Alprazolam is a drug belonging to the benzodiazepine family, a subclass of triazolbenzodiazepines, characterized by the incorporation of a triazole ring to the benzodiazepine base. This structural variant gives Alprazolam distinctive pharmacological properties, such as greater potency of action than its counterparts (Diazepam, Oxazepam, Chlordiazepoxide) and a much shorter elimination half-life, since the metabolites produced by its biodegradation are short-lived and they do not prolong the duration of the effects of the drug. This gives Alprazolam a safe and reliable use, without cumulative risks. Alprazolam binding sites are found in abundance in the frontal and/or occipital cortex, with fewer in the hypothalamus, striatum, and medulla.
The effects of Alprazolam are linked to a specific agonist action on a central receptor that is part of the "GABA-OMEGA macromolecular receptors" complex (also dominated by BZD1 and BZD2) that modulates the opening of the chloride channel.
After reaching the systemic circulation, Alprazolam is transported to the capillary circulation in the brain, where it passively diffuses extracellular water from brain tissue. The degree to which alprazolam binds to the specific benzodiazepine receptor complex depends on the absolute concentration of the drug in the whole brain.
The binding of benzodiazepines to the receptor facilitates the binding and action of the endogenous neurotransmitter GABA. In other words, benzodiazepine agonists increase the binding of GABA to the receptor complex. The reverse is also true: the presence of GABA increases the binding of benzodiazepines.
Activation of this receptor produces an increase in the permeability of the cell membrane to chloride ions. The entry of chloride ions into the cell is increased, the degree of electrical polarization across the cell membrane increases, and the cell becomes more resistant to depolarization. The functional result is the characteristic "sedative" effect of benzodiazepine agonists, observed clinically in humans as well as intact experimental animals.
Clinically available benzodiazepines differ widely in their affinity for the benzodiazepine receptor. For "high affinity" ones, such as Alprazolam, relatively small molar amounts are required to produce a given degree of receptor occupancy compared to "low affinity" benzodiazepines. Differences in receptor affinity are reflected in corresponding differences in therapeutic dosage range. The only possible exception to this general rule is that Alprazolam has been reported to produce an "up ratio" of receptors (increase in the number of receptors) when brain concentrations are below the range usually found in humans. The significance of these findings has not been established, although they could be linked to some typical clinical features of alprazolam.
Clinical experience indicates that Alprazolam 1.5 to 2 mg daily is comparable in efficacy to Diazepam 15-20 mg daily in anxious outpatients, while initial studies in both depressed and anxious patients suggest that Alprazolam is comparable. to imipramine in this group.
Alprazolam, like tricyclic antidepressants, is capable of preventing the increase in the density of beta-adrenergic receptors after reserpine administration, which does not happen with other non-antidepressant benzodiazepines. Also, Alprazolam is similar to tricyclic antidepressants and MAOIs in its ability to increase REM latency as a function of dose, an effect that other benzodiazepines do not have. The preferential indications of Alprazolam are anxiety states, somatic components of anxiety, panic states and anxious depressions.
ACTIVE INGREDIENT
ALPRAZOLAM 0.25MG
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