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Indications/Uses
For the treatment of patients with serious cerebral injuries of vascular traumatic nature with or without loss of consciousness and for the treatment of degenerative damages and chronic cerebral vascular injuries in senile dementia.
Dosage/Direction for Use
2 tablets daily or as prescribed by the physician.
Administration: Citicoline should be taken orally with a glass of water. To prevent an upset stomach, patient may take it with food. When taking citicoline or any prescription drug, always follow label closely. Do not take more than directed.
Citicoline should only be taken as instructed by a professional physician. Remember not to stop taking this medicine without consulting first the physician about how to stop safely. If researching this medication for a child, keep in mind that children often have special dosage instructions. Ask the physician about these differences prior to starting this medication if this is the case.
In the event that a dose of Citicoline was missed, take one as soon as possible. But if the next scheduled dose is near, wait until the next dose is due and skip the one missed dose.
Administration: Citicoline should be taken orally with a glass of water. To prevent an upset stomach, patient may take it with food. When taking citicoline or any prescription drug, always follow label closely. Do not take more than directed.
Citicoline should only be taken as instructed by a professional physician. Remember not to stop taking this medicine without consulting first the physician about how to stop safely. If researching this medication for a child, keep in mind that children often have special dosage instructions. Ask the physician about these differences prior to starting this medication if this is the case.
In the event that a dose of Citicoline was missed, take one as soon as possible. But if the next scheduled dose is near, wait until the next dose is due and skip the one missed dose.
Overdosage
Intoxication appearance is unlikely due to low toxicity, even in cases when the therapeutic doses are accidentally exceeded.
In case of accidental overdose a symptomatic therapy is carried out.
In case of accidental overdose a symptomatic therapy is carried out.
Administration
May be taken with or without food: Take w/ or between meals.
Contraindications
Must not be administered to patients with hypertonia of the parasympathetic nervous system. Citicoline is contraindicated in conditions like unconsciousness, brain surgery.
Special Precautions
Must not be administered in conjunction with medications containing centrophenoxine. In case of persistent intracranial hemorrhage, it is recommended not to exceed the dose of 1000 mg of Citicoline daily.
Cholines are generally regarded as safe and appear to be well-tolerated. High intake of cholines may cause low blood pressure, steatorrhea (undigested fat in stool), nausea, vomiting, salivation, diarrhea, constipation, anorexia, dizziness (vertigo), sweating, insomnia and headache. Cholines can possibly trigger existing epilepsy. Dosages at the upper limit (UL) intake levels are contraindicated for persons suffering from trimethylaminuria, Parkinson's disease, or kidney or liver disease.
Skin rash has been reported. A cold and cough were noted in patients taking citicoline in a trial. Choline should be used cautiously by people with kidney or liver disorders. Agitation, paranoia and severe depression have been reported. Use cautiously in patients with a history of depression.
Because choline is a product of the breakdown of succinylcholine, it may produce undesirable effects as the drug, like respiratory depression. A "fishy" odor has been associated with choline. Sweating and stunted growth may occur.
Cholines are generally regarded as safe and appear to be well-tolerated. High intake of cholines may cause low blood pressure, steatorrhea (undigested fat in stool), nausea, vomiting, salivation, diarrhea, constipation, anorexia, dizziness (vertigo), sweating, insomnia and headache. Cholines can possibly trigger existing epilepsy. Dosages at the upper limit (UL) intake levels are contraindicated for persons suffering from trimethylaminuria, Parkinson's disease, or kidney or liver disease.
Skin rash has been reported. A cold and cough were noted in patients taking citicoline in a trial. Choline should be used cautiously by people with kidney or liver disorders. Agitation, paranoia and severe depression have been reported. Use cautiously in patients with a history of depression.
Because choline is a product of the breakdown of succinylcholine, it may produce undesirable effects as the drug, like respiratory depression. A "fishy" odor has been associated with choline. Sweating and stunted growth may occur.
Use In Pregnancy & Lactation
During pregnancy, intake of Citicoline by the mother may influence memory and brain development in the growing infant. Studies on citicoline and lecithin supplementation clearly show an increase in blood choline levels following supplementation.
Pregnant and lactating women and children may consume choline within the recommended adequate intake (AI) parameters; supplementation outside of dietary intake is usually not necessary if a healthy diet is consumed.
Pregnant and lactating women and children may consume choline within the recommended adequate intake (AI) parameters; supplementation outside of dietary intake is usually not necessary if a healthy diet is consumed.
Drug Interactions
Interactions with Drugs: Choline supplementation has been associated with decreasing urinary excretion of carnitine in young adult women.
A study concluded that chronic treatment with lithium enhances the effects of choline in the brain. A preliminary report of MRI studies did not observe a significant positive relationship between increases in brain choline and increases in brain lithium.
COP-choline can cause an increase in plasma concentrations of dopa.
Methotrexate may diminish pools of all choline metabolites. Choline supplementation reverses fatty liver caused by methotrexate administration in rats.
