Citicoline
Citicoline: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. Use in the elderly
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Citicoline
ATX code: N06BX06
Active ingredient: citicoline (Citicoline)
Manufacturer: Ozone, LLC (Russia)
Description and photo update: 2019-10-07
Prices in pharmacies: from 449 rubles.
Buy
Citicoline is a nootropic agent.
Release form and composition
The drug is produced in the form of a solution for intravenous (i / v) and intramuscular (i / m) administration: colorless transparent liquid (4 ml in an ampoule of colorless neutral glass with a colored dot and a notch or with a colored break ring or without a colored dot, notch and ring break, 3 or 5 ampoules in a blister strip made of polyvinyl chloride film and aluminum foil or polymer film or without film and foil, or 3, 5 ampoules in a cardboard form (tray) with cells for stacking ampoules, in a cardboard package 1 or 2 blisters or cardboard trays with or without an ampoule scarifier / knife, as well as instructions for the use of Citicoline).
1 ml of solution contains:
- active substance: citicoline sodium - 130.63 or 261.3 mg, which is equivalent to citicoline in the amount of 125 and 250 mg, respectively;
- additional components: hydrochloric acid 1 M or sodium hydroxide 1 M - up to a pH level of 6.7-7.1; water for injections.
Pharmacological properties
Pharmacodynamics
Citicoline belongs to the precursors of key ultrastructural constituents of the cell membrane, mainly phospholipids. The main component of the drug demonstrates a wide spectrum of action: it participates in the restoration of damaged cell membranes, inhibits the activity of phospholipases, prevents excessive formation of free radicals, and also, by influencing the mechanisms of apoptosis, prevents cell death.
In the acute stage of stroke, citicoline reduces the amount of damage to the brain substance and improves the quality of cholinergic transmission. In the case of traumatic brain injury (TBI), it reduces the severity of neurological symptoms and the duration of post-traumatic coma, and helps to shorten the recovery period.
Against the background of chronic hypoxia of the brain, the use of citicoline is effective in the treatment of such cognitive disorders as impairment of memory functions, lack of initiative, difficulties arising in self-care and performing daily activities. The active substance helps to increase the level of consciousness and attention, as well as to weaken the clinical manifestations of amnesia.
Pharmacokinetics
Citicoline is distributed in a large volume in various structures of the brain with intensive incorporation of the choline fraction into structural phospholipids and cytidine fractions - into nucleic acids and cytidine nucleotides. In the brain, the active substance is actively introduced into the membranes of cells, mitochondria and cytoplasm, forming one of the parts of the structural phospholipid fraction.
The drug metabolism occurs in the liver tissues, as a result of its biotransformation, cytidine and choline are formed. After the administration of the drug, the plasma level of choline in the blood increases significantly.
Because the human body is eliminated about 15% of the administered dose citicoline, of which less than 3% - faeces and urine, about 12% - with exhaled CO 2. The excretion of the active substance in the urine is divided into 2 phases, the first of which lasts approximately 36 hours and is characterized by a rapid decrease in the rate of excretion, and the second - a much slower decrease. The same is observed and when the excretion of the drug via the respiratory tract, rate of excretion in exhaled CO 2 rapidly decreases after approximately 15 hours and then decreases much more slowly.
Indications for use
- acute stage of ischemic stroke (cerebral infarction) (as part of a combination treatment);
- recovery period after ischemic and hemorrhagic stroke;
- TBI, including both acute (as part of complex therapy) and recovery period;
- cognitive and behavioral disorders due to degenerative and vascular lesions of the brain.
Contraindications
Absolute:
- severe vagotomy (dominance of the patient's tone of the parasympathetic part of the autonomic nervous system);
- breast-feeding;
- age up to 18 years;
- hypersensitivity to any component of the drug.
The drug should be used with caution during pregnancy and only in cases where the expected benefit of the treatment to the mother significantly outweighs the possible threat to the fetus.
Citicoline, instructions for use: method and dosage
Citicoline is intended for intravenous and intramuscular administration.
The solution is administered intravenously by slow, over 3-5 minutes (taking into account the prescribed dose), intravenous injection or drip intravenous infusion at a rate of 40-60 drops per minute. IV administrations are preferred over i / m. When carrying out intramuscular injections, it is required to avoid injections of the drug in the same place.
