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A '''thienodiazepine''' is a heterocyclic compound containing a diazepine ring fused to a thiophene ring. The thienodiazepine ring structure forms the central core of several pharmaceutical drugs. Since thienodiazepines interact with the [[benzodiazepine]] receptor site, they typically have similar effects as benzodiazepines and can be considered as essentially identical.
A '''thienodiazepine''' is a heterocyclic compound containing a diazepine ring fused to a thiophene ring. The thienodiazepine ring structure forms the central core of several pharmaceutical drugs. Since thienodiazepines interact with the [[benzodiazepine]] receptor site, they typically have similar effects as benzodiazepines and can be considered as essentially identical.
Similar to [[benzodiazepines]], [[Thienodiazepine#Discontinuation|the sudden discontinuation of thienodiazepines]] can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. 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>
Similar to [[benzodiazepines]], [[Thienodiazepine#Discontinuation|the sudden discontinuation of thienodiazepines]] can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. 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>{{cite journal | vauthors=((Kahan, M.)), ((Wilson, L.)), ((Mailis-Gagnon, A.)), ((Srivastava, A.)) | journal=Canadian Family Physician | title=Canadian guideline for safe and effective use of opioids for chronic noncancer pain. Appendix B-6: Benzodiazepine Tapering | volume=57 | issue=11 | pages=1269–1276 | date= November 2011 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3215603/ | issn=0008-350X}}</ref>
==Subjective effects==
==Subjective effects==
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Paradoxical reactions to thienodiazepines, as well as [[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 thienodiazepines, as well as [[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>{{cite journal | vauthors=((Saïas, T.)), ((Gallarda, T.)) | journal=L’Encephale | title=[Paradoxical aggressive reactions to benzodiazepine use: a review] | volume=34 | issue=4 | pages=330–336 | date= September 2008 | issn=0013-7006 | doi=10.1016/j.encep.2007.05.005}}</ref><ref>{{cite journal | vauthors=((Paton, C.)) | journal=Psychiatric Bulletin | title=Benzodiazepines and disinhibition: a review | volume=26 | issue=12 | pages=460–462 | date= December 2002 | url=https://www.cambridge.org/core/journals/psychiatric-bulletin/article/benzodiazepines-and-disinhibition-a-review/421AF197362B55EDF004700452BF3BC6 | issn=0955-6036 | doi=10.1192/pb.26.12.460}}</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>{{cite journal | vauthors=((Bond, A. J.)) | journal=CNS Drugs | title=Drug- Induced Behavioural Disinhibition | volume=9 | issue=1 | pages=41–57 | date=1 January 1998 | url=https://doi.org/10.2165/00023210-199809010-00005 | issn=1179-1934 | doi=10.2165/00023210-199809010-00005}}</ref><ref>{{cite journal | vauthors=((Drummer, O. H.)) | journal=Forensic Science Review | title=Benzodiazepines - Effects on Human Performance and Behavior | volume=14 | issue=1–2 | pages=1–14 | date= February 2002 | issn=1042-7201}}</ref></p>
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==Toxicity and harm potential==
==Toxicity and harm potential==
[[Benzodiazepines]] and thienodiazepines are essentially identical in their pharmacological action, subjective effects, toxicity and harm potential. They can therefore be treated similarly in the appropriate efforts necessary to maximize harm reduction.
[[Benzodiazepines]] and thienodiazepines are essentially identical in their pharmacological action, subjective effects, toxicity and harm potential. They can therefore be treated similarly in the appropriate efforts necessary to maximize harm reduction.
[[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>{{cite journal | vauthors=((Nutt, D.)), ((King, L. A.)), ((Saulsbury, W.)), ((Blakemore, C.)) | journal=The Lancet | title=Development of a rational scale to assess the harm of drugs of potential misuse | volume=369 | issue=9566 | pages=1047–1053 | date=24 March 2007 | url=https://www.sciencedirect.com/science/article/pii/S0140673607604644 | issn=0140-6736 | doi=10.1016/S0140-6736(07)60464-4}}</ref>]]
===Lethal dosage===
===Lethal dosage===
The median lethal dosage varies widely between specific substances within the thienzodiazepine class. For this reason, one should always fully research the substance before administering it to themselves or others.
The median lethal dosage varies widely between specific substances within the thienzodiazepine class. For this reason, one should always fully research the substance before administering it to themselves or others.
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It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using these substances.
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using these substances.
