nucleic acid derivatives | citicoline is a kind of nucleic acid derivatives, which plays an important role in the synthesis of lecithin, improves brain function by promoting the synthesis of lecithin. Citicoline is stronger than other neuroprotective drugs in evidence-based medicine, and its clinical application is more extensive. The drug was first developed by the Japan-Japan Company in 1967, and the trade name is Nicoline. It has been used in clinical practice for nearly half a century. In 1988, it officially entered China. The bioavailability and pharmacokinetic characteristics of citicoline oral dosage forms are similar to those of intravenous drugs, and the oral absorption is complete, and the oral dosage forms are more conducive to the long-term medication of patients, which can bring greater benefits to patients, in the clinical popular. Citicoline is mainly used for the treatment of stroke, brain edema, brain injury, vertigo, encephalitis neuritis, senile dementia and various disorders of consciousness caused by nerve injury, long-term medication was needed. Injection is extremely inconvenient to use, and oral preparation because of the advantages of convenient use and safe and effective, has long been recognized by the majority of doctors and patients. |
pharmacology | citicoline (C14H26N4O11P2) is a single nucleotide derivative composed of nucleic acid, cytosine, Pyrophosphate and choline. It can be rapidly absorbed by oral administration and hydrolyzed into choline and cytosine in the intestine and liver, which enter the blood circulation system, cross the blood-brain barrier and recombine into citicoline in the central nervous system, 80% phospholipid synthesis in the central nervous system is affected by the concentration of citicoline in the body. In addition, citicoline can be converted to acetylcholine in the central nervous system and oxidized to Betaine in the kidneys and liver. Citicoline has good water solubility and bioavailability as high as 90%, and only less than 1% is excreted in feces after oral administration. There were two absorption peaks in the plasma, 1 hour and 24 hours after ingestion, respectively. In the rat model, 10 hours after the intake of radiolabeled citicoline, its content steadily increased in the brain, widely distributed in the white and gray matter of the brain. The high concentration was maintained at 48 hours, and its elimination was very slow, and only a small amount was excreted by urine, feces and respiration every day. Exogenous citicoline can promote the rapid repair of damaged cell surface and mitochondrial membrane, maintain cell integrity and biological properties, and inhibit cell apoptosis and death. |
indication | The main indication was disturbance of consciousness after acute brain surgery and brain operation; clinically, it is also used for other functions and disturbance of consciousness caused by acute injury of central nervous system, paralysis, tinnitus and nerve deafness, hypnotic poisoning, etc. In recent years, it is widely used in clinic for ischemic stroke, cerebral arteriosclerosis, multi-infarct dementia, Alzheimer's disease, viral encephalitis in children, etc. |
effect | Citicoline is an endogenous nucleoside naturally produced in the body, it is an intermediate in the main pathway of cell membrane phospholipid biosynthesis. Large amounts of citicoline are required for the repair of nerve cell membranes. Supplement of exogenous citicoline can promote the synthesis of nerve cell membrane phospholipids. Citicoline plays an essential role in maintaining a variety of cellular physiological processes. In a variety of due to ischemia, bleeding caused by cell membrane dysfunction, degenerative disease, citicoline has obvious clinical therapeutic effect. |
uses | citicoline can restore the structure of cell membrane after brain cell injury, enhance the function of cell membrane and improve the function of neurons; 2, can reduce cerebral vascular resistance, increase cerebral blood flow, promote cerebral metabolism, improve cerebral circulation, improve brain function; 3, increase the secretion of nerve conduction mediators including acetylcholine and dopamine, enhance the function of brain stem reticular structure related to consciousness, improve the body's state of consciousness, improve the speed of recovery; 4, can also inhibit the activation of phospholipase A2, thereby accelerating the reabsorption of cerebral edema. 5, can enhance the dopaminergic activity, regulate the physiological function of extrapyramidal system. 6, has been shown to increase memory, promote learning function. |