Medotilin

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

Composition:

Active substance: choline alfoscerate;

One ampoule (4 ml) of solution contains choline alfoscerate (as hydrate) 1000 mg;

Excipient: water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless or pale 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 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 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, the deterioration of which was caused by the development of brain involutional pathology.

The mechanism of action is based on the fact that, upon entering the body, choline alfoscerate is enzymatically hydrolyzed into choline and glycerophosphate: choline participates in the biosynthesis of acetylcholine—one of the main mediators of nerve excitation; glycerophosphate serves as a precursor of 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 in traumatic brain injury.

Pharmacokinetics.

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

Clinical characteristics.

Indications.

• Acute period of severe traumatic brain injury with predominant brainstem level damage (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 decreased concentration ability.
• Changes in emotional and behavioral spheres: emotional instability, irritability, indifference towards the surrounding environment; pseudomelancholia in elderly patients.

Contraindications.

• Known hypersensitivity to the active substance or to any of the other 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.

Use during pregnancy or breastfeeding.

The medicinal product is contraindicated during pregnancy or breastfeeding. Although specific studies have not revealed embryotoxic or teratogenic effects.

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 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 should be 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 effects 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 arterial pressure, headache may occur. Very rarely abdominal pain and short-term confusion may occur. In such cases, the administered dose should be reduced.

Hypersensitivity reactions are possible, including rash, pruritus, urticaria, angioneurotic edema, skin redness.

Reporting of suspected adverse reactions

Reporting of suspected adverse reactions occurring after marketing authorization is highly important. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are requested to report any suspected adverse reactions through the national reporting system.

Shelf life. 4 years.

Storage conditions.

Store at temperatures not exceeding 25 °C, in a dry, light-protected place, out of reach of children.

Incompatibilities.

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

Packaging.

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

Prescription status.

Prescription only.

Manufacturer.

C.O. Rompharm Company S.R.L., Romania /
S.C. Rompharm Company S.R.L., Romania.

Manufacturer's address and location of operations.

Otopeni city, Eroilor str. № 1A, 075100, jud. Ilfov, Romania /
Otopeni сіty, Eroilor str. № 1A, 075100, jud. Ilfov.

Marketing Authorization Holder.

LLC "WORLD MEDICINE", Ukraine /
WORLD MEDICINE LLC, Ukraine.