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Citicoline sodium tablets 500mg are a widely used medication for the treatment of neurological disorders, with its core component being phosphatidylcholine sodium, chemically known as the monosodium salt of choline cytidine diphosphate. As a nucleoside derivative, it plays multiple roles in improving brain function by promoting brain cell metabolism, repairing cell membrane structure, and enhancing neurotransmitter synthesis. Although it is difficult to penetrate the blood-brain barrier, its concentration in damaged brain tissue is significantly higher than that in normal brain tissue, and its residence time is prolonged, providing pharmacokinetic evidence for its targeted effect in nerve repair.
Appearance:
White or off white tablets, odorless, soluble in water, insoluble in ethanol and acetone.
Dosage form specifications:
Common specifications are 0.1g/tablet and 0.2g/tablet, and packaging forms include composite hard sheet PTP aluminum foil packaging (10 tablets/board/box or 10 tablets/board x 2 boards/box).
Approval number:
Taking the national drug approval number H20100008 as an example (specific to the actual product).
Usage and safety: The oral dosage is usually 0.2 grams per dose, taken 3 times a day with warm water. The adverse reactions are mild, occasionally accompanied by gastrointestinal discomfort, headache or insomnia, which can be relieved on their own after discontinuation of the medication. Please note that it is contraindicated for those who are allergic to the ingredients of the medication. Pregnant and lactating women should use the medication with caution and should not be used in combination with chlorhexidine.
Additional information of chemical compound:
| Product Name | Citicoline Sodium Powder | Citicoline Sodium Tablets | Citicoline Sodium Injection |
| Product Type | Powder | Tablet | Injection |
| Product Purity | ≥99% | ≥99% | ≥99% |
| Product Specifications | Customizable | Customizable | Customizable |
| Product Package | Customizable | Customizable | Customizable |
Our Product
Citicoline sodium +. COA
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Certificate of Analysis |
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Compound name |
Citicoline sodium | |
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CAS No. |
14769-73-4 | |
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Grade |
Pharmaceutical grade | |
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Quantity |
Customized | |
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Packaging standard |
Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
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Lot No. |
20250109001 |
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MFG |
Jan 12th 2025 |
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EXP |
Jan 8th 2029 |
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Structure |
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| TEST STANDARD | GB/T24768-2009 Industry. Stnndard | |
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Item |
Enterprise standard |
Analysis result |
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Appearance |
White or almost white powder |
Conformed |
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Water content |
≤4.5% |
0.30% |
| Loss on drying |
≤1.0% |
0.15% |
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Heavy Metals |
Pb≤0.5ppm |
N.D. |
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As≤0.5ppm |
N.D. | |
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Hg≤0.5ppm |
N.D. | |
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Cd≤0.5ppm |
N.D. | |
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Purity (HPLC) |
≥99.0% |
99.5% |
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Single impurity |
<0.8% |
0.48% |
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Residue on ignition |
<0.20% |
0.064% |
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Total microbial count |
≤750cfu/g |
80 |
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E. Coli |
≤2MPN/g |
N.D. |
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Salmonella |
N.D. | N.D. |
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Ethanol (by GC) |
≤5000ppm |
400ppm |
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Storage |
Store in a sealed, dark and dry place at-20 degrees |
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Citicoline sodium tablets 500mg, as a nucleoside derivative drug, are widely used in human medicine for the treatment of neurological diseases such as traumatic brain injury and cerebrovascular accidents. With the development of veterinary medicine, its potential application value has gradually attracted attention from the veterinary field.
Application scenarios:
Skull fractures and brain contusions caused by dog and cat traffic accidents, falls from heights.
Recovery of consciousness disorders after brain tumor resection, intracranial hematoma removal, and other surgeries.
Mechanism of action:
By activating the ascending activation system of the brainstem reticular formation, the coma time is shortened and awakening is promoted.
Enhance the function of the pyramidal tract, improve postoperative limb paralysis, and improve limb muscle strength and coordination.
Reduce brain edema, lower intracranial pressure, and alleviate secondary brain injury.