===Tolerance and addiction potential===
===Tolerance and addiction potential===
Tolerance will develop to the sedative-hypnotic effects within a couple of days.<ref>Principles and Practice of Psychopharmacotherapy | http://books.google.com/books?id=_ePK9wwcQUMC&pg=PA535</ref> Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.<ref>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</ref> <ref>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</ref>
Tolerance will develop to the sedative-hypnotic effects within a couple of days.<ref>{{cite book | vauthors=((Janicak, P. G.)), ((Marder, S. R.)), ((Pavuluri, M. N.)) | date=25 October 2010 | title=Principles and Practice of Psychopharmacotherapy | publisher=Lippincott Williams & Wilkins | isbn=9781605475653}}</ref> Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.<ref>{{cite journal | vauthors=((Verster, J. C.)), ((Volkerts, E. R.)) | journal=CNS Drug Reviews | title=Clinical Pharmacology, Clinical Efficacy, and Behavioral Toxicity of Alprazolam: A Review of the Literature | volume=10 | issue=1 | pages=45–76 | date=7 June 2006 | url=https://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00003.x | issn=1080563X | doi=10.1111/j.1527-3458.2004.tb00003.x}}</ref> <ref>{{cite book | vauthors=((Galanter, M.)), ((Kleber, H. D.)) | date= 2008 | title=The American Psychiatric Publishing Textbook of Substance Abuse Treatment | publisher=American Psychiatric Pub. | isbn=9781585622764}}</ref>
====Discontinuation====
====Discontinuation====
Similar to benzodiazepines, thienodiazepine 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.<ref>A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812</ref> Drugs which lower the seizure threshold such as [[tramadol]] should be avoided during withdrawal. Abrupt discontinuation also causes rebound stimulation which presents as [[anxiety]], [[wakefulness|insomnia]] and restlessness.
Similar to benzodiazepines, thienodiazepine 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.<ref>{{cite journal | vauthors=((Lann, M. A.)), ((Molina, D. K.)) | journal=The American Journal of Forensic Medicine and Pathology | title=A fatal case of benzodiazepine withdrawal | volume=30 | issue=2 | pages=177–179 | date= June 2009 | issn=1533-404X | doi=10.1097/PAF.0b013e3181875aa0}}</ref> Drugs which lower the seizure threshold such as [[tramadol]] should be avoided during withdrawal. Abrupt discontinuation also causes rebound stimulation which presents as [[anxiety]], [[wakefulness|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 thienodiazepine, a longer acting drug can be substituted. Symptoms may still be present, but their severity will be reduced significantly. For more information on tapering from thienodiazepine in a controlled manner, please see [http://www.benzo.org.uk/manual/bzcha02.htm this guide]. Small amounts of [[alcohol]] can also help to reduce the symptoms.
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 thienodiazepine, a longer acting drug can be substituted. Symptoms may still be present, but their severity will be reduced significantly. For more information on tapering from thienodiazepine in a controlled manner, please see [http://www.benzo.org.uk/manual/bzcha02.htm this guide]. Small amounts of [[alcohol]] can also help to reduce the symptoms.
As such, it may contain incomplete or wrong information. You can help by expanding it.
The general structure of Thienodiazepines.
A thienodiazepine is a heterocyclic compound containing a diazepine ring fused to a thiophene ring. The thienodiazepine ring structure forms the central core of several pharmaceutical drugs. Since thienodiazepines interact with the benzodiazepine receptor site, they typically have similar effects as benzodiazepines and can be considered as essentially identical.
Similar to benzodiazepines, the sudden discontinuation of thienodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. 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.[2]
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 PsychonautWikicontributors. 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 ☠.
Motor control loss - Lack of coordination may result in falls and injuries, in particular, in the elderly. Another result of motor control loss is the impairment of driving skills and the increased likelihood of road traffic accidents.
Paradoxical reactions to thienodiazepines, as well as 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%).[3][4]
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[5][6]
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.
Volumetric liquid dosing - If one's thienodiazepines 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 thienodiazepine volumetrically into a solution so as to dose it accurately based upon the instructions described in this tutorial.
Toxicity and harm potential
Benzodiazepines and thienodiazepines are essentially identical in their pharmacological action, subjective effects, toxicity and harm potential. They can therefore be treated similarly in the appropriate efforts necessary to maximize harm reduction.
Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.[7]
Lethal dosage
The median lethal dosage varies widely between specific substances within the thienzodiazepine class. For this reason, one should always fully research the substance before administering it to themselves or others.
Tolerance will develop to the sedative-hypnotic effects within a couple of days.[8] Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.[9][10]
Discontinuation
Similar to benzodiazepines, thienodiazepine 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.[11] 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 thienodiazepine, a longer acting drug can be substituted. Symptoms may still be present, but their severity will be reduced significantly. For more information on tapering from thienodiazepine 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 depend 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 thienodiazepines. Thienodiazepines with longer half-lives will exhibit withdrawal symptoms with a slow onset and extended duration.
↑Drummer, O. H. (February 2002). "Benzodiazepines - Effects on Human Performance and Behavior". Forensic Science Review. 14 (1–2): 1–14. ISSN1042-7201.
↑Janicak, P. G., Marder, S. R., Pavuluri, M. N. (25 October 2010). Principles and Practice of Psychopharmacotherapy. Lippincott Williams & Wilkins. ISBN9781605475653.
↑Galanter, M., Kleber, H. D. (2008). The American Psychiatric Publishing Textbook of Substance Abuse Treatment. American Psychiatric Pub. ISBN9781585622764.
↑Lann, M. A., Molina, D. K. (June 2009). "A fatal case of benzodiazepine withdrawal". The American Journal of Forensic Medicine and Pathology. 30 (2): 177–179. doi:10.1097/PAF.0b013e3181875aa0. ISSN1533-404X.
