Pharmacological properties
Pharmacodynamics. Choline alfoscerate is a drug that belongs to the group of central cholinomimetics with a predominant effect on the CNS. Choline alfoscerate as a choline carrier and a precursor of phosphatidylcholine can potentially prevent and correct biochemical damage, which is of particular importance among the pathogenic factors of psychoorganic involutional syndrome, i.e. it can affect the reduced cholinergic tone and the altered phospholipid composition of nerve cell membranes. The drug contains 40.5% metabolically protected choline. Metabolic protection is provided by the release of choline in the brain.
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 participates in the biosynthesis of acetylcholine - one of the main mediators of nervous excitation; glycerophosphate is a precursor of phospholipids (phosphatidylcholine) of the neuronal membrane.
Thus, choline alfoscerate improves the transmission of nerve impulses in cholinergic neurons; has a positive effect on the plasticity of neuronal membranes and the function of receptors. Choline alfoscerate improves cerebral blood flow, enhances metabolic processes in the brain, activates the structures of the reticular formation of the brain and restores consciousness in traumatic brain injury.
Pharmacokinetics. On average, almost 88% of the administered dose of choline alfoscerate is absorbed. The drug accumulates mainly in the brain (45% of the drug concentration in the blood), lungs and liver. Elimination of the drug occurs mainly through the lungs in the form of carbon dioxide (CO 2). Only 15% is excreted in the urine and bile.
Indication
Acute period of severe traumatic brain injury with predominantly brainstem level damage (impaired consciousness, comatose state, focal hemispheric symptoms, symptoms of brainstem damage).
Degenerative-involutional cerebral psychoorganic syndromes or secondary consequences of cerebrovascular insufficiency, i.e. primary and secondary disorders of mental activity in the elderly, characterized by memory impairment, confusion, disorientation, decreased motivation and initiative, decreased ability to concentrate; changes in the emotional sphere and behavioral sphere: emotional instability, irritability, indifference to the environment; pseudomelancholia in the elderly.
Application
In acute conditions, 1 g (4 ml) per day is administered intramuscularly or intravenously (slowly) for a period of 15-20 days. After stabilization of the patient's condition, it is necessary to switch to the oral dosage form of choline alfoscerate.
Contraindication
Known hypersensitivity to the drug or its components. psychosomatic syndrome, severe psychomotor agitation.
Side effects
During the use of the drug, reactions at the injection site are possible. During the first days or weeks of treatment, the following side effects may occur: anxiety, agitation, insomnia. These symptoms are temporary and do not require discontinuation of treatment, but a temporary dose reduction is possible. Nausea (which is mainly a consequence of secondary dopaminergic activation), decreased appetite, headache, very rarely abdominal pain and short-term confusion are possible. In this case, the dose of the drug should be reduced.
Hypersensitivity reactions are possible, including rash, itching, urticaria, angioedema, and skin redness.
Special instructions
Use during pregnancy and breastfeeding. The drug is contraindicated during pregnancy and breastfeeding.
Children. Due to the lack of sufficient experience in the use of the drug for the treatment of children, it should not be used in pediatric practice.
Ability to influence the reaction speed when driving vehicles or other mechanisms. The drug does not affect the ability to drive vehicles and work with complex mechanisms.
Interactions
Clinically significant drug interactions with other drugs have not been established.
Incompatibility: Should not be used in the same container with other medications.
Overdose
In case of an overdose of choline alfoscerate, which may manifest as nausea, anxiety, agitation, and insomnia, the dose of the drug should be reduced. Therapy is symptomatic.
Storage conditions
In the original packaging at a temperature not exceeding 25 °C.
