Oral Solution
CITICOLINE 1000mg
Each 10 ml sachet contains
Citicoline (as sodium salt) 1000 mg
INDICATIONS
• Treatment of neurological and cognitive disorders associated with cerebrovascular accidents.
• Treatment of neurological and cognitive disorders associated with head injuries.
SEMAZON (Citicoline) stimulates the biosynthesis of structural phospholipids of the neuronal membrane, as demonstrated in studies carried out with magnetic resonance spectroscopy. Citicoline, through this action, improves the function of membrane mechanisms, such as the functioning of the ion exchange pumps and the receptors inserted in it, whose modulation is essential for proper neurotransmission. Citicoline, due to its stabilizing action on the membrane, has properties that favor the reabsorption of cerebral edema. Experimental studies have shown that Citicoline inhibits the activation of certain phospholipases (A 1, A2, C and D), reducing the formation of free radicals, preventing the destruction of membranous systems and preserving antioxidant defense systems, such as glutathione. Citicoline preserves the neuronal energy reserve, inhibits apoptosis and stimulates the synthesis of acetylcholine. Citicoline has also been shown experimentally to exert a prophylactic neuroprotective effect in models of focal cerebral ischemia. Clinical trials have shown that Citicoline significantly improves the functional outcome of patients with acute ischemic stroke, coinciding with a lower growth of the ischemic brain injury in neuroimaging tests. In patients with head trauma, Citicoline accelerates the recovery of these patients and reduces the duration and intensity of the post-concussion syndrome. Citicoline improves the level of attention and consciousness, as well as acts favorably on amnesia and cognitive and neurological disorders associated with cerebral ischemia.
Pharmacokinetic properties
Citicoline is well absorbed after oral, intramuscular or intravenous administration. Choline levels in plasma are significantly increased by these routes. Absorption by the oral route is practically complete and its bioavailability is approximately the same as by the intravenous route. The drug is metabolized in the wall of the intestine and in the liver to choline and cytidine. Administered citicoline is widely distributed in brain structures, with rapid incorporation of the choline fraction in structural phospholipids and of the cytidine fraction in cytidine nucleotides and nucleic acids. Citicoline reaches the brain and is actively incorporated into cell, cytoplasmic and mitochondrial membranes, forming part of the fraction of structural phospholipids. Only a small amount of the dose appears in urine and feces (less than 3%). Approximately 12% of the dose is eliminated through expired CO2. Two phases are distinguished in the urinary elimination of the drug: a first phase, lasting about 36 hours, during which the excretion rate decreases rapidly, and a second phase in which the excretion rate decreases much more slowly. The same happens with expired CO2, the elimination rate of which decreases rapidly during the first fifteen hours or so, to decrease more slowly thereafter.