1: Methods Find Exp Clin Pharmacol. 1995 Oct;17 Suppl B:1-54.

CDP-choline: pharmacological and clinical review.

Secades JJ, Frontera G.

F.I.S.A. Medical Department, Barcelona.

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.


PMID: 8709678 [PubMed - indexed for MEDLINE]