| Each 4 ml ampoule contains 500 mg or

1000 mg citicoline sodium, № 5

 

PHARMACOLOGIC PROPERTIES

ATC Code: N06BX, Psychoanaleptics, psychostimulants, agents used for ADHD and nootropic, other psychostimulants and nootropics

Citicoline is a complex organic molecule that functions as an intermediate in the biosynthesis of cell membrane phospholipids. The extensive damage caused by stroke requires repair and regeneration of the axons and synapses of neurons, so new membrane production is necessary.

Pharmacologic mechanism of action:

Phospholipid Precursor: Evidence of citicoline’s role as a phosphatidylcholine precursor has been found in animal studies. Exogenous citicoline helps preserve the structural and functional integrity of the neuronal membrane. The postulated mechanism involves the bioconversion of citicoline to phosphatidylcholine.

Neuronal Membrane Repair: Citicoline has been investigated as a therapy for stroke patients. Three mechanisms are postulated: (1) ability to repair neuronal membranes via increased synthesis of phosphatidylcholine; (2) repair of damaged cholinergic neurons via potentiation of acetylcholine production; and, (3) reduction of free fatty acid build-up at the site of stroke-induced nerve damage. In addition to phosphatidylcholine, citicoline serves as an intermediate in the synthesis of sphingomyelin, another neuronal membrane phospholipid component. Citicoline also restores the levels of cardiolipin, a phospholipid component of the inner mitochondrial membrane.

Reduction of Free Fatty Acid Build-Up: Citicoline may benefit patients experiencing ischaemia by decreasing the accumulation of free fatty acids at the site of the lesion, which occurs as a result of neuronal cell damage and death.

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 (AD).

Effect on Norepinephrine: Evidence of the ability of citicoline to enhance norepinephrine release in humans was found in scientific studies.

Activation of the Dopaminergic System: With respect to dopaminergic activation, citicoline has been reported to exert dopaminergic agonist effects in the corpus striatum, enhance dopamine synthesis in the striate body (by activation of tyrosine hydroxylase), inhibit dopamine uptake by synaptosomes, and increase sensitivity of dopaminergic receptors that have been down-regulated during prolonged levodopa therapy.

 

THERAPEUTIC INDICATIONS

  • Age-related memory problems: Taking citicoline seems to help memory loss in people aged 50 to 85 years.
  • Long-term blood circulation problems in the brain (cerebrovascular diseases): There is some evidence that taking citicoline by mouth or injecting citicoline into the vein or muscle might improve memory and behavior in patients with long-term cerebrovascular diseases, such as stroke.
  • Stroke recovery: Stroke patients who take citicoline by mouth within 24 hours of having the kind of stroke that is caused by a clot (ischemic stroke) are more likely than other ischemic stroke patients to have a complete recovery within 3 months. Stroke patients who receive intravenous (IV) citicoline within 12 hours of having an ischemic stroke and daily thereafter for 7 days also have improved recovery.

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