Farmaxon
Ukraine
Table of Contents
INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT PHARMAXON
Composition:
Active substance: citicoline;
1 ml contains 250 mg of citicoline in the form of sodium salt;
Excipients: diluted hydrochloric acid or sodium hydroxide, water for injections.
Pharmaceutical form. Solution for injection.
Main physicochemical properties: clear, colorless liquid.
Pharmacotherapeutic group. Psychostimulants, drugs used in attention deficit hyperactivity disorder (ADHD), nootropic agents. Other psychostimulant and nootropic agents. ATC code N06B X06.
Pharmacological Properties
Pharmacodynamics
Citicoline stimulates the biosynthesis of structural phospholipids in neuronal membranes, as confirmed by magnetic resonance spectroscopy data. Due to this mechanism of action, citicoline improves the functioning of membrane mechanisms such as ion pump activity and receptors, the modulation of which is essential for normal nerve impulse conduction.
Due to its stabilizing effect on neuronal membranes, citicoline exhibits properties that promote reduction of brain edema.
Experimental studies have shown that citicoline inhibits the activation of certain phospholipases (A1, A2, C, and D), reduces the formation of free radicals, prevents the destruction of membrane systems, and preserves antioxidant defense systems such as glutathione.
Citicoline preserves neuronal energy reserves, inhibits apoptosis, and stimulates acetylcholine synthesis.
It has been experimentally demonstrated that citicoline also exerts a preventive neuroprotective effect in focal cerebral ischemia.
Clinical studies have shown that citicoline significantly enhances functional recovery in patients with acute ischemic stroke, which correlates with a slowed progression of ischemic brain damage as observed in neuroimaging.
In patients with traumatic brain injury, citicoline accelerates recovery and reduces the duration and severity of post-traumatic syndrome.
Citicoline improves levels of attention and consciousness, as well as cognitive and neurological deficits associated with cerebral ischemia, and helps reduce symptoms of amnesia.
Pharmacokinetics
After administration, a significant increase in plasma choline levels is observed. The drug is metabolized in the intestine and liver, forming choline and cytidine.
Following administration, citicoline is widely distributed into 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 integrates into cellular, cytoplasmic, and mitochondrial membranes, becoming incorporated into the phospholipid fraction.
Only a small amount of the administered dose is excreted in urine and feces (less than 3%). Approximately 12% of the dose is eliminated as exhaled CO₂. Renal excretion of the drug occurs in two phases: the first phase lasting 36 hours, during which the elimination rate decreases rapidly, and a second phase, during which elimination proceeds much more slowly. The same biphasic pattern is observed in elimination via the respiratory tract. The rate of CO₂ elimination decreases rapidly, within approximately 15 hours, and then declines much more slowly.
Clinical characteristics.
Indications.
- Stroke, acute phase of cerebral circulation disorders and treatment of complications and consequences of cerebral circulation disorders.
- Traumatic brain injury and its neurological consequences.
- Cognitive disorders and behavioral disturbances due to chronic vascular and degenerative cerebral disorders.
Contraindications.
- Hypersensitivity to the components of the drug.
- Increased tone of the parasympathetic nervous system.
Interaction with other medicinal products and other forms of interaction.
Pharmaxon potentiates the effect of levodopa. The drug should not be administered concurrently with medicinal products containing meclophenoxate.
Special precautions.
When administered intravenously, the drug should be injected slowly (over 3–5 minutes, depending on the dose administered).
When administered by intravenous infusion, the infusion rate should be 40–60 drops per minute.
In cases of persistent intracranial hemorrhage, the dose should not exceed 1000 mg per day and the intravenous infusion rate should not exceed 30 drops per minute.
Use during pregnancy or breastfeeding.
There are insufficient data on the use of Farmaxon in pregnant women. Data on the excretion of citicoline into breast milk and its effects on the fetus are unknown. Therefore, during pregnancy or breastfeeding, the drug should be prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus.
Ability to affect reaction speed when driving or operating machinery.
In individual cases, certain adverse reactions affecting the central nervous system may impair the ability to drive or operate complex machinery.
Method of Administration and Dosage.
The recommended dose for adults is from 500 mg to 2000 mg per day depending on the severity of symptoms.
For intravenous or intramuscular administration. For intravenous use, administer as a slow injection (over 3-5 minutes depending on the dose administered) or by intravenous infusion drip (40-60 drops per minute).
Maximum daily dose – 2000 mg.
The duration of treatment depends on the course of the disease and is determined by the physician.
Elderly patients do not require dose adjustment.
The injection solution is intended for single use only. The medication should be used immediately after opening the ampoule. Any unused portion must be discarded. The drug may be mixed with all isotonic solutions for intravenous administration, as well as with hypertonic glucose solution. If necessary, treatment may be continued with the oral solution form of the drug.
Instructions for handling the ampoule.
- Detach one ampoule from the pack and shake it, holding by the neck (Fig. 1).
- Hold the ampoule firmly in hand (ensuring no leakage of the drug) and twist off the top with a rotating motion (Fig. 2).
- Immediately connect the syringe to the opening formed (Fig. 3).
- Invert the ampoule and slowly draw the contents into the syringe (Fig. 4).
- Attach the needle to the syringe.
Fig. 1 Fig. 2 Fig. 3 Fig. 4
Children.
Experience with the use of the drug in children is limited.
Overdose.
Due to the low toxicity of the medicinal product, intoxication is not expected even if therapeutic doses have been accidentally exceeded.
In case of accidental overdose, symptomatic treatment should be administered.
Adverse Reactions
Adverse reactions occur very rarely (< 1/10,000), including isolated cases.
Psychiatric disorders: hallucinations.
Central and peripheral nervous system disorders: severe headache, vertigo.
Cardiovascular disorders: arterial hypertension, arterial hypotension.
Respiratory system disorders: dyspnea.
Gastrointestinal disorders: nausea, vomiting, intermittent diarrhea.
Skin and subcutaneous tissue disorders: rash, hyperemia, exanthema, purpura.
General reactions: chills, edema.
Reporting suspected adverse reactions
Reporting suspected adverse reactions after marketing authorization is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and pharmaceutical staff, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.
Shelf life. 2 years.
After opening, the solution in the ampoule must not be stored.
Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.
Incompatibility. Do not use solvents not specified in the section "Administration and dosage".
Packaging. 2 ml or 4 ml in ampoules, pack of 5.
Prescription status. Prescription only.
Manufacturer.
LLC "FARMASEL".
Manufacturer's address and place of business.
3, Prorizna St., Kvitneve, Brovary District, Kyiv Oblast, 07408, Ukraine.