Choline alfoscerate - instructions for use, doses, side effects, contraindications - geotar medicinal reference book. Why and how to take choline alfoscerate - clear description and instructions Kinetics in nerve tissues

Ellara, LLC

Country of origin

Russia

Product group

Nervous system

Nootropic drug

Release forms

Solution for intravenous and intramuscular administration 250 mg/ml - 4 ml in neutral glass ampoules - 3 pcs. in pack

Description of the dosage form

clear, colorless or slightly yellowish solution

Pharmacokinetics

The pharmacokinetic characteristics of the radioactively labeled drug were similar in different animal species (rats, dogs, monkeys) and were as follows: absorption from the gastrointestinal tract is complete and rapid; quickly accumulates and distributes in various organs and tissues, including the brain; renal excretion is approximately 10% of the administered dose in 96 hours; the concentration of the drug is higher in the brain compared to tritium-labeled choline.

Special conditions

Nausea may result from dopaminergic activation. If this symptom appears, it is recommended to reduce the dose of the drug. As a rule, the drug is well tolerated even with long-term use. Effect on the ability to drive vehicles and machinery During the treatment period, care must be taken when driving vehicles and when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Compound

(per 1 ml):
Active ingredient - choline alfoscerate hydrate (in terms of choline alfoscerate) - 250 mg;
Excipient: water for injection - up to 1 ml.

Choline Alfoscerate indications for use

Psychoorganic syndrome against the background of involutional and degenerative processes in the brain, the consequences of cerebrovascular insufficiency or primary and secondary cognitive impairment in the elderly, characterized by memory impairment, confusion, disorientation, decreased motivation and initiative, decreased concentration.
Behavioral and affective disorders in old age: emotional lability, increased irritability, decreased interest.
Senile pseudomelancholia.

Choline Alfoscerate contraindications

Hypersensitivity to choline alfoscerate and drugs with a similar chemical structure, pregnancy, lactation, children under 18 years of age.
Use during pregnancy and breastfeeding
The use of the drug is contraindicated during pregnancy and breastfeeding.

Dosage form: Solution for intravenous and intramuscular administration. Compound:

Active substance: choline alfoscerate polyhydrate (in terms of choline alfoscerate) - 250 mg.

Excipient: water for injection - up to 1 ml.

Description:

Transparent colorless or slightly colored solution.

Pharmacotherapeutic group:Nootropic drug. ATX:

N.07.A.X.02 Choline alphoscerate

Pharmacodynamics:is a centrally acting cholinomimetic with a predominant effect on the central nervous system. The drug contains 40.5% choline, released from a compound in the brain; choline is involved in the biosynthesis of acetylcholine (one of the main mediators of nervous excitation). Alfoscerate is biotransformed to glycerophosphate, which is a precursor of phospholipids.

Acetylcholine has a positive effect on the transmission of nerve impulses, and glycerophosphate is involved in the synthesis of phosphatidylcholine (membrane phospholipid), resulting in improved membrane elasticity and receptor function.

Choline alfoscerate increases cerebral blood flow, enhances metabolic processes and activates the structures of the reticular formation of the brain, and also restores consciousness in case of traumatic brain injury.

It has a preventive and corrective effect on the factors of involutional psychoorganic syndrome, such as changes in the phospholipid composition of neuron membranes and a decrease in cholinergic activity. Thus, it affects synaptic, including cholinergic transmission of nerve impulses (neurotransmission), plasticity of the neuronal membrane, and receptor function. Does not affect the reproductive cycle, does not have teratogenic or mutagenic effects.

Pharmacokinetics:Penetrates the blood-brain barrier (concentration in the brain is 45% of that in plasma). Both choline and glycerophosphate ion are included in general metabolism, so it is not possible to track their actual elimination from the body. However, they are known to be metabolized to carbon dioxide, water, phosphates and nitrogen-containing products. Indications:

Organic mental disorders in neurodegenerative diseases and chronic cerebral circulatory disorders; primary or secondary cognitive impairment, characterized by decreased memory, confusion and disorientation, decreased motivation and initiative, and impaired attention.

Affective disorders in senile degeneration of the brain: emotionally labile disorder, irritability, apathy.

