tofisopam

Tofisopam is a benzodiazepine derivative used as an anxiolytic in several European and other markets. It is marketed under brand names such as Grandaxin and is available in oral tablet formulations.

Medical uses and availability: Tofisopam is prescribed for anxiety disorders, including generalized anxiety and situational anxiety, especially when avoidance of sedation or cognitive impairment is desired. In some regions it remains a common alternative to sedating benzodiazepines, though regulatory approval varies by country and it is not approved in the United States.

Pharmacology: It acts as a positive allosteric modulator at the GABA-A receptor, producing anxiolytic effects. Compared with many benzodiazepines, tofisopam is noted for relatively lower sedative, psychomotor-impairing, and muscle-relaxant effects and is often described as having a lower potential for abuse, though dependence risk can still occur with prolonged use.

Pharmacokinetics: After oral administration, tofisopam is absorbed and undergoes hepatic metabolism. It is eliminated from the body via the urine and feces, with pharmacokinetic properties that vary among individuals.

Safety and side effects: Common adverse effects include dizziness, headache, and fatigue. Sedation is less frequent than with many benzodiazepines but can occur. As with other CNS-active drugs, use with alcohol or other depressants should be avoided, and caution is advised in the elderly and in patients with liver disease.

See also: Benzodiazepines, Anxiolytics.