Buy Ceresil Canon solution 250 mg/ml 4 ml 5 pcs
  • Buy Ceresil Canon solution 250 mg/ml 4 ml 5 pcs

Citicoline [CDP-Choline]

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2019-06-23
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Clinical Pharmacology

Pharmacodynamics

Citicoline is a natural endogenous compound that is an intermediate metabolite in the synthesis of phosphatidylcholine - one of the main structural components of the cell membrane. Citicoline

being a precursor of the key ultrastructural components of the cell membrane (mainly phospholipids), it has a wide spectrum of action - helps to restore damaged cell membranes, inhibits the action of phospholipases, prevents excessive formation of free radicals, and also prevents cell death by affecting the mechanisms of apoptosis. In the acute period of a stroke, citicoline reduces the amount of damage to brain tissue, improves cholinergic transmission. In traumatic brain injury, reduces the duration of post-traumatic coma and the severity of neurological symptoms, in addition, reduces the duration of the recovery period. In chronic cerebral hypoxia, citicoline is effective in treating cognitive disorders, such as memory impairment, lack of initiative, difficulties encountered in performing daily activities and self-care. Increases the level of attention and consciousness, and also reduces the manifestation of amnesia.

Citicoline is effective in treating sensory and motor neurological disorders of degenerative and vascular etiology.

Pharmacokinetics

Suction

Citicoline is well absorbed when taken orally. Absorption after oral administration is almost complete, and bioavailability is approximately the same as after intravenous administration.

Distribution

Citicoline is largely distributed in brain structures, with the rapid introduction of choline fractions into structural phospholipids and cytidine fractions - into cytidine nucleotides and nucleic acids.

Citicoline penetrates the brain and actively integrates into the cellular, cytoplasmic and mitochondrial membranes, forming part of the structural phospholipid fraction.

Metabolism

The drug is metabolized in the intestine and in the liver to form choline and cytidine. After taking the concentration of choline in the blood plasma increases significantly.

Removal

Only 15% of the administered dose of citicoline is excreted from the human body: less than 3% - by the kidneys and through the intestines, and about 12% - with exhaled CO2.

In the excretion of citicoline in the urine can be divided into 2 phases: the first phase, which lasts about 36 hours, during which the rate of excretion decreases rapidly, and the second phase, during which the excretion rate decreases much more slowly. The same is observed in exhaled CC2 - the elimination rate decreases rapidly after about 15 hours, and then decreases much more slowly.

Indications

  • The acute period of ischemic stroke (as part of complex therapy).
  • The recovery period ischemic and hemorrhagic strokes.
  • Traumatic brain injury (TBI), acute (as part of complex therapy) and the recovery period.
  • Cognitive and behavioral disorders in degenerative and vascular diseases of the brain.

Composition

1 ml of solution contains:

active ingredient: citicoline sodium 104.50 mg (in terms of citicoline 100 mg);

excipients: banana flavor (essence “Banana”) 0.4 mg, glycerin 50 mg, potassium sorbate 3 mg, methyl parahydroxybenzoate 1.45 mg, sodium saccharinate 0.2 mg, sodium citrate 6 mg, propyl parahydroxybenzoate 0.25 mg, sorbitol 200 mg, citric acid solution 50% to pH 5.9 - 6.1, purified water to 1 ml.

CDP-Choline is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Ceresil Canon solution
Recognan® Geropharm Russia solution
Neipilept® Sotex Russia solution
Ceraxon® Ferrer Internacional S.A Italy solution

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Citicoline [CDP-Choline]

Dosage and Administration

Ceresil® Canon oral solution is administered orally. Before use, the drug can be diluted in a small amount of water (100-120 ml or ½ cup).

Accepted with meals or between meals.

Recommended Dosing Regimen

Acute ischemic stroke and traumatic brain injury (TBI): 1000 mg (10 ml) every 12 hours from the first day after diagnosis, treatment duration of at least 6 weeks.

The recovery period of ischemic and hemorrhagic strokes, the recovery period of TBI, cognitive and behavioral disorders in degenerative and vascular diseases of the brain: 500-2000 mg per day (5-10 ml 1-2 times a day). Dosage and duration of treatment depending on the severity of the symptoms of the disease.

Adverse reactions

Frequency of side effects

Very rare

In some cases, Cerezil® Canon can stimulate the parasympathetic system, as well as provide a short-term change in blood pressure.

If any of the side effects indicated in the instructions are aggravated, or any other side effects that are not indicated in the instructions have been noticed, you should inform your doctor.

