabetic medicaments can be necessary).

Simultaneous use with insulin or oral hypoglycemic means, especially during heavy physical activity, can induce a hypoglycemia and mask its symptoms.

Neuromuscular blockade caused by tubocurarine can amplify due to blockade of β-adrenoceptors.

Negative inotropic effect of a sotalol of a hydrochloride and narcotic analgetics or antiarrhytmic means can be additive.

Overdose

Symptoms of overdose of a sotalol of a hydrochloride depend on the general condition of warm activity of the patient (left ventricular function, cardiac arrhythmia). in the profound heart failure, even at administration of medicament in low doses, can deterioration in warm function will come to light.

Clinical data showed that depending on degree of intoxication there were such symptoms of overdose: dizziness, faints, weakness, an asystolia, symptoms of cardiogenic or hypovolemic shock, heart failure, AV blockade, arrhythmia, cyanosis of nails or palms, spasms, the complicated breath, a bronchospasm, a hypoglycemia, fatigue, a loss of consciousness, a mydriasis, sometimes generalized attacks, arterial hypotension, a hypoglycemia, the profound bradycardia up to cardiac arrest (the replaced rhythm often on the ECG), lengthening of an interval Q–T, chronic heart failure, atypical ventricular tachycardia (torsade de pointes), symptoms of cardiovascular shock. The overdose of a sotalol of a hydrochloride in some cases led to a lethal outcome.

Treatment: it is necessary to stop medicament use; gastric lavage, support of the vital functions of an organism, therapy symptomatic is shown. According to indications enter atropine of 1-2 mg in/in in the form of infusion (perhaps bolyusny introduction); sympathomimetics depending on body weight and the gained effect: dopamine, Dobutaminum, izoprenalin, ortsiprenalin and epinephrine; use of a glucagon is effective: in the beginning 1–10 mg in/in, then — 2-2.5 mg/h in the form of continuous infusion.

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In bradycardia showed atropine oxide, other anticholinergic drugs, agonists of β-adrenoceptors or transvenous electrocardiostimulation; at heart block (II or III degree) — Isoproterenolum or transvenous electrocardiostimulation; in heart failure — cardiac glycosides, diuretics, a glucagon; in hypotension (depending on the associated factors) in addition to atropine and glycosides of a foxglove if necessary it is more reasonable to apply epinephrine, but not Isoproterenolum or Norepinephrinum, at a bronchospasm — stimulators β ₂ - adrenoceptors in the form of aerosol or Aminophyllinum; at a hypoglycemia — in/in administration of glucose; in "piruetny" tachycardia — epinephrine, magnesium sulfate, transvenous electrocardiostimulation, cardiostimulation by a direct current.

As a sotalola the hydrochloride is a competitive antagonist of Isoproterenolum, high doses of Isoproterenolum can neutralize many effects of excess doses Sotalola Sandoz, but in case of use of Isoproterenolum it is necessary to be ready to complications which can cause high doses.

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It is removed by means of a hemodialysis.

Storage conditions

does not demand special storage conditions.