Pharmacodynamics and pharmacokinetics
Citicoline, being a precursor of the ultrastructural components of the cell membrane, namely phospholipids , has a fairly wide spectrum of action. The drug restores damaged cell membranes, inhibits the action of phospholipase enzymes , and prevents excessive formation of free radicals . Thanks to this drug, it is possible to prevent or significantly reduce the intensity of cell death by influencing the mechanisms of apoptosis.
When used in the acute period of stroke , the drug reduces the volume of damaged tissue and stimulates cholinergic transmission. The drug promotes rapid recovery from traumatic brain injuries, reduces the duration of post-traumatic coma , and neurological symptoms appear with less intensity.
In patients with chronic cerebral hypoxia cognitive disorders , deterioration of memory processes and difficulties with self-care. Under the influence of this substance, the level of consciousness and attention increases, and the patient’s memory returns. The substance is also quite effective in the treatment of motor and neurological disorders of vascular or degenerative etiology.
Citicoline has good absorption capacity, both when injected and when taken orally. The medicine has high bioavailability. The drug is metabolized in the liver tissues, with the formation of cytidine and choline . The substance is evenly distributed throughout various structures of the brain, actively integrated into the membranes of mitochondria, cells, and cytoplasm with the formation of parts of fractions of structural phospholipids .
About 15% of the drug taken or administered by injection is excreted from the body. Excretion occurs through the kidneys, however, mainly through exhaled carbon dioxide. The first phase of excretion through the kidneys occurs within 36 hours, during which time almost all of the drug is eliminated. For breathing, this figure is 15 hours.
Citicoline solution d/iv and intramuscular injection 125 mg/ml amp 4 ml No. 5
Compound
Active substance: citicoline sodium 130.63 mg, which corresponds to the content of citicoline 125 mg. Excipients: hydrochloric acid 1M - up to pH 6.7-7.1, water for injection - up to 1 ml.
Pharmacokinetics
Since citicoline is a naturally occurring compound found in the body, a classic pharmacokinetic study cannot be performed due to the difficulty in quantifying exogenous and endogenous citicoline.
Indications for use
- Ischemic stroke (acute period);
- ischemic and hemorrhagic stroke (recovery period);
- traumatic brain injury (acute and recovery period);
- cognitive impairment in degenerative and vascular diseases of the brain.
Contraindications
- Vagotonia (predominance of the tone of the parasympathetic part of the autonomic nervous system);
- children and adolescents up to 18 years of age;
- hypersensitivity to citicoline.
Directions for use and doses
IV for strokes and traumatic brain injury in the acute period - 1-2 g/day, depending on the severity of the disease, for 3-7 days, followed by switching to IM administration or oral administration.
V/m - 0.5-1 g/day.
Storage conditions
The drug should be stored out of the reach of children at a temperature not exceeding 30°C.
Best before date
3 years. Do not use after expiration date.
special instructions
Citicoline should not be used concomitantly with medicinal products containing meclofenoxate.
Description
Nootropic drug.
Use in children
Contraindicated in children under 18 years of age (due to the lack of sufficient clinical data).
Pharmacodynamics
Nootropic drug. Citicoline, being a precursor of key ultrastructural components of the cell membrane (mainly phospholipids), has a wide spectrum of action: it promotes the restoration of damaged cell membranes, inhibits the action of phospholipases, preventing the excessive formation of free radicals, and also prevents cell death by affecting the mechanisms of apoptosis.
In the acute period of stroke, it reduces the volume of damaged tissue and improves cholinergic transmission.
In case of traumatic brain injury, it reduces the duration of post-traumatic coma and the severity of neurological symptoms.
Citicoline improves the symptoms observed during hypoxia: memory impairment, emotional lability, lack of initiative, difficulties in performing daily activities and self-care. Effective in the treatment of cognitive, sensory and motor neurological disorders of degenerative and vascular etiology.
Side effects
From the nervous system: insomnia, headache, dizziness, agitation, tremor, numbness in paralyzed limbs.
From the digestive system: nausea, loss of appetite, changes in the activity of liver enzymes.
Allergic reactions: rash, itchy skin, anaphylactic shock.
Other: fever; in some cases - short-term hypotensive effect, stimulation of the parasympathetic nervous system.
Use during pregnancy and breastfeeding
During pregnancy, use is possible only if the expected benefit of therapy for the mother outweighs the potential risk to the fetus.
If it is necessary to use citicoline during lactation, the issue of stopping breastfeeding should be decided, since there is no data on the excretion of citicoline in breast milk.
