Pharmacological properties of the drug Ceraxon
Citicoline stimulates the biosynthesis of structural phospholipids in neuronal membranes, which improves membrane function, including the functioning of ion exchange pumps and neuroreceptors. Due to its stabilizing effect on the membrane, citicoline has anti-edematous properties and reduces cerebral edema. Citicoline reduces the severity of symptoms of cerebral dysfunction after pathological processes such as traumatic brain injury or acute cerebrovascular accidents. Citicoline reduces the level of amnesia, improves the condition of cognitive, sensory and motor disorders, and also weakens the severity of symptoms that are observed with hypoxia and cerebral ischemia, including memory impairment, emotional lability, and impaired ability to perform normal self-care activities. Citicoline is a natural compound found in the human body, so classical pharmacokinetic studies cannot be performed due to the difficulty of quantifying exogenous and endogenous citicoline. During a pharmacokinetic study, its almost complete absorption in the gastrointestinal tract was determined - less than 1% of the dose taken was detected in the feces within 5 days after taking the drug. Two peaks of radioactivity were also noted in the blood plasma, due to metabolism in the liver and intestines: the first - after 1 hour, the second - after 24 hours. Bioavailability by oral and parenteral routes of administration is almost the same. Excretion is very slow, mainly through the respiratory system and urine. After 5 days of administration, about 16% of the drug dose was detected, which indicates the inclusion of the rest of the dose in metabolic processes.
Ceraxon tablets: composition and action
Ceraxon is sold in several forms:
- injections;
- pills;
- solution for systemic use.
The tablets contain the main active ingredient – citicoline sodium. In addition to this, the composition includes:
- talc;
- castor oil;
- magnesium stearate.
Tablets are packed in 5 pieces in a blister, each box contains 4 blisters. The solution intended for drinking contains the same basic substance - citicoline, and along with it glycerin, sorbidol, sodium citrate, sodium saccharinate, strawberry flavoring. This composition is packaged in unpainted glass bottles with plastic caps. The volume of one bottle is 30 ml. It is convenient to dose using the syringe included in each package.
The drug for administration into a vein is packaged in glass ampoules, with a break line marked. One cardboard package can contain 3 or 5 pieces. Ceraxon mainly acts on brain cells, strengthening membranes, improving the functions of ion exchange pumps of the nervous system, which is due to the production of phospholipids.
In case of severe swelling, the action of the drug relieves pressure at the site of the lesion, which returns the cognitive functions of the brain. In addition, the ability to concentrate is restored and memory improves. If Cerakson is applied promptly at the first symptoms of a stroke, it will be possible to minimize the area of spread of necrotic tissue.
Citicoline is one of the constant elements of the human body, which does not make it possible to evaluate its pharmacokinetics. The substance entering through the gastrointestinal tract is absorbed almost completely. As a rule, 1-2% of the total ingested volume remains unabsorbed. Citicoline is excreted through the kidneys in the urine.
As a result of hepatic metabolism processes, two substances are formed: cytidine and choline. Citicoline is first concentrated in the structures and tissues of the brain. At the same time, fractions of the resulting choline pass into phospholipids, and cytidine derivatives into the composition of nucleic acids.
Use of the drug Ceraxon
The solution for oral use in adults is prescribed 200 mg (2 ml) orally 3 times a day. For children, the drug can be prescribed orally from the moment of birth - 100 mg (1 ml) 2-3 times a day. The duration of treatment depends on the severity of the brain damage. The minimum recommended period is 45 days. The dose of the drug and the duration of treatment can be changed by the doctor. The drug, pre-mixed with a small amount of water, is taken using a dosing syringe. It is necessary to rinse the dosing syringe with water after each use. IV or IM administration In acute and emergency conditions, the maximum therapeutic effect is achieved when the drug is administered in the first 24 hours. IV is administered slowly (injection duration - 5 minutes) or drip (infusion rate - 40-60 drops per minute) . Treatment begins with prescribing the drug for the first 2 weeks, 500–1000 mg (depending on the patient’s condition) 2 times a day intravenously. Then - 500–1000 mg 2 times a day IM. The maximum daily dose is 2000 mg. If necessary, treatment is continued with the drug in the form of an oral solution. The recommended duration of treatment, at which the maximum therapeutic effect is noted, is 12 weeks. It is recommended for children to prescribe Ceraxon in the form of a solution for oral use.
When is Cerakson prescribed?
Treatment with Ceraxon is indicated in the following cases:
- first 4 hours during primary stroke;
- for rehabilitation after a stroke;
- emergency assistance and to restore the condition impaired as a result of severe head injury;
- cerebrovascular diseases that reduce cognitive function and provoke behavioral changes.
If the patient was administered Ceraxon in the first hours after a traumatic brain injury, the duration of post-traumatic coma will be less than without the help of the drug. In addition, there is a high probability of reducing the severity of neurological abnormalities typical of this type of injury.
If chronic hypoxia has become the reason for the predominance of lack of initiative in a person’s behavior, complete inability in matters of self-care, the drug effectively affects certain areas of the brain, restoring cognitive functions.
