Cytikolin - instructions for use, dose, side effects, contraindications

Nootropic agent. Citicoline, being the predecessor of the key ultrastructural components of the cell membrane (mainly phospholipids), has a wide spectrum of action: it helps to restore damaged cell membranes, inhibits the effect of phospholipases, prevents excessive formation of free radicals, and also prevents cell death by affecting the mechanisms of apoptosis.

In an acute period of stroke reduces the volume of damaged tissue, improves cholinergic transmission.

With craniocerebral trauma reduces the duration of post-traumatic coma and the severity of neurologic symptoms.

Citicoline improves symptoms of hypoxia: memory impairment, emotional lability, lack of initiative, difficulties in performing daily activities and self-service. Effective in the treatment of cognitive, sensory and motor neurologic disorders of degenerative and vascular etiology.

Pharmacokinetics:

Suction. Citicoline is well absorbed by intravenous and intramuscular injection. Absorption after oral administration is almost complete, and bioavailability is almost the same as after intravenous administration.

Metabolism. With intravenous and intramuscular injection citicoline metabolized in the liver with the formation of choline and cytidine. After the administration of choline concentration in the blood plasma significantly increased.

Distribution. Citicoline is largely distributed in the structures of the brain, with the rapid introduction of choline fractions into structural phospholipids and cytidine fractions into cytidine nucleotides and nucleic acids. Citicoline penetrates into the brain and actively integrates into cellular, cytoplasmic and mitochondrial membranes, forming part of the fraction of structural phospholipids.

Excretion. Only 15% of the administered dose of citicoline is excreted from the human body; less than 3% - by the kidneys and about 12% - with exhaled CO₂.

In the excretion of citicoline with urine, two phases can be identified: the first phase, lasting about 36 hours, during which the rate of elimination rapidly decreases, and the second phase, during which the rate of excretion decreases much more slowly. The same is observed in exhaled CO₂ - the elimination rate decreases rapidly after about 15 hours, and then decreases much more slowly.

Indications:

Ischemic stroke (acute period); ischemic and hemorrhagic stroke (recovery period); craniocerebral trauma (acute and recovery period); Cognitive impairment in degenerative and cerebrovascular diseases of the brain.

ICD-10

XIX.T90-T98.T90.5 Consequences of intracranial injury

IX.I60-I69.I69.3 Consequences of a cerebral infarction

IX.I60-I69.I69.1 Consequences of intracranial hemorrhage

V.F00-F09.F06.7 Mild cognitive impairment

V.F00-F09.F07 Personality and behavioral disorders due to illness, damage or dysfunction of the brain

V.F90-F98.F91 Behavioral disorders

IX.I60-I69.I61 Intracerebral haemorrhage

IX.I60-I69.I63 Cerebral infarction

IX.I60-I69.I67.9 Cerebrovascular disease, unspecified

XIX.S00-S09.S06 Intracranial injury

Contraindications:

Vagotonia (predominance of the tone of the parasympathetic part of the autonomic nervous system); children and adolescents under 18; hypersensitivity to citicoline.

Carefully:

Pregnancy and lactation.

Pregnancy and lactation:

In pregnancy, use is only possible if the expected benefit of therapy for the mother exceeds the potential risk to the fetus.

If it is necessary to use citicoline during lactation, the question of stopping breastfeeding should be resolved, since there is no data on the isolation of citicoline with breast milk.

Dosing and Administration:

When ingestion - 200-300 mg 3 times a day.

Intravenously with strokes and craniocerebral trauma in the acute period - 1-2 grams per day, depending on the severity of the disease for 3-7 days, followed by a transition to intramuscular injection or ingestion.

Intramuscularly at 0.5-1 g per day.

Side effects:

From the side CNS and peripheral nervous system: insomnia, headache, dizziness, agitation, tremor, numbness in the paralyzed limbs.

From the side digestive system: nausea, decreased appetite, changes in hepatic enzyme activity.

Allergic reactions: rash, skin itching, anaphylactic shock.

Other: heat; in some cases - a short-term hypotensive effect, stimulation of the parasympathetic nervous system.

Overdose:

Given the low toxicity of the drug, overdose cases have not been described.

Interaction:

Do not use citicoline simultaneously with drugs containing meclophenoxate.

Citicoline enhances the effects of L-dihydroxyphenylalanine.

Citicoline increases the effects of levodopa.

Special instructions:

During the treatment period, care should be taken when carrying out potentially hazardous activities requiring special attention and quick reactions (driving and other vehicles, working with moving mechanisms, dispatcher and operator work, and the like).

Solution for oral administration (optional).In the cold, a small amount of crystals may form due to the temporary partial crystallization of the preservative. With further storage under the recommended conditions, the crystals dissolve within a few months. The presence of crystals does not affect the quality of the drug.

Instructions

Citicoline (Citicolinum)