Pharmacokinetics of itraconazole oral solution in allogeneic bone marrow transplant patients receiving total body irradiation

Bone Marrow Transplant. 1998 Jun;21(12):1239-43. doi: 10.1038/sj.bmt.1701270.

Abstract

A prospective study of the pharmacokinetics of itraconazole solution was performed in 11 patients who underwent allogeneic BMT (day of BMT = day 0) after a conditioning regimen including total body irradiation (TBI). Itraconazole solution (400 mg once a day) was given 7 days before BMT and continued up to the end of neutropenia unless another antifungal treatment was necessary. Blood samples were collected before itraconazole intake (Cmin) and 4 h later (Cmax) every other day for assays of itraconazole (ITRA) and its active metabolite hydroxy-itraconazole (OH-ITRA). The mean values of Cmin ITRA and OH-ITRA, respectively, were 287 +/- 109 ng/ml and 629 +/- 227 ng/ml at day -1 and 378 +/- 147 ng/ml and 725 +/- 242 ng/ml at day +1. The maximum Cmin values were observed at day +3. Six patients at day -1 (54%) and 8 at day +1 (72%) had satisfactory residual plasma concentrations of at least 250 ng/ml of unchanged ITRA. From day +1 to day +9, eight patients discontinued the itraconazole treatment, five of them had satisfactory plasma residual concentrations at this time. This work shows a good bioavailability of itraconazole oral solution during the early phase after allogeneic BMT, but more data are needed for the late phases.

MeSH terms

  • Administration, Oral
  • Adult
  • Antifungal Agents / pharmacokinetics*
  • Bone Marrow Transplantation*
  • Female
  • Humans
  • Itraconazole / administration & dosage
  • Itraconazole / pharmacokinetics*
  • Male
  • Middle Aged
  • Solutions
  • Transplantation, Homologous
  • Whole-Body Irradiation*

Substances

  • Antifungal Agents
  • Solutions
  • Itraconazole