Citicoline

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Startornyl; France: Rexort, Citicoline; Italy: Cidilin, Citicolin, Citicolina, Difosfocin, Gerolin, Logan, Neurex, Neuroton, Sintoclar; Portugal: Hypercol, Somazina, Startornyl, Trausan; Spain: Numatol, Somazina.

Latin America

Argentina: Complegel Novo, Reagin, Somazina; Brazil: Somazina; Mexico: Onquevit, Somazina, Zunun.

Asia

Japan: Citicoline, Cyscholin, Cysgelin, Nicholin, Recognan, Tesi Cholin.

Drug combinations

Citicoline and Ergoloid Mesylates

Citicoline and Nimodipine

Chemistry

Citicoline Sodium: C~14~H~25~N~4~NaO~11~P~2~ 2H~2~O. Mw: 488.33. (1) Cytidine 5′-(trihydrogen diphosphate), P’-[2-(Trimethylammonio)ethyl], inner salt, monosodium salt; (2) Choline hydroxide, 5′-ester with cytidine 5′-(sodium dihydrogen diphosphate), inner salt. CAS-33818-15-4; CAS-987-78-0 (citicoline)(1994).

Pharmacologic Category

Anti-Dementia Agents; Neuroprotective Agents. (ATC-Code: N06BX06).

Mechanism of action

CDP-choline, supplied exogenously as citicoline, has beneficial physiological actions on cellular function. As the product of the rate-limiting step in the synthesis of phosphatidylcholine from choline, CDP-choline and its hydrolysis products (cytidine and choline) play important roles in generation of phospholipids involved in membrane formation and repair. Citicoline is efficiently utilized in brain cells for membrane lipid synthesis where it not only increases phospholipid synthesis but also inhibits phospholipid degradation.

Therapeutic use

Treatment of senile cognitive impairment, either secondary to degenerative diseases (e.g. Alzheimer’s disease) or to chronic cerebral vascular disease. In patients with chronic cerebral ischemia, citicoline improves scores in cognitive rating scales, while in patients with senile dementia of the Alzheimer type it slows down the course of disease, and neuroendocrine, neuroimmunomodulatory, and neurophysiological benefits have been reported. Citicoline has also been shown to be effective in Parkinson’s disease, drug addictions, and alcoholism, as well as in amblyopia and glaucoma. Along with its neuroprotective properties, citicoline is known to increase in some brain areas the levels and enhance the rate of synthesis of acetylcholine, dopamine, noradrenaline, and serotonin.

Pregnancy and lactiation implications

There are no adequate studies in pregnant women. Use during pregnancy and lactation only if benefit outweighs risk.

Unlabeled use

Contraindications

Hypersensitivity. Hypertonia of the parasympathetic nervous system.

Warnings and precautions

May cause asthma if administered orally, specially in allergy to acetylsalicylic acid. Citicoline promotes the effects of drugs that contain L-dopa.

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