Citicoline (Zynerva) 1 g Film-Coated Tablet is characterized by light purple to purple film coated, biconvex tablet, oval shaped, plain on both sides.
Each film-coated tablet contains: Citicoline (as sodium) 1 g.
Pharmacology: 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. It has the ability to slightly increase cerebral blood flow and exerts an anti-aggregation effect on platelets.
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 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 ischemia and necrosis.
Pharmacokinetics: Citicoline is a water-soluble compound with greater than 90% bioavailability. Pharmacokinetic studies in healthy adults have shown oral doses of Citicoline to be rapidly absorbed, with less than 1% excreted in the feces. Plasma levels peak in a biphasic manner, at 1 hour after ingestion followed by a second larger peak at 24 hours post-dosing.
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 re-synthesis into Citicoline in the brain.
Pharmacokinetic studies using Citicoline show Citicoline elimination occurs mainly via respiratory CO2 and urinary excretion, in two phases, mirroring the biphasic plasma peaks. The initial peak in plasma concentration is followed by a sharp decline, which then slows over the next 4-10 hours. In the second phase, an initially rapid decline after the 24-hour plasma peak is similarly followed by a slower elimination rate. The elimination half-life is 56 hours for CO2 and 71 hours for urinary excretion.
It is used in the treatment of cerebrovascular disorders including ischemic stroke, parkinsonism and head injuries.
Citicoline Sodium 1 g film-coated tablet once a day or as prescribed by the physician.
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 1,000 mg or placebo for consecutive five-day periods. Transient headaches occurred in four subjects on 600 mg dose, five on the 1,000 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 2,000 mg/kg body weight for 14 days. No changes in body weight, deaths, clinical symptoms or gross pathological changes were observed.
Must not be administered to patients with hypertonia of the parasympathetic.
Large doses of Citicoline could aggravate increase in cerebral blood flow in episodes of persistent intracranial hemorrhage. Citicoline should be used with caution in patients with acute, severe and progressive disturbance of consciousness, administer with hemostatics, intracranial pressure relieving drugs or use measures to keep body temperature low.
There is not enough evidence on Citicoline's safety in pregnant and breastfeeding women. Citicoline should be used in pregnancy and breastfeeding only when benefits justify the potential risks.
Increased parasympathetic effects, fleeting and discrete hypotensor effect.
Citicoline potentiates the effects of L-Dopa.
It must not be administered with meclofenoxate (clophenoxate).
Store at temperatures not exceeding 30°C.
N06BX06 - citicoline ; Belongs to the class of other psychostimulants and nootropics.
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