One Pharma


One Pharma
Full Prescribing Info
Citicoline (FC tab: sodium).
Each film-coated tablet contains: Citicoline (as Sodium) 1 g.
Each mL contains: Citicoline, KP 250 mg.
Pharmacology: Pharmacodynamics: Film-coated tablet: Citicoline is a derivative of choline and cytidine that is involved in the biosynthesis of lecithin. It is claimed to increase blood flow and oxygen consumption in the brain and has been given in the treatment of cerebrovascular disorders, Parkinsonism, and head injury.
Citicoline is an interneuronal communication enhancer. It increases the neurotransmission levels because it favors the synthesis and production speed of dopamine in the striatum, acting then as a dopaminergic agonist thru the inhibition of tyrosine hydroxylase. Citicoline acts as a presynaptic cholinergic agent which favors the synthesis of acetylcholine. It also decreases the release of serotonin. Citicoline makes the neurons more active, causing the astrocytes to loosen their grip on the capillaries, thus improving microcirculation. By virtue of this action, citicoline has an indirect effect on microcirculation. It has the ability to slightly increase cerebral blood flow and exerts an anti-aggregation effect on platelets.
Solution for injection: Citicoline, being the precursor of key ultrastructural components of a cellular membrane (mainly phospholipids), possesses wide range of activities, promotes restoration of the damaged cell membranes, inhibits action of phospholipases, what prevents excessive formation of free radicals and destruction of cells, affects the mechanisms of apoptosis. In the acute period of stroke it reduces the volume of damaged tissue, improves cholinergic transmission. In head injury it reduces duration of a post-traumatic coma and intensity of neurologic symptoms. Citicoline improves observed during hypoxia symptoms, such as memory impairment, emotional liability, lack of initiative, difficulties at conducting of daily actions and self-service. The drug product does not influence breath, pulse and arterial pressure; therefore long treatment is possible.
Pharmacokinetics: Film-coated tablet: 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 phospholipid fraction of the cellular membrane and microsomes.
The concept that administration of exogenous Citicoline can augment the synthesis of neural membrane phospholipid is attractive, because accelerated replacement or repair plays a critical role in maintaining the healthy function of numerous physiological processes. It has shown therapeutic efficacy in a variety of diseases in which membrane disorder, dysfunction, or degeneration result in cellular and tissue ischaemia and necrosis.
Solution for injection: Citicoline is a water-soluble compound with greater than 90-percent bioavailability. Pharmacokinetic studies on healthy adults show oral doses of citicoline are rapidly absorbed, with less than one percent excreted in feces. Plasma levels peak in a biphasic manner, at one hour after ingestion followed by a second larger peak at 24 hours postdosing. Citicoline is metabolized in the gut wall and liver. The byproducts of exogenous citicoline formed by hydrolysis in the intestinal wall are choline and cytidine. Following absorption, choline and cytidine are dispersed throughout the body, enter systemic circulation for utilization in various biosynthetic pathways, and cross the blood-brain barrier for resynthesis into citicoline in the brain.
Film-coated tablet: It is used in the treatment of cerebrovascular disorders including ischemic stroke, parkinsonism and head injuries.
Solution for injection: Treatment of stupor caused by head trauma, cerebral surgery, acute stage of cerebral infarction and hemiplegia after cerebral apoplexy; treatment of Parkinson's disease in combination with anticholinergics; concomitant therapy for pancreatitis with antiproteolytic agents.
Dosage/Direction for Use
Film-coated tablet: Take one 1 g FCT by mouth once a day or as prescribed by the physician.
Solution for injection: Stupor caused by head trauma and cerebral surgery: The usual adult dosage of Citicoline 100-500 mg once or twice daily given in divided intravenous or intramuscular administration.
Stupor caused by acute stage of cerebral infarction: The usual adult dosage of Citicoline is 1 g once daily for two consecutive weeks.
Hemiplegia after cerebral apoplexy: 1 g or 250 mg of Citicoline is administered intravenously once a day for four weeks. If symptoms are improved, administer intravenously for four more weeks.
Parkinson's disease: The usual daily dose is 500 mg once daily intravenously in concomitant therapy with anticholinergic agent. After concomitant therapy with anticholinergic agent for 3-4 weeks, citicoline should be discontinued and anticholinergic alone can be administered. In case symptoms are impaired, levodopa administration should be considered. Dose of anticholinergic agent may be increased or 250-500 mg of citicoline may be administered concomitantly once daily, every 2-3 weeks unless levodopa can be used. Administration of citicoline should be stopped, provided that after administration of 500 mg of Citicoline plus anticholinergic agent everyday for two weeks, diseases are not improved. It is advisable to avoid concomitant administration with levodopa since combination may cause impairment of myotonia.
Pancreatitis: Under concomitant therapy with antiproteolytic agents, 1 g of citicoline is administered intravenously once a day for 2 consecutive weeks.
Or as prescribed by the physician.
Solution for injection: Toxicity of the drug overdosage cases are not described even in case of excess therapeutic doses.
Patients with hypertonia of the parasympathetic nervous system.
Special Precautions
Film-coated tablet: Citicoline should be used with caution in patients with acute, severe, and progressive disturbances, intracranial pressure relieving drugs or use measures to keep body temperature low.
Solution for injection: In case of stupor caused by acute/severe/progressive head trauma or cerebral surgery, it should be given in concomitant with depressant and hypothermic agent.
Use in Children: It has not been established whether citicoline may adversely affect children.
Use in the Elderly: Use in elderly should be taken with caution considering manifestation of adverse effects
Use In Pregnancy & Lactation
Solution for injection: Since it has not been established whether citicoline may adversely affect pregnant women, this drug should not be used in pregnant women or women of childbearing potential unless the benefit of treatment is considered to outweigh the risk.
Adverse Reactions
Film-coated tablet: Increased parasympathetic effects, fleeting and discrete hypotensor effect.
Solution for injection: Shock: Rarely, shock may occur. It should be sufficiently observed if hypotension, compression of chest, and dyspnea have developed, administration should be discontinued and/or appropriate therapy be instituted.
Hypersensitivity: Eruption may appear occasionally, the administration should be discontinued in this case.
Psychoneurologic: Headache, vertigo, excitation can develop.
Gastrointestinal: Occasionally, nausea, and rarely, anorexia may occur.
Hepatic: Abnormalities in hepatic test may occur.
Others: Sometimes, burning sensation, temporary change in blood pressure, and malaise may appear.
Drug Interactions
Film-coated tablet: Citicoline potentiates the effects of L-dopa. It must not be administered with meclofenoxate (clophenoxate).
Solution for injection: In combination with levodopa, this drug can increase effects of levodopa.
Store at temperatures not exceeding 30°C.
MIMS Class
Other CNS Drugs & Agents for ADHD / Peripheral Vasodilators & Cerebral Activators
ATC Classification
N06BX06 - citicoline ; Belongs to the class of other psychostimulants and nootropics.
FC tab 1 g (light purple to purple, oval shaped, biconvex, plain on one side and bisected on the other side) x 30's. Soln for inj 250 mg/mL (clear, colorless) x 4 mL x 10's.
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