Pentazocine exhibits neuromuscular blocking effects in part through a depressive action on cholinoceptive sites on the nerve motor end terminals, presenting a possible interaction if administered with choline.
Although a few studies have linked choline with partially reversing the effects of scopolamine, a later study failed to demonstrate similar effects.
Choline is a product of the breakdown of succinylcholine. Taking choline with succinylcholine may theoretically intensify effects and/or toxicity.
Interactions with Herbs and Supplements: Choline, via its metabolism to betaine, works in concert with vitamins B6, B12, and folic acid in the metabolism of the potentially atherogenic substance homocysteine.
A study concluded that chronic treatment with lithium enhances the effects of choline in the brain. A preliminary report of MRI studies did not observe a significant positive relationship between increases in brain choline and increases in brain lithium.
COP-choline can cause an increase in plasma concentrations of dopa.
Methotrexate may diminish pools of all choline metabolites. Choline supplementation reverses fatty liver caused by methotrexate administration in rats.
Pentazocine exhibits neuromuscular blocking effects in part through a depressive action on cholinoceptive sites on the nerve motor end terminals, presenting a possible interaction if administered with choline.
Although a few studies have linked choline with partially reversing the effects of scopolamine, a later study failed to demonstrate similar effects.
Choline is a product of the breakdown of succinylcholine. Taking choline with succinylcholine may theoretically intensify effects and/or toxicity.
Interactions with Herbs and Supplements: Choline, via its metabolism to betaine, works in concert with vitamins B6, B12, and folic acid in the metabolism of the potentially atherogenic substance homocysteine.
Storage
Store at temperatures not exceeding 30°C.
Action
Pharmacotherapeutic Group: Psychostimulants and nootropics. ATC Code: N06BX06.
Pharmacology: Pharmacodynamics: Mechanism of Action: Citicoline stimulates the biosynthesis of structural neuronal membrane phospholipids, as demonstrated in studies with magnetic resonance spectroscopy. Citicoline by this action improves the function of the mechanisms of membrane, such as the operation of pumps and ion exchange receptors embedded in it, whose modulation is essential for proper neurotransmission. Citicoline by its membrane stabilizing action has properties that favor reabsorption of cerebral edema.
Experimental studies have shown that citicoline inhibits the activation of specific phospholipases (A1, A2, C and D), reducing free radical formation, avoiding the destruction of membranes and preserving antioxidant defense systems, such as glutathione. Citicoline protects the reserve neuronal energy; it inhibits and stimulates the synthesis of acetylcholine. Experiments have shown that citicoline also has prophylactic neuroprotective effect in models of focal cerebral ischemia.
Clinical trials have shown that citicoline significantly improves the functional development in patients with acute ischemic stroke, coinciding with slower growth of cerebral ischemic injury in brain imaging tests. In patients with head injury, citicoline accelerates recovery in these patients and reduces the duration and intensity of post-concussion syndrome. Citicoline improves the level of attention and awareness as well as acts favorably on amnesia and cognitive impairment and neurological disorder associated with cerebral ischemia.
Pharmacokinetics: Citicoline is a water-soluble compound with greater 90% 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 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 resynthesis into citicoline in the brain.
Pharmacokinetic studies using 14C citicoline show citicoline elimination occurs in two phases mirroring the biphasic plasma peaks, mainly via respiratory CO2 and urinary excretion. 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.
Endogenous citicoline serves as an intermediate in the biosynthesis of phospholipids, including phosphatidylcholine, the primary phospholipids in cell membranes.
Cytidine, a major component of RNA, undergoes cytoplasmic conversion to cytidine triphosphate (CTP). In the citicoline metabolic pathway, choline is phosphorylated by the enzyme choline kinase; the resulting phosphorylcholine combines with CTP to form citicoline. Citicoline then combines with diacylglycerol (DAG), forming phosphatidylcholine, with choline phosphotransferase serving as the enzyme catalyst in this reaction.
Oral administration of citicoline raises plasma levels of cytidine and choline in rats within six to eight hours. Prolonged administration for 42 and 90 days increases brain concentrations of phosphatidylcholine, phosphatidylethanolamine and phosphatidylserine, the three major phospholipids in brain cell membranes. Evidence for the role of these metabolites as substrates for phosphatidylcholine synthesis was found in a study giving rats daily oral doses of citicoline for 90 days. At a dose of 500 mg/kg per day phosphatidylcholine levels increased by 25 percent, phosphatidylethanolamine by 17 percent, and phosphatidylserine by 42 percent. Administration of citicoline to aged rats activates CTP:Phosphocholine cytidylyltransferase, the rate-limiting enzyme in the citicoline pathway of phosphatidylcholine synthesis in the brain cell membrane. Choline and cytidine are the major metabolites released via hydrolysis of citicoline during absorption.
