Centrolin

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT Centrolin (Centrolin)

Composition:

Active substance: choline alfoscerate;

4 ml of solution contains 1000 mg of choline alfoscerate;

Excipient: water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless liquid.

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

Pharmacological properties.

Pharmacodynamics.

Choline alfoscerate is an agent belonging to the group of central cholinomimetics with a predominant effect on the central nervous system (CNS). As a choline carrier and a precursor of phosphatidylcholine, choline alfoscerate may potentially prevent and correct biochemical impairments that are particularly significant among the pathogenic factors of psychorganic involutional syndrome; thus, it may influence reduced cholinergic tone and altered phospholipid composition of nerve cell membranes. The formulation contains 40.5% metabolically protected choline. Metabolic protection ensures the release of choline in the brain. Choline alfoscerate exerts a positive effect on memory functions and cognitive abilities, as well as on parameters of emotional state and behavior, 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 cleaved 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, choline alfoscerate improves nerve impulse transmission in cholinergic neurons and exerts a positive influence on neuronal membrane plasticity and receptor function. Choline alfoscerate enhances cerebral blood flow, intensifies metabolic processes in the brain, activates the reticular formation structures of the brain, and restores consciousness following traumatic brain injury.

Pharmacokinetics.

On average, nearly 88% of the administered dose of choline alfoscerate 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, coma, focal hemispheric symptoms, brainstem injury signs).

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; emotional and behavioral changes: emotional instability, irritability, indifference to surroundings; pseudomelancholia in elderly individuals.

Contraindications.

Known hypersensitivity to the drug or its components.

Psychotic syndrome, severe psychomotor agitation.

Pregnancy or lactation 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 and breastfeeding.

Ability to influence the reaction rate when driving or operating machinery.

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

Method of administration and dosage.

In acute conditions, administer intramuscularly or intravenously (slowly) 1 g (4 ml) daily for a period of 15 to 20 days. After stabilization of the patient's condition, switch to the oral dosage form of choline alfoscerate.

Children.

Due to insufficient experience with the use of the drug in pediatric practice, it is not recommended for use in children.

Overdose.

In case of choline alfoscerate overdose, which may manifest as nausea, restlessness, excitement, and insomnia, the dose should be reduced. Symptomatic therapy should be administered.

Side effects

The drug is usually well tolerated even during prolonged use. Injection site reactions may occur. 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, but a temporary dose reduction may be considered.

Nausea (mainly due to secondary dopaminergic activation), decreased blood pressure, headache may also occur. Abdominal pain and short-term confusion are very rare. In such cases, the drug dosage should be reduced.

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

Shelf life.

3 years.

Storage conditions.

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

Incompatibility.

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

Packaging.

4 ml solution in an ampoule. 5 ampoules in a cassette. 1 or 2 cassettes per carton.

Prescription status. Prescription only.

Manufacturer.

Public joint-stock company "Scientific and Production Center "Borshchahivskiy Chemical-Pharmaceutical Plant".

Manufacturer's address and place of business.

17 Myru Street, Kyiv, 03134, Ukraine.