MEDOTILIN

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT MEDOTILIN (MEDOTILIN)

Composition:

Active substance: choline alfoscerate;

1 ampoule (4 ml) contains choline alfoscerate (as choline alfoscerate hydrate) 1000 mg;

Excipient: water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical characteristics: clear, colorless or slightly yellow solution.

Pharmacotherapeutic group.

Agents acting on the nervous system. Parasympathomimetics. Choline alfoscerate. ATC code N07AX02.

Pharmacological Properties

Pharmacodynamics

The medicinal product belongs to the group of central cholinomimetics with predominant effects on the central nervous system (CNS). The active substance, choline alfoscerate, as a choline carrier and a precursor of phosphatidylcholine, has the potential to prevent and correct biochemical damage that plays a significant role among the pathogenic factors of psychorganic involutional syndrome. Thus, it can influence the reduced cholinergic tone and altered phospholipid composition of nerve cell membranes. The medicinal product contains 40.5% metabolically protected choline. Metabolic protection ensures the release of choline in the brain. The medicinal product positively affects memory functions and cognitive abilities, as well as parameters of emotional state and behavior, which have been 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 major mediators of nerve excitation; glycerophosphate serves as a precursor for neuronal membrane phospholipids (phosphatidylcholine). Thus, the medicinal product enhances nerve impulse transmission in cholinergic neurons, positively influences neuronal membrane plasticity and receptor function. It also improves cerebral blood flow, enhances metabolic processes in the brain, activates structures of the brain's reticular formation, and restores consciousness following traumatic brain injury.

Pharmacokinetics

Approximately 88% of the administered dose of choline alfoscerate is absorbed on average. It accumulates predominantly in the brain (45% of its plasma concentration), lungs, and liver. Elimination occurs mainly via the lungs in the form of carbon dioxide (CO₂). Only 15% of the choline alfoscerate dose is excreted in urine and bile.

Clinical characteristics.

Indications.

• Acute period of severe traumatic brain injury with predominant brainstem involvement (impaired 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 patients characterized by memory disturbances, confusion, disorientation, reduced motivation and initiative, and impaired concentration ability.
• Emotional and behavioral changes: emotional instability, irritability, indifference to surroundings; pseudomelancholia in elderly patients.

Contraindications.

• Known hypersensitivity to the active substance or to any of the excipients of the medicinal product.
• Psychotic syndrome, severe psychomotor agitation.
• Pregnancy period.
• Breastfeeding period.

Interaction with other medicinal products and other forms of interaction.

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

Special precautions for use.

Use during pregnancy or breastfeeding.

The medicinal product is contraindicated during pregnancy or breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

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

Method of Administration and Dosage.

The medicinal product is intended for parenteral administration.

Adults.

In acute conditions, administer the solution intramuscularly or intravenously (slowly) at a dose of 1 g (1 ampoule) daily for 15–20 days. After stabilization of the patient's condition, switch to the oral form of choline alfoscerate.

Children.

There is no experience with the use of choline alfoscerate in children.

Overdose.

Symptoms.

Overdose may manifest as nausea, restlessness, excitement, and insomnia.

Treatment.

The dose of the medicinal product should be reduced and symptomatic therapy administered.

Adverse Reactions

Choline alfoscerate is generally well tolerated, even during prolonged use.

Possible reactions at the injection site 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; however, a temporary dose reduction may be considered.

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 administered dose should be reduced.

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

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after medicine registration is of great importance, as it enables continuous monitoring of the benefit-risk balance of the medicine. Healthcare professionals should report any suspected adverse reactions through the national pharmacovigilance system.

Shelf life.

4 years.

Storage conditions.

Store at temperatures not exceeding 25 °C, in the original packaging, in a place inaccessible to children.

Incompatibilities.

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

Packaging.

4 ml in a glass ampoule; 3 ampoules in a blister pack; 1 blister pack in a cardboard box.

Prescription status.

Prescription only.

Manufacturer.

Mefar Ilac San. A.S.

Manufacturer's address and location of operations.

Ramazanoglu Mah. Ensar Cad. No: 20, 34906 Kurtkoy – Pendik/Istanbul, Turkey.

Marketing Authorization Holder.

WORLD MEDICINE ILAC SAN. VE TIC. A.S., Turkey.