Effect of oral citicoline therapy on retinal nerve flber layer and ganglion cell-inner plexiform layer in patients with primary open angle glaucoma

AIM: To evaluate the short-term effects of oral citicoline therapy on the retinal nerve fiber layer(RNFL) and the macular ganglion cell-inner plexiform layer(m GCIPL) in patients with primary open angle glaucoma(POAG).METHODS: Fifty-four eyes of 54 patients with POAG glaucoma included in the study.In addition to a topical hypotensive, 250-mg oral citicoline was administered to 27 patients, while 27 patients were assigned as the control group.RNFL and m GCIPL values were measured using optical coherence tomography(OCT) at 1 d before treatment and 3 mo after the initiation of treatment.At the third month visit, citicoline treatment was discontinued and drug-free control(wash-out) measurements were obtained at the fourth month in citicoline group.RESULTS: The average RNFL thickness was significantly higher at month 3 than the baseline(P=0.038) in citicoline group.However, this improvement partially regressed after a 1-month wash-out period.No statistically significant changes in RNFL were observed in the superior, nasal, temporal and inferior quadrants at months 3 and 4(P>0.05).The change in the average and inferior quadrant RNFL thickness in the citicoline group at 3 mo was significantly greater than the control group(P=0.006 and P=0.014, respectively).There were no significant differences between the groups according to the change in m GCIPL thickness and the superior, nasal and temporal quadrant RNFL thickness(P>0.05).CONCLUSION: With oral citicoline treatment, the loss in the average RNFL is prevented in POAG patients in the short-term.Study data show that citicoline may have a significant impact on slowing glaucoma progression, which could have a potential neuroprotective effect.

Improved Attentional Performance Following Citicoline Administration in Healthy Adult Women

Objectives: The present study assessed the potential cognitive-enhancing effects of citicoline, a dietary supplement, in healthy adult women. Specifically, it was hypothesized that citicoline supplementation would be associated with improved attention compared to placebo. Methods: The investigation was a double-blind, randomized, placebo-controlled three-arm study. Sixty healthy adult women ages 40 - 60 completed a clinical screening visit, including a medical exam. After study enrollment each subject was randomly assigned to one of three groups: a daily oral dose of 250 mg citicoline, 500 mg citicoline, or placebo for 28 days. Participants were evaluated with the Continuous Performance Test II (CPT-II), a measure sensitive to attentional function, during a baseline visit and 28 days after baseline. Results: All 60 participants were included in the analyses, which included an ANOVA with Tukey’s post-hoc tests and t-tests. After 28 days of supplementation, individuals in the 250 mg group made fewer omission (p = 0.04) and commission (p = 0.03) errors compared to those in the placebo group. Individuals in the 500 mg group made significantly fewer commission errors compared to those in the placebo group (p = 0.03) and trended toward making fewer omission errors (p = 0.07). Conclusion: After 28 days of daily citicoline supplementation, participants who were administered either the 250 mg or the 500 mg citicoline doses showed significantly better ability to produce correct responses on the CPT-II, likely due to improved cognitive inhibition. Our findings suggest that citicoline may improve attentional performance in middle-aged women and may ameliorate attentional deficits associated with central nervous system disorders.

Comparative Oral Absorption of Different Citicoline and Homotaurine Formulations: A Single-Dose, Two-Period Crossover Trial in the Dog

Background: Citicoline and homotaurine are compounds with a potent neuroprotective activity and they have been administered for many years in the treatment of numerous neurodegenerative and ophthalmological diseases, including glaucoma. Initially available only as liquid form, through parenteral route, nowadays citicoline can be administered also as tablet but no data on bioavailability of these different forms are available. In the present study, pharmacokinetics of citicoline in tablet versus vials, each at the therapeutic dose of 500 mg, in addition to 50 mg of homotaurine was investigated. Materials and methods: Ten mixed breed dogs received a single dose of 50 mg oral homotaurine and 500 mg citicoline in tablet and vials with the same dose were administered after a seven days wash-out period. Parameters assessed for citicoline metabolites (cytidine, uridine and choline) were AUC0−t, Cmax and Tmax. Results: Citicoline bioavailability appeared to be slightly higher for the tablet compared to the vial formulation. Cytidine is equivalent in absorption dynamics both for tablet and liquid form;uridine for tablet reaches its maximum and is reabsorbed more quickly while choline for the liquid form reaches the maximum first and is reabsorbed more quickly. Conclusions: Citicoline in tablet and liquid formulation have pharmacokinetic properties leading to a very similar bioavailability.

Simple diffusion delivery via brain interstitial route for the treatment of cerebral ischemia

Delivering pharmacologic agents directly into the brain has been proposed as a means of bypassing the blood brain barrier.However,despite 16 years of research on a number of central nervous system disorders,an effective treatment using this strategy has only been observed in the brain tumor glioblastoma multiforme.Within this study we propose a novel system for delivering drugs into the brain named the simple diffusion (SDD) system.To validate this technique,rats were subjected to a single intracranial (at the caudate nucleus),or intraperitoneal injection,of the compound citicoline,followed two hours later by a permanent middle cerebral artery occlusion (pMCAO).Results showed that 12 h after pMCAO,with 0.0025 g kg-1 citicoline,an infarct volume 1/6 the size of the intraperitoneal group was achieved with a dose 1/800 of that required for the intraperitoneal group.These results suggest that given the appropriate injection point,through SDD a pharmacologically effective concentration of citicoline can be administered.