Ceraxon

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

Composition:

Active substance: citicoline;

1 ml of solution contains 104.5 mg of sodium citicoline, equivalent to 100 mg of citicoline;

Excipients: sorbitol 70% (E 420), glycerin, methylparahydroxybenzoate (E 218), propylparahydroxybenzoate (E 216), sodium citrate, sodium saccharin, strawberry flavoring, potassium sorbate, anhydrous citric acid (50% solution) to adjust pH to 6.0, purified water.

Pharmaceutical form. Oral solution.

Main physicochemical properties: colorless clear 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, the modulation of which is essential for normal nerve impulse conduction.

Thanks to its membrane-stabilizing effect, 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 preserves 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 cerebrovascular disorders, 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 manifestations of amnesia.

Pharmacokinetics

Citicoline is almost completely absorbed following 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.

Following 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 small amount of the administered dose is excreted in urine and feces (less than 3%). Approximately 12% of the dose is eliminated via exhaled CO₂. The elimination of the drug in urine occurs in two phases: the first phase lasts 36 hours, during which the elimination rate decreases rapidly, and the second phase, during which the elimination rate declines 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 thereafter.

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 disorders due to chronic vascular and degenerative cerebral disorders.

Contraindications.

• Hypersensitivity to citicoline or to other components of the drug.
• 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.

CERAXONE® oral solution should not be administered to patients with hereditary fructose intolerance, as the product contains sorbitol. Methylparahydroxybenzoate and propylparahydroxybenzoate contained in the formulation may cause allergic reactions (usually of 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 effects on the fetus are unknown. During pregnancy or breastfeeding, the medicinal product should be administered only if the expected therapeutic benefit for the mother outweighs the potential risk to the fetus.

Ability to influence reaction rate while 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.

For oral use. The recommended dose of CERAXONE® oral solution in bottles 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 medication 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 the volume of liquid in the syringe corresponds to the prescribed dose.
• The medication may be taken directly or diluted in half a glass of water (120 ml), independent of food intake.

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

The recommended dose of CERAXONE® oral solution in sachets is 1–2 sachets (10–20 ml) per day, depending on the severity of the disease. The medication should be taken directly from the sachet or diluted in half a glass of water (120 ml), independent of food intake.

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

Elderly patients do not require dose adjustment.

Children.

Experience with the use of the medication in children is limited.

Overdose.

No cases of overdose have been reported.

Adverse Reactions

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

Psychiatric disorders: hallucinations.

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 disorders: chills, edema.

Shelf life. 3 years.

Storage conditions.

Store at a temperature not exceeding 25 °C.

Keep out of reach of children!

Do not freeze.

During storage, slight opalescence may occur, which disappears when the preparation is kept at room temperature (≈ 20 °C).

Packaging.

30 ml in a bottle; 1 bottle with a dosing syringe in a cardboard box.

10 ml in sachets; 10 sachets (1 × 10; 2 × 5) in a cardboard box.

Prescription status. Prescription only.

Manufacturer.

Ferrer Internacional, S.A., Spain / Ferrer Internacional, S.A., Spain.

Manufacturer's address.

Joan Buscalla, 1-9, Sant Cugat del Valles, 08173 Barcelona, Spain / Joan Buscalla, 1-9, Sant Cugat del Valles, 08173 Barcelona, Spain.