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Active ingredients
Tofizopam
Release form
Uncoated Tablets
Composition
Active ingredient: Tofizopam Concentration of active ingredient (mg): 50 mg
Pharmacological effect
Tranquilizer. A drug from the group of benzodiazepine derivatives (an atypical benzodiazepine derivative). It has an anxiolytic effect, almost not accompanied by a sedative, muscle relaxant, anticonvulsant effect. Is a psycho-vegetative regulator, eliminates various forms of autonomic disorders. It has a moderate stimulating activity. Due to the lack of muscle relaxant effect, the drug can be used in patients with myopathy and myasthenia. Due to the atypical nature of the chemical structure, in contrast to the classical benzodiazepine derivatives, Grandaxin does not potentiate the effect of alcohol in therapeutic doses and practically does not cause the development of physical, psychological dependence and syndrome cancellations. Grandaksin belongs to day tranquilizers.
Pharmacokinetics
AbsorptionAfter ingestion is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax in the blood plasma is reached within 2 hours, after that the plasma concentration decreases monoexponentially. Distribution Topophyzopam does not accumulate in the body. Metabolism Tofisopam metabolites do not have pharmacological activity. Excretion of T1 / 2 is 6-8 hours. Excreted mainly in urine (60-80% ) in the form of conjugates with glucuronic acid and to a lesser extent (about 30%) with feces.
Indications
Neuroses and neurosis-like states (conditions accompanied by emotional stress, autonomic disorders, moderate anxiety, apathy, diminished activity, obsessive feelings, reactive depression with moderately pronounced psychopathological symptoms; Disorder of mental adaptation (post-traumatic stress disorder); also in combination with hormonal drugs); Premenstrual syndrome; Cardialgia (as monotherapy and and in combination with other drugs); Alcohol withdrawal syndrome, Myasthenia gravis, myopathies, neurogenic muscle atrophy and other pathological states with secondary neurotic symptoms when contraindicated anxiolytics with marked myorelaxant effect.
Contraindications
hypersensitivity to the active or any other component of the drug or any other benzodiazepines; conditions accompanied by pronounced psychomotor agitation, aggressiveness or severe depression — decompensated respiratory failure; trimester of pregnancy and breastfeeding; respiratory arrest syndrome (in history); simultaneous use with tacrolimus, sirolimus, cyclosporin. angle-closure glaucoma, epilepsy, organic brain damage (for example, atherosclerosis h)
Precautionary measures
The drug should be prescribed with caution in case of decompensated chronic respiratory distress syndrome, a history of acute respiratory failure, angle-closure glaucoma, epilepsy, organic brain damage (for example, in atherosclerosis).
Use during pregnancy and lactation
Grandaksin is contraindicated for use in the first trimester of pregnancy and during lactation (breastfeeding).
Dosage and administration
The dosage regimen is set individually, taking into account the patient's condition, the clinical form of the disease and individual sensitivity to the drug. Adults appoint 50-100 mg (1-2 pills.) 1-3 times a day. With the occasional use can take 1 - 2 pills. The maximum daily dose of 300 mg. Elderly patients and patients with renal insufficiency reduce the daily dose by about 2 times.
Side effects
On the part of the gastrointestinal tract: loss of appetite, constipation, increased gas, nausea, dry mouth. In some cases, possible congestive jaundice. From the side of the central nervous system: there may be headache, insomnia, irritability, agitation. Sometimes there is confusion, seizures may occur in patients with epilepsy. Allergic reactions: exanthema, scarlet-like exanthema, itching. Musculoskeletal system: muscle tension, muscle pain.
Overdose
Symptoms: after taking the drug in high doses (50-120 mg / kg body weight), CNS functions may be suppressed: vomiting, confusion, coma, respiratory depression and / or epileptic seizures. Treatment: when expressed inhibition of the central nervous system functions, it is not recommended to cause vomiting, flush the stomach. The introduction of activated carbon helps to reduce the absorption of the drug.It is necessary to constantly monitor the basic physiological parameters and apply appropriate symptomatic therapy. When respiratory depression can be performed artificial respiration. The introduction of CNS stimulants is not recommended. Hypotension is best eliminated in / in the introduction of fluids and transfer the patient to the Trendelenburg position. If these measures do not restore normal blood pressure, you can enter dopamine or norepinephrine (norepinephrine). Dialysis and forced diuresis are not effective. In case of emergency, it is possible to use a specific benzodiazepine antagonist, flumazenil, but its use in overdose with tofisopam has not been clinically tested.
Interaction with other drugs
The simultaneous use of tacrolimus, sirolimus, cyclosporine and Grandaxin is contraindicated. plasma concentration of drugs that are metabolized by the participation isoenzyme CYP3A4, can be increased while taking a tofizopamom.Primenenie Grandaxinum with drugs that suppress the central nervous system (analgesics, general anesthetics, antidepressants, blockers of histamine H1-receptor, sedatives, hypnotics, antipsychotic drugs), enhances their effects (for example, sedation or respiratory depression). Hepatic enzyme inducers (ethanol, nicotine, barbiturates, antiepileptic media ) can increase the metabolism of tofisopam, which can lead to a decrease in its concentration in 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 the blood plasma. Some antihypertensive drugs ( clonidine, calcium channel blockers) can enhance the effects of Grandaxine. Beta-blockers can slow down the metabolism of tofisopam, but this effect does not have a clinical significance iya.Tofizopam while the use can increase the level of digoxin in plasma krovi.Benzodiazepiny, including tofizopam can affect the anticoagulant on the central nervous system.
special instructions
It should be borne in mind that in patients with mental retardation, elderly patients, patients with impaired renal and / or liver function more often than other patients, side effects may occur. It is not recommended to use tofisopam in chronic psychosis, phobias or obsessive states. In these cases, the risk of suicidal attempts and aggressive behavior increases. Therefore, Grandaxine is not recommended as a monotherapy for depression or depression, accompanied by anxiety. Care must be taken when treating patients with depersonalization, as well as with organic brain damage (for example, with atherosclerosis). In patients with epilepsy, tofisopam can increase the threshold of convulsive readiness. contains 92 mg of lactose, which should be considered in patients with lactose intolerance. The influence on the ability to drive vehicles and control mechanisms Grandaxin is essential but does not reduce attention and ability to concentrate.