Contraindications:Hypersensitivity to choline alfoscerate and drugs with a similar chemical structure, hemorrhagic stroke (acute stage), pregnancy, lactation, children under 18 years of age. Pregnancy and lactation:The drug is contraindicated for use during pregnancy and breastfeeding. Directions for use and dosage:Intramuscularly (slowly) or intravenously (drip) at a dose of 1000 mg/day (1 ampoule). For intravenous administration, the contents of one ampoule (4 ml) are diluted in 50 ml of 0.9% sodium chloride solution, the infusion rate is 60-80 drops per minute. The duration of treatment is usually 10 days, but if necessary, treatment can be continued until positive dynamics appear. Side effects:

From the digestive system : constipation, diarrhea, nausea, dry oral mucosa, pharyngitis.

From the nervous system: headache, drowsiness, insomnia, aggressiveness, anxiety, nervousness, dizziness.

From the skin : rash, urticaria.

Others: pain at the injection site, increased urination.

Overdose:

Symptoms: nausea.

Treatment: symptomatic therapy.

Interaction: No significant drug interactions between choline alfoscerate and other drugs have been identified. Special instructions:Nausea may result from dopaminergic activation. If this symptom appears, it is recommended to reduce the dose of the drug. As a rule, the drug is well tolerated even with long-term use. Impact on the ability to drive vehicles. Wed and fur.:During the treatment period, care must be taken when driving vehicles and when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Release form/dosage:Solution for intravenous and intramuscular administration 250 mg/ml. Package:

4 ml in ampoules of colorless neutral glass. 10 ampoules in a cardboard box.

3 or 5 ampoules in blister packs made of polyvinyl chloride film and printed varnished aluminum foil, or without foil. 1 or 2 blister packs in a cardboard pack. Each pack and box contains instructions for use and an ampoule scarifier.

The ampoule scarifier is not inserted when using ampoules with a break ring or with a notch and a dot.

Storage conditions:In a place protected from light at a temperature not exceeding 25 ° C. Keep out of the reach of children. Best before date: 2 years. Do not use after expiration date. Conditions for dispensing from pharmacies: On prescription Registration number: LP-002522 Registration date: 04.07.2014 Cancellation date: 2019-07-04 Owner of the Registration Certificate: SINTEZ, JSC

Latin name: Cholini alfosceras
ATX code: N07AX02
Active substance:
Manufacturer: FKP Armavir Biofactory,
Russia or Borisov Medicinal Products Plant, Belarus.
Dispensing from the pharmacy: On prescription
Storage conditions: in the dark
Best before date: 2-5 years.

Choline alfoscerate is a neurometabolic stimulant with neuroprotective properties. The nootropic drug is available in the form of solution and tablets.

In general, the drug is well tolerated. But its effect on the body has not been studied, so the medicine is not prescribed in childhood, pregnancy and lactation.

Indications for use

Cholinomimetic acts on choline receptors in the central nervous system. Choline promotes the production of acetylcholine, a neurotransmitter.

Choline alfoscerate increases the conductivity of nerve impulses in acetylcholine neurons, improving the functioning of receptors and neuronal membranes. The drug also stimulates cerebral circulation, improves central nervous system metabolism and prevents the destruction of nerve cells. In addition, choline helps to increase the concentration of good cholesterol in the body, preventing the development of atherosclerosis.

In patients with psychoorganic or involutive syndrome, Choline alfoscerate has a positive effect on:

Concentration
Storing and retrieving information
Behavioral and cognitive reactions
Mood
Thinking abilities.

Alpha-glycerophosphocholine leads to emotional stability, removes nervousness and apathy.

In case of traumatic brain injury, Alpha-GPC helps to increase linear blood flow and stabilize spatial and temporal characteristics. Cholini alfosceras also eliminates neurological manifestations.

When taken orally, up to 90% of Choline alfoscerate is absorbed. Mostly the substance penetrates the brain, the rest is collected in the liver and lungs.

85% of gliatilin is excreted from the body through the lungs. The remaining 15% of the substance exits through the kidneys and intestines.

Indications for use of Choline Alfoscerate:

Traumatic brain injuries
Ischemic stroke
Senile dementia
Behavioral and emotional disorders
Brain involutional or degenerative psychoorganic syndromes.

Release form and composition

Choline alfoscerate has different trade names - FOSAL GFKh 85, Gladilin, etc. The drug is available in the form of a solution for intravenous or intramuscular administration. Each ampoule contains 250 mg of choline alfoscerate and purified water (1 ml).

