Description
Citicoline (Injection) Solution
Composition
Each mL of Citicoline (injection) contains Citicoline sodium equivalent to 250 mg of Citicoline. The solution is clear, sterile, and preservative-free. It is formulated in water for injection with sodium hydroxide or hydrochloric acid used to adjust pH if necessary.
Description
Citicoline is a neuroprotective nootropic agent that supports brain function by enhancing phospholipid synthesis and maintaining cellular membrane integrity. It promotes recovery in ischemic neurological conditions and improves cognitive function in degenerative brain disorders. Citicoline (injection) is used in acute and chronic neurological conditions, delivered intravenously or intramuscularly for rapid onset of action.
Pharmacological Properties
- Mechanism of action: Citicoline promotes biosynthesis of structural phospholipids in neuronal membranes and enhances cerebral metabolism. It increases norepinephrine and dopamine levels in the CNS and reduces the release of free fatty acids during ischemia, stabilizing cell membranes.
- Neuroprotective effects: Citicoline reduces neuronal apoptosis and limits infarct size in cerebrovascular accidents. It also modulates neuroplasticity and has been studied for its role in neurorepair post-injury.
Pharmacokinetics
Citicoline is rapidly absorbed and hydrolyzed into cytidine and choline. These metabolites cross the blood-brain barrier and are resynthesized into Citicoline in the CNS. It is distributed systemically and eliminated mainly through respiratory CO2 excretion and to a lesser extent by the kidneys.
Indications
- Acute ischemic stroke (adjunctive therapy)
- Traumatic brain injury (TBI)
- Vascular dementia and cognitive decline
- Parkinson’s disease (adjuvant cognitive therapy)
- Alzheimer’s disease (supportive cognitive care, off-label)
Dosage and Administration
- Adults: 500–2000 mg/day via intramuscular or intravenous injection
- Route: Slow IV injection or deep IM injection, once or twice daily
- Dosage should be tailored based on the clinical condition and physician guidance
Contraindications
- Hypersensitivity to Citicoline or any component of the formulation
Precautions
- Use with caution in patients with severe renal or hepatic impairment
- Patients with known seizure disorders or those receiving anticonvulsant therapy should be closely monitored
Side Effects
- Nausea, diarrhea
- Transient hypotension or hypertension
- Insomnia, headache
- Blurred vision
- Injection site reactions (pain, redness)
Severe allergic reactions are rare but require immediate medical attention.
Drug Interactions
No significant interactions have been documented; however, caution is advised when combining Citicoline with CNS-active drugs or hepatically metabolized medications. Always consult with a physician when initiating therapy.
Overdose
Citicoline has a wide therapeutic index. In cases of overdose, symptoms may include nausea, hypotension, flushing, or gastrointestinal upset. Management is symptomatic and supportive.
Storage
- Store below 25°C
- Protect from light and do not freeze
- Keep vials in their original packaging
- Keep out of reach of children and pets
Packaging
Citicoline injection is typically supplied in ampoules of 4 mL (containing 1000 mg), 2 mL (500 mg), or 1 mL (250 mg), depending on local regulations and manufacturer.
Scientific References
Disclaimer
This information is for educational purposes only and does not substitute medical advice. Always consult your physician before using any injectable medication. Use Citicoline only under medical supervision. All treatment decisions should be made by licensed healthcare professionals.






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