Recommended dosage regimen:
- acute stage of ischemic stroke and TBI: every 12 hours at a dose of 1000 mg, course of therapy - at least 6 weeks; 3-5 days after the start of treatment (if the swallowing function is not impaired), it is possible to transfer the patient to oral forms of citicoline;
- recovery period after TBI or ischemic and hemorrhagic strokes, cognitive and behavioral disorders against the background of degenerative and vascular brain lesions: 1-2 times a day at a dose of 500-2000 mg; the duration of therapy and the dosage is set taking into account the severity of the symptoms of the disease.
The solution contained in the ampoule is intended for single use only and should be injected immediately after opening the ampoule.
Side effects
All of the following undesirable effects were observed during the period of therapy with Citicoline very rarely:
- mental disorders: agitation, insomnia, hallucinations;
- nervous system: dizziness, headache, tremors, reactions from the parasympathetic system, numbness in paralyzed limbs;
- vessels: arterial hypotension / hypertension;
- skin and subcutaneous tissues: pruritus, rash, hyperemia, purpura, urticaria, anaphylactic shock;
- respiratory system, chest and mediastinal organs: shortness of breath;
- digestive system: nausea, loss of appetite, vomiting, diarrhea;
- liver and biliary tract: changes in the activity of liver enzymes;
- general disorders and disorders at the injection site: feeling of heat, chills, edema.
Overdose
Due to the low toxicity of Citicoline, no cases of overdose have been recorded. If an accidental overdose has occurred, symptomatic treatment is prescribed.
special instructions
With persistent intracranial bleeding, it is not recommended to use the drug in a dose exceeding 1000 mg per day; the solution should be injected intravenously slowly, at a rate of 30 drops per minute.
Influence on the ability to drive vehicles and complex mechanisms
Patients driving a car or other vehicles should be careful during therapy.
Application during pregnancy and lactation
Sufficient data on the use of Citicoline in pregnant women are not available. Despite the fact that preclinical studies have not revealed the negative effect of the drug on animals, during pregnancy it should be used only in cases where the intended benefits of treatment for the mother significantly exceed the possible threat to the fetus.
If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued, since there is no information about the excretion of citicoline with breast milk in women, and therefore the risk to the child's health cannot be completely excluded.
Pediatric use
For patients under 18 years of age, treatment with Citicoline is contraindicated due to the lack of sufficient clinical data confirming the safety and effectiveness of its administration in children and adolescents.
Use in the elderly
Elderly patients do not need individual dose selection of citicoline.
Drug interactions
The drug can be combined with all types of intravenous isotonic solutions and dextrose solutions.
It is not recommended to use Citicoline concurrently with medicinal products containing meclofenoxate.
Citicoline increases the effects of levodopa.
Analogs
Citicoline analogs are: Neipilept, Noocil, Neurocholine, Ceraxon, Recognan, Proneiro, Ronocyte, Ceresil Canon, Quinel, Encetron-SOLOpharm, etc.
Terms and conditions of storage
Store out of the reach of children, protected from sunlight, at a temperature not exceeding 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Citicoline
Reviews of Citicoline are mostly positive. Patients note the effectiveness of using the drug during the recovery period after stroke and TBI, as well as in cognitive and behavioral disorders associated with vascular and degenerative brain lesions.
However, there are also reviews with complaints about the development of side effects, in most cases, such as dizziness, insomnia, headache, agitation, stimulation of the parasympathetic part of the nervous system, sometimes expressed to a large extent and causing the drug to be discontinued.
The price of Citicoline in pharmacies
There is no reliable information on the price of Citicoline, since the drug is not sold in pharmacies at the moment. The cost of an analogue of the drug, Ceraxon, solution for intravenous and intramuscular administration (1000 mg / 4 ml) can be 1000–1100 rubles. per package containing 4 ampoules.
Citicoline: prices in online pharmacies
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Drug name Price Pharmacy |
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Citicoline 250 mg / ml solution for intravenous and intramuscular administration 4 ml 5 pcs. 449 r Buy |
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Citicoline 125 mg / ml solution for intravenous and intramuscular administration 4 ml 5 pcs. 474 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
