Pharmacokinetics of itraconazole oral solution in allogeneic bone marrow transplant patients receiving total body irradiation
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.
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The bioavailability of current oral formulations of itraconazole is unpredictable.
“the bioavailability of the current oral formulations of itraconazole (including the cyclodextrin solution) is unpredictable [145,146].”
From Guidelines for Treatment of Candidiasis (2004) · cites this paper as [145]
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- Authors
- Michallet, M., Persat, F., Kranzhöfer, N., Levron, J.-C., Prat, C., Belhabri, A., Chwetzoff, E., Le Moing, J.-P., Fiere, D., & Piens, M.-A.
- Affiliations
- Hôpital Edouard Herriot (FR)
- Lyon 1 Université (FR)
- Janssen (France) (FR)
- Venue
- Bone Marrow Transplantation
- Published
- 1998-06-01
- Volume
- 21
- Issue
- 12
- Pages
- 1239-1243
- ISSN
- 0268-3369 (ISSN-L)
- 1476-5365
- OpenAlex
- W2019338455
- Cited by
- 31
- References
- 16
- Citations by year
- 2021: 1 · 2015: 1 · 2014: 2
- FWCI
- 4.72
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Bone Marrow Transplantation (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Health Sciences › Medicine › Pediatrics, Perinatology and Child Health › Pharmaceutical studies and practices
- Health Sciences › Medicine › Pharmacology › Antibiotics Pharmacokinetics and Efficacy
- Keywords
- itraconazole, pharmacokinetics, oral solution, allogeneic bone marrow transplantation, total body irradiation, bioavailability, antifungal prophylaxis, neutropenia, plasma drug concentration
- MeSH terms
- Administration, Oral, Adult, Antifungal Agents, Female, Humans, Male, Middle Aged, Solutions, Transplantation, Homologous, Whole-Body Irradiation, Bone Marrow Transplantation, Itraconazole
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