Ceraxon

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

Composition:

Active substance: citicoline;

1 ampoule contains 522.5 mg sodium citicollinate equivalent to 500 mg citicoline, or 1045 mg sodium citicollinate equivalent to 1000 mg citicoline;

Excipients: hydrochloric acid or sodium hydroxide solution for pH adjustment, water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear, colorless solution, free from visible particles.

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 properties that help reduce 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 slowing of the growth in the volume of ischemic brain damage 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

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 renal excretion of the drug, two phases are observed: the first phase lasting 36 hours, during which the elimination rate decreases rapidly, and a 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 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 interaction.

Citicoline enhances the effect of levodopa.

The drug should not be administered simultaneously with medicinal products containing meclofenoxate.

Special precautions for use.

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

In case of intravenous infusion, the infusion rate should be 40–60 drops per minute.

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

Use during pregnancy or breastfeeding.

There are insufficient data on the use of citicoline in pregnant women.

Data regarding the excretion of citicoline in breast milk and its effects on the fetus are unknown.

During pregnancy or breastfeeding, the medicinal product should be prescribed only when the expected therapeutic benefit for the mother outweighs the potential risk to 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 or operate complex machinery.

Method of administration and dosage.

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 by slow injection (over 3–5 minutes depending on the dose administered) or by infusion (administration rate of 40–60 drops per minute).

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.

Children.

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

Overdose.

Due to the low toxicity of Ceraxon®, intoxication is not expected even if therapeutic doses are accidentally exceeded.

In case of accidental overdose, symptomatic treatment should be administered.

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 disorders: arterial hypertension, arterial hypotension.

Respiratory system disorders: dyspnea.

Gastrointestinal disorders: nausea, vomiting, occasional 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 30 °C. Keep out of reach of children!

Incompatibility. Do not use solvents not specified in the section "Instructions for use and dosage".

Packaging. 4 ml in ampoules; 5 or 10 ampoules per cardboard box.

Prescription category. Prescription only.

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

Manufacturer's address and place of business.

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