Pharmacological properties

Pharmacodynamics. to tiotseta treats to group of tserebroaktivny means, has nootropic, antiischemic, antioxidant and membrane stabilizing properties. medicine improves integrative and cognitive activity of a brain, increases efficiency of process of training, promotes elimination of symptoms of amnesia, raises indicators of short-term and long-term memory.

Pharmacological effect of medicine is caused by mutually exponential action of a tiotriazolin and piracetam.

Tiotsetam has ability to accelerate oxidation of glucose in reactions of aerobic and anaerobic oxidation, normalizes biopower processes, increases the ATP level, stabilizes metabolism in brain tissues. Drug brakes ways of formation of active forms of oxygen, reactivates the antioxidant system of enzymes, especially a superoxide scavenger, slows down free radical processes in brain tissues at ischemia, improves rheological properties of blood due to activation of a fibrinolytic system, stabilizes and reduces zones of necrosis and ischemia.

Tiotsetam increases intensity of operation of the metabolic GAMK-shunt and concentration of GAMK in ischemic fabrics.

Tiotsetam improves integrative and cognitive activity of a brain, promotes training process, eliminates amnesia, raises indicators of short and long-term memory. Tiotsetam eliminates stress consequences (feeling of alarm, a phobia, depression, a sleep disorder), reduces lag in physical and intellectual development of premature children.

Pharmacodynamics. It is well soaked up at intake, gets into various bodies and fabrics, including into brain tissues. Gets through a placental barrier. Each component of medicine is metabolized separately. Piracetam is practically not metabolized in an organism and removed with urine. The t _½ — 4–8 h Tiotriazolin after intake is quickly soaked up, its absolute bioavailability is 53%. The C _max in blood plasma is reached in 1.6 h after single dose in a dose of 200 mg. The t _½ makes nearly 8 h

Indication

Tablet: the tranzitorny and chronic violations of cerebral circulation caused by atherosclerosis of vessels of a brain and violations of cerebral circulation in the past. medicine is also shown at violations of cerebral circulation, the exchange processes of a brain caused by a craniocereberal injury, intoxication, diabetic encephalopathy and also during the rehabilitation period after an ischemic and hemorrhagic stroke.

Solution for injections: treatment of an ischemic stroke and its such consequences as violation of the speech, mental and somatic disorders, decrease of the activity, violations of the emotional sphere; treatment (during the recovery period) vascular, toxic, traumatic encephalopathy; elimination of an abstinence syndrome at a drunkenness, diabetic encephalopathy.

Use

Tablet to tiotseta forte. duration of treatment is determined by the doctor in each individual case separately depending on a course of the disease.

At tranzitorny and chronic violations of cerebral circulation and during the rehabilitation period after an ischemic and hemorrhagic stroke on 2 tablets 3 times a day within 25–30 days.

Tablet Tiotsetam Forte is appointed in 30 min. prior to food.

Course of treatment makes

2–3 weeks up to 3–4 months

For treatment of diabetic encephalopathy appoint 2 tablets 3 times a day for 45 days.

Tiotsetam solution for injections. In an ischemic stroke and for treatment of its consequences appoint 20–30 ml of the medicine which is previously diluted in 100–150 ml of 0.9% of solution of sodium of chloride and enter in into by drop infusion 1 once a day. The course of treatment makes 2 weeks.

For treatment of encephalopathy and knocking over of an abstinence syndrome at a drunkenness are appointed by 5 ml of medicine in oil of 1 times a day for 10–15 days

In diabetic encephalopathy on 5 ml in oil of 1 times a day for 10 days with further appointment on 2 tablets of the medicine Tiotsetam Forte 3 times a day for 45 days in 30 min. prior to food

Contraindication

Hypersensitivity to piracetam, to derivatives of a pirrolidon, to tiazotny acid and also to any other component of medicine. an acute disorder of cerebral circulation on hemorrhagic type. end-stage of a renal failure. Hungtington's chorea.

Side effects

to tiotseta can be observed by

At clinical use of medicine side reactions:

from central nervous system and peripheral nervous system: headache, general weakness;

from a digestive tract: nausea, vomiting, diarrhea;

from the immune system: allergic reactions, including rashes, an itch, urticaria;

from a vestibular system: dizziness.

At patients the development of the side reactions caused by separate components of medicine is possible

:

piracetam:

from blood and a lymph: hemorrhagic violations;

from the immune system: hypersensitivity, anaphylactoid reactions;

mental violations: nervousness, depression, hyperexcitability, uneasiness, confusion of consciousness, hallucination;

from nervous system: hyperkinesia, drowsiness, ataxy, balance violation, increase in frequency of attacks of epilepsy, headache, insomnia, tremor;

from an organ of hearing and a labyrinth: dizziness;

from a digestive tract: abdominal pain, pain in the top part of a stomach, diarrhea, nausea, vomiting;

from skin and hypodermic fabrics: Quincke's disease, dermatitis, rashes, urticaria, itch;

from a reproductive system: increase in sexual activity;

general violations: adynamy, increase in body weight;

tiazotny acid:

from skin and hypodermic cellulose: itch, dermahemia, rashes, urticaria, Quincke's disease;

from the immune system: acute anaphylaxis;

from central nervous system and peripheral nervous system: dizziness, sonitus;

from a cardiovascular system: tachycardia, increase in the ABP;

from a digestive tract: dyspepsia, including dryness in a mouth, an abdominal distension, nausea, vomiting;

from a respiratory system: short wind, suffocation;

general violations: fever, the general weakness, pain in the injection site.

