Gliatilin

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

Composition:

Active substance: choline alfoscerate;

4 ml of solution contain choline alfoscerate 1000 mg;

Excipients: water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless solution.

Pharmacotherapeutic group.

Drugs affecting the nervous system. Parasympathomimetics. Choline alfoscerate. ATC code N07AX02.

Pharmacological Properties

Pharmacodynamics

Gliatilin belongs to the group of central cholinomimetic agents with a predominant effect on the central nervous system (CNS). Choline alfoscerate, as a choline carrier and a precursor of phosphatidylcholine, has the potential ability to prevent and correct biochemical impairments that are particularly significant among the pathogenic factors of psychorganic involutional syndrome; thus, it can influence reduced cholinergic tone and altered phospholipid composition of nerve cell membranes. The medicinal product contains 40.5% metabolically protected choline. Metabolic protection ensures the release of choline in the brain. Gliatilin exerts a positive effect on memory functions and cognitive abilities, as well as on emotional state and behavior parameters, which are impaired due to the development of brain involutional pathology.

The mechanism of action is based on the fact that after entering the body, choline alfoscerate is enzymatically hydrolyzed into choline and glycerophosphate: choline participates in the biosynthesis of acetylcholine—one of the main mediators of nerve excitation; glycerophosphate serves as a precursor for neuronal membrane phospholipids (phosphatidylcholine). Thus, Gliatilin improves nerve impulse transmission in cholinergic neurons, positively affects neuronal membrane plasticity and receptor function. Gliatilin enhances cerebral blood flow, stimulates metabolic processes in the brain, activates structures of the brain's reticular formation, and restores consciousness following traumatic brain injury.

Pharmacokinetics

On average, approximately 88% of the administered dose of Gliatilin is absorbed. The drug accumulates predominantly in the brain (45% of the drug concentration in blood), lungs, and liver. Elimination of the drug occurs mainly via the lungs in the form of carbon dioxide (CO₂). Only 15% of the drug is excreted in urine and bile.

Clinical characteristics.

Indications.

Acute period of severe traumatic brain injury with predominantly brainstem-level damage (disturbance of consciousness, comatose state, focal hemispheric symptoms, brainstem injury symptoms).

Degenerative involutional cerebral psycho-organic syndromes or secondary consequences of cerebrovascular insufficiency, i.e. primary and secondary cognitive impairments in elderly individuals characterized by memory disturbances, confusion, disorientation, reduced motivation and initiative, decreased ability to concentrate; changes in emotional and behavioral spheres: emotional instability, irritability, indifference to the surrounding environment; pseudomelancholia in elderly individuals.

Contraindications.

Hypersensitivity to the medicinal product or to any of its components.

Psychotic syndrome, severe psychomotor agitation.

Pregnancy or breastfeeding period.

Interaction with other medicinal products and other forms of interaction.

Clinically significant interaction of the drug with other medicinal products has not been established.

Special precautions for use.

Use during pregnancy or breastfeeding.

The drug is contraindicated during pregnancy or breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

The drug does not affect the ability to drive or operate machinery.

Administration and Dosage.

In acute conditions, Gliatilin should be administered intramuscularly or intravenously (slowly) at a dose of 1 g (1 ampoule) daily for 15 to 20 days. After stabilization of the patient's condition, switch to the capsule form of the drug.

Children. Experience with the use of Gliatilin in children is lacking.

Overdose.

In case of Gliatilin overdose, which may manifest as nausea, restlessness, excitement, and insomnia, the dose of the drug should be reduced. Symptomatic therapy is recommended.

Adverse reactions.

The drug is generally well tolerated even with long-term use. Reactions at the injection site are possible. During the first days or weeks of treatment, the following adverse reactions may occur: anxiety, agitation, insomnia. These symptoms are temporary and do not require discontinuation of treatment; however, a temporary dose reduction may be needed.

Nausea (mainly due to secondary dopaminergic activation), decreased blood pressure, headache may occur; abdominal pain and short-term confusion are very rare. In such cases, the dose of the medicinal product should be reduced.

Hypersensitivity reactions are possible, including rash, itching, urticaria, angioedema, skin redness.

Shelf life. 5 years.

Storage conditions.

Store at a temperature not exceeding 25 °C, in a place inaccessible to children.

Incompatibility.

Do not mix in the same container with other medicinal products.

Packaging.

Ampoules made of neutral colorless glass. 4 ml per ampoule, 3 ampoules in a plastic container, 1 container in a cardboard box.

Prescription status. Prescription only.

Manufacturer/Applicant. Italfarmaco S.p.A., Italy.

Address of manufacturer and its place of business/activity / address of applicant.

Viale Fulvio Testi, 330, 20126 Milan (MI), Italy.