Single- and repeated-dose oral toxicity studies of citicoline free-base (choline cytidine 5'-pyrophosphate) in Sprague-Dawley rats

Int J Toxicol. 2009 Nov-Dec;28(6):479-87. doi: 10.1177/1091581809349452.

Abstract

The dietary supplement Citicoline free-base (choline cytidine 5'-pyrophosphate) was toxicologically evaluated in Sprague-Dawley rats using oral gavage. In an acute 14-day study, 2000 mg/kg was well tolerated. In a 90-day study, 100, 350, and 1000 mg/kg/day doses resulted in no mortality. In males, slight significant increases in serum creatinine (350 and 1000 mg/kg/day), and decreases in urine volume (all treated groups) were observed. In females, slight significant increases in total white blood cell and absolute lymphocyte counts (1000 mg/kg/day), and blood urea nitrogen (BUN) (100 and 350, but not 1000 mg/kg/day) were noted. A dose-related increase in renal tubular mineralization, without degenerative or inflammatory reaction, was found in females (all treated groups) and two males (1000 mg/kg/day). Renal mineralization in rats (especially females) is influenced by calcium:phosphorus ratios in the diet. A high level of citicoline consumption resulted in increased phosphorus intake in the rats, and likely explains this result.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Blood Cell Count
  • Blood Chemical Analysis
  • Calcinosis / chemically induced
  • Calcinosis / pathology
  • Creatinine / blood
  • Cytidine Diphosphate Choline / toxicity*
  • Female
  • Kidney / pathology
  • Kidney Diseases / chemically induced
  • Kidney Diseases / pathology
  • Kidney Tubules / pathology
  • Lethal Dose 50
  • Male
  • Nootropic Agents / toxicity*
  • Organ Size / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Time Factors
  • Urodynamics / drug effects

Substances

  • Nootropic Agents
  • Cytidine Diphosphate Choline
  • Creatinine