Citicoline exhibits very low toxicity profile in humans. In clinical use it has been observed to be safe at doses up to 2 g/day.
The LD50 of a single IV dose of citicoline was 4.6 and 4.15 g/kg in mice and rats, respectively. An oral LD50 could not be determined as no deaths occurred at the maximum possible oral dose.
In an unpublished acute toxicity study, free-base citicoline was administered to male and female rats at a dose of 2 g/kg body weight for 14 days. No changes in body weight, deaths, clinical symptoms, or gross pathological changes were observed.