Itraconazole more bioavailable in solution [letter]

Prentice, A. G.; Warnock, DW

doi:10.1182/blood.v88.9.3662.bloodjournal8893662

Cited by 7 publications

(2 citation statements)

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“…Our patient was treated with itraconazole capsules, which resulted in concentrations of itraconazole in CSF that were below the MIC after 1 week of therapy. Treatment with itraconazole oral solution may have resulted in higher concentrations in CSF since the bioavailability of this formulation is increased (25). Nevertheless, treatment with itraconazole was discontinued in our patient because her clinical condition did not improve and, more importantly, concentrations of itraconazole in blood were not directly available.…”

mentioning

confidence: 88%

Aspergillus Meningitis: Diagnosis by Non-Culture-Based Microbiological Methods and Management

Verweij¹,

Brinkman²,

Kremer

et al. 1999

J Clin Microbiol

143

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The performance of antibody detection, antigen detection, andAspergillus genus-specific PCR for diagnosingAspergillus meningitis was investigated with 26 cerebrospinal fluid (CSF) samples obtained from a single patient with proven infection caused by Aspergillus fumigatus. Immunoglobulin G antibodies directed against Aspergilluswere not detected by enzyme-linked immunosorbent assay in CSF or serum. The antigen galactomannan was detected in the CSF 45 days before a culture became positive, and Aspergillus DNA was detected 4 days prior to culture. Decline of the galactomannan antigen titer in the CSF during treatment with intravenous and intraventricular amphotericin B and intravenous voriconazole corresponded with the clinical response to treatment.

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mentioning

confidence: 88%

Aspergillus Meningitis: Diagnosis by Non-Culture-Based Microbiological Methods and Management

Verweij¹,

Brinkman²,

Kremer

et al. 1999

J Clin Microbiol

143

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“…Recently, a solution with 10 g l −1 itraconazole in 40% hydroxypropyl‐β‐cyclodextrin, a cyclic oligosaccharide of seven glucose units with a hydrophobic interior and a hydrophilic exterior, has been licensed in Europe [14]. Several studies have shown that the bioavailability of itraconazole in the cyclodextrin solution compared to capsules is improved by about 30% in normal volunteers (Janssen Research Foundation, Belgium, data on file) and in patients receiving chemotherapy or bone marrow transplants [15–17].…”

Section: Introductionmentioning

confidence: 99%

Itraconazole trough concentrations in antifungal prophylaxis with six different dosing regimens using hydroxypropyl‐β‐cyclodextrin oral solution or coated‐pellet capsules

Glasmacher¹,

Hahn²,

Molitor

et al. 1999

Mycoses

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We have previously shown that a trough concentration of at least 500 ng ml-1 itraconazole is necessary for an effective antifungal prophylaxis in neutropenic patients. Since the bioavailability of itraconazole is reduced in these patients, a satisfactory dosing regimen remains to be defined. In this study, six dosing regimens with itraconazole capsules 400, 600 or 800 mg day-1, itraconazole solution 400 mg day-1 (additional loading dose: 400 mg day-1 solution for 2 days), 800 mg day-1 or 400 mg day-1 (additional loading dose: 800 mg day-1 capsules for 7 days, s/c1200) were compared during 160 courses of myelosuppressive chemotherapy in 123 patients with acute leukaemia. After the first week, patients taking 800 mg day-1 or 400 mg day-1 (s/c1200) itraconazole solution achieved significantly higher trough concentrations (high-performance liquid chromatography) than patients in other groups (P < 0.05) and 87 and 100%, respectively, of these had concentrations > 500 ng ml-1. Contrary to a dose of 400 mg day-1, a dose of 800 mg day-1 itraconazole solution induced severe nausea and vomiting in 46% of the patients. We conclude that 400 mg day-1 itraconazole solution with a loading dose of 800 mg day-1 capsules for 7 days resulted in sufficient trough concentrations from the first week onwards and appears to be suitable for antifungal prophylaxis in neutropenic patients.

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Drug interaction between oral solution itraconazole and calcineurin inhibitors in allogeneic hematopoietic stem cell transplantation recipients: an association with bioavailability of oral solution itraconazole

et al. 2009

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To assess the drug interaction between oral solution itraconazole and calcineurin inhibitors, 10 recipients of allogeneic hematopoietic stem cell transplantation (HSCT), in whom oral solution itraconazole was started when they had been on a steady dose of calcineurin inhibitors (cyclosporine A or tacrolimus), were retrospectively evaluated. The concentration/dose [C/D; (ng/mL)/(mg/kg)] ratio of calcineurin inhibitors significantly increased after initiating oral solution itraconazole, and the increase at 7-10 days after initiating itraconazole was 93.7%, ranging from 37.3 to 328.2%. The plasma level of itraconazole/hydroxyitraconazole was significantly correlated with the increase in the C/D ratio of calcineurin inhibitors (correlation coefficient, 0.65; P < 0.05). These results suggest that oral solution itraconazole significantly interacts with calcineurin inhibitors with a wide interindividual variability in allogeneic HSCT recipients, which could partly be explained by the variable bioavailability of oral solution itraconazole.

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Itraconazole more bioavailable in solution [letter]

Abstract: To the Editor: activity, itraconazole may be the superior prophylactic antifungal azole and reports of randomized controlled comparisons of the antifungal efficacy of these two drugs during the treatment of hematological malignancy will be available soon.

Cited by 7 publications

References 0 publications

Aspergillus Meningitis: Diagnosis by Non-Culture-Based Microbiological Methods and Management

Aspergillus Meningitis: Diagnosis by Non-Culture-Based Microbiological Methods and Management

Itraconazole trough concentrations in antifungal prophylaxis with six different dosing regimens using hydroxypropyl‐β‐cyclodextrin oral solution or coated‐pellet capsules

Drug interaction between oral solution itraconazole and calcineurin inhibitors in allogeneic hematopoietic stem cell transplantation recipients: an association with bioavailability of oral solution itraconazole

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