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We can now highlight more full and helpful features for comprehending the clinical management of benzodiazepines and their therapeutic effects thanks to recent breakthroughs in pharmacological concepts.
The activation of 2 distinct receptors is necessary for the pharmacological effects of benzodiazepines. The peripheral benzodiazepine receptor, which has been discovered in periphery, is functionally and structurally distinct from the GABA-A receptor and is a component of the more complex structure that comprises receptors called GABA-A (gamma-aminobutyric acid). Stimulation of these structures increases neurotransmission GABAergic, with intense inhibitory and neuroendocrine effects.
Endozepines are a family of naturally occurring peptides that regulate a variety of biological activities, either centrally or peripherally. Synthetic compounds like benzodiazepines imitate (at least in part) the effects of these peptides. The adrenal-hypothalamic-pituitary axis is clearly inhibited by benzodiazepines, particularly Alprazolam. These effects appear to be mediated through the hypothalamic and suprahypothalamic pathways.
The fact that Alprazolam has such a strong inhibitory effect on these neural circuits accounts for its unique effectiveness in treating clinical conditions like panic and depression. Alprazolam’s therapeutic benefits can be more easily understood if one considers its capacity to inhibit or lessen CNS functions, with a precisely proportionate dose-effect connection, resulting in everything from anxiety lysis and drowsiness to deep hypnosis.
When taken orally, alprazolam is quickly absorbed and reaches its peak plasmatic levels between the first and second hours after consumption. 94% of it is bioavailable. Two hours prior to the Alprazolam dose, some high-fat foods may improve absorption. It is 80% protein bound and has a considerably varied volume of distribution in young and old males, but not in different-aged women. In comparison to control patients, the volume of dispersion is higher in obese subjects.
Alprazolam is primarily metabolized in the liver by hydroxylation catalyzed by cytochrome P450, which results in the production of four metabolites: alpha-hydroxyAlprazolam, which has a minimal activity of about half that of Alprazolam but does not contribute to its pharmacological effects, benzophenone, an inactive metabolite, desmethyl Alprazolam, and 4-hydroxyAlprazolam, which has less than a Alprazolam has an elimination half-life of 12 to 15 hours. In 80% of cases, it has a renal elimination; this diminishes in the elderly.