Glicetile Mechanism of Action

Pharmacology: L-alpha-glycerylphosphorylcholine, also called choline alfoscerate, is a phospholipid metabolite.
After oral administration of choline alfoscerate (1200 mg) in healthy young volunteers, mean free plasma choline increased quickly (from 10.1±0.66 μM/L at 0 h to 13.6±1.04 μM/L at 2 h); the Cmax was reached in about 3 hours (14.2±1.66 μM/L) and the values recorded remained higher than basal for about 10 hours.
After oral administration, choline alfoscerate is cleaved within gut mucosal cells, by the action of glycerylphosphoryl-choline diesterase (L-3-glyceryl-phosphorylcholine glycerophosphohydrolase), into glycerylphosphate and free choline, which enters the portal circulation and can reach brain tissues, where it is incorporated into the phospholipid fraction of the neuronal plasma membrane and into microsomes. In the brain, the concentration of choline alfoscerate increases slowly and attains maximum levels 8 hours after administration, thereafter remaining constant over 30 hours.
Pharmacodynamics: Mechanism of Action: Choline alfoscerate is involved in brain phospholipid metabolism, being cleaved by the enzyme glycerylphosphorylcholine diesterase into a molecule of choline and another of glycerol-1-phosphate. Choline can be used for synthesizing acetylcholine whereas glycerol-1-phosphate, after phosphorylation, can enter the phospholipid pool. Activation of these pathways could provide both free choline and phospholipids for synthesizing acetylcholine and reconstituting nerve cell membrane components. On the other hand, both choline kinase and phosphocholine acyltransferase are able to covert choline into phospholipids. Choline alfoscerate is therefore a source of choline of the same form that a cell would obtain scavenging its own membranes and probably the form of choline that neurons use for synthesizing acetylcholine when larger amounts of choline are required, or when it is poorly available.
Pharmacokinetics: Absorption and distribution: After oral administration, absorption is 88%. Readily crosses the blood-brain barrier and accumulates mainly in the brain (the concentration reaches 45% of the level in blood plasma), lung and liver.
Metabolism and excretion: In the body of choline alfoscerate enzymatically biotransformed to choline and glycerophosphate (providing the pharmacological effects of the drug). 85% is excreted in the lungs as carbon dioxide, the remaining part (15%) is excreted in the urine and feces.