Properties
What is it?
Product General Characteristics 1. Medical Product Name Gamalate B6 coated tablets 2. Qualitative and Quantitative Composition Each coated tablet contains: - Magnesium glutamate hydrobromide (MGH) ................................................. 75 mg - γ-amino-butyric acid (GABA) ................................................................... 75 mg - γ-amino-β-hydroxybutyric acid (GABOB) ............................................ 37 mg - Pyridoxine hydrochloride ............................................................. 37 mg See section 6.1 for a list of excipients. 3. Pharmaceutical Formulation Coated tablets 4. Clinical Data 4.1 Therapeutic Indications Gamalate B6 belongs to the group of so-called psychostimulant and nootropic medications. Thanks to its active ingredients such as cerebrotonic amino acids (GABA and GABOB), mild sedative (MGH), and vitamin B6, Gamalate B6 has cerebro-energetic and neuro-regulatory effects. Amino acids and vitamin B6 participate in cerebral metabolism and increase the energy potential of nerve cells. It leads to an improvement in the quality of intellectual abilities. Indications as adjunctive therapy in functional asthenia: - Emotional instability. - Impaired concentration and memory. - Depression and nervous disorders. - Reduced adaptability. 4.2 Dosage and Method of Administration Posology Adults: 2 tablets, 2 or 3 times a day (every 12 or 8 hours). The duration of treatment is from 2 to 18 months. 4.3 Contraindications Hypersensitivity to the active substances or any of the excipients listed in section 6.1. Children and adolescents under 18 years of age. 4.4 Special Warnings and Precautions for Use Not known. 4.5 Interaction with Other Medicinal Products and Other Forms of Interaction Not known. 4.6 Pregnancy and Lactation The preparation is contraindicated during pregnancy and lactation. 4.7 Effects on Ability to Drive and Use Machines Due to the specific action of the preparation, caution is required when driving vehicles and operating potentially dangerous machinery. 4.8 Side Effects Symptoms of dyspepsia are possible. 4.9 Overdose Due to the low toxicity of the preparation, the risk of intoxication is low even in case of overdose. Symptoms: Worsening of side effects. Treatment: Symptomatic. 5. Pharmacological Properties 5.1 Pharmacodynamic Properties Pharmacotherapeutic group: Psychoanaleptics. Other psychostimulants and nootropic preparations. γ–aminobutyric acid (GABA) is formed from glutamic acid by the action of the enzyme glutamate decarboxylase (GAD) and primarily inhibits nervous excitability. It is metabolized in the brain via transamination and decarboxylation, converting to succinic acid and entering the Krebs cycle. Factors affecting GABA levels or its state in the brain significantly influence cerebral activity. GABA levels depend on the activity of decarboxylase in succinic acid, which is formed via GABA, and on transaminase, which eliminates GABA. Disturbances at the level of synaptic transmission manifest as states of hyper-excitability. In such circumstances, the levels of enzymes necessary for the conversion of glutamic acid to GABA decrease, resulting in decreased levels of glutamic acid and GABA, which are two major neurotransmitters. γ-amino-β-hydroxybutyric acid (GABOB) is a natural metabolic product and a structural precursor analog of GABA with neuromodulatory properties in the brain. It blocks excitatory synaptic terminals and modulates dopaminergic and GABAergic activity. α-amino magnesium glutamate hydrobromide (MGH) is a synthetic molecule. The main structural core of MGH is glutamic acid. It has been shown that based on its chemical structure, it has a mild sedative effect and anxiolytic activity. It acts as a partial agonist of L-glutamate and blocks its excitatory activity. Pyridoxine hydrochloride (vitamin B6) is a water-soluble vitamin involved in the conversion of glutamic acid to GABA. It plays an important role in the normal functioning of the central nervous system (CNS) and acts as a coenzyme factor in many neuronal processes. The pharmacological action of Gamalate B6 oral tablet is due to the complementary action of four components that increase the energy potential of nerve cells and also have a calming effect on their hyper-excitability, which contributes to the improvement of concentration and mental performance. Each constituent substance serves to maintain the physiological homeostasis of the central nervous system (CNS), and the purpose of combined administration is to potentiate these effects in cases where homeostasis is disturbed. GABA in Gamalate B6 ensures the correct concentration of GABA in the CNS and normalizes the biochemical processes involved in its metabolic production at the synaptic level in states of neuronal hyper-excitability; GABOB enhances the GABA-inhibitory function in the CNS; MGH helps reduce glutamate-induced excitation in the CNS by blocking its receptors, while vitamin B6 stimulates the metabolic conversion of glutamate to GABA and increases its activity. 5.2 Pharmacokinetic Properties Gamalate B6 oral tablet is well absorbed after oral administration. GABA is rapidly absorbed and crosses the blood-brain barrier. It is metabolized to succinic acid via transamination and decarboxylation and enters the Krebs cycle. Alternatively, GABA is metabolized to GABOB. GABOB has rapid oral absorption and crosses the blood-brain barrier. It is extensively metabolized and rapidly excreted in urine and saliva. Only about 1% of the dose is excreted in urine over 12 hours, confirming extensive metabolism. After oral absorption, MGH enters the bloodstream and is characterized by wide systemic distribution. Pyridoxine hydrochloride is rapidly absorbed from the gastrointestinal tract. Absorption is reduced in patients with malabsorption syndrome. It is not bound to plasma proteins. Its storage site is the liver, where it is converted to the active coenzymes pyridoxal 5´-phosphate and pyridoxamine phosphate. It is metabolized in the liver by oxidation, forming 4-pyridoxic acid and other inactive metabolites, which are excreted in the urine. The half-life is 15-20 days. It can be removed by hemodialysis. Pyridoxine crosses the placenta and is excreted in breast milk. 5.3 Preclinical Data on Safety The DL50 of Gamalate B6 coated tablets was investigated in albino rats weighing 20-25 g, which were administered a solution in distilled water via gastric cannula. A single dose of 5 g/kg did not affect mortality or signs of external toxicity at the time of administration and for 24, 48, and 72 hours after administration. Given that the maximum dose, equivalent to 22 g/kg of the preparation, was administered, it can be considered that the DL50 could not be determined in this animal model. 6. Pharmaceutical Data 6.1 List of Excipients Sucrose; anhydrous colloidal silica, polyvinylpyrrolidone (E-1201), sodium starch glycolate, magnesium stearate, talc (E-553b), corn starch, titanium dioxide (E-171), magnesium carbonate (E-504i), indigotine (E-132), Eudragit E, gum arabic (E414), propylene glycol (E-1520), carnauba wax (E-903). 6.2 Incompatibilities None observed. 6.3 Shelf Life 5 years. 6.4 Special Precautions for Storage Store at a temperature not exceeding 30 °C. 6.5 Nature and Contents of Packaging Blue round tablets, in blister packaging. The package contains 20 coated tablets. 6.6 Special Precautions for Disposal There are no special requirements for disposal. Dispensing category: Pharmaceutical product group III, available without prescription.