Neuroxone

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

Composition:

Active substance: citicoline;

1 ampoule contains 1000 mg or 500 mg of citicoline sodium equivalent to citicoline;

Excipients: 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 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, modulation of which is essential for normal nerve impulse conduction.

Thanks to its stabilizing effect on neuronal membranes, citicoline exhibits anti-edematous properties that 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 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 disorders 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.

After administration, citicoline is widely distributed throughout 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 negligible amount of the dose is found in urine and feces (less than 3%). Approximately 12% of the dose is excreted as exhaled CO₂. Renal excretion of the drug occurs in two phases: the first phase lasts up to 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 excretion via the respiratory tract. The rate of CO₂ exhalation decreases rapidly, within approximately 15 hours, and then declines much more slowly.

Clinical characteristics.

Indications.

• Stroke, acute phase of cerebral circulation disorders, 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 any of the excipients.
• Increased parasympathetic nervous system tone.

Interaction with other medicinal products and other forms of interaction.

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

Special precautions for use.

In case of intravenous administration, the drug should be administered slowly (within 3–5 minutes, depending on the administered dose).

When administered intravenously by drip infusion, the infusion rate should be 40–60 drops per minute.

In case of persistent intracranial hemorrhage, the dose should not exceed 1000 mg per day, and the intravenous infusion rate (30 drops per minute) should not be exceeded.

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. The medicinal product may be prescribed during pregnancy or breastfeeding only when the expected therapeutic benefit to the mother outweighs the potential risk to the fetus.

Ability to influence reaction speed when driving vehicles or operating machinery.

In individual cases, certain adverse reactions from the central nervous system may affect the ability to drive vehicles or operate complex machinery.

Dosage and Administration.

The recommended dose for adults is from 500 mg to 2000 mg per day depending on the severity of symptoms.

The drug is intended for intramuscular or intravenous administration. For intravenous use, the drug may be administered slowly by 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 drug 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 formulation of the drug.

Children.

Experience with use 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.

Nervous system and peripheral nervous system: severe headache, vertigo, hallucinations.

Cardiovascular system: arterial hypertension, arterial hypotension, tachycardia.

Respiratory system: dyspnea.

Gastrointestinal tract: nausea, vomiting, diarrhea.

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

General reactions: chills, reactions at the injection site.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 30 °C. Keep out of reach of children.

Packaging. 4 ml in an ampoule, 5 ampoules in a blister, 2 blisters in a carton.

Prescription status. Prescription only.

Manufacturer. JSC "Halychpharm".

Manufacturer's location and address of business activity.

6/8 Opryshkivska Street, Lviv, 79024, Ukraine.