A single oral dose of citicoline raises plasma choline levels in both younger and older subjects. Using protein magnetic resonance spectroscopy, it was found that brain choline levels in older subjects decreased after citicoline administration, but increased in younger subjects. The postulated explanation is that the cytidine moiety of citicoline may be taken up by brain cells in older subjects more rapidly than choline. Based on this finding, it is suggested that cytidine is the citicoline component primarily responsible for stimulating phosphatidylcholine synthesis in older subjects. Using protein-decoupled phosphorus magnetic resonance spectroscopy, it has been shown that citicoline administration to older subjects for six weeks increases brain levels of phosphodiesterases, byproducts of phospholipid metabolism. This is seen as evidence that citicoline increases phospholipids synthesis and turnover, which may help reverse cognitive functional deficits associated with aging. In clinical trials, citicoline has been administered orally and by intramuscular injection.
Pharmacology: Pharmacodynamics: Mechanism of Action: Citicoline stimulates the biosynthesis of structural neuronal membrane phospholipids, as demonstrated in studies with magnetic resonance spectroscopy. Citicoline by this action improves the function of the mechanisms of membrane, such as the operation of pumps and ion exchange receptors embedded in it, whose modulation is essential for proper neurotransmission. Citicoline by its membrane stabilizing action has properties that favor reabsorption of cerebral edema.
Experimental studies have shown that citicoline inhibits the activation of specific phospholipases (A1, A2, C and D), reducing free radical formation, avoiding the destruction of membranes and preserving antioxidant defense systems, such as glutathione. Citicoline protects the reserve neuronal energy; it inhibits and stimulates the synthesis of acetylcholine. Experiments have shown that citicoline also has prophylactic neuroprotective effect in models of focal cerebral ischemia.
Clinical trials have shown that citicoline significantly improves the functional development in patients with acute ischemic stroke, coinciding with slower growth of cerebral ischemic injury in brain imaging tests. In patients with head injury, citicoline accelerates recovery in these patients and reduces the duration and intensity of post-concussion syndrome. Citicoline improves the level of attention and awareness as well as acts favorably on amnesia and cognitive impairment and neurological disorder associated with cerebral ischemia.
Pharmacokinetics: Citicoline is a water-soluble compound with greater 90% 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 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 resynthesis into citicoline in the brain.
Pharmacokinetic studies using 14C citicoline show citicoline elimination occurs in two phases mirroring the biphasic plasma peaks, mainly via respiratory CO2 and urinary excretion. 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.
Endogenous citicoline serves as an intermediate in the biosynthesis of phospholipids, including phosphatidylcholine, the primary phospholipids in cell membranes.
Cytidine, a major component of RNA, undergoes cytoplasmic conversion to cytidine triphosphate (CTP). In the citicoline metabolic pathway, choline is phosphorylated by the enzyme choline kinase; the resulting phosphorylcholine combines with CTP to form citicoline. Citicoline then combines with diacylglycerol (DAG), forming phosphatidylcholine, with choline phosphotransferase serving as the enzyme catalyst in this reaction.
Oral administration of citicoline raises plasma levels of cytidine and choline in rats within six to eight hours. Prolonged administration for 42 and 90 days increases brain concentrations of phosphatidylcholine, phosphatidylethanolamine and phosphatidylserine, the three major phospholipids in brain cell membranes. Evidence for the role of these metabolites as substrates for phosphatidylcholine synthesis was found in a study giving rats daily oral doses of citicoline for 90 days. At a dose of 500 mg/kg per day phosphatidylcholine levels increased by 25 percent, phosphatidylethanolamine by 17 percent, and phosphatidylserine by 42 percent. Administration of citicoline to aged rats activates CTP:Phosphocholine cytidylyltransferase, the rate-limiting enzyme in the citicoline pathway of phosphatidylcholine synthesis in the brain cell membrane. Choline and cytidine are the major metabolites released via hydrolysis of citicoline during absorption.
A single oral dose of citicoline raises plasma choline levels in both younger and older subjects. Using protein magnetic resonance spectroscopy, it was found that brain choline levels in older subjects decreased after citicoline administration, but increased in younger subjects. The postulated explanation is that the cytidine moiety of citicoline may be taken up by brain cells in older subjects more rapidly than choline. Based on this finding, it is suggested that cytidine is the citicoline component primarily responsible for stimulating phosphatidylcholine synthesis in older subjects. Using protein-decoupled phosphorus magnetic resonance spectroscopy, it has been shown that citicoline administration to older subjects for six weeks increases brain levels of phosphodiesterases, byproducts of phospholipid metabolism. This is seen as evidence that citicoline increases phospholipids synthesis and turnover, which may help reverse cognitive functional deficits associated with aging. In clinical trials, citicoline has been administered orally and by intramuscular injection.
MedsGo Class
Peripheral Vasodilators & Cerebral Activators / Nootropics & Neurotonics/Neurotrophics
Features
Brand
QUANIL
Full Details
Dosage Strength
500 mg
Drug Ingredients
- Citicoline
Drug Packaging
Film-Coated Tablet 30's
Generic Name
Citicoline Sodium
Dosage Form
Film-Coated Tablet
Registration Number
DR-XY41458
Drug Classification
Prescription Drug (RX)