Clinical case:
A controlled study was conducted on 12 dogs with traumatic brain injury in a certain animal hospital. The treatment group (treated with 0.2g sodium phosphatidylcholine twice a day in combination with conventional therapy) had a 40% reduction in coma duration and a 2.1 point improvement in motor function score (modified Ashworth scale) 30 days after surgery (p<0.05) compared to the control group.
Application scenarios:
Recovery period for stroke in dogs and cats (such as vertebral artery embolism, carotid artery stenosis), cerebral hemorrhage (such as hypertensive intracerebral hemorrhage, secondary bleeding from coagulation disorders).
Cognitive impairment caused by brain atrophy in elderly pets.
Mechanism of action:
Increase cerebral blood flow, improve metabolism in the ischemic penumbra area, and promote neurological function recovery.
Inhibit neuronal apoptosis and reduce the extent of brain tissue necrosis.
Regulate the cholinergic system and improve cognitive indicators such as memory and attention.
Clinical research:
A randomized controlled trial of 20 stroke cats showed that the phosphatidylcholine sodium group (0.1g/time, 3 times a day, for 6 consecutive weeks) had a 35% improvement in activities of daily living (ADL) scores compared to baseline, while the control group only improved by 18% (p<0.01).
The cognitive function test on elderly dogs showed that after continuous medication for 3 months, the MMSE score increased by an average of 2.8 points, and no significant adverse reactions were observed.
Application scenarios:
Brain damage caused by carbon monoxide poisoning, organophosphate pesticide poisoning, heavy metal poisoning, etc.
Central nervous system depression caused by drug overdose (such as sedatives, antiepileptic drugs).
Mechanism of action:
Eliminate free radicals and alleviate oxidative stress damage.
Promote the repair of brain cell membrane phospholipids and restore neuronal function.
Regulate neurotransmitter balance and alleviate symptoms such as consciousness disorders and seizures caused by poisoning.
Case support:
A certain pet hospital treated 8 dogs with carbon monoxide poisoning. The group treated with phosphatidylcholine sodium (0.2g/time, twice a day, combined with hyperbaric oxygen therapy) had a 50% reduction in consciousness recovery time compared to the group treated with hyperbaric oxygen alone, and no delayed nerve damage occurred.
Adjuvant therapy for neurodegenerative diseases
Application scenarios:
Canine cognitive dysfunction syndrome (CCDS), feline Alzheimer's disease (fAD), etc.
Degenerative spinal cord disease and secondary nerve injury due to intervertebral disc herniation.
Mechanism of action:
Promote the expression of nerve growth factor (NGF), support synaptic remodeling and nerve regeneration.
Improve acetylcholine levels in the brain and delay cognitive decline.
Enhance neural plasticity and promote motor function recovery.
Research progress:
Preliminary experiments have shown that the combination of phosphatidylcholine sodium and mecobalamin treatment in CCDS dogs resulted in a 40% increase in cognitive function score (CDS) after 6 months compared to the monotherapy group, and a significant decrease in β - amyloid protein (A β) levels in cerebrospinal fluid.
Pet medication plan and safety
Dosage and administration method
Recommended dosage:
Dogs: 0.1-0.2g/time, 2-3 times a day (adjusted by weight, small dogs 0.1g/time, large dogs 0.2g/time).
Cat: 0.05-0.1g/time, twice a day (0.05g/time for weight<5kg, 0.1g/time for weight ≥ 5kg).
DRoute of administration:
Oral administration: suitable for mild to moderate cases or long-term maintenance treatment, should be taken after meals to reduce gastrointestinal irritation.
Injection: For critically ill patients or those in urgent need of rapid action, the intravenous infusion rate should be controlled within 0.5g/hour (diluted to 250ml of 5% glucose injection).
Adverse reaction monitoring
Common reactions:
Gastrointestinal tract: Nausea (5% -10%), vomiting (3% -5%), mostly transient, can be relieved by taking after meals.
Nervous system: headaches (2% -4%), insomnia (1% -2%), may be related to central nervous system excitability.
Serious risk:
Blood pressure fluctuations: Injection administration may cause transient hypotension (with an incidence rate of about 0.1%), which requires close monitoring.
