Neuroxone

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

Composition:

Active ingredient: citicoline;

One tablet contains 500 mg of citicoline sodium salt (expressed as citicoline);

Excipients: microcrystalline cellulose, sodium croscarmellose, polyoxyl 35 hydrogenated castor oil, magnesium aluminometasilicate with mineral carrier, talc, colloidal anhydrous silica, magnesium stearate, coating mixture "Aquarius Prime BKN318029 White" containing hydroxypropylmethylcellulose, hydroxypropylcellulose, medium-chain triglycerides, titanium dioxide.

Pharmaceutical form. Film-coated tablets.

Main physicochemical properties: white, oval-shaped, biconvex film-coated tablets.

Pharmacotherapeutic group. Psychostimulants, drugs used in attention deficit hyperactivity disorder (ADHD), 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 enhances the functioning of membrane mechanisms such as ion-exchange pumps and receptors, modulation of which is essential for normal nerve impulse conduction. Thanks to its stabilizing effect on neuronal membranes, citicoline exhibits anti-edematous properties that promote reabsorption of brain edema.

Experimental studies have shown that citicoline inhibits the activation of certain phospholipases (A1, A2, C, and D), reducing the formation of free radicals, preventing the destruction of membrane systems, and preserving antioxidant defense systems such as glutathione.

Citicoline preserves neuronal energy reserves, inhibits apoptosis, and stimulates acetylcholine synthesis.

It has been experimentally proven that citicoline also exerts a preventive neuroprotective effect in focal cerebral ischemia.

Clinical studies have demonstrated that citicoline significantly improves functional recovery rates in patients with acute ischemic stroke, consistent with a slowing of ischemic brain lesion progression as shown 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 disorders associated with cerebral ischemia, and helps reduce symptoms of amnesia.

Pharmacokinetics

Citicoline is well absorbed after oral administration. After administration, a significant increase in plasma choline levels is observed. When administered orally, the drug is almost completely absorbed. Studies have shown that bioavailability after oral and intravenous administration is practically equivalent.

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, participating in the formation of phospholipid fractions.

Only a negligible amount of the dose is found in urine and feces (less than 3%). Approximately 12% of the dose is excreted via exhaled CO₂. During elimination, two phases are observed in urinary excretion: the first phase—within 36 hours—during which elimination rate decreases rapidly, and the second phase—during which 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 over approximately 15 hours, then declines much more slowly thereafter.

Clinical characteristics.

Indications.

• Stroke, acute phase of cerebral circulation disorders and their neurological consequences.
• Traumatic brain injury and its neurological consequences.
• Cognitive and behavioral disorders due to chronic cerebrovascular and degenerative cerebral disorders.

Contraindications.

• Hypersensitivity to citicoline or to other components of the drug.
• High tone of the parasympathetic nervous system.

Interaction with other medicinal products and other forms of interaction.

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

Special precautions for use

The medicinal product contains hydrogenated polyoxyl 40 stearate, which may cause gastrointestinal disturbances and diarrhea. Therefore, the drug should be used with particular caution in patients with inflammatory bowel diseases.

This medicinal product contains from 25.5236 mg/tablet to 26.9096 mg/tablet of sodium. Caution should be exercised when administering to patients on a sodium-restricted diet.

Use during pregnancy or breastfeeding

Adequate data on the use of citicoline in pregnant women are lacking. Citicoline should not be used except in cases of urgent medical need. During pregnancy, the drug should be prescribed only when the expected therapeutic benefit outweighs the potential risk. Data on the passage of citicoline into breast milk and its effects on the fetus are unknown.

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 is from 500 to 2000 mg per day (1–4 tablets).

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

Elderly patients do not require dose adjustment.

Children.

Experience with the use of the drug in children is limited; therefore, the medicinal product should be prescribed only when the expected benefit outweighs any potential risk.

Overdose.

Cases of overdose have not been reported.

Side effects.

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

Psychiatric disorders: hallucinations.

Nervous system disorders: severe headache, dizziness.

Cardiovascular disorders: arterial hypertension, arterial hypotension, tachycardia.

Respiratory system disorders: dyspnea.

Gastrointestinal disorders: nausea, vomiting, occasional diarrhea.

Allergic reactions, including rash, pruritus, angioneurotic edema, anaphylactic shock, erythema, urticaria, exanthema, purpura.

General disorders: chills, swelling.

Shelf life. 2 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 ºC. Keep out of reach of children.

Packaging. 10 tablets per blister, 2 or 3 blisters per carton.

Prescription category. Prescription only.

Manufacturer. JSC "Kyivmedpreparat".

Manufacturer's address and location of business activity.

139 Saksaganskogo Street, Kyiv, 01032, Ukraine.