Benzodiazepines: Difference between revisions

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[[File:Benzodiazepine1.png|227px|thumb|right|The core structure of benzodiazepines]]

[[File:Xanax (alprazolam) 2 mg.jpg|200px|thumbnail|[[Xanax]] (alprazolam) 2 mg tri-score tablets]]

'''Benzodiazepines''' (also referred to as '''benzos''') are psychoactive ~~drugs~~ that act as central nervous system [[depressants]]. These ~~drugs~~ work by magnifying the efficiency and effects of the neurotransmitter 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> The prominent effects of benzodiazepines include [[anxiety suppression]], [[sedation]], [[muscle relaxation]], [[disinhibition]], [[sleepiness]] and [[amnesia]]. Short-acting benzodiazepines are recommended for treating insomnia while long-acting ones are recommended for the treatment of anxiety disorders.

'''Benzodiazepines''' (also referred to as '''benzos''') are psychoactive substances that act as central nervous system [[depressants]]. These substances work by magnifying the efficiency and effects of the neurotransmitter 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> The prominent effects of benzodiazepines include [[anxiety suppression]], [[sedation]], [[muscle relaxation]], [[disinhibition]], [[sleepiness]] and [[amnesia]]. Short-acting benzodiazepines are recommended for treating insomnia while long-acting ones are recommended for the treatment of anxiety disorders.

It's worth noting that [[Benzodiazepine#Discontinuation|the 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>

==Chemistry==

Benzodiazepine is a heterocyclic compound comprised of a benzene ring fused to a seven member nitrogenous diazepine ring. Benzodiazepine ~~drugs~~ contain an additional substituted phenyl ring bonded at R5, resulting in 5-phenyl-1,4-benzodiazepines with different side groups attached to the structure to create a number of ~~drugs~~ with different strength, duration and efficacy.

Benzodiazepine is a heterocyclic compound comprised of a benzene ring fused to a seven member nitrogenous diazepine ring. Benzodiazepine substances contain an additional substituted phenyl ring bonded at R5, resulting in 5-phenyl-1,4-benzodiazepines with different side groups attached to the structure to create a number of substances with different strength, duration and efficacy.

Benzodiazepine ~~drugs~~ commonly contain an aromatic electrophilic substitution such as aromatic halogenation or nitration on R7 of their rings. Benzodiazepines can be subdivided into triazolobenzodiazepines and ketone substituted benzodiazepines. Triazolobenzodiazepines contain a triazole ring bonded to the benzodiazepine structure and are distinguished by the suffix "-zolam." Ketone subsituted rings contain a ketone oxygen bond at R2 of their benzodiazepine structure and are distinguished by their suffix "-azepam."

Benzodiazepine substances commonly contain an aromatic electrophilic substitution such as aromatic halogenation or nitration on R7 of their rings. Benzodiazepines can be subdivided into triazolobenzodiazepines and ketone substituted benzodiazepines. Triazolobenzodiazepines contain a triazole ring bonded to the benzodiazepine structure and are distinguished by the suffix "-zolam." Ketone subsituted rings contain a ketone oxygen bond at R2 of their benzodiazepine structure and are distinguished by their suffix "-azepam."

==Pharmacology==

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*'''[[Thought deceleration]]'''

*'''[[Seizure suppression]]'''

*'''[[Effect::Sedation]]''' - In terms of energy level alterations, these ~~drugs~~ have the potential to be extremely sedating and this often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.

*'''[[Effect::Sedation]]''' - In terms of energy level alterations, these substances have the potential to be extremely sedating and this often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.

</li>

</ul>

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==Toxicity and harm potential==

[[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.<ref>Development of a rational scale to assess the harm of ~~drugs~~ of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644</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>Development of a rational scale to assess the harm of substances of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644</ref>]]

Benzodiazepines have a [[Toxicity::low toxicity]] relative to dose.<ref>Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614</ref> However, they are [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[opioids]]]].