Description of choline alfoscerate in ampoules instructions:

Each transparent glass ampoule contains 4 ml of medication
One cardboard box contains 10 ampoules.
A package made of aluminum foil and PVC film contains 3-5 ampoules.
Each blister pack contains 1-2 ampoules.

One of the forms of release of Choline Alfoscerate is capsules. Each pill contains 400 mg of cholini alfosceras.

The instructions for use state that the medicine, namely tablets containing choline alfoscerate, is taken orally for a long time. One package can contain 10, 14 or 28 tablets.

Instructions for using choline alfoscerate: method and dosage

The cost of Gliatilin in ampoules is from 181 rubles. The cost of the drug in tablets is from 525 to 1000 rubles.

Choline alfoscerate solution is administered intramuscularly or intravenously at a dosage of 100 mg per day (1 ampoule). For intravenous infusion, 4 ml of the drug is diluted in 50 ml of isotonic solution.

In one minute, the infusion rate is up to 80 drops. The average treatment time is 10 days, but the treatment time is determined by the doctor.

Compared to oral therapy, infusion treatment is more effective. Therefore, it is used for severe forms of brain disorders.

Instructions for use of Choline alfoscerate tablets:

For dementia syndrome and poor blood circulation, one pill (400 mg) is prescribed 3 times a day. Duration of therapy is 90-180 days.
For TBI, 0.8 g of Choline alfoscerate is prescribed in the morning and 0.4 g in the afternoon. The medicine is taken for six months.

Contraindications, drug interactions, special instructions

Choline alfoscerate is not prescribed until the age of 18, during lactation and pregnancy. Also, the use of the drug is contraindicated in acute hemorrhagic stroke and intolerance to gliatilin.

The interaction of Choline alfoscerate with other drugs has not been established.

Alpha-glycerophosphocholine affects the ability to control transport. Therefore, after taking the drug, caution should be exercised while performing complex activities.

It is noteworthy that choline is found in foods. Its food sources:

By-products
Yeast
Yolks
Beef
Sprouted wheat
Legumes
Cabbage
Cottage cheese
Spinach
Vegetable oils.

Side effects and overdose

Choline alfoscerate is often well tolerated even with prolonged use. But sometimes side effects occur after taking the medicine.

After using the drug, nausea, dry mouth, diarrhea and constipation often occur. Sometimes allergic manifestations occur - hives, skin rashes.

On the part of the nervous system after using Choline alfoscerate, the following negative reactions may develop:

Dizziness
Sleep disturbance
Nervousness
Headache
Anxiety
Aggressiveness
Drowsiness.

Other possible side effects are pharyngitis, frequent urination, discomfort in the area where the drug was administered.

In case of overdose, headache, nausea and overexcitement may occur. To eliminate negative reactions, it is necessary to reduce the dosage of the drug.

Analogs

Among the substitutes for Choline alfoscerate, the following analogues can be distinguished: Cereton and Delecite.

Manufacturer – Sotex, Russia

Price– from 400 rubles

Description – capsules or solution are prescribed for traumatic brain injuries, stroke, cognitive disorders, psychoorganic syndrome.

pros– capsules are easy to swallow, highly effective

Minuses– cost, increased excitability often occurs after taking it.

Manufacturer – Italfarmaco, Italy

Price– 450 rubles

Description – the solution is prescribed for psychoorganic syndrome and multi-infarct dementia.

pros– high efficiency, convenient packaging, pleasant taste

Minuses- cost, dry mouth may occur after taking.

Choline alfoscerate: instructions for use and reviews

Latin name: Choline alfoscerate

ATX code: N07AX02

Active substance: choline alfoscerate

Manufacturer: SINTEZ OJSC (Russia), DECO Company LLC (Russia), ATOLL LLC (Russia), PharmIntellect LLC (Russia), Borisov Medicinal Products Plant OJSC (Republic of Belarus)

Updating the description and photo: 21.11.2018

Choline alfoscerate is a nootropic agent.

Release form and composition

Dosage form - solution for intravenous and intramuscular administration: clear, colorless or slightly yellowish liquid [4 ml in ampoules: 3 or 5 ampoules in blister packs, 1 or 2 packs in a cardboard box; 5 ampoules in cardboard forms (trays) with cells for ampoules, 1 or 2 trays in a cardboard pack; 10 ampoules in blister packs, 1 pack in a cardboard pack].

Composition of 1 ml solution:

active substance: choline alfoscerate polyhydrate (in terms of choline alfoscerate) – 250 mg;
auxiliary component: water for injection.