Drug contains dye a yellow decline of FCF (E110) that can cause allergic reactions.

Special instructions

can appoint Drug by

at cerebrovascular insufficiency with the phenomena of violation of the speech, memory, attention, decrease in intellectual function of a brain and violation of the emotional sphere for increase in an opportunity to study at the cephalalgia including caused by neurocirculatory dystonia. tiotseta can apply to treatment at above-mentioned diseases against the background of the available heart pathology (an angina of exertion, a myocardial infarction), a liver (hepatitis, cirrhosis) and viral infections.

With care should use medicament to elderly people with cardiovascular pathology as the above side reactions at these patients note more often.

Allergic reactions note

at the persons inclined to an allergy more often.

Influence on aggregation of platelets. Because piracetam reduces aggregation of platelets, it is necessary to appoint with care the patient with violation of a hemostasis, states which can be followed by hemorrhages (GIT ulcers), during serious surgeries (including dental interventions), the patient with symptoms of heavy bleeding and to the patient having a hemorrhagic stroke in the anamnesis; to patients who apply anticoagulants, platelet antiagregant, including acetylsalicylic acid in a low dose. Drug is emitted with kidneys therefore it is necessary to pay special attention to patients with a renal failure.

Patients of advanced age. At long therapy at patients of advanced age it is recommended to carry out regular control of indicators of function of kidneys, if necessary korrigirut a dose depending on clearance of creatinine.

Drug in the form of tablets contains lactose as excipient that it is necessary to consider at application for patients with intolerance of a galactose, deficiency lactases or violation of absorption of glucose and a galactose.

1 the tablet Tiotsetama contains 3.5 mg of sugar powder that should be considered when assigning to patients with diabetes.

Use during pregnancy and feeding by a breast. It is not necessary to apply.

Children. Do not apply.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Use of medicine at control of vehicles and work with the mechanisms requiring special attention in connection with risk of development of possible side reactions from nervous system is not recommended.

Interaction

Tiotsetam cannot appoint

with the medicines having acid rn.

Because of existence in composition of medicine of piracetam the interaction with the following medicines is possible

:

thyroid hormones. At the combined application with thyroid hormones (T ₃ + the T ₄ ) is possible acrimony, a disorientation and a sleep disorder.

Atsenokumarol. With a heavy course of recurrent thrombosis the use of piracetam in high doses (9.6 g/days) did not demand change of a dose of an atsenokumarol for achievement of value of a prothrombin time (INR) 2.5-3.5 from patients, but at simultaneous application the considerable decrease in level of aggregation of platelets, level of fibrinogen, Villibrandt's factors was noted (VIII: C; VIII: vW: Ag; VIII: vW: Rco), viscosity of blood and blood plasma.

Pharmacokinetic interactions. Probability of change of a pharmacodynamics of piracetam under the influence of other medicines low as 90% of medicine are removed in not changed view with urine.

In vitro piracetam does not suppress an isoform of CYP P450 cytochrome 1A2, 2V6, 2S8, 2S9, 2S19, 2D6, 2E1 and 4A9/11 in concentration 142; 426 and 1422 mkg/ml.

by

At concentration of 1422 mkg/ml noted insignificant oppression of CYP 2A6 (21%) and 3A4/5 (11%). However level To _і these two CYP isomers sufficient when exceeding 1422 mkg/ml. Therefore metabolic interaction with medicines which are exposed to biotransformation these enzymes is improbable.

Antiepileptic medicines. Use of piracetam in a dose of 20 mg/days during ≥4 weeks did not change a curve of level of concentration and From _max antiepileptic medicines in blood plasma (carbamazepine, Phenytoinum, phenobarbital, sodium Valproatum) at patients with epilepsy.

Concomitant use with enalapril, captopril increases risk of development of side reactions from a cardiovascular system.

Alcohol. The combined reception with alcohol did not influence the level of concentration of piracetam in blood plasma, and concentration of alcohol in blood plasma did not change at application of 1.6 g of piracetam.

Overdose

When exceeding the doses appointed by the doctor the emergence or increase in severity of side effects of medicine (excitement, a sleep disorder, the dispeptic phenomena) is possible

. in these cases stop use of medicine and appoint symptomatic treatment (cause vomiting, wash out a stomach).

Storage conditions

In original packing at a temperature not above 25 °C.