PsychonautWiki Archive

Benzodiazepines: Difference between revisions

← Older editNewer edit →
>Unity
Standardize section to 'Medical uses' and expand.
>Unity
Use BenzoWarning and DangerousIntro template. Make 'Chemical classes' section as subsection of 'Chemistry'. 'Preparation methods' over 'Medical uses'.
Line 6: Line 6:
The characteristic effects of benzodiazepines include [[anxiety suppression]], [[sedation]], [[muscle relaxation]], [[disinhibition]], [[sleepiness]] and [[amnesia]]. In a medical context, short-acting benzodiazepines are typically recommended for treating insomnia or acute anxiety or panic attack disorders while long-acting ones are recommended for the treatment of generalized anxiety disorders.
The characteristic effects of benzodiazepines include [[anxiety suppression]], [[sedation]], [[muscle relaxation]], [[disinhibition]], [[sleepiness]] and [[amnesia]]. In a medical context, short-acting benzodiazepines are typically recommended for treating insomnia or acute anxiety or panic attack disorders while long-acting ones are recommended for the treatment of generalized anxiety disorders.


It is worth noting that [[Benzodiazepine#Discontinuation|the sudden discontinuation of benzodiazepines]] can be potentially dangerous or life-threatening for individuals that develop a physical dependence on them after using them regularly for extended periods of time, which can result in potentially fatal seizures.<ref>A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812</ref> For this reason, 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 one's usage 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>
{{BenzoWarning}}


==History==
==History==
Line 29: Line 29:
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 substituted rings contain a ketone oxygen bond at R<sub>2</sub> of their benzodiazepine structure and are distinguished by their suffix "-azepam."
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 substituted rings contain a ketone oxygen bond at R<sub>2</sub> of their benzodiazepine structure and are distinguished by their suffix "-azepam."


==Pharmacology==
===Chemical classes===
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 [[receptor]]s.<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 benzodiazepines 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>
 
==Subjective effects==
{{Preamble/SubjectiveEffects}} These effects are listed and defined in detail within their own dedicated articles below:
{{effects/base
 
|{{effects/physical|
*'''[[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.
*'''[[Effect::Muscle relaxation]]'''
*'''[[Effect::Physical euphoria]]'''
*'''[[Effect::Motor control loss]]'''
*'''[[Effect::Seizure suppression]]'''<ref>Henriksen, O. (1998) ‘An overview of Benzodiazepines in seizure management’, Epilepsia, 39(SUPPL. 1), pp. 2–6. doi: 10.1111/j.1528-1157.1998.tb02601.x.</ref>
*'''[[Effect::Respiratory depression]]'''
*'''[[Effect::Dizziness]]'''
 
}}
{{effects/paradoxical|
 
Paradoxical reactions to [[benzodiazepines]] such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).<ref>http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review</ref><ref>Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf</ref><p>
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.<ref>Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs</ref><ref>Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev</ref></p>
 
}}
|{{effects/cognitive|
*'''[[Effect::Anxiety suppression]]'''
*'''[[Effect::Disinhibition]]'''
*'''[[Effect::Cognitive euphoria]]''' - This effect is not consistently produced between individuals and seems to be highly dependent on personal factors. Some people do not report any euphoric effects following benzodiazepine use. When it does occur, it is typically described as mild to moderate and is commonly thought to occur at a higher rate in those with pre-existing [[anxiety]] issues. This may partly be the result of the immediateness in which the anxiety-relieving and disinhibiting effects are produced. While this effect may not be entirely consistent, many reports suggest that certain benzodiazepines are more reliable and effective at producing euphoria over others. <ref>https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3684331/ | Benzodiazepine Pharmacology and Central Nervous System–Mediated Effects</ref>
*'''[[Effect::Memory suppression]]'''
**'''[[Effect::Amnesia]]'''
*'''[[Effect::Information processing suppression]]'''
*'''[[Effect::Thought deceleration]]'''
*'''[[Effect::Emotion suppression]]''' - Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but less intensive than that of [[antipsychotic]]s.
*'''[[Effect::Delusions|Delusions of sobriety]]''' - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others. It most commonly occurs at heavy dosages.
*'''[[Effect::Compulsive redosing]]'''
*'''[[Dream potentiation]]'''
 
}}
{{effects/aftereffects|
 
*'''[[Effect::Anxiety|Rebound anxiety]]''' - Rebound anxiety is a commonly observed effect with [[anxiety suppression|anxiety relieving]] substances like [[benzodiazepines]]. It typically corresponds to the total duration spent under the substance's influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction.
*'''[[Effect::Dream potentiation]]'''<ref>Goyal, Sarita. "Drugs and Dreams." Indian Journal of Clinical Practice (n.d.): n. pag. Web.  | http://medind.nic.in/iaa/t13/i3/iaat13i3p624.pdf</ref> or '''[[Effect::Dream suppression]]'''
*'''[[Effect::Sleepiness|Residual sleepiness]]''' - While benzodiazepines can be used as an effective [[hypnotic|sleep-inducing]] aid, their effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours.
*'''[[Effect::Thought deceleration]]'''
*'''[[Effect::Thought disorganization]]'''
*'''[[Effect::Irritability]]'''
 
