High plasma concentrations of zidovudine (AZT) do not parallel intracellular concentrations of AZT-triphosphates in infants during prevention of mother-to-child HIV-1 transmission

E. Kinai, Shingo Kato, Shinichi Hosokawa, Miyuki Sadatsuki, Hiroyuki Gatanaga, Yoshimi Kikuchi, Nguyen Van Lam, D. Q. Ha, Nguyen Van Kinh, Nguyen Thanh Liem, Shinichi Oka

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OBJECTIVES:: Zidovudine (AZT) is mainly used to prevent mother-to-child HIV-1 transmission (PMTCT). Despite serious concerns on AZT-associated toxicity, there is little information on pharmacokinetics of intracellular AZT metabolites in infants. METHODS:: We conducted a prospective study in 31 HIV-uninfected infants who received AZT for PMTCT. Blood samples were obtained from 14 infants on post-delivery days (PDD) 1, 7, 14, and 28, and from 17 infants at 0 and 4 hours after dosing on PDD-1. Plasma AZT concentrations (pAZT) and intracellular concentrations of AZT-monophosphate (icAZT-MP), diphosphate (icAZT-DP), and triphosphate (icAZT-TP) were determined. RESULTS:: Plasma AZT and icAZT-MP concentrations were 2713 nmol/L and 79 fmol/10 cells in PDD-1, but decreased to 1437 nmol/L and 31 fmol/10 cells by PDD-28 (p=0.02 and p=0.07 for all PDDs, respectively), whereas those of icAZT-DP and icAZT-TP remained low throughout the sampling period (p=0.29 and p=0.61 for all PDDs, respectively) There were no differences in icAZT-TP between infants of the 2 mg/kg 4 times a day dose and 4 mg/kg twice daily dose (p=0.25), whereas pAZT and icAZT-MP levels were higher in the latter (p

Original languageEnglish
JournalJournal of Acquired Immune Deficiency Syndromes
Publication statusAccepted/In press - 2016 Feb 8


ASJC Scopus subject areas

  • Infectious Diseases
  • Pharmacology (medical)

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