NEUROXON

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT NEUROXON® (NEUROXON®)

Composition:

Active substance: citicoline;

1 ml of solution contains sodium citicollinate, calculated as citicoline – 100 mg;

Excipients: methylparaben (E 218); propylparaben (E 216); potassium sorbate; glycerol; sorbitol (E 420); glycerinformal; sodium citrate; sodium saccharin; citric acid monohydrate; purified water.

Pharmaceutical form. Oral solution.

Main physicochemical properties: clear liquid, yellowish or colorless, with a characteristic odor. Slight opalescence may occur.

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

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 function of membrane mechanisms such as ion-exchange pumps and receptors, modulation of which is necessary for normal nerve impulse conduction.

Due to its stabilizing effect on neuronal membranes, citicoline exhibits anti-edematous properties, which contribute to reducing 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.

It has been experimentally proven that citicoline also exerts a prophylactic 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 of the ischemic brain damage volume, 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, cognitive and neurological disorders associated with cerebral ischemia, and helps reduce symptoms of amnesia.

Pharmacokinetics.

Citicoline is almost completely absorbed after oral administration. After administration, a significant increase in plasma choline levels is observed. The drug is metabolized in the intestine and liver, forming choline and cytidine.

After 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 part of the phospholipid fraction.

Only a negligible amount of the dose is found in urine and feces (less than 3%). Approximately 12% of the dose is excreted as exhaled CO₂. During excretion 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 during excretion via the respiratory tract. The rate of CO₂ elimination decreases rapidly, approximately within 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 citicoline or to other components of the drug.
• Increased parasympathetic nervous system tone.

Interaction with other medicinal products and other forms of interactions.
Citicoline enhances the effect of levodopa. It should not be administered concurrently with medicinal products containing meclofenoxate.

Special precautions for use.

Patients with hereditary fructose intolerance should not take Neuroxon, oral solution, as the product contains sorbitol. Methylparahydroxybenzoate and propylparahydroxybenzoate contained in the formulation may cause allergic reactions (usually of the delayed type).

Use during pregnancy or breastfeeding.

There are insufficient data on the use of citicoline in pregnant women. Data regarding excretion of citicoline in breast milk and its effect on the fetus are unknown. The medicinal product may be prescribed during pregnancy or breastfeeding only when the expected therapeutic benefit for the mother outweighs the potential risk to the fetus.

Ability to influence reaction rate when driving or operating machinery. In individual cases, certain adverse reactions affecting the central nervous system may influence the ability to drive or operate complex machinery.

Method of Administration and Dosage.

For oral use. The recommended dose of the medicinal product NEUROXON®, oral solution, for adults is from 500 mg (5 ml) to 2000 mg (20 ml) per day, divided into 2–3 doses, depending on the severity of symptoms.

The medicinal product should be administered using the provided dosing syringe as follows:

• before use, fully depress the plunger of the dosing syringe;
• pull back the plunger and draw up the required dose, ensuring that the volume of liquid in the syringe corresponds to the prescribed dose;
• the medicinal product may be taken directly or diluted in half a glass of water (120 ml), independent of food intake.

The dosing syringe must be rinsed with water after each use.

Dosage and duration of treatment depend on the severity of brain damage and are determined individually by the physician.

Elderly patients do not require dose adjustment.

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

Overdose. Cases of overdose have not been reported.

Side effects.

Side effects occur very rarely (<1/10,000), including isolated cases.

Psychiatric disorders: hallucinations.

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

Cardiovascular system 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 disorders: chills, edema.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 30 °C. Keep out of reach of children. Do not freeze and do not refrigerate! During storage, slight opalescence may occur, which disappears when the preparation is kept at room temperature (≈ 20 °C).

Incompatibility. Unknown.

Packaging. 45 ml in glass bottles, stoppered with caps. Labels are affixed to the bottles. Each bottle, together with a dosing device, is placed into a carton.

Prescription status. Prescription only.

Manufacturer. JSC "Halychpharm".

Manufacturer's address and place of business. 6/8 Opryshkovska Street, Lviv, 79024, Ukraine.