LIRA

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

Composition:

Active substance: citicoline;

One tablet contains sodium citicoline 522.5 mg calculated as 100% dry substance (equivalent to citicoline 500.0 mg);

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

Film coating: Opadry white 03 F 180011 (hypromellose, titanium dioxide E 171, polyethylene glycol 8000); Opadry white II 85 F 18422 (polyvinyl alcohol, titanium dioxide E 171, polyethylene glycol 4000, talc).

Pharmaceutical form. Film-coated tablets.

Main physicochemical properties: elongated, biconvex tablets with a score line, coated with a white or almost white film coating.

Pharmacotherapeutic group. Other psychostimulants and nootropics.

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, 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), 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 and inhibits apoptosis, thereby enhancing 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 improves functional recovery rates in patients with acute cerebrovascular disorders, which correlates with slowing the progression of ischemic brain lesions 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 and helps reduce symptoms of amnesia, cognitive deficits, and other neurological disorders associated with cerebral ischemia.

Pharmacokinetics.

Citicoline is well absorbed after oral, intramuscular, and intravenous administration. Plasma choline levels increase significantly following administration by these routes. Oral absorption is practically complete, and bioavailability is nearly equivalent to that achieved with 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 dose is excreted in urine and feces (less than 3%). Approximately 12% of the dose is excreted as exhaled CO₂. The elimination of the drug in urine occurs in two phases: the first phase lasts approximately 36 hours, during which the elimination rate rapidly decreases, and the second phase, in which the elimination rate declines much more slowly. A similar biphasic pattern is observed in CO₂ excretion: the rate of CO₂ elimination rapidly decreases after approximately 15 hours, 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 disturbances due to chronic cerebrovascular 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 interactions.

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

Special precautions for use

The medicinal product contains hydrogenated castor oil, which may cause stomach discomfort and diarrhea.

This medicinal product contains 1.024 mmol/dose of sodium. Caution is advised when administering to patients on a controlled sodium diet.

Use during pregnancy or breastfeeding.

There is insufficient data on the use of Lyrica® in pregnant women.

There are no data available on the excretion of citicoline in breast milk or its effects on the fetus. During pregnancy or breastfeeding, the product should be prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus.

Ability to influence 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 (1–4 tablets).

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

Elderly patients do not require dose adjustment.

Children.

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

Overdose.

Cases of overdose have not been described.

Adverse reactions.

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

Cardiovascular disorders: arterial hypertension, arterial hypotension, tachycardia.

Respiratory system disorders: dyspnea.

Gastrointestinal disorders: nausea, vomiting, diarrhea.

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

General disorders: chills.

Shelf life.

3 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.

Keep out of reach and sight of children.

Packaging.

10 tablets in a blister. 3 blisters in a carton.

Prescription status. Prescription only.

Manufacturer.

JSC "Farmak".

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

74, Kyrylivska Street, Kyiv, 04080, Ukraine.