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.