active ingredient: citicoline;

1 ml contains 250 mg of citicoline sodium salt;

excipients: diluted hydrochloric acid or sodium hydroxide, water for injections.

Solution for injection.

Physical and chemical properties: Clear colorless liquid.

Other psychostimulants and nootropics. ATC Code N06BX06.

Pharmacodynamics.

Citicoline stimulates the structural phospholipids biosynthesis in the neural cellular membrane, which contributes to the improvement of membrane functions, including the functioning of ion-exchange pumps and neuroreceptors. Due to the stabilizing effect upon the neural membrane, citicoline manifests its anti-oedemateous properties reducing the cerebral oedema. Citicoline inhibits the activity of certain phospholipases and the residual generation of free radicals, prevents the destruction of membrane systems and ensures the preservation of a protective antioxidant system.

Citicoline reduces the volume of lesional tissue, preventing cell death by affecting the mechanisms of apoptosis, and improves cholinergic transmission. Citicoline also demonstrates preventive neuroprotective effect in focal cerebral stroke.

Citicoline contributes to rapid functional rehabilitation of patients with acute cerebrovascular diseases, reducing ischemic brain damage, which is confirmed by X-ray findings.

In traumatic brain injury, citicoline shortens the recovery period and reduces the intensity of post-traumatic syndrome.

Citicoline promotes brain activity, reduces the manifestation of amnesia, and improves the outcomes of cognitive, sensitive and motor disorders associated with cerebral ischemia.

Pharmacokinetics.

Citicoline is well absorbed after oral administration, intramuscular and intravenous injection. After the administration, the serum choline level is significantly increased.

The drug is metabolized in the intestine and the liver with the formation of choline and cytidine. After the administration, citicoline is absorbed by the brain tissue, the choline influences on phospholipids, cytidine effects on cytidine nucleotides and nucleic acids. Citicoline quickly reaches the brain tissue and is actively embeded into the cell membranes, cytoplasm and mitochondria, triggering the phospholipids’ activity.

Only a small quantity of the administered dose is excreted in urine and feces (less than 3%). Approximately 12% of the administered dose is excreted through the respiratory tract. Two phases of the renal and pulmonary excretion of the drug are distinguished: the first phase is rapid elimination (for renal excretion – lasting 36 hours after administration, for pulmonary excretion – during the first 15 hours), and the second phase is slow elimination. The most of the administered dose of the drug is metabolized.

Indications.

• Cerebral stroke, acute phase of cerebrovascular diseases and treatment of complications and outcomes of cerebrovascular diseases.
• Traumatic brain injury and its neurological outcomes.
• Cognitive impairment and behavioral disorders assosiated with chronic vascular and degenerative cerebral disorders.

• Hypersensitivity to any of the drug components.
• Predominance of the parasympathetic part of the autonomic nervous system (severe vagotonia).

Citicoline enhances the effect of levodopa. Do not administer concurrently with medications containing meclofenoxate.

In case of a sustained intracranial hemorrhage, the dose of 1000 mg per day and the intravenous infusion rate of 30 drops per minute should not be exceeded.

The drug should be used immediately when opened. The ampoule with the drug is intended for single use only. Discard unused portion of the drug.

Pregnancy and breast feeding consideration.

There is no sufficient evidence of the use of citicoline in pregnant women. There is lack of evidence of citicoline secretion into the breast milk and its effect on the foetus. Therefore, during pregnancy or breast feeding the drug should be used only when the expected maternal benefits exceed the potential foetal risk.

Effects on ability to drive and use machines.

Taking into account possible side effects, during the use of the drug it is recommended to refrain from drive the automobile transport or other mechanisms.

The drug is administered intravenously or intramuscularly. Intravenously, the drug is administered in the form of a slow injection (within 3-5 minutes depending upon the administered dose) or a drip infusion (40-60 drops per minute).

The recommended dose for adults is from 500 mg to 2000 mg per day.

Treatment:  the first 2 weeks – 500-1000 mg twice per day intravenously, then – 500-1000 mg twice per day intramuscularly. Maximum daily dose is 2000 mg.

In acute conditions and urgent cases, the maximum therapeutic effect is achieved when prescribing the drug in the first 24 hours.

Drug dosage and treatment duration depend upon the severity of brain lesions and are determined by the physician individually. The recommended treatment course, when the maximum therapeutic effect is observed, comprises 12 weeks. If necessary, the treatment should be continued with the oral solution form of the preparation.

Elderly patients. No dosage adjustment is required.

Instruction for use of ampule.

1. Separate one ampoule from the block and shake the contents gently, holding the ampoule by its neck.
2. Grasp the ampule with a hand (no leakage of the drug should occur) and rotate the head of ampoule to separate it .
3. Immediately connect a syringe to the ampoule through the formed hole.
4. Invert the ampoule and slowly aspirate its contents into the syringe.
5. Attach the needle to the syringe.

Children.

There is a lack of sufficient clinical data regarding the use of the drug Pharmaxon in children.

Overdose events have not been described.

Very rare (<1/10,000) (including patient reports).

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

Cardiovascular system: arterial hypertension, arterial hypotension, tachycardia.

Respiratory system: dyspnea.

Digestive tract: nausea, vomiting, diarrhea.

Immune system: allergic reactions including: rash, hyperaemia, exanthema, urticaria, purpura, pruritus, angioneurotic oedema, anaphylactic shock.

General reactions: chills, changes in the place of injection.

2 years.

Do not store the drug after opening the ampoule.

Store in the original package at a temperature not more than 25 С. Keep away from children.

The drug should not be mixed with other medicinal products in the same container.

2 ml or 4 ml in ampoules № 5.

Following the doctor’s prescription.