Alphacholin

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ALPHACHOLINE® ALPHACHOLINE

Composition:

Active substance: choline alfoscerate;

7 ml of the preparation contain choline alfoscerate 600 mg;

Excipients: methylparahydroxybenzoate (E 218), propylparahydroxybenzoate (E 216), sodium saccharin, orange flavoring, purified water.

Pharmaceutical form. Oral solution.

Main physicochemical characteristics: clear, colorless liquid.

Pharmacotherapeutic group.

Agents acting on the nervous system. Parasympathomimetics. Choline alfoscerate.

ATC code N07AX02.

Pharmacological Properties

Pharmacodynamics

Choline alfoscerate is a medicinal product belonging to the group of central cholinomimetics with a predominant effect on the central nervous system (CNS). Alphacholine® positively influences memory function and cognitive abilities, as well as parameters of emotional state and behavior, the deterioration of which is caused by the development of brain involutional pathology.

Choline alfoscerate, as a carrier of choline and a precursor of phosphatidylcholine, has the potential ability to prevent and correct biochemical damage that is particularly significant among the pathogenic factors of psychorganic involutional syndrome; thus, it can affect reduced cholinergic tone and altered phospholipid composition of nerve cell membranes.

The medicinal product contains 40.5% metabolically protected choline, ensuring the release of choline in the brain. Its mechanism of action is based on the fact that, upon entering the body, choline alfoscerate is hydrolyzed by enzymes into choline and glycerophosphate: choline participates in the biosynthesis of acetylcholine—one of the main neurotransmitters of nerve impulse transmission; glycerophosphate serves as a precursor for phospholipids (phosphatidylcholine) of the neuronal membrane. Thus, it enhances nerve impulse transmission in cholinergic neurons and exerts a positive effect on neuronal membrane plasticity and receptor function.

Alphacholine® improves cerebral blood flow, enhances metabolic processes in the brain, activates the reticular formation structures of the brain, and promotes recovery of consciousness following traumatic brain injury.

Pharmacokinetics

The drug is rapidly absorbed, with approximately 88% of the administered dose of choline alfoscerate being absorbed on average, and rapid distribution in organs and tissues is observed. It penetrates the blood-brain barrier. Alphacholine® accumulates predominantly in the brain (45% of the drug concentration in blood plasma), lungs, and liver. Renal excretion amounts to approximately 10%.

Clinical characteristics.

Indications.

Psychorganic syndrome against the background of involutional and degenerative processes in the brain, consequences of cerebrovascular insufficiency, or primary and secondary cognitive impairments in elderly individuals characterized by memory impairment, confusion, disorientation, reduced motivation and initiative, and decreased ability to concentrate attention. Behavioral and affective disturbances in elderly individuals: emotional lability, increased irritability, indifference to the surrounding environment, pseudomelancholia.

Contraindications.

− Hypersensitivity to the components of the medicinal product.

− Pregnancy or breastfeeding period.

− Patient age under 18 years (due to lack of data).

− Marked psychomotor agitation in patients with psychotic disorders.

Interaction with other medicinal products and other types of interactions.

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

Special precautions.

Nausea may occur due to dopaminergic stimulation. Efficacy and safety in children (under 18 years of age) have not been established.

Important information about excipients.

The presence of methylparahydroxybenzoate (E 218) and propylparahydroxybenzoate (E 216) in the formulation may cause allergic reactions (possibly delayed).

Use during pregnancy or breastfeeding.

The medicinal product is contraindicated during pregnancy and breastfeeding.

Ability to affect reaction rate when driving or operating machinery.

Caution should be exercised when driving or engaging in other activities requiring heightened attention and/or rapid reactions.

Dosage and Administration.

Take 1 vial of oral solution twice daily.

The indicated dose may be increased by a physician.

Children.

There is no experience with use in children.

Overdose.

May result in an intensification of dose-dependent adverse effects. Overdose may manifest as nausea, restlessness, excitement, and insomnia. Treatment is symptomatic: administration of adsorbent medicinal agents, including activated charcoal. The effectiveness of dialysis has not been established.

Adverse Reactions

The medicinal product is generally well tolerated, even during prolonged use.

At the beginning of treatment, the following adverse reactions may occur: anxiety, agitation, insomnia. These symptoms are transient and do not require discontinuation of treatment; however, a temporary dose reduction may be considered.

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

Nervous system disorders: short-term confusion (in such cases, dose reduction is required), headache.

Cardiovascular disorders: decreased blood pressure.

Immune system disorders: hypersensitivity reactions: skin redness, rash, pruritus, urticaria, angioneurotic edema.

Reporting of suspected adverse reactions.

Reporting suspected adverse reactions after marketing authorization is of great importance. It allows ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and/or lack of efficacy via the Automated Pharmacovigilance Information System at: 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 and sight of children.

Packaging.

7 ml in a bottle with a tamper-evident cap; 10 bottles per carton.

Prescription status. Prescription only.

Manufacturer: JSC "Pharmaceutical Company "Darnytsia".

Manufacturer's address and location of operations.

13, Boryspylska Street, Kyiv, 02093, Ukraine.