LIRA

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT LIRA® (LIRA)

Composition:

Active substance: citicoline;

1 ml of the preparation contains sodium citicoline – 104.5 mg, equivalent to citicoline – 100 mg;

Excipients: methylparahydroxybenzoate (E 218); propylparahydroxybenzoate (E 216); potassium sorbate; sodium citrate; citric acid monohydrate; sorbitol (E 420); sodium saccharin; "Strawberry" flavor; glycerin; purified water.

Pharmaceutical form. Oral solution.

Main physicochemical characteristics: clear, colorless to slightly yellowish solution.

Pharmacotherapeutic group. Psychostimulants, drugs used in attention deficit hyperactivity disorder (ADHD), nootropic agents. Other psychostimulant and nootropic agents. ATC code N06B X06.

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, the regulation of which is essential for normal nerve impulse conduction. Due to its stabilizing effect on neuronal membranes, citicoline exhibits anti-edematous properties that promote reabsorption of cerebral edema.

Clinical studies have shown that citicoline inhibits the activation of certain phospholipases (A1, A2, C, and D), 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 and inhibits apoptosis, thereby improving cholinergic transmission.

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

Clinical studies have shown that citicoline significantly increases functional recovery rates in patients with acute cerebrovascular disorders, which correlates with a slowing of the growth 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, and helps reduce symptoms of amnesia, cognitive deficits, and other neurological disorders associated with cerebral ischemia.

Pharmacokinetics

Citicoline is well absorbed following oral, intramuscular, and intravenous administration. Plasma choline levels increase significantly after administration by these routes. Absorption after oral administration is nearly complete, and bioavailability is practically equivalent to that after intravenous administration.

Depending on the route of administration, the drug is metabolized in the intestine and liver into 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. Upon reaching the brain, citicoline integrates into cellular, cytoplasmic, and mitochondrial membranes, participating in the formation of phospholipid fractions.

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. The 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 as CO₂, with the rate of exhaled CO₂ decreasing rapidly after 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 tone of the parasympathetic nervous system.

Interaction with other medicinal products and other forms of interaction.

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

Special precautions for use

Patients with hereditary fructose intolerance should not take Lira®, oral solution, as the preparation contains sorbitol. Methylparaben (E 218) and propylparaben (E 216) contained in the formulation may cause allergic reactions (usually of delayed type).

This medicinal product contains 1.2 mmol of sodium per 5 ml of solution. Caution is advised when administering to patients on a sodium-restricted diet.

Use during pregnancy or breastfeeding

There is insufficient data on the use of citicoline in pregnant women. Information regarding excretion of citicoline in breast milk and its effects on the fetus is lacking. Therefore, during pregnancy or breastfeeding, this medicinal product should be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus.

Ability to influence the speed of reactions when 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.

Oral use. The recommended dose for adults is from 500 mg (5 ml) to 2000 mg (20 ml) per day, divided into 2–3 doses. May be taken regardless of food intake.

The required amount of solution (draw into a dosing syringe or use the contents of one sachet) should be mixed with a small amount of water and taken using the dosing syringe. The dosing syringe must be rinsed with water after each use.

Dosage and duration of treatment depend on the severity of brain lesions and are determined individually by a physician.

Elderly patients do not require dose adjustment.

Children.

Experience with the use of citicoline in children is limited.

Overdose.

Cases of overdose have not been reported.

Side effects.

Very rare (<1/10,000) (including patient reports).

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

Cardiovascular system: arterial hypertension, arterial hypotension, tachycardia.

Respiratory system: dyspnea.

Gastrointestinal system: nausea, vomiting, diarrhea.

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

General reactions: chills.

Shelf life. 2 years.

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

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze or refrigerate. Keep out of reach of children.

Packaging.

30 ml or 60 ml in a bottle. 1 bottle per carton.

Or 10 ml in sachets. 10 sachets per carton.

Prescription status. Prescription only.

Manufacturer.

JSC "Farmak".

Manufacturer's name and address of the place of business.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.