@@ Line 2: / Line 2: @@
 [[File:Benzodiazepine1.png|227px|thumb|right|The core structure of benzodiazepines]]
 [[File:Xanax (alprazolam) 2 mg.jpg|200px|thumbnail|[[Xanax]] (alprazolam) 2 mg tri-score tablets]]
-'''Benzodiazepines''' (also referred to as '''benzos''') are psychoactive drugs that act as central nervous system [[depressants]]. These drugs work by magnifying the efficiency and effects of the neurotransmitter 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> The prominent effects of benzodiazepines include [[anxiety suppression]], [[sedation]], [[muscle relaxation]], [[disinhibition]], [[sleepiness]] and [[amnesia]]. Short-acting benzodiazepines are recommended for treating insomnia while long-acting ones are recommended for the treatment of anxiety disorders.
+'''Benzodiazepines''' (also referred to as '''benzos''') are psychoactive substances that act as central nervous system [[depressants]]. These substances work by magnifying the efficiency and effects of the neurotransmitter 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> The prominent effects of benzodiazepines include [[anxiety suppression]], [[sedation]], [[muscle relaxation]], [[disinhibition]], [[sleepiness]] and [[amnesia]]. Short-acting benzodiazepines are recommended for treating insomnia while long-acting ones are recommended for the treatment of anxiety disorders.
 It's worth noting that [[Benzodiazepine#Discontinuation|the 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>
 ==Chemistry==
-Benzodiazepine is a heterocyclic compound comprised of a benzene ring fused to a seven member nitrogenous diazepine ring. Benzodiazepine drugs contain an additional substituted phenyl ring bonded at R<sub>5</sub>, resulting in 5-phenyl-1,4-benzodiazepines with different side groups attached to the structure to create a number of drugs with different strength, duration and efficacy.
+Benzodiazepine is a heterocyclic compound comprised of a benzene ring fused to a seven member nitrogenous diazepine ring. Benzodiazepine substances contain an additional substituted phenyl ring bonded at R<sub>5</sub>, resulting in 5-phenyl-1,4-benzodiazepines with different side groups attached to the structure to create a number of substances with different strength, duration and efficacy.
-Benzodiazepine drugs commonly contain an aromatic electrophilic substitution such as aromatic halogenation or nitration on R<sub>7</sub> of their rings. Benzodiazepines can be subdivided into triazolobenzodiazepines and ketone substituted benzodiazepines. Triazolobenzodiazepines contain a triazole ring bonded to the benzodiazepine structure and are distinguished by the suffix "-zolam." Ketone subsituted rings contain a ketone oxygen bond at R<sub>2</sub> of their benzodiazepine structure and are distinguished by their suffix "-azepam."
+Benzodiazepine substances commonly contain an aromatic electrophilic substitution such as aromatic halogenation or nitration on R<sub>7</sub> of their rings. Benzodiazepines can be subdivided into triazolobenzodiazepines and ketone substituted benzodiazepines. Triazolobenzodiazepines contain a triazole ring bonded to the benzodiazepine structure and are distinguished by the suffix "-zolam." Ketone subsituted rings contain a ketone oxygen bond at R<sub>2</sub> of their benzodiazepine structure and are distinguished by their suffix "-azepam."
 ==Pharmacology==
@@ Line 36: / Line 36: @@
 *'''[[Thought deceleration]]'''
 *'''[[Seizure suppression]]'''
-*'''[[Effect::Sedation]]''' -  In terms of energy level alterations, these drugs have the potential to be extremely sedating and this often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
+*'''[[Effect::Sedation]]''' -  In terms of energy level alterations, these substances have the potential to be extremely sedating and this often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
 				</li>
 			</ul>
@@ Line 279: / Line 279: @@
 ==Toxicity and harm potential==
-[[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.<ref>Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644</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>Development of a rational scale to assess the harm of substances of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644</ref>]]
 Benzodiazepines have a [[Toxicity::low toxicity]] relative to dose.<ref>Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614</ref>  However, they are [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[opioids]]]].