Red coloured, capsule shaped, biconvex, film coated tablets with breakline on one side and plain on other side.
Each film coated tablet contains: Citicoline Sodium equivalent to Citicoline 500 mg.
Pharmacology: Citicoline is a pyrimidine 5'-nucleotide which serves as an essential precursor in the synthesis of lecithin (phosphatidylcholine) and other phospholipids.
Mechanism of Action: The extensive damage caused by stroke requires repair and regeneration of axons and synapses of neurons, so new membrane production is essential. The primary mechanism by which citicoline is believed to have a therapeutic effect in stroke is its ability to increase the synthesis of phosphatidylcholine, the primary neuronal membrane component. It also enhances acetylcholine synthesis, and might thus ameliorate symptoms caused by the stroke induced loss of cholinergic neurons.
Another mechanism by which citicoline may have a more acute effect on the outcome of stroke patients relates to its ability to reduce free fatty acid accumulation at the site of injury, and thus to prevent further damage.
Citicoline avoids, reduces or reverses the effects of ischemia and/or hypoxia in major part of animals and cellular models studied and acts in the cranial traumatic forms, reduces and limits the injuries to the membranes of the nerve cells, re-establishes the sensitivity and the function of the regulatory intracellular enzymes and accelerates the re-absorption of the cerebral edema.
Thus considerable evidence accumulated supports the use of citicoline for increasing and maintaining and repairing the membranes and the neuronal function in situations such as ischemia and traumatic injuries. In patients with senile dementia, citicoline reduces the evolution of damages.
Pharmacokinetics: Citicoline is well absorbed after oral administration. It has an absolute bioavailability of approximately 99%. Citicoline is metabolized in the liver to free choline. The liver is capable of synthesizing lecithin from choline, and resynthesizing citicoline from cytidine and choline.
Due to difficulties in detecting plasma levels of citicoline itself, assays have been performed for free choline or total plasma radioactivity in terms of citicoline equivalents. Plasma choline levels are elevated significantly after oral administration. Two peaks of plasma citicoline equivalents have been reported after oral doses of radiolabeled citicoline (300 mg). An initial peak is observed in approximately 1 hour (1.5 mcg/mL), presumably related to a mixture of unchanged citicoline and its metabolites (choline and cytidine diphosphate). A second peak of approximately 3 mcg/mL is seen 24 hours postdose, and may be due to delayed absorption of the drug or continued metabolite accumulation over this time period. Choline derived from citicoline crosses the blood brain barrier, presumably serving as a source for acetylcholine and phosphatidylcholine (lecithin) synthesis. The major portion of a dose of citicoline appears to be incorporated into tissues and/ or used in biosynthetic/biodegradation pathways, including lecithin/lipid membrane synthesis.
Small amounts of a dose are recovered in urine (2% to 3%) and in feces (less than 1%). Approximately 12% of a dose is eliminated as respiratory carbon dioxide. Elimination half life of citicoline is 3.5 hours (first peak concentration), 125 hours (second peak concentration).
Used in the treatment of cerebrovascular disorder (including ischaemic stroke) parkinsonism and head injury.
Dosage should be individualized. The usually recommended dose of citicoline is 500 to 1000 mg daily.
Elderly: No dosage adjustment is required in this patient population and the usually recommended adult dose can be administered.
Citicoline exhibits very low toxicity profile in humans. In a short term, placebo-controlled, cross-over study, 12 healthy adults took citicoline at daily doses of 600 and 1000 mg or placebo for consecutive five-day periods. Transient headaches occurred in four subjects on 600-mg dose, five on the 1000-mg dose, and one in placebo. No changes or abnormalities were observed in hematology, clinical biochemistry or neurological test.
The LD50 of a single intravenous dose of citicoline was 4,600 mg/kg and 4,150 mg/kg in mice and rats, respectively.
In an unpublished acute toxicity study, free-base citicoline was administered to male and female rats at a dose of 2000 mg/kg body weight for 14 days. No changes in body weight, deaths, clinical symptoms or gross pathological changes were observed.
Hypersensitivity to citicoline or any other component of the formulation.
Citicoline may cause hypotension and in case necessary the hypotensive effect can be treated with corticosteroids or sympathomimetics.
Use in Pregnancy & Lactation: See Use in Pregnancy & Lactation section for further information.
There are no adequate and well controlled studies of citicoline during pregnancy and lactation. Citicoline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Caution should be exercised during breast feeding because it is not known whether citicoline is excreted in human breast milk.
Citicoline is generally well tolerated. Few adverse effects that are reported with oral citicoline include gastrointestinal disturbances, dizziness and fatigue.
Citicoline must not be used with medicines containing meclophenoxate (or centrophenoxine). Citicoline increases the effects of L-dopa.
Incompatibilities: None known.
Store at temperatures not exceeding 30°C.
N06BX06 - citicoline ; Belongs to the class of other psychostimulants and nootropics.
RiteMED Citicoline FC tab 500 mg
30's
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