Thiocetam solution for injection 5ml, No. 10

In complex therapy: chronic cerebral ischemia during the recovery period of ischemic stroke (including in patients with non-dementia cognitive impairment) with diabetic encephalopathy.

The drug is administered intravenously intramuscularly only if it is impossible to take it inside.

In chronic disorders of cerebral circulation and in the recovery period after ischemic stroke, 20-30 ml of the drug, previously diluted in 100-150 ml of 09% sodium chloride solution, is prescribed and administered intravenously by drop infusion once a day. The course of treatment is 2 weeks; in the future, they switch to a tablet form.

In diabetic encephalopathy, 5 ml is prescribed intramuscularly 1 time per day for 10 days, with the further appointment of a tablet form.

Active ingredient: piracetam - 100.0 mg; morpholinium-methyl-triazolyl-thioacetate (thiotriazoline) - 25.0 mg;

excipients: water for injection - up to 1 ml.

• - hypersensitivity to piracetam derivatives of pyrrolidone or thiortiazoline, as well as to other components of the drug;

  - Huntington's chorea;

  - Acute violation of cerebral circulation (hemorrhagic stroke);

  - severe chronic renal failure (creatinine clearance less than 20 ml / min); acute renal failure.

  - psychomotor agitation at the time of prescribing the drug;

  - children up to age 18;

  - pregnancy and lactation.

Carefully:

Chronic renal failure (creatinine clearance 20-80 ml / min); in case of hemostasis disorders, conditions that may be accompanied by bleeding (ulcers of the gastrointestinal tract); with major surgical interventions (including dental); with severe bleeding; hemorrhagic stroke (history). With simultaneous use with anticoagulants, platelet antiplatelet agents (including acetylsalicylic acid).

The drug should be used with caution in the elderly with cardiovascular pathology due to the fact that this group of patients is more likely to have adverse reactions.

Trade name of the drug

Thiocetam

International non-proprietary name

Piracetam + Thiotriazolin

Dosage form

solution for intravenous and intramuscular administration

Composition for 1 ml:

Active ingredient: piracetam - 100.0 mg; morpholinium-methyl-triazolyl-thioacetate (thiotriazoline) - 25.0 mg;

excipients: water for injection - up to 1 ml.

Description

Transparent, colorless or slightly yellowish liquid.

Pharmacotherapeutic group

Nootropic remedy

ATX code

N06BX

Pharmacodynamics:

Thiocetam belongs to the group of cerebroactive agents and exhibits nootropic anti-ischemic and antioxidant properties. The pharmacological effect of the drug is due to the mutually potentiating effect of thiotriazoline and piracetam.

Piracetam - a nootropic agent acts on the central nervous system in various ways: modifies neurotransmission in the brain; improves conditions conducive to neuronal plasticity; improves microcirculation by affecting the rheological characteristics of blood and not causing vasodilation. The use of piracetam in patients with cerebral dysfunction increases concentration and improves cognitive function, which is accompanied by changes in the electroencephalogram (increased calamus activity, decreased activity 5). Reduces the duration of the induced vestibular neuronitis. Promotes the restoration of cognitive functions due to various disorders such as hypoxia, intoxication or electroconvulsive therapy.

Piracetam inhibits the increased aggregation of activated platelets and, in the case of pathological rigidity of erythrocytes, improves their deformability and filtration capacity.

Thiotriazoline reacts with reactive oxygen species and lipid radicals due to the pronounced reducing properties of the thiol group and prevents the emergence of reactive oxygen species by reactivating antiradical enzymes: catalase superoxide dismutase and glutathione peroxidase. Thiotriazoline blocks oxidative stress both in the initial stages and in the expanded stage. The membrane stabilizing effect is also due to the antioxidant effect of the drug, as a result of which the cell membranes preserve their physicochemical properties to a greater extent: plasticity, fluidity, permeability, preservation of the transmembrane potential. Thiotriazoline effectively affects the energy metabolism of cells, reduces their need for oxygen, stabilizes the cytoplasmic membrane.

Thiocetam improves the integrative and cognitive activity of the brain; improves the learning process; eliminates amnesia; increases the indicators of short-term and long-term memory.

Pharmacokinetics:

Piracetam

Distribution

The volume of distribution (Vd) is about 06 l / kg. Does not bind to plasma proteins. Piracetam crosses the blood-brain and placental barriers as well as hemodialysis membranes.

In a study on animals, it was found that piracetam selectively accumulates in the tissues of the cerebral cortex, mainly in the frontal parietal and occipital lobes in the cerebellum and basal nuclei.

