Alphacholine

APPROVED

by the Order of the Ministry of Health of Ukraine

06.02.2020 No. 269

Marketing Authorization

No. UA/17917/02/01

VARIATONS APPLIED

By the Order of the Ministry of

Health of Ukraine

1752 № 18.08.2021

PACKAGE LEAFLET

for medical use of a medicinal product

Alphacholine®

Qualitative and quantitative composition:

active substance: choline alfoscerate;

1 ampoule of 4 ml of solution contains 1 000 mg choline alfoscerate;

list of excipients: water for injection.

Pharmaceutical form .Solution for injection.

Main physical and chemical properties: clear colorless liquid.

Pharmacotherapeutic group.

Other nervous system drugs. Parasympathomimetics. Choline alfoscerate. ATC code N07A X02.

Pharmacological properties.

Pharmacodynamic properties.

Alphacholine® is a medicinal product that belongs to the group of central cholinomimetics with a predominant effect on the central nervous system (CNS). Choline alfoscerate as a carrier of choline and a precursor agent of phosphatidylcholine has the potential ability to prevent and correct biochemical damage, which are of particular importance among the pathogenic factors of psychoorganic involution syndrome, that is, it can affect reduced cholinergic tone and altered the phospholipid composition of the membranes of nerve cells. The medicinal product contains 40.5% of metabolically protected choline. Metabolic protection provides the release of choline in the brain. Alphacholine® has a positive effect on memory functions and cognitive abilities, as well as on indicators of emotional state and behavior, the deterioration of which was caused by the development of involutional brain pathology.

The mechanism of action is based on the fact that when choline enters the body, alfoscerate is cleaved by enzymes into choline and glycerophosphate: choline is involved in the biosynthesis of acetylcholine – one of the main mediators of nervous agitation; glycerophosphate is a precursor of phospholipids (phosphatidylcholine) of the neuronal membrane. Thus, Alphacholine® improves the transmission of nerve impulses in cholinergic neurons; has a positive effect on the plasticity of neuronal membranes and the function of receptors. Alphacholine® improves cerebral blood flow, enhances metabolic processes in the brain, activates the structures of the reticular formation of the brain and restores consciousness in case of traumatic brain injury.

Pharmacokinetic properties.

On average, almost 88% of the administered dose of Alphacholine® is absorbed. The medicinal product accumulates mainly in the brain (45% of the medicinal product concentration in the blood), lungs and liver. Elimination of the medicinal product occurs mainly through the lungs in the form of carbon dioxide (CO2). Only 15% of the medicinal product is excreted in the urine and bile.

Clinical particulars.

Therapeutic indications.

Acute period of severe traumatic brain injury with mainly stem level of damage (impaired consciousness, coma, focal hemispheric symptoms, symptoms of brain stem damage).

Degenerative-involutional cerebral psychoorganic syndromes or secondary consequences of cerebrovascular insufficiency, that is, primary and secondary mental disorders in the elderly, characterized by memory impairment, confusion, disorientation, decreased motivation and initiative, decreased ability to concentrate; changes in the emotional sphere and the sphere of behavior: emotional instability, irritability, indifference to the environment; pseudomelancholia in the elderly.

Contraindications.

Hypersensitivity to the medicinal product or its components.

Psychotic syndrome, with severe psychomotor agitation.

During pregnancy and lactation.

Interaction with other medicinal products and other forms of interaction.

No clinically relevant interactions of medicinal product with other medications were detected.

Fertility, pregnancy and lactation.

The medicinal product is contraindicated for use during pregnancy or lactation.

Effects on ability to drive and use machines.

The medicinal product does not affect driving or operating other machinery.

Posology and method of administration.

In acute conditions, Alphacholine® should be administered intramuscularly or intravenously (slowly) in 1 g (1 ampoule) per day for 15 to 20 days. Then, after the patient's condition is stabilized, switch to the oral dosage form of the medicinal product.

Children.

There is no experience of using Alphacholine® in children.

Overdose.

In case of Alphacholine® overdose, which may be manifested by nausea, anxiety, agitation, insomnia, the dose of the medicinal product should be reduced. Therapy is symptomatic.

Undesirable effects.

As a rule, the medicinal product is well tolerated even with prolonged 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, but a temporary dose reduction may be required.

Nausea (which is mainly a consequence of secondary dopaminergic activation), decreased blood pressure, headache, very rarely abdominal pain and short-term confusion are possible. In this case, it is necessary to reduce the dose of the medicinal product.

Hypersensitivity reactions are possible, including rash, pruritus, urticaria, angioneurotic edema, and reddening of the skin.

Reported suspected adverse reactions.

Reporting suspected adverse reactions after registration of a medicinal product is an important procedure. This allows for continued monitoring of the benefit/risk ratio for the respective drug. Healthcare providers should be informed of any suspected adverse reactions through the national alert system.

Shelf life. 2 years.

Special precautions for storage.

Store in the original package at a temperature below 25°C. Do not freeze.

Keep out of the reach of children.

Incompatibilities.

It is not recommended to use choline alfoscerate in one container with other medicinal products.

Nature and contents of container.

4 ml in an ampoule; 5 ampoules in a blister container; 1 blister containers in a pack.

Category of release. Prescription only medicine.

Manufacturer. PrJSC “Pharmaceutical firm “Darnitsa”.

The manufacturer's location and address of the place of business.

13, Boryspilska Street, Kyiv, 02093, Ukraine.

Date of last revision.