Instructions for use: Axotilin solution for injection 1000 mg/4 ml ampoule 4 ml cassette No. 10
Composition
active ingredient: citicoline;
1 ampoule (4 ml) contains 1000 mg of citicoline (as citicoline sodium);
Excipients: hydrochloric acid or sodium hydroxide for pH adjustment, water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: clear colorless liquid.
Pharmacotherapeutic group
Psychostimulants, drugs used for attention deficit hyperactivity disorder (ADHD), nootropics. Other psychostimulants and nootropics.
ATX code N06B X06.
Pharmacological properties
Pharmacodynamics
Citicoline stimulates the biosynthesis of structural phospholipids of neuronal membranes. Citicoline improves the functioning of membrane mechanisms such as ion pumps and neuroreceptors, without the regulation of which normal conduction of nerve impulses is impossible. Due to its stabilizing effect on the neuronal membrane, citicoline exhibits anti-edematous properties that contribute to the reabsorption of brain edema.
Citicoline inhibits the activation of certain phospholipases (A1, A2, C, and D), reducing the formation of free radicals, preventing the destruction of membrane systems, and preserving antioxidant defense systems such as glutathione.
Citicoline preserves neuronal energy reserves, inhibits apoptosis, and stimulates acetylcholine synthesis.
Citicoline also has a preventive neuroprotective effect in focal cerebral ischemia.
Citicoline significantly increases functional recovery rates in patients with acute cerebrovascular accident, which coincides with a slowdown in the growth of ischemic brain damage according to neuroimaging data.
In patients with traumatic brain injury, citicoline accelerates recovery and reduces the duration and intensity of post-traumatic syndrome.
Citicoline improves the level of attention and consciousness, helps reduce the manifestations of amnesia, cognitive and neurological disorders associated with cerebral 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 to form choline and cytidine.
After administration, citicoline is widely distributed in brain structures with rapid incorporation of the choline fraction into structural phospholipids and the cytidine fraction into cytidine nucleotides and nucleic acids. In the brain, citicoline is incorporated into cellular, cytoplasmic and mitochondrial membranes, integrating into the structure of the phospholipid fraction.
Only a small amount of the dose is found in the urine and feces (less than 3%). Approximately 12% of the dose is excreted through exhaled CO2. During the excretion of the drug with urine, two phases are distinguished: the first phase - within 36 hours, in which the rate of excretion decreases rapidly, and the second phase - in which the rate of excretion decreases much more slowly. The same phasic nature is observed in excretion through the respiratory tract. The rate of CO2 excretion decreases rapidly, for about 15 hours, then decreases much more slowly.
Indication
Stroke, acute phase of cerebrovascular disorders and complications and consequences of cerebrovascular disorders. Traumatic brain injury and its neurological consequences. Cognitive and behavioral disorders due to chronic vascular and degenerative cerebral disorders.
Contraindication
Hypersensitivity to any component of the drug. Increased tone of the parasympathetic nervous system.
Interaction with other medicinal products and other types of interactions
Enhances the effect of levodopa.
Citicoline can be used simultaneously with hemostatic, anti-edematous drugs and perfusion solutions.
The drug should not be used simultaneously with drugs containing meclofenoxate.
Application features
In the case of intravenous administration, the drug should be administered slowly (over 3-5 minutes depending on the dose administered). In the case of intravenous drip administration, the infusion rate should be 40-60 drops per minute.
In severe and acute cases or with progressive changes in consciousness, simultaneous use with hemostatic drugs, drugs that reduce intracranial pressure, and perfusion solutions is possible.
In case of severe cerebral edema, it is necessary to simultaneously administer drugs that reduce intracranial pressure, such as mannitol and corticosteroids.
In the presence of intracranial hemorrhage, the intravenous infusion rate should not be exceeded (30 drops per minute), high doses should be avoided (more than 500 mg in a single dose and more than 1000 mg per day), as an increase in cerebral blood flow is possible. In this case, it is acceptable to divide the daily dose into 2-3 injections.
Citicoline should not be used as monotherapy, it should be combined with various therapeutic treatments indicated for the different pathological conditions in which it must be administered.
Ability to influence reaction speed when driving vehicles or other mechanisms
In individual cases, some adverse reactions from the central nervous system may affect the ability to drive or operate complex machinery.
Use during pregnancy or breastfeeding
There are insufficient data on the use of citicoline in pregnant women. Data on the excretion of citicoline into breast milk and its effect on the fetus are unknown. During pregnancy or breastfeeding, the drug can be prescribed only if the expected therapeutic benefit to the mother outweighs the potential risk to the fetus or child.
Method of administration and doses
The recommended dose for adults is 500 mg to 2000 mg per day, depending on the severity of symptoms.
The drug is intended for intramuscular or intravenous use. Intravenously, the drug can be administered by slow injection (over 3-5 minutes depending on the dose administered) or drip (rate: 40-60 drops per minute).
The maximum daily dose is 2000 mg.
The duration of treatment depends on the course of the disease and is determined by the doctor.
Elderly patients do not require dose adjustment.
The solution for injection is intended for single use only. The drug should be used immediately after opening the ampoule. Any remaining drug should be discarded. The drug can be mixed with all isotonic intravenous solutions and hypertonic glucose solution.
If necessary, continue treatment with the drug in the form of a solution for oral administration.
Children
Experience with the use of the drug in children is limited.
Overdose
There have been no reports of overdose. In case of accidental overdose with the drug, symptomatic treatment should be carried out.
Adverse reactions
Nervous system: severe headache, vertigo, hallucinations.
Cardiovascular system: arterial hypertension, arterial hypotension, tachycardia.
Respiratory system: shortness of breath.
Digestive tract: nausea, vomiting, diarrhea.
Immune system: allergic reactions, including: rash, hyperemia, exanthema, urticaria, purpura, itching, angioedema, anaphylactic shock.
General reactions: chills, fever, increased sweating, changes at the injection site.
Expiration date
2 years.
Storage conditions
In the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children!
Packaging
4 ml in ampoules; 5 ampoules in a cassette; 2 cassettes in a pack.
Vacation category
According to the recipe.
Producer
Public Joint Stock Company "Research and Production Center "Borshchagov Chemical and Pharmaceutical Plant".
Location of the manufacturer and its business address
Ukraine, 03134, Kyiv, Myru St., 17.
