Alprazolam: Difference between revisions

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==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]]) ~~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>

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 GABAA receptor, a chloride ion channel, enhances the effects of GABA, a neurotransmitter. When GABA binds the GABAA 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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It is strongly recommended that one use [[harm reduction practices]] when using this substance.

The acute oral [[LD50|LD50]] 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.

The acute oral [[LD50|LD50]] in rats is 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===

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*'''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}}

*'''Czechia''': Alprazolam is a Schedule IV <ref>https://eur-lex.europa.eu/resource.html?uri=cellar:6b5e9beb-1d9b-11ea-95ab-01aa75ed71a1.0001.02/DOC_1&format=PDF</ref> (List 7) substance. Sold on exclusively with a prescription "without a blue stripe" (§ 1, g), 1. of ''Nařízení vlády č. 463/2013 Sb.'') <ref>https://www.zakonyprolidi.cz/cs/2013-463</ref>

*'''Germany''': Alprazolam is controlled under Anlage III BtMG (''Narcotics Act, Schedule III'') as of August 1, 1986.<ref>{{cite web|url=http://www.bgbl.de/xaver/bgbl/start.xav?startbk=Bundesanzeiger_BGBl&jumpTo=bgbl186s1099.pdf|title=Zweite Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften|publisher=Bundesanzeiger Verlag|access-date=December 26, 2019|language=de}}</ref> It can only be prescribed on a narcotic prescription form, except preparations which contain up to 1 mg triazolam in each dosage form.<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html|title=Anlage III BtMG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 26, 2019|language=de}}</ref>

*'''Ireland''': Alprazolam is a Schedule 4 medicine.<ref>{{Citation | vauthors=((eISB)) | title=Misuse Of Drugs (Amendment) Regulations | url=https://www.irishstatutebook.ie/eli/1993/si/342/made/en/print}}</ref>

@@ Line 18: / Line 18: @@
 ==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]]) 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>
+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>
@@ Line 99: / Line 99: @@
 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 [[Tel:331–2171|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 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===
@@ Line 123: / Line 123: @@
 *'''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}}
+*'''Czechia''': Alprazolam is a Schedule IV <ref>https://eur-lex.europa.eu/resource.html?uri=cellar:6b5e9beb-1d9b-11ea-95ab-01aa75ed71a1.0001.02/DOC_1&format=PDF</ref> (List 7) substance. Sold on exclusively with a prescription "without a blue stripe" (§ 1, g), 1. of ''Nařízení vlády č. 463/2013 Sb.'') <ref>https://www.zakonyprolidi.cz/cs/2013-463</ref>
 *'''Germany''': Alprazolam is controlled under Anlage III BtMG (''Narcotics Act, Schedule III'') as of August 1, 1986.<ref>{{cite web|url=http://www.bgbl.de/xaver/bgbl/start.xav?startbk=Bundesanzeiger_BGBl&jumpTo=bgbl186s1099.pdf|title=Zweite Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften|publisher=Bundesanzeiger Verlag|access-date=December 26, 2019|language=de}}</ref> It can only be prescribed on a narcotic prescription form, except preparations which contain up to 1&nbsp;mg triazolam in each dosage form.<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html|title=Anlage III BtMG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 26, 2019|language=de}}</ref>
 *'''Ireland''': Alprazolam is a Schedule 4 medicine.<ref>{{Citation | vauthors=((eISB)) | title=Misuse Of Drugs (Amendment) Regulations | url=https://www.irishstatutebook.ie/eli/1993/si/342/made/en/print}}</ref>