Citicoline Injection

 Composition:

Each ml contains citicoline sodium equivalent to citicoline 250 mg.

Clinical Pharmacology:

Citicoline is a pyrimidine 5′-nucleotide which serves as an essential precursor in the synthesis of lecithin (phosphatidylcholine) and other phospholipids.

Mechanism of Action

The extensive damage caused by stroke requires repair and regeneration of axons and synapses of neurons. So new membrane production is essential.  The primary mechanism by which citicoline is believed to have a therapeutic effect in stroke is its ability to increase the synthesis of phosphatidylcholine, the primary neuronal membrane component. It also enhances acetylcholine synthesis, and might thus ameliorate symptoms caused by the stroke induced loss of cholinergic neurons.

Another mechanism by which citicoline may have a more accurate effect on the outcome of stroke patients relates to its ability to reduce fatty acid accumulation at the site of injury, and thus to prevent further damage.

Citicoline avoids, reduces or reverses the effects of ischemia and/or hypoxia in major parts of animal and cellular models studied and acts in the cranial traumatic forms, reduces and limits the injuries to the membranes of the nerve cells, re-establishes the sensitivity and the function of the regulatory intracellular enzymes and accelerates the re-absorption of the cerebral edema.

Thus considerable evidence accumulated supports the use of citicoline for increasing and maintaining and repairing the membranes and the neuronal function in situations such as ischemia and traumatic injuries. In patients with senile dementia, citicoline reduces the evolution of damage.

Pharmacokinetics

Citicoline is well absorbed following intramuscular administration. After intramuscular doses of citicoline 1000mg, peak increases in plasma choline level were seen in 0.4 hour, with levels increasing from 11 micromol/L (baseline) to 25 micromol/L. Choline delivered from citicoline crosses blood brain barrier. The major portion of  a dose of citicoline appears to be incorporated into tissues and/or used in biosynthetic/biodegradation pathways, including lecithin/lipid membrane synthesis. Citicoline is a metabolized in the liver to free choline. The liver is capable of synthesizing lecithin from choline, and resynthesizing citicoline from cytidine and choline. Half life of free choline is of 2 hours after intramuscular administration. Only small amounts of dose are recovered in urine and feces (less than 3% each.) Approximately 12% of a dose is eliminated through lungs as carbon dioxide.

Indications:

Strocit Injection is indicated for the treatment of patients with disturbances of consciousness resulting from head injury, brain operation, and in the acute stage of cerebral infarction.