| Cytidine 5'-diphosphocholine, CDP-choline or citicoline, is an
essential intermediate in the biosynthetic pathway of the structural
phospholipids of cell membranes, especially in that of
phosphatidylcholine. Upon oral or parenteral administration, CDP-
choline releases its two principle components, cytidine and choline.
When administered orally, it is absorbed almost completely, and its
bioavailability is approximately the same as when administered
intravenously. Once absorbed, the cytidine and choline disperse
widely throughout the organism, cross the blood-brain barrier and
reach the central nervous system (CNS), where they are incorporated
into the phospholipid fraction of the membrane and microsomes. CDP-
choline activates the biosynthesis of structural phospholipids in the
neuronal membranes, increases cerebral metabolism and acts on the
levels of various neurotransmitters. Thus, it has been experimentally
proven that CDP-choline increases noradrenaline and dopamine levels
in the CNS. Due to these pharmacological activities, CDP-choline has
a neuroprotective effect in situations of hypoxia and ischemia, as
well as improved learning and memory performance in animal models of
brain aging. Furthermore, it has been demonstrated that CDP-choline
restores the activity of mitochondrial ATPase and of membranal Na+/K+
ATPase, inhibits the activation of phospholipase A2 and accelerates
the reabsorption of cerebral edema in various experimental models.
CDP-choline is a safe drug, as toxicological tests have shown; it has
no serious effects on the cholinergic system and it is perfectly
tolerated. These pharmacological characteristics, combined with CDP-
choline's mechanisms of action, suggest that this drug may be
suitable for the treatment of cerebral vascular disease, head trauma
of varying severity and cognitive disorders of diverse etiology. In
studies carried out on the treatment of patients with head trauma,
CDP-choline accelerated the recovery from post-traumatic coma and the
recuperation of walking ability, achieved a better final functional
result and reduced the hospital stay of these patients, in addition
to improving the cognitive and memory disturbances which are observed
after a head trauma of lesser severity and which constitute the
disorder known as postconcussion syndrome. In the treatment of
patients with acute cerebral vascular disease of the ischemic type,
CDP-choline accelerated the recovery of consciousness and motor
deficit, attaining a better final result and facilitating the
rehabilitation of these patients. The other important use for CDP-
choline is in the treatment of senile cognitive impairment, which is
secondary to degenerative diseases (e.g., Alzheimer's disease) and to
chronic cerebral vascular disease. In patients with chronic cerebral
ischemia, CDP-choline improves scores on cognitive evaluation scales,
while in patients with senile dementia of the Alzheimer's type, it
slows the disease's evolution. Beneficial neuroendocrine,
neuroimmunomodulatory and neurophysiological effects have been
described. CDP-choline has also been shown to be effective as co-
therapy for Parkinson's disease. No serious side effects have been
found in any of the groups of patients treated with CDP-choline,
which demonstrates the safety of the treatment.
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