Pharmacodynamics of citicoline relevant to the treatment of glaucoma

Abstract

Citicoline (exogenous CDP‐choline) is a nontoxic and well‐tolerated drug used in pharmacotherapy of brain insufficiency and some other neurological disorders, such as stroke, brain trauma, and Parkinson's disease. A few reports indicate that citicoline treatment may also be beneficial in glaucoma. Currently glaucoma is considered a neurodegenerative disease in which retinal ganglion cells (RGC) slowly die, likely in the apoptotic mechanism. Endogenous CDP‐choline is a natural precursor of cellular synthesis of phospholipids, mainly phosphatydylcholine (PtdCho). Enhancement of PtdCho synthesis may counteract neuronal apoptosis and provide neuroprotection. Citicoline, when administered, undergoes a quick transformation to cytidine and choline, which are believed to enter brain cells separately and provide neuroprotection by enhancing PtdCho synthesis; similar effect may be expected to occur in glaucomatous RGC. Furthermore, citicoline stimulates some brain neurotransmitter systems, including the dopaminergic system, and dopamine is known as a major neurotransmitter in retina and postretinal visual pathways. In a double‐blind, placebo‐controlled study, treatment of glaucoma resulted in functional improvement in the visual system noted with electrophysiological methods. Development of citicoline as a treatment for glaucoma is indicated. © 2002 Wiley‐Liss, Inc.

Proton Magnetic Resonance Spectroscopy (1H-MRS) Reveals Geniculocalcarine and Striate Area Degeneration in Primary Glaucoma

“…Intraocular pressure elevation and hypoperfusion cause the blockage of anterograde axonal transport and retrograde axonal transport in optic nerve fibers. These actions are followed by the suspending of target-derived neurotrophic factors along with massive excitotoxins [28]. Increased reactive oxygen species and decreased concentrations of antioxidants have been found in the glaucomatous vitreous, as have oxidative DNA damage and oxidative alterations of the trabecular meshwork [12].…”

Citicoline Oral Solution in Glaucoma: Is There a Role in Slowing Disease Progression?

“…In addition, a beneficial effect of citicoline has been described in a number of conditions affecting the visual system, like amblyopia [21,22,23,24] and nonarteritic ischemic optic neuropathy [25]. There are interesting findings concerning the use of citicoline in glaucoma [26,27,28,29,30,31]. In particular, in a double-blind placebo-controlled study with glaucoma patients, citicoline given by intramuscular injections for 60 consecutive days has been found to shorten the visual evoked potential P100 latency and increase the N75-P100 amplitude [26].…”

http://www.esciencecentral.org/journals/seizures-as-an-adverse-event-of-cellular-therapy-in-pediatric-neurological-disorders-and-its-prevention-2329-6895-2-164.php?aid=28197

“…Clinical trials have suggested that citicholine repairs the damage to optic nerve which occurs in glaucoma [39]. It provides neuroprotection to retina by enhancing phosphatidylcholine synthesis.…”

“…It provides neuroprotection to retina by enhancing phosphatidylcholine synthesis. It is postulated that dopaminergic stimulation is the major mechanism for the effect of citicholine on the retina [39]. In a double-blind, placebo-controlled trial using citicholine, retinal and visual functions were improved in patients of open angle glaucoma [40].…”