Brotizolam
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Pharmacokinetics
Half-life
4.4 hours.
Absorption
The plasma concentration profile of brotizolam can be described as a one compartmental open model with first-order absorption.
0.63 l/kg.
Total clearance: 109 ml/min.
Metabolism
There are two primary metabolites: 1-methyl-hydroxy- and the 4-hydroxy-derivatives (Eberts et al., 1981; Boehringer Ingelheim, product information). The 4-hydroxymetabolites have a pharmacological activity which is far less than that of the parent drugs, but the 1-methyl-hydroxymetabolites probably have comparable activity (Gall et al., 1978; Jochemsen et al., 1982; Sethy & Harris, 1982; Jochemsen et al., unpublished results). These active compounds are, however, not present in plasma in measurable amounts following a single dose of brotizolam to young healthy subjects (Jochemsen et al., 1982; Jochemsen et al., unpublished results).
Brotizolam has known human metabolites that include alpha-hydroxy-BRT and 6-hydroxy-BRT.
Protein binding
The mean value of the free fraction (%): 8.4 ± 0.7.
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