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Alprazolam: Difference between revisions
>Discount Pharmacologist Chemistry and pharmacology info added |
>Jubba m Corrected small typo - "he" to "The". Changed the word "Depolarization" (originally "Depolarisation") to the more common English spelling with a "z" in place of the "s". |
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Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter [[GABA|gamma aminobutyric acid (GABA)]] by acting on its [[receptors]].<ref>Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796</ref> Alprazolam is a positive allosteric modulator of the gamma-aminobutyric acid (GABA) type A receptor. As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the [[sedating]] (or [[anxiety suppression|calming effects]]) of alprazolam on the nervous system. The [[anticonvulsant]] properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.<ref>Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2450203</ref> | Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter [[GABA|gamma aminobutyric acid (GABA)]] by acting on its [[receptors]].<ref>Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796</ref> Alprazolam is a positive allosteric modulator of the gamma-aminobutyric acid (GABA) type A receptor. As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the [[sedating]] (or [[anxiety suppression|calming effects]]) of alprazolam on the nervous system. The [[anticonvulsant]] properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.<ref>Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2450203</ref> | ||
Alprazolam causes a marked suppression of the hypothalamic pituitary-adrenal axis. Administration of alprazolam has been demonstrated to elicit an increase in striatal [[dopamine]] concentrations.<ref>Role of dopaminergic and serotonergic systems on behavioral stimulatory effects of low-dose alprazolam and lorazepam (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/11226811</ref> This results in effects including reduced anxiety, muscle relaxant, antidepressant and anticonvulsant activity. | Alprazolam causes a marked suppression of the hypothalamic pituitary-adrenal axis. Administration of alprazolam has been demonstrated to elicit an increase in striatal [[dopamine]] concentrations.<ref>Role of dopaminergic and serotonergic systems on behavioral stimulatory effects of low-dose alprazolam and lorazepam (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/11226811</ref> This results in effects including reduced anxiety, muscle relaxant, antidepressant and anticonvulsant activity. The GABA chemical and receptor system mediates inhibitory or calming effects of alprazolam on the nervous system. Binding of alprazolam to the GABA<sub>A</sub> receptor, a chloride ion channel, enhances the effects of GABA, a neurotransmitter. When GABA binds the GABA<sub>A</sub> receptor the channel opens and chloride enters the cell which makes it more resistant to depolarization. Therefore, alprazolam has a depressant effect on synaptic transmission to reduce anxiety.<ref>Andrew, Hitchings (2014). ''Top 100 drugs : clinical pharmacology and practical prescribing''. Lonsdale, Dagan,, Burrage, Daniel,, Baker, Emma. Edinburgh. ISBN <bdi>9780702055164</bdi>. OCLC 864676781.</ref> | ||
The GABA<sub>A</sub> receptor is made up of 5 subunits out of a possible 19, and GABA<sub>A</sub> receptors made up of different combinations of subunits have different properties, different locations within the brain, and, importantly, different activities with regard to benzodiazepines. Alprazolam and other triazolobenzodiazepines such as triazolam that have a triazole ring fused to their diazepine ring appear to have antidepressant properties.<ref>Barbee JG (October 1993). "Memory, benzodiazepines, and anxiety: integration of theoretical and clinical perspectives". ''The Journal of Clinical Psychiatry''. 54 Suppl (Suppl): 86–97, discussion 98–101. <nowiki>PMID 8262893</nowiki>.</ref> This is perhaps due to the similarities shared with tricyclic antidepressants, as they have two benzene rings fused to a diazepine ring. Alprazolam causes a marked suppression of the hypothalamic-pituitary-adrenal axis. The therapeutic properties of alprazolam are similar to other benzodiazepines and include anxiolytic, anticonvulsant, muscle relaxant, hypnotic and amnesic; however, it is used mainly as an anxiolytic. | The GABA<sub>A</sub> receptor is made up of 5 subunits out of a possible 19, and GABA<sub>A</sub> receptors made up of different combinations of subunits have different properties, different locations within the brain, and, importantly, different activities with regard to benzodiazepines. Alprazolam and other triazolobenzodiazepines such as triazolam that have a triazole ring fused to their diazepine ring appear to have antidepressant properties.<ref>Barbee JG (October 1993). "Memory, benzodiazepines, and anxiety: integration of theoretical and clinical perspectives". ''The Journal of Clinical Psychiatry''. 54 Suppl (Suppl): 86–97, discussion 98–101. <nowiki>PMID 8262893</nowiki>.</ref> This is perhaps due to the similarities shared with tricyclic antidepressants, as they have two benzene rings fused to a diazepine ring. Alprazolam causes a marked suppression of the hypothalamic-pituitary-adrenal axis. The therapeutic properties of alprazolam are similar to other benzodiazepines and include anxiolytic, anticonvulsant, muscle relaxant, hypnotic and amnesic; however, it is used mainly as an anxiolytic. | ||