Novaxon

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT NOVAXON (NOVAXON)

Composition:

Active substance: citicoline sodium;

1 vial (4 ml) contains citicoline sodium equivalent to citicoline 500 mg or 1000 mg;

Excipients: hydrochloric acid concentrated or sodium hydroxide, water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless solution.

Pharmacotherapeutic group. Psychostimulants, drugs used in attention deficit hyperactivity disorder (ADHD), nootropic agents. Other psychostimulant and nootropic agents.

ATC code N06BX06.

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-exchange pumps and receptors, the modulation of which is necessary for normal nerve impulse conduction.

Thanks to its stabilizing effect on neuronal membranes, citicoline exhibits anti-edematous properties, which contribute to a reduction in cerebral 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 maintains neuronal energy reserves, inhibits apoptosis, and stimulates acetylcholine synthesis.

Experimental evidence has 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 slowing of the growth in volume of ischemic brain damage as demonstrated by 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 dose is found in urine and feces (less than 3%). Approximately 12% of the dose is excreted as exhaled CO₂. During the elimination of the drug in urine, two phases are observed: the first phase—within 36 hours—during which the elimination rate decreases rapidly, and the second phase, during which the elimination rate decreases 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 cerebrovascular and degenerative cerebral disorders.

Contraindications.

• Hypersensitivity to citicoline or to other components of the medicinal product.
• Increased tone of the parasympathetic nervous system.

Interaction with other medicinal products and other forms of interaction.

Citicoline enhances the effect of levodopa. The drug should not be administered simultaneously with medicinal products containing meclofenoxate.

Special precautions for use.

When administered intravenously, the medicinal product should be given 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 (30 drops per minute).

This medicinal product contains 4.096 mmol (or 94.2 mg) of sodium per 2000 mg dose of citicoline. Caution should be exercised when administering the product to patients on a sodium-restricted diet.

Use during pregnancy or breastfeeding.

Adequate data on the use of citicoline in pregnant women are lacking. Data regarding the excretion of citicoline in breast milk and its effects on the fetus are unknown. During pregnancy or breastfeeding, the medicinal product should be prescribed only if the expected therapeutic benefit for the mother outweighs the potential risk to the fetus.

Ability to influence 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.

The medicinal product should be administered by intramuscular or intravenous injection. For intravenous administration, the medicinal product may be given as a slow intravenous injection (over 3–5 minutes, depending on the dose administered) or by infusion (rate: 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 medicinal product should be used immediately after opening the vial. Any unused portion must be discarded. The medicinal product 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 formulation.

Children.

Experience with the use of the medicinal product in children is limited.

Overdose.

Cases of overdose have not been reported.

Adverse reactions.

Adverse reactions occur very rarely (<1/10,000), including isolated cases.

Central and peripheral nervous system disorders: severe headache, vertigo, hallucinations.

Cardiovascular system disorders: arterial hypertension, arterial hypotension, tachycardia.

Respiratory system disorders: dyspnea.

Gastrointestinal disorders: nausea, vomiting, diarrhea.

Immune system disorders: allergic reactions, including rash, hyperemia, exanthema, urticaria, purpura, pruritus, angioedema, anaphylactic shock.

General disorders: chills, injection site reactions.

Shelf life. 2 years.

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 "Instructions for use and dosage".

Packaging.

4 ml in vials; 5 vials in a blister pack; 1 or 2 blister packs in a cardboard box.

Prescription status. Prescription only.

Manufacturer. Limited liability company "Novopharm-Biosyntez".

Manufacturer's address and location of business activity.

Ukraine, 11700, Zhytomyr region, Zvyagel district, city of Zvyagel, 38 Zhytomyrska Street.