Metabolism

Not metabolized.

Withdrawal

The half-life of piracetam from blood plasma (T1 / 2) is 4-5 hours and 85 hours from cerebrospinal fluid; the half-life is lengthened in renal failure. It is excreted by the kidneys unchanged. Renal excretion is almost complete (> 95%) within 30 hours.

The total clearance of piracetam in healthy volunteers is 86 ml / min.

Thiotriazoline

When administered intramuscularly, the maximum concentration of thiotriazoline in the blood plasma is reached after 0.84 hours; when administered intravenously, after 01 hours. Binding to blood proteins is not more than 10%. It accumulates mainly in the kidneys - 31% and also in large quantities in the large intestine, heart, spleen, least of all - in the small intestine and lungs (1-2%).

Indications:

In complex therapy: chronic cerebral ischemia during the recovery period of ischemic stroke (including in patients with non-dementia cognitive impairment) with diabetic encephalopathy.

Contraindications:

• - hypersensitivity to piracetam derivatives of pyrrolidone or thiortiazoline, as well as to other components of the drug;

  - Huntington's chorea;

  - Acute violation of cerebral circulation (hemorrhagic stroke);

  - severe chronic renal failure (creatinine clearance less than 20 ml / min); acute renal failure.

  - psychomotor agitation at the time of prescribing the drug;

  - children up to age 18;

  - pregnancy and lactation.

Carefully:

Chronic renal failure (creatinine clearance 20-80 ml / min); in case of hemostasis disorders, conditions that may be accompanied by bleeding (ulcers of the gastrointestinal tract); with major surgical interventions (including dental); with severe bleeding; hemorrhagic stroke (history). With simultaneous use with anticoagulants, platelet antiplatelet agents (including acetylsalicylic acid).

The drug should be used with caution in the elderly with cardiovascular pathology due to the fact that this group of patients is more likely to have adverse reactions.

Pregnancy and lactation:

Pregnancy

There is no sufficient data on the use of piracetam during pregnancy. Animal studies have not shown a direct or indirect effect on pregnancy, fetal / fetal development, labor, or postnatal development.

Piracetam crosses the placental barrier. The plasma concentration of piracetam in newborns reaches 70-90% of that of the mother.

There is no experience of using the drug Thiocetam during pregnancy, therefore, the drug should not be prescribed to this category of women.

Lactation

Piracetam passes into breast milk. If it is necessary to use the drug during lactation, it is necessary to stop breastfeeding for the duration of treatment.

Method of administration and dosage:

The drug is administered intravenously intramuscularly only if it is impossible to take it inside.

In chronic disorders of cerebral circulation and in the recovery period after ischemic stroke, 20-30 ml of the drug, previously diluted in 100-150 ml of 09% sodium chloride solution, is prescribed and administered intravenously by drop infusion once a day. The course of treatment is 2 weeks; in the future, they switch to a tablet form.

In diabetic encephalopathy, 5 ml is prescribed intramuscularly 1 time per day for 10 days, with the further appointment of a tablet form.

Side effects:

The frequency of adverse events for the drug based on the results of clinical trials and according to the data of post-marketing use cannot be established because there were only isolated cases of the development of undesirable phenomena.

Thiocetam:

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

from the digestive tract: nausea vomiting;

from the immune system: allergic reactions including rash itching urticaria angioedema anaphylactic shock;

on the part of the cardiovascular system: lowering blood pressure;

from the vestibular system: dizziness;

general disorders and disorders at the injection site: skin hyperemia and itching at the injection site.

Patients may develop adverse reactions due to individual components of the drug:

Piracetam:

in terms of frequency, adverse reactions are divided into the following categories: very often (? 1/10); often (? 1/100 <1/10); infrequently (? 1/1000 <1/100); rarely (? 1/10 000 to <1/1000); very rare (<1/10 000) frequency unknown (frequency cannot be estimated from available data).

from the nervous system: infrequently - drowsiness frequency unknown - hyperkinesis ataxia imbalance aggravation of epilepsy headache insomnia tremor;

on the part of the psyche: often - nervousness infrequently - depression frequency unknown - agitation anxiety confusion hallucinations drowsiness.

on the part of the hearing organs and the labyrinth: the frequency is unknown - vertigo;

from the digestive system: frequency unknown - abdominal pain (including in the upper parts) diarrhea nausea vomiting;

from the immune system: the frequency is unknown - anaphylactoid reactions, hypersensitivity;

on the part of the skin and subcutaneous tissues: frequency unknown - angioedema dermatitis urticaria itching;

on the part of the reproductive system: the frequency is unknown - increased sexual desire;

vascular disorders: rarely - hypotension, thrombophlebitis;

on the part of metabolism and nutrition: often - increased body weight;

general disorders and disorders at the injection site: infrequently - asthenia rarely - pain at the injection site; fever frequency is unknown - thrombophlebitis.

