Tiodaron

General characteristics. Structure:

1 tablet contains Amiodaronum of a hydrochloride-0,2 of; tiotriazolina-0,1
excipients cellulose-102 microcrystallic, sodium of a kroskarmeloz, potato starch, twin-80, talc, calcium stearate.

Pharmacological properties:

Pharmacodynamics. The combined drug which properties are caused by its compound - Amiodaronum a hydrochloride and tiotriazoliny. Amiodaronum the hydrochloride influences preferential heart and vessels. It has antiarrhytmic and anti-anginal effect, thanks to ability to block ionic (mainly potassium, to a lesser extent - calcic and sodium)
channels of membranes of cardiomyocytes and also to slow down mediator processes of excitement alpha and beta adrenoceptors. Amiodaronum the hydrochloride has negative chronotropic influence. Sympatholytic activity and blockade of potassium and calcium channels reduce the need of a myocardium for oxygen, result in negative dromotropic effect: delay of conductivity and
lengthening of the refractory period in sinus and AV nodes. Besides, it has also properties of a vazodilatator thanks to which it can reduce resistance of coronary vessels. The second component – тиотриазолин which effects are caused by the prevailing influence on biochemical processes in heart and vessels. It revealed antiischemic, membrane stabilizing, antioxidant and immunomodulatory properties. It strengthens compensatory activation of anaerobic glycolysis, activates processes of oxidation in a tricarbonic acid cycle with preservation of the ATP intracellular fund. Drug also activates antioxidant system and slows down processes of oxidation of lipids in ischemic sites of a myocardium, reduces sensitivity of a cardiac muscle to action of catecholamines, prevents progressive oppression of sokratitelny function of cardiomyocytes, stabilizes and reduces the area and volume of a zone of a necrosis and activates
fibrinolitic system.

Pharmacokinetics. It is caused by pharmacological properties of both components. Amiodaronum a hydrochloride is slowly absorbed from digestive tract. Bioavailability makes 30-80%. After one-time reception the maximum concentration in a blood plasma is reached in 3-7 hours. In the first days of use collects practically in all fabrics, especially in fatty inclusions, a liver, a spleen, lungs. Amiodaronum a hydrochloride with bile and a stake is removed. Renal
excretion is insignificant. The elimination half-life makes 20-100 days. Relative biological availability of a tiotriazolin – 64,5%, the semi-absorption period – 0,28 h, semi-removal – 1,3 h, the maximum kontsengtration in a blood plasma – 1,18 h, linkng with blood proteins does not exceed 10%. In considerable concentration collects in tissues of heart, liver, spleen, rectum and kidneys, in insignificant quantity – in lungs and a small bowel. Tiotriazolin does not influence acidity of a stomach and is allocated mainly with kidneys therefore does not influence removal of Amiodaronum of a hydrochloride.

Indications to use:

Prevention of a recurrence: ventricular tachycardia or fibrillation of ventricles which threaten life; ventricular tachycardia with clinical manifestations; supraventricular tachycardia; disturbances of a rhythm at resistance or existence of contraindications to other methods of treatment; the disturbances of a rhythm caused by WPW syndrome.

Treatments of supraventricular tachycardia for delay of a rhythm of reductions of ventricles or recovery of a sinoatrial rate during the blinking and an atrial flutter. Drug is recommended to patients with coronary heart disease and/or dysfunction of a left ventricle for treatment of documentary supraventricular tachycardia for the purpose of control of heart rate when blinking an atrial flutter.

Route of administration and doses:

Tiodaron appoint inside in doses in terms of Amiodaronum a hydrochloride. The sating dose for adults makes 600 – 1000 mg/days (3-5 tablets) for 8 – 10 days, under control of an ECG. A maintenance dose for adults – 100 – 400 mg a day (½ - 2 tablets). Drug it is possible to appoint in a dose 200 mg (1 tablet) a day every other day or po100 in mg (½ tablets) a day daily. It is possible having rummaged in inclusion for 2 days a week.

