Citicoline Injection IP 250 mg/ml (For IM/IV injection use only)
COMPOSITION
Each ml contains:
Citicoline Sodium IP equ. to Citicoline 250 mg
Water for Injections BP q. s.
DESCRIPTION
A clear, colorless to almost colorless solution.
ATC code: N06BX06
PHARMACODYNAMIC
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 acute effect on the outcome of stroke patients relates to its ability to reduce free 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 animals 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 reabsorption of the cerebral edema. Thus, considerable evidence accumulated supports the use of citicoline for increasing, maintaining and repairing the membranes and neuronal function in situations e.g., ischemia and traumatic injuries. In patients with senile dementia, citicoline reduces the evolution of damages.
PHARMACOKINETICS
Absorption
Citicoline is well absorbed following intramuscular administration. After intramuscular dose of citicoline 1000 mg, peak increases in plasma choline levels were seen in 0.4 hours, with levels increasing from 11 micromole/L (baseline) to 25 micromole/L.
Distribution
Choline derived from citicoline crosses the blood-brain barrier, presumably serving as a source of acetylcholine and phosphatidylcholine (lecithin) synthesis. 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.
Metabolism
Citicoline is metabolized in the liver to free choline. The liver is capable of synthesizing lecithin from choline. The half-life of free choline is of 2 hours after intramuscular administration.
Excretion
Only small amounts of dose are recovered in the urine and faeces (less than 3% each). Approximately 12% of a dose is eliminated through the lungs as carbon dioxide.
THERAPEUTIC INDICATION
For the treatment of disturbance of consciousness as resulting from head injuries, parkinsonism, depression, impaired brain functions due to ischaemic stroke, acute stage of cerebral infarction in adult only.
DOSAGE AND ADMINISTRATION
Disturbance of consciousness resulting from head injury or brain operation.
Usually, for adults, a dose of 100/500 mg citicoline injection is administered once or twice a day, by intravenous drip infusion, intravenous or intramuscular injection. The dose may be adjusted to the patient’s age and condition.
Disturbance of consciousness in the acute stage of cerebral infraction.
Usually, a dose of 1,000 mg of citicoline injection is administered once a day, by intravenous injection, for 2 consecutive weeks.
OVERDOSE
There are no known cases of overdose in humans available for citicoline.
CONTRAINDICATION
Hypersensitivity to Citicoline Injection or any other component of the formulation.
WARNING AND PRECAUTIONS
General
For patients with acute, severe and progressive disturbance of consciousness resulting from a head injury or brain operation, citicoline injection should be administered in conjunction with haemostatics and an intracranial pressure-relieving drug, or a treatment such as hypothermia. For patients with disturbance of consciousness in the acute stage of cerebral infarction, it is recommended to start the administration of citicoline injection within 2 weeks after an 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. Care should be exercised to avoid injection at sites along the course of the nerves. In case of 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 maintained. If any such abnormalities such as a drop in blood pressure, a distressing feeling of the chest or dyspnoea are observed, citicoline injection should be discontinued and appropriate measures are taken.
Persistent Intracranial Haemorrhage
In case of persistent intracranial haemorrhage, it is recommended not to exceed the dose of 1,000mg of citicoline daily, given through very slow intravenous administration (30 drops/minute).
PREGNANCY, LACTATION
Pregnancy
There are no adequate and well-controlled studies of citicoline during pregnancy. Citicoline should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus.
Breast-feeding
Caution should be exercised during breastfeeding because it is not known whether citicoline is excreted in breast milk.
DRUG INTERACTION
Carbidopa, Levodopa and Entacapone
Citicoline may enhance the effects of levodopa, carbidopa and entacapone. The exact mechanism is unknown, but animal models suggest that citicoline may increase dopamine levels in the brain and/or improve dopaminergic cell survival. In patients with Parkinson’s disease, a few studies have demonstrated levodopa-saving effects, whereby the addition of citicoline (500/1,200 mg/day) allowed for lower dosages of levodopa to be used with stable or improved therapeutic efficacy and reduced the side effects in some patients. However, data are limited.
Co-administration with Meclofenoxate
Must not be administered in conjunction with medications containing meclofenoxate.
ADVERSE EFFECTS
Stop taking medicine right away and talk to your doctor if you have any of the following adverse effects. Allergic reaction: Itching or hives, swelling in your face or hands, swelling or tingling in your mouth or throat, chest tightness, trouble breathing, or rash. Some Citicoline side effects include elevated body temperature, restlessness, and difficulty sleeping if the supplement is taken in the evening.
PRESENTATION
BRANTON Injections are supplied in 2 ml flint, Type-I USP Ampoule.
STORAGE AND OTHER INFORMATION
Store in a cool and dry place. Protect from light.
Store at below 30°C temperature.
Caution: Not to be used if container is found leaking or solution is hazy or contain any visible solid particles. Keep this medicine out of the sight and reach of children.
