Summary
Seven healthy volunteers received a single oral dose of triazolam 0.25 mg after 7 days on troleandomycin 2 g/day p.o. or placebo in a double-blind cross-over study. Plasma triazolam and psychometric and memory tests (including Critical Flicker Fusion threshold, Choice Reaction Time, Digit Symbol Substitution and Self-Rating Scales) were assessed at regular intervals after the final treatment.
Troleandomycin was found to prolong the psychomotor impairment and amnesia produced by triazolam.
There was a significant enhancement of the AUC, the peak concentration and the delay to tmax of triazolam after 7 days treatment with troleandomycin compared to placebo.
Thus, there is a pharmacokinetic interaction, and the combination of triazolam and troleandomycin should be avoided or the dose of triazolam should be adjusted. The most likely mechanism is a diminished hepatic first-pass effect, and a decrease in the apparent oral clearance of triazolam.
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Warot, D., Bergougnan, L., Lamiable, D. et al. Troleandomycin-triazolam interaction in healthy volunteers: Pharmacokinetic and psychometric evaluation. Eur J Clin Pharmacol 32, 389–393 (1987). https://doi.org/10.1007/BF00543975
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DOI: https://doi.org/10.1007/BF00543975