Features of use:

Against the background of treatment by Tiodaron ECG control as changes of an ECG are possible is obligatory: moderate lengthening of an interval of Q-T (with an invariable width of QRS), expansion of a tooth of T, decrease in its amplitude, sploshcheny tops or two-staging; emergence or increase in amplitude of a tooth of U. With care combine with beta blockers, and also with drugs which cause a hypopotassemia (diuretics, corticosteroids, Amphotericinum In for intravenous administration). Care is necessary at disturbances
to atrioventricular conductivity and bronchial asthma, and also at disturbances of electrolytic balance. It is necessary to consider what at patients of advanced age is noted more expressed
decrease in heart rate. At emergence of AV of blockade ІІ or ІІІ degrees, sinuatrial or bifastsikulyarny blockade it is necessary to stop use of drug. At long treatment it is necessary to address the ophthalmologist, regular control of function of a thyroid gland, radiological control of lungs. Patients should be warned that they during treatment avoided influence of a sunlight or used measures of protection. Before operation it is necessary to report to the anesthesiologist about what you accept Tiodaron. Influence on ability to drive the car and to perform works which require special attention. There are no data on Tiodaron's influence on ability to drive the car and to perform works which require special attention.

Side effects:

Are possible:
from cardiovascular system: bradycardia (degree depends on a dose); in isolated cases – blockade of a sinus node (usually at dysfunction of a sinus node or at patients of old age); seldom – sinuatrial blockade, an atrioventricular block;
from an organ of sight: adjournment of lipofuscin in a cornea epithelium, in rare instances considerable;
dermatological reactions: photosensitization, lead-blue or bluish xanthopathy; rash on skin, an alopecia;
from endocrine system: at long use development of a hypothyroidism is in rare instances possible, is much more rare – a hyperthyroidism;
from the central nervous system and peripheral nervous system: seldom – neuropathy, a myopathy (disappear after drug withdrawal), an extrapyramidal tremor, a brain ataxy, nightmares, a brain pseudoneoplasm;
from the alimentary system: seldom – nausea, vomiting, taste disturbance, hepatitis, cirrhosis, increase in level of transaminases;
from respiratory system: pneumonitis, bronchospasm, fibrosis, pleurisy, bronchiolitis, pneumonia.
others: vasculitis, damage of kidneys, thrombocytopenia, hemolitic or aplastic anemia.

Interaction with other medicines:

Increases concentration in plasma of quinidine, procaineamide, a flekainid, Phenytoinum, cyclosporine, digoxin (at simultaneous use the digoxin dose decline for 25-50% and control of its plasma concentration is recommended). Strengthens effects of anticoagulants of indirect action – warfarin and an atsenokumarol (interaction at the level of a microsomal oxidation). In these cases a warfarin dose
it is necessary to reduce up to 66%, and an atsenokumarol – to 50% and to control a prothrombin time. Antiaretmichesky medicines Іа a class, a fenotiazina, tricyclic antidepressants, "loopback" diuretics, tiazida, fenotiazina, астемизол, терфенадин, соталол, purgatives, glucocorticosteroids for system use, тетракозактид, pentamidine, Amphotericinum In for intravenous administration – risk of development of aritmogenny action (lengthening of an interval of Q-T, polymorphic ventricular tachycardia, predisposition to a sinus bradycardia, blockade of a sinus node
or an atrioventricular block) the Beta – adrenoblockers, verapamil and cardiac glycosides increase risk of development of bradycardia and oppression of atrioventricular conductivity. The general anesthesia (means for inhalation anesthesia), an oxygenotherapy – risk of developing of bradycardia (resistant to atropine), arterial hypotension, disturbance of conductivity, decrease in minute volume of blood. The medicines causing a photosensitization have the adititvny photosensitizing effect. Tiodaron can suppress absorption by a thyroid gland of Natrii iodidum and sodium of a pertekhnetat; lithium increases risk of a hypothyroidism. Klestiramin reduces absorption, and Cimetidinum increases an elimination half-life and concentration of Amiodaronum of a hydrochloride in plasma. At simultaneous use with anticoagulants the risk of development of bleedings increases.

Contraindications:

Sinus bradycardia, AV-blockade ІІ and ІІІ degrees (in the absence of a pacemaker); sick sinus syndrome, sinuatrial blockade; heavy disturbances of conductivity, hypersensitivity to iodine and Amiodaronum of a hydrochloride, dysfunction of a thyroid gland, arterial hypotension of a heavy current; pregnancy and period of a lactation.

Overdose:

Symptoms: a sinus bradycardia, conductivity blockade, Bouveret's ventricular disease like "pirouette", blood circulation disturbance, an abnormal liver function.
Treatment: carry out symptomatic therapy. Dialysis is inefficient.

Storage conditions:

To store in the unavailable to children, dry, protected from light place, at a temperature from 15ºС to 25ºС. Period of storage 2 years.

Issue conditions:

According to the recipe

Packaging:

No. 10 h3 and No. 10 x 6 tablets in the blister and a pack.