Thiotriazoline:

The data of clinical studies and post-registration observations are insufficient to determine the frequency of adverse reactions.

In predominantly elderly patients, in particular while taking other drugs, cases are described:

on the part of the immune system of the skin and subcutaneous tissue: hypersensitivity reactions, including skin rashes (urticarial papular small-spotted spotted) itching, hyperemia of the skin, fever; individual cases of urticaria, angioedema, anaphylactic shock are described;

from the nervous system - dizziness; tinnitus;

on the part of the cardiovascular system: tachycardia; increased blood pressure;

from the gastrointestinal tract: dry mouth bloating nausea vomiting;

from the respiratory system: shortness of breath, asthma attacks.

Overdose:

Symptoms: the occurrence or increase in the severity of dose-dependent side effects of the drug.

Treatment: drug withdrawal symptomatic therapy. The effectiveness of hemodialysis for piracetam is 50-60%.

Interaction:

Thiocetam should not be administered with acidic solutions.

The interaction of thiotriazoline with other drugs has not been studied.

Thyroid hormones

With the simultaneous use of piracetam and thyroid hormone preparations, confusion of consciousness, irritability and sleep disturbance were noted.

And cenocoumarol

According to a published clinical study in patients with recurrent venous thrombosis, piracetam at a dose of 96 g / day does not affect the dose of acenocoumarol required to achieve an international normalized ratio of 25-35, but compared with the effects of acenocoumarol alone, the addition of piracetam at a dose of 96 g / day is significant reduces platelet aggregation, p-thromboglobin release, fibrinogen and von Willebrand factor concentration (VIII: C; VIII: vW: Ag; VIII: vW: RCo) as well as the viscosity of whole blood and plasma.

Pharmacokinetic interactions

The possibility of changing the pharmacokinetics of piracetam under the influence of other drugs is low, since about 90% of piracetam is excreted unchanged in the urine.

At concentrations 142 426 and 1422 ?g / ml, piracetam does not inhibit cytochrome P450 isoenzymes (CYP 1A2 2B6 2C8. 2C9 2C19 2D6 2E1 and 4A9 / 11) in in vitro experiments. At a concentration of 1422 ?g / ml, minimal inhibition of the isoenzyme CYP2A6 (21%) and 3A4 / 5 (I%) was observed. However, the values ??of the inhibition constant (Ki) are likely to go far beyond the concentration of 1422 ?g / ml. Thus, metabolic interactions of piracetam with other drugs are unlikely.

Anticonvulsants

Taking piracetam at a dose of 20 g / day for more than 4 weeks in patients with epilepsy who took constant doses of antiepileptic drugs (carbamazepine phenytoin phenobarbital and valproic acid) did not change the curve of the concentration level of these drugs and their maximum concentration.

Alcohol

Concomitant use with alcohol did not affect the plasma concentration of piracetam; when taking 16 g of piracetam, the concentration of ethanol in plasma did not change.

Special instructions:

Elderly patients

With long-term treatment of elderly patients, regular monitoring of creatinine clearance is necessary since dose adjustment may be required.

Impact on the ability to drive vehicles. Wed and fur .:

”читыва¤ профиль нежелательных реакций в период лечени¤ необходимо соблюдать осторожность при управлении транспортными средствами работе с механизмами и зан¤ти¤х другими потенциально опасными видами де¤тельности требующими повышенной концентрации внимани¤ и быстроты психомоторных реакций.

‘орма выпуска/дозировка:

–аствор дл¤ внутривенного и внутримышечного введени¤.

”паковка:

ѕо 5 мл или 10 мл в ампулы из бесцветного прозрачного стекла с кольцом излома зеленого цвета или с точкой излома или без кольца и точки излома.

ѕо 5 ампул в контурную ¤чейковую упаковку из пленки поливинилхлоридной. ?ве контурные ¤чейковые упаковки вместе с инструкцией по применению и скарификатором ампульным вкладывают в пачку.

ѕримечание. ѕри использовании ампул с точкой или кольцом излома вкладывание скарификаторов не предусмотрено.

”слови¤ хранени¤:

Store in original packaging at a temperature not exceeding 25 ? C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date indicated on the package.

Vacation conditions

On prescription