Lyra

INSTRUCTIONS for medical use of the medicinal product LIRA® (LIRA)

Composition:

Active ingredient: citicoline;

One ampoule (4 ml) contains 500 mg or 1000 mg of citicoline sodium, recalculated to 100% substance;

Excipients: hydrochloric acid concentrated or sodium hydroxide, water for injections.

Pharmaceutical form. Solution for injection.

Main physico-chemical characteristics: clear colorless or slightly yellowish liquid.

Pharmacotherapeutic group.

Psychostimulants 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. Citicoline improves the functioning of membrane mechanisms such as ion pumps and receptors, without which normal nerve impulse conduction is impossible. Due to its membrane-stabilizing effect, citicoline has anti-edematous properties and thus reduces cerebral edema. Research results have shown that citicoline inhibits the activity of certain phospholipases (A1, A2, C, and D), prevents residual release of free radicals, protects membrane systems from damage, and maintains the integrity of the antioxidant defense system.

Citicoline preserves neuronal energy reserves and inhibits apoptosis, thereby enhancing cholinergic transmission.

Citicoline also exerts a preventive neuroprotective effect in focal cerebral ischemia.

Citicoline promotes rapid functional recovery of patients with acute cerebrovascular disorders by reducing ischemic brain tissue damage, as confirmed by radiographic findings.

In traumatic brain injuries, citicoline shortens the duration of the recovery period and reduces the severity of post-traumatic syndrome.

Citicoline improves attention and level of consciousness, helps reduce symptoms of amnesia, and improves the condition in cognitive and other neurological disorders associated with cerebral ischemia.

Pharmacokinetics.

Citicoline is well absorbed following oral, intramuscular, and intravenous administration. After administration, a significant increase in plasma choline levels is observed. Following oral administration, the drug is almost completely absorbed. Studies have shown that bioavailability is practically equivalent following both oral and parenteral administration.

The drug is metabolized in the intestine and liver, forming choline and cytidine. After administration, citicoline is taken up by brain tissue, where choline acts on phospholipids and cytidine acts on cytidine nucleotides and nucleic acids. Citicoline rapidly reaches brain tissue and actively incorporates into cell membranes, cytoplasm, and mitochondria, stimulating phospholipid activity.

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

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 any component of the drug.

Increased parasympathetic nervous system tone.

Interaction with other medicinal products and other types of interactions.

The drug should not be used simultaneously with preparations containing meclofenoxate. Enhances the effect of levodopa.

Special precautions for use.

In 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 Cereaxon® in pregnant women. Data on the excretion of citicoline in breast milk and its effect on the fetus are lacking. Therefore, during pregnancy or breastfeeding, the drug should be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus.

Ability to affect reaction rate while 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.

Dosage and Administration

The drug is intended for intravenous or intramuscular administration. For intravenous use, it should be administered as a slow intravenous injection (over 3–5 minutes, depending on the prescribed dose) or by intravenous infusion (40–60 drops per minute).

The recommended dose for adults is 500–2000 mg per day, depending on the severity of the patient's condition.

The maximum daily dose is 2000 mg.

In acute and emergency conditions, maximum therapeutic effect is achieved when the drug is administered within the first 24 hours.

The duration of treatment depends on the course of the disease and is determined by the physician.

Dosage adjustment is not required for elderly patients.

The drug is compatible with all isotonic intravenous solutions as well as hypertonic glucose solutions.

This solution is intended for single use only. The solution should be administered immediately after opening the ampoule. Any unused solution must be discarded.

If necessary, treatment may be continued with the drug in the form of an oral solution or tablets.

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.

Very rare (< 1/10000) (including patient reports).

Central 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, changes at the injection site.

Shelf life.

2 years.

Do not use the medicinal product after the expiry date stated on the packaging.

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 "Method of administration and dosage".

Packaging.

4 ml in an ampoule. 5 or 10 ampoules per pack.

Prescription status.

Prescription only.

Manufacturer. JSC "Farmak".

Manufacturer's address and place of business.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.