Interaction
Citicoline enhances the effects of levodopa.
Should not be used simultaneously with drugs containing meclofenoxate.
Citicoline in the form of a solution for IV and IM administration is compatible with all types of IV isotonic solutions and dextrose solutions.
Overdose
Given the low toxicity of citicoline, cases of overdose have not been described, even when therapeutic doses are exceeded.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, care should be taken when performing potentially hazardous activities that require special attention and speed of reactions (including driving a car and other vehicles, working with moving mechanisms, working as a dispatcher and operator).
Side effects
Adverse reactions when using the drug occur rarely.
May appear:
- sleep disturbances , dizziness, tremors , headaches, increased agitation;
- numbness of the limbs, loss of appetite, nausea, increased activity of liver enzymes;
- anaphylactic reactions , skin rashes, allergic itching;
- rarely - hypotension or hypertension , hyperstimulation of the parasympathetic nervous system.
If these adverse reactions worsen, unusual symptoms and side effects occur, it is recommended to consult with your doctor.
Buy Ceraxon solution intravenously and intramuscularly 1000 mg 4 ml No. 5 in pharmacies
Oral solution in the form of a clear, colorless liquid with a characteristic strawberry odor. Indications : acute period of ischemic stroke (as part of complex therapy); — recovery period of ischemic and hemorrhagic strokes; — traumatic brain injury, acute (as part of complex therapy) and recovery period; — cognitive and behavioral disorders in degenerative and vascular diseases of the brain. Dosage regimen IV drug is administered as a slow injection (over 3-5 minutes, depending on the prescribed dose) or drip infusion (40-60 drops/min). The intravenous route of administration is preferable to the intramuscular route. When administered intramuscularly, repeated administration of the drug in the same place should be avoided. Acute period of ischemic stroke and traumatic brain injury: the recommended dose is 1000 mg every 12 hours from the first day after diagnosis; Duration of treatment is at least 6 weeks. 3-5 days after the start of treatment (if swallowing function is not impaired), it is possible to switch to oral forms of the drug Ceraxon®. Recovery period for ischemic and hemorrhagic strokes, recovery period for traumatic brain injury, cognitive and behavioral disorders in degenerative and vascular diseases of the brain: the recommended dose is 500-2000 mg/day (5-10 ml 1-2 times/day). The dose and duration of treatment depend on the severity of the symptoms of the disease. Elderly patients do not require dose adjustment of Ceraxon® for intravenous or intramuscular administration. A solution for intravenous and intramuscular administration in an ampoule is intended for single use. After opening the ampoule, the solution should be used immediately. The drug is compatible with all types of intravenous isotonic solutions and dextrose solutions. Side effects Very rare (<1/10,000) (including individual cases): allergic reactions (rash, itching, anaphylactic shock), headache, dizziness, feeling of heat, tremor, nausea, vomiting, diarrhea, hallucinations, swelling, shortness of breath , insomnia, agitation, loss of appetite, numbness in paralyzed limbs, changes in the activity of liver enzymes. In some cases, Ceraxon® can stimulate the parasympathetic system and also cause a short-term change in blood pressure. If any of the side effects indicated in the instructions get worse, or any other side effects not listed in the instructions are noticed, you should inform your doctor. Contraindications for use : severe vagotonia (predominance of the tone of the parasympathetic part of the autonomic nervous system); - children and adolescents under 18 years of age (due to the lack of sufficient clinical data); - hypersensitivity to the components of the drug. Use during pregnancy and lactation There is not enough clinical data on the use of citicoline during pregnancy. Although experimental studies on animals have not revealed any negative effects, during pregnancy the drug is prescribed only when the expected benefit of therapy for the mother outweighs the potential risk to the fetus. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided, since there is no data on the excretion of citicoline in breast milk. Use in children Contraindicated in children and adolescents under 18 years of age. Use in elderly patients Elderly patients do not require dose adjustment of Ceraxon®. Special instructions Impact on the ability to drive vehicles and operate machinery During the treatment period, patients should be careful when performing potentially dangerous activities that require special attention and speed of psychomotor reactions (including driving a car and other vehicles, working with moving mechanisms, work of the dispatcher and operator). Overdose Due to the low toxicity of the drug, cases of overdose have not been described. Drug interactions Citicoline enhances the effects of levodopa. Ceraxon® should not be prescribed concomitantly with medications containing meclofenoxate. Conditions and periods of storage The drug should be stored out of the reach of children at a temperature not exceeding 30°C. Shelf life: 3 years. Conditions for dispensing from pharmacies The drug is dispensed with a prescription.
