Warning
This is an unofficial archive of PsychonautWiki as of 2025-08-11T15:14:44Z. Content on this page may be outdated, incomplete, or inaccurate. Please refer to the original page for the most up-to-date information.

Benzodiazepines: Difference between revisions

From PsychonautWiki Archive
Jump to navigation Jump to search
>Unity
Reworded to improve language economy and conform to style/grammar standards.
>Unity
Flexgrid. Some effects reordering.
Line 21: Line 21:
{{Preamble/SubjectiveEffects}} These effects are listed and defined in detail within their own dedicated articles below:
{{Preamble/SubjectiveEffects}} These effects are listed and defined in detail within their own dedicated articles below:


<div class='flex-panel'>
{{effects/base
    <div class='flex-column'>
<div class="panel radius">
<h3 class="panel-header">'''Physical effects''' [[File:Child.svg|x20px|right|link=]]</h3>


<ul class="featured-table">
|{{effects/physical|
<li class="featured list-item">


*'''[[Dizziness]]'''
*'''[[Effect::Muscle relaxation]]'''
*'''[[Motor control loss]]'''
*'''[[Effect::Physical euphoria]]'''
*'''[[Muscle relaxation]]'''
*'''[[Effect::Motor control loss]]'''
*'''[[Physical euphoria]]'''
*'''[[Effect::Seizure suppression]]'''{{citation needed}}
*'''[[Seizure suppression]]'''
*'''[[Effect::Respiratory depression]]'''
*'''[[Effect::Dizziness]]'''
*'''[[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 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.
</li>
</ul>
</div>


<div class="panel radius">
}}
<h3 class="panel-header">'''Paradoxical effects''' [[File:Fa-exclamation-circle.png|x20px|right|link=]]</h3>
{{effects/paradoxical|


<ul class="featured-table">
<li class="featured list-item">
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>
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>
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>
</li>
</ul>
</div>
</div>


<div class="flex-column">
}}
<div class="panel radius">
|{{effects/cognitive|
<h3 class="panel-header">'''Cognitive effects''' [[File:User.svg|x20px|right|link=]]</h3>
 
<ul class="featured-table">
<li class="featured list-item">
*'''[[Effect::Anxiety suppression]]'''
*'''[[Effect::Anxiety suppression]]'''
*'''[[Effect::Amnesia]]'''
*'''[[Effect::Compulsive redosing]]'''
*'''[[Effect::Disinhibition]]'''
*'''[[Effect::Disinhibition]]'''
*'''[[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>
*'''[[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::Information processing suppression]]'''
*'''[[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::Thought deceleration]]'''
*'''[[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::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::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.
</li>
*'''[[Effect::Compulsive redosing]]'''
</ul>
*'''[[Dream potentiation]]'''
</div>
 
</div>
}}
</div>
{{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==
==Pharmacological classes==

Revision as of 16:30, 14 June 2017

Fatal overdose may occur when benzodiazepines are combined with other depressants such as opiates, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

The core structure of benzodiazepines
Xanax (alprazolam) 2 mg tri-score tablets

Benzodiazepines (commonly referred to as benzos) are a class of psychoactive substances that act as central nervous system depressants. These substances work by magnifying the efficiency and effects of the principal inhibitory neurotransmitter gamma-aminobutyric acid (GABA) by binding to and acting on its receptors.[2]

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 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.[3] 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.[4]

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 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 substituted rings contain a ketone oxygen bond at R2 of their benzodiazepine structure and are distinguished by their suffix "-azepam."

Pharmacology

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors.[5] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or 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.[6]

Subjective effects

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠. These effects are listed and defined in detail within their own dedicated articles below:


Physical effects

Paradoxical effects

Cognitive effects

After effects


Pharmacological classes

Equivalent dosages

The dosages below represent approximate equivalent dosages between various benzodiazepines in comparison to 10mg of diazepam.

