Nurocol

Nurocol

citicoline

Manufacturer:

Micro Labs

Distributor:

Zizawa Healthcare
Full Prescribing Info
Contents
Citicoline.
Description
Each Nurocol film-coated tablet contains: Citicoline Sodium equivalent to Citicoline 500 mg.
International Non-proprietary Name (INN) for each active ingredient: Citicoline.
Each ml of Nurocol injection contains: Citicoline Sodium equivalent to Citicoline 250 mg.
Action
Pharmacological Category: Nootropic preparation.
Pharmacology:
Pharmacodynamics: FC Tablet: It is a nootropic preparation. Citicoline as a predecessor of key ultrastructural component of cell membrane (mainly phospholipids) has a wide spectrum of action: it promotes a restoration of damaged cell membranes, inhibits an action of phospholipase, preventing a formation of free radicals and prevents cell death by acting on mechanisms of apoptosis. It is a source of choline; it increases a synthesis of acetylcholine and stimulates biosynthesis of structural (foot) phospholipids in neuron membrane. It improves the transmission of nerve impulses in cholinergic neurons; it has a positive effect on plasticity of neuronal membranes and receptor function. It improves cerebral blood flow, enhances cerebral metabolic processes and activates the structure of cerebral reticular formation. In acute phase of a stroke it reduces the volume of damaged tissue and improves cholinergic transmission.
Citicoline alleviates symptoms, which occur during hypoxia and cerebral ischemia, including memory impairment, emotional liability, lack of initiative, difficulty during daily activities and self-service. In craniocerebral injury it reduces the duration of post-traumatic coma and the severity of neurological symptoms. Citicoline has anti-edema properties and reduces cerebral edema due to its stabilizing effect on neuronal membrane. It accelerates the recovery and reduces the duration and intensity of post-traumatic syndrome. Citicoline is effective in the treatment of cognitive, sensory and motor neurological disorders of degenerative and vascular etiology.
Injection: Citicoline is a complex organic molecule that functions as an intermediate in the biosynthesis of cell membrane phospholipids. Citicoline is also known as CDP-choline or cytidine diphosphate choline (cytidine 5'-diphosphocholine). CDP-choline belongs to the group of biomolecules in living systems known as nucleotides that play important roles in cellular metabolism. The pharmacologic action of Citicoline appears to involve mechanisms that extend beyond phospholipid metabolism. Citicoline metabolites-choline, methionine, betaine, and cytidine derived nucleotides - enter a number of metabolic pathways. Biochemical markers of cholinergic nerve transmission are known to be deficient in conditions characterized by degeneration of cholinergic neurons, such as Alzheimer's disease (AD). Citicoline modestly improves cognitive function in AD by serving as an acetylcholine precursor. The brain uses choline preferentially for acetylcholine synthesis, which can limit the amount of choline available for phosphatidylcholine production.
Citicoline has also been investigated as a therapy for stroke patients. Three mechanisms are postulated: repair of the neuronal membrane via increased synthesis of phosphatidylcholine; repair of damaged cholinergic neurons via potentiation of acetylcholine production; and reduction of free fatty acid build-up at the site of stroke-induced nerve damage. Citicoline protects cholinergic neurons from auto cannibalism, a process in which membrane phospholipids are catabolized to provide choline for synthesis of acetylcholine. This occurs when choline supplies are depleted, necessitating sacrifice of membrane phospholipids to maintain neurotransmission. As an exogenous source of choline for acetylcholine production, Citicoline thus spares membrane phospholipids (in particular, phosphatidylcholine) and prevents neuronal cell death.
Pharmacokinetics: FC Tablet: Citicoline is well absorbed in oral, intramuscular and intravenous introduction. After the preparation introduction it is observed a significant increase of choline in plasma. The preparation is almost completely absorbed in oral administration. Studies have shown that the bioavailability in per oral and parenteral routes of introduction was similar.
The preparation is metabolized in intestine and liver with the formation of choline and cytidine. After Citicoline introduction it is assimilated by cerebral tissues, while cholines act on phospholipids, cytidine on cytidine nucleoids and nucleic acids. Citicoline quickly reaches cerebral tissues and actively integrates into cell membrane, cytoplasm and mitochondria, activating an activity of phospholipids.
