Grandaxin (tofisopam)

Non-sedating benzodiazepine tranqulizer

Grandaxin (Tofisopam) is the representative of a group of drugs belonging to the class of tranquilizers.

The main feature of tofisopam is the location of the nitrogen group. In traditional benzodiazepines, the nitrogen group located at positions 1 and 4 of the diazepine ring, while in Grandaxin nitrogen atoms is located at 2-3 positions. Thus, grandaxin is commonly referred to 2-3 benzodiazepines.

Like all benzodiazepine tranquilizers, the drug enhances the inhibitory effect of GABA in the central nervous system by increasing the sensitivity of GABA-benzodiazepine receptors in the reticular formation of the brain stem and intercalary neurons of the lateral horns of the spinal cord. Tofisopam reduces the excitability of subcortical structures of the brain (limbic system, thalamus, hypothalamus), and inhibits polysynaptic spinal reflexes. Anxiolytic action is mediated by its influence on the amygdala complex of the limbic system and manifests itself in reducing emotional tension, fear, and anxiety.

Being an atypical tranquilizer, Grandaxin has the following unique properties:

  • Does not develop physical dependence
  • Does not have sedative, muscle relaxant, anticonvulsant effects
  • Does not potentiate the effect of ethanol
  • Does not impair cognitive functions (in particular, does not impair attention),
  • Does not have cardiotoxic effect (on the contrary, it shows a beneficial effect on coronary blood flow and myocardial oxygen demand);
  • Has a moderate stimulating effect and therefore belongs to the group of “daytime” tranquilizers.

Tofisopam is an anxiolytic without hypnotic action, thus it does not impair psychomotor, intellectual, and working performance. Grandaxin quickly and effectively suppresses both mental, motor and autonomic anxiety symptoms and is indicated to treat any anxiety, especially anxiety disorders followed by disturbances in the autonomic nervous system.

It is shown that the use of grandaxin in the complex therapy of peptic ulcer helps to improve the functional state of the gastroduodenal zone, accelerate the scarring of ulcers due to the restoration of psychovegetative balance and neurohormonal regulation.

Grandaxin also has a positive effect in patients with chronic heart failure in the early post-infarction period, and also improves the quality of life of post-infarct patients, shortens the terms of the rehabilitation period.

Tofisopam is successfully used in gynecological practice for the correction of psychovegetative manifestations of the premenstrual syndrome, the initial manifestations of arterial hypertension in the premenopausal and perimenopausal period, and in the complex treatment of gestosis and chronic pelvic pain syndrome.

In case of mixed anxiety-depressive disorder, it is advisable to use grandaxin as a measure to accelerate the clinical effect of antidepressants of the group of selective serotonin reuptake inhibitors (SSRIs), since their antidepressant and anxiolytic action takes time to take effect. Grandaxin also can be used for the correction of anxiety and panic attacks, the increase of which can be triggered by the initiation of antidepressant medication, and in cases when the antidepressant dose is insufficient, and its increase is limited by side effects.

Moreover, grandaxin is widely used in neurological practice. In particular, the drug is used for psycho-vegetative disorders of neurotic genesis, when combined with cerebrovascular diseases, including somatic and cognitive disorders in elderly patients. In outpatient practice, tofisopam used in the treatment of stress disorders and adjustment disorders without interruption from professional activity, since the drug has a favorable tolerability profile.

The safety of the drug and good tolerability makes it possible to recommend it as a basic component of the treatment regimen for a significant part of neurological patients. In the neurological practice, the administration of Grandaxin in conjunction with traditional therapy of patients with psycho-vegetative disorders significantly increases the effectiveness of treatment in chronic neurological diseases (such as vascular, degenerative, and demyelinating disorders).