Pharmacokinetic and pharmacodynamic assessment of oral valganciclovir in the treatment of symptomatic congenital cytomegalovirus disease

J Infect Dis. 2008 Mar 15;197(6):836-45. doi: 10.1086/528376.

Abstract

Background: Intravenous ganciclovir administered for 6 weeks improves hearing outcomes in infants with symptomatic congenital cytomegalovirus (CMV) disease involving the central nervous system.

Methods: Twenty-four subjects received antiviral therapy for 6 weeks. Serial pharmacokinetic assessments were performed after administration of valganciclovir oral solution and of intravenous ganciclovir.

Results: On the basis of a previous pharmacokinetic study of the use of intravenous ganciclovir in this population, a target AUC12 (area under the concentration-time curve over a 12-h period) of 27 mg x h/L was defined. The median dose of oral valganciclovir administered in the present trial was 16 mg/kg, which produced a geometric mean AUC12 of 27.4 mg x h/L. The bioavailability of valganciclovir was 41.1%. Of the 18 subjects who had detectable CMV in whole blood at baseline or during therapy, 11 had <4 log viral DNA copies/mL at baseline, and 7 had > or =4 log viral DNA copies/mL at baseline; subjects who started the study with the higher viral burden experienced greater decreases in viral load but did not clear virus during the 42-day course of therapy. Neutropenia of grade 3 or 4 developed in 38% of subjects.

Conclusions: In neonates with symptomatic congenital CMV disease, valganciclovir oral solution provides plasma concentrations of ganciclovir comparable to those achieved with administration of intravenous ganciclovir. The results of the present study cannot be extrapolated to extemporaneously compounded liquid formulations of valganciclovir.

Publication types

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

MeSH terms

  • Administration, Oral
  • Area Under Curve
  • Cytomegalovirus / isolation & purification*
  • Cytomegalovirus Infections / blood
  • Cytomegalovirus Infections / congenital
  • Cytomegalovirus Infections / drug therapy*
  • Cytomegalovirus Infections / virology
  • Drug Administration Schedule
  • Female
  • Ganciclovir / adverse effects
  • Ganciclovir / analogs & derivatives*
  • Ganciclovir / blood
  • Ganciclovir / pharmacokinetics
  • Ganciclovir / pharmacology
  • Humans
  • Infant, Newborn
  • Male
  • Valganciclovir
  • Viral Load

Substances

  • Valganciclovir
  • Ganciclovir