Only a minor part of introduced dose is excreted with urine and feces (less than 3%). Approximately 12% of introduced dose are excreted via respiratory tract. The preparation excretion via urine and respiratory tract has two phases: first phase rapid excretion (with urine within the first 36 hours, via airways within the first 15 hours), the second phase slow excretion. Major part of the dose is included into the process of metabolism.
Injection: Absorption: Citicoline is well absorbed following intramuscular administration. After intramuscular doses of Citicoline 1,000 mg, peak increases in plasma choline levels were seen in 0.4 hours, with levels increasing from 11 micromol/L (baseline) to 25 micromol/L.
Distribution: Choline derived from Citicoline crosses the blood-brain barrier, presumably serving as a source of 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.
Metabolism: Citicoline is metabolized in the liver to free choline. The liver is capable of synthesizing lecithin from choline. The half-life of free choline is of 2 hours after intramuscular administration.
Excretion: Only small amounts of dose are recovered in the urine and faeces (less than 3% each). Approximately 12% of a dose is eliminated through the lungs as carbon dioxide.
Indications/Uses
Acute phase of a stroke.
Treatment of complications and consequences of a stroke.
Craniocerebral injury and its consequences.
Cognitive, sensitive, motor and neurological disorders caused by cerebral pathology of degenerative or vascular origin.
Dosage/Direction for Use
FC Tablet: Dosage regimens, including for children: Recommended dose is 500-2000 mg per day.
Doses of the preparation and treatment course duration depend on severity of cerebral lesion, they are adjusted by a doctor.
Elderly patients do not need the dose adjustment.
Method of administration: Orally administer.
Injection: Disturbance of Consciousness Resulting from Head Injury or Brain Operation: Usually, for adults, a dose of 100-500 mg of Citicoline Injection is administered once or twice a day by intravenous drip infusion, Intravenous injection or intramuscular injection. The dose may be adjusted according to the patient's age and condition. Disturbance of Consciousness in the Acute Stage of Cerebral Infarction: Usually, a dose of 1,000 mg of Citicoline Injection is administered once a day, by intravenous injection, for 2 consecutive weeks.
250 mg/mL Solution for Injection: Usual Dose: 1 injection daily. Or, as prescribed by the doctor.
Method of administration: For IV or IM use only.
Overdosage
FC Tablet: 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.
Injection: 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.
Contraindications
FC Tablet: Hypersensitivity to Citicoline, or any of the excipients.
Injection: Must not be administered to patients with hypertonic of the parasympathetic.
Special Precautions
FC Tablet: Citicoline may cause hypotension and in case necessary the hypotensive effect can be treated with corticosteroids or sympathomimetics.
In case of persistent intracranial hemorrhage, it is recommended not to exceed the dose of 1000 mg of citicoline daily, in very slow intravenous administration (30 drops/minute).
Peculiarities in usage: Citicoline preparation should be administered with caution to patients who suffer from trimethylaminuria, Parkinson's disease and patients with depression in anamnesis.
Injection: General: For patients with acute, severe and progressive disturbance of consciousness resulting from a head injury or brain operation, Citicoline injection should be administered in conjunction with haemostatics and an intracranial pressure relieving drug, or a treatment such as hypothermia. For patients with disturbance of consciousness in the acute stage of cerebral infarction, it is recommended to start the administration of Citicoline injection within 2 weeks after an apoplectic stroke.
In administering Citicoline injection intramuscularly, caution should be exercised so as not to affect the tissues, nerves, etc. Intramuscular injection should be given only when indispensable, and should be restricted to the minimum to be required. In particular, repeated injection at the same site should be avoided. Care should be exercised to avoid injection at sites along the course of the nerves. In case of intense pain or backflow of blood upon insertion of the injection needle, the needle should be withdrawn immediately and injected at a different site. In intravenous administration, inject as slowly as possible. Since shock may occur, a close observation should be maintained. If any such abnormalities such as drop in blood pressure, distressed feeling of the chest or dyspnoea are observed, Citicoline injection should be discontinued and appropriate measures taken.
