Cereaxon

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

Composition:

Active substance: citicoline;

One tablet contains 522.5 mg of sodium citicoline, equivalent to 500 mg of citicoline;

Excipients: talc; magnesium stearate; anhydrous colloidal silicon dioxide; sodium croscarmellose; hydrogenated castor oil; microcrystalline cellulose;

Coating: talc; magnesium stearate; titanium dioxide (E 171); polyethylene glycol 6000; methacrylate copolymer (type A).

Pharmaceutical form. Film-coated tablets.

Main physicochemical characteristics: white, elongated film-coated tablets with the imprint «С500».

Pharmacotherapeutic group. Psychostimulants, drugs used in attention deficit hyperactivity disorder (ADHD), 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, the modulation of which is necessary for normal nerve impulse conduction. Thanks to its membrane-stabilizing effect, 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), thereby 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.

Experimental evidence has demonstrated that citicoline also exerts a preventive neuroprotective effect in models of focal cerebral ischemia.

Clinical studies have shown that citicoline significantly improves functional recovery parameters in patients with acute ischemic cerebrovascular disorders, which correlates with a slowed progression of ischemic brain lesions 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, alleviates cognitive and neurological deficits associated with cerebral ischemia, and helps reduce symptoms of amnesia.

Pharmacokinetics.

Citicoline is well absorbed after oral administration. Following administration, a significant increase in plasma choline levels is observed. After oral intake, 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, becoming part of the phospholipid fraction.

Only a small amount of the administered dose is found in urine and feces (less than 3%). Approximately 12% of the dose is excreted as exhaled CO₂. Urinary excretion of the drug occurs in two phases: the first phase lasts 36 hours, during which the excretion rate decreases rapidly, and the second phase, during which the excretion rate declines much more slowly. A similar biphasic pattern is observed in excretion via the respiratory tract. The rate of CO₂ excretion decreases rapidly over approximately 15 hours, after which it declines much more slowly.

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 other components of the drug.
• High parasympathetic nervous system tone.

Interaction with other medicinal products and other forms of interactions.

Citicoline enhances the effect of levodopa. Should not be administered concurrently with medicinal products containing meclofenoxate.

Special precautions for use.

The medicinal product contains hydrogenated castor oil, which may cause stomach upset and diarrhea. Therefore, patients with inflammatory bowel diseases should use the drug with special caution.

Use during pregnancy or breastfeeding.

There are insufficient data on the use of citicoline in pregnant women. Citicoline should not be used during pregnancy except in cases of urgent necessity. The medicinal product should be prescribed during pregnancy only when the expected therapeutic benefit outweighs the potential risk. There are no data on the passage of citicoline into breast milk or its effects on the fetus.

Ability to affect reaction speed when driving or operating machinery. In individual cases, certain adverse reactions from the central nervous system may affect the ability to drive a vehicle or operate complex machinery.

Method of Administration and Dosage.

The recommended dose is from 500 to 2000 mg per day (1–4 tablets), depending on the severity of symptoms and the patient's condition.

The dosage and duration of treatment 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.

Adverse Reactions

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

Psychiatric disorders: hallucinations.

Nervous system disorders: severe headache, dizziness.

Cardiovascular disorders: arterial hypertension, arterial hypotension.

Respiratory system disorders: dyspnea.

Gastrointestinal disorders: nausea, vomiting, occasional diarrhea.

Skin and subcutaneous tissue disorders: allergic reactions, including rash, pruritus, angioneurotic edema, anaphylactic shock, erythema, urticaria, exanthema, purpura.

General disorders: chills, swelling.

Shelf life: 3 years.

Storage conditions: Store at a temperature not exceeding 30 °C. Keep out of reach of children!

Packaging: 5 tablets per blister; 2 or 4 blisters per cardboard box.

Prescription status: Prescription only.

Manufacturer: Ferrer Internacional, S.A., Spain.

Manufacturer's address and place of business:
Joan Buscalla, 1–9, Sant Cugat del Valls, 08173 Barcelona, Spain / Joan Buscalla, 1–9, Sant Cugat del Valls, 08173 Barcelona, Spain.