Grandaxin is a non-sedating tranquilizer that is used in Russia and some European countries to treat anxiety. Although being a benzodiazepine derivative, tofisopam is not addictive and does not bind to benzodiazepine receptors.
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Tofisopam (primarily known as Grandaxin) is an atypical benzodiazepine tranquilizer drug. It is currently used in Russia, Japan, and several European countries to treat various psychiatric conditions (mainly anxiety disorders). Several studies also suggests that Tofisopam does have antipsychotic effect.
One of the biggest advantages of Grandaxin over conventional benzos is that it does not cause sedation and is not addictive, because of the structural differences.
The official indications for use are:
- Conditions accompanied with anxiety, emotional tension, physical anxiety, apathy, and obsessive worrying.
- Situational depression
- Post-traumatic stress disorder
- Menopausal syndrome (as a standalone drug or as adjuvant therapy with hormonal drugs)
- Premenstrual syndrome
- Non-cardiac chest pain
- Alcohol withdrawal syndrome
- Myasthenia, myopathy, neurogenic atrophy and other conditions with secondary psychiatric symptoms, when typical tranquilizers with muscle relaxant action are contraindicated.
Tofisopam has unique chemical structure, which determines its pharmacological effects that are differs from that of other benzodiazepine tranquilizers. Tofisopam is not a GABA receptors agonist does not binds to benzodiazepine receptors.
It is suggested that a possible target of action of 2,3-benzodiazepines is the opioid signal transduction. This suggestion is consistent with the results of animal studies, which shown that 2,3-BZDs potentiate the effects of opioid agonists, and their behavioral effects were inhibited by induced state of opioid tolerance.
Besides having anxiolytic action, Grandaxin has mild stimulating effect. Studies suggest that Tofisopam increase the sensitivity of central dopamine receptors, as it is shown to potentiate the effects of dopaminergic stimulants.
If you want to read more about the pharmacology of Grandaxin, you can read a detailed article here.
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Dosage and Administration
Set individually, taking into account the patient's condition, the clinical form of the disease and individual sensitivity to the drug.
For adults appoint 50-100 mg (1-2 tab.) 1-3 times / day. The maximum daily dose of 300 mg.
Children over 14 years old appoint up to 200 mg / day.
To prevent falling asleep, the drug is recommended to be taken no later than 15-16 hours a day.
Elderly patients and patients with renal insufficiency the daily dose is reduced by about 2 times.
With alcohol withdrawal syndromefor prevention and treatment delirium a short course of therapy is shown: from several days to 3-6 weeks.
From the digestive tract: loss of appetite, constipation, increased gas, nausea, dry mouth. In some cases, possible stagnant jaundice.
From the side of the central nervous system: headache, insomnia, irritability, psychomotor agitation, confusion, seizures may occur in patients with epilepsy.
Allergic reactions: rash, scarlet-like rash, itching.
From the musculoskeletal system: muscle tension, muscle pain.
On the part of the respiratory system: respiratory depression.
Caution should be prescribed the drug in the following cases:
Decompensated chronic respiratory distress syndrome.
Acute respiratory failure in history.
Closed angle glaucoma.
Organic brain damage (eg, atherosclerosis).
Simultaneous use of tacrolimus, sirolimus, cyclosporine and tofisopam is contraindicated. Plasma concentrations of drugs that are metabolized by CYP3A4 may increase when taken concomitantly with tofisopam.
The use of tofisopam with drugs that suppress the functions of the central nervous system (analgesics, general anesthesia, antidepressants, H1- antihistamine, sedative, hypnotic, antipsychotic, enhances their effects (for example, sedation or respiratory depression).
Hepatic enzyme inducers (alcohol, nicotine, barbiturates, antiepileptic drugs) can increase the metabolism of tofisopam, which can lead to a decrease in its concentration in the blood plasma and a weakening of the therapeutic effect.
Some antifungal drugs (ketoconazole, itraconazole) can slow down the hepatic metabolism of tofisopam, which leads to an increase in its concentration in blood plasma.
