Citicoline-zdorovya

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT CYTICOLINE-ZDOROV'YA

Composition:

Active substance: citicoline;

1 ampoule (4 ml) of the medicinal product contains citicoline 500 mg or 1000 mg;

Excipients: concentrated hydrochloric acid or sodium hydroxide; water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical characteristics: clear, colorless solution.

Pharmacotherapeutic group. Psychostimulants, agents used in attention deficit hyperactivity disorder (ADHD), nootropic agents. Other psychostimulant and nootropic agents. ATC code N06B X06.

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 stabilizing effect on neuronal membranes, citicoline exhibits anti-edematous properties, which contribute to a reduction in cerebral edema.

Citicoline inhibits the activation of certain phospholipases (A1, A2, C, and D), reduces the formation of free radicals, prevents the destruction of membrane systems, and preserves antioxidant defense systems such as glutathione.

Citicoline preserves neuronal energy reserves, inhibits apoptosis, and stimulates acetylcholine synthesis.

It has been demonstrated that citicoline also exerts a preventive neuroprotective effect in focal cerebral ischemia.

It is known that citicoline significantly enhances functional recovery in patients with acute ischemic stroke, which correlates with a slowing of the growth in volume of ischemic brain damage, as shown 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, as well as cognitive and neurological disorders associated with cerebral ischemia, and helps reduce symptoms of amnesia.

Pharmacokinetics.

After administration, a significant increase in plasma choline levels is observed. The drug is metabolized in the intestine and liver, forming choline and cytidine.

After administration, citicoline is widely distributed in brain structures, with rapid incorporation of the choline fraction into structural phospholipids and the cytidine fraction into cytidine nucleotides and nucleic acids. In the brain, citicoline integrates into cellular, cytoplasmic, and mitochondrial membranes, becoming incorporated into the phospholipid fraction.

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

Clinical characteristics.

Indications.

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

Contraindications.

• Hypersensitivity to citicoline or to other components of the drug.
• Increased tone of the parasympathetic nervous system.

Interaction with other medicinal products and other types of interactions.

Citicoline enhances the effect of levodopa. The drug should not be administered concurrently with medicinal products containing meclofenoxate.

Special precautions for use.

In case of intravenous administration, the drug should be administered slowly (over 3–5 minutes depending on the dose administered).

When administered intravenously by drip infusion, the infusion rate should be 40–60 drops per minute.

In the case of persistent intracranial hemorrhage, the dose should not exceed 1000 mg per day and the intravenous infusion rate (30 drops per minute).

This medicinal product contains 4.096 mmol (or 94.2 mg) of sodium per 2000 mg dose of citicoline. Caution should be exercised when administering the drug to patients on a sodium-restricted diet.

Use during pregnancy or breastfeeding.

Adequate data on the use of citicoline in pregnant women are lacking. Data on the excretion of citicoline in breast milk and its effects on the fetus are unknown. The drug may be prescribed during pregnancy or breastfeeding only if the expected therapeutic 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 or operate complex machinery.

Method of administration and dosage.

The recommended dose for adults is from 500 mg to 2000 mg per day depending on the severity of symptoms.

The drug is intended for intramuscular or intravenous administration. For intravenous use, the drug may be administered by slow injection (over 3–5 minutes depending on the dose administered) or by infusion (rate: 40–60 drops per minute).

Maximum daily dose – 2000 mg.

The duration of treatment depends on the course of the disease and is determined by the physician.

Elderly patients do not require dose adjustment.

The injection solution is intended for single use only. The drug should be used immediately after opening the ampoule. Any unused portion must be discarded. The drug may be mixed with all isotonic solutions for intravenous administration, as well as with hypertonic glucose solution.

If necessary, treatment may be continued with the oral solution form of the drug.

Children. Experience with use in children is limited.

Overdose.

No cases of overdose have been reported.

Side effects.

Side effects occur very rarely (<1/10,000), including isolated cases.

Central and peripheral nervous system disorders: severe headache, vertigo, hallucinations.

Cardiovascular disorders: arterial hypertension, arterial hypotension, tachycardia.

Respiratory system 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, local reactions at the site of administration.

Shelf life. 2 years.

Storage conditions.

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

Keep out of reach of children.

Incompatibility. Do not use solvents not specified in the section "Instructions for use and dosage".

Packaging. 4 ml in a vial № 5 (5×1), № 10 (5×2) in a blister pack in a carton.

Prescription status. Prescription only.

Manufacturer. Limited liability company "Pharmaceutical Company "Zdorovia".

Manufacturer's address and place of business.

22 Shevchenka Street, Kharkiv, Kharkiv region, 61013, Ukraine.