Choline alfoscerate is a trade name for analogues. Why and how to take choline alfoscerate - clear description and instructions. Choline alfoscerate: side effects

Instructions:

Clinical and pharmacological group

02.052 (Nootropic drug. Centrally acting cholinomimetic)

Release form, composition and packaging

Soft gelatin capsules, red to brown, oblong; the contents of the capsules are an oily, transparent, colorless or slightly colored liquid.

Excipients: glycerol, purified water.

Shell composition: medical gelatin, glycerol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, red iron oxide, titanium dioxide, purified water.

14 pcs. - blisters (1) - cardboard packs. 14 pcs. - dark glass jars (1) - cardboard packs.

The solution for intravenous and intramuscular administration is transparent, colorless.

4 ml - ampoules (3) - cardboard packs. 4 ml - ampoules (3) - contour cell packaging (1) - cardboard packs.

pharmachologic effect

Centrally acting cholinomimetic, which contains 40.5% metabolically protected choline (metabolic protection promotes the release of choline in the brain). When it enters the body, it is broken down by enzymes into choline and glycerophosphate: choline is involved in the biosynthesis of acetylcholine, one of the main mediators of nervous excitation; glycerophosphate is a precursor to phospholipids (phosphatidylcholine) in the neuronal membrane. The drug ensures the synthesis of acetylcholine and phosphatidylcholine in neuronal membranes, improves blood flow and enhances metabolic processes in the central nervous system, activates the reticular formation; increases the linear speed of blood flow on the side of the traumatic brain injury, helps to normalize the spatiotemporal characteristics of spontaneous bioelectrical activity of the brain; has a positive effect on the cognitive and behavioral reactions of patients with vascular diseases of the brain.

The drug improves brain function by affecting the pathogenetic factors of involutional psychoorganic syndrome, changes the phospholipid composition of neuronal membranes and reduces cholinergic activity. Dose-dependently stimulates the release of acetylcholine, participating in the synthesis of phosphatidylcholine (membrane phospholipid), improves synaptic transmission, plasticity of neuronal membranes, and receptor function.

Pharmacokinetics

Suction and distribution

After oral administration, absorption is 88%.

Easily penetrates the BBB, the concentration in the brain reaches 45% of the level in the blood plasma.

Metabolism and excretion

In the body, choline alfoscerate is biotransformed under the action of enzymes to choline and glycerophosphate (providing the pharmacological effects of the drug). 85% is excreted by the lungs as carbon dioxide; the remainder (15%) is excreted in urine and feces.

Dosage

In acute conditions, the drug is administered intramuscularly or intravenously (slowly) in a daily dose of 1 g (1 ampoule) for 10-15 days, then switch to oral administration of the drug in a daily dose of 1.2 g (800 mg / 2 caps. / in the morning and 400 mg / 1 capsule / in the afternoon) for 6 months.

For chronic conditions, the drug is prescribed orally at 400 mg (1 capsule) 3 times a day. Duration of therapy is 3-6 months.

Overdose

Symptoms: dyspepsia.

Treatment: gastric lavage, taking activated carbon, symptomatic therapy.

Drug interactions

Drug interactions with Cerepro have not been established.

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Experimental studies did not reveal any mutagenic or teratogenic effects of the drug, or any effect on reproductive functions.

Side effects

From the digestive system: nausea (as a result of dopaminergic activation).

Other: allergic reactions.

Storage conditions and periods

List B. The drug should be stored in a dry place, protected from light and out of reach of children, at a temperature not exceeding 25°C. Shelf life – 2 years.

Indications

- acute and recovery periods of severe traumatic brain injury and ischemic stroke, recovery period of hemorrhagic stroke, occurring with focal hemispheric symptoms or symptoms of brain stem damage;

— psychoorganic syndrome against the background of degenerative and involutional changes in the brain;

— chronic cerebral circulatory failure;

- cognitive disorders (impaired mental function, memory, confusion, disorientation, decreased motivation, initiative and ability to concentrate), incl. for dementia and encephalopathy;

- senile pseudomelancholy.

Contraindications

- pregnancy;

- lactation period (breastfeeding);

- hypersensitivity to the components of the drug.

special instructions

If nausea occurs after taking the drug, the dose should be reduced.

Impact on the ability to drive vehicles and operate machinery

Cerepro does not affect the speed of psychomotor reactions.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Registration numbers

. solution for intravenous and intramuscular administration of 1 g/4 ml: amp. 3 pcs. LS-000476 (2002-06-10 - 0000-00-00)
. caps. 400 mg: 10 or 14 pcs. LS-000475 (2031-05-10 - 0000-00-00) 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.

Gross formula

C 8 H 20 NO 6 P

Pharmacological group of the substance Choline alfoscerate

Nosological classification (ICD-10)

CAS code

28319-77-9

Pharmacology

pharmachologic effect- neuroprotective.

Excites cholinergic receptors, mainly central (has a cholinomimetic effect). In the body it is broken down into choline and glycerophosphate. The substrate provides the synthesis of acetylcholine and phosphatidylcholine of neuronal membranes. Stimulates cholinergic neurotransmission, improves the plasticity of neuronal membranes and receptor function, activates cerebral blood flow, stimulates central nervous system metabolism and reticular formation. Increases mood, improves mental activity, concentration, memorization and the ability to reproduce received information, optimizes cognitive and behavioral reactions, eliminates emotional instability and apathy. In the acute period of traumatic brain injury, it helps to normalize blood flow and bioelectrical activity of the brain on the affected side, and contributes to the regression of neurological symptoms.

