Citicoline

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Citicoline is a psychostimulant/nootropic. It is an intermediate in the generation of phosphatidylcholine from choline and a precursor for the neurotransmitter acetylcholine. This neurotransmitter (acetylcholine) is thought to play a vital role in a number of cognitive processes.

Contents

[edit] BRAND NAMES

  • Italy: Citicolin, Difosfocin, Cebrolux, Synapsine

[edit] STRUCTURE

Citicoline.jpg

[edit] MECHANISM OF ACTION

Citicoline (CDP-choline, cytidine diphosphate choline, cytidine 5-diphosphocholine,) is a nucleotide composed of ribose, pyrophosphate, cytosine and choline. It is a naturally occurring, water-soluble biological compound that is an essential intermediate for the synthesis of phosphatidylcholine, a major constituent of the gray matter of brain tissue. Citicoline promotes brain metabolism by enhancing the synthesis of acetylcholine and restoring phospholipid content in the brain.

Citicoline acts by various mechanisms listed below:

  • Phospholipid Precursor: Citicholine activates the biosynthesis of phosphatidylcholine, a structural phospholipid of cell membranes, including neurons.
  • Neuronal Membrane Repair: Citicholine has shown neuroprotective effects in situations of hypoxia and ischaemia
  • Effect on beta-Amyloid: Evidence has surfaced that citicoline counteracts the deposition of beta-amyloid, a neurotoxic protein believed to play a central role in the pathophysiology of Alzheimer’s disease. Citicoline improved learning and memory performance in brain aging.
  • Effect on Neurotransmitters: Citicholine increases the levels of various neurotransmitters, including acetylcholine and dopamine. Acetylcholine is thought to play a vital role in a number of cognitive processes including memory , learning, attention span, concentration, and improved speed of thought.

Furthermore, it has been demonstrated that Citicoline restores the activity the activity of mitochondrial ATPase and of membranal Na+/K+ATPase, inhibits the activation of phospholipase A2 and accelerates the re-absorption of cerebral edema in various experimental models.

When administered orally, Citicoline is absorbed almost completely, and its bioavailability is approximately the same when administered intravenously.

[edit] INDICATIONS

  • Cerebrovascular diseases - e.g. from ischemia due to stroke, where Citicoline accelerates the recovery of consciousness and overcoming motor deficit. Treatment with oral citicoline within the first 24 hours after onset in patients with moderate to severe stroke increases the probability of complete recovery at 3 months [1]
  • Head Trauma of varying severity: In a clinical trial, Citicoline accelerated the recovery from post-traumatic coma and the recuperation of walking ability, achieved a better final functional result and reduced hospital stay. [2]
  • Cognitive disorders of diverse etiology: e.g. senile cognitive impairment which is secondary to degenerative diseases (e.g. Alzheimer's disease) and to chronic cerebral vascular disease. Citicoline improves scores on cognitive evaluation scales and slowed the progression of Alzheimer's disease. [3]
  • Parkinson's disease : Citicoline shown to be effective as co-therapy for Parkinson's disease. Citicoline increases striatal dopamine, allowing significantly reduced doses of levodopa to be used to greater effect. [4]
  • Citicoline improves visual function in patients with glaucoma, amblyopia (lazy eye), and optic neuropathy [5] [6]

[edit] DOSAGE

  • 500-2000 mg daily. Dosage may be adjusted based on the seriousness of the disease. It can be administered orally, intramuscularly, intravenously (3 to 5 minute) injection and in intravenous drop perfusion (dripping speed 40-60 drops/minute). Direct administration in the vein, if it is not made very slowly, can produce hypotension.

[edit] CONTRAINDICATIONS

Patients with hypertonic of the parasympathetic.

[edit] PRECAUTIONS

In case of persistent intracranial hemorrhage, it is recommended not to exceed the dose of 1000 mg daily, in very slow intravenous administration (dripping speed 30 drops/minute). The administration of larger doses could provoke an increase of the cerebral blood flow.

[edit] INTERACTIONS

  • Citicoline must not be administered in conjunction with medication containing meclofenoxate (also known as clophenoxate).
  • Citicoline potentiates the effects of L-dopa.

[edit] PREGNANCY AND LACTATION

There is inadequate evidence of safe use of Citicoline in human pregnancy. Citicoline should be used in pregnancy and lactation only if the potential benefits justify the potential risks.

[edit] SIDE EFFECTS

Occasionally, citicoline may exert a stimulating action of the parasympathetic system, as well as a fleeting and discrete hypotensive effect.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

  1. http://www.ncbi.nlm.nih.gov/pubmed/12468781
  2. http://www.ncbi.nlm.nih.gov/pubmed/8709678
  3. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3363302/
  4. http://www.ncbi.nlm.nih.gov/pubmed/2289218
  5. http://www.ncbi.nlm.nih.gov/pubmed/18929133
  6. http://onlinelibrary.wiley.com/doi/10.1111/j.1468-1331.2008.02099.x/abstract;jsessionid=FA96263B2BE6D0726B206E970BF6AF45.f03t01
Alzheimer/Dementia
Anticholinesterases Donepezil (Aricept, Memac)   Galantamine (Reminyl)   Rivastigmine (Oral) (Exelon)   Rivastigmine (Transdermal) (Exelon Patch)
Glutamatergic NMDA receptor antagonists Memantine (Ebixa)
Psychostimulants and nootropics Aniracetam   Choline   Citicoline   Ginkgo biloba   Piracetam