Tofisopam - Active Substances. Instruction and Application, Dosage

Name: Tofisopam

The Latin name of the substance Tofisopam

Tofisopamum (genus Tofisopami)

Chemical name: 1- (3,4-dimethoxyphenyl) -5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine

Formula - C22H26N2O4

Therapeutic substances Tofisopam- anxiolytics

The nosological classification (ICD-10)

F10.3 abstinence
F10.4 abstinent state with delirium
F11 Mental and behavioral disorders due to use of opioids
F32.0 Depressive episode mild
F40.2 Specific (isolated) phobias
F41.1 Generalized anxiety disorder
F43.1 Post-traumatic stress disorder
F43.2 Disorder adaptive reactions
F45 Somatoform disorders
F48 Other neurotic disorders
F60.3 Emotionally unstable personality disorder
N94.3 syndrome premenstrual tension
N95.1 menopausal and menopausal status of women
R07.2 Pain in the heart

CAS code - 22345-47-7

Characteristics substance Tofisopam
"Full-time" antianxiety drug, an atypical benzodiazepine derivative (2,3-benzodiazepine). White to yellowish white crystalline powder. Practically insoluble in water, soluble in alcohol difficult.

Pharmacology

Mode of action - anxiolytic.

Interacts with benzodiazepine receptors increases the sensitivity of the GABA neurotransmitter-receptor enhances GABA-mimetic processes in the CNS. It has anxiolytic activity, accompanied by virtually no sedative, muscle relaxant and anticonvulsant properties. Has vegetative stabilizing and stress-protective effect, dilates coronary vessels. Especially effective for physical symptoms of anxiety.

When administered is rapidly and almost completely absorbed from the gastrointestinal tract, Cmax in the blood is reached within 2 hours after the plasma concentration decreased monoexponential. T1 / 2 6-8 h, the biotransformation products formed have no anxiolytic effect. Write mainly in the urine (60-80%) in the form of glucuronide, 20-30% is excreted in the faeces. Not accumulates.

Application of the substance Tofisopam

Neuroses and neurosis-like states; State, accompanied by emotional stress, autonomic disorders, moderate, fear, apathy, decreased activity, intrusive experiences; reactive depression with moderately severe psychopathological symptoms; post-traumatic stress disorder; disorder mental adaptation; cardiology (monotherapy or in combination with other drugs), climacteric syndrome (monotherapy and in combination with hormonal therapy); premenstrual stress syndrome; myasthenia gravis, myopathies, neurogenic muscle atrophy and other pathological states with secondary neurotic symptoms when anxiolytics contraindicated with pronounced muscle relaxant effect.

The Addictions: alcohol withdrawal syndrome, delirious state (for de-excitation and vegetative symptoms), opium withdrawal syndrome and post-abstinent state. Neurotic, psychotic disorders with alcoholism, as well as conditions characterized by apathy, decreased activity in alcoholism.

Contraindications

Hypersensitivity (including to other benzodiazepines), psychosis and psychopathy with pronounced psychomotor agitation, aggressiveness or deep depression; decompensated respiratory failure, apnea syndrome during sleep (in history), the simultaneous application of tacrolimus, sirolimus, cyclosporine; pregnancy (I term), breast-feeding, age under 18 years.

Restrictions of application of Tofisopam

Decompensated chronic respiratory distress syndrome, acute respiratory failure in the history of angle-closure glaucoma, epilepsy, organic brain damage (such as atherosclerosis).

Side effects of Tofisopam substance 

From the nervous system and sensory organs: headache, agitation, irritability, aggressiveness, irritability, sleep disorder; sometimes - confusion, seizures in patients with epilepsy.

From the respiratory system: respiratory depression.

From the digestive tract: loss of appetite, nausea, dry mouth, gastralgia, dyspepsia, increased separation of gas, constipation; in some cases - congestive jaundice.

From the musculoskeletal system: muscle tension, muscle pain.

Allergic reactions: itching, rash.

Interaction

It contraindicated Tofisopam combined use with tacrolimus, sirolimus, cyclosporine. Hepatic enzyme inducers (alcohol, nicotine, barbiturates, antiepileptics) Tofisopam may enhance metabolism, which may lead to a decrease in its plasma concentration and therapeutic effect of weakening.

Some antifungal drugs (ketoconazole, itraconazole) may slow Tofisopam hepatic metabolism, which leads to an increase in its concentration in plasma. Some antihypertensives (clonidine, BPC) may enhance the effects Tofisopam.

Together with the admission Tofisopam may increase plasma levels of drugs that are metabolized by CYP3A4.

Overdose of Tofisopam

Symptoms: deep sleep, in severe cases (after receiving doses of 50-120 mg / kg) - vomiting, confusion, coma, respiratory depression and / or seizures.

Treatment: restoration of function of respiration and cardiovascular activity.

Dosing and Administration of Tofisopam

Inside. The mode set individually, depending on the indication, the patient's condition, drug tolerability. Single dose - 50-100 mg, the daily average - 150-300 mg 1-3 reception, the maximum - 300 mg / day for 4-12 weeks, including the time of gradual withdrawal of the drug. In the elderly and patients with renal insufficiency dose reduced by 2 times.

Precautions substance Tofisopam
When an allergic reaction or severe sleep disorders should be discontinued. For the prevention of sleep disorders is recommended to take the drug last time no later than 15-16 hours.

It should be noted that patients with mental retardation, elderly patients, as well as having disorders of the kidneys and / or liver disease, are more likely than other patients may experience side effects.

Not recommended for use Tofisopam with chronic psychosis, phobias or obsessive-compulsive disorder. In these cases, the risk of suicide attempts and aggressive behavior. Therefore Tofisopam not recommended as monotherapy depression or depression accompanied by anxiety.

Care should be taken when treating patients with depersonalization, and organic brain damage (such as atherosclerosis). Permanent medical supervision is required when administered to patients with myasthenia gravis.

In patients with epilepsy Tofisopam may increase the seizure threshold.

Tofisopam does not significantly reduce the ability to concentrate. The question of the means of transport management capabilities solved after assessing the patient's individual response to the drug.

Trading names of drugs with Tofisopam working substance

Trade Name Index 

Grandaxin, Tofisopam