友情提示：此款药品最小订购量80 strips。

---------------------------------------------------------------
 部分中文胞磷胆碱钠处方资料（仅供参考）
---------------------------------------------------------------

胞磷胆碱钠片
英文名：Citicoline Sodium Tablets

药品成分：胆碱胞嘧啶核苷二磷酸酯的单钠盐。

功能主治：用于急性颅脑外伤和脑术后意识障碍。

口服：每日2次～3次，成人每次0.1g～0.2g，儿童每次0.1g 

注意事项：脑出血急性期不宜大剂量应用。肌注一般不采用，若用时应经常更换注射部位。

贮藏方法：密封

不良反应：本品对人及动物均无明显的毒性作用，对呼吸、脉搏、血压无影响，偶有一过性血压下降、失眠、兴奋及给药后发热等，停药后即可消失。

药物相互作用：如与其他药物同时使用可能会发生药物相互作用，详情请咨询医师或药师。

药代动力学：注入本品可迅速进入血流，并有部分通过血脑屏障进入脑组织。其中胆碱部分在体内成为良好的甲基化供体，可对多种化合物有转甲基化作用，约有1%的胆碱可从尿中排出。

药理毒理：本品为核苷衍生物，通过降低脑血管阻力，增加脑血流而促进脑物质代谢，改善脑循环。另外，他可增强脑干网状结构上行激活系统的机能，增强锥体系统的机能，改善运动麻痹，故对促进大脑功能的恢复和促进苏醒，有一定作用。

Citicoline
Citicoline (INN), also known as cytidine diphosphate-choline (CDP-Choline) & cytidine 5'-diphosphocholine is a psychostimulant/nootropic. It is an intermediate in the generation of phosphatidylcholine from choline.

Studies suggest that CDP-choline supplements increase dopamine receptor densities,and suggest that CDP-choline supplementation can ameliorate memory impairment caused by environmental conditions.Preliminary research has found that citicoline supplements help improve focus and mental energy and may possibly be useful in the treatment of attention deficit disorder.Citicoline has also been shown to elevate ACTH independently from CRH levels and to amplify the release of other HPA axis hormones such as LH, FSH, GH and TSH in response to hypothalamic releasing factors.These effects on HPA hormone levels may be beneficial for some individuals but, may have undesirable effects in those with medical conditions featuring ACTH or cortisol hypersecretion including, but not limited to, PCOS, type II diabetes and major depressive disorder.

Medical Uses
Citicoline is available as a supplement online and in stores. It is sold in over 70 countries under a variety of brand names: Ceraxon, Cognizin, NeurAxon, Somazina etc. When taken as a supplement citicoline is hydrolyzed into choline and cytidine in the intestine. Once these cross the blood-brain barrier it is reformed into citicoline by the rate-limiting enzyme in phosphatidylcholine synthesis, CTP-phosphocholine cytidylyltransferase.

Memory Disorders
In the hippocampi of rats with induced Alzheimer’s Disease, citicoline counteracts neuronal degeneration and reduces the number of apoptotic cells present. Citicoline supplementation also improves memory retention.

Ischemic stroke
Citicoline is approved for treatment in cases of head trauma, stroke, and neurodegenerative disease in Japan and Europe. Citicoline improves the clinical outcome following an ischemic stroke, as evinced by the reduction in size of lesions caused by ischemic strokes after supplementation. Citicoline reduces rates of death and disability following an ischemic stroke.

Vision
Citicoline improves visual function in patients with glaucoma, amblyopia, and non-arteritic ischaemic optic neuropathy.

Satiety
Cocaine dependence is associated with depleted dopamine levels in the central nervous system. In cocaine-dependent individuals citicoline increases brain dopamine levels and reduces cravings.  In the general population citicoline increases brain responses to food stimuli, specifically in the amygdala, insula, and lateral orbitofrontal cortex, which correlate with decreased appetite.

Mechanism Of Action
Neuroprotective effects
The neuroprotective effects exhibited by citicoline may be due to its preservation of cardiolipin and sphingomyelin, preservation of arachidonic acid content of phosphatidylcholine and phosphatidylethanolamine, partial restoration of phosphatidylcholine levels, and stimulation of glutathione synthesis and glutathione reductase activity. Citicoline’s effects may also be explained by the reduction of phospholipase A2 activity.  Citicoline increases phosphatidylcholine synthesis.The mechanism for this may be:
By converting 1, 2-diacylglycerol into phosphatidylcholine
Stimulating the synthesis of SAMe, which aids in membrane stabilization and reduces levels of arachidonic acid. This is especially important after an ischemia, when arachidonic acid levels are elevated.

Neuronal Membrane
The brain prefers to use choline to synthesize acetylcholine. This limits the amount of choline available to synthesize phosphatidylcholine. When the availability of choline is low or the need for acetylcholine increases, phospholipids containing choline can be catabolized from neuronal membranes. These phsopholipids include sphingomyelin and phosphatidylcholine. Supplementation with citicoline can increase the amount of choline available for acetylcholine synthesis and aid in rebuilding membrane phospholipid stores after depletion.Citicoline decreases phospholipase stimulation. This can lower levels of hydroxyl radicals produced after an ischemia and prevent cardiolipin from being catabolized by phospholipase A2. It can also work to restore cardiolipin levels in the inner mitochondrial membrane.

Cell Signalling
Citicoline enhances cellular communication by increasing the availability of neurotransmitters, including acetylcholine, norepinephrine, and dopamine.

Blood Flow
Citicoline increases glucose metabolism in the brain and cerebral blood flow.

Inflammation and Stress
Citicoline reduces oxidative stress. It also prevents excessive inflammatory response in the brain by inhibiting the release of free fatty acids and decreasing blood-brain barrier breakdown.

Glutamate transport
Citicoline lowers increased glutamate concentrations and raises decreased ATP concentrations induced by ischemia. Citicoline also increases glutamate uptake by increasing expression of EAAT2, a glutamate transporter, in vitro in rat astrocytes. It is suggested that the neuroprotective effects of citicoline after a stroke are due in part to citicoline’s ability to decrease levels of glutamate in the brain.

Pharmacokinetics
Citicoline is water-soluble, with more than 90% bioavailability. Plasma levels peak one hour after oral ingestion, and a majority of the citicoline is excreted as CO2 in respiration, and again 24 hours after ingestion, where the remaining citicoline is excreted through urine.

Dosage
The most effective oral dosages appear to be between 500 and 2,000 mg.

Side Effects
Citicoline has a very low toxicity profile in animals and humans. Clinically it doses of 2000 mg per day have been observed and approved. Minor transient adverse effects are rare and most commonly include stomach pain and diarrhea.

Synthesis
In vivo
phosphatidylcholine is a major phospholipid in eukaryotic cell membranes. Close regulation of its biosynthesis, degradation, and distribution is essential to proper cell function. phosphatidylcholine is synthesized in vivo by two pathways
The Kennedy pathway, which includes the transformation of choline to citicoline, by way of phosphorylcholine, to produce phosphatidylcholine when condensed with diacylglycerol.
Phosphatidylcholine can also be produced by the methylation pathway, where phosphatidylethanolamine is sequentially methylated.

---------------------------------------------------------------