}}
 
}}
 
==Pharmacological classes==
<div class="flex-panel">
<div class="flex-panel">
     <div class="flex-column">
     <div class="flex-column">
Line 158: Line 106:
</div>
</div>
</div>
</div>




Line 181: Line 127:


</div>
</div>
==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 [[receptor]]s.<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 benzodiazepines 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>
==Subjective effects==
{{Preamble/SubjectiveEffects}} These effects are listed and defined in detail within their own dedicated articles below:
{{effects/base
|{{effects/physical|
*'''[[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.
*'''[[Effect::Muscle relaxation]]'''
*'''[[Effect::Physical euphoria]]'''
*'''[[Effect::Motor control loss]]'''
*'''[[Effect::Seizure suppression]]'''<ref>Henriksen, O. (1998) ‘An overview of Benzodiazepines in seizure management’, Epilepsia, 39(SUPPL. 1), pp. 2–6. doi: 10.1111/j.1528-1157.1998.tb02601.x.</ref>
*'''[[Effect::Respiratory depression]]'''
*'''[[Effect::Dizziness]]'''
}}
{{effects/paradoxical|
Paradoxical reactions to [[benzodiazepines]] such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).<ref>http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review</ref><ref>Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf</ref><p>
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.<ref>Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs</ref><ref>Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev</ref></p>
}}
|{{effects/cognitive|
*'''[[Effect::Anxiety suppression]]'''
*'''[[Effect::Disinhibition]]'''
*'''[[Effect::Cognitive euphoria]]''' - This effect is not consistently produced between individuals and seems to be highly dependent on personal factors. Some people do not report any euphoric effects following benzodiazepine use. When it does occur, it is typically described as mild to moderate and is commonly thought to occur at a higher rate in those with pre-existing [[anxiety]] issues. This may partly be the result of the immediateness in which the anxiety-relieving and disinhibiting effects are produced. While this effect may not be entirely consistent, many reports suggest that certain benzodiazepines are more reliable and effective at producing euphoria over others. <ref>https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3684331/ | Benzodiazepine Pharmacology and Central Nervous System–Mediated Effects</ref>
*'''[[Effect::Memory suppression]]'''
**'''[[Effect::Amnesia]]'''
*'''[[Effect::Information processing suppression]]'''
*'''[[Effect::Thought deceleration]]'''
*'''[[Effect::Emotion suppression]]''' - Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but less intensive than that of [[antipsychotic]]s.
*'''[[Effect::Delusions|Delusions of sobriety]]''' - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others. It most commonly occurs at heavy dosages.
*'''[[Effect::Compulsive redosing]]'''
*'''[[Dream potentiation]]'''


}}
{{effects/aftereffects|
*'''[[Effect::Anxiety|Rebound anxiety]]''' - Rebound anxiety is a commonly observed effect with [[anxiety suppression|anxiety relieving]] substances like [[benzodiazepines]]. It typically corresponds to the total duration spent under the substance's influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction.
*'''[[Effect::Dream potentiation]]'''<ref>Goyal, Sarita. "Drugs and Dreams." Indian Journal of Clinical Practice (n.d.): n. pag. Web.  | http://medind.nic.in/iaa/t13/i3/iaat13i3p624.pdf</ref> or '''[[Effect::Dream suppression]]'''
*'''[[Effect::Sleepiness|Residual sleepiness]]''' - While benzodiazepines can be used as an effective [[hypnotic|sleep-inducing]] aid, their effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours.
*'''[[Effect::Thought deceleration]]'''
*'''[[Effect::Thought disorganization]]'''
*'''[[Effect::Irritability]]'''
}}
}}
==Equivalent dosages==
==Equivalent dosages==
The dosages below represent approximate equivalent dosages between various benzodiazepines in comparison to 10mg of [[diazepam]].
The dosages below represent approximate equivalent dosages between various benzodiazepines in comparison to 10mg of [[diazepam]].
Line 283: Line 278:
</div>
</div>
</div>
</div>
==Preparation methods==
*'''[[Volumetric liquid dosing]]''' - If one's benzodiazepines are in powder form, they are unlikely to weigh out accurately without the most expensive of scales due to their extreme potency. To avoid this, one can dissolve the benzodiazepine volumetrically into a solution and dose it accurately based upon the methodological instructions linked within this tutorial [[Volumetric liquid dosing|here]].


==Medical uses==
==Medical uses==
Line 308: Line 306:


===Dangerous interactions===
===Dangerous interactions===
{{DangerousInteractions/Intro}}
{{DangerousInteractions/Depressants}}
{{DangerousInteractions/Depressants}}
==Preparation methods==
*'''[[Volumetric liquid dosing]]''' - If one's benzodiazepines are in powder form, they are unlikely to weigh out accurately without the most expensive of scales due to their extreme potency. To avoid this, one can dissolve the benzodiazepine volumetrically into a solution and dose it accurately based upon the methodological instructions linked within this tutorial [[Volumetric liquid dosing|here]].


==See also==
==See also==
Retrieved from "http://psy.st/wiki/Benzodiazepines"