[An experimental study of the pharmacokinetic mechanisms for the development of gidazepam tolerance]

It has been shown that the basis for the development of tolerance to the myorelaxant effect of gidazepam given long to rats is biotransformational changes followed by varying pharmacokinetic parameters: decreases in the AUC of gidazepam and its desalkyl metabolite in plasma, in brain in particular, redistribution of these substances between the plasma and brain of tolerant rats. Changes in pharmacokinetic parameters have no influence on their anxiolytic effects.