2004
DOI: 10.1111/j.1365-2125.2004.02208.x
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Effect of itraconazole on the pharmacokinetics and pharmacodynamics of a single oral dose of brotizolam

Abstract: Br J Clin PharmacolBritish Journal of Clinical Pharmacology DOI:10.1111DOI:10. /j.1365DOI:10. -2125DOI:10. .2004 et al. Correspondence AimsTo assess the effect of itraconazole, a potent inhibitor of cy tochrome P450 (CYP)3A4, on the single oral dose pharmacokinetics and pharmacodynamics of brotizolam. MethodsIn this randomized, double-blind, cross-over trial 10 healthy male subjects received either itraconazole 200 mg or matched placebo once daily for 4 days. On day 4, a single 0.5 mg dose of brotizolam was a… Show more

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Cited by 16 publications
(6 citation statements)
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“…It is mainly metabolised by CYP3A4 (Figure 8), as demonstrated by the increase in the drug plasma levels, AUC and t 1/2 , in volunteers taking simultaneously brotizolam and the antibiotic erythromycin, a known CYP3A4 inhibitor [101]. A similar effect was observed when administering the antifungal itraconazole [102]. Conversely, rifampicin (a CYP3A4 inducer) significantly decreases C max (69%), AUC (90%) and t 1/2 (79%) of the drug [103].…”
Section: -Pharmacokinetics and Metabolismmentioning
confidence: 70%
“…It is mainly metabolised by CYP3A4 (Figure 8), as demonstrated by the increase in the drug plasma levels, AUC and t 1/2 , in volunteers taking simultaneously brotizolam and the antibiotic erythromycin, a known CYP3A4 inhibitor [101]. A similar effect was observed when administering the antifungal itraconazole [102]. Conversely, rifampicin (a CYP3A4 inducer) significantly decreases C max (69%), AUC (90%) and t 1/2 (79%) of the drug [103].…”
Section: -Pharmacokinetics and Metabolismmentioning
confidence: 70%
“…324 ng/mL). 16 In six patients, however, the plasma concentrations achieved for both itraconazole and hydroxyitraconazole appeared low, with the observed itraconazole Cmax being less than 100 ng/mL (range 14.6 to 71.6 ng/mL). There was no clear evidence that these patients were those where the smallest effect was seen on olaparib suggesting that sufficient itraconazole exposure to inhibit CYP3A4 had still been achieved in these patients.…”
Section: Study 7 (Cyp3a4 Inhibition)mentioning
confidence: 81%
“…Taken together, these results suggest that the Cmax and AUC of sunitinib increase non-linearly with the dose in the event of an overdose together with brotizolam probably due to the saturation of CYP3A4 by concomitant use of brotizolam. It is further strengthened by the results that tmax (9 h) and the elimination half-life (23.7 h) of brotizolam were considerably increased compared with reported values (0.75 and 4.51 h, respectively) [3]. Maintenance of plasma sunitinib concentrations above 50 ng ml −1 is required to inhibit vascular endothelial growth factor receptor [1], which is essential for haematopoietic development [4].…”
Section: Discussionmentioning
confidence: 78%