Raltegravir in Vitro Effect on Bilirubin Binding

Pediatr Infect Dis J. 2013 Sep;32(9):978-80. doi: 10.1097/INF.0b013e31829044a8.

Abstract

Drugs that displace bilirubin from albumin may increase the risk of kernicterus in neonates. We evaluated the effect of raltegravir on bilirubin-albumin binding in pooled neonatal serum using the peroxidase method. Raltegravir had minimal effect on bilirubin-albumin binding at concentrations of 5 and 10 µM, caused a small but statistically significant increase in unbound bilirubin at 100 µM and caused potentially harmful increases at 500 and 1000 µM. Our data suggest that the effect of raltegravir on neonatal bilirubin binding is unlikely to be clinically significant at typical peak concentrations reached with usual dosing.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / adverse effects
  • Anti-HIV Agents / metabolism*
  • Bilirubin / metabolism*
  • Humans
  • Infant, Newborn
  • Protein Binding
  • Pyrrolidinones / adverse effects
  • Pyrrolidinones / metabolism*
  • Raltegravir Potassium
  • Serum / chemistry
  • Serum Albumin / metabolism*

Substances

  • Anti-HIV Agents
  • Pyrrolidinones
  • Serum Albumin
  • Raltegravir Potassium
  • Bilirubin