Ceralin-Lekpharm (Solution) Instructions for Use

Marketing Authorization Holder

Lekpharm, SOOO (Republic of Belarus)

ATC Code

N06BX06 (Citicoline)

Active Substance

Citicoline (Rec.INN registered by WHO)

Dosage Forms

	Ceralin-Lekpharm	Solution for intravenous and intramuscular administration 125 mg/1 ml: amp. 4 ml 5 or 10 pcs.
		Solution for intravenous and intramuscular administration 250 mg/1 ml: amp. 4 ml 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for intravenous and intramuscular administration transparent, colorless or slightly yellowish in color.

Excipients: 1M sodium hydroxide solution or 1M hydrochloric acid solution – to pH 7.2±0.1, water for injections – up to 1 ml.

4 ml – ampoules of colorless glass (5) – blister packs (1) – cardboard packs.
4 ml – ampoules of colorless glass (5) – blister packs (2) – cardboard packs.

Solution for intravenous and intramuscular administration transparent, colorless or slightly yellowish in color.

Excipients: 1M sodium hydroxide solution or 1M hydrochloric acid solution – to pH 7.2±0.1, water for injections – up to 1 ml.

4 ml – ampoules of colorless glass (5) – blister packs (1) – cardboard packs.
4 ml – ampoules of colorless glass (5) – blister packs (2) – cardboard packs.

Clinical-Pharmacological Group

Nootropic drug

Pharmacotherapeutic Group

Nootropic agent

Pharmacological Action

Citicoline, being a precursor of key ultrastructural components of the cell membrane (mainly phospholipids), has a wide spectrum of action: it promotes the restoration of damaged cell membranes, inhibits the action of phospholipases, preventing the excessive formation of free radicals, and also prevents cell death by acting on apoptosis mechanisms.

In the acute period of stroke, it reduces the volume of damaged tissue and improves cholinergic transmission.

In traumatic brain injury, it reduces the duration of post-traumatic coma and the severity of neurological symptoms, and also contributes to a reduction in the duration of the recovery period.

Citicoline is effective in the treatment of cognitive, sensory, and motor neurological disorders of degenerative and vascular etiology.

In chronic cerebral ischemia, Citicoline is effective in the treatment of disorders such as memory impairment, lack of initiative, and difficulties in performing daily activities and self-care. It increases the level of attention and consciousness and also reduces the manifestation of amnesia.

Pharmacokinetics

After parenteral administration, the plasma concentration of choline increases significantly. Citicoline is largely distributed in the structures of the brain, with rapid incorporation of choline fractions into structural phospholipids and cytidine fractions into cytidine nucleotides and nucleic acids. Citicoline penetrates the brain and is actively incorporated into cellular, cytoplasmic, and mitochondrial membranes, becoming part of the structural phospholipid fraction.

With intravenous and intramuscular administration, Citicoline is metabolized in the liver to form choline and cytidine. Only 15% of the administered dose of citicoline is excreted from the human body: less than 3% by the kidneys and through the intestines and about 12% in exhaled air. Two phases can be distinguished in the urinary excretion of citicoline: the first phase, lasting about 36 hours, during which the excretion rate decreases rapidly, and the second phase, during which the excretion rate decreases much more slowly. The same is observed in exhaled air – the excretion rate decreases rapidly after approximately 15 hours and then decreases much more slowly.

Indications

Acute period of ischemic stroke (as part of complex therapy); recovery period of ischemic and hemorrhagic strokes; traumatic brain injury, acute (as part of complex therapy) and recovery period; cognitive and behavioral disorders in degenerative and vascular brain diseases.

ICD codes

Dosage Regimen

Administer parenterally as a slow intravenous injection, intravenous infusion, or by intramuscular injection.

For the acute period of ischemic stroke, use 1000 mg every 12 hours or 2000 mg once daily.

In severe traumatic brain injury and during the acute phase, administer 1000 mg to 2000 mg daily.

For the recovery period of stroke or head injury and for chronic neurological disorders, the dose is 500 mg to 1000 mg daily.

The total daily dosage range is 500 mg to 2000 mg; adjust based on the patient’s condition and clinical response.

The duration of treatment is determined by the severity of the condition; continue therapy through the acute phase and into the rehabilitation period as needed.

For intravenous infusion, dilute the required dose in 50 ml to 250 ml of an appropriate infusion solution, such as 0.9% Sodium Chloride or 5% Dextrose.

Administer the intravenous infusion at a rate of approximately 40-60 drops per minute.

For intramuscular injection, administer deeply into a large muscle mass; rotate injection sites to prevent tissue irritation.

Do not mix Ceralin-Lekpharm in the same syringe or infusion bag with other medications unless compatibility is confirmed.

For oral administration, which may follow parenteral therapy, the daily dose is also 500 mg to 2000 mg, divided into one or two doses.

Adhere strictly to the prescribed dosage and administration route; do not exceed the maximum recommended daily dose.

Adverse Reactions

Allergic reactions: very rarely – rash, skin itching, anaphylactic shock.

Nervous system disorders: very rarely – headache, dizziness, insomnia, agitation, hallucinations. In some cases, the drug may stimulate the parasympathetic system and also briefly change blood pressure.

Digestive system disorders: very rarely – nausea, vomiting, diarrhea, decreased appetite, changes in liver enzyme activity.

General reactions: very rarely – feeling of heat, tremor, shortness of breath, numbness in paralyzed limbs, edema.

Contraindications

Hypersensitivity to citicoline; vagotonia (predominance of the tone of the parasympathetic part of the autonomic nervous system); children and adolescents under 18 years of age.

Use in Pregnancy and Lactation

During pregnancy, use is possible only if the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

If it is necessary to use citicoline during lactation, the issue of discontinuing breastfeeding should be decided, since there are no data on the excretion of citicoline in breast milk.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Dosage adjustment is not required.

Special Precautions

Citicoline should not be used simultaneously with medicines containing meclofenoxate.

Drug Interactions

Citicoline enhances the effects of levodopa.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.