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Alprazolam: Difference between revisions
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==Pharmacology== | ==Pharmacology== | ||
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>{{cite journal | vauthors=((Haefely, W.)) | journal=Neuroscience Letters | title=Benzodiazepine interactions with GABA receptors | volume=47 | issue=3 | pages=201–206 | date=29 June 1984 | issn=0304-3940 | doi=10.1016/0304-3940(84)90514-7}}</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 | 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>{{cite journal | vauthors=((Haefely, W.)) | journal=Neuroscience Letters | title=Benzodiazepine interactions with GABA receptors | volume=47 | issue=3 | pages=201–206 | date=29 June 1984 | issn=0304-3940 | doi=10.1016/0304-3940(84)90514-7}}</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>{{cite journal | vauthors=((McLean, M. J.)), ((Macdonald, R. L.)) | journal=The Journal of Pharmacology and Experimental Therapeutics | title=Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture | volume=244 | issue=2 | pages=789–795 | date= February 1988 | issn=0022-3565}}</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 name="Bentue-Ferrer2001">{{cite journal | vauthors=((Bentué-Ferrer, D.)), ((Reymann, J. M.)), ((Tribut, O.)), ((Allain, H.)), ((Vasar, E.)), ((Bourin, M.)) | journal=European Neuropsychopharmacology: The Journal of the European College of Neuropsychopharmacology | title=Role of dopaminergic and serotonergic systems on behavioral stimulatory effects of low-dose alprazolam and lorazepam | volume=11 | issue=1 | pages=41–50 | date= February 2001 | issn=0924-977X | doi=10.1016/s0924-977x(00)00137-1}}</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>{{cite book | vauthors=((Hitchings, A.)), ((Lonsdale, D.)), ((Burrage, D.)), ((Baker, E.)) | date= 2014 | title=Top 100 drugs: clinical pharmacology and practical prescribing | publisher=Churchill Livingstone | isbn=9780702055164}}</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 name="Bentue-Ferrer2001">{{cite journal | vauthors=((Bentué-Ferrer, D.)), ((Reymann, J. M.)), ((Tribut, O.)), ((Allain, H.)), ((Vasar, E.)), ((Bourin, M.)) | journal=European Neuropsychopharmacology: The Journal of the European College of Neuropsychopharmacology | title=Role of dopaminergic and serotonergic systems on behavioral stimulatory effects of low-dose alprazolam and lorazepam | volume=11 | issue=1 | pages=41–50 | date= February 2001 | issn=0924-977X | doi=10.1016/s0924-977x(00)00137-1}}</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>{{cite book | vauthors=((Hitchings, A.)), ((Lonsdale, D.)), ((Burrage, D.)), ((Baker, E.)) | date= 2014 | title=Top 100 drugs: clinical pharmacology and practical prescribing | publisher=Churchill Livingstone | isbn=9780702055164}}</ref> | ||
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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>{{cite journal | vauthors=((Barbee, J. G.)) | journal=The Journal of Clinical Psychiatry | title=Memory, benzodiazepines, and anxiety: integration of theoretical and clinical perspectives | volume=54 Suppl | pages=86–97; discussion 98-101 | date= October 1993 | issn=0160-6689}}</ref> This is perhaps due to the similarities shared with tricyclic antidepressants, as they have two benzene rings fused to a diazepine ring. 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>{{cite journal | vauthors=((Barbee, J. G.)) | journal=The Journal of Clinical Psychiatry | title=Memory, benzodiazepines, and anxiety: integration of theoretical and clinical perspectives | volume=54 Suppl | pages=86–97; discussion 98-101 | date= October 1993 | issn=0160-6689}}</ref> This is perhaps due to the similarities shared with tricyclic antidepressants, as they have two benzene rings fused to a diazepine ring. 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. | ||
Giving alprazolam, as compared to lorazepam, has been demonstrated to elicit a statistically significant increase in extracellular dopamine D1 and D2 concentrations in the striatum.<ref name="Bentue-Ferrer2001"/> | Giving alprazolam, as compared to lorazepam, has been demonstrated to elicit a statistically significant increase in extracellular dopamine D1 and D2 concentrations in the striatum.<ref name="Bentue-Ferrer2001" /> | ||
==Subjective effects== | ==Subjective effects== | ||
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{{toxicity}} | {{toxicity}} | ||
[[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.<ref>{{cite journal | vauthors=((Nutt, D.)), ((King, L. A.)), ((Saulsbury, W.)), ((Blakemore, C.)) | journal=The Lancet | title=Development of a rational scale to assess the harm of drugs of potential misuse | volume=369 | issue=9566 | pages=1047–1053 | date=24 March 2007 | url=https://www.sciencedirect.com/science/article/pii/S0140673607604644 | issn=0140-6736 | doi=10.1016/S0140-6736(07)60464-4}}</ref>]] | [[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.<ref>{{cite journal | vauthors=((Nutt, D.)), ((King, L. A.)), ((Saulsbury, W.)), ((Blakemore, C.)) | journal=The Lancet | title=Development of a rational scale to assess the harm of drugs of potential misuse | volume=369 | issue=9566 | pages=1047–1053 | date=24 March 2007 | url=https://www.sciencedirect.com/science/article/pii/S0140673607604644 | issn=0140-6736 | doi=10.1016/S0140-6736(07)60464-4}}</ref>]] | ||
Alprazolam has a [[Toxicity::low toxicity]] relative to dose.<ref name="Mandroili2008"/> However, it is [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[opioids]]]]. | Alprazolam has a [[Toxicity::low toxicity]] relative to dose.<ref name="Mandroili2008" /> However, it is [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[opioids]]]]. | ||
It is strongly recommended that one use [[harm reduction practices]] when using this substance. | It is strongly recommended that one use [[harm reduction practices]] when using this substance. | ||
The acute oral [[LD50|LD<sub>50</sub>]] in rats is 331–2171 mg/kg. Other experiments in animals have indicated that cardiopulmonary collapse can occur following massive intravenous doses of alprazolam. | The acute oral [[LD50|LD<sub>50</sub>]] in rats is [[Tel:331–2171|331–2171]] mg/kg. Other experiments in animals have indicated that cardiopulmonary collapse can occur following massive intravenous doses of alprazolam. | ||
===Dependence and abuse potential=== | ===Dependence and abuse potential=== | ||