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Thienodiazepines: Difference between revisions
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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 | 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> | 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 | 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 | [[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 | | 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. | 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. | ||