Absorption when taken orally - 88%; easily penetrates the BBB, accumulates mainly in the brain (concentration in the brain reaches 45% of the level in the blood), lungs and liver; 85% is excreted by the lungs in the form of carbon dioxide, the remaining amount (15%) is excreted by the kidneys and through the intestines.

Does not affect the reproductive cycle, does not have teratogenic or mutagenic effects.

Application of the substance Choline alfoscerate

Traumatic brain injury (acute period) with a predominantly brainstem level of damage, chronic cerebrovascular insufficiency (dyscirculatory encephalopathy), dementia (Alzheimer's type, senile, mixed forms), ischemic stroke (recovery period), Huntington's chorea, functional disorders of the central nervous system, memory impairment, confusion, disorientation, decreased motivation, initiative and concentration, senile pseudomelancholia.

Contraindications

Hypersensitivity, pregnancy, breastfeeding.

Use during pregnancy and breastfeeding

Contraindicated during pregnancy. Breastfeeding should be stopped during treatment.

Side effects of the substance Choline alfoscerate

Nausea, allergic reactions.

Routes of administration

Inside.

special instructions

Interactions with other active ingredients

Trade names

Name The value of the Vyshkowski Index ®
0.1482
0.1095
0.0923
0.0101

Belongs to the group of neurometabolic stimulants and has a neuroprotective effect. Cholinomimetic with a predominant effect on choline receptors in the central nervous system.
Excites cholinergic receptors, mainly central (has a cholinomimetic effect).
The mechanism of action is based on the fact that when choline enters the body, alfoscerate is broken down by enzymes into choline and glycerophosphate: choline is involved in the biosynthesis of acetylcholine, one of the main mediators of nervous excitation; glycerophosphate is a precursor of phospholipids (phosphatidylcholine) in the neuron membrane. Stimulates cholinergic neurotransmission - improves the transmission of nerve impulses in cholinergic neurons, improves the plasticity of neuronal membranes and receptor function, activates cerebral blood flow, stimulates central nervous system metabolism and reticular formation. In patients with involutive or hereditary degenerative psychoorganic syndrome, it has a positive effect on cognitive and behavioral reactions, improves concentration, memorization and reproduction of information. Improves mood, helps eliminate emotional instability, irritability and apathy. Activates mental activity. In the acute period of traumatic brain injury in patients with preserved mechanisms of autoregulation of cerebral blood flow, choline alfoscerate causes an increase in the linear velocity of blood flow on the affected side, helps to normalize the spatiotemporal characteristics of spontaneous bioelectrical activity of the brain, regression of neurological symptoms and restoration of consciousness.
When taken orally, an average of about 88% of the administered dose is absorbed. Easily penetrates the BBB, accumulates mainly in the brain (concentration in the brain reaches 45% of the level in the blood), lungs and liver. Elimination occurs primarily through the lungs in the form of carbon dioxide. Only 15% of the drug is excreted by the kidneys and intestines.
Does not affect the reproductive cycle, does not have teratogenic or mutagenic effects.

Indications for use of the drug Choline alfoscerate

  • in the acute and recovery period of severe traumatic brain injury with a predominantly brain stem level of damage (impaired consciousness, coma, focal hemispheric symptoms, symptoms of brain stem damage);
  • degenerative or involutional brain psychoorganic syndromes and consequences of cerebrovascular insufficiency, such as primary and secondary disorders of mental function in the elderly, characterized by memory impairment, confusion, disorientation, decreased motivation and initiative, decreased ability to concentrate;
  • dementia of various origins (including Alzheimer's disease);
  • changes in the emotional and behavioral sphere: emotional instability, irritability, decreased interest;
  • senile pseudomelancholia.

Use of the drug Choline alfoscerate

In acute conditions, choline alfoscerate is administered intramuscularly or intravenously (slowly) at 1000 mg per day (in the morning) for 15-20 days. Then - 1200 mg (800 mg in the morning, 400 mg in the afternoon) for 6 months. For chronic cerebrovascular insufficiency and dementia syndromes, 400 mg (1 capsule) is prescribed orally 2-3 times a day, preferably before meals. The duration of treatment is 3-6 months.

Contraindications to the use of the drug Choline alfoscerate

Individual hypersensitivity to the drug, pregnancy and lactation.

Side effects of the drug Choline alfoscerate

Nausea may occur (mainly as a consequence of dopaminergic activation), in which case the dose of the drug is reduced. The same recommendations for overdose.

Special instructions for the use of Choline alfoscerate

It is not recommended to use choline alfoscerate during pregnancy and lactation, although special studies have shown the absence of embryotoxic or teratogenic activity; does not have a negative impact on drivers and machine operators.

Drug interactions Choline alfoscerate

No significant interactions with other drugs have been established.

Overdose of the drug Choline alfoscerate, symptoms and treatment

There is no information about overdose.

List of pharmacies where you can buy Choline alfoscerate:

  • Saint Petersburg
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