Persistent Intracranial Haemorrhage: In case of persistent intracranial haemorrhage, it is recommended not to exceed the dose of 1,000 mg of Citicoline daily, given through very slow intravenous administration (30 drops/minute).
Use in Pregnancy & Lactation: FC Tablet: Preparation administration during pregnancy and lactation period is possible only in case when expected benefit for a mother overweighs a potential risk for a fetus or baby.
Use in Children: FC Tablet: There is no sufficient data concerning Citicoline administration to children, therefore Citicoline should not be administered to this age group of patients.
Use in Elderly: Injection: No dosage adjustment is required in this patient population and the usually recommended adult dose can be administered.
Use In Pregnancy & Lactation
FC Tablet: Preparation administration during pregnancy and lactation period is possible only in case when expected benefit for a mother overweighs a potential risk for a fetus or baby.
Injection: Pregnancy: There are no adequate and well-controlled studies of Citicoline during pregnancy. Citicoline should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus.
Lactation: Caution should be exercised during breastfeeding because it is not known whether Citicoline is excreted in breast milk.
Adverse Reactions
FC Tablet: Adverse reactions occur very rarely (<1/10000), including single cases.
Mentality: hallucinations, excitement, insomnia.
CNS: headache, dizziness, tremor.
Cardio-vascular system: arterial hypotension or hypotension.
Respiratory system: dyspnea.
Digestive tract: nausea, vomiting, gastric pain, hyper salivation, insignificant change of hepatic function indexes, diarrhea.
Skin: redness, urticaria, exanthem.
General disorders: increase of body temperature, fever sensation, trembling, and edema.
Injection: The commonly observed adverse effects (0.1-5%) with intravenous use of Citicoline were rash, insomnia, occurrence or intensification of numbness of paralyzed extremities (when used in patients with post-apoplectic hemiplegia), nausea, abnormal laboratory values for function of the liver, and feeling of warmth. The other adverse reactions (<0.1%) were excitation, convulsions, anorexia, transient diplopia, transient blood pressure changes, malaise, shock, distressed feeling of the chest, and dyspnoea. In a short-term, placebo-controlled, crossover study, 12 healthy adults took Citicoline at daily doses of 600 mg and 1,000 mg or placebo for consecutive 5-day periods. Transient headaches occurred in 4 subjects on the 600 mg dose, 5 on the 1,000 mg dose, and 1 on placebo. No changes or abnormalities were observed in haematology, clinical biochemistry or neurological tests. A large drug surveillance study analysed the results of Citicoline treatment in 2,817 patients aged 60 to 80 years, suffering from senility and cerebral vascular insufficiency. A total of 151 incidents of side effects were recorded, representing 5% of the patient sample. The most common adverse effects were transient in nature and included stomach pain and diarrhoea in 102 cases. Vascular symptoms of hypotension, tachycardia or bradycardia occurred in 16 cases.
Drug Interactions
FC Tablet: Citicoline enhances effects of L-dihydroxyphenylalanine and levodopa.
It should not be synchronously used with drugs, which contain meclofenoxate.
Alcohol should not be consumed while the preparation usage.
Injection: Carbidopa, Levodopa and Entacapone: Citicoline may enhance the effects of levodopa, carbidopa and entacapone. The exact mechanism is unknown, but animal models suggest that Citicoline may increase dopamine levels in the brain and/or improve dopaminergic cell survival. In patients with Parkinson's disease, a few studies have demonstrated levodopa-saving effects, whereby the addition of Citicoline (500-1,200 mg/day) allowed for lower dosages of levodopa to be used with stable or improved therapeutic efficacy and reduced the side effects in some patients. However, data are limited.
Co-administration with Centrophenoxine: Must not be administered in conjunction with medications containing Centrophenoxine.
Storage
FC Tablet: Store below 30°C.
Injection: Store in a cool place, Protect from light.
ATC Classification
N06BX06 - citicoline ; Belongs to the class of other psychostimulants and nootropics.
Presentation/Packing
FC tab 500 mg x 10's. Inj 250 mg/mL (amp) x 2 mL x 5's, 4 mL x 5's.
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