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.
Contra-indications:
History of hypersensitivity to any of the ingredients of this drug.
Warnings and Precautions:
For patients with acute, severe and progressive disturbances of consciousness resulting from head injury or brain operation, citicoline injection should be administered in conjunction with haemostatic and intracranial pressure relieving drug, or such treatment as hypothermia.
For patients with disturbances of consciousness in acute stage of cerebral infarction, it is recommended to start the administration of citicoline injection within two weeks after apoplectic stroke.
In administering citicoline injection intramuscularly, caution should be exercised so as not to affect the tissues, nerves, etc. Intramuscular injection should be given only when indispensable, and should be restricted to the minimum to be required. In particular, repeated injection at the same site should be avoided. Extra care should be exercised in treating prematures, newborns, nursing infants and children. Care should be exercised to avoid injection at sites along the course of nerves. In case intense pain or backflow of blood upon insertion of the injection needle, the needle should be withdrawn immediately and injected at a different site.
In intravenous administration, inject as slowly as possible.
Since shock may occur, close observation should be made. If any such abnormalities such as drop of blood pressure, distressed feeling of the chest or dyspnea is observed, citicoline injection should be discontinued and appropriate measures is taken.
Pregnancy & Lactation
There are no adequate and well controlled studies of citicoline during pregnancy and lactation. Citicoline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Caution should be exercised during breast feeding because it is not known whether citicoline is excreted in human breast milk.
Drug Interactions:
Citicoline must be used with medicines containing meclophenoxate (or centraphenoxine). Citicoline increases the effects of L-dopa.

Side effects:
The commonly observed adverse effects (<0.1-5%) were rash, insomnia, occurrence or intensification on numbness or paralyzed extremities (when used in patients with postapoplectic hemiplegia), nausea, abnormal laboratory values for liver function, and feeling of warmth.
The other adverse effects (<0.1%) were headache, dizziness, excitation, convulsions, anorexia, transient diplopia, transient blood pressure changes, malaise shock, distressed feeling of the chest, and dyspnea.

Dosage and Administration:
Disturbance of consciousness resulting from head injury or brain operation: Usually, for adults, a dose of 100-500 mg of citicoline is administered once or twice a day, by intravenous drip infusion, intravenous injection on intramuscular injection. The dose may be adjusted according to the patient's age and condition.
Disturbance of consciousness in the acute stage of cerebral infarction: Usually, a dose of 100 mg of citicoline is administered once a day, by intravenous injection, for two consecutive weeks.
Storage:
Store in a cool dry place, protected from light.
Presentation:

Citicoline injection is available in 2 ml, and 4 ml ampoules.