CDP-Choline (cytidine-5'-diphosphocholine) is a unique form of choline that readily passes through the blood-brain barrier directly into brain tissue. CDP-choline is a rate-limiting intermediate in the biosynthesis of phosphatidylcholine, an important component of the neural cell membrane. CDP-choline has been found to be of value in studies on animals and humans.
CDP-Choline (cytidine-5'-diphosphocholine) is also known by its drug name, Citicholine. Citicoline is approved as a drug in Europe and Japan for use in stroke, head trauma, and other neurological disorders. It is presently being evaluated in phase II/III stroke trials in the United States. (D'Orlando and Sandage 1995)
Citicoline [stabilized CDP Choline (cytidine 5' diphosphocholine)] is a naturally occurring, water soluble biological compound that is an essential intermediate for the synthesis of phosphatidylcholine, a major constituent of the gray matter of brain tissue (30%). Citicoline is metabolized to yield the free nucleotide cytidine and choline. Scientific research demonstrates that Citicoline consumption promotes brain metabolism by enhancing the synthesis of acetylcholine, restoring phospholipid content in the brain and regulation of neuronal membrane excitability and osmolarity (by its effect on the ATP-dependent sodium and potassium pump).
Citicoline (cytidine diphosphate choline, or CDP-choline) is not just a source of choline, the main building block of the neurotransmitter acetylcholine. Instead, Citicoline is a brain phospholipid booster. The most popular and well-known brain phospholipids supplement is phosphatidylserine (PS). But brain function relies on a wide spectrum of phospholipids, and not just PS. Of course, PS supplements contain small amounts of some of the other key brain phospholipids, such as (phosphatidylcholine [PC] and phosphatidylinositol [PI]). But they don’t contain these nutrients, in the same proportions as are found in a healthy, functioning brain. Taking individual phospholipids, such as PS, forces more of the specific phospholipid that you’re taking into the membranes of nerve and other cells. But it cannot restore the youthful balance of all brain phospholipids.
Choline and pantothenic acid (vitamin B5) are used to produce acetylcholine, the major neurotransmitter that transmits nerve impulses between neurons. Choline is also needed for cell membrane integrity, and to move fats in and out of cells. Choline is, therefore, essential for proper brain function as the brain is composed of millions of nerve cells and is composed almost entirely of fats. CDP-choline may reduce central nervous system ischemic injury by stabilizing cell membranes and reducing free radical generation.
Human Studies of CDP Choline
Four studies of intravenously administered CDP-choline have been conducted outside the United States:
A multi-center double-blind placebo-controlled study of citicoline (1000 mg per day intravenously for 14 days was conducted on patients with acute, moderate to severe cerebral infarction. One hundred thirty-three patients received CDP-choline treatment, and 139 received placebo. The group treated with CDP-choline showed significant improvements in level of consciousness compared with the placebo-treated group, and CDP-choline was an entirely safe treatment. (Tazaki, Sakai et al. 1988)
A double-blind placebo-controlled study of citicoline (750 mg per day intravenously for 10 days) used within 48 hours of stroke onset showed a significant improvement on a quantified neurological assessment scale rating motor strength, muscular force, sensation, higher cortical function, and ambulation at 90 days. Patients treated with citicoline were significantly more likely to be ambulatory compared with placebo-treated patients at 90 days. (Goyas, Bastard et al. 1980)
A second double-blind, placebo-controlled trial of intravenous citicoline (250 mg three times a day for 10 days) in stroke patients treated within 48 hours of their symptoms found that a significantly higher percentage of patients had a very good to fairly good recovery with citicoline versus placebo treatment at 10 days after stroke. (Boudouresques and Michel 1980)
A small double-blind, placebo-controlled study examined the effects of citicoline (1000 mg per day of intravenous for 30 days) or placebo in 19 patients with acute stroke treated within 48 hours. In comparison to their baseline assessments, 76% of the citicoline-treated patients demonstrated improvement compared with only 31% of the placebo-treated patients. (Corso, Arena et al. 1982)