Instructions for use of Citicoline (Method and dosage)
The solution for intravenous or intramuscular administration is used in a dosage depending on the indications.
Intravenous injections take at least 3 minutes; it is better to infuse the medicine dropwise at a rate of 40 to 60 drops per minute. The intramuscular route of administration is used less frequently. With such injections, the medicine should be injected into a new location each time.
Instructions for the use of Citicoline in the acute period of traumatic brain injury or ischemic stroke
1 gram of the drug is administered every 12 hours, immediately after the diagnosis has been made. Treatment must be carried out for at least 6 weeks. If the patient maintains normal swallowing function, it is recommended to switch to the oral form of the medication within 3-5 days after starting therapy.
During the recovery period, 0.5 to 2 grams of the drug per day is prescribed. The dosage regimen and duration of treatment are determined individually by the attending physician.
No dosage adjustment is required for elderly people. After opening the ampoule, its contents must be used immediately. The medicine can be mixed in one syringe or infusion system with all types of isotonic solutions dextrose solution .
Instructions for oral solution
The medicine can be diluted in a small amount of water. It is recommended to drink the product before or during meals. As a rule, 200 to 300 mg of medication is prescribed 3 times a day. The course of treatment is determined depending on the effectiveness of therapy and the patient’s condition.
Citicoline 125mg/ml 4ml 5 pcs. solution for intravenous and intramuscular administration
pharmachologic effect
Nootropic drug.
Composition and release form Citicoline 125 mg/ml 4 ml 5 pcs. solution for intravenous and intramuscular administration
Composition per 1 ml 125 mg/ml:
- Active ingredient: citicoline sodium - 130.63 mg, in terms of citicoline - 125.00 mg;
- Excipients: hydrochloric acid 1 M or sodium hydroxide 1 M - up to pH 6.7-7.1, water for injection - up to 1.0 ml.
Solution for intravenous and intramuscular administration 125 mg/ml and 250 mg/ml. 4 ml in ampoules of colorless neutral glass type I with a colored break ring or with a colored dot and a notch or without a break ring, a colored dot and notch. The ampoules may additionally be coated with one, two or three color rings and/or a two-dimensional barcode, and/or alphanumeric coding, or without additional color rings, a two-dimensional barcode, or alphanumeric coding. 3 or 5 ampoules in a blister pack made of polyvinyl chloride film and varnished aluminum foil or polymer film, or without foil and without film. Or 3.5 ampoules are placed in a pre-made form (tray) made of cardboard with cells for laying ampoules. 1 or 2 contour blister packs or cardboard trays together with instructions for use and an ampoule scarifier or an ampoule knife, or without an ampoule scarifier and an ampoule knife are placed in a cardboard package (pack).
Description of the dosage form
Transparent colorless liquid.
Directions for use and doses
The drug is prescribed intravenously or intramuscularly. The drug is administered intravenously in the form of a slow intravenous injection (over 3-5 minutes, depending on the prescribed dose) or intravenous drip (40-60 drops per minute). The intravenous route of administration is preferable to the intramuscular route. When administered intramuscularly, injections of the drug into the same place should be avoided. Recommended dosage regimen. Acute period of ischemic stroke and traumatic brain injury (TBI): 1000 mg every 12 hours. Treatment duration is at least 6 weeks. 3-5 days after the start of treatment (if swallowing function is not impaired), a transition to oral forms of citicoline is possible. Recovery period of ischemic and hemorrhagic strokes, recovery period of head injury, cognitive and behavioral disorders in degenerative and vascular diseases of the brain: 500-2000 mg per day (1-2 times a day). Dosage and duration of treatment depending on the severity of the symptoms of the disease. Elderly patients. When prescribing the drug to elderly patients, no dose adjustment is required. The solution in the ampoule is intended for single use. It must be used immediately after opening the ampoule. The drug is compatible with all types of intravenous isotonic solutions and dextrose solutions.
Pharmacodynamics
There are no sufficient data on the use of citicoline in pregnant women. Although animal studies have not revealed any negative effects, during pregnancy the drug is prescribed only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.
When prescribing the drug during lactation, women should stop breastfeeding, since there is no data on the excretion of citicoline in human milk, and the risk to the child cannot be completely excluded.
Pharmacokinetics
Distribution
Citicoline is widely distributed in brain structures, with the rapid introduction of the choline fraction into structural phospholipids and the cytidine fraction into cytidine nucleotides and nucleic acids. Citicoline penetrates the brain and is actively incorporated into cellular, cytoplasmic and mitochondrial membranes, forming part of the fraction of structural phospholipids.