  • Hypersensitivity to any of the components of the drug;
  • Severe vagotonia (predominance of the parasympathetic part of the autonomic nervous system);
  • Due to the lack of sufficient clinical data, it is not recommended for use in children under 18 years of age.

Drug interactions

Citicoline enhances the effects of levodopa.

It should not be used simultaneously with drugs containing meklofenoksat.

Pregnancy and Lactation

Sufficient data on the use of citicoline in pregnant women are not available. Although no negative effects have been identified in animal studies, during pregnancy the drug Ceresil® Canon is prescribed only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

When prescribing Ceresil® Canon during lactation, women should stop breastfeeding, since there are no data on the allocation of citicoline with breast milk.

Special instructions

In the cold, a small amount of crystals may form due to the temporary partial crystallization of the preservative. Upon further storage in recommended conditions, the crystals dissolve within a few months. The presence of crystals does not affect the quality of the drug.

Influence on ability to drive vehicles and mechanisms

During the period of treatment, care should be taken when performing potentially hazardous activities that require special attention and quick reactions (driving and other vehicles, working with moving machinery, the work of the dispatcher and operator, etc.).

Overdosage

Given the low toxicity of the drug overdose cases are not described, even in case of exceeding therapeutic doses.

  • Brand name: Ceresil Canon
  • Active ingredient: Citicoline
  • Dosage form: Oral solution
  • Manufacturer: Veropharm

Studies and clinical trials of CDP-Choline (Click to expand)

  1. Idarubicin alone or in combination with citarabine and etoposide (3 + 3 + 5 protocol) in acute non-lymphoblastic leukaemia
  2. Mapping of the basal forebrain cholinergic system of the dog: A choline acetyltransferase immunohistochemical study
  3. Distribution of choline acetyltransferase and acetylcholinesterase in vocal control nuclei of the budgerigar (Melopsittacus undulatus)
  4. Development of cholinergic and GABAergic neurons in the rat medial septum: Different onset of choline acetyltransferase and glutamate decarboxylase mRNA expression
  5. Distribution of choline acetyltransferase immunoreactivity in the brain of anuran (Rana perezi,Xenopus laevis) and urodele (Pleurodeles waltl) amphibians
  6. Choline acetyltransferase expression during a putative developmental waiting period
  7. Distribution of acetylcholinesterase and choline acetyltransferase in the main and accessory olfactory bulbs of the hedgehog(Erinaceus europaeus)
  8. Estrogen receptor immunoreactivity in the adult primate brain: Neuronal distribution and association with p75,trkA, and choline acetyltransferase
  9. Ovarian hormones differentially influence immunoreactivity for dopamine ?- hydroxylase, choline acetyltransferase, and serotonin in the dorsolateral prefrontal cortex of adult rhesus monkeys
  10. Preservation of nucleus basalis neurons containing choline acetyltransferase and the vesicular acetylcholine transporter in the elderly with mild cognitive impairment and early Alzheimer's disease
  11. Localization of NADPH diaphorase/nitric oxide synthase and choline acetyltransferase in the spinal cord of the frog,Rana perezi
  12. Distribution of choline acetyltransferase immunoreactivity in the brain of an elasmobranch, the lesser spotted dogfish (Scyliorhinus canicula)
  13. Localization of choline acetyltransferase in the developing and adult turtle retinas
  14. Colocalization of choline acetyltransferase and ?-aminobutyric acid in the developing and adult turtle retinas
  15. The determination of the choline content of feed ingredients using choline kinase
  16. The choline content of feed ingredients and mixed feeds determined by an enzymatic assay
  17. Localization of choline acetyltransferase-expressing neurons inDrosophila nervous system
  18. Variations in intracellular choline levels may account for differences in glycine betaine synthesis between conspecific oyster populations responding to hyperosmotic stress
  19. Choline dehydrogenase kinetics contribute to glycine betaine regulation differences in Chesapeake Bay and Atlantic oysters
  20. Positron emission tomography of esophageal carcinoma using 11C-choline and 18F-fluorodeoxyglucose : A novel method of preoperative lymph node staging
  21. Brain-derived neurotrophic factor spares choline acetyltransferase mRNA following axotomy of motor neurons in vivo
  22. Inhibition of dopamine and choline acetyltransferase concentrations in rat CNS neurons by rat α1- and α2-macroglobulins
  23. CDP-choline: Neuroprotection in transient forebrain ischemia of gerbils
  24. Methyl-group donors cannot prevent apoptotic death of rat hepatocytes induced by choline-deficiency
  25. Differential regulation of choline acetyltransferase expression in adult Drosophila melanogaster brain

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