Itraconazole brotizolam

H4N2 302-01-2) see Acetazolaraide Allopurinol Brotizolam Carbidopa Cibenzoline Desmopressin Estazolam Etizolam Guanadrel Isoniazid Itraconazole Mitopodozide Niftiroxazide Nifurtimox Nitrofurantoin Phenelzine Primaquine Ziprasidone hydrochloride hydrazine-1,2-bis(thiocarbaxamide)... 

The metabolism of brotizolam is altered by drugs that inhibit CYP3A4, such as erythromycin and itraconazole. 

In a randomized, double-blind, placebo-controlled, crossover study in 10 healthy men, itraconazole 200 mg/day for 4 days significantly altered the pharmacokinetics of a single dose of brotizolam 0.5 mg it reduced the apparent oral clearance four-fold, increased the AUC0 24h more than two-fold, and prolonged the half-life five-fold (6). The digit symbol substitution test and sleepiness were significantly altered as a result. 

Osanai T, Ohkubo T, Yasui N, Kondo T, Kaneko S. Effect of itraconazole on the pharmacokinetics and pharmacodynamics of a single oral dose of brotizolam. Br J Clin Pharmacol 2004 58(5) 476-81. 

Fluconazole, itraconazole and ketoconazole very markedly increase the serum levels of midazolam and triazolam, thereby increasing and prolonging their sedative and amnesic effects. Similar but smaller effects are seen with itraconazole or ketoconazole and alprazolam and with itraconazole and brotizolam. Even less effect is seen with etizolam and itraconazole and no important interaction occurs between estazolam and itraconazole. Small effects are found with the non-benzodiazepine hypnotic, zolpidem, with ketoconazole and even less effects with zopiclone and itraconazole. 

A placebo-controlled study in 10 healthy subjects found that itraconazole 200 mg daily for 4 days increased the AUCo 24 and maximum plasma levels of a single 500-microgram dose of brotizolam given on day 4 by about 2.5-fold and 25%, respectively. The elimination half-life of brotizolam was also increased, from 4.51 to 23.27 hours, and sedation was increased. ... 

The effects of alprazolam and brotizolam are increased and prolonged by ketoconazole and itraconazole, but the extent of this is less than that seen with midazolam or triazolam. However, some dosage reductions may still be necessary. 

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See also in sourсe #XX -- [ ]

See also in sourсe #XX -- [ ]

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