Grandaxin (Tofisopam)

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Grandaxin (aka tofisopam)

Grandaxin (Tofisopam) is a benzodiazepine anxiolytic drug that is used in Russia and some European countries. Despite being a benzodiazepine derivative, pharmacological action of Grandaxin is differs from that of typical benzos because of the structural differences.

Grandaxin is a 2,3- benzodiazepine derivative and belongs to the novel class of drugs called homophthalazines. Tofisopam does not cause sedation or cognitive functions impairments; moreover, it may produce a moderate stimulative action, possibly by increasing the sensitivity of dopaminergic receptors.

The drug does not bind to benzodiazepine receptors, it is suggested that its anxiolytic effect is mediated through its effect on opioid signal transduction.

One of the most important advantages of Grandaxin over commonly used benzodiazepines is that Tofisopam does not form an addiction.

Indications for use are:

  • Conditions followed by emotional tension, anxiety, apathy, and obsessive worrying
  • Reactive depression
  • Post-traumatic stress disorder
  • Menopause (as a standalone therapy or as adjuvant therapy with hormonal preparations)
  • Premenstrual syndrome
  • Alcohol abstinence syndrome

Dosage and administration

The dosage is 1-2 pills 1-3 times a day, the maximum daily dosage is 300mg. If taken occasionally, the dosage is 1-2 pills. Aged patients and patients with renal insufficiency should cut the dosage in half.

Side effects

  • Side effects on digestive system: loss of appetite, constipation, nausea, dry mouth.
  • Nervous system: headaches, insomnia, irritability, agitation, delirium, may provoke seizures in epileptic patients.
  • Allergic reactions
  • Muscle tension
  • Respiratory depression

Contraindications

  • Hypersensitivity
  • Conditions followed by psychomotor agitation, aggression or pronounced depression
  • Decompensated respiratory failure
  • Pregnancy and lactation
  • Sleep apnea
  • Coadministration with Tacrolimus, Sirolimus, or Cyclosporine
  • Lactose intolerance