Lira solution for infection. 500mg/4ml amp. 4 ml No. 5

Pharmacological properties

Pharmacodynamics. tsitikolin stimulates biosynthesis of structural phospholipids of membranes of neurons that is confirmed by data of magnetic and resonant spectroscopy. tsitikolin improves functioning of such membrane mechanisms as ionic pumps and receptors without which regulation normal carrying out nervous impulses is impossible. thanks to the stabilizing action on a membrane of neurons tsitikolin shows antiedematous properties which promote a wet brain reabsorption.

Clinical trials showed that tsitikolin inhibits activation of some phospholipases (A1, A2, C and D), reducing education of free radicals, prevents destruction of membrane systems and keeps antioxidant protective systems, such as glutathione.

Tsitikolin keeps a neural stock of energy, inhibits apoptosis that improves cholinergic transfer.

it is Experimentally proved that tsitikolin also has preventive neurotyre-tread effect in focal ischemia of a brain.

Clinical trials showed that tsitikolin authentically increases indicators of functional recovery at patients with an acute disorder of cerebral circulation that matches delay of growth of an ischemic brain damage according to neuroimaging. At patients with a craniocereberal injury tsitikolin accelerates restoration and reduces duration and intensity of a posttraumatic syndrome.

Tsitikolin improves the level of attention and consciousness, promotes reduction of manifestations of amnesia, the cognitive and other neurologic disorders connected with brain ischemia.

Pharmacokinetics. Tsitikolin is well absorbed after peroral, in oil and in/in introductions. Sincaline level in blood plasma considerably increases after introduction in the above-mentioned ways. Absorption after oral introduction almost full, and bioavailability practically same, as well as at in in use.

Depending on a way of introduction in intestines, a liver to sincaline and cytidine. After introduction tsitikolin it is widely distributed in structures of a brain with fast inclusion of fraction of sincaline in structural phospholipids and fractions of cytidine in cytidine nucleotides and nucleic acids. Having reached a brain, tsitikolin it is built in cellular, cytoplasmic and mitochondrial membranes, participating in creation of fraction of phospholipids.

with urine and a stake (less than 3%). About 12% of a dose are removed with the exhaled CO ₂ . In excretion of medicament with urine allocate two phases: the first phase — about 36 h in which excretion speed quickly decreases and the second phase in which the speed of excretion decreases much more slowly. The same staging is observed at excretion with CO ₂ : speed of excretion of the exhaled CO ₂ quickly decreases approximately in 15 h, then it decreases much more slowly.

Indication

Stroke, sharp phase of disturbances of cerebral circulation and treatment of complications and consequences of disturbances of cerebral circulation; craniocereberal injury and its neurologic consequences; cognitive disturbances and behavior disorders owing to chronic vascular and degenerative cerebral disorders.

Use

For in/in or introductions in oil.

Recommended dose for adults makes 500–2000 mg/days depending on weight of a condition of the patient. The maximum daily dose — 2000 mg. At acute and medical emergencies the maximum therapeutic effect is reached at use of medicament in the first 24 h

In/in appoint in the form of a slow injection (within 3–5 min. depending on the entered dose) or drop injection (40–60 drops a minute).

to Patients of advanced age does not need dose adjustment.

to all in/in isotonic solutions and also to hypertensive solutions of glucose.

This solution it is intended for single use. Solution needs to be entered at once after opening of an ampoule. Unused solution should be destroyed.

If necessary treatment is continued tsitikoliny in the form of solution for intake.

Contraindication

Hypersensitivity to medicament components, the raised tone of parasympathetic nervous system.

Side effects

Side reactions arise very seldom (1/10,000), including isolated cases.

Mental disturbances: hallucinations.

from nervous system: severe headache, vertigo.

from a cardiovascular system: AG, arterial hypotension, tachycardia.

from a respiratory system: asthma.

from digestive system: nausea, vomiting, diarrhea.

from the immune system: allergic reactions, including: rash, hyperaemia, dieback, urticaria, purpura, itching, Quincke's disease, acute anaphylaxis.

General disturbances: a fever, reactions in the injection site.

Special instructions

in case of steady intracraneal hemorrhage should not exceed a dose of 1000 mg/days and speed of injection of 30 drops in a minute.

Use during pregnancy and feeding by a breast. There are no sufficient data concerning use of a tsitikolin for pregnant women. Data on excretion of a tsitikolin in breast milk and to its action on a fruit are absent. Therefore during pregnancy and feeding a breast medicament is appointed only when the expected advantage for mother exceeds potential risk for a fruit.

Children. Experience of use of medicament for children is limited. Drug is used in urgent cases when the expected advantage of use exceeds possible risk.

Ability to influence speed of response at control of vehicles or work with other mechanisms. In some cases some side reactions from central nervous system can affect ability to run vehicles or to work with mechanisms.

Interaction

Tsitikolin enhances effect of a levodopa. it is not necessary to appoint medicament along with the medicines containing Meclofenoxatum.

Incompatibility. Not to apply the solvents specified in the section USE.

Cases of overdose are not described by

.

Storage conditions

At a temperature not above 30 °C.