The authors of this table specifically state that their equivalents differ from those used by other authors and "are firmly based on clinical experience during switch-over to diazepam at the start of withdrawal programs but may vary between individuals."[13]

Prescription benzodiazepines Half-life (Hours)
[active metabolite]
Approx. equivalent
oral dosage (mg)
Predominant effect
(a= anxiolytic,
c= anticonvulsant,
h= hypnotic)
Alprazolam 6-12 0.5 a
Bromazepam 10-20 5-6 a
Chlordiazapoxide 5-30 [36-200] 25 a
Clobazam 12-60 20 a, c
Clonazepam 18-50 0.5 a, c
Clorazepate 20-179 [36-200] 15 a
Diazepam 20-100 [36-200] 10 a, h, c
Estazolam 10-24 1-2 h
Etizolam 4-12 1 a
Flunitrazepam 18-36 [36-200] 1 h
Flurazepam 40-250 15-30 h
Halazepam 14 [30-200] 20 a
Ketazolam 30-100 [36-200] 15-30 a
Loprazolam 6-12 1-2 h
Lorazepam 10-20 1 a
Lormetazepam 10-12 1-2 h
Medazepam 36-200 10 a
Nitrazepam 15-38 10 h
Nordazepam 36-200 10 a
Oxazepam 4-15 20 a
Prazepam 29-224 [36-200] 10-20 a
Quazepam 25-100 20 h
Temazepam 8-22 20 h
Triazolam 2 0.5 h
Research chemicals Half-life (Hours)
[active metabolite]
Approx. equivalent
oral dosage (mg)
Predominant effect
(a= anxiolytic,
c= anticonvulsant,
h= hypnotic)
Clonazolam ? 0.5 h
Deschloroetizolam ~9-20 6 a
Diclazepam ~120 1 a, h
Flubromazepam 106 4 h
Flubromazolam ? 0.25 h
Nifoxipam 4-6 2 a
Meclonazepam ? 5 a, c
Metizolam ~9-20 2 a
Phenazepam 60 1 a
Pyrazolam 17 1 a
Z-drugs Half-life (Hours)
[active metabolite]
Approx. equivalent
oral dosage (mg)
Predominant effect
(a= anxiolytic,
c= anticonvulsant,
h= hypnotic)
Zaleplon 2 20 h
Zolpidem 2 20 h
Zopiclone 5-6 15 h
Eszopiclone 6 3 h

Toxicity and harm potential

Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.[14]

Benzodiazepines have a low toxicity relative to dose.[15] However, they are [[Toxicity::potentially lethal when mixed with depressants like alcohol or opioids]].

It is strongly recommended that one use harm reduction practices when using this class of compounds.

Tolerance and addiction potential

Benzodiazepines are extremely physically and psychologically addictive.

Tolerance will develop to the sedative-hypnotic effects within a couple of days of continuous use.[16] After cessation, the tolerance returns to baseline in 7-14 days. Withdrawal symptoms or rebound symptoms may occur after ceasing one's usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.[17][18]

Discontinuation

Benzodiazepine discontinuation is notoriously difficult; it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of high blood pressure, seizures, and death.[19] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal. Abrupt discontinuation also causes rebound stimulation which presents as anxiety, insomnia and restlessness.

It is safest to reduce the dose each day by a very small amount, for a couple of weeks until close to abstinence. If using a short half-life benzodiazepine, a longer acting variety such as diazepam can be substituted. Symptoms may still be present, but their severity will be reduced significantly. For more information on tapering from benzodiazepines in a controlled manner, please see this guide. Small amounts of alcohol can also help to reduce the symptoms.

The duration and severity of withdrawal symptoms depends on a number of factors including the half-life of the drug used, tolerance and the duration of abuse. Major symptoms will usually start within just a few days after discontinuation and persist for around a week for shorter lasting benzodiazepines. Benzodiazepines with longer half-lives will exhibit withdrawal symptoms with a slow onset and extended duration.

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 here.

See also

References

  1. Risks of Combining Depressants - TripSit 
  2. Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796
  3. A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812
  4. 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
  5. Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796
  6. 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
  7. http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
  8. Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
  9. Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
  10. Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
  11. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3684331/ | Benzodiazepine Pharmacology and Central Nervous System–Mediated Effects
  12. Goyal, Sarita. "Drugs and Dreams." Indian Journal of Clinical Practice (n.d.): n. pag. Web. | http://medind.nic.in/iaa/t13/i3/iaat13i3p624.pdf
  13. BENZODIAZEPINE EQUIVALENCE TABLE | http://www.benzo.org.uk/bzequiv.htm
  14. Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  15. Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614
  16. Principles and Practice of Psychopharmacotherapy | http://books.google.com/books?id=_ePK9wwcQUMC&pg=PA535
  17. Clinical Pharmacology, Clinical Efficacy, and Behavioral Toxicity of Alprazolam: A Review of the Literature | http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00003.x/pdf
  18. The American Psychiatric Publishing Textbook of Substance Abuse Treatment | http://books.google.com/books?id=6wdJgejlQzYC&pg=PA222&hl=en#v=onepage&q&f=false
  19. A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812