Neurocytin®c

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT NEUROCITIN® C (NEUROCITIN C)

Composition:

Active substance: citicoline;

1 ml of solution contains sodium citicoline 104.5 mg (equivalent to 100 mg of citicoline);

Excipients: potassium sorbate; methylparahydroxybenzoate (E 218); propylparahydroxybenzoate (E 216); sorbitol (E 420); glycerin; disodium citrate dihydrate; sodium saccharin; citric acid monohydrate; water for injections.

Pharmaceutical form. Oral solution.

Main physicochemical properties: clear, colorless or slightly yellowish viscous solution.

Pharmacotherapeutic group.

Medicinal products affecting the nervous system. Psychostimulants. Psychostimulants, drugs used in attention deficit hyperactivity disorder (ADHD) and nootropic agents. Other psychostimulants and nootropics. Citicoline.

ATC code N06BX06.

Pharmacological Properties.

Pharmacodynamics.

Citicoline stimulates the biosynthesis of structural phospholipids in neuronal membranes, as confirmed by magnetic resonance spectroscopy data. Due to this mechanism of action, citicoline improves the functioning of membrane mechanisms such as ion-exchange pumps and receptors, the modulation of which is necessary for normal nerve impulse conduction.

Thanks to its membrane-stabilizing effect, citicoline exhibits anti-edematous properties, which contribute to reducing cerebral edema.

Clinical studies have shown that citicoline inhibits the activation of certain phospholipases (A1, A2, C, and D), reducing the formation of free radicals, preventing the destruction of membrane systems, and preserving antioxidant defense systems such as glutathione.

Citicoline preserves neuronal energy reserves and inhibits apoptosis, thereby improving cholinergic transmission.

Experimental evidence has demonstrated that citicoline also exerts a preventive neuroprotective effect in focal cerebral ischemia.

Clinical studies have shown that citicoline significantly increases functional recovery rates in patients with acute cerebrovascular disorders, which correlates with a slowing of the progression of ischemic brain lesions as demonstrated by neuroimaging.

In patients with traumatic brain injury, citicoline accelerates recovery and reduces the duration and severity of post-traumatic syndrome.

Citicoline improves levels of attention and consciousness, helps reduce symptoms of amnesia, and alleviates cognitive and other neurological disorders associated with cerebral ischemia.

Pharmacokinetics.

Citicoline is well absorbed after oral, intramuscular, and intravenous administration. Plasma choline levels increase significantly following administration by these routes. Citicoline is almost completely absorbed after oral administration, and its bioavailability is practically equivalent to that achieved with intravenous administration.

Depending on the route of administration, the drug is metabolized in the intestine and liver into choline and cytidine. After administration, citicoline is widely distributed into brain structures, with rapid incorporation of the choline fraction into structural phospholipids and the cytidine fraction into cytidine nucleotides and nucleic acids. Upon reaching the brain, citicoline is incorporated into cellular, cytoplasmic, and mitochondrial membranes, participating in the formation of phospholipid fractions.

Only a small amount of the dose is excreted in urine and feces (less than 3%). Approximately 12% of the dose is excreted as exhaled CO₂. The excretion of the drug in urine shows two phases: the first phase—approximately 36 hours—during which the excretion rate rapidly decreases, and the second phase—during which the excretion rate decreases much more slowly. A similar biphasic pattern is observed in excretion as exhaled CO₂: the rate of CO₂ excretion rapidly decreases after approximately 15 hours, then declines much more slowly.

Clinical characteristics.

Indications.

• Stroke, acute phase of cerebrovascular disorders, and treatment of complications and consequences of cerebrovascular disorders.
• Traumatic brain injury and its neurological consequences.
• Cognitive disorders and behavioral disturbances due to chronic vascular and degenerative cerebral disorders.

Contraindications.

• Hypersensitivity to citicoline or to any of the excipients of the medicinal product.
• Increased parasympathetic nervous system tone.

Interaction with other medicinal products and other forms of interaction.

The drug should not be used simultaneously with medicinal products containing meclofenoxate.

Citicoline enhances the effect of levodopa.

Special precautions for use.

Neurocitin® C, oral solution, contains sorbitol; therefore, if a patient has been diagnosed with intolerance to certain sugars, consultation with a physician is necessary before taking this medicinal product.

Methylparahydroxybenzoate (E 218) and propylparahydroxybenzoate (E 216) contained in the formulation may cause allergic reactions (possibly delayed-type).

Neurocitin® C contains:

0.476 mmol (or 10.95 mg) of sodium per 1 ml of medicinal product;

9.52 mmol (or 219 mg) of sodium per 20 ml of medicinal product. Caution is advised when administering to patients on a controlled sodium intake diet.

0.4 mmol (or 15.6 mg) of potassium per 20 ml of the product, i.e. practically potassium-free.

The medicinal product contains a small amount of glycerol – 1 g per 20 ml of the product, which is safe and has no significant effect on the patient's organism.

Use during pregnancy or breastfeeding.

There are insufficient data on the use of citicoline in pregnant women. Data regarding excretion of citicoline in breast milk and its effects on the fetus are lacking. Therefore, during pregnancy or breastfeeding, the medicinal product should be prescribed only when the expected benefit to the mother outweighs the potential risk to the fetus.

Ability to affect reaction speed when driving or operating machinery.

In individual cases, certain adverse reactions from the central nervous system may affect the ability to drive a vehicle or operate complex machinery.

Method of Administration and Dosage

For oral use.

The recommended dose of Neurocytin® S for adults is from 500 mg (5 mL) to 2000 mg (20 mL) per day, divided into 2–3 doses. May be taken independently of food intake.

The medication should be administered using an oral syringe as follows:

• Before use, fully depress the plunger of the oral syringe.
• Pull back the plunger and draw up the required dose, ensuring that the volume of liquid in the oral syringe corresponds to the prescribed dose.
• Administer the medication directly from the oral syringe, or after mixing with a small amount of water (120 mL).

The oral syringe must be rinsed with water after each use.

Dosage and duration of treatment depend on the severity of brain damage and are determined individually by the physician.

Elderly patients

Dose adjustment is not required.

Children

Experience with use in children is limited.

Overdose

Cases of overdose have not been reported.

Adverse reactions.

The adverse reactions listed below are classified by organs and systems and by frequency of occurrence. The frequency of occurrence is classified as follows: common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), rare (≥ 1/10000 to < 1/1000), very rare (< 1/10000), frequency not known (cannot be estimated from the available data).

Adverse reactions occur very rarely (<1/10000), including isolated cases.

Neurological disorders: severe headache, vertigo, hallucinations.

Cardiovascular system disorders: arterial hypertension, arterial hypotension, tachycardia.

Respiratory, thoracic and mediastinal disorders: dyspnea.

Gastrointestinal disorders: nausea, vomiting, diarrhea.

Immune system disorders: allergic reactions, including: rash, hyperemia, exanthema, urticaria, purpura, pruritus, angioedema, anaphylactic shock.

General disorders: chills.

Shelf life. 2 years.

Shelf life after first opening of the vial – 40 days.

Storage conditions.

Store at a temperature not exceeding 25 °C in the original packaging.

Keep out of reach and sight of children.

Packaging.

30 ml, or 100 ml, or 200 ml of solution in a polymer vial. 1 vial with an oral syringe in a cardboard box.

Prescription category. Prescription only.

Manufacturer.

LLC "Yuria-Pharm".

Manufacturer's address and place of business.

108, Kozbirska St., Cherkasy, Cherkasy region, 18030, Ukraine. Tel.: (044) 281-01-01.