Metabolism
The drug is metabolized in the liver to form choline and cytidine. After administration, the concentration of choline in the blood plasma increases significantly.
Removal
Only 15% of the administered dose of citicoline is excreted from the human body: less than 3% by the kidneys and through the intestines and about 12% by exhaled CO2.
The excretion of citicoline in urine can be divided into 2 phases: a first phase, lasting about 36 hours, during which the rate of excretion decreases rapidly, and a second phase, during which the rate of excretion decreases much more slowly. The same thing is observed in exhaled CO2 - the rate of elimination decreases rapidly after about 15 hours, and then decreases much more slowly.
Indications for use Citicoline 125 mg/ml 4 ml 5 pcs. solution for intravenous and intramuscular administration
- Acute period of ischemic stroke (cerebral infarction) (as part of complex therapy).
- Recovery period of ischemic and hemorrhagic stroke.
- Traumatic brain injury (TBI): acute (as part of complex therapy) and recovery period.
- Cognitive and behavioral disorders in degenerative and vascular diseases of the brain.
Contraindications
- Hypersensitivity to any of the components of the drug,
- patients with severe vagotomy (predominance of the tone of the parasympathetic part of the autonomic nervous system),
- children under 18 years of age (due to the lack of sufficient clinical data).
special instructions
For persistent intracranial bleeding, it is recommended not to exceed a dose of 1000 mg per day; the drug is administered intravenously slowly (30 drops per minute).
Impact on the ability to drive vehicles and operate machinery During the treatment period, care should be taken when performing potentially hazardous activities that require special attention and speed of psychomotor reactions (driving a car and other vehicles, working with moving mechanisms, working as a dispatcher and operator, etc. .).
Side effects Citicoline 125 mg/ml 4 ml 5 pcs. solution for intravenous and intramuscular administration
Adverse events (AEs) are grouped by systems and organs in accordance with the MedDRA dictionary and the WHO classification of the frequency of AEs: Very common (>1/10); Often (>1/100 to 1/1000 to 1/10000 to
From the nervous system: Very rarely - headache, dizziness, reactions from the parasympathetic system, tremor, numbness in paralyzed limbs. From the psyche: Very rarely - hallucinations, insomnia, agitation. From the blood vessels: Very rarely - arterial hypotension, arterial hypertension. Disorders of the respiratory system, chest organs and mediastinum: Very rarely - shortness of breath. From the digestive system: Very rarely - loss of appetite, nausea, vomiting, diarrhea. From the skin and subcutaneous tissues: Very rarely - hyperemia, purpura, anaphylactic shock, urticaria, rash, itching. General disorders and disorders at the injection site: Very rarely - chills, feeling of heat, swelling. Disorders of the liver and biliary tract: Very rarely - changes in the activity of liver enzymes. If any of the above In the instructions, the side effects are aggravated, or any other side effects not listed in the instructions have been noticed, you should report this to your doctor.
Drug interactions
Citicoline enhances the effects of levodopa.
Should not be used concomitantly with medicinal products containing meclofenoxate.
Drugs containing (Citicoline analogues)
Level 4 ATX code matches:
Bravinton
Acefen
Carnicetine
Pyracesin
Nooclerin
Semax
Piracetam
Olatropil
Fezam
Vinpocetine
Cerebrocurin
Cavinton Forte
Calcium hopantenate
Glutamic acid
Cephabol
Olanzapine
Cerebrolysate
Pramistar
Sidnocarb
Vinpotropil
Common analogues of Citicoline: Ceraxon , Lyra , Citicoline monosodium salt , Neypilept , Citicoline sodium .
Reviews
Some reviews about the drug:
- “... My father started taking the medicine after a stroke. I drank it for about 3 months. Now noticeable improvements in the condition are visible, the numbness of the hand has passed, fine motor skills, memory have improved and motor activity has increased. It’s a good drug, however, it was sometimes difficult to get, and it’s not cheap”;
- “... After my uncle had an accident, received a TBI and was discharged from the hospital, he was prescribed a course of Citicoline for a month. First in injections, then in syrup. My uncle tolerated the treatment well and now he feels much better. The drug is expensive, but effective”;
- “... An oral solution was prescribed by a neurologist for my child (congenital injury, cyst in the brain). My daughter did not tolerate the drug well, did not sleep at night, had hypertonicity in her legs and back, and the child was constantly capricious. As a result, after visiting another doctor, we switched to another medicine.”
