ALPHACHOLIN®

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

Composition:

Active substance: choline alfoscerate;

1 ampoule of 4 ml solution contains choline alfoscerate 1000 mg;

Excipients: water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless liquid.

Pharmacotherapeutic group.

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

Pharmacological Properties

Pharmacodynamics

Alfacholin® is a drug belonging to the group of central cholinomimetics with a predominant effect on the central nervous system (CNS). As a choline carrier and precursor of phosphatidylcholine, choline alfoscerate has the potential to 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 drug formulation contains 40.5% metabolically protected choline. Metabolic protection ensures the release of choline in the brain. Alfacholin® exerts a positive effect on memory functions and cognitive abilities, as well as on 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 hydrolyzed into choline and glycerophosphate: choline participates in the biosynthesis of acetylcholine—one of the principal mediators of nerve excitation; glycerophosphate serves as a precursor for phospholipids (phosphatidylcholine) of neuronal membranes. Thus, Alfacholin® improves nerve impulse transmission in cholinergic neurons and exerts a beneficial effect on neuronal membrane plasticity and receptor function. Alfacholin® enhances cerebral blood flow, stimulates metabolic processes in the brain, activates structures of the brain's reticular formation, and promotes recovery of consciousness following traumatic brain injury.

Pharmacokinetics

Approximately 88% of the administered dose of Alfacholin® is absorbed on average. 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; emotional and behavioral changes: emotional instability, irritability, indifference to surroundings; pseudomelancholia in elderly individuals.

Contraindications.

Hypersensitivity to the components of the medicinal product.

Psychotic syndrome, in cases of severe psychomotor agitation.

Pregnancy or breastfeeding period.

Interaction with other medicinal products and other types of interactions.

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

Use during pregnancy or breastfeeding.

The medicinal product is contraindicated during pregnancy and breastfeeding.

Ability to influence reaction speed when driving or operating machinery.

The medicinal product does not affect the ability to drive vehicles or operate machinery.

Method of Administration and Dosage

In acute conditions, administer Alphacholin® 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 oral dosage form.

Children

There is no experience with the use of Alphacholin® in children.

Overdose

Overdose of Alphacholin® may manifest as nausea, restlessness, excitement, and insomnia. In such cases, the dose of the drug should be reduced. Symptomatic therapy is recommended.

Adverse reactions.

The medicinal product 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 effects may occur: anxiety, agitation, insomnia. These symptoms are temporary and do not require discontinuation of treatment; however, a temporary dose reduction may be necessary.

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, pruritus, urticaria, angioneurotic edema, skin redness.

Reporting suspected adverse reactions.

Reporting of suspected adverse reactions after registration of the medicinal product is of great importance. It enables ongoing monitoring of the benefit-risk balance of the use of this medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report all cases of suspected adverse reactions and/or lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.

Keep out of reach of children.

Incompatibility.

Must not be used in the same container with other medicinal products.

Packaging. 4 ml in an ampoule; 5 ampoules in a contour cell pack; 1 contour cell pack in a carton.

Prescription category. Prescription only.

Manufacturer. JSC "Pharmaceutical company "Darnytsia".

Manufacturer's address and location of its business activities.

13, Boryspylska Street, Kyiv, 02093, Ukraine.