Pharmacological properties

Pharmacodynamics

Choline alphoscerate is a phosphatidylcholine precursor and choline carrier. It has the potential ability to correct and prevent biochemical damage, which is of particular importance among the pathogenetic factors of psychoorganic involution syndrome, namely to reduce cholinergic transmission and change the damaged phospholipid composition of the membranes of nerve cells.

The chemical formula of choline alfoscerate contains 40.5% choline. It has metabolic protection properties and ensures the release of choline in brain tissue.

The drug is involved in the synthesis of phosphatidylcholine and acetylcholine in neuronal membranes, enhances metabolic processes and improves blood flow in the central nervous system, activates the reticular formation. Increases the linear speed of blood flow on the side of the traumatic brain injury. Normalizes the spatiotemporal characteristics of spontaneous bioelectrical activity of the brain. Promotes regression of neurological symptoms, restores consciousness.

The drug has a positive effect on cognitive abilities and memory functions, indicators of behavior and emotional state, which can be reduced due to involutional pathology of the brain.

Choline alfoscerate stimulates the dose-dependent release of acetylcholine under physiological conditions. Participates in the synthesis of membrane phospholipid (phosphatidylcholine), thereby improving receptor function, plasticity of neuronal membranes and synaptic transmission.

It does not have mutagenic or teratogenic effects and does not have a negative effect on the reproductive cycle.

Pharmacokinetics

In studies on different animal species (dogs, rats, monkeys), it was found that the pharmacokinetic characteristics of the radiolabeled drug are similar.

Choline alfoscerate is quickly and completely absorbed from the gastrointestinal tract. Rapidly accumulates and distributes in various tissues and organs, including the brain, where the concentration is higher compared to tritium-labeled choline. Easily penetrates the blood-brain barrier.

The drug is excreted primarily by the lungs (85%) in the form of carbon dioxide, as well as by the kidneys and intestines (15%).

Indications for use

psychoorganic syndrome against the background of degenerative and involutional processes in the brain;
senile pseudomelancholia;
behavioral and affective disorders in old age: decreased interest, increased irritability, emotional lability;
consequences of cerebrovascular insufficiency, primary and secondary cognitive impairment in older people: memory impairment, disorientation, confusion, decreased concentration, initiative and motivation;
traumatic brain injury with a predominantly brainstem level of damage (acute period);
multi-infarct dementia.

Contraindications

acute stage of hemorrhagic stroke;
age under 18 years;
During pregnancy and breastfeeding;
hypersensitivity to any component of the drug or drugs with a similar chemical structure.

Instructions for use of Choline alfoscerate: method and dosage

Choline alfoscerate is administered slowly intramuscularly or intravenously.

For intravenous use, the contents of one ampoule are diluted in 50 ml of 0.9% sodium chloride solution. The drug is administered at a rate of 60–80 drops per minute.

Therapy is usually carried out over 10 days. If necessary, the doctor may increase the dose and/or prolong treatment if this is justified by the clinical picture and characteristics of the course of the disease, taking into account the patient’s age and tolerability of the drug.

After stabilization of the patient's condition, the patient is transferred to oral dosage forms of choline.

Side effects

from the nervous system: drowsiness or insomnia, headache, dizziness, anxiety, aggressiveness, nervousness;
from the digestive system: pharyngitis, dry oral mucosa, diarrhea or constipation;
from the skin: skin rashes, urticaria;
other: pain at the injection site, increased urination.

Overdose

In case of overdose, the severity of dose-dependent side effects may increase.

Treatment is symptomatic. The effectiveness of dialysis has not been established.

special instructions

Nausea is possible during therapy, but may be a consequence of dopaminergic activation.

Impact on the ability to drive vehicles and complex mechanisms

During the treatment period, care should be taken when driving vehicles and performing work that requires increased attention, speed of mental and motor reactions.

Use during pregnancy and lactation

According to the instructions, Choline alfoscerate is contraindicated in pregnant and breastfeeding women.

Use in childhood

The drug is not used to treat patients under 18 years of age.

Drug interactions

Interactions of Choline alfoscerate with other drugs that would have clinical significance have not been established.

Analogs

Analogues of Choline alfoscerate are Gleatser, Gliatilin, Delecit, Cholitilin, Cerepro, Noocholin Rompharm, Cereton.

Terms and conditions of storage

Store out of reach of children, protected from light at temperatures up to 25 °C. Avoid freezing.

