Alphacholine

APPROVED

by the Order of the Ministry of Health of Ukraine

06.02.2020 No. 269

Marketing Authorization

No. UA/17917/01/01

PACKAGE LEAFLET

for medical use of a medicinal product

ALPHACHOLINE^®

Qualitative and quantitative composition:

active substance: choline alfoscerate;

7 ml of medicinal product contains 600 mg choline alfoscerate;

list of excipients: methyl parahydroxybenzoate (E 218), propyl parahydroxybenzoate (E 216), sodium saccharin, flavor "Orange", purified water.

Pharmaceutical form. Oral solution.

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). 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.

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. 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.

The medicinal product is rapidly absorbed, an average of about 88% of the administered dose of choline alfoscerate is absorbed, there is a rapid distribution in organs and tissues. It penetrates the blood-brain barrier. Alphacholine^® accumulates mainly in the brain (45% of the medicinal product concentration in blood plasma), in lungs and liver. Renal excretion is about 10%.

Clinical particulars.

Therapeutic indications.

Psychoorganic syndrome on the background of involutional and degenerative processes in the brain, the consequences of cerebrovascular insufficiency or primary and secondary cognitive impairment in the elderly patients, characterized by memory impairment, confusion, disorientation, decreased motivation and initiative, decreased ability to concentrate attention. Behavioral and affective sphere disorders in the elderly patients: emotional lability, increased irritability, indifference to the environment, pseudomelancholia.

Contraindications.

• Hypersensitivity to the components of the medicinal product.
• During pregnancy and lactation.
• Patient age up to 18 years old (due to lack of data).
• Severe psychomotor agitation in patients with psychotic disorders.

Interaction with other medicinal products and other forms of interaction.

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

Special warnings and precautions for use.

Nausea may occur due to dopaminergic activation. Efficacy and safety for children (under 18 years) have not been established.

Important information about list of excipients.

The presence of methyl parahydroxybenzoate (E 218) and propyl parahydroxybenzoate (E 216) can cause allergic reactions (possibly delayed type).

Fertility, pregnancy and lactation.

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

Effects on ability to drive and use machines.

Caution should be taken when driving or engaging in other activities that require increased concentration and/or rapid reaction.

Posology and method of administration.

Take 1 vial of oral solution 2 times a day.

The specified dose can be increased by the physician.

Children.

There is no paediatric experience.

Overdose.

Increasing of the severity of dose-dependent side effects is possible. Overdose can be manifested by nausea, anxiety, agitation, insomnia. Treatment is symptomatic: taking adsorption medicinal products, including the reception of activated charcoal. The effectiveness of dialysis has not been established.

Undesirable effects.

As a rule, the medicinal product is well tolerated even with prolonged use. Reactions at the injection site are possible. At the beginning of treatment, the following manifestations of undesirable effects can occur: anxiety, agitation, insomnia. These symptoms are transient and do not require cessation of treatment, but a temporary dose reduction is possible.

Gastrointestinal disorders: nausea (which is mainly due to secondary dopaminergic activation), abdominal pain.

Nervous system disorders: short-term confused consciousness (in this case it is necessary to reduce the dose), headache.

Cardiac disorders: decreasing blood pressure.

Immune system disorders: hypersensitivity reactions: redness of the skin, rash, itching, urticaria, angioedema.

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. 1,5 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.

Nature and contents of container.

7 ml in a vial with a tamper-evident cup; 10 vials 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. 06.02.2020.