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Alprazolam: Difference between revisions
>Dextromethorphan may need to be reworded, and a solid citation with statistic needed, but though this might have to be included |
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The [[Benzodiazepine#Discontinuation|sudden discontinuation of benzodiazepines]] can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death.<ref>A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812</ref> It is highly recommended to [[taper]] one's dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping abruptly.<ref>Canadian Guideline for Safe and Effective Use of Opioids for Chronic Non-Cancer Pain - Appendix B-6: Benzodiazepine Tapering | http://nationalpaincentre.mcmaster.ca/opioid/cgop_b_app_b06.html</ref> | The [[Benzodiazepine#Discontinuation|sudden discontinuation of benzodiazepines]] can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death.<ref>A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812</ref> It is highly recommended to [[taper]] one's dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping abruptly.<ref>Canadian Guideline for Safe and Effective Use of Opioids for Chronic Non-Cancer Pain - Appendix B-6: Benzodiazepine Tapering | http://nationalpaincentre.mcmaster.ca/opioid/cgop_b_app_b06.html</ref> | ||
[[File:Xanax (alprazolam) 2 mg.jpg|200px|thumbnail|Xanax (Alprazolam) 2 mg tri-score tablets]] | [[File:Xanax (alprazolam) 2 mg.jpg|200px|thumbnail|Xanax (Alprazolam) 2 mg tri-score tablets]] | ||
==Chemistry== | ==Chemistry== | ||
Alprazolam is a drug of the benzodiazepine class. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R<sub>1</sub> and R<sub>4</sub>. The benzyl ring of alprazolam is substituted at R<sub>8</sub> with a chlorine group. Further, the diazepine ring is bonded at R<sub>5</sub> to a phenyl ring. Alprazolam also contains a 1-methylated triazole ring fused to and incorporating R<sub>1</sub> and R<sub>2</sub> of its diazepine ring. Alprazolam belongs to a class of benzodiazepines containing this fused triazole ring, called triazolobenzodiazepines, distinguished by the suffix "-zolam". | Alprazolam is a drug of the benzodiazepine class. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R<sub>1</sub> and R<sub>4</sub>. The benzyl ring of alprazolam is substituted at R<sub>8</sub> with a chlorine group. Further, the diazepine ring is bonded at R<sub>5</sub> to a phenyl ring. Alprazolam also contains a 1-methylated triazole ring fused to and incorporating R<sub>1</sub> and R<sub>2</sub> of its diazepine ring. Alprazolam belongs to a class of benzodiazepines containing this fused triazole ring, called triazolobenzodiazepines, distinguished by the suffix "-zolam". | ||
Alprazolam is substituted with a phenyl group at position 6, with a chlorine atom at position 8 and with a methyl group at position 1. It is an analogue of triazolam, the difference between them being the absence of a chlorine atom in the 'ortho' position of the phenyl ring. It is soluble in alcohol and insoluble in water. | |||
==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>Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796</ref> 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. | 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. he 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 depolarisation. 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 | 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. | ||
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>Bentué-Ferrer D, Reymann JM, Tribut O, Allain H, Vasar E, Bourin M (February 2001). "Role of dopaminergic and serotonergic systems on behavioral stimulatory effects of low-dose alprazolam and lorazepam". ''European Neuropsychopharmacology''. '''11''' (1): 41–50. doi:10.1016/S0924-977X(00)00137-1. <nowiki>PMID 11226811</nowiki>. S2CID 24653686.</ref> | |||
==Subjective effects== | ==Subjective effects== | ||
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Additional experience reports can be found here: | Additional experience reports can be found here: | ||
* [https://www.erowid.org/experiences/subs/exp_Pharms_Alprazolam.shtml Erowid Experience Vaults: Alprazolam] | *[https://www.erowid.org/experiences/subs/exp_Pharms_Alprazolam.shtml Erowid Experience Vaults: Alprazolam] | ||
==Toxicity and harm potential== | ==Toxicity and harm potential== | ||
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==Legal status== | ==Legal status== | ||
Internationally, alprazolam is included under the United Nations Convention on Psychotropic Substances as Schedule IV.<ref>List of Psychotropic Substances under International Control | http://www.incb.org/documents/Psychotropics/green_lists/Green_list_ENG_2014_85222_GHB.pdf</ref> | Internationally, alprazolam is included under the United Nations Convention on Psychotropic Substances as Schedule IV.<ref>List of Psychotropic Substances under International Control | http://www.incb.org/documents/Psychotropics/green_lists/Green_list_ENG_2014_85222_GHB.pdf</ref> | ||
*'''Australia''': Alprazolam was originally a Schedule 4 (prescription only) medication; however, as of January 2014, it will become a Schedule 8 medication, subjecting it to more rigorous prescribing requirements.<ref>Alprazolam to be rescheduled from next year | http://www.australiandoctor.com.au/news/latest-news/alprazolam-to-be-rescheduled-from-next-year</ref> | *'''Australia''': Alprazolam was originally a Schedule 4 (prescription only) medication; however, as of January 2014, it will become a Schedule 8 medication, subjecting it to more rigorous prescribing requirements.<ref>Alprazolam to be rescheduled from next year | http://www.australiandoctor.com.au/news/latest-news/alprazolam-to-be-rescheduled-from-next-year</ref> | ||
*'''Austria''': Alprazolam is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).{{citation needed}} | *'''Austria''': Alprazolam is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).{{citation needed}} | ||
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==See also== | ==See also== | ||
*[[Responsible use]] | *[[Responsible use]] | ||
**[[Volumetric dosing]] | **[[Volumetric dosing]] | ||
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==External links== | ==External links== | ||
*[https://en.wikipedia.org/wiki/Alprazolam Alprazolam (Wikipedia)] | *[https://en.wikipedia.org/wiki/Alprazolam Alprazolam (Wikipedia)] | ||
*[https://erowid.org/pharms/alprazolam/alprazolam.shtml Alprazolam (Erowid Vault)] | *[https://erowid.org/pharms/alprazolam/alprazolam.shtml Alprazolam (Erowid Vault)] | ||
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==Further reading== | ==Further reading== | ||
*[https://www.benzo.org.uk/manual/index.htm The Ashton Manual] - Useful information on safe withdrawal from long-term benzodiazepine use and dependence | *[https://www.benzo.org.uk/manual/index.htm The Ashton Manual] - Useful information on safe withdrawal from long-term benzodiazepine use and dependence | ||