Molecule Info

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Description

Citicoline also known as cytidine diphosphate-choline (CDP-Choline) & cytidine 5'-diphosphocholine is a psychostimulant/nootropic. It is an intermediate in the generation of phosphatidylcholine from choline and is indicated in the treatment of unconsciousness following cerebral trauma, traffic accident & brain operation. Chronic stage: Neural & psychiatric disorders (hemiplegia, dyskinesia, motorpalsy, amnesia aphasia, disorientation & headache) following apoplexy, head injury & cerebral operation.

ATC Classification N06BX06 - citicoline; Belongs to the class of other agents used as CNS stimulant.
Indication(s) & Dosage

Citicoline is indicated in the treatment of unconsciousness following cerebral trauma, traffic accident & brain operation. Chronic stage: Neural & psychiatric disorders (hemiplegia, dyskinesia, motorpalsy, amnesia aphasia, disorientation & headache) following apoplexy, head injury & cerebral operation.

Oral Formulation:

Head injury Adult: 200-600 mg daily in divided doses. Cerebrovascular disorders Adult: 200-600 mg daily in divided doses. Parkinsonism Adult: 200-600 mg daily in divided doses.

Parenteral Formulation:

Head injury Adult: Up to 1 g IM/IV daily. Cerebrovascular disorders Adult: Up to 1 g IM/IV daily. Parkinsonism Adult: Up to 1 g IM/IV daily.

Contraindication(s)
  • Unconciousness
  • Brain surgery
  • Pregnancy
  • Breast feeding
Precaution(s)

For patients with acute, severe and progressive disturbances of consciousness due to head injury and brain surgery, Citicoline injection should be administered in conjunction with hemostatics and intracranial pressure relieving drugs, or treatment such as hypothermyPatients are advised not to operate heavy machinery or automobiles until the full effect of Citicoline is known. Do not consume alcohol while taking Citicoline. Make sure your doctor is aware of upcoming surgeries you may have scheduled; or will be scheduling while taking this medication. Contact your doctor for professional advice if you experience a cold, coughs or allergies. You should not try to treat yourself for such symptoms. Some ingredients found in other medications may have conflicting affects while taking Citicoline and may affect desired results.

Adverse Drug Reaction(s)

Most common adverse reactions associated with Citicoline are:

  • Insomnia
  • Headache
  • Diarrhea,
  • Low or high blood pressure
  • Nausea
  • Blurred vision
  • Chest pains
Pregnancy Category (FDA)

Category D : There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Nursing mothers: There is not enough evidence on citicoline’s safety in breastfeeding women. Citicoline should be used in lactation only when benefits justify the potential risks.

Pharmacology

Citicoline is reported to increase blood flow and O2 consumption in the brain. It is also involved in the biosynthesis of lecithin. 

When infused intravenously in humans, it is rapidly hydrolyzed to choline and cytidine for delivery to tissues throughout the body. In normal volunteers, at the end of a 30 minute infusion, plasma levels of citicoline are already virtually undetectable, while choline and cytidine levels are at a peak, with continued elevated circulating concentrations for 6 hours. Though not as rapid as intravenous administration, oral administration also provides an efficient means of delivery, with choline and cytidine plasma levels peaking 2 hours after a single oral dose.
Passage across the blood‐brain barrier is efficient. Radioactive tracer studies in rats show that, after intravenous administration of radioactively labeled citicoline, labeled phospholipid concentrations in the brain increase steadily over the next 10 hours and remain high at 48 hours. Exogenous citicoline achieves wide distribution throughout the brain.

PHARMACODYNAMICS:
When administered orally, it is absorbed almost completely, and its bioavailability is approximately the same when administered intravenously. Once absorbed, the cytidine and choline disperse widely throughout the body, cross the blood‐brain barrier, and reach the central nervous system (CNS), where they are incorporated into the phospholipids fraction of the cellular membrane and microsomes.
The concept that the administration of exogenous Citicoline can augment the synthesis of neural membrane phospholipids is attractive, because accelerated replacement or repair plays a critical role in maintaining the healthy function of numerous physiological processes. It has shown the therapeutic efficacy in a variety of diseases in which membrane disorder, dysfunction, or degeneration result in cellular and tissue ischaemia and necrosis.


PHARMACOLOGICAL PROPERTIES:
Citicoline activates the bio‐synthesis of structural phospholipids in the neuronal membrane, increases cerebral metabolism and increases the level of various neurotransmitters, including acetylcholine and dopamine. Citicoline has shown neuro‐protective effects in situations of hypoxia and ischaemia, as well as improved learning and memory performance in animal models for the brain aging. 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.

 

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