Some antihypertensive drugs (clonidine, calcium channel antagonists) may enhance the effects of tofisopam. Beta-blockers may slow down the metabolism of the drug, but this effect has no clinical significance.
Tofisopam can increase the level of digoxin in the blood plasma.
Benzodiazepines may affect the anticoagulant effect of warfarin.
Prolonged use of disulfiram may inhibit the metabolism of tofisopam.
Antacids may affect the absorption of tofisopam. Cimetidine and omeprazole inhibit the metabolism of tofisopam.
Oral contraceptives can reduce the intensity of the metabolism of tofisopam.
Tofisopam weakens the inhibitory effect of alcohol on the central nervous system.
Pregnancy and Lactation
Grandaksin is contraindicated for use in the first trimester of pregnancy and lactation.
Treatment of patients with myasthenia with Grandaxin should be carried out under strict permanent medical supervision.
With affective-shock reactions within the framework of reactive psychosis, as well as with deep depression, active combination therapy with the use of antidepressants is indicated.
The appearance of increased excitability during treatment with Grandaxin, dyspepsia in some cases can be eliminated by reducing the dose of the drug.
With the development of insomnia, the last drug intake should be done no later than 15 hours. The appearance of exanthema in the course of treatment with Grandaxin requires discontinuation of the drug.
In the event of allergic reactions to the drug or serious sleep disorders, Grandaxin should be stopped.
Influence on ability to drive motor transport and control mechanisms
Grandaxin does not cause a significant reduction in the ability to concentrate.
The question of the possibility of driving vehicles and driving mechanisms should be addressed only after evaluating the patient's individual response to the drug.
Symptoms: drowsiness, slight respiratory depression, in severe cases - coma.
Treatment: carrying out activities aimed at restoring respiratory function and cardiovascular activity. Recommended gastric lavage, taking activated charcoal. In emergency cases, it is possible to use a specific benzodiazepine antagonist, flumazenil.
- Brand name: Grandaxin
- Active ingredient: Tofisopam
- Dosage form: Pills
- Manufacturer: Egis
- Country of Origin: Hungary
- Arzneimittelanalysen mittels polarographischer Methoden, 24. Mitt. Über das polarographische Verhalten des Tofisopam
- The effects of tofisopam, a 3,4-benzodiazepine, in animal models of anziety, sedation, and convulsions
- Method validation and determination of enantiomers and conformers in tofisopam drug substances and drug products by chiral high-performance liquid chromatography and kinetic and thermodynamic study of the interconversion of the conformers
- Gas chromatography nitrogen phosphorous detection (GC-NPD) assay of tofisopam in human plasma for pharmacokinetic evaluation
- Spectrofluorimetric method for the determination of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine (tofisopam)
- Determination of tofisopam in serum by high-performance liquid chromatography
- Tofisopam, a novel 3,4,-benzodiazepine: Multiple-dose effects on psychomotor skills and memory. Comparison with diazepam and interactions with ethanol
- A comparison of the psychotropic profiles of tofisopam and diazepam
- Effect of tofisopam on the single-oral-dose pharmacokinetics and pharmacodynamics of the cyp3a4 probe drug alprazolam
- Tofisopam inhibits the pharmacokinetics of CYP3A4 substrate midazolam
- The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis
- Is tofisopam an atypical anxiolytic?
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- A population-based case–control teratologic study of nitrazepam, medazepam, tofisopam, alprazolum and clonazepam treatment during pregnancy
- Tofisopam and midazolam: differences in clinical effects and in changes of CSF monoamine metabolites.
- P.3.035 The profile of anti-anxiety action of tofisopam in the treatment of generalized anxiety disorder
- SEPARATION AND IDENTIFICATION OF TOFISOPAM STEREOISOMERS BY HYPHENATED HPLC-CD TECHNIQUE
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- Tofisopam, a new 2,3-benzodiazepine. Inhibition of changes induced by stress loading and hypothalamic stimulation
- Different Techniques for the Determination of Tofisopam
- In Vitro Prediction and in Vivo Verification of Enantioselective Human Tofisopam Metabolite Profiles