Pharmacological properties
Pharmacodynamics. The active substance of the drug - citicoline - stimulates the biosynthesis of structural phospholipids in the membrane of neurons, helps to improve membrane functions, including the functioning of ion-exchange pumps and neuroreceptors. Due to its stabilizing effect on the membrane, it has anti-edema properties, therefore it reduces brain edema. Research results have shown that citicoline inhibits the activity of some phospholipases, prevents the residual occurrence of free radicals, prevents damage to membrane systems and ensures the preservation of the protective antioxidant system. It also reduces the volume of damaged tissue, preventing cell death by acting on apoptosis mechanisms, and improves cholinergic transmission.
Due to its properties, citicoline:
provides a preventive neuroprotective effect in focal brain strokes; promotes rapid functional rehabilitation of patients with acute cerebral circulation disorders, reducing ischemic damage to brain tissue, which is confirmed by the results of X-ray studies; reduces the duration of the recovery period and reduces the intensity of post-traumatic syndrome in traumatic brain injuries; helps increase the level of brain activity, reduces the level of amnesia, improves the condition in cognitive, sensitive and motor disorders observed in brain ischemia.
Pharmacokinetics. After administration of the drug, a significant increase in the level of choline in the blood plasma is observed. The drug is metabolized in the intestines and liver with the formation of choline and cytidine. After administration, citicoline is absorbed by brain tissues, while cholines act on phospholipids, cytidine - on cytidine nucleoids and nucleic acids. Citicoline quickly reaches brain tissues and is actively incorporated into cell membranes, cytoplasm and mitochondria, activating the activity of phospholipids.
Only a small amount of the administered drug is excreted in the urine and feces (3%) and approximately 12% - through the respiratory tract. The excretion of the drug in the urine and through the respiratory tract has two phases: the first phase - rapid excretion (with urine - during the first 36 hours, through the respiratory tract - during the first 15 hours), the second phase - slow excretion. The main part of citicoline is involved in metabolic processes.
Indication
Acute phase of cerebrovascular disorders and treatment of their consequences. craniocerebral trauma and its consequences. neurological disorders (cognitive, sensitive, motor) caused by cerebral pathology of degenerative and vascular origin.
Application
The drug is administered intravenously or intramuscularly. In the case of intravenous administration, the drug should be administered in the form of a slow intravenous injection (over 3-5 minutes, depending on the dose administered) or a drip intravenous infusion (40-60 drops per minute).
The recommended dose for adults is 500-2000 mg/day. The maximum daily dose is 2000 mg.
In the first 2 weeks, the drug is used at a dose of 500-1000 mg 2 times a day intravenously, then 500-1000 mg 2 times a day intramuscularly.
In acute and emergency conditions, the maximum therapeutic effect is achieved when the drug is administered in the first 24 hours.
The recommended duration of treatment, at which the maximum therapeutic effect is observed, is 12 weeks. If necessary, continue therapy with citicoline in a dosage form for oral administration.
Elderly patients do not require dose adjustment.
The doses of the drug and the duration of treatment depend on the severity of the brain lesions and are set individually.
Contraindication
Hypersensitivity to the active substance or other components of the drug. Increased tone of the parasympathetic nervous system.
Side effects
From the cardiovascular system: angina, arterial hypotension, tachycardia.
From the nervous system and psyche: severe headache, dizziness, hallucinations.
From the respiratory system: dyspnea.
Gastrointestinal tract: nausea, vomiting, diarrhea.
Immune system, skin and subcutaneous tissue disorders: hypersensitivity reactions, including rash, purpura, pruritus, angioedema, anaphylactic shock.
General disorders: chills, edema, fever, increased sweating, changes at the injection site.
Special instructions
The drug should be used immediately after opening the ampoule. The ampoule is intended for single use only. Any remaining drug should be discarded.
In case of persistent intracranial hemorrhage, the dose of citicoline should not exceed 1000 mg/day and the intravenous infusion rate should not exceed 30 drops per minute.
Use during pregnancy and breastfeeding. There are no sufficient data on the use of citicoline in pregnant women. It is not known whether citicoline passes into breast milk. During pregnancy and breastfeeding, the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus.
Children: There are insufficient data on the use of citicoline in children. The drug should be used only when the expected benefit outweighs the potential risk.
Ability to influence the speed of reaction when driving vehicles or other mechanisms. In individual cases, some adverse reactions from the central nervous system may affect the ability to drive vehicles and other mechanisms.
With simultaneous use of citicoline and levodopa, the effect of the latter is enhanced. The drug should not be prescribed simultaneously with drugs containing meclofenoxate.
Incompatibility: The drug should not be mixed with other drugs in the same container.
Overdose
There are no data on cases of drug overdose.
Storage conditions
In the original packaging at a temperature not exceeding 25 °C. Do not freeze.
