Farmapram (alprazolam) is an anxiolytic, benzodiazepine derivative. The spectrum of action of benzodiazepines is traditionally divided into several main effects: anxiolytic (anti-anxiety), sedative, hypnotic, muscle relaxant, anticonvulsant and amnesic. Currently, their anxiolytic and hypnotic effects are the most important for clinical practice, while the others are hardly used or considered as side effects. Farmapram a typical representative of benzodiazepine anxiolytics, has all the properties of the drugs of this group to varying degrees. The main for it is anxiolytic action. Alprazolam belongs to high-potency benzodiazepines, i.e. a pronounced anxiolytic effect develops when using low doses of the drug. This is explained by the fact that alprazolam has a higher affinity for specific benzodiazepine receptors.
A potent agent. Alprazolam has anxiolytic, central myorelaxant, anticonvulsant, sedative-hypnotic and antipanic effects. It has a depressant effect on the central nervous system (CNS), which is realized mainly in the thalamus, hypothalamus and limbic system. It enhances inhibitory effect of gamma-aminobutyric acid (GABA), which is one of the main mediators of pre- and postsynaptic inhibition of nerve impulse transmission in CNS.
The mechanism of action of alprazolam is determined by stimulation of benzodiazepine receptors of supramolecular GABA-benzodiazepine-chlorionophore receptor complex, resulting in activation of GABA receptor, causing reduction of excitability of subcortical structures of the brain, inhibition of polysynaptic spinal reflexes. After oral administration it is rapidly absorbed from the gastrointestinal tract. Cmax is reached after 1-2 hours. Binding to plasma proteins is 80%. It passes through the HEB and the placental barrier, penetrates into breast milk. It is metabolized in the liver. T1/2 is 16 hours. It is mainly excreted by the kidneys. Repeated administration at intervals of less than 8-12 hours may lead to cumulation.
Anxiolytic effect is manifested by reduction of emotional tension, easing of symptoms of anxiety, fear. Expressed anxiolytic activity is combined with moderate soporific action; it shortens the period of falling asleep, increases the duration of sleep, reduces the number of nocturnal awakenings. The mechanism of hypnotic action is inhibition of the reticular formation cells of the brain stem. It reduces the impact of emotional, vegetative and motor stimuli that disturb the mechanism of falling asleep.
It is used for anxiety states and neurosis with anxiety, tension, restlessness, irritability, worsening of sleep, somatic disorders. Anxiety associated with depression (as part of complex therapy). Panic disorders (treatment). Tremor (senile, essential). Insomnia.