title: Raltegravir in vitro effect on bilirubin binding.
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.
authors.affiliation: From the *Department of Pediatrics, Boston University School of Medicine/Boston Medical Center, Boston, MA; †Department of Pediatrics, Division of Neonatal and Developmental Medicine, Stanford University School of Medicine, Stanford, CA; and ‡Merck & Co., Inc., Whitehouse Station, NJ.
authors.forename: Diana F
authors.initials: DF
authors.lastname: Clarke
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Wong
authors.forename: Larissa
authors.initials: L
authors.lastname: Wenning
authors.forename: David K
authors.initials: DK
authors.lastname: Stevenson
authors.forename: Mark
authors.initials: M
authors.lastname: Mirochnick
mesh_terms: D019380:Anti-HIV Agents / Q000009:adverse effects / Q000378:metabolism*; D001663:Bilirubin / Q000378:metabolism*; D006801:Humans; D007231:Infant, Newborn; D011485:Protein Binding; D011760:Pyrrolidinones / Q000009:adverse effects / Q000378:metabolism*; D000068898:Raltegravir Potassium; D044967:Serum / Q000737:chemistry; D012709:Serum Albumin / Q000378:metabolism*
chemical_list: D019380:Anti-HIV Agents; D011760:Pyrrolidinones; D012709:Serum Albumin; D000068898:Raltegravir Potassium; D001663:Bilirubin