Special instructions for the use of the drug Ceraxon
There are no age restrictions for oral use of the drug. Pregnancy and lactation Although no evidence of risk to the fetus has been obtained when using the drug, during pregnancy the drug is used only when the expected benefit outweighs the potential risk. There are no data on the passage of citicoline into breast milk and its effect on the fetus is unknown. Effect on the ability to drive vehicles and operate complex mechanisms. Citicoline does not affect the ability to drive vehicles and operate complex mechanisms.
Contraindications for use
If, as a result of diagnosing the patient’s condition, the following features are revealed, Cerakson is not prescribed:
- individual intolerance to one of the components of the drug;
- tone of the autonomic nervous system, in its parasympathetic part;
- hereditary fructose intolerance.
Adverse reactions during treatment with Cerakson are extremely rare, among them are:
- coordination problems;
- pain in the occipital region;
- diarrhea;
- appetite disorders;
- insomnia;
- rash.
Sometimes short-term changes in blood pressure are observed, as well as loss of sensation, mainly in the arm and leg on the paralyzed side, if the patient has suffered a stroke.
If any of these reactions occur, you should discuss changing the course of therapy with your doctor.
Buy Ceraxon solution for internal use 100 mg/ml 30 ml in pharmacies
Oral solution in the form of a clear, colorless liquid with a characteristic strawberry odor. Indications : acute period of ischemic stroke (as part of complex therapy); — recovery period of ischemic and hemorrhagic strokes; — traumatic brain injury, acute (as part of complex therapy) and recovery period; — cognitive and behavioral disorders in degenerative and vascular diseases of the brain. Dosage regimen The drug is taken with meals or between meals. Before use, the drug can be diluted in a small amount of water (120 ml or 1/2 cup). Acute period of ischemic stroke and traumatic brain injury: the recommended dose is 1000 mg (10 ml or 1 sachet) every 12 hours. Duration of treatment is at least 6 weeks. Recovery period of ischemic and hemorrhagic strokes, recovery period of traumatic brain injury, cognitive and behavioral disorders in degenerative and vascular diseases of the brain: the recommended dose is 500-2000 mg/day (5-10 ml 1-2 times/day or 1 sachet ( 1000 mg) 1-2 times/day). The dose and duration of treatment depend on the severity of the symptoms of the disease. Elderly patients do not require dose adjustment of Ceraxon®. Rules for using a dosing syringe 1. Place the dosing syringe in the bottle (the syringe plunger is completely lowered). 2. Carefully pull the plunger of the dosing syringe until the solution level is equal to the corresponding mark on the syringe. 3. Before taking, the required amount of solution can be diluted in 1/2 glass of water (120 ml). After each use, it is recommended to rinse the dosing syringe with water. Rules for using the drug in sachets 1. Holding the sachet vertically, carefully tear off its edge along the o. 2.The contents of the sachet can be drunk immediately after opening or before use can be diluted in 1/2 glass of water (120 ml). Side effects Very rare (<1/10,000) (including individual cases): allergic reactions (rash, itching, anaphylactic shock), headache, dizziness, feeling of heat, tremor, nausea, vomiting, diarrhea, hallucinations, swelling, shortness of breath , insomnia, agitation, loss of appetite, numbness in paralyzed limbs, changes in the activity of liver enzymes. In some cases, Ceraxon® can stimulate the parasympathetic system and also cause a short-term change in blood pressure. If any of the side effects indicated in the instructions get worse, or any other side effects not listed in the instructions are noticed, you should inform your doctor. Contraindications for use : severe vagotonia (predominance of the tone of the parasympathetic part of the autonomic nervous system); - children and adolescents under 18 years of age (due to the lack of sufficient clinical data); - rare hereditary diseases associated with fructose intolerance; - hypersensitivity to the components of the drug. Use during pregnancy and lactation There is not enough clinical data on the use of citicoline during pregnancy. Although experimental studies on animals have not revealed any negative effects, during pregnancy the drug is prescribed only when the expected benefit of therapy for the mother outweighs the potential risk to the fetus. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided, since there is no data on the excretion of citicoline in breast milk. Use in children Contraindicated in children and adolescents under 18 years of age. Use in elderly patients Elderly patients do not require dose adjustment of Ceraxon®. Special instructions In the solution for oral administration in the cold, a small amount of crystals may form due to temporary partial crystallization of the preservative. With further storage under recommended conditions, the crystals dissolve within several months. The presence of crystals does not affect the quality of the drug. Impact on the ability to drive vehicles and operate machinery During treatment, patients should be careful when performing potentially dangerous activities that require special attention and speed of psychomotor reactions (including driving a car and other vehicles, working with moving mechanisms, working as a dispatcher and operator). Overdose Due to the low toxicity of the drug, cases of overdose have not been described. Drug interactions Citicoline enhances the effects of levodopa. Ceraxon® should not be prescribed concomitantly with medications containing meclofenoxate. Conditions and periods of storage The drug should be stored out of the reach of children at a temperature not exceeding 30°C. Shelf life: 3 years. Conditions for dispensing from pharmacies The drug is dispensed with a prescription.