Shelf life – 3 years.

Choline alfoscerate is an active medicinal component that is found in many medications. You will learn about what properties this substance has, what it is indicated for and what drugs it is included in from the materials in this article.

Where is choline alphoscerate found?

Instructions for the use of those medications that include the presented component are available in each package along with the medicine.

The most well-known and widely used medications with this active ingredient are the following drugs:

"Gleazer."
"Gliatilin".
"Cerepro."
"Glycerylphosphorylcholine hydrate."
"Cereton".
"Holitilin" etc.

Existing forms of release

Preparations with such an active substance as choline alfoscerate, reviews of which are mostly positive, are available in the form of capsules and injection solutions. As a rule, they go on sale in cardboard packages or small plastic jars.

pharmachologic effect

Choline alfoscerate has an exciting effect on central cholinergic receptors. Entering the human body, such an active substance breaks down into choline and glycerophosphate.

The presented medicinal component ensures the complete formation of phosphatidylcholine. In addition, it significantly improves the plasticity and function of receptors, neuronal membranes, and also activates cerebral blood flow, stimulating cholinergic neurotransmission, nervous system metabolism and

It should also be noted that choline alfoscerate greatly improves concentration, the ability to memorize and further reproduce information, significantly improves mood, mental activity, and also eliminates negative emotions, including apathy, and optimizes cognitive reactions.

In case of traumatic brain injury, this substance normalizes blood flow in the affected area and the bioelectrical activity of the brain. In addition, this component of the drug helps suppress neurological symptoms.

Pharmacokinetics

After oral administration, the absorption of this component is about 88%. Choline alfoscerate passes through fairly easily. It should also be noted that this substance accumulates in the brain, lungs and liver. Its level in the central nervous system reaches approximately 45% of the content in blood plasma.

Indications for use

Why is choline alfoscerate prescribed to a patient? Analogs of this drug and the drug itself are used for:

acute period of traumatic brain injury;
dyscirculatory encephalopathy;
dementia (Alzheimer's type, senile or mixed forms);
during the recovery period of ischemic stroke;
memory disorders;
functional disorders of the central nervous system;
confusion;
decreased initiative, concentration and motivation;
disorientation;
senile pseudomelancholia.

Choline alfoscerate: instructions

Medicines (capsules) containing this active substance should be taken orally immediately before meals. As a rule, such drugs are prescribed by doctors in one dosage or another depending on the existing disease. But, according to the attached instructions, choline alfoscerate must be taken three times a day, 400 mg. The duration of such therapy is usually about 4-6 months.

If the patient has an acute condition, then the presented component is slowly administered intravenously or intramuscularly. In this case, the dosage of the injection solution is 1 g per day.

If after using the drug the patient experiences severe nausea, then it is advisable to reduce the dose by 1.5 or 2 times.

Contraindications for use

It is not recommended to use drugs that contain this component if you are hypersensitive to it. In addition, choline alfoscerate is strictly prohibited for use by pregnant women and nursing mothers.

Possible side effects

According to reviews, medications with the active substance choline alfoscerate almost never cause any side effects. However, occasionally, patients may experience severe or moderate nausea. As mentioned above, in such cases you should either reduce the dosage or completely stop taking the drug.

Drug overdose

If the drug choline alfoscerate is used uncontrolledly, the patient may experience an overdose. As a rule, the patient in such situations feels a strong feeling of nausea, which ends with vomiting, and allergic reactions (rash, itchy skin, etc.) may also occur.

Drug interactions

To date, no interaction of this substance with other medicinal components has been identified.

Price of drugs

The cost of medicines that contain the active substance choline alfoscerate varies significantly. Let's consider the price category of each drug in more detail:

Medicine "Gleatser". For three ampoules of this product you will have to pay about 260-270 Russian rubles.
The drug "Gliatilin". The price of 14 capsules of this medicine is about 740-760 rubles. If you need to purchase the medicine in ampoules, then for three pieces they will ask you about 570 rubles.
Medicine "Cerepro". This medicine in capsules is sold for 500 rubles (14 pieces). If you need the drug in ampoules, then for three pieces you will have to pay about 400 rubles.
Means "Cereton". Ampoules of this drug can be purchased for 280-300 rubles (3 pieces).
Medication "Holitilin". This product (ampoules) is sold in pharmacy chains for 370-380 rubles (3 jokes).