Allergic reactions: rash (0.5% -1%), itching (0.3%), and rare occurrence of anaphylactic shock.
Taboos and Caution
Absolute taboo:
Individuals allergic to citicoline sodium tablets 500mg or excipients.
Individuals with a history of severe allergy to chloroesters.
Relative taboos:
Acute phase of cerebral hemorrhage (within 72 hours).
Uncontrolled intracranial pressure increase.
Patients with severe arrhythmia.
Pharmacokinetic characteristics: dynamic distribution of targeted brain injury areas
Intravenous administration: The drug rapidly enters the bloodstream, and the blood drug concentration reaches its peak within 5 minutes (Cmax about 50-100 μ g/mL), followed by biphasic decay (alpha phase half-life of 15 minutes, beta phase half-life of 3.5 hours).
Penetration of blood-brain barrier: About 1% -3% of drugs can penetrate the blood-brain barrier, and their concentration in damaged brain tissue is significantly increased (up to 5-10 times that of normal brain tissue), and the residence time is prolonged (active ingredients can still be detected after 24 hours).
Metabolic pathway: Mainly through liver dephosphorylation to generate choline and cytidine diphosphate, some choline is converted to trimethylamine (TMA) and excreted through the lungs, while cytidine diphosphate is further metabolized into uric acid and excreted in urine.
Excretion characteristics: 70% -80% of drugs are excreted in the form of metabolites through the kidneys, 10% -15% are excreted through bile, and less than 1% of the original drug is excreted.
Elderly individuals: Decreased liver and kidney function leads to a 30% increase in AUC, with a half-life extended to 5 hours. The dosage needs to be adjusted to 0.1-0.2g/day.
Children: The body surface area is small and the distribution volume is reduced. It is recommended to administer 0.02-0.05g/kg/day.
Liver and kidney dysfunction: When the AUC of patients with severe liver injury increases by 2 times and the creatinine clearance rate is less than 30mL/min, the half-life is prolonged to 8 hours and needs to be reduced by 50%.
Collaborative application with other drugs
Combination therapy of antibiotics for infectious encephalopathy
Case: Encephalitis caused by meningococcal infection, the combination of sodium phosphatidylcholine and ceftriaxone (50mg/kg, twice daily) can simultaneously control infection and repair nerve damage.
Mechanism: Antibiotics clear pathogens, and phosphatidylcholine sodium reduces secondary damage caused by inflammation.
Used in combination with neuroprotective agents
Solution: Sodium phosphatidylcholine (0.2g/time, twice daily)+Mecobalamin (0.5mg/time, once daily).
Advantages: Mecobalamin promotes myelin repair, while sodium phosphatidylcholine enhances neuronal metabolism and synergistically improves neurological function.
Synergy with antiepileptic drugs
Application:
After status epilepticus induced brain injury, the combination of phosphatidylcholine sodium and phenobarbital (2-4mg/kg, twice daily) can reduce epilepsy recurrence and promote brain function recovery.
Limitations and Future Directions of Research
Existing shortcomings
Lack of pet specific dosage forms:
Currently, drug specifications (0.1g/tablet, 0.2g/tablet) are mostly designed based on human dosage, and there is a need to develop pet specific low-dose formulations.
Long term safety data is missing:
Existing studies mostly focus on short-term efficacy, and further evaluation is needed for long-term effects on liver and kidney function, endocrine system, and other factors.
Pharmacokinetic differences:
There are differences in metabolic enzyme activity and plasma protein binding rate between pets and humans, and targeted optimization of the dosing regimen is needed.
Future research directions
Targeted delivery system:
Study carriers such as liposomes and nanoparticles to increase the concentration of drugs in pet brain tissue.
Development of Compound Preparations:
Explore the combination of compound preparations with methylcobalamin, nerve growth factor, etc. to enhance therapeutic efficacy.
Indications expansion:
Conduct clinical trials in neurodegenerative diseases such as Parkinson's disease in dogs and multiple sclerosis in cats.
Citicoline sodium tablets 500mg have broad application prospects in the field of pets, especially in the treatment of traumatic brain injury, cerebrovascular accidents, toxic encephalopathy, and neurodegenerative diseases, showing potential value.
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