From the Research
Definition and Characteristics of Tofisopam
- Tofisopam is a 2,3-benzodiazepine compound that differs from classical 1,4-benzodiazepines in its structure and pharmacological profile 1, 2.
- It is marketed for the treatment of anxiety in some European countries and has been shown to have anxiolytic activity without appreciable sedative and muscle relaxant side effects 3, 4.
- Tofisopam does not bind to the benzodiazepine binding site of the γ-aminobutyric acid receptor and its psychopharmacological profile differs from that of classical benzodiazepines 1, 2.
Pharmacological Effects
- Tofisopam has been shown to have indirect dopaminergic effects, enhancing the behavioral actions of various dopaminergic drugs, and has mixed dopamine agonist and antagonist-like properties 5, 4.
- It acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with highest affinity to PDE-4A1, followed by PDE-10A1, PDE-3, and PDE-2A3 2.
- Tofisopam does not induce sleep even in subtoxic doses and only high doses enhance the effect of barbiturates and ethanol 1.
Clinical Use and Comparison to Other Anxiolytics
- Tofisopam has been compared to diazepam in the treatment of anxiety symptoms, with both drugs showing significant improvement on the Hamilton Anxiety Rating Scale, but with fewer adverse effects and withdrawal symptoms in the tofisopam group 3.
- Tofisopam has been proposed as a novel class of compounds that reduce anxiety by increasing the ability of patients to cope with daily tasks, rather than classical anxiolytics that reduce anxiety by tranquilization 4.